PE20070978A1 - COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks) - Google Patents

COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks)

Info

Publication number
PE20070978A1
PE20070978A1 PE2007000145A PE2007000145A PE20070978A1 PE 20070978 A1 PE20070978 A1 PE 20070978A1 PE 2007000145 A PE2007000145 A PE 2007000145A PE 2007000145 A PE2007000145 A PE 2007000145A PE 20070978 A1 PE20070978 A1 PE 20070978A1
Authority
PE
Peru
Prior art keywords
pyridin
amino
pi3ks
phosphatidylinositol
kinases
Prior art date
Application number
PE2007000145A
Other languages
English (en)
Inventor
Zhi-Jie Ni
Sabina Pecchi
Matthew Burger
Wooseok Han
Aaron Smith
Gordana Atallah
Sarah Bartulis
Kelly Frazier
Joelle Verhagen
Yanchen Zhang
Ed Iwanowicz
Tom Hendrickson
Mark Knapp
Hanne Merritt
Charles Voliva
Marion Wiesmann
Darren Mark Legrand
Ian Bruce
James Dale
Jiong Lan
Barry Levine
Abran Costales
Jie Liu
Teresa Pick
Daniel Menezes
Original Assignee
Novartis Ag
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 Novartis Ag filed Critical Novartis Ag
Publication of PE20070978A1 publication Critical patent/PE20070978A1/es

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    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • 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
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • AHUMAN NECESSITIES
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    • A61P17/06Antipsoriatics
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    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • 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
    • A61P3/04Anorexiants; Antiobesity agents
    • 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
    • A61P31/04Antibacterial agents
    • 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
    • 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
    • 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
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • 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

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

Abstract

SE REFIERE A COMPUESTOS DE FORMULA (I) DONDE Q ES O U S; X ES CR3 O N; W ES C O N; V ES CR2, O U S; L1 ES CR9 O N, DONDE R2, R3, R7 Y R9 SON CADA UNO H, ALQUIL(C1-C10), ALQUENIL(C2-C6), ALCOXI(C1-C10), CICLOALQUIL(C3-C10), ENTRE OTROS; L2 ES CR6 O N, DONDE R4, R5 Y R6 SON CADA UNO H, HALOGENO, CN, NITRO, AMINO, ENTRE OTROS; R1 ES H, ALQUIL(C1-C10), ALCOXI(C1-C10), ARIL(C6-C14), CICLOALQUIL(C3-C10), ENTRE OTROS; R8 ES H, ALQUIL(C1-C10), CICLOALQUIL(C3-C7), ENTRE OTROS. SON COMPUESTOS PREFERIDOS: N-(6-(6-AMINO-5-(TRIFLUOROMETIL)PIRIDIN-3-IL)IMIDAZO[1.2-b]PIRIDAZIN-2-IL)ACETAMIDA, METIL 6-(6-AMINO-5-(TRIFLUOROMETIL)PIRIDIN-3-IL)IMIDAZO[1.2-a]PIRIDIN-2-ILCARBAMATO, N-(6-(6-AMINO-5-(TRIFLUOROMETIL)PIRIDIN-3-IL)-3-BROMO-IMIDAZO[1.2-a]PIRIDIN-2-IL)ACETAMIDA, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks) SIENDO UTILES EN EL TRATAMIENTO DE GLIOMA, MELANOMA, ASMA, FIBROSIS PULMONAR, PSORIASIS, DERMATITIS
PE2007000145A 2006-02-14 2007-02-12 COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks) PE20070978A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US77347606P 2006-02-14 2006-02-14
US87672906P 2006-12-22 2006-12-22

Publications (1)

Publication Number Publication Date
PE20070978A1 true PE20070978A1 (es) 2007-11-15

Family

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PE2007000145A PE20070978A1 (es) 2006-02-14 2007-02-12 COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks)

Country Status (13)

Country Link
US (1) US20100075965A1 (es)
EP (1) EP1989201A1 (es)
JP (1) JP2009530233A (es)
KR (1) KR20080112202A (es)
AR (1) AR059506A1 (es)
AU (1) AU2007214462A1 (es)
BR (1) BRPI0707816A2 (es)
CA (1) CA2642738A1 (es)
MX (1) MX2008010397A (es)
PE (1) PE20070978A1 (es)
RU (1) RU2008136783A (es)
TW (1) TW200804379A (es)
WO (1) WO2007095588A1 (es)

