[go: up one dir, main page]

AR051135A1 - Fenilpirazoles - Google Patents

Fenilpirazoles

Info

Publication number
AR051135A1
AR051135A1 ARP050104228A ARP050104228A AR051135A1 AR 051135 A1 AR051135 A1 AR 051135A1 AR P050104228 A ARP050104228 A AR P050104228A AR P050104228 A ARP050104228 A AR P050104228A AR 051135 A1 AR051135 A1 AR 051135A1
Authority
AR
Argentina
Prior art keywords
atoms
replaced
het
hal
con
Prior art date
Application number
ARP050104228A
Other languages
English (en)
Inventor
Hans-Michael Eggenweiler
Michael Wolf
Original Assignee
Merck Patent Gmbh
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 Patent Gmbh filed Critical Merck Patent Gmbh
Publication of AR051135A1 publication Critical patent/AR051135A1/es

Links

Classifications

    • 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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • A61P17/06—Antipsoriatics
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A61P3/08—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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • 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
    • 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
    • A61P39/00—General protective or antinoxious agents
    • A61P39/02—Antidotes
    • 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
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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
    • C07D231/18—One oxygen or sulfur atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Immunology (AREA)
  • Molecular Biology (AREA)
  • Neurology (AREA)
  • Pulmonology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Biotechnology (AREA)
  • Reproductive Health (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Psychiatry (AREA)
  • Obesity (AREA)
  • AIDS & HIV (AREA)
  • Ophthalmology & Optometry (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)

