AR059246A1 - Compuestos heterobiciclicos de tiofeno y metodos de uso - Google Patents

Compuestos heterobiciclicos de tiofeno y metodos de uso

Info

Publication number
AR059246A1
AR059246A1 ARP070100391A ARP070100391A AR059246A1 AR 059246 A1 AR059246 A1 AR 059246A1 AR P070100391 A ARP070100391 A AR P070100391A AR P070100391 A ARP070100391 A AR P070100391A AR 059246 A1 AR059246 A1 AR 059246A1
Authority
AR
Argentina
Prior art keywords
nr10r11
aryl
alkyl
cr14r15
heteroaryl
Prior art date
Application number
ARP070100391A
Other languages
English (en)
Original Assignee
Array Biopharma Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Array Biopharma Inc filed Critical Array Biopharma Inc
Publication of AR059246A1 publication Critical patent/AR059246A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • 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
    • 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
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P25/06—Antimigraine agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—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
    • 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/04—Immunostimulants
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic 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
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • 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
    • A61P9/08—Vasodilators for multiple indications
    • 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
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Abstract

Compuesto de formula (1) y sus sales farmacéuticamente aceptables, que son utiles para inhibir las quirosin quinasas receptoras y para tratar trastornos intermediados por éstas. Se describen métodos de uso de los compuestos de formula (1) y sus sales farmacéuticamente aceptables para el diagnostico, prevencion o tratamiento in vitro, in situ e in vivo de dichos trastornos en células de mamíferos o trastornos patologicos asociados. Reivindicacion 1: Un compuesto seleccionado de la formula (1), y sus sales farmacéuticamente aceptables, donde: X es O, S o NR10; Z2 y Z3 están independientemente seleccionados entre CR4 y N, donde unicamente uno de Z2 y Z3 es N; R1 es H, alquilo C1-12, alquenilo C2-8, alquinilo C2-8, -C(=O)NR10R11, N- (CR14R15)tNR10R11, -NR10C(=Y)R11, -NR10C(=Y)OR11, -NR12C(=Y)NR10R11, o -NR12SO2NR10R11, o R1 es un carbociclilo C3-12, heterociclilo C2-20, arilo C6-20 o heteroarilo C1-20 monocíclico o bicíclico, donde dichos alquilo, alquenilo, alquinilo, carbociclilo, heterociclilo, arilo y heteroarilo están sustituidos opcionalmente con uno o más grupos seleccionados independientemente entre