CN1251097B - 具有血管生成抑制活性的酞嗪类化合物 - Google Patents

具有血管生成抑制活性的酞嗪类化合物 Download PDF

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Publication number
CN1251097B
CN1251097B CN988036045A CN98803604A CN1251097B CN 1251097 B CN1251097 B CN 1251097B CN 988036045 A CN988036045 A CN 988036045A CN 98803604 A CN98803604 A CN 98803604A CN 1251097 B CN1251097 B CN 1251097B
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China
Prior art keywords
compound
formula
group
picolyl
phthalazines
Prior art date
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Expired - Fee Related
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CN988036045A
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English (en)
Chinese (zh)
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CN1251097A (zh
Inventor
G·波德
J·弗莱
P·特拉克斯勒
K-H·奥特曼
H·麦特
D·R·斯多沃
J·伍德
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Novartis AG
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Novartis AG
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Anticipated expiration legal-status Critical
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms 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

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyridine Compounds (AREA)
CN988036045A 1997-02-13 1998-02-11 具有血管生成抑制活性的酞嗪类化合物 Expired - Fee Related CN1251097B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CH315/97 1997-02-13
CH31597 1997-02-13
PCT/EP1998/000764 WO1998035958A1 (en) 1997-02-13 1998-02-11 Phthalazines with angiogenesis inhibiting activity

Publications (2)

Publication Number Publication Date
CN1251097A CN1251097A (zh) 2000-04-19
CN1251097B true CN1251097B (zh) 2011-10-19

Family

ID=4184213

Family Applications (1)

Application Number Title Priority Date Filing Date
CN988036045A Expired - Fee Related CN1251097B (zh) 1997-02-13 1998-02-11 具有血管生成抑制活性的酞嗪类化合物

Country Status (32)

Country Link
US (3) US6258812B1 (enExample)
EP (1) EP0970070B1 (enExample)
JP (1) JP3544675B2 (enExample)
KR (1) KR100441362B1 (enExample)
CN (1) CN1251097B (enExample)
AR (1) AR011135A1 (enExample)
AT (1) ATE278686T1 (enExample)
AU (1) AU731852B2 (enExample)
BR (1) BR9807685B1 (enExample)
CA (1) CA2281721C (enExample)
CO (1) CO4950519A1 (enExample)
CY (1) CY2550B1 (enExample)
CZ (1) CZ297534B6 (enExample)
DE (1) DE69826841T2 (enExample)
DK (1) DK0970070T3 (enExample)
ES (1) ES2234097T3 (enExample)
HU (1) HU227972B1 (enExample)
ID (1) ID23698A (enExample)
IL (1) IL131273A0 (enExample)
MY (1) MY128645A (enExample)
NO (1) NO317367B1 (enExample)
NZ (1) NZ337064A (enExample)
PE (1) PE52499A1 (enExample)
PL (1) PL197371B1 (enExample)
PT (1) PT970070E (enExample)
RU (1) RU2207132C2 (enExample)
SI (1) SI0970070T1 (enExample)
SK (1) SK285757B6 (enExample)
TR (1) TR199901953T2 (enExample)
TW (1) TWI250151B (enExample)
WO (1) WO1998035958A1 (enExample)
ZA (1) ZA981155B (enExample)

Families Citing this family (311)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998013350A1 (en) 1996-09-25 1998-04-02 Zeneca Limited Qinoline derivatives inhibiting the effect of growth factors such as vegf
GB9718972D0 (en) 1996-09-25 1997-11-12 Zeneca Ltd Chemical compounds
CO4950519A1 (es) * 1997-02-13 2000-09-01 Novartis Ag Ftalazinas, preparaciones farmaceuticas que las comprenden y proceso para su preparacion
ATE368665T1 (de) 1997-08-22 2007-08-15 Astrazeneca Ab Oxindolylchinazolinderivate als angiogenesehemmer
WO2000009495A1 (en) * 1998-08-11 2000-02-24 Novartis Ag Isoquinoline derivatives with angiogenesis inhibiting activity
EP1105136B1 (en) * 1998-08-13 2007-08-29 Novartis AG Method for treating ocular neovascular diseases
PT1165085E (pt) 1999-03-30 2006-10-31 Novartis Ag Derivados de ftalazina para tratar doencas inflamatorias
US6271233B1 (en) 1999-08-10 2001-08-07 Ciba Vision Corporation Method for treating ocular neovascular diseases
AR025068A1 (es) * 1999-08-10 2002-11-06 Bayer Corp Pirazinas sustituidas y piridazinas fusionadas, composicion farmaceutica que las comprenden, uso de dichos compuestos para la manufactura de un medicamentocon actividad inhibidora de angiogenesis
DOP2000000070A (es) * 1999-09-28 2002-02-28 Bayer Healthcare Llc Piridinas y piridacinas sustituidas con actividad de inhibición de angiogénesis
US6689883B1 (en) 1999-09-28 2004-02-10 Bayer Pharmaceuticals Corporation Substituted pyridines and pyridazines with angiogenesis inhibiting activity
PL203782B1 (pl) 1999-11-05 2009-11-30 Astrazeneca Ab Pochodne chinazoliny,sposoby ich wytwarzania,ich kompozycje farmaceutyczne oraz ich zastosowania
DE19963607B4 (de) * 1999-12-23 2005-12-15 Schering Ag Verfahren zur Herstellung von 4-(Heteroaryl-methyl) halogen-1(2H)-phthalazinonen
WO2001058899A1 (en) * 2000-02-09 2001-08-16 Novartis Ag Pyridine derivatives inhibiting angiogenesis and/or vegf receptor tyrosine kinase
US7087608B2 (en) 2000-03-03 2006-08-08 Robert Charles Atkins Use of PDGF receptor tyrosine kinase inhibitors for the treatment of diabetic nephropathy
AU779695B2 (en) 2000-04-07 2005-02-10 Astrazeneca Ab Quinazoline compounds
US7977333B2 (en) 2000-04-20 2011-07-12 Bayer Healthcare Llc Substituted pyridines and pyridazines with angiogenesis inhibiting activity
