[go: up one dir, main page]

AR049140A1 - N-(2-bencil)-2-fenilbutamidas como moduladores del receptor de androgeno - Google Patents

N-(2-bencil)-2-fenilbutamidas como moduladores del receptor de androgeno

Info

Publication number
AR049140A1
AR049140A1 ARP050102284A ARP050102284A AR049140A1 AR 049140 A1 AR049140 A1 AR 049140A1 AR P050102284 A ARP050102284 A AR P050102284A AR P050102284 A ARP050102284 A AR P050102284A AR 049140 A1 AR049140 A1 AR 049140A1
Authority
AR
Argentina
Prior art keywords
alkyl
aryl
heterocyclyl
carbonyl
heterocycloalkyl
Prior art date
Application number
ARP050102284A
Other languages
English (en)
Original Assignee
Merck & Co Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Merck & Co Inc filed Critical Merck & Co Inc
Publication of AR049140A1 publication Critical patent/AR049140A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/20—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof
    • C07D295/205—Radicals derived from carbonic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/26—Androgens
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/12—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by halogen atoms or by nitro or nitroso groups
    • C07C233/13—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by halogen atoms or by nitro or nitroso groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/32—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings
    • C07C235/34—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/58—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton
    • C07C255/60—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton at least one of the singly-bound nitrogen atoms being acylated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/12—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/22—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/61—Halogen atoms or nitro radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/73—Unsubstituted amino or imino radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/02—Systems containing only non-condensed rings with a three-membered ring

