[go: up one dir, main page]

AR048691A1 - Compuestos con estructura de alquino con accion antagonista de mch y medicamentos que contienen estos compuestos - Google Patents

Compuestos con estructura de alquino con accion antagonista de mch y medicamentos que contienen estos compuestos

Info

Publication number
AR048691A1
AR048691A1 ARP050101439A ARP050101439A AR048691A1 AR 048691 A1 AR048691 A1 AR 048691A1 AR P050101439 A ARP050101439 A AR P050101439A AR P050101439 A ARP050101439 A AR P050101439A AR 048691 A1 AR048691 A1 AR 048691A1
Authority
AR
Argentina
Prior art keywords
alkyl
group
cycloalkyl
phenyl
atoms
Prior art date
Application number
ARP050101439A
Other languages
English (en)
Inventor
Dirk Stenkamp
Stephan Georg Mueller
Philipp Lustenberger
Gerald Juergen Roth
Klaus Rudolf
Marcus Schindler
Leo Thomas
Ralf Lotz
Thorsten Lehmann-Lintz
Original Assignee
Boehringer Ingelheim Int
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34964523&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR048691(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of AR048691A1 publication Critical patent/AR048691A1/es

Links

Classifications

    • 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
    • C07D213/24—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 substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/28—Radicals substituted by singly-bound oxygen or sulphur atoms
    • C07D213/30—Oxygen atoms
    • 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
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • 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
    • 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
    • A61P39/00—General protective or antinoxious agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • 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
    • A61P9/12—Antihypertensives
    • 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
    • C07D213/24—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 substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
    • C07D213/38—Radicals substituted by singly-bound nitrogen atoms having only hydrogen or hydrocarbon radicals attached to the substituent nitrogen atom
    • 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
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/08—Bridged systems