Families Citing this family (133)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20090163600A1 (en) 2006-03-30 2009-06-25 Hiroshi Maeda Anti-Inflammatory Agent and Cancer-Preventive Agent Comprising Canolol or Prodrug Thereof and Pharmaceutical, Cosmetic and Food Comprising the Same
US20100029619A1 (en) * 2006-08-04 2010-02-04 Takeda Pharmaceutical Company Limted Fused heterocyclic compound
JP5336375B2 (ja) 2006-08-30 2013-11-06 セルゾーム リミテッド キナーゼ阻害剤としてのトリアゾール誘導体
WO2008070994A1 (en) 2006-12-14 2008-06-19 Nps Pharmaceuticals, Inc. Use of d-serine derivatives for the treatment of anxiety disorders
US8263585B2 (en) 2007-05-04 2012-09-11 Novartis Ag Organic compounds
TW200911798A (en) * 2007-08-02 2009-03-16 Amgen Inc PI3 kinase modulators and methods of use
CN101835776A (zh) 2007-08-14 2010-09-15 拜耳先灵医药股份有限公司 用于癌症治疗的稠合的咪唑
EP2062893A1 (en) * 2007-10-18 2009-05-27 Bayer Schering Pharma AG Fused imidazoles for cancer treatment
KR20100044852A (ko) * 2007-08-17 2010-04-30 이카겐, 인코포레이티드 칼륨 채널 조절제로서의 헤테로사이클
US8431608B2 (en) 2007-08-17 2013-04-30 Icagen Inc. Heterocycles as potassium channel modulators
MX2010002312A (es) 2007-08-31 2010-03-18 Merck Serono Sa Compuestos de triazolopiridina y su uso como inhibidores de cinasa reguladora de señal de apoptosis.
UA102828C2 (en) * 2007-11-27 2013-08-27 Целльзом Лимитед Amino triazoles as p13k inhibitors
PE20091268A1 (es) * 2007-12-19 2009-09-19 Amgen Inc Derivados heterociclicos como inhibidores de pi3 quinasa
US8268834B2 (en) * 2008-03-19 2012-09-18 Novartis Ag Pyrazine derivatives that inhibit phosphatidylinositol 3-kinase enzyme
US20090258907A1 (en) * 2008-04-09 2009-10-15 Abbott Laboratories Compounds useful as inhibitors of rock kinases
WO2009129211A1 (en) 2008-04-16 2009-10-22 Vertex Pharmaceuticals Incorporated Inhibitors of phosphatidylinositol 3-kinase
EP2444403A1 (en) 2008-04-18 2012-04-25 Shionogi Co., Ltd. Heterocyclic compound having inhibitory activity on PI3K
AR071523A1 (es) * 2008-04-30 2010-06-23 Merck Serono Sa 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
WO2009155052A1 (en) * 2008-05-28 2009-12-23 Wyeth 3-substituted-1h-pyrrolo[2,3-b]pyridine and 3-substituted-1h-pyrrolo[3,2-b]pyridine compounds, their use as mtor kinase and pi3 kinase inhibitors, and their syntheses
EP2307400B1 (en) 2008-05-30 2014-04-23 Amgen, Inc Inhibitors of pi3 kinase
CA2726844C (en) 2008-06-20 2016-08-30 Genentech, Inc. Triazolopyridine jak inhibitor compounds and methods
MX2010014005A (es) 2008-06-20 2011-02-15 Genentech Inc Compuestos de triazolopiridina inhibidores de jak y los metodos.
US20110178070A1 (en) * 2008-06-24 2011-07-21 Takeda Pharmaceutical Company Limited PI3K/mTOR INHIBITORS
WO2010007100A1 (en) * 2008-07-15 2010-01-21 Cellzome Ltd 7-substituted amino triazoles as pi3k inhibitors
WO2010007099A1 (en) * 2008-07-15 2010-01-21 Cellzome Limited 2-aminoimidazo[1,2-b]pyridazine derivatives as pi3k inhibitors