F, CI, Br, I, CN, CF3, oxo, OR10, SR10, -C(=Y)R10, -C(=Y)OR10, -C(=Y)NR10R11, -(CR14R15)n-NR10R11, - NR10C(=Y)R13, -NR10C(=Y)OR11, --NR12C(=Y)NR10R11, -NR12SO2R10, -OC(=Y)R10, -OC(=Y)OR10, -OC(=Y)NR10R11, -OS(O)2(OR10), -OP(=Y)(OR10)(OR11), -OP(OR10)(OR11), -S(O)R10, -S(O)2R10, -S(O)2NR10R11, -S(O)(OR10), -S(O)2(OR10), -SC(=Y)R10, -SC(=Y)OR10, - SC(=Y)NR10R11, alquilo C1-12, alquenilo C2-8, alquinilo C2-8, cicloalquilo C3-12, heterociclilo C2-20, arilo C6-20 y heteroarilo C1-20, -(CR14R15)n-NR12C(=O)(CR14R15)mNR10R11, y -C(O)(CR14R15)nNR10R11; R2 y R4 son independientemente H, F, CI, Br, I, CN, -C(=Y)R10, -C(=Y)OR10, -C(=Y)NR10R11, -NR10R11, -NR10C(=Y)R11, -NR10C(=Y)OR11, -NR12C(=Y)NR10R11, -NR12SO2R10R11, -OR10, -OC(=Y)R10, -OC(=Y)OR10, -OC(=Y)NR10R11, -C(=O)NR12(CR14R15)tNR10R11, -OP(=Y)(OR10)(OR11), -OP(OR10)(OR11), -SR10, -S(O)R10, -S(O)2R10, -S(O)2NR10R11, -SC(=Y)R10, -SC(=Y)OR10, alquilo C1-12, alquenilo C2-8, alquinilo C2-8, carbociclilo C3-12, heterociclilo C2-20, arilo C6-20, o heteroarilo C1-20, donde dichos alquilo, alquenilo, alquinilo, carbociclilo, heterociclilo, arilo, y heteroarilo están sustituidos opcionalmente con uno o más grupos seleccionados independientemente entre F, CI, Br, I, OR10, y NR10R11; R3 es un carbociclilo C3-12, heterociclilo C2-20, arilo C6-20 o heteroarilo C1-20 monocíclicos o bicíclicos, donde dichos carbociclilo, heterociclilo, arilo y heteroarilo están sustituidos opcionalmente con uno o más grupos seleccionados independientemente entre F, CI, Br, I, CN, CF3, OR10, SR10, -C(=Y)R10, -C(=Y)OR10, -C(=Y)NR10R11, -NR10R11, - NR10C(=Y)R13, -NR10C(=Y)OR11, -NR12C(=Y)NR10R11, -NR12C(=Y)NR10R11, -NR12C(=O)C(=O)R10R11, -NR12C(=O)C(=O)NR10R11, -NR12C(=O)C(=O)Ora, -NR12SO2R10, -NR12C(=Y1)(CR14R15)nC(=Y2)NR10R11, -NR12C(=Y1)NR10C(=Y2)(CR14R15)nR11, - NR12C(=Y1)(CR14R15)nC(=Y2)(CR14R15)mR10, -OC(=Y)R10, -OC(=Y)OR10, -OC(=Y)NR10R11, -OS(O)2(OR10), -OP(=Y)(OR10)(OR11), -OP(OR10)(OR11), -S(O)R10, -S(O)2R10, -S(O)2NR10R11, -S(O)(OR10), -S(O)2(OR10), -SC(=Y)R10, -SC(=Y)OR10, -SC(=Y)NR10R11, alquilo C1- 12, alquenilo C2-8, alquinilo C2-8, cicloalquilo C3-12, heterociclilo C2-20, arilo C6-20 y heteroarilo C1-20, donde dichos alquilo, alquenilo, alquinilo, cicloalquilo, heterociclilo, arilo, y heteroarilo están sustituidos opcionalmente con uno o más grupos seleccionados independientemente entre F, CI, Br, I, OH, alquilo C1-12, oxo, NR10R11, -C(=Y)NR10R11 y(CR14R15)n-arilo; R10, R11 y R12 son independientemente H, ORa, alquilo C1-12, alquenilo C2-8, o alquinilo C2-8, o carbociclilo C3-12, heterociclilo C2-20, arilo C6-20, o heteroarilo C1-20 monocíclicos o bicíclicos donde dichos alquilo, alquenilo, alquinilo, carbociclilo, heterociclilo, arilo, y heteroarilo están sustituidos opcionalmente con uno o más grupos seleccionados independientemente entre F, CI, Br, I, SO2RC, CN, ORa, NRaRb, C(=O)NRaRb, CRaC(=O)Rb, alquilo C1-12, alquenilo C2-8, alquinilo C2-8, carbociclilo C3-20, arilo C6-20, y heteroarilo C1-20, o R10 y R11 conjuntamente con el nitrogeno al cual están unidos