WO2001097850A2 (en) * 2000-06-23 2001-12-27 Schering Aktiengesellschaft Combinations and compositions which interfere with vegf/vegf and angiopoietin/tie receptor function and their use (ii)
EP1166799A1 (en) * 2000-06-28 2002-01-02 Schering Aktiengesellschaft Combinations and compositions which interfere with VEGF/VEGF and angiopoietin/Tie receptor function and their use (II)
EP1166798A1 (en) * 2000-06-23 2002-01-02 Schering Aktiengesellschaft Combinations and compositions which interfere with VEGF/VEGF and angiopoietin/ Tie receptor function and their use
WO2002012227A2 (en) * 2000-08-09 2002-02-14 Astrazeneca Ab Indole, azaindole and indazole derivatives having vegf inhibiting activity
US6903101B1 (en) 2000-08-10 2005-06-07 Bayer Pharmaceuticals Corporation Substituted pyridazines and fused pyridazines with angiogenesis inhibiting activity
ATE419239T1 (de) 2000-10-20 2009-01-15 Eisai R&D Man Co Ltd Verfahren zur herstellung von 4-phenoxy chinolin derivaten
HU228960B1 (hu) * 2000-10-30 2013-07-29 Kudos Pharm Ltd Ftalazinon-származékok
EP1339458B1 (en) * 2000-11-22 2007-08-15 Novartis AG Combination comprising an agent decreasing vegf activity and an agent decreasing egf activity
US7814641B2 (en) * 2001-01-09 2010-10-19 Black & Decker Inc. Method of forming a power tool
US7096566B2 (en) 2001-01-09 2006-08-29 Black & Decker Inc. Method for making an encapsulated coil structure
EP3342411B1 (en) 2001-02-19 2019-08-21 Novartis Pharma AG Rapamycin derivative for treating pancreas cancer
GB0111078D0 (en) * 2001-05-04 2001-06-27 Novartis Ag Organic compounds
KR20080091866A (ko) 2001-05-16 2008-10-14 노파르티스 아게 Ν-｛5-[4-(4-메틸-피페라지노-메틸)-벤조일아미도]-2-메틸페닐｝-4-(3-피리딜)-2-피리미딘-아민 및 화학치료제를 포함하는 배합물
TWI315982B (en) 2001-07-19 2009-10-21 Novartis Ag Combinations comprising epothilones and pharmaceutical uses thereof
US20030073692A1 (en) 2001-08-07 2003-04-17 Pharmacia & Upjohn S.P.A. Amino-phthalazinone derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions containing them
RU2320344C2 (ru) * 2001-09-12 2008-03-27 Новартис Аг Применение 4-пиридилметилфталазинов для лечения рака
IL160382A0 (en) * 2001-09-12 2004-07-25 Novartis Ag Use of 4-pyridylmethylphthalazines for cancer treatment
SI1427420T1 (sl) * 2001-09-12 2006-12-31 Novartis Ag Uporaba kombinacije, ki vsebuje 4-piridilmetilftalazine za zdravljenje raka
US20040266779A1 (en) * 2001-09-27 2004-12-30 Anderson Kenneth C. Use of c-kit inhibitors for the treatment of myeloma
ES2295428T3 (es) * 2001-10-25 2008-04-16 Novartis Ag Combinaciones que comprenden un inhibidor selectivo de ciclooxigenasa-2.
CA2471314A1 (en) * 2001-12-21 2003-07-24 Bayer Pharmaceuticals Corporation Anti-angiogenesis combination therapies comprising pyridazine or pyridine derivatives
EP1458713B1 (en) * 2001-12-27 2005-08-24 Theravance, Inc. Indolinone derivatives useful as protein kinase inhibitors
US20030171375A1 (en) * 2002-02-13 2003-09-11 Brazzell Romulus Kimbro Method for treating ocular neovascular diseases
GB0206215D0 (en) 2002-03-15 2002-05-01 Novartis Ag Organic compounds
WO2003092696A1 (en) * 2002-04-30 2003-11-13 Novartis Ag Method for decreasing capillary permeability in the retina
NZ560662A (en) 2002-05-16 2009-09-25 Novartis Ag Use of EDG receptor binding agents in cancer
CN100355423C (zh) * 2002-06-28 2007-12-19 诺瓦提斯公司 用于治疗肿瘤的包含血管抑制化合物和烷化剂的组合
AU2003259713A1 (en) * 2002-08-09 2004-02-25 Theravance, Inc. Oncokinase fusion polypeptides associated with hyperproliferative and related disorders, nucleic acids encoding the same and methods for detecting and identifying the same
EP1545534B1 (en) * 2002-09-24 2007-04-18 Novartis AG Use of 4-pyridylmethyl-phthalazine derivatives for the manufacture of a medicament for the treatment of myelodysplastic syndromes
GB0223341D0 (en) * 2002-10-08 2002-11-13 Groningen Acad Ziekenhuis Organic compounds
EP1554015A1 (en) * 2002-10-10 2005-07-20 Novartis AG Treatment of amm
US7268137B2 (en) 2002-11-07 2007-09-11 Campochiaro Peter A Ocular therapy
WO2004043459A1 (en) * 2002-11-12 2004-05-27 Novartis Ag Treatment of mesothelioma
US7094785B1 (en) 2002-12-18 2006-08-22 Cornell Research Foundation, Inc. Method of treating polycythemia vera
AU2003286373A1 (en) * 2002-12-20 2004-07-14 Dana-Farber Cancer Institute Inc. Treatment of von hippel lindau disease
JP2006514991A (ja) * 2002-12-27 2006-05-18 シエーリング アクチエンゲゼルシャフト 新規医薬組合せ
TWI422583B (zh) 2003-03-07 2014-01-11 參天製藥股份有限公司 具有以４-吡啶烷硫基為取代基之新穎化合物
US20050043233A1 (en) 2003-04-29 2005-02-24 Boehringer Ingelheim International Gmbh Combinations for the treatment of diseases involving cell proliferation, migration or apoptosis of myeloma cells or angiogenesis
US20040242886A1 (en) * 2003-04-30 2004-12-02 Sandeep Gupta Monocyclic diazodioxide based Bcl-2 protein antagonists related applications
MY150088A (en) 2003-05-19 2013-11-29 Irm Llc Immunosuppressant compounds and compositions
WO2005000833A1 (en) 2003-05-19 2005-01-06 Irm, Llc Immunosuppressant compounds and compositions
MXPA06000508A (es) 2003-07-18 2006-04-05 Amgen Inc Agentes de union especifica al factor del crecimiento de los hepatocitos.