WO2010057877A1 (en) * 2008-11-18 2010-05-27 Cellzome Limited 7-pyridinyl- or phenyl- substituted triazolo [1, 5 -a] pyridines as pi3k inhibitors
LT3354650T (lt) 2008-12-19 2022-06-27 Vertex Pharmaceuticals Incorporated Junginiai, naudingi kaip atr kinazės inhibitoriai
WO2010092015A1 (en) 2009-02-10 2010-08-19 Cellzome Limited Urea triazololo [1, 5-a] pyridine derivatives as pi3k inhibitors
EA201101188A1 (ru) 2009-02-13 2012-04-30 Фовеа Фармасьютикалз [1,2,4]триазоло[1,5-а]пиридины в качестве ингибиторов киназы
JP2012518011A (ja) 2009-02-17 2012-08-09 バーテックス ファーマシューティカルズ インコーポレイテッド ホスファチジルイノシトール3−キナーゼのテトラヒドロチアゾロピリジン阻害剤
AU2010250055A1 (en) 2009-02-27 2011-09-15 Vertex Pharmaceuticals Incorporated Tri-cyclic pyrazolopyridine kinase inhibitors
WO2010100144A1 (en) * 2009-03-04 2010-09-10 Merck Serono S.A. Fused bicyclic compounds as inhibitors for pi3 kinase
JP2012521354A (ja) 2009-03-20 2012-09-13 アムジエン・インコーポレーテツド Pi3キナーゼの阻害薬
US20120071475A1 (en) 2009-04-27 2012-03-22 Shionogi & Co., Ltd. Urea derivatives having pi3k-inhibiting activity
WO2010133534A1 (en) * 2009-05-19 2010-11-25 Cellzome Limited Bicyclic amino substituted compounds as pi3k inhibitors
EP2432782A1 (en) * 2009-05-20 2012-03-28 Cellzome Ag Methods for the identification of phosphatidylinositol kinase interacting molecules and for the purification of phosphatidylinositol kinase proteins
WO2010141796A2 (en) 2009-06-05 2010-12-09 Cephalon, Inc. PREPARATION AND USES OF 1,2,4-TRIAZOLO [1,5a] PYRIDINE DERIVATIVES
CA2766100C (en) 2009-06-29 2018-05-22 Incyte Corporation Pyrimidinones as pi3k inhibitors
UY32748A (es) 2009-07-02 2011-01-31 Novartis Ag 2-carboxamida-cicloamino-ureas
US8293753B2 (en) * 2009-07-02 2012-10-23 Novartis Ag Substituted 2-carboxamide cycloamino ureas
SG178454A1 (en) * 2009-08-17 2012-03-29 Intellikine Inc Heterocyclic compounds and uses thereof
US8759359B2 (en) 2009-12-18 2014-06-24 Incyte Corporation Substituted heteroaryl fused derivatives as PI3K inhibitors
CA2796311A1 (en) 2010-04-14 2011-10-20 Incyte Corporation Fused derivatives as pi3k.delta. inhibitors
US8487102B2 (en) * 2010-04-20 2013-07-16 Hoffmann-La Roche Inc. Pyrrazolopyridine compounds as dual NK1/NK3 receptor antagonists
EP2563792B1 (en) 2010-04-28 2014-08-27 Bristol-Myers Squibb Company Imidazopyridazinyl compounds and their uses for cancer
JP2013529200A (ja) * 2010-05-12 2013-07-18 バーテックス ファーマシューティカルズ インコーポレイテッド Atrキナーゼ阻害剤として有用な化合物
JP2013526540A (ja) 2010-05-12 2013-06-24 バーテックス ファーマシューティカルズ インコーポレイテッド Atrキナーゼ阻害剤として有用な化合物
EP2569284B1 (en) * 2010-05-12 2015-07-08 Vertex Pharmaceuticals Incorporated 2-aminopyridine derivatives useful as inhibitors of atr kinase
KR20130066633A (ko) 2010-05-12 2013-06-20 버텍스 파마슈티칼스 인코포레이티드 Atr 키나제의 억제제로서 유용한 화합물
EP2575462B1 (en) * 2010-05-24 2016-06-22 Intellikine, LLC Heterocyclic compounds and uses thereof
TW201204723A (en) 2010-06-22 2012-02-01 Fovea Pharmaceuticals Heterocyclic compounds, their preparation and their therapeutic application
