TWI250151B - Phthalazine derivatives and pharmaceutical composition comprising same - Google Patents

Phthalazine derivatives and pharmaceutical composition comprising same Download PDF

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Publication number
TWI250151B
TWI250151B TW087102062A TW87102062A TWI250151B TW I250151 B TWI250151 B TW I250151B TW 087102062 A TW087102062 A TW 087102062A TW 87102062 A TW87102062 A TW 87102062A TW I250151 B TWI250151 B TW I250151B
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TW
Taiwan
Prior art keywords
group
compound
formula
pyridylmethyl
alkyl
Prior art date
Application number
TW087102062A
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English (en)
Chinese (zh)
Inventor
Guido Bold
Jorg Frei
Peter Traxler
Karl-Heinz Altmann
Helmut Mett
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
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Publication of TWI250151B publication Critical patent/TWI250151B/zh

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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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyridine Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
TW087102062A 1997-02-13 1998-03-17 Phthalazine derivatives and pharmaceutical composition comprising same TWI250151B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CH31597 1997-02-13

Publications (1)

Publication Number Publication Date
TWI250151B true TWI250151B (en) 2006-03-01

Family

ID=4184213

Family Applications (1)

Application Number Title Priority Date Filing Date
TW087102062A TWI250151B (en) 1997-02-13 1998-03-17 Phthalazine derivatives and pharmaceutical composition comprising same

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 (302)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9718972D0 (en) 1996-09-25 1997-11-12 Zeneca Ltd Chemical compounds
US6809097B1 (en) 1996-09-25 2004-10-26 Zeneca Limited Quinoline derivatives inhibiting the effect of growth factors such as VEGF
CO4950519A1 (es) * 1997-02-13 2000-09-01 Novartis Ag Ftalazinas, preparaciones farmaceuticas que las comprenden y proceso para su preparacion
AU8816298A (en) 1997-08-22 1999-03-16 Zeneca Limited Oxindolylquinazoline derivatives as angiogenesis inhibitors
EP1107964B8 (en) * 1998-08-11 2010-04-07 Novartis AG Isoquinoline derivatives with angiogenesis inhibiting activity
PT1105136E (pt) * 1998-08-13 2007-12-03 Novartis Ag Método para tratar doenças oculares neovasculares
EP1165085B1 (en) 1999-03-30 2006-06-14 Novartis AG Phthalazine derivatives for treating inflammatory 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
US6271233B1 (en) 1999-08-10 2001-08-07 Ciba Vision Corporation Method for treating ocular neovascular diseases
CO5200835A1 (es) * 1999-09-28 2002-09-27 Bayer Corp Piridinas y piridacinas sustituidas con actividad de inhibicion de angiogenesis
US6689883B1 (en) 1999-09-28 2004-02-10 Bayer Pharmaceuticals Corporation Substituted pyridines and pyridazines with angiogenesis inhibiting activity
EE05330B1 (et) 1999-11-05 2010-08-16 Astrazeneca Ab Kinasoliini derivaadid kui VEGF-i inhibiitorid
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
CN1240688C (zh) 2000-04-07 2006-02-08 阿斯特拉曾尼卡有限公司 喹唑啉化合物
US7977333B2 (en) 2000-04-20 2011-07-12 Bayer Healthcare Llc Substituted pyridines and pyridazines with angiogenesis inhibiting activity
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
PL359653A1 (en) * 2000-06-23 2004-08-23 Schering Aktiengesellschaft Combinations and compositions which interfere with vegf/vegf and angiopoietin/tie receptor function and their use (ii)
MXPA03000874A (es) * 2000-08-09 2003-06-06 Astrazeneca Ab Compuestos quimicos.