Landscapes

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

Abstract

La presente se refiere a compuestos con estructura de alquino de formula general (1), en la que: R1, R2 significan, de modo independiente entre sí, H, alquilo C1-8, cicloalquilo C3-7 o un radical fenilo o piridinilo opcionalmente mono- o polisustituido con radicales R20 iguales o diferentes y/o monosustituido con nitro, donde el grupo alquilo o cicloalquilo puede estar mono- o polisustituido con radicales R11 iguales o diferentes, y donde un grupo -CH2- puede estar reemplazado en la posicion 3 o 4 de un grupo cicloalquilo de 5, 6 o 7 miembros con -O-, -S- o -NR13-; o R1 y R2 forman un puente alquileno C3-8, donde un grupo -CH2- no adyacente al átomo de N del grupo R1R2N puede estar reemplazado por -CH=N-, -CH=CH-, -O-, -S-, - SO, -(SO2)-, -CO-, -C(=CH2)- o -NR13-, donde en el puente alquileno C3-8 antes definido uno o varios átomos de H pueden estar reemplazados por radicales R14 iguales o diferentes, y donde el puente de alquileno antes definido puede estar reemplazados por uno o varios grupos carbocíclicos o heterocíclicos Cy iguales o diferentes de modo tal que el enlace entre el grupo alquileno y el grupo Cy se produzca: a través de un enlace simple o doble; a través de un átomo de C comun, formándose un sistema de anillos espirocíclicos; a través de dos átomos de C y/o N comunes adyacentes, formándose un sistema de anillos bicíclicos condensados; o a través de tres o más átomos de C y/o N, formándose un sistema de anillos en puente; X significa un puente alquileno C1-6 que presenta uno o varios sustituyentes de modo independiente entre sí, seleccionados de fluor, cloro, hidroxi, ciano, CF3, alquilo C1-4, hidroxi-alquilo C1-4, cicloalquilo C3-6 y alcoxi C1-4, donde dos sustituyentes alquilo pueden estar unidos entre sí, formando un grupo cicloalquilo C3-7; o un grupo alquilenoxi C2-4 o alquilenimino C2-4, donde el grupo imino puede estar sustituido con un grupo alquilo C1-4, y donde la unidad de alquileno presenta uno o varios sustituyentes de modo independiente entre sí, seleccionados de fluor, cloro, CF3, hidroxi-alquilo C1-4, alquilo C1-4 y cicloalquilo C3-6, donde dos grupos alquilo pueden estar unidos entre sí, formando un grupo cicloalquilo C3-7 o cicloalquilenimino C4-6; o un puente alquenileno C3-6 o alquinileno C3-6, que es no sustituido o que presenta uno o varios sustituyentes seleccionados, de modo independiente entre sí, de fluor, CF3, hidroxi-alquilo C1-4, alquilo C1-4 y cicloalquilo C3-6, donde dos sustituyentes alquilo pueden estar unidos entre sí, formando un grupo cicloalquilo C3-7 o cicloalquenilo C5-7; y W, Z significan, de modo independiente entre sí, un enlace simple o un puente alquileno C1-2; donde dos átomos de C adyacentes con un puente adicional alquileno C1-4, pueden estar unidos entre sí; y donde uno o dos átomos de C pueden estar sustituidos, de modo independiente entre sí, con uno o dos radicales alquilo C1-3 iguales o diferentes, donde dos radicales alquilo pueden estar unidos entre sí formando un anillo carbocíclico; e Y, A se seleccionan, de modo independiente entre sí, del grupo compuesto por los grupos cíclicos bivalentes fenilo, piridinilo, pirimidinilo, pirazinilo, piridazinilo, naftilo, tetrahidronaftilo, indolilo, dihidroindolilo, quinolinilo, dihidroquinolinilo, tetrahidroquinolinilo, isoquinolinilo, dihidroisoquinolinilo, tetrahidro-isoquinolinilo, benzimidazolilo, benzoxazolilo, cromanilo, cromen-4-onilo, tienilo, furanilo, benzotienilo