CN101337930B (zh) 2003-11-11 2010-09-08 卫材R&D管理有限公司 脲衍生物的制备方法
JP4762150B2 (ja) 2003-11-18 2011-08-31 ノバルティス アーゲー Ｋｉｔの変異体の阻害剤
JP2007513967A (ja) * 2003-12-11 2007-05-31 セラヴァンス， インコーポレーテッド 変異レセプターチロシンキナーゼが駆動する細胞増殖性疾患の処置において使用するための組成物
WO2005085201A1 (ja) 2004-02-17 2005-09-15 Santen Pharmaceutical Co., Ltd. 置換又は無置換アミノ基を導入した４－ピリジルアルキルチオ基を有する新規環式化合物
EP1568368A1 (en) * 2004-02-26 2005-08-31 Schering Aktiengesellschaft Pharmaceutical combination comprising a CDK inhibitor and a VEGF receptor inhibitor
FR2868780B1 (fr) * 2004-04-13 2008-10-17 Sanofi Synthelabo Derives de la 1-amino-phthalazine, leur preparation et leur application en therapeutique
GB0512324D0 (en) 2005-06-16 2005-07-27 Novartis Ag Organic compounds
WO2006002422A2 (en) 2004-06-24 2006-01-05 Novartis Vaccines And Diagnostics Inc. Compounds for immunopotentiation
WO2006030947A1 (ja) 2004-09-13 2006-03-23 Eisai R & D Management Co., Ltd. スルホンアミド含有化合物の血管新生阻害物質との併用
US8772269B2 (en) 2004-09-13 2014-07-08 Eisai R&D Management Co., Ltd. Use of sulfonamide-including compounds in combination with angiogenesis inhibitors
PE20060664A1 (es) * 2004-09-15 2006-08-04 Novartis Ag Amidas biciclicas como inhibidores de cinasa
JP4834553B2 (ja) 2004-09-17 2011-12-14 エーザイ・アール・アンド・ディー・マネジメント株式会社 医薬組成物
ES2325344B1 (es) * 2004-11-02 2010-06-09 Univ Madrid Autonoma Inhibidores de angiogenesis multifuncionales y multivalentes.
JP2008521900A (ja) 2004-11-30 2008-06-26 アムジエン・インコーポレーテツド キノリン及びキナゾリン類似体並びにがん治療のための医薬としてのその使用
ES2351613T3 (es) * 2005-03-03 2011-02-08 Santen Pharmaceutical Co., Ltd. Nuevo compuesto cíclico que tiene un grupo quinolilalquiltio.
US20060216288A1 (en) * 2005-03-22 2006-09-28 Amgen Inc Combinations for the treatment of cancer
US7906511B2 (en) 2005-03-31 2011-03-15 Santen Pharmaceutical Co., Ltd. Cyclic compound having pyrimidinylalkylthio group
GT200600147A (es) * 2005-04-13 2006-11-24 Uso de inhibidores de receptor de factor de crecimiento endotelial vascular para el tratamiento de canceres gastrointestinal, genitourinario, linfoide y pulmonar
CN101171013A (zh) 2005-05-02 2008-04-30 诺瓦提斯公司 嘧啶基氨基苯甲酰胺衍生物用于治疗全身性肥大细胞增多症的应用
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
EP1731153A1 (en) * 2005-06-07 2006-12-13 Schering Aktiengesellschaft Immediate-release and high-drug-load pharmaceutical formulations of non-micronised (4-chlorophenyl)¬4-(4-pyridylmethyl)phthalazin-1-yl| and salts thereof
EP1731154A1 (en) 2005-06-07 2006-12-13 Schering Aktiengesellschaft Immediate-release and high-drug-load pharmaceutical formulations of micronised (4-chlorophenyl)|4-(4-pyridylmethyl)pht halazin-1-yl| and salts thereof
EP1925676A4 (en) 2005-08-02 2010-11-10 Eisai R&D Man Co Ltd TEST METHOD FOR THE EFFECT OF A VASCULARIZATION INHIBITOR
GB0517205D0 (en) * 2005-08-22 2005-09-28 Novartis Ag Organic compounds
US7915410B2 (en) 2005-09-09 2011-03-29 Bristol-Myers Squibb Company Acyclic IKur inhibitors
EP1996550A2 (en) 2005-09-27 2008-12-03 Novartis AG Carboxyamine compounds and their use in the treatment of hdac dependent diseases
UA96139C2 (uk) 2005-11-08 2011-10-10 Дженентек, Інк. Антитіло до нейропіліну-1 (nrp1)
NO20220050A1 (no) 2005-11-21 2008-08-12 Novartis Ag Neuroendokrin tumorbehandling
US7989461B2 (en) 2005-12-23 2011-08-02 Amgen Inc. Substituted quinazolinamine compounds for the treatment of cancer
US20080108664A1 (en) * 2005-12-23 2008-05-08 Liu Belle B Solid-state form of AMG 706 and pharmaceutical compositions thereof
JO2660B1 (en) 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
AR059066A1 (es) * 2006-01-27 2008-03-12 Amgen Inc Combinaciones del inhibidor de la angiopoyetina -2 (ang2) y el inhibidor del factor de crecimiento endotelial vascular (vegf)
ES2353482T3 (es) 2006-02-10 2011-03-02 Amgen, Inc Formas hidrato de amg706.
PE20070978A1 (es) * 2006-02-14 2007-11-15 Novartis Ag COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks)
WO2007124252A2 (en) 2006-04-05 2007-11-01 Novartis Ag Combinations of therapeutic agents for treating cancer
AR060358A1 (es) * 2006-04-06 2008-06-11 Novartis Vaccines & Diagnostic Quinazolinas para la inhibicion de pdk 1
US8777120B2 (en) * 2006-04-15 2014-07-15 International Business Machines Corporation Hydronic radiant flooring heating system
PE20110235A1 (es) 2006-05-04 2011-04-14 Boehringer Ingelheim Int Combinaciones farmaceuticas que comprenden linagliptina y metmorfina
EA200802058A1 (ru) 2006-05-09 2009-06-30 Пфайзер Продактс Инк. Производные циклоалкиламинокислот и их фармацевтические композиции
KR20090007635A (ko) 2006-05-09 2009-01-19 노파르티스 아게 철 킬레이터 및 항-신생물 약제를 포함하는 조합물 및 그의용도
RU2448708C3 (ru) 2006-05-18 2017-09-28 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Противоопухолевое средство против рака щитовидной железы
GB0610925D0 (en) * 2006-06-02 2006-07-12 Novartis Ag Use of vascular endothelial growth factor receptor inhibitors for the treatment of cancer
GB0612721D0 (en) 2006-06-27 2006-08-09 Novartis Ag Organic compounds
US8217177B2 (en) 2006-07-14 2012-07-10 Amgen Inc. Fused heterocyclic derivatives and methods of use
PE20080403A1 (es) 2006-07-14 2008-04-25 Amgen Inc Derivados heterociclicos fusionados y metodos de uso
JP5238697B2 (ja) 2006-08-04 2013-07-17 武田薬品工業株式会社 縮合複素環誘導体およびその用途
US8865737B2 (en) 2006-08-28 2014-10-21 Eisai R&D Management Co., Ltd. Antitumor agent for undifferentiated gastric cancer
RU2009115954A (ru) 2006-09-29 2010-11-10 Новартис АГ (CH) Пиразолопиримидины в качестве ингибиторов липидной киназы р13к
JP5528807B2 (ja) 2006-10-12 2014-06-25 アステックス、セラピューティックス、リミテッド 複合薬剤
JP5528806B2 (ja) 2006-10-12 2014-06-25 アステックス、セラピューティックス、リミテッド 複合薬剤
EP2125781A2 (en) 2006-12-20 2009-12-02 Amgen Inc. Substituted heterocycles and methods of use
ES2449482T3 (es) 2007-01-09 2014-03-19 Amgen Inc. Derivados de bis-aril-amida útiles para el tratamiento de cáncer
WO2008093674A1 (ja) 2007-01-29 2008-08-07 Santen Pharmaceutical Co., Ltd. キナーゼ阻害活性を有する新規チアジアゾール誘導体
WO2008093855A1 (ja) 2007-01-29 2008-08-07 Eisai R & D Management Co., Ltd. 未分化型胃癌治療用組成物
US20100069458A1 (en) 2007-02-15 2010-03-18 Peter Wisdom Atadja Combination of lbh589 with other therapeutic agents for treating cancer
CA2676173A1 (en) 2007-02-16 2008-08-28 Amgen Inc. Nitrogen-containing heterocyclyl ketones and their use as c-met inhibitors
CA2689514C (en) 2007-06-05 2015-09-29 Takeda Pharmaceutical Company Limited Heterobicyclic compounds as kinase inhibitors
US20090023727A1 (en) * 2007-07-05 2009-01-22 Muhammad Hashim Javaid Phthalazinone derivatives
MX2010001918A (es) 2007-08-21 2010-03-11 Amgen Inc Proteinas enlazadas al antigeno humano de celula de cepa mcdonough de felino.
