TWI699206B - Ｎ-(５-氰基-４-((２-甲氧乙基)胺基)吡啶-２-基)-７-甲醯基-６-((４-甲基-２-側氧基哌-１-基)甲基)-３,４-二氫-１,８-萘啶-１(２ｈ)-甲醯胺之顆粒 - Google Patents

Ｎ-(５-氰基-４-((２-甲氧乙基)胺基)吡啶-２-基)-７-甲醯基-６-((４-甲基-２-側氧基哌-１-基)甲基)-３,４-二氫-１,８-萘啶-１(２ｈ)-甲醯胺之顆粒 Download PDF

Info

Publication number
TWI699206B
TWI699206B TW105109283A TW105109283A TWI699206B TW I699206 B TWI699206 B TW I699206B TW 105109283 A TW105109283 A TW 105109283A TW 105109283 A TW105109283 A TW 105109283A TW I699206 B TWI699206 B TW I699206B
Authority
TW
Taiwan
Prior art keywords
methyl
amino
naphthyridine
methoxyethyl
dihydro
Prior art date
Application number
TW105109283A
Other languages
English (en)
Chinese (zh)
Other versions
TW201641106A (zh
Inventor
尼可 布舒曼
羅賓 艾拉克 菲哈斯特
派斯可 佛瑞特
韓波
湯瑪士 諾普菲爾
凱薩琳 萊柏蘭克
廖律
羅伯 馬
法蘭克 瑪蕾特
茱莉 馬爾茲
王燦
熊淨
趙祥麟
Original Assignee
瑞士商諾華公司
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 瑞士商諾華公司 filed Critical 瑞士商諾華公司
Publication of TW201641106A publication Critical patent/TW201641106A/zh
Application granted granted Critical
Publication of TWI699206B publication Critical patent/TWI699206B/zh

Links

Images

Classifications

    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C51/00—Preparation of carboxylic acids or their salts, halides or anhydrides
    • C07C51/41—Preparation of salts of carboxylic acids
    • C07C51/412—Preparation of salts of carboxylic acids by conversion of the acids, their salts, esters or anhydrides with the same carboxylic acid part
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/235—Saturated compounds containing more than one carboxyl group
    • C07C59/245—Saturated compounds containing more than one carboxyl group containing hydroxy or O-metal groups
    • C07C59/265—Citric acid
    • 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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Epidemiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pulmonology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Urology & Nephrology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Neurology (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
TW105109283A 2015-03-25 2016-03-24 Ｎ-(５-氰基-４-((２-甲氧乙基)胺基)吡啶-２-基)-７-甲醯基-６-((４-甲基-２-側氧基哌-１-基)甲基)-３,４-二氫-１,８-萘啶-１(２ｈ)-甲醯胺之顆粒 TWI699206B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
WOPCT/CN2015/000202 2015-03-25
CN2015000202 2015-03-25

Publications (2)

Publication Number Publication Date
TW201641106A TW201641106A (zh) 2016-12-01
TWI699206B true TWI699206B (zh) 2020-07-21

Family

ID=55637404

Family Applications (1)

Application Number Title Priority Date Filing Date
TW105109283A TWI699206B (zh) 2015-03-25 2016-03-24 Ｎ-(５-氰基-４-((２-甲氧乙基)胺基)吡啶-２-基)-７-甲醯基-６-((４-甲基-２-側氧基哌-１-基)甲基)-３,４-二氫-１,８-萘啶-１(２ｈ)-甲醯胺之顆粒

Country Status (14)

