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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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/4353—Heterocyclic 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
    • A61K31/437—Heterocyclic 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—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
    • A61P31/04—Antibacterial agents
    • 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
    • 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
    • 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
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

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

ID=38226373

Family Applications (1)

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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 (129)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007116432A1 (ja) 2006-03-30 2007-10-18 Aichi Prefecture キャノロールまたはそのプロドラッグ（ｐｄ）を含む抗炎症剤および癌予防剤ならびにこれらを含む医薬、化粧品および食品
WO2008016131A1 (fr) * 2006-08-04 2008-02-07 Takeda Pharmaceutical Company Limited Composé hétérocyclique à cycles fusionnés
CA2662074A1 (en) 2006-08-30 2008-03-06 Cellzome Limited Triazole derivatives as kinase inhibitors
US8450336B2 (en) 2006-12-14 2013-05-28 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
CA2694136C (en) 2007-08-02 2013-09-17 Amgen Inc. Pi3 kinase modulators and methods of use
DE602008005894D1 (de) * 2007-08-14 2011-05-12 Bayer Schering Pharma Ag Kondensierte imidazole zur krebsbehandlung
EP2062893A1 (en) * 2007-10-18 2009-05-27 Bayer Schering Pharma AG Fused imidazoles for cancer treatment
US8431608B2 (en) 2007-08-17 2013-04-30 Icagen Inc. Heterocycles as potassium channel modulators
ES2400604T3 (es) * 2007-08-17 2013-04-11 Icagen, Inc. Heterociclos como moduladores del canal de potasio
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.
SG186040A1 (en) * 2007-11-27 2012-12-28 Cellzome Ltd Amino triazoles as pi3k inhibitors
JP5520831B2 (ja) * 2007-12-19 2014-06-11 アムジエン・インコーポレーテツド Ｐｉ３キナーゼの阻害薬
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
WO2009128520A1 (ja) 2008-04-18 2009-10-22 塩野義製薬株式会社 Ｐ１３ｋ阻害活性を有する複素環化合物
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
MX315904B (es) 2008-05-30 2013-11-29 Amgen Inc Inhibidores de fosfoinosituro-3 cinasa.
PE20110063A1 (es) 2008-06-20 2011-02-16 Genentech Inc DERIVADOS DE [1, 2, 4]TRIAZOLO[1, 5-a]PIRIDINA COMO INHIBIDORES DE JAK
CA2727036C (en) 2008-06-20 2017-03-21 Genentech, Inc. Triazolopyridine jak inhibitor compounds and methods
WO2010008847A2 (en) * 2008-06-24 2010-01-21 Takeda Pharmaceutical Company Limited Pi3k/m tor 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
CN106496210B (zh) 2008-12-19 2020-06-09 沃泰克斯药物股份有限公司 用作atr激酶抑制剂的化合物
WO2010092015A1 (en) 2009-02-10 2010-08-19 Cellzome Limited Urea triazololo [1, 5-a] pyridine derivatives as pi3k inhibitors
EP2396324A1 (en) 2009-02-13 2011-12-21 Fovea Pharmaceuticals Ý1, 2, 4¨triazolo ý1, 5 -a¨pyridines as kinase inhibitors
AU2010216219A1 (en) 2009-02-17 2011-09-01 Vertex Pharmaceuticals Incorporated Tetrahydrothiazolopyridine inhibitors of phosphatidylinositol 3-kinase
WO2010135014A1 (en) * 2009-02-27 2010-11-25 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
MX2011009796A (es) 2009-03-20 2011-12-14 Amgen Inc Inhibidores de la cinasa pi3.
TW201103943A (en) 2009-04-27 2011-02-01 Shionogi & Co Urea derivative having pi3k inhibitory activity
WO2010133534A1 (en) * 2009-05-19 2010-11-25 Cellzome Limited Bicyclic amino substituted compounds as pi3k inhibitors
WO2010133318A1 (en) * 2009-05-20 2010-11-25 Cellzome Ag Methods for the identification of phosphatidylinositol kinase interacting molecules and for the purification of phosphatidylinositol kinase proteins
MX2011012961A (es) 2009-06-05 2012-01-30 Cephalon Inc Preparacion y usos de derivados de 1,2,4-triazolo[1,5a]-piridina.