JP5270553B2 (ja) 2007-08-23 2013-08-21 武田薬品工業株式会社 複素環化合物およびその用途
CN101116664B (zh) * 2007-08-28 2010-05-19 山东省科学院生物研究所 化合物1-(4-氯苯胺基)-4-(4-甲基吡啶基)-2,3-二氮杂萘的应用
KR101513326B1 (ko) 2007-11-09 2015-04-17 에자이 알앤드디 매니지먼트 가부시키가이샤 혈관 신생 저해 물질과 항종양성 백금 착물의 병용
BRPI0820722A2 (pt) 2007-12-20 2015-06-16 Novartis Ag Derivados de tiazol usados como inibidores de pi 3 cinases
PT2260020E (pt) 2008-03-26 2014-10-28 Novartis Ag Inibidores das desacetilases b baseados no hidroxamato
UY32030A (es) 2008-08-06 2010-03-26 Boehringer Ingelheim Int "tratamiento para diabetes en pacientes inapropiados para terapia con metformina"
CN103816158A (zh) 2008-08-15 2014-05-28 勃林格殷格翰国际有限公司 用于治疗fab-相关疾病的嘌呤衍生物
US20110223241A1 (en) 2008-10-16 2011-09-15 Celator Pharmaceuticals, Inc. Combination methods and compositions
EP2399921B1 (en) 2008-12-01 2015-08-12 Takeda Pharmaceutical Company Limited Heterocyclic compound and use thereof
JO3101B1 (ar) 2008-12-02 2017-09-20 Takeda Pharmaceuticals Co مشتقات بنزوثيازول كعوامل مضادة للسرطان
KR20160064245A (ko) 2008-12-18 2016-06-07 노파르티스 아게 1-［4-［1-(4-시클로헥실-3-트리플루오로메틸-벤질옥시이미노)-에틸］-2-에틸-벤질］-아제티딘-3-카르복실산의 헤미푸마레이트 염
MX2011006610A (es) 2008-12-18 2011-06-30 Novartis Ag Nueva forma polimorfica de acido 1-(4-{l-[(e)-4-ciclohexil-3 -trifluorometil-benciloxi-imino]-etil)-2-etil-bencil)-azetidin-3 carboxilico.
ES2478842T3 (es) 2008-12-18 2014-07-23 Novartis Ag Sal clorhidrato del ácido 1-(4-(1-((E)-4-ciclohexil-3-trifluorometil-benziloxiimino)-etil)-2-etil-benzil)-azetidina-3-carboxílico
CN107011345A (zh) 2008-12-23 2017-08-04 勃林格殷格翰国际有限公司 有机化合物的盐形式
TW201036975A (en) 2009-01-07 2010-10-16 Boehringer Ingelheim Int Treatment for diabetes in patients with inadequate glycemic control despite metformin therapy
TWI466672B (zh) 2009-01-29 2015-01-01 Boehringer Ingelheim Int 小兒科病人糖尿病之治療
HRP20121006T1 (hr) 2009-01-29 2013-01-31 Novartis Ag Supstituirani benzimidazoli za lijeäśenje astrocitoma
AU2010212823B2 (en) 2009-02-13 2016-01-28 Boehringer Ingelheim International Gmbh Antidiabetic medications comprising a DPP-4 inhibitor (linagliptin) optionally in combination with other antidiabetics
WO2010108503A1 (en) 2009-03-24 2010-09-30 Life & Brain Gmbh Promotion of neuronal integration in neural stem cell grafts
WO2010120386A1 (en) 2009-04-17 2010-10-21 Nektar Therapeutics Oligomer-protein tyrosine kinase inhibitor conjugates
UY32730A (es) 2009-06-26 2011-01-31 Novartis Ag Inhibidores de cyp17
US8293753B2 (en) 2009-07-02 2012-10-23 Novartis Ag Substituted 2-carboxamide cycloamino ureas
US8389526B2 (en) 2009-08-07 2013-03-05 Novartis Ag 3-heteroarylmethyl-imidazo[1,2-b]pyridazin-6-yl derivatives
CA2770873A1 (en) 2009-08-12 2011-02-17 Novartis Ag Heterocyclic hydrazone compounds and their uses to treat cancer and inflammation
GEP201706639B (en) 2009-08-17 2017-03-27 Intellikine Llc Heterocyclic compounds and uses thereof
TH121482A (th) 2009-08-19 2013-02-28 นางสาวปัณณพัฒน์ เหลืองธาตุทอง องค์ประกอบทางเภสัชกรรมที่ประกอบด้วยอนุพันธ์ของควิโนลีน
CA2771432A1 (en) 2009-08-20 2011-02-24 Novartis Ag Heterocyclic oxime compounds
IN2012DN01693A (enExample) 2009-08-26 2015-06-05 Novartis Ag
WO2011029915A1 (en) 2009-09-10 2011-03-17 Novartis Ag Ether derivatives of bicyclic heteroaryls
ES2942185T3 (es) 2009-10-02 2023-05-30 Boehringer Ingelheim Int Composiciones farmacéuticas que comprenden BI-1356 y metformina
EA201200651A1 (ru) 2009-11-04 2012-12-28 Новартис Аг Гетероциклические сульфонамидные производные, применимые в качестве ингибиторов мек
US20120289501A1 (en) 2009-11-25 2012-11-15 Novartis Ag Benzene-fused 6-membered oxygen-containing heterocyclic derivatives of bicyclic heteroaryls
EP2504002B1 (en) 2009-11-27 2019-10-09 Boehringer Ingelheim International GmbH Treatment of genotyped diabetic patients with dpp-iv inhibitors such as linagliptin
ES2484171T3 (es) 2009-12-08 2014-08-11 Novartis Ag Derivados de sulfonamidas heterocíclicas
CU24130B1 (es) 2009-12-22 2015-09-29 Novartis Ag Isoquinolinonas y quinazolinonas sustituidas
US8440693B2 (en) 2009-12-22 2013-05-14 Novartis Ag Substituted isoquinolinones and quinazolinones
WO2011113947A1 (en) 2010-03-18 2011-09-22 Boehringer Ingelheim International Gmbh Combination of a gpr119 agonist and the dpp-iv inhibitor linagliptin for use in the treatment of diabetes and related conditions
