AU2020276695B2 - New crystalline forms of N-(3-(2-(2-hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methvlphenyl)-2 (trifluoromethyl)isonicotinamide as RAF inhibitors for the treatment of cancer - Google Patents

New crystalline forms of N-(3-(2-(2-hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methvlphenyl)-2 (trifluoromethyl)isonicotinamide as RAF inhibitors for the treatment of cancer

Info

Publication number
AU2020276695B2
AU2020276695B2 AU2020276695A AU2020276695A AU2020276695B2 AU 2020276695 B2 AU2020276695 B2 AU 2020276695B2 AU 2020276695 A AU2020276695 A AU 2020276695A AU 2020276695 A AU2020276695 A AU 2020276695A AU 2020276695 B2 AU2020276695 B2 AU 2020276695B2
Authority
AU
Australia
Prior art keywords
crystalline
monohydrate
temperature
cancer
pct
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
AU2020276695A
Other languages
English (en)
Other versions
AU2020276695A1 (en
Inventor
Cornelius Stephen HARLACHER
Zaixing LI
Liladhar Murlidhar Waykole
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Novartis AG
Original Assignee
Novartis AG
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Novartis AG filed Critical Novartis AG
Publication of AU2020276695A1 publication Critical patent/AU2020276695A1/en
Application granted granted Critical
Publication of AU2020276695B2 publication Critical patent/AU2020276695B2/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
AU2020276695A 2019-05-13 2020-05-12 New crystalline forms of N-(3-(2-(2-hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methvlphenyl)-2 (trifluoromethyl)isonicotinamide as RAF inhibitors for the treatment of cancer Active AU2020276695B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN2019086595 2019-05-13
CNPCT/CN2019/086595 2019-05-13
PCT/IB2020/054491 WO2020230028A1 (en) 2019-05-13 2020-05-12 New crystalline forms of n-(3-(2-(2-hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methvlphenyl)-2 (trifluoromethyl)isonicotinamide as raf inhibitors for the treatment of cancer

Publications (2)

Publication Number Publication Date
AU2020276695A1 AU2020276695A1 (en) 2021-12-23
AU2020276695B2 true AU2020276695B2 (en) 2025-12-18

Family

ID=70740724

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2020276695A Active AU2020276695B2 (en) 2019-05-13 2020-05-12 New crystalline forms of N-(3-(2-(2-hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methvlphenyl)-2 (trifluoromethyl)isonicotinamide as RAF inhibitors for the treatment of cancer

Country Status (13)