CA2822070C (en) 2010-12-20 2019-09-17 Incyte Corporation N-(1-(substituted-phenyl)ethyl)-9h-purin-6-amines as pi3k inhibitors
BR112013018286A2 (pt) * 2011-01-19 2016-11-16 Galapagos Nv derivados d azetidina úteis para o tratamento de doenças metabólicas e inflamatórias
CN106619647A (zh) 2011-02-23 2017-05-10 因特利凯有限责任公司 激酶抑制剂的组合及其用途
US9127000B2 (en) 2011-02-23 2015-09-08 Intellikine, LLC. Heterocyclic compounds and uses thereof
US9108984B2 (en) 2011-03-14 2015-08-18 Incyte Corporation Substituted diamino-pyrimidine and diamino-pyridine derivatives as PI3K inhibitors
WO2012135009A1 (en) 2011-03-25 2012-10-04 Incyte Corporation Pyrimidine-4,6-diamine derivatives as pi3k inhibitors
CU24263B1 (es) 2011-04-07 2017-07-04 Bayer Ip Gmbh Derivados de imidazopiridazinas inhibidores de quinasa akt, útiles para el tratamiento del cáncer
KR102371532B1 (ko) 2011-09-02 2022-03-07 인사이트 홀딩스 코포레이션 Pi3k 억제제로서 헤테로시클릴아민
WO2013049859A1 (en) 2011-09-30 2013-04-04 Vertex Pharmaceuticals Incorporated Treating pancreatic cancer and non-small cell lung cancer with atr inhibitors
IN2014KN00929A (es) 2011-09-30 2015-08-21 Vertex Pharma
AR090548A1 (es) 2012-04-02 2014-11-19 Incyte Corp Azaheterociclobencilaminas biciclicas como inhibidores de pi3k
WO2013152298A1 (en) 2012-04-05 2013-10-10 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase and combination therapies thereof
EP2852661A1 (en) 2012-05-23 2015-04-01 F. Hoffmann-La Roche AG Compositions and methods of obtaining and using endoderm and hepatocyte cells
JP6259823B2 (ja) * 2012-07-13 2018-01-10 ユーシービー バイオファルマ エスピーアールエル Tnf活性の調節物質としてのイミダゾピリジン誘導体
US8999632B2 (en) 2012-10-04 2015-04-07 Vertex Pharmaceuticals Incorporated Method for measuring ATR inhibition mediated increases in DNA damage
US9227978B2 (en) 2013-03-15 2016-01-05 Araxes Pharma Llc Covalent inhibitors of Kras G12C
WO2014144850A1 (en) 2013-03-15 2014-09-18 Genentech, Inc. Methods of treating cancer and preventing cancer drug resistance
RU2015140600A (ru) * 2013-03-20 2017-04-26 Ф. Хоффманн-Ля Рош Аг Производные мочевины и их применение в качестве ингибиторов белка, связывающего жирные кислоты
TWI659021B (zh) 2013-10-10 2019-05-11 亞瑞克西斯製藥公司 Kras g12c之抑制劑
CN105764514B (zh) * 2013-11-27 2019-07-12 圣诺康生命科学公司 作为tam族激酶抑制剂的氨基吡啶衍生物
GB201321733D0 (en) 2013-12-09 2014-01-22 Ucb Pharma Sa Therapeutic agents
CN111454188A (zh) 2014-02-13 2020-07-28 因赛特公司 作为lsd1抑制剂的环丙胺
US9493442B2 (en) 2014-02-13 2016-11-15 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
CN106488915B (zh) 2014-02-13 2020-10-02 因赛特公司 作为lsd1抑制剂的环丙胺
US9527835B2 (en) 2014-02-13 2016-12-27 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
US9598424B2 (en) 2014-03-06 2017-03-21 Takeda Pharmaceutical Company Limited Heteroarylamide inhibitors of TBK1
WO2015191677A1 (en) 2014-06-11 2015-12-17 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors
TW201613925A (en) 2014-07-10 2016-04-16 Incyte Corp Imidazopyrazines as LSD1 inhibitors