Abstract

Los derivados de fenil-pirazoles de la formula (1) en la que R1 es OH, OCH3, OCF3, OCHF2, OBzl, OAc, p-metoxibenciloxi, SH, S(O)mCH3, SO2NH2, Hal, CF3 o CH3; R2, R3 son cada uno, de modo independiente entre sí, H, Hal, CN, NO2, A, Alk, (CH2)nAr, (CH2)nHet, COOH, COOA, COOAr, COOHet, CONH2, CONHA, CONAA', CONHAr, CONAAr, CON(Ar)2, CONHHet, CON(Het)2, NH2, NHA, NHAR, NHHet, NAA', NHCOA, NACOA, NHCOAr, NHCOHet, NHCOOA, NHCOOAr, NHCOOHet, NHCONHA, NHCONHAr, NHCONHHet, OH, OA, OAr, OHet, SH, S(O)mA, S(O)mAr, S(O)mHet, SO2NH2, SO2NHA, SO2NAA', SO2NH(CH2)nAr, SO2NAAr, SO2NH(CH2)nHet, SO2N(Ar)2 o SO2N(Het)2; R4, R5, R6 son cada uno, de modo independiente entre sí, H, Hal, CN, NO2, A, Alk, (CH2)nAr, (CH2)nHet, COOH, COOA, COOAr, COOHet, CONH2, CONHA, CONAA', CONHAr, CONAAr, CON(Ar)2, CONHHet, CON(Het)2, NH2, NHA, NHAR, NHHet, NAA', NHCOA, NHCONH2, NACOA', NHCOAr, NHCOHet, NHCOOA, NHCOOAr, NHCOOHet, NHCONHA, NHCONHAr, NHCONH-Het, OH, OA, OAr, OHet, SH, S(O)mA, S(O)mAr, S(O)mHet, SO2NH2, SO2NHA, SO2NAA', SO2NHAr, SO2NAAr, SO2NHHet, SO2N(Ar)2 o SO2N(Het)2; R4 y R5 también son juntos OCH2O, OCH2CH2O, NH-CH=CH o CH=CH-NH; X es O, S, SO o SO2; Y es A, Ar o Het; A, A' son cada uno, de modo independiente entre sí, alquilo no ramificado o ramificado con 1-10 átomos de C, en donde uno, dos o tres grupos CH2 pueden estar reemplazados por O, S, SO, SO2, NH, NR8 y/o por grupos -CH=CH y/o también 1-5 átomos de H pueden estar reemplazados por F, Cl, y/o R7, Alk o alquilo cíclico con 3-7 átomos de C; A y A' también son juntos una cadena alquileno con 2, 3, 4, 5 o 6 átomos de C, en donde un grupo CH2 puede estar reemplazado por O, S, SO, SO2, NH, NR8, NCOR8 o NCOOR8; Alk es alquenilo con 2-6 átomos de C; R7 es COOR9, CONR9R10, NR9R10, NHCOR9, NHCOOR9 u OR9; R8 es cicloalquilo con 3-7 átomos de C, cicloalquilalquileno con 4-10 átomos de C, Alk o alquilo no ramificado o ramificado con 1-6 átomos de C, en donde uno, dos, o tres grupos CH2 pueden estar reemplazados por O, S, SO, SO2, NH y/o también 1-5 átomos de H pueden estar reemplazados por F y/o Cl; R9, R10 son cada uno, de modo independiente entre sí, H o alquilo con 1-5 átomos de C, en donde 1-3 grupos CH2 pueden estar reemplazados por O, S, SO, SO2, NH, NMe o NEt y/o también 1-5 átomos de H pueden estar reemplazados por F y/o Cl; R9 y R10 también son juntos una cadena alquileno con 2, 3, 4, 5, o 6 átomos de C, en donde un grupo CH2 puede estar reemplazado por O, S, SO, SO2, NH, NR8, NCOR8 o NCOOR8; Ar es fenilo, naftilo o bifenilo no sustituido o mono-, di- o trisustituido con Hal; A, OR11, N(R11)2, NO2, CN, fenilo, CON(R11)2, NR11COA, NR11CON(R11)2, NR11SO2A, COR11, SO2N(R11)2, S(O)mA, [C(R11)2]n-COOR y/u -O[C(R11)2]o-COOR11; Het es un heterociclo mono- o bicíclico saturado, insaturado o aromático con 1 a 4 átomos de N, O y/o S, que puede estar mono-, di- o trisustituido con Hal, A, (CH2)nOR11, (CH2)nN(R11)2, NO2, CN, COOR11, CON(R11)2, NR11COA, NR11SO2A, COR11, SO2NR11, S(O)mA, =S, =NR11 y/u =O (el oxígeno del carbonilo); R11 es H o A; Hal es F, Cl, Br o I; m es 0, 1 o 2; n es 0, 1,2 ,3 o 4; o es 1, 2 o 3; así como sus derivados, sales, solvatos, tautomeros y estereoisomeros de utilidad farmacéutica, incluyendo sus mezclas en todas las proporciones, excluyendo los compuestos de la formula (1), en la que R1 es OH u OCH3; R2 es H o etilo; R3 es H o metilo; R4 es H, NO2, F, Cl, Br, fenilo, i-propilo, n-propilo, COOH, COOCH3 o etoxi; R5 es H o Cl; R6 es H; X es O; Y es H, Ch3 o CF3, son inhibidores de la HSP90 y pueden ser utilizados para preparar un medicamento para el tratamiento de enfermedades en las que la inhibicion, la regulacion y/o la modulacion de la HSP90 desempena un papel importante.
ARP050104228A 2004-10-08 2005-10-07 Fenilpirazoles AR051135A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE102004049078A DE102004049078A1 (de) 2004-10-08 2004-10-08 Phenylpyrazole

Publications (1)

Publication Number Publication Date
AR051135A1 true AR051135A1 (es) 2006-12-20

Family

ID=35427769

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP050104228A AR051135A1 (es) 2004-10-08 2005-10-07 Fenilpirazoles

Country Status (17)