Country Link
US (2) US12187703B2 (https=)
EP (2) EP3969449B1 (https=)
JP (1) JP2022531969A (https=)
KR (1) KR102881316B1 (https=)
CN (1) CN113795490A (https=)
AU (1) AU2020276695B2 (https=)
CA (1) CA3138123A1 (https=)
CL (1) CL2021002963A1 (https=)
ES (1) ES3025633T3 (https=)
IL (1) IL287030A (https=)
MX (1) MX2021013817A (https=)
TW (1) TWI849124B (https=)
WO (1) WO2020230028A1 (https=)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2017329090B9 (en) 2016-09-19 2019-09-05 Novartis Ag Therapeutic combinations comprising a RAF inhibitor and a ERK inhibitor
CA3057969A1 (en) 2017-05-02 2018-11-08 Novartis Ag Combination therapy
WO2019217307A1 (en) 2018-05-07 2019-11-14 Mirati Therapeutics, Inc. Kras g12c inhibitors
EA202190749A1 (ru) 2018-09-10 2021-07-09 Мирати Терапьютикс, Инк. Способы комбинированной терапии
EP3849535A4 (en) 2018-09-10 2022-06-29 Mirati Therapeutics, Inc. Combination therapies
EP3849537B1 (en) 2018-09-10 2024-10-23 Mirati Therapeutics, Inc. Combination therapies
JP2022500385A (ja) 2018-09-10 2022-01-04 ミラティ セラピューティクス， インコーポレイテッド 組み合わせ療法
MX2021002804A (es) 2018-12-05 2021-07-15 Mirati Therapeutics Inc Terapias de combinacion.
EP3908283A4 (en) 2019-01-10 2022-10-12 Mirati Therapeutics, Inc. KRAS G12C INHIBITORS
EP3969449B1 (en) 2019-05-13 2025-02-12 Novartis AG New crystalline forms of n-(3-(2-(2-hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methvlphenyl)-2(trifluoromethyl)isonicotinamide as raf inhibitors for the treatment of cancer
MX2022002465A (es) 2019-08-29 2022-05-19 Mirati Therapeutics Inc Inhibidores de kras g12d.
WO2021061749A1 (en) 2019-09-24 2021-04-01 Mirati Therapeutics, Inc. Combination therapies
PH12022551513A1 (en) 2019-12-20 2023-04-24 Mirati Therapeutics Inc Sos1 inhibitors
EP4210833A4 (en) 2020-09-11 2024-09-11 Mirati Therapeutics, Inc. CRYSTALLINE FORMS OF A KRAS G12C INHIBITOR
JP2023553492A (ja) 2020-12-15 2023-12-21 ミラティ セラピューティクス， インコーポレイテッド アザキナゾリン汎ＫＲａｓ阻害剤
EP4262803A4 (en) 2020-12-16 2025-03-12 Mirati Therapeutics, Inc. Tetrahydropyridopyrimidine pan-kras inhibitors
WO2022253334A1 (zh) * 2021-06-04 2022-12-08 南京明德新药研发有限公司 一种raf激酶抑制剂的晶型及其制备方法
CA3240263A1 (en) 2021-12-09 2023-06-15 Daniel L. Flynn Raf kinase inhibitors and methods of use thereof
AU2023227427A1 (en) 2022-03-02 2024-09-19 Novartis Ag Precision therapy for the treatment of cancer
KR20250041176A (ko) 2022-08-10 2025-03-25 노파르티스 아게 나포라페닙을 포함하는 무정형 고체 분산물

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014151616A1 (en) * 2013-03-14 2014-09-25 Novartis Ag Biaryl amide compounds as kinase inhibitors