KR101927068B1 (ko) 2010-05-05 2018-12-10 베링거 인겔하임 인터내셔날 게엠베하 체중 감소 치료에 후속하는 dpp-4 억제제에 의한 순차적 병용 요법
EP2582680A1 (en) 2010-06-17 2013-04-24 Novartis AG Biphenyl substituted 1,3-dihydro-benzoimidazol-2-ylideneamine derivatives
EP2582681A1 (en) 2010-06-17 2013-04-24 Novartis AG Piperidinyl substituted 1,3-dihydro-benzoimidazol-2-ylideneamine derivatives
WO2011161217A2 (en) 2010-06-23 2011-12-29 Palacký University in Olomouc Targeting of vegfr2
KR20200028498A (ko) 2010-06-24 2020-03-16 베링거 인겔하임 인터내셔날 게엠베하 당뇨병 요법
AU2011270165B2 (en) 2010-06-25 2015-12-24 Eisai R&D Management Co., Ltd. Antitumor agent using compounds having kinase inhibitory effect in combination
JP2013539962A (ja) 2010-07-09 2013-10-31 ジェネンテック， インコーポレイテッド 抗ニューロピリン抗体及び使用方法
AR082418A1 (es) 2010-08-02 2012-12-05 Novartis Ag Formas cristalinas de 1-(4-metil-5-[2-(2,2,2-trifluoro-1,1-dimetil-etil)-piridin-4-il]-tiazol-2-il)-amida de 2-amida del acido (s)-pirrolidin-1,2-dicarboxilico
EP2627648A1 (en) 2010-09-16 2013-08-21 Novartis AG 17aHYDROXYLASE/C17,20-LYASE INHIBITORS
AR083878A1 (es) 2010-11-15 2013-03-27 Boehringer Ingelheim Int Terapia antidiabetica vasoprotectora y cardioprotectora, linagliptina, metodo de tratamiento
CA2817564A1 (en) 2010-11-18 2012-05-24 Ronald K. Blackman Preselection of subjects for therapeutic treatment based on hypoxic status
JP2014503500A (ja) 2010-11-18 2014-02-13 シンタ ファーマスーティカルズ コーポレーション 低酸素状態に基づく酸素感受性薬剤による治療に適した被験体の事前選択
MX343706B (es) 2011-01-31 2016-11-18 Novartis Ag Derivados heterocíclicos novedosos.
JP2014505088A (ja) 2011-02-10 2014-02-27 ノバルティス アーゲー Ｃ−ＭＥＴチロシンキナーゼ阻害剤としての［１，２，４］トリアゾロ［４，３−ｂ］ピリダジン化合物
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
US20130338152A1 (en) 2011-03-08 2013-12-19 Irm Llc Fluorophenyl bicyclic heteroaryl compounds
PT2688887E (pt) 2011-03-23 2015-07-06 Amgen Inc Inibidores duais tricíclicos fusionados de cdk 4/6 e flt3
WO2012144463A1 (ja) 2011-04-18 2012-10-26 エーザイ・アール・アンド・ディー・マネジメント株式会社 腫瘍治療剤
MX359399B (es) 2011-04-28 2018-09-27 Novartis Ag Inhibidores de 17alfa-hidroxilasa/c17-20-liasa.
EP3444363B1 (en) 2011-06-03 2020-11-25 Eisai R&D Management Co., Ltd. Biomarkers for prediciting and assessing responsiveness of thyroid and kidney cancer subjects to lenvatinib compounds
KR20140034898A (ko) 2011-06-09 2014-03-20 노파르티스 아게 헤테로시클릭 술폰아미드 유도체
US9346749B2 (en) * 2011-06-16 2016-05-24 Korea Research Institute Of Chemical Technology 1,3-di-oxo-indene derivative, pharmaceutically acceptable salt or optical isomer thereof, preparation method thereof, and pharmaceutical composition containing same as an antiviral, active ingredient
US8859535B2 (en) 2011-06-20 2014-10-14 Novartis Ag Hydroxy substituted isoquinolinone derivatives
WO2012175487A1 (en) 2011-06-20 2012-12-27 Novartis Ag Cyclohexyl isoquinolinone compounds
HUE061596T2 (hu) 2011-07-15 2023-07-28 Boehringer Ingelheim Int Szubsztituált dimer kinazolin származék, annak elõállítása és alkalmazása az I. és II. típusú cukorbetegség kezelésére szolgáló gyógyszerkészítményekben
WO2013025939A2 (en) 2011-08-16 2013-02-21 Indiana University Research And Technology Corporation Compounds and methods for treating cancer by inhibiting the urokinase receptor
WO2014081405A2 (en) 2011-08-17 2014-05-30 Dennis Brown Compositions and methods to improve the therapeutic benefit of suboptimally administered chemical compounds including substituted hexitols such as dibromodulcitol
AU2012310168B2 (en) 2011-09-15 2015-07-16 Novartis Ag 6 - substituted 3 - (quinolin- 6 - ylthio) - [1,2,4] triazolo [4, 3 -a] pyradines as tyrosine kinase
BR112014009890A2 (pt) 2011-10-28 2020-10-27 Novartis Ag derivados de purina e seu uso no tratamento de doença
WO2013080141A1 (en) 2011-11-29 2013-06-06 Novartis Ag Pyrazolopyrrolidine compounds
BR112014015322A8 (pt) 2011-12-23 2017-06-13 Novartis Ag compostos e composições para inibir a interação de bcl2 com parceiros de ligação
CA2859873A1 (en) 2011-12-23 2013-06-27 Novartis Ag Compounds for inhibiting the interaction of bcl2 with binding partners
WO2013096055A1 (en) 2011-12-23 2013-06-27 Novartis Ag Compounds for inhibiting the interaction of bcl2 with binding partners
MX2014007731A (es) 2011-12-23 2015-01-12 Novartis Ag Compuestos para inhibir la interaccion de bcl2 con los componentes de enlace.
