ES2289116T3 - Nuevos derivados de pirrol como agentes farmaceuticos. - Google Patents

Nuevos derivados de pirrol como agentes farmaceuticos. Download PDF

Info

Publication number
ES2289116T3
ES2289116T3 ES02744115T ES02744115T ES2289116T3 ES 2289116 T3 ES2289116 T3 ES 2289116T3 ES 02744115 T ES02744115 T ES 02744115T ES 02744115 T ES02744115 T ES 02744115T ES 2289116 T3 ES2289116 T3 ES 2289116T3
Authority
ES
Spain
Prior art keywords
alkyl
substituted
unsubstituted
amino
ring
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Lifetime
Application number
ES02744115T
Other languages
English (en)
Inventor
Jason Scott Sawyer
Douglas Wade Beight
Paola Ciapetti
Todd Vincent Decollo
Alexander Glenn Godfrey
Theodore Goodson, Jr.
David Kent Herron
Hong-Yu Li
Junkai Liao
William Thomas Mcmillen
Shawn Christopher Miller
Nicolas Anthony Mort
Jonathan Michael Yingling
Edward C. R. Smith
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Eli Lilly and Co
Original Assignee
Eli Lilly and Co
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 Eli Lilly and Co filed Critical Eli Lilly and Co
Application granted granted Critical
Publication of ES2289116T3 publication Critical patent/ES2289116T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/12Keratolytics, e.g. wart or anti-corn preparations
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02Muscle relaxants, e.g. for tetanus or cramps
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems

Landscapes

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

Abstract

Un compuesto de estructura, en la que **fórmula** es un anillo saturado de cuatro, cinco o seis miembros y X es C, O ó S; con la condición de que el anillo es un anillo de carbono completamente saturado en el que X en el anillo puede ser una sustitución única de cualquier C, O ó S, excepto que X no puede ser O cuando esté adyacente al carbono del anillo de pirazolo y R1 es piridina y R2 es un sulfonil fenilo o tienilo; R1 es fenilo sustituido o no sustituido; piridina sustituida o no sustituida; N-óxido de piridina sustituida o no sustituida; quinolina sustituida o no sustituida; N-óxido de quinolina sustituida o no sustituida; naftpiridina sustituida o no sustituida; pirazina sustituida o no sustituida; furilo; tiazolilo sustituido o no sustituido; imidazolilo sustituido o no sustituido; pirazolilo sustituido o no sustituido; o tiofenilo sustituido o no sustituido; en el que la sustitución puede ser una o más de las siguientes: alquilo (C1-C6), alquenilo (C2-C6), alquinilo (C2-C6), alcoxi (C1-C6), alqueniloxi (C2-C6), alquiniloxi (C2-C6), alquiltio (C1-C6), alquil (C1-C6) sulfinilo, alquil (C1-C6) sulfonilo, alquil (C1-C6) amino, di-[alquil (C1-C6)]amino, alcoxi (C1-C6) carbonilo, N-alquil (C1-C6)-carbamoílo, N, N-di-[alquil (C1-C6)]carbamoílo, alcanoílo (C2-C6), alcanoiloxi (C2-C6), alcanoil (C2-C6) amino, N-alquil (C1-C6)-alcanoil(C2-C6)amino, alquenoil (C3-C6)amino, N-alquil (C1-C6)-alquenoil (C3-C6)amino, alquinoil (C3-C6)amino, N-alquil (C1-C6)-alquinoil (C3-C6)amino, N-alquil (C1-C6)sulfamoílo, N, N-di-[alquil(C1-C6)]sulfamoílo, alcano (C1-C6) sulfonilamino, N-alquil (C1-C6)-alcano (C1-C6) sulfonilamino, carboxamida, tiofenilo, aminofenilo, trifluorometilo, halo, trifluorometoxi, hidroximetilo, N-pirrolidino, N-morfolino, feniltio, dialquil (C1-C4) aminometilo, metoxifenilo, amino, hidroxi, carboxilo, fenilo, arilalquilo.
ES02744115T 2001-05-24 2002-05-13 Nuevos derivados de pirrol como agentes farmaceuticos. Expired - Lifetime ES2289116T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US29346401P 2001-05-24 2001-05-24
US293464P 2001-05-24

Publications (1)

Publication Number Publication Date
ES2289116T3 true ES2289116T3 (es) 2008-02-01

Family

ID=23129192

Family Applications (1)

Application Number Title Priority Date Filing Date
ES02744115T Expired - Lifetime ES2289116T3 (es) 2001-05-24 2002-05-13 Nuevos derivados de pirrol como agentes farmaceuticos.