Family Cites Families (136)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3707475A (en) 1970-11-16 1972-12-26 Pfizer Antiinflammatory imidazoles
DE3029376A1 (de) 1980-07-31 1982-03-18 Nepera Chemical Co. Inc., Harriman, N.Y. Verfahren zur herstellung von 2,4,5-tris-pyridylimidazolen
EP0149884B1 (en) 1983-09-09 1992-12-16 Takeda Chemical Industries, Ltd. 5-pyridyl-1,3-thiazole derivatives, their production and use
JP2722586B2 (ja) 1989-01-13 1998-03-04 大正製薬株式会社 インドリルイミダゾール誘導体
JP2808460B2 (ja) 1989-11-16 1998-10-08 大正製薬株式会社 イミダゾール誘導体
US6358932B1 (en) 1994-05-31 2002-03-19 Isis Pharmaceticals, Inc. Antisense oligonucleotide inhibition of raf gene expression
US5717100A (en) 1995-10-06 1998-02-10 Merck & Co., Inc. Substituted imidazoles having anti-cancer and cytokine inhibitory activity
GB2306108A (en) 1995-10-13 1997-04-30 Merck & Co Inc Treatment of Raf-mediated cancers with imidazole derivatives
US6268308B1 (en) 1996-08-27 2001-07-31 Syngenta Crop Protection, Inc. Herbicidal S-substituted 1,2,4,6-thiatriazines
AU743024B2 (en) 1997-03-05 2002-01-17 Sugen, Inc. Formulations for hydrophobic pharmaceutical agents
AR012634A1 (es) 1997-05-02 2000-11-08 Sugen Inc Compuesto basado en quinazolina, composicion famaceutica que lo comprende, metodo para sintetizarlo, su uso, metodos de modulacion de la funcion deserina/treonina proteinaquinasa con dicho compuesto y metodo in vitro para identificar compuestos que modulan dicha funcion
GB9711650D0 (en) 1997-06-05 1997-07-30 Pfizer Ltd Compounds useful in therapy
GB9716557D0 (en) 1997-08-06 1997-10-08 Glaxo Group Ltd Benzylidene-1,3-dihydro-indol-2-one derivatives having anti-cancer activity
US6022884A (en) 1997-11-07 2000-02-08 Amgen Inc. Substituted pyridine compounds and methods of use
US6211177B1 (en) 1998-11-24 2001-04-03 Cell Pathways, Inc. Method for treating neoplasia by exposure to substituted 2-aryl-benzimidazole derivatives
EP1140840B1 (en) 1999-01-13 2006-03-22 Bayer Pharmaceuticals Corp. -g(v)-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
US6548529B1 (en) 1999-04-05 2003-04-15 Bristol-Myers Squibb Company Heterocyclic containing biphenyl aP2 inhibitors and method
DE60001229T2 (de) 1999-04-09 2003-10-30 Smithkline Beecham Corp., Philadelphia Triarylimidazole
EP1169038B9 (en) 1999-04-15 2013-07-10 Bristol-Myers Squibb Company Cyclic protein tyrosine kinase inhibitors
JP2000302680A (ja) 1999-04-23 2000-10-31 Takeda Chem Ind Ltd 脳保護剤
AU7031500A (en) 1999-09-23 2001-04-24 Astrazeneca Ab Therapeutic quinazoline compounds
AU1529901A (en) 1999-11-22 2001-06-04 Smithkline Beecham Plc Compounds
JP2003520233A (ja) 2000-01-18 2003-07-02 バーテックス ファーマシューティカルズ インコーポレイテッド ジャイレースインヒビターおよびそれらの使用
AU2001232809A1 (en) 2000-01-18 2001-07-31 Vertex Pharmaceuticals Incorporated Gyrase inhibitors and uses thereof
CO5271680A1 (es) 2000-02-21 2003-04-30 Smithkline Beecham Corp Compuestos
GB0005357D0 (en) 2000-03-06 2000-04-26 Smithkline Beecham Plc Compounds
ATE266022T1 (de) 2000-03-06 2004-05-15 Smithkline Beecham Plc Imidazol derivate als raf kinase inhibitoren
GB0007405D0 (en) 2000-03-27 2000-05-17 Smithkline Beecham Corp Compounds