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurology (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Reproductive Health (AREA)
  • Obesity (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Transplantation (AREA)
  • Cardiology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Los compuestos de formula estructural (1) son moduladores del receptor de androgeno (RA) de un modo selectivo de tejido. Estos compuestos son utiles en la mejora del tono muscular debilitado y en el tratamiento de afecciones provocadas por deficiencia en androgeno o que se pueden aliviar por administracion de androgeno, incluyendo osteoporosis, osteopenia, osteoporosis inducida por glucocorticoides, enfermedad periodontal, fractura osea, dano oseo que sigue a cirugía reconstructiva del hueso, sarcopenia, fragilidad, piel envejecida, hipogonadismo masculino, síntomas posmenopáusicos en mujeres, ateroesclerosis, hipercolesterolemia, hiperlipidemia, obesidad, anemia aplásica y otros trastornos hematopoyéticos, artritis inflamatoria y reparacion de las articulaciones, consuncion por VIH, cáncer de prostata, hiperplasia prostática benigna (BPH), adiposidad abdominal, síndrome metabolico, diabetes de tipo II, caquexia cancerosa, enfermedad de Alzheimer, distrofias musculares, disminucion cognitiva, disfuncion sexual, apnea del sueno, depresion, insuficiencia ovárica prematura y enfermedad autoinmune, solo o junto con otros agentes activos. Reivindicacion 1: Un compuesto de formula estructural (1), o una de sus sales o estereoisomeros farmacéuticamente aceptables, en la que: X es -CH-, o -N-; n es 0, 1, 2, o 3; m es 0, 1, o 2; R1, R4 y R5 se eligen cada uno de forma independiente de H, halogeno, ciano, perfluoroalquilo C1-6, perfluoroalcoxi C1-6, alquilo C1-10, alquenilo C2-10, alquinilo C2-10, alquiltio C1-10, aril alquilo C0-10, cicloalquil C3-8alquilo C0-10, heterociclil C3-8alquilo C2-10, heterocicloalquil C3-8alquilo C2-10, (alquil C0-10)1-2amino alquilo C0-10, (aril alquil C0-10)1- 2amino alquilo C0-10, (cicloalquil C3-8 alquil C0-10)1-2amino alquilo C0-10, (heterociclil C3-8 alquil C0-10)1-2amino alquilo C0-10, (heterocicloalquil C3-8 alquil C0-10)1-2amino alquilo C0-10, (alquil C0-10)1-2aminocarbonilamino alquilo C0-10, (aril alquil C0-10)1-2aminocarbonilamino alquilo C0-10, heterociclil C3-8 alquil C0-10 aminocarbonilamino alquilo C0-10, heterocicloalquil C3-8 alquil C0-10 aminocarbonilamino alquilo C0-10, cicloalquil C3-8 alquil C0-10 aminocarbonilamino alquilo C0-10, (alquil C0-10)1-2aminocarbonil alquilo C0-10, (aril alquil C0-10)1-2aminocarbonil alquilo C0-10, cicloalquil C3-8 alquil C0-10aminocarbonil alquilo C0-10, heterociclil C3-8 alquil C0-10aminocarbonil alquilo C0-10, heterocicloalquil C3-8alquil C0-10aminocarbonil alquilo C0-10, alquil C0-10 carbonilamino alquilo C0-10, cicloalquil C3-8 alquil C0-10carbonilamino alquilo C0-10, heterociclil C3-8alquil C0-10carbonilamino alquilo C0-10, heterocicloalquil C3-8alquil C0-10 carbonilamino alquilo C0-10, aril alquil C0-10 carbonilamino alquilo C0-10, alquiloxi C0-10 carbonilamino alquilo C0-10, cicloalquil C3-8alquiloxi C0-10 carbonilamino alquilo C0-10, heterociclil C3-8alquiloxi C0-10 carbonilamino alquilo C0-10, heterocicloalquil C3- 8alquiloxi C0-10 carbonilamino alquilo C0-10, aril alquiloxi C0-10 carbonilamino alquilo C0-10, alquiloxi C0-10carboniloxi alquilo C0-10, cicloalquil C3-8alquiloxi C0-10carboniloxi alquilo C0-10, heterociclil C3-8alquiloxi C0-10 carboniloxi alquilo C0-10, heterocicloalquil C3-8alquiloxi C0-10 carboniloxi alquilo C0-10, aril alquiloxi C0-10 carboniloxi alquilo C0-10, alcoxi C1-10(carbonil)0-1alquilo C0-10, alquil C0-10 carboxi alquilamino C0-10, hidroxicarbonil alquilo C0-10, hidroxicarbonil alquenilo C2-10, hidroxicarbonil alquinilo C2-10, alcoxi C1-10, alquiloxi C1-10alquilo C0-10, ariloxi alquilo C0-10, cicloalquiloxi C3-8alquilo C0-10, heterociclil C3-8alquiloxi C2-10alquilo C0-10, heterocicloalquil C3-8alquiloxi C2-10alquilo C0-10, alquilcarboniloxi C1-10alquilo C0-10, (alquil C1-10)1-2aminosulfonil alquilo C0-10, (aril alquil C1-10)1-2aminosulfonil alquilo C0-10, cicloalquil C3-8alquil C1-10 aminosulfonil alquilo C0-10, heterociclil C3-8alquil C1-10 aminosulfonil alquilo C0- 10, heterocicloalquil C3-8alquil C1-10 aminosulfonil alquilo C0-10, alquil C0-10 sulfonilamino alquilo C0-10, cicloalquil C3-8alquil C0-10 sulfonilamino alquilo C0-10, heterociclil C3-8 alquil C0-10 sulfonilamino alquilo C0-10, heterocicloalquil C3- 8 alquil C0-10 sulfonilamino alquilo C0-10, aril alquil C0-10 sulfonilamino alquilo C0-10, alquiloxi C1-10(carbonil)0-1 alquil C0-10amino, heterociclil C3-8 alquiloxi C0-10(carbonil)0-1alquilamino C0-10, heterocicloalquil C3-8alquiloxi C0- 10(carbonil)0-1alquilamino C0-10, cicloalquil C3-8alquiloxi C0-10(carbonil)0-1alquilamino C0-10, aril alquiloxi C0-10(carbonil)0-1alquilamino C0-10, (alquil C0-10)1-2aminocarboniloxi, (aril alquil C0-10)1-2aminocarboniloxi, (heterociclil C3-8alquil C0-10)1-2aminocarboniloxi, (heterocicloalquil C3-8 alquil C0-10)1-2aminocarboniloxi, (cicloalquil C3-8 alquil C0-10)1-2aminocarboniloxi, hidroxialquilo C0-10, y con la condicion de que cuando X es -N- entonces R5 es diferente de un resto elegido de (alquil C0-10)1-2amino, alquiloxi C0-10 carbonilamino, cicloalquil C3-8 alquiloxi C0-10 carbonilamino, aril alquiloxi C0-10carbonilamino, alquiloxi C1-10(carbonil)0-1alquilamino C0-10, alquiloxi C0-10(carbonil)0-1alquilamino C0-10, cicloalquil C3- 8alquiloxi C0-10(carbonil)0-1alquilamino C0-10 y aril alquiloxi C0-10(carbonil)0-1alquilamino C0-10; R2 y R3 se eligen cada uno de forma independiente de H, halogeno, ciano, amino, hidroxialquilo C0-10, perfluoroalquilo C1-6, perfluoroalcoxi C1-6, alquilo C1-10, alquenilo C2-10, alquinilo C2-10, aril alquilo C0-10, cicloalquil C3-8alquilo C0-10, heterociclil C3-8alquilo C2-10, heterocicloalquil C3-8alquilo C2-10, (alquil C0-10)1-2amino alquilo C0-10, (aril alquil C0-10)1-2amino alquilo C0-10, (cicloalquil C3-8 alquil C0-10)1-2amino alquilo C0-10, (heterociclil C3-8 alquil C0-10)1-2amino alquilo C0-10, (heterocicloalquil C3-8 alquil C0-10)1-2amino alquilo C0-10, (alquil C0-10)1-2aminocarboniloxi alquilo C0-10, (aril alquil C0-10)1- 2aminocarboniloxi alquilo C0-10, (cicloalquil C3-8 alquil C0-10)1-2aminocarboniloxi alquilo C0-10, (heterociclil C3-8 alquil C0-10)1-2 aminocarboniloxi alquilo C0-10, (heterocicloalquil C3-8 alquil C0-10)1-2 aminocarboniloxi alquilo C0-10, (alquil C0-10)1-2aminocarbonilamino alquilo C0-10, (aril alquil C0-10)1-2aminocarbonilamino alquilo C0-10, (cicloalquil C3-8 alquil C0-10)1-2aminocarboniloxi alquilo C0-10, (heterociclil C3-8 alquil C0-10)1-2aminocarboniloxi alquilo C0-10, (heterocicloalquil C3-8alquil C0-10)1-2aminocarboniloxi alquilo C0-10, (alquil C0-10)1-2 aminocarbonilamino alquilo C0-10, (aril alquil C0-10)1-2aminocarbonilamino alquilo C0-10, (cicloalquil C3-8 alquil C0-10)1-2aminocarbonilamino alquilo C0-10, (heterociclil C3-8alquil C0-10)1-2aminocarbonilamino alquilo C0-10, (heterocicloalquil C3-8alquil C0-10)1-2aminocarbonilamino alquilo C0-10, 8alquil C0-10)1-2aminocarbonil alquilo C0-10, (aril alquil C0-10)1-2 aminocarbonil alquilo C0-10, cicloalquil C3-8alquiloxi C0-10 aminocarbonil alquilo C0-10, heterociclil C3-8alquiloxi C0-10 aminocarbonil alquilo C0-10, heterocicloalquil C3-8alquiloxi C0-10 aminocarbonil alquilo C0-10, alquil C0-10carbonilamino alquilo C0-10, cicloalquil C3- 8alquil C0-10carbonilamino alquilo C0-10, heterociclil C3-8alquil C0-10 carbonilamino alquilo C0-10, heterocicloalquil C3-8alquil C0-10 carbonilamino alquilo C0-10, aril alquil C0-10carbonilamino alquilo C0-10, alquiloxi C0-10 carbonilamino alquilo C0-10, cicloalquil C3-8alquiloxi C-10 carbonilamino alquilo C0-10, heterociclil C3-8alquiloxi C0-10carbonilamino alquilo C0-10, heterocicloalquil C3-8alquiloxi C0-10carbonilamino alquilo C0-10, aril alquiloxi C0-10carbonilamino alquilo C0-10, alquiloxi C0-10carboniloxi alquilo C0-10, cicloalquil C3-8alquiloxi C0-10carboniloxi alquilo C0-10, heterociclil C3-8 alquiloxi C0-10 carboniloxi alquilo C0-10, heterocicloalquil C3-8 alquiloxi C0-10 carboniloxi alquilo C0-10, aril alquiloxi C0-10 carboniloxi alquilo C0-10, alcoxi C1-10(carbonil)0-1 alquil C0-10, alquilcarboxi C1-10alquilamino C0-10, alquiloxi C1-10alquilo C0-10, ariloxi alquilo C0-10, cicloalquiloxi C3-8alquilo C0-10, heterocicliloxi C3-8alquil C0-10, heterociclil C3-8 alquiloxi C0-10alquilo C0-10, alquilcarboniloxi C1-10alquilo C0-10, alquiloxi C1-10(carbonil)0-1alquilamino C0-10, heterociclil C3-8alquiloxi C0-10(carbonil)0-1alquilamino C0-10,heterocicloalquil C3-8alquiloxi C0-10(carbonil)0-1alquilamino C0-10, cicloalquil C3-8alquiloxi C0-10(carbonil)0-1alquilamino C0-10,aril alquiloxi C0-10(carbonil)0-1alquilamino C0-10, en los que en R1, R2, R3, R4 y R5, dicho alquilo, alquenilo, alquinilo, arilo, heterociclilo, heterocicloalquilo y cicloalquilo se sustituyen opcionalmente cada uno con uno o más grupos elegidos de hidroxi, alquilo C1-6, alcoxi C1-6, halogeno, CO2H, ciano, O(C=O)alquilo C1-6, NO2, trifluorometoxi, trifluoroetoxi, -O(0-1)perfluoroalquilo C1-10, alquilaminocarbonilamino C1-10, alquiloxicarbonilamino C1-10, alquilcarbonilamino C1-10, alquilaminosulfonilamino C1-10, alquilsulfonilamino C1-10, alquilsulfonilo C1-10, alquilaminosulfonilo C1-10, alquilaminocarbonilo C1-10 y NH2.
ARP050102284A 2004-06-07 2005-06-03 N-(2-bencil)-2-fenilbutamidas como moduladores del receptor de androgeno AR049140A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US57769804P 2004-06-07 2004-06-07