Country Link
US (1) US9802917B2 (enExample)
EP (1) EP3274349B1 (enExample)
JP (1) JP6696995B2 (enExample)
KR (1) KR102606643B1 (enExample)
CN (1) CN107406448B (enExample)
AR (1) AR104060A1 (enExample)
AU (2) AU2016238437B2 (enExample)
CA (1) CA2977326C (enExample)
ES (1) ES2803028T3 (enExample)
MX (1) MX2017012293A (enExample)
PL (1) PL3274349T3 (enExample)
RU (1) RU2720456C2 (enExample)
TW (1) TWI699206B (enExample)
WO (1) WO2016151500A1 (enExample)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2756748T3 (es) 2014-10-03 2020-04-27 Novartis Ag Uso de derivados de piridilo bicíclicos de anillo fusionado como inhibidores de fgfr4
CN113105454B (zh) * 2016-05-20 2022-10-11 江苏豪森药业集团有限公司 Fgfr4抑制剂、其制备方法和应用
CN107619388A (zh) 2016-07-13 2018-01-23 南京天印健华医药科技有限公司 作为fgfr抑制剂的杂环化合物
EP3691616A1 (en) * 2017-10-02 2020-08-12 Novartis AG Method for preparing a pharmaceutical product
CN110234649B (zh) * 2017-10-31 2021-10-15 江苏豪森药业集团有限公司 Fgfr4抑制剂的盐、晶体、制备方法及其用途
CN110225913B (zh) * 2017-10-31 2021-10-15 江苏豪森药业集团有限公司 Fgfr4抑制剂晶型及其制备方法
CN109745321B (zh) * 2017-11-08 2022-04-29 上海翰森生物医药科技有限公司 包含fgfr4抑制剂的药物组合物
EP3986405A4 (en) * 2019-06-21 2023-06-14 Terns Pharmaceuticals, Inc. Compounds for inhibiting fgfr4