WO2001074811A2 (en) 2000-03-30 2001-10-11 Takeda Chemical Industries, Ltd. Substituted 1,3-thiazole compounds, their production and use
US6608053B2 (en) 2000-04-27 2003-08-19 Yamanouchi Pharmaceutical Co., Ltd. Fused heteroaryl derivatives
ES2320973T3 (es) 2000-06-12 2009-06-01 EISAI R&D MANAGEMENT CO., LTD. Compuestos de 1,2-dihidropiridina, procedimiento para su preparacion y uso de los mismos.
JP3811775B2 (ja) 2000-07-19 2006-08-23 ワーナー−ランバート カンパニー リミティド ライアビリティー カンパニー ４−ヨードフェニルアミノベンズヒドロキサム酸の酸素化エステル
EP1332131A2 (en) 2000-11-07 2003-08-06 Bristol-Myers Squibb Company Acid derivatives useful as serine protease inhibitors
ATE365730T1 (de) 2000-11-20 2007-07-15 Smithkline Beecham Corp Neuartige verbindungen
JP2004517080A (ja) 2000-11-29 2004-06-10 グラクソ グループ リミテッド Ｔｉｅ−２および／またはｖｅｇｆｒ−２の阻害剤として有用なベンゾイミダゾール誘導体
ES2274005T3 (es) 2001-01-26 2007-05-16 Chugai Seiyaku Kabushiki Kaisha Inhibidores de malonyl-coa decarboxilasa usados como moduladores metabolicos.
US7199124B2 (en) 2001-02-02 2007-04-03 Takeda Pharmaceutical Company Limited JNK inhibitor
US20030009034A1 (en) 2001-03-22 2003-01-09 Neil Wishart Transition metal mediated process
JP2002338537A (ja) 2001-05-16 2002-11-27 Mitsubishi Pharma Corp アミド化合物およびその医薬用途
GB0112348D0 (en) 2001-05-19 2001-07-11 Smithkline Beecham Plc Compounds
GB0129260D0 (en) 2001-12-06 2002-01-23 Eisai London Res Lab Ltd Pharmaceutical compositions and their uses
WO2003082272A1 (en) 2002-03-29 2003-10-09 Chiron Corporation Substituted benzazoles and use thereof as raf kinase inhibitors
US8299108B2 (en) 2002-03-29 2012-10-30 Novartis Ag Substituted benzazoles and methods of their use as inhibitors of raf kinase
AR039241A1 (es) 2002-04-04 2005-02-16 Biogen Inc Heteroarilos trisustituidos y metodos para su produccion y uso de los mismos
AU2003262642B2 (en) 2002-08-14 2010-06-17 Vertex Pharmaceuticals Incorporated Protein kinase inhibitors and uses thereof
AU2003256003A1 (en) 2002-09-18 2004-04-08 Pfizer Products Inc. Novel oxazole and thiazole compounds as transforming growth factor (TGF) inhibitors
MXPA05002981A (es) 2002-09-18 2005-06-22 Pfizer Prod Inc Nuevos compuestos de imidazol como inhibidores del factor de crecimiento transformante (tgf).
US7531553B2 (en) 2003-03-21 2009-05-12 Amgen Inc. Heterocyclic compounds and methods of use
AR045944A1 (es) 2003-09-24 2005-11-16 Novartis Ag Derivados de isoquinolina 1.4-disustituidas
AU2004279427B2 (en) 2003-10-08 2008-07-03 Irm Llc Compounds and compositions as protein kinase inhibitors
KR20060118472A (ko) 2003-10-16 2006-11-23 카이론 코포레이션 치환 벤자졸 및 ｒａｆ 키나아제의 저해제로서 그것의 사용
CA2545942C (en) 2003-11-14 2012-07-10 Lorus Therapeutics Inc. Aryl imidazoles and their use as anti-cancer agents
RU2367661C2 (ru) 2004-03-05 2009-09-20 Тайсо Фармасьютикал Ко., Лтд. Производные тиазола
KR100749566B1 (ko) 2004-04-21 2007-08-16 이화여자대학교 산학협력단 Ａｌｋ5 및/또는 ａｌｋ4 억제제로 유효한 2-피리딜이치환된 이미다졸 유도체
US20060106020A1 (en) 2004-04-28 2006-05-18 Rodgers James D Tetracyclic inhibitors of Janus kinases
PE20060315A1 (es) 2004-05-24 2006-05-15 Irm Llc Compuestos de tiazol como moduladores de ppar