US9695167B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted triazolo[1,5-a]pyridines and triazolo[1,5-a]pyrazines as LSD1 inhibitors
US9695168B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted imidazo[1,5-α]pyridines and imidazo[1,5-α]pyrazines as LSD1 inhibitors
WO2016007727A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
JO3556B1 (ar) 2014-09-18 2020-07-05 Araxes Pharma Llc علاجات مدمجة لمعالجة السرطان
WO2016097359A1 (en) * 2014-12-19 2016-06-23 Janssen Pharmaceutica Nv Heterocyclyl linked imidazopyridazine derivatives as pi3kbeta inhibitors
EP3831833B1 (en) 2015-02-27 2022-10-26 Incyte Holdings Corporation Processes for the preparation of a pi3k inhibitor
AU2016243939B2 (en) 2015-04-03 2020-09-03 Incyte Holdings Corporation Heterocyclic compounds as LSD1 inhibitors
ES2898765T3 (es) 2015-04-10 2022-03-08 Araxes Pharma Llc Compuestos de quinazolina sustituidos y métodos de uso de los mismos
MX2017013275A (es) 2015-04-15 2018-01-26 Araxes Pharma Llc Inhibidores triciclicos fusionados de kras y metodos de uso de los mismos.
US9988401B2 (en) 2015-05-11 2018-06-05 Incyte Corporation Crystalline forms of a PI3K inhibitor
US9732097B2 (en) 2015-05-11 2017-08-15 Incyte Corporation Process for the synthesis of a phosphoinositide 3-kinase inhibitor
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
BR112018002553A8 (pt) 2015-08-12 2023-01-24 Incyte Corp Sais de um inibidor de lsd1
EP3356349A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356353A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
US10647703B2 (en) 2015-09-28 2020-05-12 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
WO2017058805A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
EP3356359B1 (en) 2015-09-28 2021-10-20 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356347A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
WO2017058902A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
CA3000684A1 (en) 2015-09-30 2017-04-06 Vertex Pharmaceuticals Incorporated Method for treating cancer using a combination of dna damaging agents and atr inhibitors
KR20240113606A (ko) 2015-11-16 2024-07-22 아락세스 파마 엘엘씨 치환된 헤테로사이클릭 그룹을 포함하는 2-치환된 퀴나졸린 화합물 및 이의 사용 방법
WO2017152117A1 (en) 2016-03-03 2017-09-08 Cornell University Small molecule ire1-alpha inhibitors
EP3445339B1 (en) 2016-04-22 2023-08-23 Incyte Corporation Formulations of an lsd1 inhibitor
US11352328B2 (en) 2016-07-12 2022-06-07 Arisan Therapeutics Inc. Heterocyclic compounds for the treatment of arenavirus
US10646488B2 (en) 2016-07-13 2020-05-12 Araxes Pharma Llc Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof
EP3519402A1 (en) 2016-09-29 2019-08-07 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
US10377743B2 (en) 2016-10-07 2019-08-13 Araxes Pharma Llc Inhibitors of RAS and methods of use thereof