SG177384A1 (en) 2009-06-29 2012-02-28 Incyte Corp Pyrimidinones as pi3k inhibitors
EP2448946B1 (en) 2009-07-02 2013-07-24 Novartis AG 2-carboxamide cycloamino ureas useful as pi3k inhibitors
US8293753B2 (en) * 2009-07-02 2012-10-23 Novartis Ag Substituted 2-carboxamide cycloamino ureas
WO2011022439A1 (en) * 2009-08-17 2011-02-24 Intellikine, Inc. Heterocyclic compounds and uses thereof
WO2011075643A1 (en) 2009-12-18 2011-06-23 Incyte Corporation Substituted heteroaryl fused derivatives as pi3k inhibitors
EP2558463A1 (en) 2010-04-14 2013-02-20 Incyte Corporation Fused derivatives as i3 inhibitors
US8487102B2 (en) * 2010-04-20 2013-07-16 Hoffmann-La Roche Inc. Pyrrazolopyridine compounds as dual NK1/NK3 receptor antagonists
WO2011137155A1 (en) 2010-04-28 2011-11-03 Bristol-Myers Squibb Company Imidazopyridazinyl compounds and their uses for cancer
WO2011143425A2 (en) 2010-05-12 2011-11-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
EP2569286B1 (en) * 2010-05-12 2014-08-20 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
WO2011143422A1 (en) * 2010-05-12 2011-11-17 Vertex Pharmaceuticals Incorporated 2 -aminopyridine derivatives useful as inhibitors of atr kinase
AU2011253025A1 (en) 2010-05-12 2012-11-29 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
CA2804304C (en) * 2010-05-24 2020-02-25 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
TW201249844A (en) 2010-12-20 2012-12-16 Incyte Corp N-(1-(substituted-phenyl)ethyl)-9H-purin-6-amines as PI3K inhibitors
RU2013138372A (ru) * 2011-01-19 2015-02-27 Галапаго Нв Производные азетидина, применяемые для лечения метаболических и воспалительных заболеваний
CA2828483A1 (en) 2011-02-23 2012-11-01 Intellikine, Llc Combination of kinase inhibitors and uses thereof
JP5808826B2 (ja) 2011-02-23 2015-11-10 インテリカイン， エルエルシー 複素環化合物およびその使用
US9108984B2 (en) 2011-03-14 2015-08-18 Incyte Corporation Substituted diamino-pyrimidine and diamino-pyridine derivatives as PI3K inhibitors
US9126948B2 (en) 2011-03-25 2015-09-08 Incyte Holdings Corporation Pyrimidine-4,6-diamine derivatives as PI3K inhibitors
CN103596957B (zh) 2011-04-07 2016-12-07 拜耳知识产权有限责任公司 作为akt激酶抑制剂的咪唑并哒嗪
MX2020004502A (es) 2011-09-02 2022-01-20 Incyte Holdings Corp Heterociclilaminas como inhibidores de fosfoinositida 3-cinasas (pi3k).