Country Status (38)

Country Link
US (1) US7087626B2 (es)
EP (1) EP1397364B1 (es)
JP (2) JP4519407B2 (es)
KR (1) KR100861630B1 (es)
CN (2) CN1269820C (es)
AR (1) AR036034A1 (es)
AT (1) ATE368041T1 (es)
AU (1) AU2002339268B2 (es)
BR (1) BR0209939A (es)
CA (1) CA2446820C (es)
CO (1) CO5540282A2 (es)
CY (1) CY1106871T1 (es)
CZ (1) CZ303808B6 (es)
DE (1) DE60221392T2 (es)
DK (1) DK1397364T3 (es)
DZ (1) DZ3506A1 (es)
EA (1) EA007782B1 (es)
EC (1) ECSP034859A (es)
EG (1) EG25614A (es)
ES (1) ES2289116T3 (es)
HK (1) HK1064375A1 (es)
HR (1) HRP20030961B1 (es)
HU (1) HU228844B1 (es)
IL (2) IL158512A0 (es)
MX (1) MXPA03010630A (es)
MY (1) MY134586A (es)
NO (1) NO326701B1 (es)
NZ (1) NZ528525A (es)
PE (1) PE20030117A1 (es)
PL (1) PL221339B1 (es)
PT (1) PT1397364E (es)
SI (1) SI1397364T1 (es)
SK (1) SK287857B6 (es)
SV (1) SV2003001054A (es)
TW (1) TWI329644B (es)
UA (1) UA76461C2 (es)
WO (1) WO2002094833A1 (es)
ZA (1) ZA200308546B (es)