CN104125955A (zh) 2011-12-23 2014-10-29 诺华股份有限公司 用于抑制bcl2与结合配偶体相互作用的化合物
US20130172244A1 (en) 2011-12-29 2013-07-04 Thomas Klein Subcutaneous therapeutic use of dpp-4 inhibitor
US8815926B2 (en) 2012-01-26 2014-08-26 Novartis Ag Substituted pyrrolo[3,4-D]imidazoles for the treatment of MDM2/4 mediated diseases
AR090263A1 (es) 2012-03-08 2014-10-29 Hoffmann La Roche Terapia combinada de anticuerpos contra el csf-1r humano y las utilizaciones de la misma
EP3964513A1 (en) 2012-04-03 2022-03-09 Novartis AG Combination products with tyrosine kinase inhibitors and their use
US20130303462A1 (en) 2012-05-14 2013-11-14 Boehringer Ingelheim International Gmbh Use of a dpp-4 inhibitor in podocytes related disorders and/or nephrotic syndrome
ES2929025T3 (es) 2012-05-14 2022-11-24 Boehringer Ingelheim Int Linagliptina, un derivado de xantina como inhibidor de dpp-4, para su uso en el tratamiento del SRIS y/o de la septicemia
BR112014028420A2 (pt) 2012-05-16 2017-09-19 Novartis Ag regime de dosagem para um inibidor de quinase pi-3
CN104321325B (zh) 2012-05-24 2016-11-16 诺华股份有限公司 吡咯并吡咯烷酮化合物
WO2013174767A1 (en) 2012-05-24 2013-11-28 Boehringer Ingelheim International Gmbh A xanthine derivative as dpp -4 inhibitor for use in modifying food intake and regulating food preference
JP6374862B2 (ja) 2012-05-24 2018-08-15 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 自己免疫性糖尿病、特に、ｌａｄａの治療に使用するためのｄｐｐ−４阻害剤としてのキサンチン誘導体
CA2880896C (en) 2012-06-26 2021-11-16 Del Mar Pharmaceuticals Methods for treating tyrosine-kinase-inhibitor-resistant malignancies in patients with genetic polymorphisms or ahi1 dysregulations or mutations employing dianhydrogalactitol, diacetyldianhydrogalactitol, dibromodulcitol, or analogs or derivatives thereof
US9505749B2 (en) 2012-08-29 2016-11-29 Amgen Inc. Quinazolinone compounds and derivatives thereof
US9790197B2 (en) 2012-12-14 2017-10-17 Katholieke Universiteit Leuven K.U. Leuven R & D Compound, pharmaceutically acceptable salt or optical isomer thereof, method for preparing the same, and pharmaceutical composition for prevention or treatment of viral diseases containing same as active ingredient
RU2015115397A (ru) 2012-12-21 2017-01-25 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Аморфная форма производного хинолина и способ его получения
WO2014115077A1 (en) 2013-01-22 2014-07-31 Novartis Ag Substituted purinone compounds
WO2014115080A1 (en) 2013-01-22 2014-07-31 Novartis Ag Pyrazolo[3,4-d]pyrimidinone compounds as inhibitors of the p53/mdm2 interaction
WO2014124860A1 (en) 2013-02-14 2014-08-21 Boehringer Ingelheim International Gmbh Specific pde4b-inhibitors for the treatment of diabetes mellitus
WO2014140284A1 (en) 2013-03-15 2014-09-18 Boehringer Ingelheim International Gmbh Use of linagliptin in cardio- and renoprotective antidiabetic therapy
WO2014151147A1 (en) 2013-03-15 2014-09-25 Intellikine, Llc Combination of kinase inhibitors and uses thereof
WO2014155268A2 (en) 2013-03-25 2014-10-02 Novartis Ag Fgf-r tyrosine kinase activity inhibitors - use in diseases associated with lack of or reduced snf5 activity
CN105492011A (zh) 2013-04-08 2016-04-13 丹尼斯·M·布朗 不理想给药化学化合物的治疗增效
ES2687968T3 (es) 2013-05-14 2018-10-30 Eisai R&D Management Co., Ltd. Biomarcadores para pronosticar y evaluar la reactividad de sujetos con cáncer de endometrio a compuestos con lenvatinib
WO2015022664A1 (en) 2013-08-14 2015-02-19 Novartis Ag Compounds and compositions as inhibitors of mek
WO2015022663A1 (en) 2013-08-14 2015-02-19 Novartis Ag Compounds and compositions as inhibitors of mek
US9227969B2 (en) 2013-08-14 2016-01-05 Novartis Ag Compounds and compositions as inhibitors of MEK
TW201605450A (zh) 2013-12-03 2016-02-16 諾華公司 Ｍｄｍ２抑制劑與ＢＲＡＦ抑制劑之組合及其用途
PL3076969T3 (pl) 2013-12-06 2022-01-17 Novartis Ag Schemat dawkowania selektywnego inhibitora 3-kinazy fosfatydynozytolu alfa-izoformy
BR112017001695A2 (pt) 2014-07-31 2017-11-21 Novartis Ag terapia de combinação
KR20230043234A (ko) 2014-08-28 2023-03-30 에자이 알앤드디 매니지먼트 가부시키가이샤 고순도의 퀴놀린 유도체 및 이를 제조하는 방법
EP3233918A1 (en) 2014-12-19 2017-10-25 Novartis AG Combination therapies
AU2016205311B2 (en) 2015-01-08 2022-02-17 The Board Of Trustees Of The Leland Stanford Junior University Factors and cells that provide for induction of bone, bone marrow, and cartilage
US20180093956A1 (en) * 2015-02-06 2018-04-05 Abbvie Inc. Substituted phthalazines
LT3263106T (lt) 2015-02-25 2024-01-10 Eisai R&D Management Co., Ltd. Chinolino darinių kartumo sumažinimo būdas
KR102662228B1 (ko) 2015-03-04 2024-05-02 머크 샤프 앤드 돔 코포레이션 암을 치료하기 위한 pd-1 길항제 및 vegfr/fgfr/ret 티로신 키나제 억제제의 조합
CA2979215A1 (en) 2015-03-10 2016-09-15 Aduro Biotech, Inc. Compositions and methods for activating "stimulator of interferon gene"-dependent signalling
MX373231B (es) 2015-06-16 2020-05-08 Eisai R&D Man Co Ltd Agente anticancerigeno.
CA2994925C (en) 2015-08-20 2023-08-29 Eisai R&D Management Co., Ltd. Tumor therapeutic agent
MX2018005298A (es) 2015-11-02 2018-06-22 Novartis Ag Regimen de dosificacion para un inhibidor de fosfatidilinositol 3-quinasa.