Family Cites Families (43)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9420999D0 (en) 1994-10-18 1994-12-07 Smithkline Beecham Plc Novel compounds
AU3633997A (en) 1996-07-29 1998-02-20 Banyu Pharmaceutical Co., Ltd. Chemokine receptor antagonists
SK9192000A3 (en) 1997-12-17 2001-03-12 Merck & Co Inc Integrin receptor antagonists
WO1999041239A1 (en) 1998-02-10 1999-08-19 Novartis Ag B cell inhibitors
US7115750B1 (en) 1999-09-20 2006-10-03 Takeda Pharmaceutical Company Limited Melanin concentrating hormone antagonist
TW200305423A (en) 2002-02-14 2003-11-01 Ono Pharmaceutical Co N-carbamoyl nitrogen-containing condensed ring compound and medicament containing same as active ingredient
WO2004007472A1 (ja) 2002-07-10 2004-01-22 Ono Pharmaceutical Co., Ltd. Ｃｃｒ４アンタゴニストおよびその医薬用途
US7098332B2 (en) * 2002-12-20 2006-08-29 Hoffmann-La Roche Inc. 5,8-Dihydro-6H-pyrido[2,3-d]pyrimidin-7-ones
WO2004056820A1 (en) 2002-12-20 2004-07-08 Warner-Lambert Company Llc Benzoxazines and derivatives thereof as inhibitors of pi3ks
JP4736043B2 (ja) 2003-03-14 2011-07-27 小野薬品工業株式会社 含窒素複素環誘導体およびそれらを有効成分とする薬剤
CA2521619A1 (en) 2003-04-11 2004-10-28 Taigen Biotechnology Aminoquinoline compounds
SG146624A1 (en) 2003-09-11 2008-10-30 Kemia Inc Cytokine inhibitors
AU2006271781A1 (en) 2005-07-15 2007-01-25 F. Hoffmann-La Roche Ag Novel heteroaryl fused cyclic amines
ME00011A (me) 2005-12-21 2009-02-10 Novartis Ag Derivati pirimidinilaril uree kao fgf inhibitori
CA2635845A1 (en) 2005-12-29 2007-07-12 Janssen Pharmaceutica N.V. Prokineticin 2 receptor antagonists
RU2008140144A (ru) 2006-03-10 2010-04-20 Оно Фармасьютикал Ко., Лтд. (Jp) Азотосодержащее гетероциклическое производное и фармацевтическое средство, включающее такое производное в качестве активного ингредиента
WO2007146230A2 (en) 2006-06-14 2007-12-21 Merck & Co., Inc. Non-nucleoside reverse transcriptase inhibitors
JP2010520881A (ja) 2007-03-09 2010-06-17 ノバルティス アーゲー 黒色腫の処置
EP2234618A4 (en) 2007-12-21 2011-04-27 Scripps Research Inst BENZOPYRANE AND ANALOGUE AS RHO KINASE INHIBITORS
EP2341052A4 (en) 2008-09-05 2011-10-12 Shionogi & Co RING-CONDENSED MORPHOLINE DERIVATIVITY WITH PI3K-INHIBITING EFFECT
EP2376085B1 (en) 2008-12-19 2014-02-26 Genentech, Inc. Compounds and methods of use
GB0906472D0 (en) 2009-04-15 2009-05-20 Astex Therapeutics Ltd New compounds
SG175877A1 (en) 2009-05-04 2011-12-29 Plexxikon Inc Compounds and methods for inhibition of renin, and indications therefor
WO2011059839A1 (en) 2009-10-29 2011-05-19 Sirtris Pharmaceuticals, Inc. Bicyclic pyridines and analogs as sirtuin modulators
ES2524548T3 (es) 2009-10-30 2014-12-10 Novartis Ag N-óxido de 3-(2,6-dicloro-3,5-dimetoxi-fenil)-1-{6-[4-(4-etil-piperacin-1-il)-fenilamino]-pirimidin-4-il}-1-metil-urea
EP2532656A1 (en) 2010-02-01 2012-12-12 Nippon Chemiphar Co., Ltd. Gpr119 agonist
WO2011111880A1 (ko) 2010-03-08 2011-09-15 주식회사 메디젠텍 세포핵에서 세포질로의 ｇｓｋ３의 이동을 억제하는 화합물을 함유하는 세포핵에서 세포질로의 gsk3 이동에 의해 발생되는 질환의 치료 또는 예방용 약학적 조성물
HUE052110T2 (hu) 2010-07-29 2021-04-28 Rigel Pharmaceuticals Inc AMPK-t aktiváló heterociklusos vegyületek és alkalmazásuk
JP5620417B2 (ja) * 2011-02-07 2014-11-05 中外製薬株式会社 アミノピラゾール誘導体を含む医薬
SG193331A1 (en) 2011-03-18 2013-10-30 Lupin Ltd Benzo [b] [1, 4] oxazin derivatives as calcium sensing receptor modulators
GB201118656D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
NZ703495A (en) 2012-07-11 2018-02-23 Blueprint Medicines Corp Inhibitors of the fibroblast growth factor receptor
EP2906552B1 (en) 2012-10-12 2017-11-22 Bristol-Myers Squibb Company Guanidine substituted tetrahydroisoquinoline compounds as factor xia inhibitors
US9403774B2 (en) 2012-10-12 2016-08-02 Bristol-Myers Squibb Company Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors
WO2014079709A1 (en) 2012-11-23 2014-05-30 Ab Science Use of small molecule inhibitors/activators in combination with (deoxy)nucleoside or (deoxy)nucleotide analogs for treatment of cancer and hematological malignancies or viral infections
PH12015502383B1 (en) 2013-04-19 2023-02-03 Incyte Holdings Corp Bicyclic heterocycles as fgfr inhibitors
GB201307577D0 (en) 2013-04-26 2013-06-12 Astex Therapeutics Ltd New compounds
AU2014287209B2 (en) 2013-07-09 2019-01-24 Dana-Farber Cancer Institute, Inc. Kinase inhibitors for the treatment of disease
TW201605452A (zh) 2013-08-28 2016-02-16 安斯泰來製藥股份有限公司 以嘧啶化合物作爲有效成分之醫藥組成物
SG11201602069WA (en) 2013-10-18 2016-04-28 Eisai R&D Man Co Ltd Pyrimidine fgfr4 inhibitors
PT3395814T (pt) 2013-10-25 2022-07-27 Blueprint Medicines Corp Inibidores do recetor do fator de crescimento de fibroblastos
CN105683188B (zh) * 2013-10-25 2018-02-09 诺华股份有限公司 作为fgfr4抑制剂的稠环二环吡啶基衍生物
MA38393B1 (fr) 2014-03-13 2018-11-30 Sanofi Sa Composés hétéroaryle et utilisations associées