SI1761528T1 (sl) 2004-06-11 2008-06-30 Japan Tobacco Inc 5-amino-2,4,7-triokso-3,4,7,8-tetrahidro-2H-pirido(2,3-D)pirimidinski derivati in sorodne spojine za zdravljenje raka
US7453002B2 (en) 2004-06-15 2008-11-18 Bristol-Myers Squibb Company Five-membered heterocycles useful as serine protease inhibitors
GB0415367D0 (en) 2004-07-09 2004-08-11 Astrazeneca Ab Pyrimidine derivatives
GB0415364D0 (en) 2004-07-09 2004-08-11 Astrazeneca Ab Pyrimidine derivatives
GB0415365D0 (en) 2004-07-09 2004-08-11 Astrazeneca Ab Pyrimidine derivatives
AU2005280168A1 (en) 2004-08-31 2006-03-09 Biogen Idec Ma Inc. Pyrimidinylimidazoles as TGF-beta inhibitors
WO2006038734A1 (en) 2004-10-08 2006-04-13 Astellas Pharma Inc. Pyridazinone derivatives cytokines inhibitors
AU2005295734A1 (en) 2004-10-15 2006-04-27 Biogen Idec Ma Inc. Methods of treating vascular injuries
JP2007246520A (ja) 2006-02-15 2007-09-27 Takeda Yuichiro Ｒａｇｅ阻害剤
WO2007118149A2 (en) 2006-04-07 2007-10-18 Board Of Supervisors Of Louisiana State University And Agricultural And Mechanical Lollege Thiazole and thiophene analogues, and their use in treating autoimmune diseases and cancers
EP2050749B1 (en) 2006-08-08 2017-11-22 Chugai Seiyaku Kabushiki Kaisha Pyrimidine derivative as pi3k inhibitor and use thereof
WO2008071605A2 (en) 2006-12-15 2008-06-19 F. Hoffmann-La Roche Ag Methods of treating inflammatory diseases
JP5140154B2 (ja) 2007-06-27 2013-02-06 アストラゼネカ・アクチエボラーグ ピラジノン誘導体および肺疾患の処置におけるそれらの使用
CL2008001933A1 (es) 2007-06-29 2009-09-25 Millennium Pharm Inc Compuestos derivados de pirimidina, inhibidores de la raf quinasa; compuestos intermediarios; procedimiento de preparacion; composicion farmaceutica; y su uso para tratar trastornos proliferativos, cardiacos, neurodegenerativos, inflamatorios, oseos, inmunologicos enfermedad viral, entre otros.
US7968536B2 (en) 2007-06-29 2011-06-28 Millennium Pharmaceuticals, Inc. Heterocyclic compounds useful as RAF kinase inhibitors
CA2692379A1 (en) 2007-07-02 2009-01-08 Boehringer Ingelheim International Gmbh Antiproliferative compounds based on 5-membered heterocycles
US20100261723A1 (en) 2007-07-09 2010-10-14 Astrazeneca Ab Trisubstituted pyrimidine derivatives for the treatment of proliferative diseases
WO2009012283A1 (en) 2007-07-17 2009-01-22 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
MY150032A (en) 2007-07-19 2013-11-29 Merck Sharp & Dohme Heterocyclic amide compounds as protein kinase inhibitors
WO2009032667A1 (en) 2007-08-29 2009-03-12 Smithkline Beecham Corporation Thiazole and oxazole kinase inhibitors
WO2009030952A2 (en) 2007-09-05 2009-03-12 Astrazeneca Ab Phenylcarboxamide derivatives as inhibitors and effectors of the hedgehog pathway
WO2009047163A1 (en) 2007-10-10 2009-04-16 F. Hoffmann-La Roche Ag Methods of treating inflammatory diseases
TW200940537A (en) 2008-02-26 2009-10-01 Astrazeneca Ab Heterocyclic urea derivatives and methods of use thereof
US8865732B2 (en) 2008-03-21 2014-10-21 Novartis Ag Heterocyclic compounds and uses thereof
WO2009115572A2 (en) 2008-03-21 2009-09-24 Novartis Ag Novel heterocyclic compounds and uses therof
