CN104640865B - 作为激酶抑制剂的二氢吡咯烷子基-嘧啶 - Google Patents

作为激酶抑制剂的二氢吡咯烷子基-嘧啶 Download PDF

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Publication number
CN104640865B
CN104640865B CN201380048493.XA CN201380048493A CN104640865B CN 104640865 B CN104640865 B CN 104640865B CN 201380048493 A CN201380048493 A CN 201380048493A CN 104640865 B CN104640865 B CN 104640865B
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China
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alkyl
compound
cycloalkyl
independently
mmol
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English (en)
Chinese (zh)
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CN104640865A (zh
Inventor
M·P·狄龙
M·林德瓦尔
D·蓬
S·拉默西
V·劳尼亚尔
C·谢弗
S·苏布拉马尼安
H·塔纳
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Novartis AG
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Novartis AG
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/527—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim spiro-condensed
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/36—Oxygen or sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/10—Spiro-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201380048493.XA 2012-09-19 2013-09-17 作为激酶抑制剂的二氢吡咯烷子基-嘧啶 Active CN104640865B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261702981P 2012-09-19 2012-09-19
US61/702,981 2012-09-19
PCT/US2013/060032 WO2014047020A1 (en) 2012-09-19 2013-09-17 Dihydropyrrolidino-pyrimidines as kinase inhibitors

Publications (2)

Publication Number Publication Date
CN104640865A CN104640865A (zh) 2015-05-20
CN104640865B true CN104640865B (zh) 2018-05-11

Family

ID=49274870

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201380048493.XA Active CN104640865B (zh) 2012-09-19 2013-09-17 作为激酶抑制剂的二氢吡咯烷子基-嘧啶

Country Status (13)

Country Link
US (1) US9546173B2 (2)
EP (1) EP2897961B1 (2)
JP (1) JP6186440B2 (2)
KR (1) KR20150056550A (2)
CN (1) CN104640865B (2)
AU (1) AU2013318283A1 (2)
BR (1) BR112015005982A2 (2)
CA (1) CA2882410A1 (2)
EA (1) EA201590600A1 (2)
ES (1) ES2612885T3 (2)
IN (1) IN2015DN01328A (2)
MX (1) MX2015003535A (2)
WO (1) WO2014047020A1 (2)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2013318283A1 (en) * 2012-09-19 2015-03-05 Novartis Ag Dihydropyrrolidino-pyrimidines as kinase inhibitors
CA3103711A1 (en) 2018-07-12 2020-01-16 UCB Biopharma SRL Spirocyclic indane analogues as il-17 modulators
WO2020243457A1 (en) * 2019-05-29 2020-12-03 Viogen Biosciences, Llc Compounds and therapeutic uses thereof
CN114502546A (zh) * 2019-08-01 2022-05-13 普拉特戈公司 晚期糖基化终产物的抑制剂
KR20220112777A (ko) * 2019-12-10 2022-08-11 에프. 호프만-라 로슈 아게 패러독스 파괴제로서의 새로운 braf 억제제
FI4073065T3 (fi) 2019-12-10 2025-04-16 Hoffmann La Roche Uusia metyylikinatsolinonijohdannaisia
CA3177298C (en) * 2020-04-30 2023-11-21 Xile LIU Compounds containing benzosultam as erk inhibitors

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4530852B2 (ja) * 2002-07-15 2010-08-25 メルク・シャープ・エンド・ドーム・コーポレイション 糖尿病治療のためのピペリジノピリミジンジペプチジルペプチダーゼ阻害剤
CA2514733A1 (en) 2003-02-28 2004-09-16 Transform Pharmaceuticals, Inc. Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen
AU2004313928A1 (en) * 2003-12-02 2005-07-28 Vertex Pharmaceuticals, Inc. Heterocyclic protein kinase inhibitors and uses thereof
PE20060426A1 (es) 2004-06-02 2006-06-28 Schering Corp DERIVADOS DE ACIDO TARTARICO COMO INHIBIDORES DE MMPs, ADAMs, TACE Y TNF-alfa
KR100919343B1 (ko) 2005-01-10 2009-09-25 화이자 인코포레이티드 키네이스 억제제로서 피롤로피라졸
RU2442778C9 (ru) 2005-12-13 2012-08-10 Шеринг Корпорейшн Новые соединения, действующие как ингибиторы erk
AR068046A1 (es) 2007-06-05 2009-11-04 Schering Corp Derivados policiclicos de indazol y su uso como inhibidores de erk para el tratamiento del cancer
EP2613782B1 (en) 2010-09-01 2016-11-02 Merck Sharp & Dohme Corp. Indazole derivatives useful as erk inhibitors
US9242981B2 (en) * 2010-09-16 2016-01-26 Merck Sharp & Dohme Corp. Fused pyrazole derivatives as novel ERK inhibitors
WO2012065935A1 (en) 2010-11-17 2012-05-24 F. Hoffmann-La Roche Ag Methods of treating tumors
CN103635472B (zh) 2011-02-28 2018-01-12 阵列生物制药公司 丝氨酸/苏氨酸激酶抑制剂
CN104507936A (zh) 2012-03-02 2015-04-08 基因科技股份有限公司 吡啶基和嘧啶基亚砜和砜衍生物
AU2013318283A1 (en) * 2012-09-19 2015-03-05 Novartis Ag Dihydropyrrolidino-pyrimidines as kinase inhibitors

Also Published As

Publication number Publication date
MX2015003535A (es) 2015-07-14
BR112015005982A2 (pt) 2017-07-04
CA2882410A1 (en) 2014-03-27
WO2014047020A1 (en) 2014-03-27
CN104640865A (zh) 2015-05-20
KR20150056550A (ko) 2015-05-26
US20150274733A1 (en) 2015-10-01
IN2015DN01328A (2) 2015-07-03
EP2897961A1 (en) 2015-07-29
ES2612885T3 (es) 2017-05-19
EA201590600A1 (ru) 2015-07-30
AU2013318283A1 (en) 2015-03-05
JP6186440B2 (ja) 2017-08-23
US9546173B2 (en) 2017-01-17
JP2015529248A (ja) 2015-10-05
EP2897961B1 (en) 2016-10-26

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