o benzofuranilo, donde los grupos cíclicos mencionados pueden estar mono- o polisustituidos en uno o varios átomos de C con radicales R20 igual o diferentes, en el caso de un anillo fenilo también monosustituido con nitro, y/o en uno o varios grupos NH con R21; B presenta uno de los significados indicados para Y, A o alquilo C1-6, alquenilo C1-6, alquinoilo C1-6, cicloalquilo C3-7, cicloalquenilo C5-7, cicloalquil C3-7-alquilo C1-3, cicloalquenil C3-7-alquilo C1-3, cicloalquil C3-7-alquenilo C1-3- o cicloalquil C3-7-alquinilo C1-3, donde uno o varios átomos de C de modo independiente entre sí, mono o polisustituidos con halogeno y/o monosustituidos con hidroxi o ciano y/o grupos cíclicos mono- o polisustituidos con radicales R20 iguales o diferentes; Cy es un grupo carbocíclico o heterocíclico seleccionado de uno de los siguientes significados: un grupo carbocíclico saturado de 3 a 7 miembros; un grupo carbocíclico insaturado de 4 a 7 miembros; un grupo fenilo; un grupo heterocíclico saturado de 4 a 7 miembros o insaturado de 5 a 7 miembros con un átomo de N, O o S como heteroátomo; un grupo heterocíclico saturado o insaturado de 5 a 7 miembros con dos o más átomos de N o con uno o dos átomos de N y un átomo de O o S como heteroátomos; un grupo heterocíclico aromático de 5 o 6 miembros con uno o varios heteroátomos iguales o diferentes seleccionados de N, O y/o S; donde los grupos saturados de 6 o 7 miembros antes descritos también pueden estar presentes como sistemas cíclicos en puente con un puente imino, (alquil C1-4)-imino, metileno, (alquil C1-4)-metileno o di-(alquil C1-4)-metileno; y donde los grupos cíclicos antes mencionados mono- o polisustituidos en uno o varios átomos de C pueden estar sustituidos con radicales R20 iguales o diferentes, en el caso de un grupo fenilo también adicionalmente monosustituidos con nitro, y/o uno o varios grupos NH sustituidos con R21; R11 significa halogeno, alquilo C1-6, alquenilo C2-6, alquinoilo C2- 6, R15-O, R15-O-CO-, R15-CO-O-, ciano, R16R17N-, R18R19N-CO- o Cy-, donde en los grupos antes indicados uno o varios átomos de C pueden estar mono- o polisustituidos, de modo independiente entre sí, por sustituyentes seleccionados de halogeno, OH, CN, CF3, alquilo C1-3, hidroxi-alquilo C1-3; R13 tiene uno de los significados indicados para R17; R14 es halogeno, ciano, alquilo C1-6, alquenilo C2-6, alquinoilo C2-6, R15-O-, R15-O-CO-, R15-CO-, R15-CO-O-, R16R17N-, R18R19N-CO-, R15-O-alquilo C1- 3, R15-O-CO-alquilo C1-3, R15-SO2-NH-, R15-O-CO-NH-alquilo C1-3, R15-SO2-NH-alquilo C1-3, R15-CO-alquilo C1-3, R15-CO-O-alquilo C1-3, R16R17N-alquilo C1-3, R18R19N-CO-alquilo C1-3 o Cy-alquilo C1-3; R15 es H, alquilo C1-4, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-3, fenilo, fenil-alquilo C1-3, piridinilo o piridinil-alquilo C1-3; R16 es H, alquilo C1-6, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-3, cicloalquenilo C4-7, cicloalquenil C4-7-alquilo C1-3, w-hidroxi-alquilo C2-3, w- (alcoxi C1-4)-alquilo C2-3, amino-alquilo C2-6, alquil C1-4-amino-alquilo C2-6, di-(alquil C1-4)-amino-alquilo C2-6 o ciclo-alquilenimino C3-6-alquilo C2-6; R17 tiene uno de los significados indicados para R16 o es fenilo, fenil-alquilo C1-3, piridinilo, alquil C1-4-carbonilo, hidroxicarbonil-alquilo C1-3, alcoxicarbonilo C1-4, alcoxicarbonil C1-4-alquilo C1-3, alquilcarbonilamino C1-4-alquilo C2-3, N-(alquilcarbonil C1-4)-N-(alquil C1-4)-amino-alquilo C2-3, alquilsulfonilo