UA103319C2 (en) 2008-05-06 2013-10-10 Глаксосмитклайн Ллк Thiazole- and oxazole-benzene sulfonamide compounds
CN102089278A (zh) 2008-06-11 2011-06-08 Irm责任有限公司 用于治疗疟疾的化合物和组合物
PT2324008E (pt) 2008-07-24 2012-06-25 Nerviano Medical Sciences Srl 3,4-diarilpirazoles como inibidores da proteína quinase
ES2522346T3 (es) 2008-08-22 2014-11-14 Novartis Ag Compuestos de pirrolopirimidina como inhibidores de CDK
WO2010048149A2 (en) 2008-10-20 2010-04-29 Kalypsys, Inc. Heterocyclic modulators of gpr119 for treatment of disease
ES2921576T3 (es) 2008-12-19 2022-08-29 Vertex Pharma Compuestos útiles como inhibidores de la quinasa ATR
US8242260B2 (en) 2009-08-28 2012-08-14 Novartis Ag Compounds and compositions as protein kinase inhibitors
WO2011026911A1 (en) 2009-09-04 2011-03-10 Novartis Ag Bipyridines useful for the treatment of proliferative diseases
EP2498608A4 (en) 2009-11-10 2013-04-24 Glaxosmithkline Llc BENZOLSULFONAMIDE THIAZOL AND OXAZOLE COMPOUNDS
PL2520575T3 (pl) 2009-12-28 2017-05-31 General Incorporated Association Pharma Valley Project Supporting Organization Związek 1,3,4-oksadiazolo-2-karboksyamidowy
US9315491B2 (en) 2009-12-28 2016-04-19 Development Center For Biotechnology Pyrimidine compounds as mTOR and PI3K inhibitors
KR20110123657A (ko) 2010-05-07 2011-11-15 에스케이케미칼주식회사 피콜린아마이드 및 피리미딘-4-카복사미드 화합물, 이의 제조방법 및 이를 함유하는 약제학적 조성물
JP2013529619A (ja) 2010-06-25 2013-07-22 ノバルティス アーゲー タンパク質キナーゼ阻害剤としてのヘテロアリール化合物および組成物
JP5903433B2 (ja) 2010-08-26 2016-04-13 ノバルティス アーゲー 癌の治療に有用なｖｅｇｆｒ阻害剤およびｍｅｋ阻害剤の医薬的組み合わせ
CN101993415B (zh) 2010-09-15 2013-08-14 北京韩美药品有限公司 作为Hedgehog通路抑制剂的化合物以及包含该化合物的药物组合物及其应用
US20120115878A1 (en) 2010-11-10 2012-05-10 John Vincent Calienni Salt(s) of 7-cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7h-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide and processes of making thereof
TWI505828B (zh) 2010-12-20 2015-11-01 葛蘭素史克智慧財產（第二）有限公司 新穎醫藥組成物
US9624213B2 (en) 2011-02-07 2017-04-18 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
US20140221374A1 (en) 2011-03-17 2014-08-07 Ruga Corporation Raf kinase inhibitors
EP2739143B1 (en) 2011-08-05 2018-07-11 Gary A. Flynn Preparation and methods of use for ortho-aryl 5- membered heteroaryl-carboxamide containing multi-targeted kinase inhibitors
EP2751104B1 (en) 2011-09-01 2019-09-25 Novartis AG Compounds and compositions as c-kit kinase inhibitors
WO2013041652A1 (en) 2011-09-21 2013-03-28 Cellzome Limited Morpholino substituted urea or carbamate derivatives as mtor inhibitors
CA2871270A1 (en) 2012-05-02 2013-11-07 Lupin Limited Substituted pyridine compounds as crac modulators
CN104379574B (zh) 2012-05-15 2017-03-01 诺华股份有限公司 用于抑制abl1、abl2和bcr‑abl1的活性的苯甲酰胺衍生物
AR091654A1 (es) 2012-07-02 2015-02-18 Biogen Idec Inc COMPUESTOS QUE CONTIENEN BIARILO COMO AGONISTAS INVERSOS DE RECEPTORES ROR-g
AR091876A1 (es) 2012-07-26 2015-03-04 Novartis Ag Combinaciones farmaceuticas para el tratamiento de enfermedades proliferativas
JP6342396B2 (ja) 2012-08-07 2018-06-13 ノバルティス アーゲー Ｂ−Ｒａｆ阻害薬、ＥＧＦＲ阻害薬及び場合によってはＰＩ３Ｋ−α阻害薬を含む組合せ医薬
CN104582706A (zh) 2012-09-04 2015-04-29 葛兰素史克有限责任公司 辅助癌症治疗的方法