forman opcionalmente un anillo heterocíclico C3-20 saturado, parcialmente insaturado o totalmente insaturado que contiene opcionalmente uno o más átomos de anillos adicionales seleccionados entre N, O o S, donde dicho anillo heterocíclico está sustituido opcionalmente con uno o más grupos seleccionados independientemente entre oxo, ORa NRaRb, CF3, F, CI, Br, I, SO2Ra, C(=O)Ra, NR10C(=Y)R11, C(=Y)NR10R11, alquilo C1-12, alquenilo C2-8, alquinilo C2-8, cicloalquilo C3-12, heterociclilo C2-20, arilo C6-20 y heteroarilo C1-20, R13 es H, alquilo C1-12, alquenilo C2-8, alquinilo C2-8, (CR14R15)n-cicloalquilo, -(CR14R15)n-heterocicliIo, (CR14R15)n-arilo, (CR14R15)n-heteroarilo, (CR14R15)n-O-(CR14R15)m-arilo, (CR14R15)n-OR10, (CR14R15)n- NR10R11, (CR14R15)n-NR10C(=O)R11, o (CR14R15)n-NR10(SO2Me)-R11, donde dichas porciones alquilo, alquenilo, alquinilo, cicloalquilo, heterocicloalquilo, y heteroarilo están sustituidas opcionalmente con uno o más grupos seleccionados independientemente entre F, CI, Br, I, oxo, SO2RC, CN, ORa, C(=O)Ra, C(=O)ORa, NRaRb, NRaC(=O)Rb, alquilo C1-12, alquenilo C2-8, alquinilo C2-8, cicloalquilo C3-12, heterociclilo C2-20, arilo C6-20, y heteroarilo C1-20; R14 y R15 son independientemente H, alquilo C1-12, o (CR14R15)tariIo, o R14 y R15 conjuntamente con los átomos a los cuales están unidos forman un anillo carbocíclico C3-12 saturado o parcialmente insaturado; o R10 y R15 conjuntamente con los átomos a los cuales están unidos forman un anillo heterocíclico C1-20 saturado o parcialmente insaturado que está opcionalmente sustituido con uno o más grupos seleccionados independientemente entre F, CI, Br, I, ORa, alquilo C1-12, alquenilo C2-8, alquinilo C2-8, cicloalquilo C3-12, heterociclilo C2-20, arilo C6-20, y heteroarilo C1-20, donde dichos alquilo y arilo están sustituidos opcionalmente con uno o más grupos seleccionados independientemente entre F, CI, Br, y I, o R14 es nulo y R10 y R15 conjuntamente con los átomos a los cuales están unidos forman un anillo heteroarilo C1-20 que tiene uno o más heteroátomos; Ra y Rb son independientemente H, alquilo C1-12, alquenilo C2-8, alquinilo C2-8, carbociclilo C3-12, heterociclilo C2-20, arilo C6-20, o heteroarilo C1-20, donde dichos alquilo, alquenilo, alquinilo, carbociclilo, heterociclilo, arilo, y heteroarilo están sustituidos opcionalmente con uno o más grupos alquilo o halogeno; Rc es alquilo C1-12 o arilo C6-20, donde dichos alquilo y arilo están sustituidos opcionalmente con uno o más grupos seleccionados independientemente entre F, CI, Br, I, ORa y C(=O)NRaRb; Y, Y1 y Y2 son independientemente O o S; t es 1,2,3,4,5 o 6;y n y m son independientemente 0, 1, 2, 3, 4, 5 o 6.
ARP070100391A 2006-01-30 2007-01-30 Compuestos heterobiciclicos de tiofeno y metodos de uso AR059246A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US76341406P 2006-01-30 2006-01-30