BR112018072401A2 (pt) 2016-06-10 2019-02-19 Boehringer Ingelheim International Gmbh combinações de linagliptina e metformina
WO2018009466A1 (en) 2016-07-05 2018-01-11 Aduro Biotech, Inc. Locked nucleic acid cyclic dinucleotide compounds and uses thereof
WO2018060833A1 (en) 2016-09-27 2018-04-05 Novartis Ag Dosage regimen for alpha-isoform selective phosphatidylinositol 3-kinase inhibitor alpelisib
NZ754994A (en) 2016-12-22 2022-12-23 Amgen Inc Benzisothiazole, isothiazolo[3,4-b]pyridine, quinazoline, phthalazine, pyrido[2,3-d]pyridazine and pyrido[2,3-d]pyrimidine derivatives as kras g12c inhibitors for treating lung, pancreatic or colorectal cancer
US12303505B2 (en) 2017-02-08 2025-05-20 Eisai R&D Management Co., Ltd. Tumor-treating pharmaceutical composition
UY37695A (es) 2017-04-28 2018-11-30 Novartis Ag Compuesto dinucleótido cíclico bis 2’-5’-rr-(3’f-a)(3’f-a) y usos del mismo
BR112019023064A2 (pt) 2017-05-16 2020-06-09 Eisai R&D Man Co Ltd tratamento de carcinoma hepatocelular
JOP20190272A1 (ar) 2017-05-22 2019-11-21 Amgen Inc مثبطات kras g12c وطرق لاستخدامها
ES2928576T3 (es) 2017-09-08 2022-11-21 Amgen Inc Inhibidores de KRAS G12C y métodos de uso de los mismos
WO2019077037A1 (en) 2017-10-18 2019-04-25 Chemotherapeutisches Forschungsinstitut Georg-Speyer-Haus METHODS AND COMPOUNDS FOR ENHANCED IMMUNE CELL THERAPY
AU2017444054B2 (en) 2017-12-21 2021-10-07 Hefei Institutes Of Physical Science, Chinese Academy Of Sciences Class of pyrimidine derivative kinase inhibitors
MA52501A (fr) 2018-05-04 2021-03-10 Amgen Inc Inhibiteurs de kras g12c et leurs procédés d'utilisation
CA3099118A1 (en) 2018-05-04 2019-11-07 Amgen Inc. Kras g12c inhibitors and methods of using the same
EP3790886B1 (en) 2018-05-10 2024-06-26 Amgen Inc. Kras g12c inhibitors for the treatment of cancer
EP3802535B1 (en) 2018-06-01 2022-12-14 Amgen, Inc Kras g12c inhibitors and methods of using the same
CA3099799A1 (en) 2018-06-11 2019-12-19 Amgen Inc. Kras g12c inhibitors for treating cancer
MA51848A (fr) 2018-06-12 2021-04-21 Amgen Inc Inhibiteurs de kras g12c et leurs procédés d'utilisation
BR112020024793A2 (pt) 2018-07-17 2021-03-02 Boehringer Ingelheim International Gmbh terapia antidiabética cardiossegura
BR112020026164A2 (pt) 2018-07-17 2021-03-23 Boehringer Ingelheim International Gmbh terapia antidiabética cardioprotetora e nefroprotetora
JP7516029B2 (ja) 2018-11-16 2024-07-16 アムジエン・インコーポレーテツド Ｋｒａｓ ｇ１２ｃ阻害剤化合物の重要な中間体の改良合成法
US11053226B2 (en) 2018-11-19 2021-07-06 Amgen Inc. KRAS G12C inhibitors and methods of using the same
JP7377679B2 (ja) 2018-11-19 2023-11-10 アムジエン・インコーポレーテツド がん治療のためのｋｒａｓｇ１２ｃ阻害剤及び１種以上の薬学的に活性な追加の薬剤を含む併用療法
AU2019401495B2 (en) 2018-12-20 2025-06-26 Amgen Inc. Heteroaryl amides useful as KIF18A inhibitors
MA54550A (fr) 2018-12-20 2022-03-30 Amgen Inc Inhibiteurs de kif18a
MA54546A (fr) 2018-12-20 2022-03-30 Amgen Inc Amides d'hétéroaryle utiles en tant qu'inhibiteurs de kif18a
EA202191730A1 (ru) 2018-12-20 2021-08-24 Эмджен Инк. Ингибиторы kif18a
CN113727758A (zh) 2019-03-01 2021-11-30 锐新医药公司 双环杂环基化合物及其用途
KR20210146287A (ko) 2019-03-01 2021-12-03 레볼루션 메디슨즈, 인크. 이환식 헤테로아릴 화합물 및 이의 용도
BR112021022734A2 (pt) * 2019-05-14 2022-03-08 Scripps Research Inst Compostos para tratamento de distúrbios neurodegenerativos e metabólicos
EP3738593A1 (en) 2019-05-14 2020-11-18 Amgen, Inc Dosing of kras inhibitor for treatment of cancers
EP3972973A1 (en) 2019-05-21 2022-03-30 Amgen Inc. Solid state forms
CN114391012B (zh) 2019-08-02 2025-10-31 美国安进公司 作为kif18a抑制剂的吡啶衍生物
JP7640521B2 (ja) 2019-08-02 2025-03-05 アムジエン・インコーポレーテツド Ｋｉｆ１８ａ阻害剤として有用なヘテロアリールアミド
ES3051918T3 (en) 2019-08-02 2025-12-30 Amgen Inc Kif18a inhibitors
WO2021026098A1 (en) 2019-08-02 2021-02-11 Amgen Inc. Kif18a inhibitors
EP4048671B1 (en) 2019-10-24 2026-03-18 Amgen Inc. Pyridopyrimidine derivatives useful as kras g12c and kras g12d inhibitors in the treatment of cancer
JP7823816B2 (ja) 2019-11-04 2026-03-04 レヴォリューション・メディスンズ，インコーポレイテッド Ｒａｓ阻害剤
EP4054719B1 (en) 2019-11-04 2026-02-11 Revolution Medicines, Inc. Ras inhibitors
KR20220109407A (ko) 2019-11-04 2022-08-04 레볼루션 메디슨즈, 인크. Ras 억제제
BR112022008858A2 (pt) 2019-11-08 2022-09-06 Revolution Medicines Inc Composto, composição farmacêutica e métodos para inibir sos1 em um sujeito, para inibir a interação de sos1 e uma proteína, para tratar ou prevenir uma doença e para tratar ou prevenir câncer
JP2023501528A (ja) 2019-11-14 2023-01-18 アムジエン・インコーポレーテツド Ｋｒａｓ ｇ１２ｃ阻害剤化合物の改善された合成
WO2021097207A1 (en) 2019-11-14 2021-05-20 Amgen Inc. Improved synthesis of kras g12c inhibitor compound
US20220395553A1 (en) 2019-11-14 2022-12-15 Cohbar, Inc. Cxcr4 antagonist peptides
WO2021108683A1 (en) 2019-11-27 2021-06-03 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
CN114929279A (zh) 2020-01-07 2022-08-19 锐新医药公司 Shp2抑制剂给药和治疗癌症的方法
US12286423B2 (en) 2020-04-20 2025-04-29 Novartis Ag Antiviral 1,3-di-oxo-indene compounds
KR20230024887A (ko) 2020-04-20 2023-02-21 노파르티스 아게 항바이러스성 1,3-디-옥소-인덴 화합물
CA3183032A1 (en) 2020-06-18 2021-12-23 Mallika Singh Methods for delaying, preventing, and treating acquired resistance to ras inhibitors
MX2023002248A (es) 2020-09-03 2023-05-16 Revolution Medicines Inc Uso de inhibidores de sos1 para tratar neoplasias malignas con mutaciones de shp2.