US6903101B1 (en) * 2000-08-10 2005-06-07 Bayer Pharmaceuticals Corporation Substituted pyridazines and fused pyridazines with angiogenesis inhibiting activity
WO2002032872A1 (fr) 2000-10-20 2002-04-25 Eisai Co., Ltd. Composes a noyau aromatique azote
BR0115062A (pt) * 2000-10-30 2004-02-17 Kudos Pharm Ltd Derivados de ftalazinona
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
PT2269603E (pt) 2001-02-19 2015-09-09 Novartis Ag Tratamento de tumores da mama com um derivado de rapamicina em combinação com exemestano
GB0111078D0 (en) * 2001-05-04 2001-06-27 Novartis Ag Organic compounds
PT1392313E (pt) 2001-05-16 2007-07-17 Novartis Ag Combinação que compreende n - ( 5- [ 4- ( metil-piperazinomrtil ) - benxoilamido ] - 2 -metilfenil ) - 4 -( 3 - piridil ) - 2 - pirimidina-amina e um agente quimioterapêutico
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
CN1330308C (zh) * 2001-09-12 2007-08-08 诺瓦提斯公司 含有4－吡啶基甲基酞嗪的联合产品及其应用
RU2320344C2 (ru) * 2001-09-12 2008-03-27 Новартис Аг Применение 4-пиридилметилфталазинов для лечения рака
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
CN100506224C (zh) * 2001-10-25 2009-07-01 诺瓦提斯公司 包含选择性环加氧酶-2抑制剂的组合
CA2471314A1 (en) * 2001-12-21 2003-07-24 Bayer Pharmaceuticals Corporation Anti-angiogenesis combination therapies comprising pyridazine or pyridine derivatives
IL162203A0 (en) 2001-12-27 2005-11-20 Theravance Inc Indolinone derivatives useful as protein inase 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
PL372103A1 (en) * 2002-05-16 2005-07-11 Novartis Ag Use of edg receptor binding agents in cancer
JP2005531622A (ja) * 2002-06-28 2005-10-20 ノバルティス アクチエンゲゼルシャフト 血管沈静化合物とアルキル化剤を含む腫瘍処置用の組合せ剤
WO2004015082A2 (en) * 2002-08-09 2004-02-19 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
AU2003288034A1 (en) * 2002-11-12 2004-06-03 Novartis Ag Treatment of mesothelioma
US7094785B1 (en) 2002-12-18 2006-08-22 Cornell Research Foundation, Inc. Method of treating polycythemia vera
JP2006512360A (ja) * 2002-12-20 2006-04-13 ダナ−ファーバー　キャンサー　インスティテュート，インコーポレイテッド ＶｏｎＨｉｐｐｅｌ−Ｌｉｎｄａｕ病の処置
WO2004058234A2 (en) * 2002-12-27 2004-07-15 Schering Aktiengesellschaft Pharmaceutical combinations of phthalazine vegf inhibitors and benzamide hdac inhibitors
EP2527326B1 (en) 2003-03-07 2014-10-08 Santen Pharmaceutical Co., Ltd Novel compounds having 4-pyridylalkylthio group as substituent
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
WO2004099158A1 (en) * 2003-04-30 2004-11-18 Ricerca Biosciences, Llc. Monocyclic diazodioxide based bcl-2 protein antagonists
AU2004251146A1 (en) 2003-05-19 2005-01-06 Irm, Llc Immunosuppressant compounds and compositions
MY150088A (en) 2003-05-19 2013-11-29 Irm Llc Immunosuppressant compounds and compositions
RS53476B (sr) 2003-07-18 2014-12-31 Amgen Fremont Inc. Sredstva za specifično vezivanje faktora rasta hepatocita
EP1683785B1 (en) 2003-11-11 2013-10-16 Eisai R&D Management Co., Ltd. Urea derivative and process for producing the same
DE602004020654D1 (de) 2003-11-18 2009-05-28 Novartis Ag Hemmer der mutanten form von kit
US20050171182A1 (en) * 2003-12-11 2005-08-04 Roger Briesewitz Methods and compositions for use in the treatment of mutant receptor tyrosine kinase driven cellular proliferative diseases
KR101179840B1 (ko) 2004-02-17 2012-09-04 산텐 세이야꾸 가부시키가이샤 치환 또는 무치환 아미노기를 도입한 4-피리딜알킬티오기를갖는 신규 고리형 화합물
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
EP1765313A2 (en) 2004-06-24 2007-03-28 Novartis Vaccines and Diagnostics, Inc. Compounds for immunopotentiation
WO2006030941A1 (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
WO2006030826A1 (ja) 2004-09-17 2006-03-23 Eisai R & D Management Co., Ltd. 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
EP1854787B1 (en) * 2005-03-03 2010-09-01 Santen Pharmaceutical Co., Ltd. Novel cyclic compound having quinolylalkylthio group
US20060216288A1 (en) * 2005-03-22 2006-09-28 Amgen Inc Combinations for the treatment of cancer
ES2548729T3 (es) 2005-03-31 2015-10-20 Santen Pharmaceutical Co., Ltd. Nuevo compuesto cíclico que tiene grupo pirimidinilalquiltio