Publications (1)

Publication Number Publication Date
AR059246A1 true AR059246A1 (es) 2008-03-19

Family

ID=39272752

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP070100391A AR059246A1 (es) 2006-01-30 2007-01-30 Compuestos heterobiciclicos de tiofeno y metodos de uso

Country Status (8)

Country Link
US (1) US8003662B2 (es)
EP (1) EP1989211A2 (es)
JP (1) JP2009526761A (es)
CN (1) CN101522687A (es)
AR (1) AR059246A1 (es)
CA (1) CA2636242A1 (es)
TW (1) TW200806675A (es)
WO (1) WO2008063202A2 (es)

Families Citing this family (38)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2003201573B2 (en) * 2002-01-22 2009-02-26 Biomatera Inc. Method of drying biodegradable polymers
AU2006229343A1 (en) * 2005-03-28 2006-10-05 Kirin Pharma Kabushiki Kaisha Thienopyridine derivative, or quinoline derivative, or quinazoline derivative, having c-Met autophosphorylation inhibiting potency
CA2608726C (en) 2005-05-20 2013-07-09 Methylgene Inc. Inhibitors of vegf receptor and hgf receptor signaling
EP1957498B1 (en) * 2005-05-20 2017-02-15 MethylGene Inc. Inhibitors of vegf receptor and hgf receptor signaling
AU2007240568A1 (en) * 2006-04-21 2007-11-01 Amgen Inc. Thieno-[2,3-d]pyrimidine and thieno-pyridazine compounds and methods of use
US20110053931A1 (en) * 2006-06-08 2011-03-03 John Gaudino Quinoline compounds and methods of use
JP5642963B2 (ja) * 2006-06-30 2014-12-17 スネシス ファーマシューティカルズ，インコーポレイティド ピリジノニルｐｄｋ１阻害剤
AU2008236670B2 (en) * 2007-04-05 2011-12-01 Amgen Inc. Aurora kinase modulators and method of use
US8907091B2 (en) 2007-08-29 2014-12-09 Methylgene Inc. Processes and intermediates for preparing fused heterocyclic kinase inhibitors
CA2697795C (en) * 2007-08-29 2016-08-16 Methylgene Inc. Thieno[3,2,b]pyridinyl compounds as inhibitors of protein tyrosine kinase activity
CN101977905B (zh) 2008-01-23 2014-07-02 百时美施贵宝公司 4-吡啶酮化合物及其对于癌症的用途
JPWO2009110415A1 (ja) 2008-03-03 2011-07-14 武田薬品工業株式会社 併用剤
CA2717816A1 (en) * 2008-03-05 2009-09-11 Tetsuyuki Uno Inhibitors of protein tyrosine kinase activity
EP2257293A2 (en) * 2008-03-06 2010-12-08 Genentech, Inc. Combination therapy with c-met and egfr antagonists
TW201000099A (en) 2008-06-20 2010-01-01 Amgen Inc S1P1 receptor agonists and use thereof
MX2011004018A (es) * 2008-10-14 2011-06-24 Ning Xi Compuestos y metodos de uso.
MX2011011326A (es) * 2009-04-27 2012-02-13 Elan Pharm Inc Antagonistas de piridinona de las integrinas alfa-4.
CA2762680C (en) 2009-05-21 2018-04-17 Chlorion Pharma, Inc. Methyl sulfanyl pyrmidmes useful as antiinflammatories, analgesics, and antiepileptics