RU2677292C2 (ru) 2011-09-30 2019-01-16 Вертекс Фармасьютикалз Инкорпорейтед Способы получения соединений, которые можно использовать в качестве ингибиторов киназы atr
CA2850491C (en) 2011-09-30 2020-10-27 Vertex Pharmaceuticals Incorporated Treating pancreatic cancer and non-small cell lung cancer with atr inhibiors
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
JP6301316B2 (ja) 2012-05-23 2018-03-28 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ 内胚葉細胞および肝実質細胞の組成物ならびにそれらの細胞を入手および使用する方法
ES2689429T3 (es) * 2012-07-13 2018-11-14 Ucb Biopharma Sprl Derivados de imidazopiridina como moduladores de actividad de TNF
DK2904406T3 (en) 2012-10-04 2018-06-18 Vertex Pharma METHOD OF DETERMINING THE ATR INHIBITION, INCREASED DNA DAMAGE
US9227978B2 (en) 2013-03-15 2016-01-05 Araxes Pharma Llc Covalent inhibitors of Kras G12C
JP2016520528A (ja) 2013-03-15 2016-07-14 ジェネンテック， インコーポレイテッド 癌の治療及び抗癌剤耐性の防止方法
BR112015024113A2 (pt) * 2013-03-20 2017-07-18 Hoffmann La Roche derivados de uréia e seu uso como inibidores da proteína de ligação de ácido graxo (fabp)
JO3805B1 (ar) 2013-10-10 2021-01-31 Araxes Pharma Llc مثبطات كراس جي12سي
CA2930324C (en) * 2013-11-27 2022-01-18 Signalchem Lifesciences Corporation Aminopyridine derivatives as tam family kinase inhibitors
GB201321733D0 (en) 2013-12-09 2014-01-22 Ucb Pharma Sa Therapeutic agents
WO2015123437A1 (en) 2014-02-13 2015-08-20 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
CA2939082C (en) 2014-02-13 2022-06-07 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
LT3105226T (lt) 2014-02-13 2019-11-11 Incyte Corp Ciklopropilaminai, kaip lsd1 inhibitoriai
WO2015123408A1 (en) 2014-02-13 2015-08-20 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
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
WO2016007727A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
WO2016007731A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Imidazopyridines and imidazopyrazines as lsd1 inhibitors
US9695180B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted imidazo[1,2-a]pyrazines as LSD1 inhibitors
JO3556B1 (ar) 2014-09-18 2020-07-05 Araxes Pharma Llc علاجات مدمجة لمعالجة السرطان
ES2760507T3 (es) * 2014-12-19 2020-05-14 Janssen Pharmaceutica Nv Derivados de imidazopiridazina enlazados a heterociclilo como inhibidores de PI3Kß
NZ734993A (en) 2015-02-27 2024-03-22 Incyte Holdings Corp Salts of pi3k inhibitor and processes for their preparation
EP3626720A1 (en) 2015-04-03 2020-03-25 Incyte Corporation Heterocyclic compounds as lsd1 inhibitors
CN107849022A (zh) 2015-04-10 2018-03-27 亚瑞克西斯制药公司 取代的喹唑啉化合物和其使用方法
WO2016168540A1 (en) 2015-04-15 2016-10-20 Araxes Pharma Llc Fused-tricyclic inhibitors of kras and methods of use thereof
WO2016183060A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Process for the synthesis of a phosphoinositide 3-kinase inhibitor
WO2016183063A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Crystalline forms of a pi3k inhibitor
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
MX2018001706A (es) 2015-08-12 2018-09-06 Incyte Corp Sales de un inhibidor de dimetilasa 1 especifica para lisina (lsd1).
EP3356359B1 (en) 2015-09-28 2021-10-20 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
US10875842B2 (en) 2015-09-28 2020-12-29 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
US10858343B2 (en) 2015-09-28 2020-12-08 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
US10689356B2 (en) 2015-09-28 2020-06-23 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
WO2017058915A1 (en) 2015-09-28 2017-04-06 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
EP3356351A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
AU2016331955B2 (en) 2015-09-30 2022-07-21 Vertex Pharmaceuticals Incorporated Method for treating cancer using a combination of DNA damaging agents and ATR inhibitors
AU2016355433C1 (en) 2015-11-16 2021-12-16 Araxes Pharma Llc 2-substituted quinazoline compounds comprising a substituted heterocyclic group and methods of use thereof
CA3016196A1 (en) 2016-03-03 2017-09-08 Cornell University Small molecule ire1-alpha inhibitors