WO2006113172A1 (en) * 2005-04-13 2006-10-26 Novartis Ag Use of vascular endothelial growth factor receptor inhibitors for the treatment of gastrointestinal, genitourinary, lymphoid and pulmonary cancers
JP5129123B2 (ja) 2005-05-02 2013-01-23 ノバルティス アーゲー 全身性肥満細胞症の処置のためのピリミジルアミノベンズアミド誘導体の使用
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
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
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
JP4989476B2 (ja) 2005-08-02 2012-08-01 エーザイ・アール・アンド・ディー・マネジメント株式会社 血管新生阻害物質の効果を検定する方法
GB0517205D0 (en) * 2005-08-22 2005-09-28 Novartis Ag Organic compounds
EP1922311A2 (en) 2005-09-09 2008-05-21 Brystol-Myers Squibb Company Acyclic ikur inhibitors
KR20080054417A (ko) 2005-09-27 2008-06-17 노파르티스 아게 카르복시아민 화합물 및 ｈｄａｃ 의존성 질환의 치료에있어서의 그의 용도
UA96139C2 (uk) 2005-11-08 2011-10-10 Дженентек, Інк. Антитіло до нейропіліну-1 (nrp1)
AU2006314444C1 (en) 2005-11-21 2018-01-04 Novartis Ag Neuroendocrine tumor treatment using mTOR inhibitors
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)
JP2009526050A (ja) 2006-02-10 2009-07-16 アムジエン・インコーポレーテツド Ａｍｇ７０６の水和物形態
PE20070978A1 (es) * 2006-02-14 2007-11-15 Novartis Ag COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks)
CN101415409B (zh) 2006-04-05 2012-12-05 诺瓦提斯公司 用于治疗癌症的治疗剂的组合
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
PE20080251A1 (es) 2006-05-04 2008-04-25 Boehringer Ingelheim Int Usos de inhibidores de dpp iv
EP2026800A1 (en) 2006-05-09 2009-02-25 Novartis AG Combination comprising an iron chelator and an anti-neoplastic agent and use thereof
EP2258700A1 (en) 2006-05-09 2010-12-08 Pfizer Products Inc. Cycloalkylamino acid derivatives and pharmaceutical compositions thereof
CA2652442C (en) 2006-05-18 2014-12-09 Eisai R & D Management Co., Ltd. Antitumor agent for thyroid cancer
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
PE20121506A1 (es) 2006-07-14 2012-11-26 Amgen Inc Compuestos triazolopiridinas como inhibidores de c-met
KR20090047509A (ko) 2006-08-04 2009-05-12 다케다 야쿠힌 고교 가부시키가이샤 융합 헤테로시클릭 유도체 및 이의 용도
KR101472600B1 (ko) 2006-08-28 2014-12-15 에자이 알앤드디 매니지먼트 가부시키가이샤 미분화형 위암에 대한 항종양제
BRPI0717564A2 (pt) 2006-09-29 2013-10-22 Novartis Ag Pirazolopirimidinas como inibidores de pi3k lipídeo cinase
EP2073807A1 (en) 2006-10-12 2009-07-01 Astex Therapeutics Limited Pharmaceutical combinations
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
AU2007338792B2 (en) 2006-12-20 2012-05-31 Amgen Inc. Substituted heterocycles and methods of use
EP2118069B1 (en) 2007-01-09 2014-01-01 Amgen Inc. Bis-aryl amide derivatives useful for the treatment of cancer
WO2008093677A1 (ja) 2007-01-29 2008-08-07 Santen Pharmaceutical Co., Ltd. 血管新生阻害活性を有する新規オキサジアゾール誘導体およびチアジアゾール誘導体
CN101600694A (zh) 2007-01-29 2009-12-09 卫材R&D管理有限公司 未分化型胃癌治疗用组合物
EP2491923A3 (en) 2007-02-15 2012-12-26 Novartis AG Combinations of therapeutic agents for treating cancer
AU2008219166B2 (en) 2007-02-16 2013-05-16 Amgen Inc. Nitrogen-containing heterocyclyl ketones and their use as c-Met inhibitors
AR066845A1 (es) 2007-06-05 2009-09-16 Takeda Pharmaceutical Derivados de triazolopiridina e imidazopiridina una composicion farmaceutica que los comprende y su uso en la preparacion de un medicamento para el tratamiento del cancer
US20090023727A1 (en) * 2007-07-05 2009-01-22 Muhammad Hashim Javaid Phthalazinone derivatives
TWI595005B (zh) 2007-08-21 2017-08-11 安健股份有限公司 人類ｃ－ｆｍｓ抗原結合蛋白質
EP2181987B9 (en) 2007-08-23 2014-09-03 Takeda Pharmaceutical Company Limited 2-Carbonylaminobenzothiazoles and their use for the prophylaxis and treatment of cancer
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
WO2009060945A1 (ja) 2007-11-09 2009-05-14 Eisai R & D Management Co., Ltd. 血管新生阻害物質と抗腫瘍性白金錯体との併用
AU2008340053A1 (en) 2007-12-20 2009-07-02 Novartis Ag Thiazole derivatives used as PI 3 kinase inhibitors
EP2260020B1 (en) 2008-03-26 2014-07-23 Novartis AG Hydroxamate-based inhibitors of deacetylases b
UY32030A (es) 2008-08-06 2010-03-26 Boehringer Ingelheim Int "tratamiento para diabetes en pacientes inapropiados para terapia con metformina"
NZ604091A (en) 2008-08-15 2014-08-29 Boehringer Ingelheim Int Purin derivatives for use in the treatment of fab-related diseases