MX2012002596A (es) * 2009-09-03 2012-07-03 Allergan Inc Compuestos como moduladores de tirosina cinasas.
US9340555B2 (en) 2009-09-03 2016-05-17 Allergan, Inc. Compounds as tyrosine kinase modulators
US8258158B2 (en) * 2009-09-11 2012-09-04 Hoffmann-La Roche Inc. HSL inhibitors useful in the treatment of diabetes
JP5795630B2 (ja) 2010-04-29 2015-10-14 デシフェラ ファーマシューティカルズ，エルエルシー 抗癌及び抗増殖活性を示すシクロプロピルジカルボキサミド及び類似体
WO2011139891A1 (en) 2010-04-29 2011-11-10 Deciphera Pharmaceuticals, Llc Pyridone amides and analogs exhibiting anti-cancer and anti-proliferative activites
TW201204733A (en) * 2010-06-25 2012-02-01 Kowa Co Novel condensed pyridine or condensed pyrimidine derivative, and medicinal agent comprising same
EP4238566A1 (en) 2012-05-02 2023-09-06 Georgetown University Treating amyotrophic lateral sclerosis with tyrosine kinase inhibitors
WO2014038881A2 (ko) * 2012-09-06 2014-03-13 씨제이제일제당 (주) 피리돈 유도체를 포함하는 단백질 키나제 억제제
US9574135B2 (en) * 2013-08-22 2017-02-21 Nanoco Technologies Ltd. Gas phase enhancement of emission color quality in solid state LEDs
BR112016021383A2 (pt) 2014-03-24 2017-10-03 Genentech Inc Método para identificar um paciente com câncer que é susceptível ou menos susceptível a responder ao tratamento com um antagonista de cmet, método para identificar um paciente apresentando câncer previamente tratado, método para determinar a expressão do biomarcador hgf, antagonista anti-c-met e seu uso, kit de diagnóstico e seu método de preparo
WO2015162515A1 (en) 2014-04-25 2015-10-29 Pfizer Inc. Heteroaromatic compounds and their use as dopamine d1 ligands
US20190262323A1 (en) * 2016-10-31 2019-08-29 Georgetown University Compositions and methods for treating neurodegenerative disorders
EA039189B1 (ru) 2017-05-11 2021-12-15 Бристол-Маерс Сквибб Компани Тиенопиридины и бензотиофены в качестве ингибиторов irak4
CN109206435B (zh) * 2017-06-29 2020-09-08 中国医药研究开发中心有限公司 噻吩并[3,2-d]嘧啶类化合物及其制备方法和医药用途
US11447500B2 (en) 2018-03-08 2022-09-20 Wellmarker Bio Co., Ltd. Thienopyridine derivatives and pharmaceutical composition comprising same
WO2021025407A1 (ko) * 2019-08-02 2021-02-11 웰마커바이오 주식회사 옥소-피리딘 융합고리 유도체 및 이를 포함하는 약학적 조성물
KR20220059386A (ko) * 2019-09-06 2022-05-10 웰마커바이오 주식회사 바이오마커 기반 치료용 조성물
JP7434575B2 (ja) 2020-01-07 2024-02-20 メッドシャイン ディスカバリー インコーポレイテッド 重水素化チエノピリジン系化合物
CN115745999A (zh) * 2021-11-19 2023-03-07 浙江奥洋新材料有限公司 一种可提高反应活性的纤维素碱性醚化、酯化反应溶剂叔丁五元二环胍的结构及其合成路线
CN115177618A (zh) * 2022-07-26 2022-10-14 广州市第一人民医院（广州消化疾病中心、广州医科大学附属市一人民医院、华南理工大学附属第二医院） Flt3抑制剂在制备治疗急性髓系白血病药物中的应用