EP3573971A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1yl)prop-2-en-1-one derivatives and similar compounds as kras g12c modulators for treating cancer
US11136308B2 (en) 2017-01-26 2021-10-05 Araxes Pharma Llc Substituted quinazoline and quinazolinone compounds and methods of use thereof
EP3573954A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
JP7327802B2 (ja) 2017-01-26 2023-08-16 アラクセス ファーマ エルエルシー 縮合ヘテロ-ヘテロ二環式化合物およびその使用方法
EP3573964A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Benzothiophene and benzothiazole compounds and methods of use thereof
CN110869358A (zh) 2017-05-25 2020-03-06 亚瑞克西斯制药公司 Kras的共价抑制剂
WO2018218071A1 (en) 2017-05-25 2018-11-29 Araxes Pharma Llc Compounds and methods of use thereof for treatment of cancer
US11639346B2 (en) 2017-05-25 2023-05-02 Araxes Pharma Llc Quinazoline derivatives as modulators of mutant KRAS, HRAS or NRAS
WO2019070093A1 (en) * 2017-10-02 2019-04-11 1ST Biotherapeutics, Inc. BENZOTHIAZOL COMPOUNDS AND METHODS OF USING THE SAME FOR TREATING NEURODEGENERATIVE DISORDERS
HUE058292T2 (hu) * 2017-10-30 2022-07-28 Bristol Myers Squibb Co Aminoimidazopiridazinok mint kináz inhibitorok
CN112088157B (zh) * 2017-12-22 2023-12-26 拉文纳制药公司 作为磷脂酰肌醇磷酸激酶抑制剂的芳基-联吡啶胺衍生物
JP7569688B2 (ja) 2017-12-22 2024-10-18 ハイバーセル,インコーポレイテッド ホスファチジルイノシトールリン酸キナーゼ阻害剤としてのアミノピリジン誘導体
AU2019213484A1 (en) * 2018-02-05 2020-07-02 Centre National De La Recherche Scientifique Compounds and compositions for the treatment of pain
EP3829580A1 (en) 2018-08-01 2021-06-09 Araxes Pharma LLC Heterocyclic spiro compounds and methods of use thereof for the treatment of cancer
US10968200B2 (en) 2018-08-31 2021-04-06 Incyte Corporation Salts of an LSD1 inhibitor and processes for preparing the same
US20220242861A1 (en) * 2019-02-22 2022-08-04 1ST Biotherapeutics, Inc. Imidazopyridinyl compounds and use thereof for treatment of proliferative disorders
KR20210126146A (ko) * 2019-03-07 2021-10-19 주식회사 퍼스트바이오테라퓨틱스 Pet 방사선추적자로서의 [18f]-라벨링된 벤조티아졸 유도체
US10385046B1 (en) 2019-03-19 2019-08-20 1ST Biotherapeutics, Inc. Processes for preparing benzothiazol compounds and methods of using the same for treating neurodegenerative disorders
WO2020194260A1 (en) * 2019-03-28 2020-10-01 1ST Biotherapeutics, Inc. Pharmaceutical salts of benzothiazol compounds, polymorphs and methods for preparation thereof
EP3946618A1 (en) * 2019-04-05 2022-02-09 Storm Therapeutics Ltd Mettl3 inhibitory compounds
TW202112767A (zh) 2019-06-17 2021-04-01 美商佩特拉製藥公司 作為磷脂酸肌醇磷酸激酶抑制劑之胺基吡啶衍生物
CN112047950B (zh) * 2020-09-14 2023-07-25 华东师范大学 咪唑并吡嗪类衍生物及其合成方法和应用
WO2022058890A1 (en) * 2020-09-15 2022-03-24 1ST Biotherapeutics, Inc. 2-amino-3-carbonyl imidazopyridine and pyrazolopyridine compounds
US11649255B2 (en) * 2020-09-28 2023-05-16 1ST Biotherapeutics, Inc. Indazoles as hematopoietic progenitor kinase 1 (HPK1) inhibitors and methods using same
WO2023134692A1 (zh) * 2022-01-13 2023-07-20 浙江同源康医药股份有限公司 多环类化合物及其用途
CN115850263A (zh) * 2022-12-28 2023-03-28 浙江工业大学 一种2,7-二取代苯并噻唑类化合物及其应用