C1-4, alquilsulfonilamino C1-4-alquilo C2-3 o N-(alquilosulfonil C1-4)-N-(alquil C1-4)-amino-alquilo C2-3; R18, R19 son, de modo independiente entre sí, H o alquilo C1-6; R20 es halogeno, hidroxi, ciano, alquilo C1-6, alquenilo C2-6, alquinoilo C2-6, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-3, hidroxi-alquilo C1-3, R22-alquilo C1-3 o uno de los significados indicados para R22; R21 es alquilo C1-4, w-hidroxi-alquilo C2-6, w-alcoxi C1-4-alquilo C2-6, w-alquil C1-4-amino-alquilo C2-6, w-di- (alquil C1-4)-amino-alquilo C2-6, w-ciclo-alquilenimino C3-6-alquilo C2-6, fenilo, fenil-alquilo C1-3, alquil C1-4-carbonilo, alcoxi C1-4-carbonilo, alquilsulfonilo C1-4, aminosulfonilo, alquilaminosulfonilo C1-4, di-alquilaminosulfonilo C1-4 o ciclo-alquilen C3-6-imino-sulfonilo; R22 es piridinilo, fenilo, fenil-alcoxi C1-3, cicloalquilenimino C3-6-alcoxi C2-4, OHC-, HO-N=HC-, alcoxi C1-4-N=HC-, alcoxi C1-4, alquiltio C1-4, carboxi, alquilcarbonilo C1-4, alcoxicarbonilo C1-4, aminocarbonilo, alquilaminocarbonilo C1-4, di-(alquil C1-4)-aminocarbonilo, cicloalquil C3-6-amino-carbonilo, cicloalquilenimino C3-6-carbonilo, fenilaminocarbonilo, cicloalquilenimino C3-6-alquil C2-4-aminocarbonilo, alquilsulfonilo C1-4, alquilsulfinilo C1-4, alquilsulfonilamino C1-4, amino, alquilamino C1-4, di-(alquil C1-4)-amino, alquil C1-4-carbonil-amino, cicloalquilenimino C3-6, fenil-alquilamino C1-3, N-(alquil C1-4)-fenil-alquilamino C1-3, acetilamino, propionilamino, fenilcarbonilo, fenilcarbonilamino, fenilcarbonilmetilamino, hidroxi-alquilaminocarbonilo C2-3, (4-morfolinil)carbonilo, (1-pirrolidinil)carbo-nilo, (1-piperidinil)carbonilo, (hexahidro-1-azepinil)carbonilo, (4-metil-1-piperazinil)carbonilo, metilendioxi, aminocarbonilamino o alquilaminocarbonilamino C1-4; donde en los grupos y radicales antes mencionados, en especial en W, Z, R13 a R22, uno o varios átomos de C adicionalmente mono o polisustituidos con F y/o uno o dos átomos de C, de modo independiente entre sí, adicionalmente monosustituidos con Cl o Br y/o uno o varios anillos fenilo, de mono independiente entre sí, presentan adicionalmente uno, dos o tres sustituyentes seleccionados del grupo F, Cl, Br, I, ciano, alquilo C1- 4, alcoxi C1-4-, difluorometilo, trifluorometilo, hidroxi, amino, alquilamino C1-3, di-(alquil C1-3)-amino, acetilamino, aminocarbonilo, difluorometoxi, trifluorometoxi, amino-alquilo C1-3, alquilamino C1-3-alquilo C1-3 y di-(alquil C1-3)-amino- alquilo C1-3 y/o pueden estar monosustituido con nitro; y el átomo de H de un grupo carboxi existente o un átomo de H unido a un átomo de N puede estar reemplazado por un radical escindible in vivo, sus tautomeros, sus diasteroisomeros, sus enantiomeros, sus mezclas y sus sales; donde los siguientes compuestos no están comprendidos: (1-{5-[5-(4-cloro-fenil)-piridin-2-iletinil]-piridin-2-il}-pirrolidin-3-il)-dimetil-amina; 5'-[5-(4-cloro-fenil)-piridin-2-iletinil]-3-pirrolidin-1-il- 3,4,5,6-tetrahidro-2H-[1,2']bipiridinilo; 1'-{5-[5-(4-cloro-fenil)-piridin-2-iletinil]-piridin-2-il-}-[1,3']bipirrolidinilo; {5-[5-(4-cloro-fenil)-piridin-2-iletinil]-pirid
ARP050101439A 2004-04-14 2005-04-13 Compuestos con estructura de alquino con accion antagonista de mch y medicamentos que contienen estos compuestos AR048691A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE102004017930A DE102004017930A1 (de) 2004-04-14 2004-04-14 Neue Alkin-Verbindungen mit MCH-antagonistischer Wirkung und diese Verbindungen enthaltende Arzneimittel