KR102215272B1 (ko) 2012-09-28 2021-02-15 이그니타, 인코포레이티드 비정형 단백질 키나제 c의 아자퀴나졸린 억제제
EP2903613B1 (en) 2012-10-08 2017-11-22 Merck Sharp & Dohme Corp. Pyrazole derivatives useful as inhibitors of irak4 activity
US9867825B2 (en) 2012-12-20 2018-01-16 Novartis Ag Pharmaceutical combination comprising binimetinib
MA38522A1 (fr) 2013-03-21 2017-10-31 Novartis Ag Thérapie de combinaison comprenant un inhibiteur de b-raf et un second inhibiteur.
AP2016009099A0 (en) 2013-11-01 2016-03-31 Novartis Ag Aminoheteroaryl benzamides as kinase inhibitors
US10668055B2 (en) 2013-12-20 2020-06-02 Biomed Valley Discoveries, Inc. Cancer treatment using combinations of ERK and RAF inhibitors
UY36294A (es) 2014-09-12 2016-04-29 Novartis Ag Compuestos y composiciones como inhibidores de quinasa
EP3191467B1 (en) 2014-09-12 2020-10-21 Novartis AG Compounds and compositions as kinase inhibitors
CN107074828B (zh) 2014-09-12 2020-05-19 诺华股份有限公司 用作raf激酶抑制剂的化合物和组合物
WO2016115376A1 (en) 2015-01-14 2016-07-21 The Regents Of The University Of California Detection and treatment of double drug resistant melanomas
CN113307805A (zh) 2015-04-15 2021-08-27 百济神州有限公司 B-raf激酶抑制剂的马来酸盐、其结晶形式、制备方法和用途
PL3319993T3 (pl) 2015-07-10 2020-07-27 Genmab A/S Specyficzne wobec AXL koniugaty przeciwciało-lek do leczenia raka
EP3340987A1 (en) 2015-08-28 2018-07-04 Novartis AG Combination of ribociclib and dabrafenib for treating or preventing cancer
WO2017037575A1 (en) 2015-08-28 2017-03-09 Novartis Ag A pharmaceutical combination comprising the pi3k inhibitor alpelisib and the cdk4/6 inhibitor ribociclib, and the use thereof in the treatment/prevention of cancer
FI3463345T3 (fi) 2016-06-03 2023-01-31 Farmaseuttisia yhdistelmiä
CA3026876A1 (en) 2016-06-10 2017-12-14 Novartis Ag Therapeutic uses of a c-raf inhibitor
AU2017329090B9 (en) 2016-09-19 2019-09-05 Novartis Ag Therapeutic combinations comprising a RAF inhibitor and a ERK inhibitor
WO2018107146A1 (en) 2016-12-11 2018-06-14 Memorial Sloan Kettering Cancer Center Methods and compositions for treatment of braf mutant cancers
CA3057969A1 (en) 2017-05-02 2018-11-08 Novartis Ag Combination therapy
EP3624896A4 (en) 2017-05-16 2021-03-31 Biomed Valley Discoveries, Inc. COMPOSITIONS AND METHODS OF TREATMENT OF CANCER WITH ATYPICAL BRAF MUTATIONS
KR102811888B1 (ko) 2017-09-08 2025-05-27 에프. 호프만-라 로슈 아게 암의 진단 및 치료 방법
TW202023556A (zh) 2018-08-27 2020-07-01 美商庫拉腫瘤技術股份有限公司 以mapk路徑抑制劑治療腺癌
CA3123510A1 (en) 2018-12-20 2020-06-25 Novartis Ag Combination therapy with a raf inhibitor and a cdk4/6 inhibitor for use in the treatment of cancer
EP3969449B1 (en) 2019-05-13 2025-02-12 Novartis AG New crystalline forms of n-(3-(2-(2-hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methvlphenyl)-2(trifluoromethyl)isonicotinamide as raf inhibitors for the treatment of cancer
EP4106756A1 (en) 2020-02-18 2022-12-28 Novartis AG Therapeutic combinations comprising a raf inhibitor for use in treating braf mutant nsclc
US20240000789A1 (en) 2020-05-12 2024-01-04 Novartis Ag Therapeutic combinations comprising a craf inhibitor
TW202227088A (zh) 2020-08-31 2022-07-16 瑞士商諾華公司 組合療法