Families Citing this family (88)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT1397364E (pt) * 2001-05-24 2007-10-22 Lilly Co Eli Novos derivados de pirrole como agentes farmacêuticos
ATE373000T1 (de) * 2001-12-11 2007-09-15 Smithkline Beecham Corp Pyrazolopyridin-derivate als antiherpesmittel
ES2291664T3 (es) 2002-09-17 2008-03-01 Eli Lilly And Company Derivados de pirazolopiridina como inhibidores de la transduccion de señales de tgf beta para el tratamiento del cancer.
WO2004048383A1 (en) * 2002-11-21 2004-06-10 Eli Lilly And Company Mixed lineage kinase modulators
AU2003291642A1 (en) * 2002-11-22 2004-06-18 Eli Lilly And Company Pyrazoloazepine compounds as pharmaceutical agents
UA80571C2 (en) * 2002-11-22 2007-10-10 Lilly Co Eli Quinolinyl-pyrrolopyrazoles
US7405299B2 (en) * 2002-11-27 2008-07-29 Eli Lilly And Company Compounds as pharmaceutical agents
CL2004000234A1 (es) * 2003-02-12 2005-04-15 Biogen Idec Inc Compuestos derivados 3-(piridin-2-il)-4-heteroaril-pirazol sustituidos, antagonistas de aik5 y/o aik4; composicion farmaceutica y uso del compuesto en el tratamiento de desordenes fibroticos como esclerodermia, lupus nefritico, cicatrizacion de herid
US7511065B2 (en) * 2003-11-12 2009-03-31 Eli Lilly And Company Mixed lineage kinase modulators
WO2005092894A1 (en) * 2004-03-01 2005-10-06 Eli Lilly And Company Fused pyrazole derivatives as tgf-beta signal transduction inhibitors for the treatment of fibrosis and neoplasms
TW200639163A (en) * 2005-02-04 2006-11-16 Genentech Inc RAF inhibitor compounds and methods
WO2006103120A2 (en) * 2005-04-01 2006-10-05 Insa Rouen New heterocyclic compounds, their preparation and their use as medicaments, in particular as anti-alzheimer agents
WO2007018818A1 (en) 2005-07-22 2007-02-15 Eli Lilly And Company A pyridin quinolin substituted pyrrolo [1,2-b] pyrazole monohydrate as tgf-beta inhibitor
CA2618377A1 (en) 2005-08-12 2007-02-22 Synta Pharmaceuticals Corp. Pyrazole compounds that modulate hsp90 activity
WO2007076127A2 (en) * 2005-12-22 2007-07-05 Biogen Idec Ma Inc Condensed imidazoles or pyrazoles and their use as transforming growth factor modulators
DE102005061840A1 (de) * 2005-12-23 2007-06-28 Merck Patent Gmbh Triazolderivate
TW200800260A (en) * 2006-05-25 2008-01-01 Synta Pharmaceuticals Corp Method for treating proliferative disorders associated with protooncogene products
PL2083863T3 (pl) 2006-10-03 2015-08-31 Genzyme Corp Przeciwciała przeciwko TGF-beta do stosowania w leczeniu niemowląt obarczonych ryzykiem rozwinięcia się dysplazji oskrzelowo-płucnej
PE20090717A1 (es) * 2007-05-18 2009-07-18 Smithkline Beecham Corp Derivados de quinolina como inhibidores de la pi3 quinasa
US8288375B2 (en) 2007-12-12 2012-10-16 E.I. Du Pont De Nemours And Company Fungicidal bicyclic pyrazoles
EP2373664B1 (en) * 2008-12-19 2013-06-12 Nerviano Medical Sciences S.r.l. Bicyclic pyrazoles as protein kinase inhibitors
EP2419105A4 (en) * 2009-04-17 2012-09-12 Summa Health Systems Llc USE OF TRANSFORMATION OF GROWTH FACTOR B RECEPTOR INHIBITORS TO SUPPRESS OCULAR HEALING
AR081810A1 (es) 2010-04-07 2012-10-24 Bayer Cropscience Ag Piridinilpirazoles biciclicos
EP2560640A1 (en) 2010-04-19 2013-02-27 Synta Pharmaceuticals Corp. Cancer therapy using a combination of a hsp90 inhibitory compounds and a egfr inhibitor
EP2402338A1 (en) 2010-06-29 2012-01-04 Basf Se Pyrazolopyridine compounds
EP2402340A1 (en) 2010-06-29 2012-01-04 Basf Se Pyrazolopyridine compounds
EP2402337A1 (en) * 2010-06-29 2012-01-04 Basf Se Pyrazolopyridine compounds
EP2402339A1 (en) * 2010-06-29 2012-01-04 Basf Se Pyrazolopyridine compounds
EP2401915A1 (en) 2010-06-29 2012-01-04 Basf Se Pyrazolopyridine compounds
US8871744B2 (en) 2010-07-21 2014-10-28 B & G Partyers, LLC Compounds and methods for selectively targeting tumor-associated mucins
WO2012138945A1 (en) 2011-04-08 2012-10-11 Aestus Therapeutics, Inc. Methods of treating schizophrenia with pyrazole derivative inhibitors of tgf - beta
EP2737083A1 (en) 2011-07-27 2014-06-04 INSERM (Institut National de la Santé et de la Recherche Scientifique) Methods for diagnosing and treating myhre syndrome
CA2853484C (en) 2011-10-26 2018-08-21 Seattle Children's Research Institute Cysteamine in the treatment of fibrotic disease
US20140286902A1 (en) 2011-11-02 2014-09-25 Synta Pharmaceuticals Corp. Combination therapy of hsp90 inhibitors with platinum-containing agents
JP2014532712A (ja) 2011-11-02 2014-12-08 シンタ ファーマシューティカルズ コーポレーション トポイソメラーゼi阻害剤とhsp90阻害剤の組合せを使用する癌療法
EP2780010A1 (en) 2011-11-14 2014-09-24 Synta Pharmaceuticals Corp. Combination therapy of hsp90 inhibitors with braf inhibitors
US9782452B2 (en) 2011-11-22 2017-10-10 Cornell University Methods for stimulating hematopoietic recovery by inhibiting TGFβ signaling
JP6449772B2 (ja) 2012-10-05 2019-01-09 カドモン コーポレイション,リミティド ライアビリティ カンパニー ヒト抗vegfr2/kdr抗体
TWI443096B (zh) 2012-12-18 2014-07-01 Ind Tech Res Inst 3-(5-(4-(3-氟丙基)哌嗪-1-基)苯並咪唑-2-基)-1-氮雜薁-2-酮之單水合晶型及其製備方法與藥學組成物
EP2953933A1 (en) * 2013-02-07 2015-12-16 Merck Patent GmbH Substituted acetylene derivatives and their use as positive allosteric modulators of mglur4
KR102168088B1 (ko) 2013-03-14 2020-10-20 더 브리검 앤드 우먼즈 하스피털, 인크. 상피 줄기 세포 확장 및 배양을 위한 조성물 및 방법
US8975417B2 (en) * 2013-05-27 2015-03-10 Novartis Ag Pyrazolopyrrolidine derivatives and their use in the treatment of disease
CA2938311C (en) 2014-02-03 2023-03-07 Vitae Pharmaceuticals, Inc. Dihydropyrrolopyridine inhibitors of ror-gamma