EP2344161B1 (en) 2008-10-16 2018-12-19 Celator Pharmaceuticals, Inc. Combinations of a liposomal water-soluble camptothecin with cetuximab or bevacizumab
WO2010064611A1 (ja) 2008-12-01 2010-06-10 武田薬品工業株式会社 複素環化合物およびその用途
JO3101B1 (ar) 2008-12-02 2017-09-20 Takeda Pharmaceuticals Co مشتقات بنزوثيازول كعوامل مضادة للسرطان
WO2010071794A1 (en) 2008-12-18 2010-06-24 Novartis Ag New polymorphic form of 1- (4- { l- [ (e) -4-cyclohexyl--3-trifluoromethyl-benzyloxyimino] -ethyl) -2-ethyl-benzy l) -azetidine-3-carboxylic
PL2676953T3 (pl) 2008-12-18 2017-09-29 Novartis Ag Sól hemifumaranowa kwasu 1-[4-[1-(4-cykloheksylo-3-trifluorometylobenzyloksyimino)-etylo]-2-etylobenzylo]-azetydyno-3-karboksylowego
CN102256941A (zh) 2008-12-18 2011-11-23 诺瓦提斯公司 新的盐
AU2009331471B2 (en) 2008-12-23 2015-09-03 Boehringer Ingelheim International Gmbh Salt forms of organic compound
AR074990A1 (es) 2009-01-07 2011-03-02 Boehringer Ingelheim Int Tratamiento de diabetes en pacientes con un control glucemico inadecuado a pesar de la terapia con metformina
DK2391366T3 (da) 2009-01-29 2013-01-07 Novartis Ag Substituerede benzimidazoler til behandling af astrocytomer
AR075204A1 (es) 2009-01-29 2011-03-16 Boehringer Ingelheim Int Inhibidores de dpp-4 y composiciones farmaceuticas que los comprenden, utiles para tratar enfermedades metabolicas en pacientes pediatricos, particularmente diabetes mellitus tipo 2
MX2011008416A (es) 2009-02-13 2011-09-08 Boehringer Ingelheim Int Medicaciones antidiabeticas que comprenden un inhibidor de dpp-4 (linagliptina) opcionalmente en combinacion con otros antidiabeticos.
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
UA105794C2 (uk) 2009-06-26 2014-06-25 Новартіс Аг 1,3-ДИЗАМІЩЕНІ ПОХІДНІ ІМІДАЗОЛІДИН-2-ОНУ ЯК ІНГІБІТОРИ 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
JP5781510B2 (ja) 2009-08-12 2015-09-24 ノバルティス アーゲー ヘテロ環式ヒドラゾン化合物および癌および炎症の処置のためのそれらの使用
HRP20190016T1 (hr) 2009-08-17 2019-03-08 Intellikine, Llc Heterociklički spojevi i njihova upotreba
MX2012002179A (es) 2009-08-20 2012-03-16 Novartis Ag Compuestos heterociclicos de oxima.
EA201200321A1 (ru) 2009-08-26 2012-09-28 Новартис Аг Тетразамещенные гетероарильные соединения и их применение в качестве модуляторов mdm2 и/или mdm4
EA201200471A1 (ru) 2009-09-10 2012-10-30 Новартис Аг Простые эфирные производные бициклических гетероарилов
US20120219623A1 (en) 2009-10-02 2012-08-30 Boehringer Ingelheim International Gmbh Pharmaceutical compositions comprising bi-1356 and metformin
JP5466767B2 (ja) 2009-11-04 2014-04-09 ノバルティス アーゲー Ｍｅｋ阻害剤として有用なヘテロ環式スルホンアミド誘導体
US20120289501A1 (en) 2009-11-25 2012-11-15 Novartis Ag Benzene-fused 6-membered oxygen-containing heterocyclic derivatives of bicyclic heteroaryls
PH12012501037A1 (en) 2009-11-27 2013-01-14 Boehringer Ingelheim Int 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
US8440693B2 (en) 2009-12-22 2013-05-14 Novartis Ag Substituted isoquinolinones and quinazolinones
CU24130B1 (es) 2009-12-22 2015-09-29 Novartis Ag Isoquinolinonas y quinazolinonas sustituidas
JP2013522279A (ja) 2010-03-18 2013-06-13 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 糖尿病及び関連状態の治療で用いるｇｐｒ１１９作動薬とｄｄｐ−ｉｖ阻害薬リナグリプチンの組合せ
CA2797310C (en) 2010-05-05 2020-03-31 Boehringer Ingelheim International Gmbh Glp-1 receptor agonist and dpp-4 inhibitor combination therapy
US20130085161A1 (en) 2010-06-17 2013-04-04 Novartis Ag Piperidinyl substituted 1,3-dihydro-benzoimidazol-2-ylideneamine derivatives
EP2582680A1 (en) 2010-06-17 2013-04-24 Novartis AG Biphenyl substituted 1,3-dihydro-benzoimidazol-2-ylideneamine derivatives
WO2011161217A2 (en) 2010-06-23 2011-12-29 Palacký University in Olomouc Targeting of vegfr2
KR20230051307A (ko) 2010-06-24 2023-04-17 베링거 인겔하임 인터내셔날 게엠베하 당뇨병 요법
CA2802644C (en) 2010-06-25 2017-02-21 Eisai R & D Management Co., Ltd. Antitumor agent using compounds having kinase inhibitory effect in combination
RU2571226C2 (ru) 2010-07-09 2015-12-20 Дженентек, Инк. Антитела против нейропилина и способы их применения
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