Publications (1)

Publication Number Publication Date
AR048691A1 true AR048691A1 (es) 2006-05-17

Family

ID=34964523

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP050101439A AR048691A1 (es) 2004-04-14 2005-04-13 Compuestos con estructura de alquino con accion antagonista de mch y medicamentos que contienen estos compuestos

Country Status (9)

Country Link
EP (1) EP1737824A2 (es)
JP (1) JP2007532596A (es)
AR (1) AR048691A1 (es)
CA (1) CA2558755A1 (es)
DE (1) DE102004017930A1 (es)
PE (1) PE20060254A1 (es)
TW (1) TW200538102A (es)
UY (1) UY28852A1 (es)
WO (1) WO2005103032A2 (es)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7452911B2 (en) 2002-10-31 2008-11-18 Boehringer Ingelheim Pharma Gmbh & Co. Kg Alkyne compounds with MCH antagonistic activity and medicaments comprising these compounds
DE102004017935A1 (de) * 2004-04-14 2005-11-03 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Alkin-Verbindungen mit MCH-antagonistischer Wirkung und diese Verbindungen enthaltende Arzneimittel
MX2008016343A (es) 2006-06-23 2009-01-19 Abbott Lab Derivados ciclopropil amina como moduladores del receptro de histamina h3.
US9108948B2 (en) 2006-06-23 2015-08-18 Abbvie Inc. Cyclopropyl amine derivatives
CA2657183A1 (en) 2006-08-25 2008-02-28 Boehringer Ingelheim International Gmbh New pyridone derivatives with mch antagonistic activity and medicaments comprising these compounds
TW200831485A (en) * 2006-12-11 2008-08-01 Boehringer Ingelheim Int New pyridazine derivatives with MCH antagonistic activity and medicaments comprising these compounds
US9186353B2 (en) 2009-04-27 2015-11-17 Abbvie Inc. Treatment of osteoarthritis pain
US20130143869A1 (en) * 2010-07-16 2013-06-06 Merz Pharma Gmbh & Co. Kgaa Use of a cationic amphiphilic drug for the preparation of a formulation for the reduction of subcutaneous adipose tissue
US8853390B2 (en) 2010-09-16 2014-10-07 Abbvie Inc. Processes for preparing 1,2-substituted cyclopropyl derivatives
US8633182B2 (en) 2012-05-30 2014-01-21 Boehringer Ingelheim International Gmbh Indanyloxyphenylcyclopropanecarboxylic acids
AR097617A1 (es) 2013-09-13 2016-04-06 Actelion Pharmaceuticals Ltd Derivados antibacterianos del 2h-indazol
MA39189A1 (fr) 2013-12-19 2017-06-30 Actelion Pharmaceuticals Ltd Dérivés de 1h-indazole et de 1h-indole antibactériens
AR099612A1 (es) 2014-03-04 2016-08-03 Actelion Pharmaceuticals Ltd Derivados antibacterianos de 1,2-dihidro-3h-pirrolo[1,2-c]imidazol-3-ona
US10538490B2 (en) 2016-10-25 2020-01-21 Boehringer Ingelheim International Gmbh Benzylaminopyridylcyclopropanecarboxylic acids, pharmaceutical compositions and uses thereof
EP3544958B1 (en) 2016-11-28 2021-03-24 Boehringer Ingelheim International GmbH Indanylaminopyridylcyclopropanecarboxylic acids, pharmaceutical compositions and uses thereof
US10913720B2 (en) 2017-01-26 2021-02-09 Boehringer Ingelheim International Gmbh Benzyloxypyridylcyclopropanecarboxylic acids, pharmaceutical compositions and uses thereof
US10919859B2 (en) 2017-01-26 2021-02-16 Boehringer Ingelheim International Gmbh Benzylaminopyridylcyclopropanecarboxylic acids, pharmaceutical compositions and uses thereof
US10603317B2 (en) 2017-01-26 2020-03-31 Boehringer Ingelheim International Gmbh Benzylaminopyridylcyclopropanecarboxylic acids, pharmaceutical compositions and uses thereof
WO2018138026A1 (en) 2017-01-26 2018-08-02 Boehringer Ingelheim International Gmbh Indanylaminopyrazinylcyclopropanecarboxylic acids, pharmaceutical compositions and uses thereof
CN110248929B (zh) 2017-01-26 2023-05-12 勃林格殷格翰国际有限公司 苄基氨基吡嗪基环丙烷甲酸、其药物组合物和用途
TWI830733B (zh) * 2018-05-11 2024-02-01 中國大陸商迪哲（江蘇）醫藥有限公司 環戊烷化合物

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5856510A (en) * 1996-12-16 1999-01-05 Allelix Biopharmaceuticals Inc. 5-alkenyl and 5-alkynyl indole compounds
TW544448B (en) * 1997-07-11 2003-08-01 Novartis Ag Pyridine derivatives
CA2386474A1 (en) * 1999-09-20 2001-03-29 Takeda Chemical Industries, Ltd. Melanin concentrating hormone antagonist
EP1285651B1 (en) * 2000-04-28 2010-09-01 Takeda Pharmaceutical Company Limited Melanin concentrating hormone antagonists
EP1366030A2 (en) * 2000-07-06 2003-12-03 Neurogen Corporation Melanin concentrating hormone receptor ligands
JP2002167382A (ja) * 2000-07-13 2002-06-11 Sankyo Co Ltd アミノアルコ−ル誘導体
GB0119474D0 (en) * 2001-08-09 2001-10-03 Astrazeneca Ab Compounds
JO2311B1 (en) * 2001-08-29 2005-09-12 ميرك فروست كندا ليمتد Alkyl inhibitors Ariel phosphodiesterase-4
DE10250708A1 (de) * 2002-10-31 2004-05-19 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Alkin-Verbindungen mit MCH-antagonistischer Wirkung und diese Verbindungen enthaltende Arzneimittel
DE102004017935A1 (de) * 2004-04-14 2005-11-03 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Alkin-Verbindungen mit MCH-antagonistischer Wirkung und diese Verbindungen enthaltende Arzneimittel