CR20230165A (es) 2020-09-15 2023-06-02 Revolution Medicines Inc Derivados indólicos como inhibidores de ras en el tratamiento del cáncer
CN117396472A (zh) 2020-12-22 2024-01-12 上海齐鲁锐格医药研发有限公司 Sos1抑制剂及其用途
CN117355303A (zh) * 2021-01-28 2024-01-05 佛罗里达大学研究基金会公司 化合物及其用于治疗神经退行性、退行性和代谢病症的用途
IL308193A (en) 2021-05-05 2024-01-01 Revolution Medicines Inc RAS inhibitors
CR20230558A (es) 2021-05-05 2024-01-24 Revolution Medicines Inc Inhibidores de ras para el tratamiento del cáncer
WO2022235866A1 (en) 2021-05-05 2022-11-10 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
US20250059182A1 (en) * 2021-06-21 2025-02-20 Mirati Therapeutics, Inc. Sos1 inhibitors
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
JP2025500878A (ja) 2021-12-17 2025-01-15 ジェンザイム・コーポレーション Ｓｈｐ２阻害剤としてのピラゾロピラジン化合物
KR20230098078A (ko) * 2021-12-24 2023-07-03 제일약품주식회사 신규한 바이사이클릭 헤테로사이클릴 화합물 및 이의 용도
EP4227307A1 (en) 2022-02-11 2023-08-16 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
IL314883A (en) 2022-03-07 2024-10-01 Amgen Inc A process for preparing 4-methyl-2-propan-2-yl-pyridine-3-carbonitrile
CN119136806A (zh) 2022-03-08 2024-12-13 锐新医药公司 用于治疗免疫难治性肺癌的方法
WO2023240263A1 (en) 2022-06-10 2023-12-14 Revolution Medicines, Inc. Macrocyclic ras inhibitors
PE20251879A1 (es) 2022-10-14 2025-07-22 Black Diamond Therapeutics Inc Metodos de tratamiento del cancer usando derivados de isoquinolina o 6-aza-quinolina
AU2024241633A1 (en) 2023-03-30 2025-11-06 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof
WO2024211663A1 (en) 2023-04-07 2024-10-10 Revolution Medicines, Inc. Condensed macrocyclic compounds as ras inhibitors
PE20260039A1 (es) 2023-04-07 2026-01-09 Revolution Medicines Inc Inhibidores macrociclicos de ras
TW202448897A (zh) 2023-04-14 2024-12-16 美商銳新醫藥公司 Ｒａｓ抑制劑之結晶形式、含有其之組合物及其使用方法
CN121100123A (zh) 2023-04-14 2025-12-09 锐新医药公司 Ras抑制剂的结晶形式
WO2024229406A1 (en) 2023-05-04 2024-11-07 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
US20250049810A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
TW202530228A (zh) 2023-10-12 2025-08-01 美商銳新醫藥公司 Ｒａｓ抑制劑
TW202542151A (zh) 2023-12-22 2025-11-01 美商銳格醫藥有限公司 Ｓｏｓ１抑制劑及其用途
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
TW202547461A (zh) 2024-05-17 2025-12-16 美商銳新醫藥公司 Ｒａｓ抑制劑
WO2025255438A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025265060A1 (en) 2024-06-21 2025-12-26 Revolution Medicines, Inc. Therapeutic compositions and methods for managing treatment-related effects
WO2026006747A1 (en) 2024-06-28 2026-01-02 Revolution Medicines, Inc. Ras inhibitors
WO2026015790A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015796A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
WO2026050446A1 (en) 2024-08-29 2026-03-05 Revolution Medicines, Inc. Ras inhibitors

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BE567431A (enExample) * 1957-05-07
US2960504A (en) 1957-05-07 1960-11-15 Ciba Pharm Prod Inc 1-hydrazino, 4-pyridyl methyl-phthalazines
GB1094044A (en) 1965-07-12 1967-12-06 Vantorex Ltd Phthalazine derivatives
DE1695994A1 (de) 1967-05-05 1971-05-19 Vantorex Ltd Verfahren zur Herstellung von Phthalazinen
GB1293565A (en) 1969-05-03 1972-10-18 Aspro Nicholas Ltd Aminophthalazines and pharmaceutical compositions thereof
JPH03106875A (ja) * 1989-09-20 1991-05-07 Morishita Pharmaceut Co Ltd １―（３―ピリジルメチル）フタラジン誘導体
EP0600831A1 (de) 1992-11-27 1994-06-08 Ciba-Geigy Ag Phthalazinonderivate
UA32427C2 (uk) * 1993-10-15 2000-12-15 Елі Ліллі Енд Компані Застосування бензотіофенів або їх фармацевтично прийнятних солей або сольватів для інгібування ангіогенезу і/або ангіогенних захворювань
CA2173493C (en) * 1994-08-09 2008-03-25 Nobuhisa Watanabe Fused pyridazine compounds
CA2237273C (en) * 1996-01-15 2009-01-13 Janssen Pharmaceutica N.V. Angiogenesis inhibiting pyridazinamines
DE19617863A1 (de) 1996-04-23 1997-10-30 Schering Ag Phthalazinderivate, deren Herstellung und Verwendung als Arzneimittel
CO4950519A1 (es) * 1997-02-13 2000-09-01 Novartis Ag Ftalazinas, preparaciones farmaceuticas que las comprenden y proceso para su preparacion
ITMI981670A1 (it) * 1998-07-21 2000-01-21 Zambon Spa Derivati ftalazinici inibitori della fosfodiesterasi 4
EP1105136B1 (en) * 1998-08-13 2007-08-29 Novartis AG Method for treating ocular neovascular diseases

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