JP2013537210A (ja) 2010-09-16 2013-09-30 ノバルティス アーゲー １７α−ヒドロキシラーゼ／Ｃ１７，２０−リアーゼ阻害剤
US9034883B2 (en) 2010-11-15 2015-05-19 Boehringer Ingelheim International Gmbh Vasoprotective and cardioprotective antidiabetic therapy
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
WO2012068483A1 (en) 2010-11-18 2012-05-24 Synta Pharmaceuticals Corp. Preselection of subjects for therapeutic treatment based on hypoxic status
TW201309700A (zh) 2011-01-31 2013-03-01 Novartis Ag 新穎雜環衍生物
US20130324526A1 (en) 2011-02-10 2013-12-05 Novartis Ag [1,2,4] triazolo [4,3-b] pyridazine compounds as inhibitors of the c-met tyrosine kinase
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
MY161199A (en) 2011-03-23 2017-04-14 Amgen Inc Fused tricyclic dual inhibitors of cdk 4/6 and flt3
CA2828946C (en) 2011-04-18 2016-06-21 Eisai R&D Management Co., Ltd. Therapeutic agent for tumor
EA023064B1 (ru) 2011-04-28 2016-04-29 Новартис Аг ИНГИБИТОРЫ 17α-ГИДРОКСИЛАЗЫ/C-ЛИАЗЫ
US9945862B2 (en) 2011-06-03 2018-04-17 Eisai R&D Management Co., Ltd. Biomarkers for predicting and assessing responsiveness of thyroid and kidney cancer subjects to lenvatinib compounds
MX2013014398A (es) 2011-06-09 2014-03-21 Novartis Ag Derivados de sulfonamida heterociclicos.
WO2012173447A2 (ko) * 2011-06-16 2012-12-20 한국화학연구원 1,3-다이옥소인덴 유도체, 이의 약학적으로 허용되는 염 또는 이의 광학 이성질체, 이의 제조방법 및 이를 유효성분으로 함유하는 항바이러스용 약학적 조성물
US8859535B2 (en) 2011-06-20 2014-10-14 Novartis Ag Hydroxy substituted isoquinolinone derivatives
US8859586B2 (en) 2011-06-20 2014-10-14 Novartis Ag Cyclohexyl isoquinolinone compounds
ES2713566T3 (es) 2011-07-15 2019-05-22 Boehringer Ingelheim Int Derivado de quinazolina dimérico sustituido, su preparación y su uso en composiciones farmacéuticas para el tratamiento de la diabetes de tipo I y II
US9745288B2 (en) 2011-08-16 2017-08-29 Indiana University Research And Technology Corporation Compounds and methods for treating cancer by inhibiting the urokinase receptor
CA2863679A1 (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
WO2013038362A1 (en) 2011-09-15 2013-03-21 Novartis Ag 6 - substituted 3 - (quinolin- 6 - ylthio) - [1,2,4] triazolo [4, 3 -a] pyradines as tyrosine kinase
WO2013061305A1 (en) 2011-10-28 2013-05-02 Novartis Ag Novel purine derivatives and their use in the treatment of disease
EP2785717B1 (en) 2011-11-29 2016-01-13 Novartis AG Pyrazolopyrrolidine compounds
CA2859873A1 (en) 2011-12-23 2013-06-27 Novartis Ag Compounds for inhibiting the interaction of bcl2 with binding partners
AU2012355619A1 (en) 2011-12-23 2014-07-17 Novartis Ag Compounds for inhibiting the interaction of BCL2 with binding partners
AU2012355613A1 (en) 2011-12-23 2014-07-17 Novartis Ag Compounds for inhibiting the interaction of BCL2 with binding partners
AU2012355624A1 (en) 2011-12-23 2014-07-17 Novartis Ag Compounds for inhibiting the interaction of BCL2 with binding partners
EA201491264A1 (ru) 2011-12-23 2014-11-28 Новартис Аг Соединения для ингибирования взаимодействия bcl-2 с партнерами по связыванию
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
WO2013149581A1 (en) 2012-04-03 2013-10-10 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
EP4151218A1 (en) 2012-05-14 2023-03-22 Boehringer Ingelheim International GmbH Linagliptin, a xanthine derivative as dpp-4 inhibitor, for use in the treatment of sirs and/or sepsis
EP2849756A1 (en) 2012-05-16 2015-03-25 Novartis AG Dosage regimen for a pi-3 kinase inhibitor
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
WO2013175417A1 (en) 2012-05-24 2013-11-28 Novartis Ag Pyrrolopyrrolidinone compounds
AU2013280644B2 (en) 2012-06-26 2018-08-02 Jeffrey A. BACHA 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
EP4585266A3 (en) 2012-12-14 2025-09-17 Korea Research Institute of Chemical Technology Compound, pharmaceutically acceptable salt or optical isomer thereof, method for preparing same, and pharmaceutical composition for prevention or treatment of viral diseases containing same as active ingredient
MX2015004979A (es) 2012-12-21 2015-07-17 Eisai R&D Man Co Ltd Forma amorfa de derivado de quinolina y metodo para su produccion.