Also Published As

Publication number Publication date
DE102004017930A1 (de) 2005-11-03
EP1737824A2 (de) 2007-01-03
TW200538102A (en) 2005-12-01
UY28852A1 (es) 2005-11-30
PE20060254A1 (es) 2006-03-31
WO2005103032A2 (de) 2005-11-03
CA2558755A1 (en) 2005-11-03
WO2005103032A3 (de) 2006-02-02
JP2007532596A (ja) 2007-11-15

Similar Documents

Publication Publication Date Title
AR048691A1 (es) Compuestos con estructura de alquino con accion antagonista de mch y medicamentos que contienen estos compuestos
AR041734A1 (es) Compuestos de alquino con efecto antagonico de la hcm y medicamentos que contienen estos compuestos
AR041735A1 (es) Compuestos de amida con accion antagonista de mch y medicamentos que contienen estos compuestos
AR043046A1 (es) Compuestos de amida de acido carboxilico con efecto antagonico de la hcm, medicamentos que contienen estos compuestos y procedimientos para su preparacion
ES2569528T3 (es) 4-pirazolil-N-arilpirimidin-2-aminas y 4-pirazolil-N-heteroarilpirimidin-2-aminas como inhibidores de quinasas Janus
AR062510A1 (es) Derivados de piridona con actividad antagonista de mch y medicamentos que comprenden estos compuestos
AR051294A1 (es) Derivados heterociclicos y su uso como inhibidores de la estearoil-coa desaturasa
AR061844A1 (es) Pirimidil-ciclopentanos como inhibidores de protein-quinasa akt
ES2570127T3 (es) Compuestos y composiciones como inhibidores de la proteína quinasa
AR069526A1 (es) Compuesto heterociclico que contiene nitrogeno y su uso
HRP20120968T1 (hr) Spojevi
PE20070218A1 (es) COMPUESTOS DE CICLOALQUILO AMINO-HIDANTOINA Y USO DE ESTOS PARA LA MODULACION DE ß-SECRETASA
AR051202A1 (es) Derivados heterociclicos y su uso como inhibidores de la estearoil-coa desaturasa
AR038914A1 (es) Indazoles substituidos, composiciones que los contienen, procedimiento de fabricacion y utilizacion para fabricar un medicamento
AR066669A1 (es) Derivados de imidazolona como inhibidores de bencimidazolona quimasa. composiciones farmaceuticas.
AR072900A1 (es) Agentes terapeuticos derivados de pirazolo[3,4-d]pirimidina
AR047454A1 (es) Oxadiazoles sustituidos y composiciones farmaceuticas que los contienen.
PE20060573A1 (es) Derivados de urea ciclicos sustituidos como inhibidores de proteinas quinasas
AR057109A1 (es) Benzimidazoles sustituidos y metodos para usarlos como inhibidores de las quinasas asociadas con la tumorigenesis
AR049294A1 (es) DERIVADOS DE QUINAZOLINA; INHIBIDORES DE LA TIROSINA QUINASA DEL RECEPTOR ERBB2; COMPOSICIONES FARMACÉUTICAS QUE LOS CONTIENEN; MÉTODOS PARA SU PREPARACIoN Y SU USO COMO MEDICAMENTO PARA EL TRATAMIENTO O PREVENCIoN DE TUMORES SoLIDOS.
AR047449A1 (es) Amino-benzazoles como inhibidores del receptor p2y1, composiciones farmaceuticas y metodos de tratamiento
PE20091433A1 (es) Agonistas de receptores muscarinicos, composiciones, metodos de tratamiento de los mismos, y procedimientos para su preparacion 177
AR042148A1 (es) Derivados de indazol como antagonistas de crf
HRP20140252T1 (hr) Derivati imidazola kao inhibitori kazeinske kinaze
AR049696A1 (es) Derivados de indol

Legal Events

Date Code Title Description
FB Suspension of granting procedure