Publications (1)

Publication Number Publication Date
AR049140A1 true AR049140A1 (es) 2006-06-28

Family

ID=35415107

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP050102284A AR049140A1 (es) 2004-06-07 2005-06-03 N-(2-bencil)-2-fenilbutamidas como moduladores del receptor de androgeno

Country Status (24)

Country Link
US (3) US7268153B2 (es)
EP (1) EP1755572B1 (es)
JP (1) JP4881865B2 (es)
CN (1) CN1976902A (es)
AR (1) AR049140A1 (es)
AT (1) ATE545631T1 (es)
AU (1) AU2005251766B9 (es)
BR (1) BRPI0511862A (es)
CA (1) CA2569124C (es)
CR (1) CR8777A (es)
EC (1) ECSP067061A (es)
IL (1) IL179843A0 (es)
MA (1) MA28677B1 (es)
MX (1) MXPA06014235A (es)
MY (1) MY147997A (es)
NO (1) NO20070085L (es)
NZ (1) NZ551738A (es)
PE (1) PE20060401A1 (es)
RU (1) RU2378255C2 (es)
SG (1) SG169398A1 (es)
TW (1) TW200610755A (es)
UA (1) UA87854C2 (es)
WO (1) WO2005120477A2 (es)
ZA (1) ZA200609673B (es)

Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA87854C2 (en) * 2004-06-07 2009-08-25 Мерк Энд Ко., Инк. N-(2-benzyl)-2-phenylbutanamides as androgen receptor modulators
AU2005310238A1 (en) * 2004-10-29 2006-06-08 Merck Sharp & Dohme Corp. N-(pyridin-3-yl)-2-phenylbutanamides as androgen receptor modulators
WO2007016358A1 (en) * 2005-08-02 2007-02-08 Merck & Co., Inc. N-(pyridin-4-yl)-2-phenylbutanamides as androgen receptor modulators
JP2009522246A (ja) * 2005-12-30 2009-06-11 ランバクシー ラボラトリーズ リミテッド ムスカリン性レセプターアンタゴニスト
AU2007313295A1 (en) * 2006-10-18 2008-04-24 Merck Sharp & Dohme Corp. 2-hydroxy-2-phenyl/thiophenyl propionamides as androgen receptor modulators
EP2489656A1 (en) 2007-12-21 2012-08-22 Ligand Pharmaceuticals Inc. Selective androgen receptor modulators (sarms) and uses thereof
US20090197947A1 (en) * 2008-02-01 2009-08-06 The Research Foundation Of State University Of New York Medicaments and methods for lowering plasma lipid levels and screening drugs
US8623909B2 (en) * 2008-05-09 2014-01-07 Aska Pharmaceutical Co., Ltd. Prophylactic/therapeutic agents for lifestyle-related diseases
ES2627692T3 (es) 2010-06-10 2017-07-31 Aragon Pharmaceuticals, Inc. Moduladores de receptores de estrógenos y usos de los mismos
US9763678B2 (en) 2010-06-24 2017-09-19 DePuy Synthes Products, Inc. Multi-segment lateral cage adapted to flex substantially in the coronal plane
FR2982261B1 (fr) * 2011-11-04 2014-06-13 Galderma Res & Dev Nouveaux amides, et leur utilisation pharmaceutique ou cosmetique
EA029559B1 (ru) 2011-12-14 2018-04-30 Серагон Фармасьютикалс, Инк. Фторированные модуляторы рецепторов эстрогенов и их применение
CN103288669B (zh) * 2013-07-01 2015-06-24 南开大学 一种阿卓乳酸酰胺衍生物及应用
US9868705B2 (en) 2013-09-27 2018-01-16 The Board Of Trustees Of The University Of Illinois Tetra-aryl cyclobutane inhibitors of androgen receptor action for the treatment of hormone refractory cancer
EP3094323A4 (en) 2014-01-17 2017-10-11 Ligand Pharmaceuticals Incorporated Methods and compositions for modulating hormone levels
US10806720B2 (en) 2015-04-21 2020-10-20 University Of Tennessee Research Foundation Selective androgen receptor degrader (SARD) ligands and methods of use thereof
US10093613B2 (en) 2015-04-21 2018-10-09 Gtx, Inc. Selective androgen receptor degrader (SARD) ligands and methods of use thereof
US10865184B2 (en) 2015-04-21 2020-12-15 University Of Tennessee Research Foundation Selective androgen receptor degrader (SARD) ligands and methods of use thereof
WO2016172330A1 (en) * 2015-04-21 2016-10-27 Gtx, Inc. Selective androgen receptor degrader (sard) ligands and methods of use thereof
US10441570B2 (en) 2015-04-21 2019-10-15 University Of Tennessee Research Foundation Selective androgen receptor degrader (SARD) Ligands and methods of use thereof
US10654809B2 (en) 2016-06-10 2020-05-19 University Of Tennessee Research Foundation Selective androgen receptor degrader (SARD) ligands and methods of use thereof
US11230523B2 (en) 2016-06-10 2022-01-25 University Of Tennessee Research Foundation Selective androgen receptor degrader (SARD) ligands and methods of use thereof
EP3692144A1 (en) 2017-10-05 2020-08-12 Fulcrum Therapeutics, Inc. Use of p38 inhibitors to reduce expression of dux4
US10342786B2 (en) 2017-10-05 2019-07-09 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD
CN112566666A (zh) 2018-05-14 2021-03-26 努瓦申生物公司 靶向抗癌核激素受体的化合物
WO2020048826A1 (en) 2018-09-03 2020-03-12 Bayer Aktiengesellschaft 5-substituted 1-oxa-3,9-diazaspiro[5.5]undecan-2-one compounds
US12202815B2 (en) 2018-09-05 2025-01-21 University Of Tennessee Research Foundation Selective androgen receptor degrader (SARD) ligands and methods of use thereof
CA3133929A1 (en) 2019-04-19 2020-10-22 Lin Zhi Crystalline forms and methods of producing crystalline forms of a compound
AU2020274113A1 (en) 2019-05-14 2021-11-11 Nuvation Bio Inc. Anti-cancer nuclear hormone receptor-targeting compounds
US20210024636A1 (en) * 2019-07-26 2021-01-28 Chemistryrx Compositions and methods for treating sexual dysfunction
WO2021097046A1 (en) 2019-11-13 2021-05-20 Nuvation Bio Inc. Anti-cancer nuclear hormone receptor-targeting compounds
JP2024510792A (ja) 2021-03-23 2024-03-11 ニューベイション・バイオ・インコーポレイテッド 抗がん核内ホルモン受容体標的化化合物
JP2024516024A (ja) 2021-05-03 2024-04-11 ニューベイション・バイオ・インコーポレイテッド 抗がん核内ホルモン受容体標的化化合物
CN113816900B (zh) * 2021-10-18 2024-06-25 宁夏瑞泰科技股份有限公司 一种2-氯-5-甲基吡啶-3-甲醛的合成方法