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Wenjun Zhou, "A Structure-Guided Approach to Creating Covalent FGFR Inhibitors" , Chemistry & Biology, Volume 17, Issue 3, 26 March 2010, Pages 285-295. *

Also Published As

Publication number Publication date
RU2720456C2 (ru) 2020-04-30
EP3274349A1 (en) 2018-01-31
CA2977326C (en) 2023-08-29
RU2017133243A (ru) 2019-04-05
AU2016238437B2 (en) 2018-11-08
BR112017016991A2 (pt) 2018-04-10
CN107406448B (zh) 2021-03-09
EP3274349B1 (en) 2020-04-22
CN107406448A (zh) 2017-11-28
JP6696995B2 (ja) 2020-05-20
ES2803028T3 (es) 2021-01-22
RU2017133243A3 (enExample) 2019-07-29
TW201641106A (zh) 2016-12-01
KR102606643B1 (ko) 2023-11-28
US9802917B2 (en) 2017-10-31
AU2016238437A1 (en) 2017-08-17
MX2017012293A (es) 2018-01-09
AR104060A1 (es) 2017-06-21
KR20170129758A (ko) 2017-11-27
CA2977326A1 (en) 2016-09-29
US20160304489A1 (en) 2016-10-20
AU2019200936A1 (en) 2019-02-28
WO2016151500A1 (en) 2016-09-29
JP2018509446A (ja) 2018-04-05
PL3274349T3 (pl) 2020-10-05

Similar Documents

Publication Publication Date Title
JP6696995B2 (ja) Ｎ−（５−シアノ−４−（（２−メトキシエチル）アミノ）ピリジン−２−イル）−７−ホルミル−６−（（４−メチル−２−オキソピペラジン−１−イル）メチル）−３，４−ジヒドロ−１，８−ナフチリジン−１（２ｈ）−カルボキサミドの粒子
TWI750188B (zh) 用於製備經取代多環吡啶酮衍生物之方法及其結晶
TWI648274B (zh) 作為激酶抑制劑之雜環醯胺類 （二）
US7074799B2 (en) Substituted quinazolin-4-ylamine analogues
CN102743385B (zh) Atp结合盒转运蛋白的异喹啉调节剂
TWI518086B (zh) ＰＩ３－激酶／ｍＴＯＲ雙重抑制劑
TW200804386A (en) Imidazopyrazines as protein kinase inhibitors
CN107787226A (zh) 药物组合
CN102227430A (zh) 囊性纤维化跨膜传导调节因子的调节剂
JP2008528506A (ja) ヘテロアリール置換ピペラジニル−ピリジン類縁体
TW200803863A (en) Method for inhibiting protein kinases
CN103857288A (zh) 作为激酶抑制剂的氨基-喹啉
JP2016527296A (ja) Ｃｆｔｒモジュレーターとしてのチエノ［２，３−ｃ］ピラン
KR20220113771A (ko) 마크로사이클릭 구조를 갖는 불소-함유 헤테로사이클릭 유도체 및 이의 용도
JP2008526997A (ja) ヘテロアリール置換キノリン−４−イルアミン類縁体
JP2008528613A (ja) 置換ピリダジニル−及びピリミジニル−キノリン−４−イルアミン類縁体
TW201902892A (zh) 化合物
BR112017016991B1 (pt) Partículas de n-(5-ciano-4-((2-metóxi-etil)amino)piridin-2-il)-7-formil-6-((4- metil-2-oxopiperazin-1-il)metil)-3,4-di-hidro-1,8-naftiridina-1(2h)-carboxamida, seu uso e seu processo de preparação, aglomerado, e composição farmacêutica
WO2015162584A1 (en) Crystalline forms of the sulfate salt of n-[5-(3-imidazol-1-yl-4-methanesulfonyl-phenyl)-4-methyl-thiazol-2-yl]-acetamide
AU2003205217A1 (en) Substituted quinazolin-4-ylamine analogues as modulators of capsaicin