IL299964A (en) 2014-09-03 2023-03-01 Massachusetts Inst Technology Preparations, systems and methods for producing hair cells in the inner ear to treat hearing loss
TWI582083B (zh) 2014-10-07 2017-05-11 美國禮來大藥廠 胺基吡啶基氧基吡唑化合物
US9663515B2 (en) 2014-11-05 2017-05-30 Vitae Pharmaceuticals, Inc. Dihydropyrrolopyridine inhibitors of ROR-gamma
EP3277673B1 (en) 2015-04-01 2022-05-04 Rigel Pharmaceuticals, Inc. Tgf-beta inhibitors
EP3313420B1 (en) 2015-06-25 2024-03-13 The Children's Medical Center Corporation Methods and compositions relating to hematopoietic stem cell expansion, enrichment, and maintenance
US10301261B2 (en) 2015-08-05 2019-05-28 Vitae Pharmaceuticals, Llc Substituted indoles as modulators of ROR-gamma
CN108463458B (zh) 2015-11-20 2022-02-01 生命医药有限责任公司 ROR-γ的调节剂
CA3010610A1 (en) 2016-01-08 2017-07-13 The Brigham And Women's Hospital, Inc. Production of differentiated enteroendocrine cells and insulin producing cells
TW202220968A (zh) 2016-01-29 2022-06-01 美商維它藥物有限責任公司 ROR-γ調節劑
US10213511B2 (en) 2016-03-02 2019-02-26 Frequency Therapeutics, Inc. Thermoreversible compositions for administration of therapeutic agents
US11260130B2 (en) 2016-03-02 2022-03-01 Frequency Therapeutics, Inc. Solubilized compositions for controlled proliferation of stem cells / generating inner ear hair cells using a GSK3 inhibitor: IV
US10201540B2 (en) 2016-03-02 2019-02-12 Frequency Therapeutics, Inc. Solubilized compositions for controlled proliferation of stem cells / generating inner ear hair cells using GSK3 inhibitors: I
WO2017161001A1 (en) 2016-03-15 2017-09-21 Children's Medical Center Corporation Methods and compositions relating to hematopoietic stem cell expansion
CN109415341B (zh) * 2016-06-13 2021-02-26 劲方医药科技(上海)有限公司 作为TGF-βR1抑制剂的苯并三氮唑衍生的α,β不饱和酰胺类化合物
WO2018019106A1 (zh) 2016-07-29 2018-02-01 上海璎黎药业有限公司 含氮芳香杂环化合物、其制备方法、药物组合物和应用
CA3048220A1 (en) 2016-12-30 2018-07-05 Frequency Therapeutics, Inc. 1h-pyrrole-2,5-dione compounds and methods of using them to induce self-renewal of stem/progenitor supporting cells
PL3618829T3 (pl) 2017-05-05 2023-11-20 Arcus Biosciences, Inc. Pochodne chinazolinopirydyny do leczenia zaburzeń związanych z nowotworem
WO2019018975A1 (en) 2017-07-24 2019-01-31 Vitae Pharmaceuticals, Inc. INHIBITORS OF ROR GAMMA
WO2019023207A1 (en) 2017-07-24 2019-01-31 Vitae Pharmaceuticals, Inc. INHIBITORS OF RORƳ
WO2019071147A1 (en) 2017-10-05 2019-04-11 Fulcrum Therapeutics, Inc. INHIBITORS OF KINASE P38 REDUCING EXPRESSION OF DUX4 GENE AND DOWNSTREAM GENES FOR THE TREATMENT OF FSHD
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
MA50356A (fr) 2017-10-11 2021-04-21 Hoffmann La Roche Composés bicycliques destinés à être utilisés en tant qu'inhibiteurs de la kinase rip1
JP2021035911A (ja) * 2017-11-15 2021-03-04 大日本住友製薬株式会社 縮環ピラゾール誘導体及びその医薬用途
BR112020011602A2 (pt) * 2017-12-13 2020-12-08 Genfleet Therapeutics (Shanghai) Inc. Forma cristalina e forma salina de um inibidor tgf-ssri e método de preparação dos mesmos
CN110066276B (zh) 2018-01-24 2020-09-18 上海璎黎药业有限公司 芳香杂环化合物、其中间体、制备方法、药物组合物和应用
CN110066277B (zh) 2018-01-24 2021-07-23 上海璎黎药业有限公司 芳香杂环取代烯烃化合物、其制备方法、药物组合物和应用
US11866427B2 (en) 2018-03-20 2024-01-09 Icahn School Of Medicine At Mount Sinai Kinase inhibitor compounds and compositions and methods of use
WO2019236766A1 (en) 2018-06-06 2019-12-12 Ideaya Biosciences, Inc. Methods of culturing and/or expanding stem cells and/or lineage committed progenitor cells using lactam compounds
CN112867724B (zh) * 2018-07-23 2024-06-04 熙源安健医药(北京)有限公司 二膦酸盐药物缀合物
EP3837352A1 (en) 2018-08-17 2021-06-23 Frequency Therapeutics, Inc. Compositions and methods for generating hair cells by upregulating jag-1
US11617745B2 (en) 2018-08-17 2023-04-04 Frequency Therapeutics, Inc. Compositions and methods for generating hair cells by downregulating FOXO
WO2020088526A1 (zh) * 2018-10-31 2020-05-07 南京明德新药研发有限公司 作为TGF-βR1激酶抑制剂的双环吡唑类化合物
US20220089600A1 (en) * 2018-11-22 2022-03-24 Fundació Institut De Recerca Biomèdica (Irb Barcelona) TGFß INHIBITOR AND PRODRUGS
BR112021007006A2 (pt) 2018-12-27 2021-08-10 Nexys Therapeutics, Inc. derivados de (piridin-2-il)amina como inibidores de tgf-beta r1(alk5) para o tratamento de câncer
US20220162182A1 (en) 2018-12-31 2022-05-26 Icahn School Of Medicine At Mount Sinai Kinase inhibitor compounds and compositions and methods of use
KR20210118891A (ko) 2019-01-24 2021-10-01 지앙수 아오사이캉 파마수티칼 씨오., 엘티디. TGF-β R1 키나아제 억제제로서의 5-(4-피리딜옥시)피라졸 화합물
US20220073494A1 (en) * 2019-01-31 2022-03-10 Kyorin Pharmaceutical Co., Ltd. 15-pgdh inhibitors
US20220177978A1 (en) 2019-04-02 2022-06-09 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods of predicting and preventing cancer in patients having premalignant lesions
CN113557236B (zh) * 2019-06-10 2022-05-10 中国科学院广州生物医药与健康研究院 一种双功能免疫调节剂及其在药学上可接受的盐、药物组合物
EP4087657A1 (en) 2020-01-08 2022-11-16 Synthis Therapeutics, Inc. Alk5 inhibitor conjugates and uses thereof
CN114867723B (zh) * 2020-07-23 2023-05-30 江苏奥赛康药业有限公司 作为TGF-βR1抑制剂的吡啶氧基连吡唑类化合物的盐型、晶型以及其药物组合物
US20230303562A1 (en) 2020-09-28 2023-09-28 Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. Pyrazole compound and preparation method therefor and use thereof
CN115703750B (zh) * 2021-08-17 2024-07-02 黑龙江华瑞生物科技有限公司 一种1-氨基-4-甲基哌嗪的提取纯化方法
CN114249742B (zh) * 2021-11-22 2022-11-01 郑州大学 一种光气探针、荧光书写检测笔及其在光气检测中的应用
CN115969801B (zh) * 2023-03-21 2023-08-25 劲方医药科技(上海)有限公司 用于癌症的药物组合物及其制备方法