EP2948453B1 (en) 2013-01-22 2017-08-02 Novartis AG Pyrazolo[3,4-d]pyrimidinone compounds as inhibitors of the p53/mdm2 interaction
WO2014115077A1 (en) 2013-01-22 2014-07-31 Novartis Ag Substituted purinone compounds
WO2014124860A1 (en) 2013-02-14 2014-08-21 Boehringer Ingelheim International Gmbh Specific pde4b-inhibitors for the treatment of diabetes mellitus
JP2016510795A (ja) 2013-03-15 2016-04-11 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 心臓保護及び腎臓保護の抗糖尿病治療におけるリナグリプチンの使用
HK1219421A1 (zh) 2013-03-15 2017-04-07 因特利凯有限责任公司 激酶抑制剂的组合及其用途
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
JP2016519684A (ja) 2013-04-08 2016-07-07 デニス エム ブラウン 準最適に投与された薬物療法の有効性を改善するための及び／又は副作用を低減するための方法および組成物
SG11201509278XA (en) 2013-05-14 2015-12-30 Eisai R&D Man Co Ltd Biomarkers for predicting and assessing responsiveness of endometrial cancer subjects to lenvatinib compounds
WO2015022664A1 (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
WO2015022663A1 (en) 2013-08-14 2015-02-19 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
CA2930359C (en) 2013-12-06 2022-03-01 Novartis Ag Dosage regimen for an alpha-isoform selective phosphatidylinositol 3-kinase inhibitor
BR112017001695A2 (pt) 2014-07-31 2017-11-21 Novartis Ag terapia de combinação
IL302218B2 (en) 2014-08-28 2024-10-01 Eisai R&D Man Co Ltd Methods for manufacturing high-purity lenvatinib and its derivatives
WO2016100882A1 (en) 2014-12-19 2016-06-23 Novartis Ag Combination therapies
EP3242934B1 (en) 2015-01-08 2021-08-18 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
JP6792546B2 (ja) 2015-02-25 2020-11-25 エーザイ・アール・アンド・ディー・マネジメント株式会社 キノリン誘導体の苦味抑制方法
AU2015384801B2 (en) 2015-03-04 2022-01-06 Eisai R&D Management Co., Ltd. Combination of a PD-1 antagonist and a VEGFR/FGFR/RET tyrosine kinase inhibitor for treating cancer
US10449211B2 (en) 2015-03-10 2019-10-22 Aduro Biotech, Inc. Compositions and methods for activating “stimulator of interferon gene”—dependent signalling
EP3311841B1 (en) 2015-06-16 2021-07-28 PRISM BioLab Co., Ltd. Anticancer agent
CN108135894B (zh) 2015-08-20 2021-02-19 卫材R&D管理有限公司 肿瘤治疗剂
CN108472289A (zh) 2015-11-02 2018-08-31 诺华股份有限公司 磷脂酰肌醇3-激酶抑制剂的给药方案
WO2017211979A1 (en) 2016-06-10 2017-12-14 Boehringer Ingelheim International Gmbh Combinations of linagliptin and metformin
US11098077B2 (en) 2016-07-05 2021-08-24 Chinook Therapeutics, 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
EP3558955B1 (en) 2016-12-22 2021-08-11 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
RU2750539C2 (ru) 2017-02-08 2021-06-29 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Фармацевтическая композиция для лечения опухоли
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
AU2018269996A1 (en) 2017-05-16 2019-11-21 Eisai R&D Management Co., Ltd. Treatment of hepatocellular carcinoma
JOP20190272A1 (ar) 2017-05-22 2019-11-21 Amgen Inc مثبطات kras g12c وطرق لاستخدامها
EP3679040B1 (en) 2017-09-08 2022-08-03 Amgen Inc. Inhibitors of kras g12c and methods of using the same
EP3697425A1 (en) 2017-10-18 2020-08-26 Chemotherapeutisches Forschungsinstitut Georg-Speyer-Haus Methods and compounds for improved immune cell therapy
WO2019119486A1 (zh) 2017-12-21 2019-06-27 中国科学院合肥物质科学研究院 一类嘧啶类衍生物激酶抑制剂
AU2019262589B2 (en) 2018-05-04 2022-07-07 Amgen Inc. KRAS G12C inhibitors and methods of using the same
ES2995514T3 (en) 2018-05-04 2025-02-10 Amgen Inc Kras g12c inhibitors and methods of using the same
MX2020011907A (es) 2018-05-10 2021-01-29 Amgen Inc Inhibidores de kras g12c para el tratamiento de cancer.