Family Cites Families (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1280580A (zh) * 1997-11-11 2001-01-17 辉瑞产品公司 用作抗癌药的噻吩并嘧啶和噻吩并吡啶衍生物
ATE277933T1 (de) * 2000-06-06 2004-10-15 Pfizer Prod Inc Thiophenverbindungen zur verwendung als antikrebsmittel
US20020004511A1 (en) * 2000-06-28 2002-01-10 Luzzio Michael Joseph Thiophene derivatives useful as anticancer agents
WO2003000194A2 (en) * 2001-06-21 2003-01-03 Pfizer Inc. Thienopyridine and thienopyrimidine anticancer agents
DE60233736D1 (de) * 2001-06-22 2009-10-29 Kirin Pharma K K Chinolinderivat und chinazolinderivat, die die selbstphosphorylierung des hepatocytus-proliferator-rezeptors hemmen, und diese enthaltende medizinische zusammensetzung
AU2002357193A1 (en) * 2001-12-19 2003-07-09 Smithkline Beecham Corporation Thienopyrimidine compounds as protein tyrosine kinase inhibitors
MXPA04008403A (es) * 2002-03-01 2004-11-26 Pfizer Indolil-urea derivados de tienopiridinas utiles como agentes antiangiogenicos, y procedimientos para su uso.
UA77303C2 (en) * 2002-06-14 2006-11-15 Pfizer Derivatives of thienopyridines substituted by benzocondensed heteroarylamide useful as therapeutic agents, pharmaceutical compositions and methods for their use
US7560558B2 (en) 2002-08-23 2009-07-14 Kirin Beer Kabushiki Kaisha Compound having TGFβ inhibitory activity and medicinal composition containing the same
CL2003002287A1 (es) * 2002-11-25 2005-01-14 Wyeth Corp COMPUESTOS DERIVADOS DE TIENO[3,2-b]-PIRIDINA-6-CARBONITRILOS Y TIENEO[2,3-b]-PIRIDINA-5-CARBONITRILOS, COMPOSICION FARMACEUTICA, PROCEDIMIENTO DE PREPARACION Y COMPUESTOS INTERMEDIARIOS, Y SU USO EN EL TRATAMIENTO DEL CANCER, APOPLEJIA, OSTEOPOROSIS
CA2536788A1 (en) * 2003-08-29 2005-03-10 Pfizer Inc. Naphthalene carboxamides and their derivatives useful as new anti-angiogenic agents
JP2007504122A (ja) * 2003-08-29 2007-03-01 ファイザー・インク 新規抗血管形成剤として有用なチエノピリジン−フェニルアセトアミドおよびその誘導体
ATE517091T1 (de) * 2003-09-26 2011-08-15 Exelixis Inc C-met-modulatoren und verwendungsverfahren
WO2005080377A1 (ja) * 2004-02-20 2005-09-01 Kirin Beer Kabushiki Kaisha TGFβ阻害活性を有する化合物およびそれを含んでなる医薬組成物
US7459562B2 (en) * 2004-04-23 2008-12-02 Bristol-Myers Squibb Company Monocyclic heterocycles as kinase inhibitors
TW200538453A (en) 2004-04-26 2005-12-01 Bristol Myers Squibb Co Bicyclic heterocycles as kinase inhibitors
WO2005121125A1 (en) * 2004-06-09 2005-12-22 Pfizer Inc. Ether-linked heteroaryl compounds
JP5368701B2 (ja) 2004-07-02 2013-12-18 エクセリクシス、インコーポレイテッド ｃ−Ｍｅｔモジュレーター及び使用方法
EP1781664B1 (en) * 2004-07-30 2013-09-04 MethylGene Inc. Inhibitors of vegf receptor and hgf receptor signaling
MX2007006230A (es) * 2004-11-30 2007-07-25 Amgen Inc Quinolinas y analogos de quinazolinas y su uso como medicamentos para tratar cancer.
AU2006229343A1 (en) * 2005-03-28 2006-10-05 Kirin Pharma Kabushiki Kaisha Thienopyridine derivative, or quinoline derivative, or quinazoline derivative, having c-Met autophosphorylation inhibiting potency
US20080161305A1 (en) 2005-04-06 2008-07-03 Exelixis, Inc. C-Met Modulators and Methods of Use
JO2787B1 (en) 2005-04-27 2014-03-15 امجين إنك, Alternative amide derivatives and methods of use
CA2608726C (en) * 2005-05-20 2013-07-09 Methylgene Inc. Inhibitors of vegf receptor and hgf receptor signaling
EP1957498B1 (en) * 2005-05-20 2017-02-15 MethylGene Inc. Inhibitors of vegf receptor and hgf receptor signaling
US7732613B2 (en) * 2005-09-14 2010-06-08 Bristol-Myers Squibb Company Met kinase inhibitors
US7998978B2 (en) * 2006-05-01 2011-08-16 Pfizer Inc. Substituted 2-amino-fused heterocyclic compounds
WO2008054674A2 (en) 2006-10-31 2008-05-08 Merck & Co., Inc. Antidiabetic bicyclic compounds