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5356897A (en) * 1991-09-09 1994-10-18 Fujisawa Pharmaceutical Co., Ltd. 3-(heteroaryl)-pyrazololi[1,5-a]pyrimidines
ES2130269T3 (es) * 1992-06-17 1999-07-01 Upjohn Co Oximas sustituidas con piridina, pirrolidina y azepina utiles como agentes contra la aterosclerosis y antihipercolesterolemicos.
GB9303993D0 (en) * 1993-02-26 1993-04-14 Fujisawa Pharmaceutical Co New heterocyclic derivatives
WO1995003806A1 (fr) * 1993-07-27 1995-02-09 Kyowa Hakko Kogyo Co., Ltd. Remede contre la maladie de parkinson
US5358947A (en) 1993-09-13 1994-10-25 American Cyanamid Company Angiotensin II receptor blocking 2,3-substituted pyrazolo[1,5-a]-1,3,5-triazin-4(3H)-ones
AUPN419395A0 (en) * 1995-07-17 1995-08-10 Treescope Development Co. Pty. Ltd. Plant protector
FR2746306B1 (fr) * 1996-03-22 1998-04-30 Oreal Compositions de teinture des fibres keratiniques contenant des pyrazolo-azoles ; leur utilisation pour la teinture comme coupleurs, procede de teinture
SK157899A3 (en) 1997-05-22 2000-08-14 Searle & Co Substituted pyrazoles as p38 kinase inhibitors, process for their preparation and pharmaceutical compositions
FR2772379B1 (fr) 1997-12-16 2000-02-11 Oreal Compositions de teinture des fibres keratiniques contenant des pyrazolo-azoles; leur utilisation pour la teinture comme base d'oxydation, procede de teinture; nouveaux pyrazolo-azoles
GB9809869D0 (en) 1998-05-09 1998-07-08 Medical Res Council Inhibition of protein kinases
AU2319100A (en) * 1999-01-28 2000-08-18 Nippon Shinyaku Co. Ltd. Amide derivatives and drug compositions
JP2002541253A (ja) 1999-04-09 2002-12-03 スミスクライン・ビーチャム・コーポレイション トリアリールイミダゾール
JP2003508401A (ja) * 1999-08-27 2003-03-04 アボット・ラボラトリーズ Cox−2阻害薬として有用なスルホニルフェニルピラゾール化合物
GB0007405D0 (en) 2000-03-27 2000-05-17 Smithkline Beecham Corp Compounds
PE20020506A1 (es) 2000-08-22 2002-07-09 Glaxo Group Ltd Derivados de pirazol fusionados como inhibidores de la proteina cinasa
WO2002034716A2 (en) * 2000-10-11 2002-05-02 Merck & Co., Inc. Pyrrolidine modulators of ccr5 chemokine receptor activity
US20040087623A1 (en) 2001-02-02 2004-05-06 Gellibert Francoise Jeanne Pyrazole derivatives against tgf overexpression
PT1397364E (pt) * 2001-05-24 2007-10-22 Lilly Co Eli Novos derivados de pirrole como agentes farmacêuticos
JP2006529006A (ja) * 2003-05-28 2006-12-28 エム アンド ジェイ フィブレテック アー/エス 繊維を空気により敷き詰めるための方法および繊維分配装置
JP4882198B2 (ja) 2003-09-25 2012-02-22 日産自動車株式会社 燃料電池システム