ES2938987T3 (es) 2018-06-01 2023-04-18 Amgen Inc Inhibidores de KRAS G12c y métodos de uso de los mismos
MX2020012204A (es) 2018-06-11 2021-03-31 Amgen Inc Inhibidores de kras g12c para tratar el cáncer.
CA3100390A1 (en) 2018-06-12 2020-03-12 Amgen Inc. Kras g12c inhibitors encompassing piperazine ring and use thereof in the treatment of cancer
EP3823625A1 (en) 2018-07-17 2021-05-26 Boehringer Ingelheim International GmbH Cardio- and renosafe antidiabetic therapy
US20210299129A1 (en) 2018-07-17 2021-09-30 Boehringer Ingelheim International Gmbh Cardiosafe Antidiabetic Therapy
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
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
WO2020106640A1 (en) 2018-11-19 2020-05-28 Amgen Inc. Kras g12c inhibitors and methods of using the same
CA3123871A1 (en) 2018-12-20 2020-06-25 Amgen Inc. Kif18a inhibitors
WO2020132651A1 (en) 2018-12-20 2020-06-25 Amgen Inc. Kif18a inhibitors
JP7676308B2 (ja) 2018-12-20 2025-05-14 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
MA54546A (fr) 2018-12-20 2022-03-30 Amgen Inc Amides d'hétéroaryle utiles en tant qu'inhibiteurs de kif18a
MX2021010323A (es) 2019-03-01 2021-12-10 Revolution Medicines Inc Compuestos bicíclicos de heterociclilo y usos de este.
WO2020180768A1 (en) 2019-03-01 2020-09-10 Revolution Medicines, Inc. Bicyclic heteroaryl compounds and uses thereof
EP3738593A1 (en) 2019-05-14 2020-11-18 Amgen, Inc Dosing of kras inhibitor for treatment of cancers
JP2022532379A (ja) * 2019-05-14 2022-07-14 ザ スクリプス リサーチ インスティテュート 神経変性および代謝障害の処置のための化合物
PH12021552922A1 (en) 2019-05-21 2022-04-04 Amgen Inc Solid state forms
MX2022001295A (es) 2019-08-02 2022-02-22 Amgen Inc Inhibidores de kif18a.
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
AU2020324406A1 (en) 2019-08-02 2022-03-17 Amgen Inc. KIF18A inhibitors
JP7756070B2 (ja) 2019-08-02 2025-10-17 アムジエン・インコーポレーテツド Ｋｉｆ１８ａ阻害剤としてのピリジン誘導体
AU2020369569A1 (en) 2019-10-24 2022-04-14 Amgen Inc. Pyridopyrimidine derivatives useful as KRAS G12C and KRAS G12D inhibitors in the treatment of cancer
CA3159561A1 (en) 2019-11-04 2021-05-14 Revolution Medicines, Inc. Ras inhibitors
WO2021091956A1 (en) 2019-11-04 2021-05-14 Revolution Medicines, Inc. Ras inhibitors
AU2020379731A1 (en) 2019-11-04 2022-05-05 Revolution Medicines, Inc. Ras inhibitors
MX2022005525A (es) 2019-11-08 2022-06-08 Revolution Medicines Inc Compuestos de heteroarilo bicíclicos y usos de estos.
EP4058465A1 (en) 2019-11-14 2022-09-21 Cohbar Inc. Cxcr4 antagonist peptides
AR120456A1 (es) 2019-11-14 2022-02-16 Amgen Inc Síntesis mejorada del compuesto inhibidor de g12c de kras
US12466825B2 (en) 2019-11-14 2025-11-11 Amgen Inc. Synthesis of KRAS G12C inhibitor compound
EP4065231A1 (en) 2019-11-27 2022-10-05 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
MX2022008305A (es) 2020-01-07 2022-08-08 Revolution Medicines Inc Dosificacion de inhibidores de shp2 y metodos de tratamiento del cancer.