Country Link
US (1) US20080090880A1 (es)
EP (1) EP1799649B1 (es)
JP (1) JP2008515823A (es)
KR (1) KR20070098782A (es)
CN (1) CN101035766A (es)
AR (1) AR051135A1 (es)
AU (1) AU2005293937A1 (es)
BR (1) BRPI0515582A (es)
CA (1) CA2583292A1 (es)
DE (1) DE102004049078A1 (es)
DK (1) DK1799649T3 (es)
ES (1) ES2494920T3 (es)
MX (1) MX2007004041A (es)
PT (1) PT1799649E (es)
RU (1) RU2007116868A (es)
WO (1) WO2006039977A1 (es)
ZA (1) ZA200703677B (es)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2586612C (en) 2004-11-18 2016-10-11 Synta Pharmaceuticals Corp. Triazole compounds that modulate hsp90 activity
SI1877379T1 (sl) 2005-04-13 2013-05-31 Astex Therapeutics Limited Derivati hidroksibenzinamida in njih uporaba kot inhibitorji HSP90
US7754725B2 (en) 2006-03-01 2010-07-13 Astex Therapeutics Ltd. Dihydroxyphenyl isoindolymethanones
DE102006023336A1 (de) 2006-05-18 2007-11-22 Merck Patent Gmbh 1,5-Diphenyl-pyrazole II
WO2008044041A1 (en) 2006-10-12 2008-04-17 Astex Therapeutics Limited Pharmaceutical combinations
GB0620259D0 (en) 2006-10-12 2006-11-22 Astex Therapeutics Ltd Pharmaceutical compounds
US8779132B2 (en) 2006-10-12 2014-07-15 Astex Therapeutics Limited Pharmaceutical compounds
WO2008044029A1 (en) 2006-10-12 2008-04-17 Astex Therapeutics Limited Pharmaceutical combinations
JP5528807B2 (ja) 2006-10-12 2014-06-25 アステックス、セラピューティックス、リミテッド 複合薬剤
EP2073804B1 (en) 2006-10-12 2017-09-13 Astex Therapeutics Limited Hydroxy-substituted benzoic acid amide compounds for use in the treatment of pain
GB0806527D0 (en) 2008-04-11 2008-05-14 Astex Therapeutics Ltd Pharmaceutical compounds
WO2009139834A1 (en) * 2008-05-13 2009-11-19 Poniard Pharmaceuticals, Inc. Bioactive compounds for treatment of cancer and neurodegenerative diseases
US20110144056A1 (en) * 2008-06-11 2011-06-16 Lin Linus S Pyrazole derivatives useful as inhibitors of faah
US9205086B2 (en) 2010-04-19 2015-12-08 Synta Pharmaceuticals Corp. Cancer therapy using a combination of a Hsp90 inhibitory compounds and a EGFR inhibitor
AU2012332421A1 (en) 2011-11-02 2014-06-05 Synta Pharmaceuticals Corp. Cancer therapy using a combination of Hsp90 inhibitors with topoisomerase I inhibitors
EP2776025A1 (en) 2011-11-02 2014-09-17 Synta Pharmaceuticals Corp. Combination therapy of hsp90 inhibitors with platinum-containing agents
CA2854188A1 (en) 2011-11-14 2013-05-23 Synta Pharmaceuticals Corp. Combination therapy of hsp90 inhibitors with braf inhibitors
WO2015089800A1 (en) * 2013-12-19 2015-06-25 Eli Lilly And Company Fluorophenyl pyrazol compounds
ES2968785T3 (es) * 2014-10-31 2024-05-14 Hoffmann La Roche Nuevos compuestos de piridiniloxi- y feniloxipirazolilo
WO2017155942A2 (en) 2016-03-07 2017-09-14 Northwestern University Substituted heterocycles as c-myc targeting agents
US11142504B2 (en) 2016-03-07 2021-10-12 Northwestern University Substituted heterocycles as c-MYC targeting agents
CN114174265A (zh) * 2018-08-31 2022-03-11 西北大学 作为c-MYC靶向剂的取代的杂环
WO2020257261A1 (en) 2019-06-17 2020-12-24 Northwestern University SUBSTITUTED HETEROCYCLES AS c-MYC TARGETING AGENTS
CN118125978B (zh) * 2024-01-31 2025-08-12 安徽中医药大学 一种myc抑制剂及其制备方法和应用

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5968921A (en) 1997-10-24 1999-10-19 Orgegon Health Sciences University Compositions and methods for promoting nerve regeneration
AU3378599A (en) 1998-04-03 1999-10-25 University Of Pittsburgh Benzoquinoid ansamycins for the treatment of cardiac arrest and stroke
CA2367108A1 (en) 1999-03-12 2000-09-14 The United States Of America, Represented By The Secretary, Department O F Health And Human Services Method of inhibiting a chaperone protein
CA2429196A1 (en) 2000-03-24 2001-10-04 Duke University Characterization of grp94-ligand interactions and purification, screening, and therapeutic methods relating thereto
WO2002002123A1 (en) 2000-06-29 2002-01-10 Trustees Of Boston University Use of geldanamycin and related compounds for prophylaxis or treatment of fibrogenic disorders
WO2002007761A1 (en) 2000-07-20 2002-01-31 Merck & Co., Inc. Inhibiting hepatitis c virus processing and replication
CA2417495C (en) 2000-07-28 2013-04-30 Sloan-Kettering Institute For Cancer Research Methods for treating cell proliferative disorders and viral infections
JP4406205B2 (ja) 2000-11-02 2010-01-27 スローン−ケッタリング・インスティテュート・フォー・キャンサー・リサーチ Ｈｓｐ９０に結合するための小分子組成物
WO2003041643A2 (en) 2001-11-09 2003-05-22 Conforma Therapeutics Corporation Hsp90-inhibiting zearalanol compounds and methods of producing and using same
DE60222804T2 (de) 2001-12-21 2008-07-03 Vernalis (Cambridge) Ltd., Abington 3-(2,4)dihydroxyphenyl-4-phenylpyrazole und deren medizinische verwendung
GB0228417D0 (en) * 2002-12-05 2003-01-08 Cancer Rec Tech Ltd Pyrazole compounds
GB0229618D0 (en) 2002-12-19 2003-01-22 Cancer Rec Tech Ltd Pyrazole compounds
JP2005225787A (ja) * 2004-02-12 2005-08-25 Nippon Kayaku Co Ltd Ｈｓｐ９０阻害剤