Also Published As

Publication number Publication date
IL158512A0 (en) 2004-05-12
EA007782B1 (ru) 2007-02-27
CN1951939A (zh) 2007-04-25
UA76461C2 (en) 2006-08-15
PE20030117A1 (es) 2003-02-12
JP4519407B2 (ja) 2010-08-04
HUP0400451A2 (hu) 2004-12-28
NO326701B1 (no) 2009-02-02
JP2004535404A (ja) 2004-11-25
SV2003001054A (es) 2003-03-18
NO20035193D0 (no) 2003-11-21
NO20035193L (no) 2003-11-21
IL158512A (en) 2009-07-20
DZ3506A1 (fr) 2002-11-28
MXPA03010630A (es) 2004-03-09
CY1106871T1 (el) 2012-09-26
CZ20033128A3 (cs) 2004-06-16
ATE368041T1 (de) 2007-08-15
SK14162003A3 (en) 2004-11-03
EP1397364B1 (en) 2007-07-25
TWI329644B (en) 2010-09-01
PL221339B1 (pl) 2016-03-31
US20040106604A1 (en) 2004-06-03
EA200301289A1 (ru) 2004-06-24
DE60221392D1 (de) 2007-09-06
DK1397364T3 (da) 2007-11-26
HU228844B1 (en) 2013-06-28
DE60221392T2 (de) 2008-04-17
CA2446820A1 (en) 2002-11-28
EP1397364A1 (en) 2004-03-17
MY134586A (en) 2007-12-31
NZ528525A (en) 2005-10-28
JP2009197016A (ja) 2009-09-03
CZ303808B6 (cs) 2013-05-09
PT1397364E (pt) 2007-10-22
CN1269820C (zh) 2006-08-16
SK287857B6 (sk) 2012-01-04
SI1397364T1 (sl) 2007-12-31
BR0209939A (pt) 2004-03-30
KR20030097895A (ko) 2003-12-31
ECSP034859A (es) 2004-01-28
ZA200308546B (en) 2005-04-26
HUP0400451A3 (en) 2008-08-28
AR036034A1 (es) 2004-08-04
AU2002339268B2 (en) 2007-05-31
HRP20030961B1 (en) 2012-01-31
EG25614A (en) 2012-03-22
WO2002094833A1 (en) 2002-11-28
CO5540282A2 (es) 2005-07-29
US7087626B2 (en) 2006-08-08
HRP20030961A2 (en) 2005-08-31
CN1511157A (zh) 2004-07-07
HK1064375A1 (en) 2005-01-28
CA2446820C (en) 2010-07-13
KR100861630B1 (ko) 2008-10-07
PL367199A1 (en) 2005-02-21