Family Cites Families (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS6041077B2 (ja) * 1976-09-06 1985-09-13 喜徳 喜谷 1,2‐ジアミノシクロヘキサン異性体のシス白金(2)錯体
US4323581A (en) * 1978-07-31 1982-04-06 Johnson & Johnson Method of treating carcinogenesis
IL73534A (en) * 1983-11-18 1990-12-23 Riker Laboratories Inc 1h-imidazo(4,5-c)quinoline-4-amines,their preparation and pharmaceutical compositions containing certain such compounds
US4904768A (en) * 1987-08-04 1990-02-27 Bristol-Myers Company Epipodophyllotoxin glucoside 4'-phosphate derivatives
US5238944A (en) * 1988-12-15 1993-08-24 Riker Laboratories, Inc. Topical formulations and transdermal delivery systems containing 1-isobutyl-1H-imidazo[4,5-c]quinolin-4-amine
US4929624A (en) * 1989-03-23 1990-05-29 Minnesota Mining And Manufacturing Company Olefinic 1H-imidazo(4,5-c)quinolin-4-amines
US5389640A (en) * 1991-03-01 1995-02-14 Minnesota Mining And Manufacturing Company 1-substituted, 2-substituted 1H-imidazo[4,5-c]quinolin-4-amines
US5451700A (en) * 1991-06-11 1995-09-19 Ciba-Geigy Corporation Amidino compounds, their manufacture and methods of treatment
US5268376A (en) * 1991-09-04 1993-12-07 Minnesota Mining And Manufacturing Company 1-substituted 1H-imidazo[4,5-c]quinolin-4-amines
AU661533B2 (en) * 1992-01-20 1995-07-27 Astrazeneca Ab Quinazoline derivatives
US5621100A (en) * 1992-07-24 1997-04-15 Cephalon, Inc. K-252a derivatives for treatment of neurological disorders
US5395937A (en) * 1993-01-29 1995-03-07 Minnesota Mining And Manufacturing Company Process for preparing quinoline amines
US5352784A (en) * 1993-07-15 1994-10-04 Minnesota Mining And Manufacturing Company Fused cycloalkylimidazopyridines
CA2167042A1 (en) * 1993-07-15 1995-01-26 Kyle J. Lindstrom Imidazo[4,5-c]pyridin-4-amines
IT1261907B (it) * 1993-09-15 1996-06-03 Sasib Spa Dispositivo alimentatore di foglietti con ruota di confezionamento, in particolare nelle macchine impacchettatrici di sigarette.
US6083903A (en) * 1994-10-28 2000-07-04 Leukosite, Inc. Boronic ester and acid compounds, synthesis and uses
US5482936A (en) * 1995-01-12 1996-01-09 Minnesota Mining And Manufacturing Company Imidazo[4,5-C]quinoline amines
GB9508538D0 (en) * 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivatives
US6331555B1 (en) * 1995-06-01 2001-12-18 University Of California Treatment of platelet derived growth factor related disorders such as cancers
US5747498A (en) * 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
US5880141A (en) * 1995-06-07 1999-03-09 Sugen, Inc. Benzylidene-Z-indoline compounds for the treatment of disease
KR100447918B1 (ko) * 1996-07-25 2005-09-28 동아제약주식회사 대장을포함한위장관보호작용을갖는플라본및플라바논화합물
CO4950519A1 (es) * 1997-02-13 2000-09-01 Novartis Ag Ftalazinas, preparaciones farmaceuticas que las comprenden y proceso para su preparacion
US6166037A (en) * 1997-08-28 2000-12-26 Merck & Co., Inc. Pyrrolidine and piperidine modulators of chemokine receptor activity
RS49779B (sr) * 1998-01-12 2008-06-05 Glaxo Group Limited, Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze
CA2398754A1 (en) * 2000-02-07 2001-08-09 Abbott Gmbh & Co. Kg 2-benzothiazolyl urea derivatives and their use as protein kinase inhibitors
DE60115069T2 (de) * 2000-09-11 2006-08-03 Chiron Corp., Emeryville Chinolinonderivate als tyrosin-kinase inhibitoren
SI1341769T1 (sl) * 2000-12-15 2008-02-29 Vertex Pharma Inhibitorji bakterijske giraze in njihove uporabe
US20030134846A1 (en) * 2001-10-09 2003-07-17 Schering Corporation Treatment of trypanosoma brucei with farnesyl protein transferase inhibitors
EP1485082A4 (en) * 2002-02-19 2009-12-30 Xenoport Inc PROCESS FOR THE SYNTHESIS OF PROMEDICAMENTS FROM 1-ACYL-ALKYL DERIVATIVES AND CORRESPONDING COMPOSITIONS
US6900342B2 (en) * 2002-05-10 2005-05-31 Dabur India Limited Anticancer taxanes such as paclitaxel, docetaxel and their structural analogs, and a method for the preparation thereof
AU2004215428B2 (en) * 2003-02-26 2009-08-27 Sugen LLC Aminoheteroaryl compounds as protein kinase inhibitors
WO2005035526A1 (en) * 2003-10-09 2005-04-21 Argenta Discovery Ltd. Bicyclic compounds and their therapeutic use
CA2559229A1 (en) * 2004-03-19 2005-09-29 Warner-Lambert Company Llc Imidazopyridine and imidazopyrimidine derivatives as antibacterial agents
US20100029619A1 (en) * 2006-08-04 2010-02-04 Takeda Pharmaceutical Company Limted Fused heterocyclic compound

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