Also Published As

Publication number Publication date
US8003662B2 (en) 2011-08-23
CA2636242A1 (en) 2008-05-29
EP1989211A2 (en) 2008-11-12
WO2008063202A2 (en) 2008-05-29
JP2009526761A (ja) 2009-07-23
TW200806675A (en) 2008-02-01
WO2008063202A3 (en) 2009-01-22
US20070197537A1 (en) 2007-08-23
CN101522687A (zh) 2009-09-02

Similar Documents

Publication Publication Date Title
AR059246A1 (es) Compuestos heterobiciclicos de tiofeno y metodos de uso
AR059887A1 (es) Compuestos pirazolicos heterobiciclicos, composiciones farmaceuticas que los contienen, y usos en trastornos hiperproliferativos, tales como cancer
AR060632A1 (es) Compuestos inhibidores de fosfoinositida 3- quinasa y metodos de uso
AR050788A1 (es) Compuestos de aminoheteroarilo enantiomericamente puros como inhibidores de proteina quinasa
PE20190509A1 (es) 3-oxo-2,6-difenil-2,3-dihidropiridazin-4-carboxamidas
AR053728A1 (es) Pirimidinas condensadas como agonistas del receptor de acido nicotinico para el tratamiento de dislipidemia y composiciones farmaceuticas que las contienen en combinacion con otros agentes terapeuticos
PE20110028A1 (es) Derivados de isoxazol y su uso como potenciadores de los receptores metabotropicos de glutamato
PE20091204A1 (es) Derivados de 2-aminoquinolina como antagonistas del receptor de 5-ht5a
PE20210040A1 (es) Moduladores de la via de estres integrada
CO5011121A1 (es) Derivados de isotiazol utiles como agentes anticancerosos
AR067093A1 (es) N-(2-(hetaril) arilsulfonamidas y n-(2-( heteraril) hetaril) arilsulfonamidas
PE20061298A1 (es) Compuestos derivados de dihidrobenzofurano como agonistas del receptor de serotonina 5-ht2c
PE20090493A1 (es) DERIVADOS DE LA 6-CICLOAMINO-3-(PIRIDAZIN-4-IL)IMIDAZO[1,2-b]-PIRIDAZINA, SU PREPARACION Y SU APLICACION EN TERAPEUTICA
AR052682A1 (es) DERIVADOS DE 5, 6, 7, 8 - TETRAHIDROTIEN[2, 3 - B]QUINOLINA uTILES PARA INHIBIR LA ACTIVIDAD DE QUINESINA DE KSP, COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN Y SU USO EN EL TRATAMIENTO DE ENFERMEDADES PROLIFERATIVAS.
AR050529A1 (es) Compuestos de aminoheteroarilo sustituidos con pirazol como inhibidores de proteina quinasa
AR050274A1 (es) Derivados triciclicos del indeno-pirrol como moduladores de la serotonina
PE20070016A1 (es) Compuestos heterociclicos n-enlazados como antagonistas del receptor p2y1
PE20091068A1 (es) Compuestos pirrolo[3,2-d]pirimidina y su uso como inhibidores de quinasa pi3 y quinasa mtor
PE20060185A1 (es) ANTAGONISTA DEL RECEPTOR A2A DE LA ADENOSINA CON ESTRUCTURA DE PIRAZOLO--[4,3-e]-1,2,4-TRIAZOLO-[1,5-c]-PIRIMIDINA
PE20061367A1 (es) Nuevos derivados del fluoreno y composiciones que los contienen
AR064155A1 (es) Compuestos de inhibidores de fosfoinositido-3 quinasa y metodos de uso
AR049319A1 (es) Derivados de 6-heteroarilfenantridinas
AR068898A1 (es) Compuestos de tienopirimidinas y pirazolopirimidina y su uso como inhibidores de mtor y pi3k
PE20060604A1 (es) Derivados del tetrahidronaftaleno como agentes antiinflamatorios y procedimiento para su preparacion
PE20090714A1 (es) Imidazopiridazinas y pirrolo-pirimidinas sustituidas como inhibidores de cinasa de lipido

Legal Events

Date Code Title Description
FB Suspension of granting procedure