Family Cites Families (139)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2809965A (en) * 1956-04-30 1957-10-15 Dow Chemical Co Phthalides
CA777769A (en) 1963-03-18 1968-02-06 H. Roy Clarence Substituted methylene diphosphonic acid compounds and detergent compositions
US3239345A (en) 1965-02-15 1966-03-08 Estrogenic compounds and animal growth promoters
US4411890A (en) 1981-04-14 1983-10-25 Beckman Instruments, Inc. Synthetic peptides having pituitary growth hormone releasing activity
US4036979A (en) 1974-01-25 1977-07-19 American Cyanamid Company Compositions containing 4,5,6,7-tetrahydrobenz[b]thien-4-yl-ureas or derivatives and methods of enhancing growth rate
US4342767A (en) 1980-01-23 1982-08-03 Merck & Co., Inc. Hypocholesteremic fermentation products
US4444784A (en) 1980-08-05 1984-04-24 Merck & Co., Inc. Antihypercholesterolemic compounds
MX7065E (es) 1980-06-06 1987-04-10 Sankyo Co Un procedimiento microbiologico para preparar derivados de ml-236b
FR2531088B1 (fr) 1982-07-29 1987-08-28 Sanofi Sa Produits anti-inflammatoires derives de l'acide methylenediphosphonique et leur procede de preparation
US5354772A (en) 1982-11-22 1994-10-11 Sandoz Pharm. Corp. Indole analogs of mevalonolactone and derivatives thereof
GB8332704D0 (en) 1983-12-07 1984-01-11 Pfizer Ltd Growth promotants for animals
US4761406A (en) 1985-06-06 1988-08-02 The Procter & Gamble Company Regimen for treating osteoporosis
DE3623397A1 (de) 1986-07-11 1988-01-14 Boehringer Mannheim Gmbh Neue diphosphonsaeurederivate, verfahren zu deren herstellung und diese verbindungen enthaltende arzneimittel
GB8726179D0 (en) * 1987-11-09 1987-12-16 Fujisawa Pharmaceutical Co Heterocyclic derivatives
CA1339805C (en) 1988-01-20 1998-04-07 Yasuo Isomura (cycloalkylamino)methylenebis(phosphonic acid) and medicines containing the same as an active
US4922007A (en) 1989-06-09 1990-05-01 Merck & Co., Inc. Process for preparing 4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid or salts thereof
FI94339C (fi) 1989-07-21 1995-08-25 Warner Lambert Co Menetelmä farmaseuttisesti käyttökelpoisen /R-(R*,R*)/-2-(4-fluorifenyyli)- , -dihydroksi-5-(1-metyylietyyli)-3-fenyyli-4-/(fenyyliamino)karbonyyli/-1H-pyrroli-1-heptaanihapon ja sen farmaseuttisesti hyväksyttävien suolojen valmistamiseksi
US5019651A (en) 1990-06-20 1991-05-28 Merck & Co., Inc. Process for preparing 4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid (ABP) or salts thereof
US5177080A (en) 1990-12-14 1993-01-05 Bayer Aktiengesellschaft Substituted pyridyl-dihydroxy-heptenoic acid and its salts
US5206235A (en) 1991-03-20 1993-04-27 Merck & Co., Inc. Benzo-fused lactams that promote the release of growth hormone
JP2648897B2 (ja) 1991-07-01 1997-09-03 塩野義製薬株式会社 ピリミジン誘導体
US5283241A (en) 1992-08-28 1994-02-01 Merck & Co., Inc. Benzo-fused lactams promote release of growth hormone
US5583130A (en) 1992-09-25 1996-12-10 Merck & Co., Inc. Benzo-fused lactams promote release of growth hormone
US5317017A (en) 1992-09-30 1994-05-31 Merck & Co., Inc. N-biphenyl-3-amido substituted benzolactams stimulate growth hormone release
US5374721A (en) 1992-10-14 1994-12-20 Merck & Co., Inc. Benzo-fused lactams promote release of growth hormone
EP0669830A4 (en) 1992-11-06 1997-02-26 Merck & Co Inc SUBSTITUTED DIPEPTIDE ANALOGS, WHICH SUPPORT THE RELEASE OF GROWTH HORMONE.
US5578593A (en) 1992-12-11 1996-11-26 Merck & Co., Inc. Spiro piperidines and homologs promote release of growth hormone
HUT72076A (en) 1992-12-11 1996-03-28 Merck & Co Inc Process for preparing spiro piperidines and homologs which promote release of growth hormone and pharmaceutical compositions containing them
US5284841A (en) 1993-02-04 1994-02-08 Merck & Co., Inc. Benzo-fused lactams promote release of growth hormone
US5434261A (en) 1993-07-26 1995-07-18 Merck & Co., Inc. Benzo-fused lactams promote release of growth hormone
US5430144A (en) 1993-07-26 1995-07-04 Merck & Co., Inc. Benzo-fused lactams promote release of growth hormone
US5952281A (en) 1993-08-04 1999-09-14 Colgate Palmolive Company Aqueous cleaning composition which may be in microemulsion form containing a silicone antifoam agent
US5510517A (en) 1993-08-25 1996-04-23 Merck & Co., Inc. Process for producing N-amino-1-hydroxy-alkylidene-1,1-bisphosphonic acids
TW257765B (es) 1993-08-25 1995-09-21 Merck & Co Inc
US5631365A (en) 1993-09-21 1997-05-20 Schering Corporation Hydroxy-substituted azetidinone compounds useful as hypocholesterolemic agents
DE4332384A1 (de) 1993-09-23 1995-03-30 Merck Patent Gmbh Adhäsionsrezeptor-Antagonisten III
US5545735A (en) 1993-10-04 1996-08-13 Merck & Co., Inc. Benzo-Fused Lactams promote release of growth hormone
AU8083694A (en) 1993-10-19 1995-05-08 Merck & Co., Inc. Combination of bisphosphonates and growth hormone secretagogues
US5438136A (en) 1993-11-02 1995-08-01 Merck & Co., Inc. Benzo-fused macrocycles promote release of growth hormone
US5492916A (en) 1993-12-23 1996-02-20 Merck & Co., Inc. Di- and tri-substituted piperidines, pyrrolidines and hexahydro-1H-azepines promote release of growth hormone
US5494919A (en) 1993-11-09 1996-02-27 Merck & Co., Inc. 2-substituted piperidines, pyrrolidines and hexahydro-1H-azepines promote release of growth hormone
EP0739204A4 (en) 1993-11-09 2000-03-15 Merck & Co Inc PIPERIDINE, PYRROLIDINE AND HEXAHYDRO-1H-AZEPINE SUPPORT THE RELEASE OF THE GROWTH HORMONE
WO1995014666A1 (en) 1993-11-24 1995-06-01 Merck & Co., Inc. Indolyl group containing compounds and the use thereof to promote the release of growth hormone(s)
WO1995016675A1 (en) 1993-12-13 1995-06-22 Merck & Co., Inc. Benzo-fused lactams promote release of growth hormone