Also Published As

Publication number Publication date
US20080090880A1 (en) 2008-04-17
ZA200703677B (en) 2008-08-27
ES2494920T3 (es) 2014-09-16
WO2006039977A1 (de) 2006-04-20
CA2583292A1 (en) 2006-04-20
DK1799649T3 (da) 2014-08-11
JP2008515823A (ja) 2008-05-15
AU2005293937A1 (en) 2006-04-20
DE102004049078A1 (de) 2006-04-13
RU2007116868A (ru) 2008-11-20
CN101035766A (zh) 2007-09-12
EP1799649B1 (de) 2014-06-25
MX2007004041A (es) 2007-05-24
KR20070098782A (ko) 2007-10-05
EP1799649A1 (de) 2007-06-27
PT1799649E (pt) 2014-10-01
BRPI0515582A (pt) 2008-07-29

Similar Documents

Publication Publication Date Title
AR051135A1 (es) Fenilpirazoles
AR052482A1 (es) Derivados de triazol como inhibidores de hsp90
AR061010A1 (es) Derivados de triazol i i
AR061009A1 (es) 1,2-difenil-pirazoles i i como inhibidores de hsp90
AR061735A1 (es) Derivados de indazol, composiciones farmaceuticas y uso de los mismos
AR050454A1 (es) 1,5-difenil-pirazoles.
AR067506A1 (es) Derivados de quinazolinamida
AR070649A1 (es) Derivados de 1,3- dihidro -isoindol
AR081828A1 (es) Compuestos de biguanida y su uso para el tratamiento del cancer
AR058546A1 (es) Derivados de 2- adamantilurea como inhibidores selectivos de 11 beta - hsd1
AR054047A1 (es) Derivados de fenilquinazolina
AR045731A1 (es) Compuestos de aminotriazol utiles como inhibidores de quinasas de proteinas
AR039695A1 (es) Derivados de tiazol, uso de los mismos para preparar un medicamento y conjunto en envases (kit)
AR072192A1 (es) Derivados de tiazolil-piperidina
AR074418A1 (es) Compuestos de benzonaftiridina, procedimiento de preparacion y su uso en el tratamiento de tumores
AR074493A1 (es) Derivados de quinazolinamida
CO5261616A1 (es) Inhibidores no peptidicos de la union celular dependientes de vla-4 utiles en el tratamiento de enfermedades inflamatorias, autoinmunes y respiratorias
AR035789A1 (es) Compuestos de 1h-imidazol 4- o 5- sustituidos, agoinistas selectivos de los receptores adrenergicos alfa 2b aisladamente o de alfa 2b/alfa 2c
AR071523A1 (es) Compuestos biciclicos fusionados, un proceso para su preparacion, el compuesto para ser utilizado como medicamento en el tratamiento y profilaxis de enfermedades, una composicion farmaceutica y un conjunto que comprende paquetes separados del compuesto y de un ingrediente activo del medicamento
AR068659A1 (es) Derivados de imidazol inhibidores de autotaxina
CO5170521A1 (es) Compuestos farmaceuticos de pirimidinona
RU2011152369A (ru) Производные n-гидроксилсульфонамида в качестве новых физиологически полезных доноров нитроксила
RU2013108865A (ru) Производные хинолина и содержащие их ингибиторы melk
AR082726A1 (es) Derivados de triazolopirazina
RU2013111317A (ru) Производные n-гидроксилсульфонамида как новые физиологически применимые доноры нитроксила

Legal Events

Date Code Title Description
FB Suspension of granting procedure