UA125559C2 (uk) 2016-04-22 2022-04-20 Інсайт Корпорейшн Композиції інгібітора lsd1
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
JP2019529484A (ja) 2016-09-29 2019-10-17 アラクセス ファーマ エルエルシー Ｋｒａｓ ｇ１２ｃ変異体タンパク質の阻害剤
US10377743B2 (en) 2016-10-07 2019-08-13 Araxes Pharma Llc Inhibitors of RAS and methods of use thereof
US11136308B2 (en) 2017-01-26 2021-10-05 Araxes Pharma Llc Substituted quinazoline and quinazolinone compounds and methods of use thereof
US11358959B2 (en) 2017-01-26 2022-06-14 Araxes Pharma Llc Benzothiophene and benzothiazole compounds 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
EP3573954A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
EP3573967A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Fused hetero-hetero bicyclic compounds and methods of use thereof
US10736897B2 (en) 2017-05-25 2020-08-11 Araxes Pharma Llc Compounds and methods of use thereof for treatment of cancer
WO2018218069A1 (en) 2017-05-25 2018-11-29 Araxes Pharma Llc Quinazoline derivatives as modulators of mutant kras, hras or nras
KR20200010306A (ko) 2017-05-25 2020-01-30 아락세스 파마 엘엘씨 Kras의 공유적 억제제
WO2019070093A1 (en) 2017-10-02 2019-04-11 1ST Biotherapeutics, Inc. BENZOTHIAZOL COMPOUNDS AND METHODS OF USING THE SAME FOR TREATING NEURODEGENERATIVE DISORDERS
SG11202003824PA (en) * 2017-10-30 2020-05-28 Bristol Myers Squibb Co Aminoimidazopyridazines as kinase inhibitors
WO2019126731A1 (en) 2017-12-22 2019-06-27 Petra Pharma Corporation Aminopyridine derivatives as phosphatidylinositol phosphate kinase inhibitors
BR112020012651A2 (pt) * 2017-12-22 2020-12-01 Ravenna Pharmaceuticals, Inc. compostos derivados de aril-bipiridina amina como inibidores da fosfatidilinositol fosfato quinase, composição farmacêutica compreendendo os mesmos e usos terapêuticos dos ditos compostos
MX2020008082A (es) * 2018-02-05 2020-09-24 Univ Strasbourg Compuestos y composiciones para el tratamiento del dolor.
US10968200B2 (en) 2018-08-31 2021-04-06 Incyte Corporation Salts of an LSD1 inhibitor and processes for preparing the same
EP3927705A4 (en) * 2019-02-22 2022-12-07 1st Biotherapeutics, Inc. IMIDAZOPYRIDINYL COMPOUNDS AND THEIR USE FOR THE TREATMENT OF NEURODEGENERATIVE DISORDERS
EP3934702A4 (en) * 2019-03-07 2023-02-22 1st Biotherapeutics, Inc. [18F]-LABELED BENZOTHIAZOLE DERIVATE AS PET RADIOTRACER
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
US20220177463A1 (en) * 2019-03-28 2022-06-09 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
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
KR20230104143A (ko) * 2020-09-28 2023-07-07 주식회사 퍼스트바이오테라퓨틱스 조혈 전구 키나아제 1(hpk1) 억제제로서의 인다졸 및 이의 사용 방법
CN116425757A (zh) * 2022-01-13 2023-07-14 浙江同源康医药股份有限公司 多环类化合物及其用途

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
GB9300059D0 (en) * 1992-01-20 1993-03-03 Zeneca Ltd 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
WO1995002597A1 (en) * 1993-07-15 1995-01-26 Minnesota Mining And Manufacturing Company IMIDAZO[4,5-c]PYRIDIN-4-AMINES
US5352784A (en) * 1993-07-15 1994-10-04 Minnesota Mining And Manufacturing Company Fused cycloalkylimidazopyridines
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
JP2003521543A (ja) * 2000-02-07 2003-07-15 アボット ゲーエムベーハー ウント カンパニー カーゲー ２−ベンゾチアゾリル尿素誘導体およびそのプロテインキナーゼ阻害剤としての使用
BRPI0113757B8 (pt) * 2000-09-11 2017-11-07 Chiron Corp derivados de quinolinona como inibidores de tirosina quinase
MXPA03005298A (es) * 2000-12-15 2003-10-06 Vertex Pharma Inhibidores de girasa y usos de los mismos.
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
PL216368B1 (pl) * 2003-02-26 2014-03-31 Sugen Związki aminoheteroarylowe oraz ich zastosowanie
WO2005035526A1 (en) * 2003-10-09 2005-04-21 Argenta Discovery Ltd. Bicyclic compounds and their therapeutic use
ES2328047T3 (es) * 2004-03-19 2009-11-06 Warner-Lambert Company Llc Derivados de imidazopiridina e imidazopirimidina como agentes antibacterianos.
WO2008016131A1 (fr) * 2006-08-04 2008-02-07 Takeda Pharmaceutical Company Limited Composé hétérocyclique à cycles fusionnés

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