US5606054A (en) 1993-12-14 1997-02-25 Merck & Co., Inc. Heterocyclic-fused lactams promote release of growth hormone
UA45962C2 (uk) 1993-12-23 2002-05-15 Ново Нордіск А/С Похідні пептидів, фармацевтична композиція,спосіб стимулювання секреції гормону росту з гіпофізу
ES2153469T3 (es) 1993-12-23 2001-03-01 Novo Nordisk As Compuestos con propiedades para liberar la hormona del crecimiento.
US5501969A (en) 1994-03-08 1996-03-26 Human Genome Sciences, Inc. Human osteoclast-derived cathepsin
JPH10501222A (ja) 1994-05-27 1998-02-03 メルク エンド カンパニー インコーポレーテッド 破骨細胞仲介骨吸収を抑制するための化合物
AU2695795A (en) 1994-06-13 1996-01-05 Merck & Co., Inc. Piperazine compounds promote release of growth hormone
JPH10504807A (ja) 1994-06-29 1998-05-12 スミスクライン・ビーチャム・コーポレイション ビトロネクチン受容体拮抗剤
PL318199A1 (en) 1994-06-29 1997-05-26 Smithkline Beecham Corp Antagonists of vitronectin receptors
US5783582A (en) 1994-07-20 1998-07-21 Merck & Co., Inc. Piperidines and hexahydro-1H-azepines spiro substituted at the 4-position promote release of growth hormone
JPH10504825A (ja) 1994-08-22 1998-05-12 スミスクライン・ビーチャム・コーポレイション 二環式化合物
US5494920A (en) 1994-08-22 1996-02-27 Eli Lilly And Company Methods of inhibiting viral replication
US6544767B1 (en) 1994-10-27 2003-04-08 Axys Pharmaceuticals, Inc. Cathespin O2 protease
US5736357A (en) 1994-10-27 1998-04-07 Arris Pharmaceutical Cathespin O protease
DE19504379A1 (de) * 1995-02-10 1996-08-14 Hoechst Ag Substituierte Benzolsulfonylharnstoffe und -thioharnstoffe, Verfahren zu ihrer Herstellung und ihre Verwendung zur Herstellung pharmazeutischer Präparate sowie sie enthaltende pharmazeutische Präparate
WO1996026190A1 (en) 1995-02-22 1996-08-29 Smithkline Beecham Corporation Integrin receptor antagonists
US5710159A (en) 1996-05-09 1998-01-20 The Dupont Merck Pharmaceutical Company Integrin receptor antagonists
SI0910563T1 (en) 1995-06-29 2003-10-31 Smithkline Beecham Corporation Integrin receptor antagonists
US6008213A (en) 1995-06-29 1999-12-28 Smithkline Beecham Corporation Integrin receptor antagonists
AU702487B2 (en) 1995-08-30 1999-02-25 G.D. Searle & Co. Meta-guanidine, urea, thiourea or azacyclic amino benzoic acid derivatives as integrin antagonists
US6204293B1 (en) * 1995-11-06 2001-03-20 University Of Pittsburgh Inhibitors of protein isoprenyl transferases
AU725622B2 (en) 1995-12-22 2000-10-19 Kowa Company, Ltd. Pharmaceutical composition stabilized with a basic agent
US5760028A (en) 1995-12-22 1998-06-02 The Dupont Merck Pharmaceutical Company Integrin receptor antagonists
JP2000502708A (ja) 1995-12-29 2000-03-07 スミスクライン・ビーチャム・コーポレイション ビトロネクチン受容体拮抗物質
JP2000502704A (ja) 1995-12-29 2000-03-07 スミスクライン・ビーチャム・コーポレイション ビトロネクチン受容体拮抗物質
CA2241633A1 (en) 1995-12-29 1997-07-10 William Henry Miller Vitronectin receptor antagonists
ES2171768T3 (es) 1996-03-20 2002-09-16 Hoechst Ag Inhibidores de la resorcion osea y antagonistas de receptores de vitronectina.
AP806A (en) 1996-03-20 2000-01-28 Aventis Pharma Sa Tricyclic compounds having activity specific for integrins, particularly avB3 integrins, method for preparing same, intermediates therefor, use of said compounds as drugs, and pharmaceutical compositions containing same.
JP2000507575A (ja) 1996-03-29 2000-06-20 ジー．ディー．サール アンド カンパニー シクロプロピルアルカノイック酸誘導体
JP2000510098A (ja) 1996-03-29 2000-08-08 ジー．ディー．サール アンド カンパニー 桂皮酸誘導体
EP0889876B1 (en) 1996-03-29 2001-07-25 G.D. SEARLE & CO. Meta-substituted phenylene sulphonamide derivatives
ES2162676T3 (es) 1996-03-29 2002-01-01 Searle & Co Derivados de fenileno sustituidos en meta y su uso como antagonistas o inhibidores de integrina alfav,beta3.
US5925655A (en) 1996-04-10 1999-07-20 Merck & Co., Inc. αv β3 antagonists
KR20000022190A (ko) 1996-06-28 2000-04-25 플레믹 크리스티안 인테그린 저해제로서의 페닐알라닌 유도체
DE19629816A1 (de) 1996-07-24 1998-01-29 Hoechst Ag Neue Cycloalkyl-Derivate als Inhibitoren der Knochenresorption und Vitronectinrezeptor-Antagonisten
DE19629817A1 (de) 1996-07-24 1998-01-29 Hoechst Ag Neue Imino-Derivate als Inhibitoren der Knochenresorption und Vitronectinrezeptor-Antagonisten
US5981546A (en) 1996-08-29 1999-11-09 Merck & Co., Inc. Integrin antagonists
UA60311C2 (uk) 1996-10-02 2003-10-15 Смітклайн Бічам Корпорейшн Антагоністи рецептора вітронектину, спосіб одержання цих сполук та фармацевтична композиція
JP2001501951A (ja) 1996-10-07 2001-02-13 スミスクライン・ビーチャム・コーポレイション 骨形成刺激方法
US5919792A (en) 1996-10-30 1999-07-06 Merck & Co., Inc. Integrin antagonists
US6130231A (en) 1996-11-27 2000-10-10 Dupont Pharmaceuticals Integrin receptor antagonists
DE19653646A1 (de) 1996-12-20 1998-06-25 Hoechst Ag Substituierte Purinderivate, Verfahren zu deren Herstellung, sie enthaltende Mittel und deren Verwendung
CO4920232A1 (es) 1997-01-08 2000-05-29 Smithkline Beecham Corp Acidos aceticos dibenzo [a,d] cicloheptano con actividad antagonista del receptor de vitronectin
DE19705450A1 (de) 1997-02-13 1998-08-20 Merck Patent Gmbh Bicyclische aromatische Aminosäuren
JP2002510328A (ja) 1997-07-25 2002-04-02 スミスクライン・ビーチャム・コーポレイション ビトロネクチン受容体アンタゴニスト
CA2298544A1 (en) 1997-08-04 1999-02-11 Smithkline Beecham Corporation Integrin receptor antagonists
EP1027337A4 (en) 1997-09-04 2002-04-03 Smithkline Beecham Corp Integrin receptor Antagonist
DZ2609A1 (fr) 1997-09-19 2003-03-01 Smithkline Beecham Corp Composés nouveaux antagonistes des récepteurs de vitronectine et compositions pharmaceutiques les contenant.
CA2304000A1 (en) 1997-09-24 1999-04-01 William E. Bondinell Vitronectin receptor antagonist
KR20010024247A (ko) 1997-09-24 2001-03-26 스튜어트 알. 수터 비트로넥틴 수용체 길항제