Similar Documents

Publication Publication Date Title
ES2289116T3 (es) Nuevos derivados de pirrol como agentes farmaceuticos.
RS20050469A (en) Pyrrolopyrimidine derivatives
EP1248612A4 (en) NEW SUBSTANCES AND COMPOUNDS AS PROTEASE INHIBITORS
AU2009258496A8 (en) Sulfur-containing heterocyclic derivative having beta-secretase-inhibiting activity
WO2006106423A8 (en) Amino sulfonyl derivatives as inhibitors of human 11-.beta.-hydrosysteroid dehydrogenase
TW200745029A (en) Sulfonamide derivatives exhibiting PGD2 receptor antagonism
ZA200609261B (en) Fused quinoline derivative and use thereof
CO6251368A2 (es) Derivados de (1)-2- dihidro-4h, 9h-imidazo[1, 2, 3-ij]-1, 8- naftiridina-4,9-diona o 1, 2-dihidro-3h, 8h-2a,5, 8a- triazaacenaphtileno-3, 8- diona utiles como antibacterianos
ZA200610122B (en) 3-(heteroaryl-oxy)-2-alkyl-1-aza-bicycloalkyl derivatives as alpha.7-NACHR ligands for the treatment of CNS diseases
EA200501265A1 (ru) Производные пиримидина для профилактики вич-инфекции
TR200401962T4 (tr) Heteroaromatik karboksamid türevleri ve bunların IKK-2 enziminin inhibitörleri olarak kullanımı
RS52865B (en) Phenyl-piperazine Derivatives As Serotonin Resorption Inhibitors
NO331068B1 (no) Benzazepinderivater for behandling av nevrologiske forstyrrelser.
DK1625126T3 (da) Imidazo- og thiazolopyridiner som JAK3-kinaseinhibitorer
EA200702498A1 (ru) N-(пиридин-2-ил)сульфонамидные производные
AR042658A1 (es) Derivados de 1,5-diaril-pirrol-3-carboxamida y su uso como moduladores de receptores canabinoides
CO5690551A2 (es) Derivados de tetrazol y metodos para el tratamiento con los mismos de trastornos relacionados con el metabolismo
EA200700901A1 (ru) Производные 2-амидо-4-фенилтиазола, их получение и применение в терапии
AP1564A (en) Piperazinyl sulfonic acid derivatives, their pharmaceutical compositions and methods of use.
AR044830A1 (es) Derivados de 4,5 diaril -3-heterociclilpirazin- 2- ester
EP2205088A4 (en) NAPHTHALIN-BASED INHIBITORS OF ANTI-APOPTOTIC PROTEINS
TN2009000109A1 (en) New benzamide derivatives as brad ykinin antagonists
AR050250A1 (es) Derivados de tetrahidroisoquinolilsulfonamidas, su preparacion y su utilizacion en terapeutica
NO20080563L (no) Pyrazol[3,4-d]azepinderivater som histamin H3 antagonister
EP1535922A4 (en) PYRROLOPYRIDINE DERIVATIVE AND ITS USE