WO2021214080A1 (en) 2020-04-20 2021-10-28 Novartis Ag Antiviral 1,3-di-oxo-indene compounds
TWI832045B (zh) 2020-04-20 2024-02-11 瑞士商諾華公司 抗病毒性1,3-二氧代茚化合物
TW202214253A (zh) 2020-06-18 2022-04-16 美商銳新醫藥公司 延遲、預防及治療對ｒａｓ抑制劑之後天抗性之方法
CA3187757A1 (en) 2020-09-03 2022-03-24 Ethan AHLER Use of sos1 inhibitors to treat malignancies with shp2 mutations
PE20231207A1 (es) 2020-09-15 2023-08-17 Revolution Medicines Inc Derivados indolicos como inhibidores de ras en el tratamiento del cancer
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
US20240174651A1 (en) * 2021-01-28 2024-05-30 The Scripps Research Institute Compounds and use thereof for treatment of neurodegenerative, degenerative and metabolic disorders
MX2023013085A (es) 2021-05-05 2023-11-16 Revolution Medicines Inc Inhibidores de ras.
PE20240089A1 (es) 2021-05-05 2024-01-16 Revolution Medicines Inc Inhibidores de ras para el tratamiento del cancer
CN117500811A (zh) 2021-05-05 2024-02-02 锐新医药公司 共价ras抑制剂及其用途
WO2022271679A1 (en) * 2021-06-21 2022-12-29 Mirati Therapeutics, Inc. Sos1 inhibitors
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
TW202340214A (zh) 2021-12-17 2023-10-16 美商健臻公司 做為shp2抑制劑之吡唑并吡𠯤化合物
WO2023121413A1 (ko) * 2021-12-24 2023-06-29 제일약품주식회사 신규한 바이사이클릭 헤테로사이클릴 화합물 및 이의 용도
EP4227307A1 (en) 2022-02-11 2023-08-16 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
JP2025509217A (ja) 2022-03-07 2025-04-11 アムジエン・インコーポレーテツド ４－メチル－２－プロパン－２－イル－ピリジン－３－カルボニトリルを調製するための方法
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
CN120504682A (zh) 2022-06-10 2025-08-19 锐新医药公司 大环ras抑制剂
IL320217A (en) 2022-10-14 2025-06-01 Black Diamond Therapeutics Inc Methods for treating cancer using isoquinoline or 6-azaquinoline derivatives
KR20250164828A (ko) 2023-03-30 2025-11-25 레볼루션 메디슨즈, 인크. Ras gtp 가수분해 유도를 위한 조성물 및 이의 용도
AU2024253668A1 (en) 2023-04-07 2025-11-13 Revolution Medicines, Inc. Macrocyclic ras inhibitors
WO2024211712A1 (en) 2023-04-07 2024-10-10 Revolution Medicines, Inc. Condensed macrocyclic compounds as ras inhibitors
US20240352038A1 (en) 2023-04-14 2024-10-24 Revolution Medicines, Inc. Crystalline forms of ras inhibitors, compositions containing the same, and methods of use thereof
CN121100123A (zh) 2023-04-14 2025-12-09 锐新医药公司 Ras抑制剂的结晶形式
TW202508595A (zh) 2023-05-04 2025-03-01 美商銳新醫藥公司 用於ｒａｓ相關疾病或病症之組合療法
WO2025034702A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Rmc-6291 for use in the treatment of ras protein-related disease or disorder
WO2025080946A2 (en) 2023-10-12 2025-04-17 Revolution Medicines, Inc. Ras inhibitors
WO2025137507A1 (en) 2023-12-22 2025-06-26 Regor Pharmaceuticals, Inc. Sos1 inhibitors and uses thereof
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2960504A (en) 1957-05-07 1960-11-15 Ciba Pharm Prod Inc 1-hydrazino, 4-pyridyl methyl-phthalazines
BE567431A (enExample) 1957-05-07
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
CN1058390C (zh) * 1993-10-15 2000-11-15 伊莱利利公司 苯并噻吩类化合物的用途
NZ290952A (en) 1994-08-09 1998-05-27 Eisai Co Ltd Phthalazine derivatives optionally substituted in position-1 by (generally benzyl) amino groups
ES2162235T3 (es) 1996-01-15 2001-12-16 Janssen Pharmaceutica Nv Piridazinaminas inhibidoras de la angiogenesis.
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
PT1105136E (pt) * 1998-08-13 2007-12-03 Novartis Ag Método para tratar doenças oculares neovasculares

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