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014151616A1 (en) * 2013-03-14 2014-09-25 Novartis Ag Biaryl amide compounds as kinase inhibitors

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Ramurthy, S., et al. J. Med. Chem., 2020, 63(5), p 2013−2027. *

Also Published As

Publication number Publication date
AU2020276695A1 (en) 2021-12-23
WO2020230028A1 (en) 2020-11-19
JP2022531969A (ja) 2022-07-12
IL287030A (en) 2021-12-01
EP3969449A1 (en) 2022-03-23
US20220267299A1 (en) 2022-08-25
TW202108579A (zh) 2021-03-01
TWI849124B (zh) 2024-07-21
KR102881316B1 (ko) 2025-11-05
BR112021022335A2 (pt) 2021-12-28
EP4563150A2 (en) 2025-06-04
EP4563150A3 (en) 2025-07-23
US12187703B2 (en) 2025-01-07
MX2021013817A (es) 2021-12-14
CA3138123A1 (en) 2020-11-19
EP3969449B1 (en) 2025-02-12
US20250188054A1 (en) 2025-06-12
CL2021002963A1 (es) 2022-09-09
CN113795490A (zh) 2021-12-14
KR20220008273A (ko) 2022-01-20
ES3025633T3 (en) 2025-06-09

Similar Documents

Publication Publication Date Title
AU2020276695B2 (en) New crystalline forms of N-(3-(2-(2-hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methvlphenyl)-2 (trifluoromethyl)isonicotinamide as RAF inhibitors for the treatment of cancer
TWI858258B (zh) Ｌｎｐ０２３之結晶形式
EP3808742A1 (en) Polymorph of selinexor
WO2018106657A1 (en) Compositions and methods related to pyridinoylpiperidine 5-ht1f agonists
KR20140047483A (ko) 피마살탄 포타슘염의 일수화물 결정, 그 제조방법, 및 그를 포함하는 약제학적 조성물
US9708301B2 (en) Crystalline forms of afatinib monomaleate, preparation methods and pharmaceutical compositions thereof
CN103889971B (zh) (1，1-二氧代-4-硫代吗啉基)-[6-[[3(4-氟苯基)-5-甲基-4-异噁唑基]甲氧基]-3-吡啶]-甲酮的固体形式
HK40127061A (en) New crystalline forms of n-(3-(2-(2-hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methvlphenyl)-2(trifluoromethyl) isonicotinamide as raf inhibitors for the treatment of cancer
HK40065390A (en) New crystalline forms of n-(3-(2-(2-hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methvlphenyl)-2(trifluoromethyl)isonicotinamide as raf inhibitors for the treatment of cancer
HK40065390B (en) New crystalline forms of n-(3-(2-(2-hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methvlphenyl)-2(trifluoromethyl)isonicotinamide as raf inhibitors for the treatment of cancer
CN107868059B (zh) 一种喹唑啉衍生物的盐、其制备方法及应用
BR112021022335B1 (pt) Formas cristalinas de n-(3-(2-(2-hidroxietoxi)-6-morfolinopiridin4-il)-4- metilfenil)-2 (trifluorome-til)isonicotinamida como inibidores raf, seus usos, e composição farmacêutica
EP3408264A1 (en) Nilotinib dinitrate (v) and crystalline forms thereof
US20230105181A1 (en) Salts and polymorphic forms of 6-chloro-7-(4-(4-chlorobenzyl)piperazin-1-yl)-2-(1,3-dimethyl-1h-pyrazol-4-yl)-3h-imidazo[4,5-b]pyridine
WO2022199707A1 (zh) 哌马色林药用盐、制备方法、含其的药物组合物及应用
TW202140493A (zh) 2-吲哚啉螺環酮類化合物或其鹽、溶劑錯合物之非晶形式或結晶形式

Legal Events

Date Code Title Description
FGA Letters patent sealed or granted (standard patent)