FR2768736B1 (fr) 1997-09-24 2000-05-26 Roussel Uclaf Nouveaux composes tricycliques, leur procede de preparation et les intermediaires de ce procede, leur application a titre de medicaments et les compositions pharmaceutiques les renfermant
JP2001524481A (ja) 1997-11-26 2001-12-04 デュポン ファーマシューティカルズ カンパニー αＶβ３アンタゴニストとしての１，３，４−チアジアゾール類および１，３，４−オキサジアゾール類
US6066648A (en) 1997-12-17 2000-05-23 Merck & Co., Inc. Integrin receptor antagonists
US6017926A (en) 1997-12-17 2000-01-25 Merck & Co., Inc. Integrin receptor antagonists
AU738452B2 (en) 1997-12-17 2001-09-20 Merck & Co., Inc. Integrin receptor antagonists
JP3589633B2 (ja) 1997-12-17 2004-11-17 メルク エンド カムパニー インコーポレーテッド インテグリン受容体拮抗薬
JP2002508323A (ja) 1997-12-17 2002-03-19 メルク エンド カムパニー インコーポレーテッド インテグリン受容体拮抗薬
EP0933367A1 (en) 1997-12-19 1999-08-04 Hoechst Marion Roussel Deutschland GmbH Novel acylguanidine derivates as inhibitors of bone resorption and as vitronectin receptor antagonists
AU1687699A (en) 1997-12-25 1999-07-19 Yamanouchi Pharmaceutical Co., Ltd. Nitrogenous heterocyclic derivatives
SI0928790T1 (en) 1998-01-02 2003-06-30 F. Hoffmann-La Roche Ag Thiazole derivatives
EP0928793B1 (en) 1998-01-02 2002-05-15 F. Hoffmann-La Roche Ag Thiazole derivatives
HUP0100520A3 (en) 1998-01-23 2002-11-28 Genentech Inc Novel sulfonamide derivatives as inhibitors of bone resorption and as inhibitors of cell adhesion
ZA994406B (en) 1998-03-04 2000-02-11 Searle & Co Meta-azacyclic amino benzoic acid and derivatives thereof.
AR015241A1 (es) 1998-03-10 2001-04-18 Smithkline Beecham Corp Antagonistas del receptor de vitronectina composicion farmaceutica que los contiene, procedimiento para su preparacion y su empleo para la fabricacion deun medicamento.
US6420558B1 (en) 1998-04-09 2002-07-16 Meiji Seika Kaisha, Ltd. Aminopiperidine derivates as integrin αvβ3 antagonists
JP2002511462A (ja) 1998-04-10 2002-04-16 ジー・ディー・サール・アンド・カンパニー ビトロネクチンアンタゴニストとしてのヘテロ環式グリシルβ−アラニン誘導体
WO1999052879A1 (en) 1998-04-14 1999-10-21 American Home Products Corporation Acylresorcinol derivatives as selective vitronectin receptor inhibitors
EP0960882A1 (en) 1998-05-19 1999-12-01 Hoechst Marion Roussel Deutschland GmbH Thienyl substituted acylguanidines as inhibitors of bone resorption and vitronectin receptor antagonists
EP1091952B1 (en) 1998-06-29 2003-10-29 Biochem Pharma Inc Thiophene and furan 2,5-dicarboxamides useful in the treatment of cancer
AR019190A1 (es) * 1998-07-08 2001-12-26 Sod Conseils Rech Applic Derivados de 2-aminopiridinas, productos intermedios para su preparacion, medicamentos y composiciones farmaceuticas que los contienen y su uso para preparar medicamentos
WO2000006169A1 (en) 1998-07-29 2000-02-10 Merck & Co., Inc. Integrin receptor antagonists
WO2000009503A1 (en) 1998-08-13 2000-02-24 Merck & Co., Inc. Integrin receptor antagonists
GB9828442D0 (en) * 1998-12-24 1999-02-17 Karobio Ab Novel thyroid receptor ligands and method II
WO2001011965A1 (en) * 1999-08-18 2001-02-22 Aventis Cropscience Gmbh Fungicides
AU6865100A (en) 1999-09-02 2001-04-10 Mitsubishi Pharma Corporation Osteogenesis promoting agents
JP2003525874A (ja) 2000-01-06 2003-09-02 メルク フロスト カナダ アンド カンパニー プロテアーゼ阻害剤としての新規化合物および組成物
AU2001256981A1 (en) 2000-04-06 2001-10-23 Axys Pharmaceuticals, Inc. Cathepsin cysteine protease inhibitors
PT1302461E (pt) * 2000-05-31 2007-12-13 Santen Pharmaceutical Co Ltd Inibidores de produção de tnf-alpha
EP1193248A1 (en) 2000-09-30 2002-04-03 Aventis Pharma Deutschland GmbH Malonamid and malonamic ester derivatives with antithrombotic activity, their preparation and their use
US7214690B2 (en) * 2001-02-23 2007-05-08 Ligand Pharmaceuticals Incorporated Tricyclic quinolinone and tricyclic quinoline androgen receptor modulator compounds and methods
US20050009812A1 (en) * 2001-10-05 2005-01-13 Takuya Seko Remedies for stress diseases comprising mitochondrial benzodiazepine receptor antagonists
KR20100112659A (ko) * 2002-02-07 2010-10-19 지티엑스, 인코포레이티드 선택적 안드로겐 수용체 조절자를 이용한 양성 전립선 과형성증의 치료 방법
WO2003074473A2 (en) 2002-02-28 2003-09-12 University Of Tennessee Research Foundation Irreversible selective androgen receptor modulators and methods of use thereof
CA2484173A1 (en) * 2002-04-30 2003-11-13 Merck & Co., Inc. 4-azasteroid derivatives as androgen receptor modulators
EP1562906A4 (en) * 2002-10-15 2009-12-02 Univ Tennessee Res Foundation HETEROCYCLIC SELECTIVE ANDROGEN RECEPTOR MODULATORS AND METHOD FOR THEIR USE
US20040087810A1 (en) * 2002-10-23 2004-05-06 Dalton James T. Irreversible selective androgen receptor modulators and methods of use thereof
TW200410921A (en) * 2002-11-25 2004-07-01 Hoffmann La Roche Mandelic acid derivatives
WO2004089297A2 (en) * 2003-04-02 2004-10-21 Suntory Pharmaceutical Research Laboratories, Llc Compounds and methods for treatment of thrombosis
US7268147B2 (en) * 2003-05-15 2007-09-11 Pfizer Inc Compounds useful for the treatment of diseases
EP1477167A1 (en) * 2003-05-15 2004-11-17 Pfizer Limited [(2-hydroxy-2-(4-hydroxy-3-hydroxymethylphenyl)-ethylamino)-propyl] phenyl derivatives as beta2 agonists
US7375100B2 (en) * 2003-06-04 2008-05-20 Pfizer Inc 2-amino-pyridine derivatives useful for the treatment of diseases
GB0312832D0 (en) 2003-06-04 2003-07-09 Pfizer Ltd 2-amino-pyridine derivatives useful for the treatment of diseases
DE602004027301D1 (de) * 2003-12-22 2010-07-01 Merck Sharp & Dohme Alpha-hydroxyamide als bradykininantagonisten oder inverse agonisten
US7629358B2 (en) 2004-03-17 2009-12-08 Pfizer Inc Compounds useful for the treatment of diseases
EA200601510A1 (ru) 2004-03-17 2007-04-27 Пфайзер Инк. Производные фенилэтаноламина в качестве бета-2-агонистов
UA87854C2 (en) 2004-06-07 2009-08-25 Мерк Энд Ко., Инк. N-(2-benzyl)-2-phenylbutanamides as androgen receptor modulators

Also Published As

Publication number Publication date
EP1755572A2 (en) 2007-02-28
WO2005120477A3 (en) 2006-03-02
CA2569124C (en) 2013-04-23
JP4881865B2 (ja) 2012-02-22
EP1755572B1 (en) 2012-02-15
PE20060401A1 (es) 2006-05-15
NO20070085L (no) 2007-03-06
ECSP067061A (es) 2007-01-26
MY147997A (en) 2013-02-28
CA2569124A1 (en) 2005-12-22
US7629367B2 (en) 2009-12-08
AU2005251766A1 (en) 2005-12-22
US20070225229A1 (en) 2007-09-27
ZA200609673B (en) 2008-09-25
MXPA06014235A (es) 2007-02-14
TW200610755A (en) 2006-04-01
JP2008501800A (ja) 2008-01-24
BRPI0511862A (pt) 2008-01-15
US7268153B2 (en) 2007-09-11
UA87854C2 (en) 2009-08-25
SG169398A1 (en) 2011-03-30
NZ551738A (en) 2009-11-27
AU2005251766B2 (en) 2009-01-15
IL179843A0 (en) 2007-05-15
AU2005251766B9 (en) 2009-05-28
CN1976902A (zh) 2007-06-06
WO2005120477A2 (en) 2005-12-22
US20080139630A1 (en) 2008-06-12
CR8777A (es) 2007-08-28
RU2006146678A (ru) 2008-07-20
ATE545631T1 (de) 2012-03-15
US7763659B2 (en) 2010-07-27
RU2378255C2 (ru) 2010-01-10
MA28677B1 (fr) 2007-06-01
US20050277681A1 (en) 2005-12-15

Similar Documents

Publication Publication Date Title
AR049140A1 (es) N-(2-bencil)-2-fenilbutamidas como moduladores del receptor de androgeno
AR041170A1 (es) Derivados de bencimidazol, benzoxazol y benzotiazol
AR057217A1 (es) Polimorfos de un modulador de receptor de androgeno
PE20120575A1 (es) Derivados de pirazolopirimidina como inhibidores de jak quinasas
AR045082A1 (es) Compuestos de aminobenzofenona y su uso en tratamientos terapeuticos
AR037487A1 (es) Compuestos derivados de pirimidina, proceso para prepararlos, composicion farmaceutica y el uso de los mismos en la fabricacion de medicamentos que producen un efecto inhibidor del ciclo celular (anti-proliferacion celular)
UY28752A1 (es) Agentes terapeuticos
PE20040650A1 (es) Moduladores del receptor de glucocorticoides
PE20081579A1 (es) Derivados de benzamida como agonistas del receptor
NO20073019L (no) Pyrasolonforbindelser som metabotrope glutamatreseptor-antagonister for behandlingen av nevrotiske og psykiatriske lidelser
PE20081689A1 (es) Derivados de n-(heteroaril)-1-heteroaril-1h-indol-2-carboxamidas y su preparacion
EA200901160A1 (ru) Производные 3-циано-4-(4-тетрагидропиранфенил)пиридин-2-она
AR076460A1 (es) Antagonistas del receptor cxcr3
EA201071317A1 (ru) ТЕТРАГИДРОЦИКЛОПЕНТА[b]ИНДОЛЬНЫЕ МОДУЛЯТОРЫ РЕЦЕПТОРОВ АНДРОГЕНОВ
PE20081609A1 (es) Compuestos carboxamida y su uso como inhibidores de calpaina
UY28374A1 (es) Agentes terapéuticos
ATE545413T1 (de) Antagonisten des opioidrezeptors
PE20130149A1 (es) Derivados de la cromenona con actividad anti-tumoral
AR063643A1 (es) Compuestos quimicos derivados de quinolina, un metodo de preparacion y composiciones farmaceuticas
JP2008540554A5 (es)
DE602005016601D1 (de) 5ht2c-rezeptor-modulator-zusammensetzungen und anwendungsverfahren
UY28144A1 (es) Agentes terapéuticos
PE20090591A1 (es) Derivados monoamida como antagonistas del receptor de orexina
DK1701940T3 (da) 2-(1H-indolylsulfanyl)-bensylaminderivater som SSRI
AR031867A1 (es) Compuestos derivados de fenoxibencilamina como ssri, su uso en la preparacion de medicamentos, procedimiento de preparacion del compuesto e intermediarios utiles

Legal Events

Date Code Title Description
FA Abandonment or withdrawal