RU2014115476A - Производные пиразоло[4, 3-с]птридина в качестве ингибиторов киназ - Google Patents

Производные пиразоло[4, 3-с]птридина в качестве ингибиторов киназ Download PDF

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Publication number: RU2014115476A
Authority: RU; Russia
Prior art keywords: alkyl; optionally substituted; alkenyl; same; different
Prior art date: 2011-09-20

Application number

RU2014115476/04A

Other languages

English (en)

Russian (ru)

Inventor

Найджель Рэмсден

Клаудио Дагостин

Original Assignee

Целльзом Лимитед

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.)

2011-09-20

Filing date

2012-09-20

Publication date

2015-10-27

2012-09-20 Application filed by Целльзом Лимитед filed Critical Целльзом Лимитед

2015-10-27 Publication of RU2014115476A publication Critical patent/RU2014115476A/ru

Links

229940043355 kinase inhibitor Drugs 0.000 title 1
239000003757 phosphotransferase inhibitor Substances 0.000 title 1
125000000217 alkyl group Chemical group 0.000 claims abstract 42
125000000882 C2-C6 alkenyl group Chemical group 0.000 claims abstract 27
125000003601 C2-C6 alkynyl group Chemical group 0.000 claims abstract 27
229910052736 halogen Inorganic materials 0.000 claims abstract 26
150000001875 compounds Chemical class 0.000 claims abstract 24
229910052799 carbon Inorganic materials 0.000 claims abstract 21
229910052739 hydrogen Inorganic materials 0.000 claims abstract 16
125000005843 halogen group Chemical group 0.000 claims abstract 12
229910052757 nitrogen Inorganic materials 0.000 claims abstract 10
150000003839 salts Chemical class 0.000 claims abstract 10
125000000623 heterocyclic group Chemical group 0.000 claims abstract 8
125000003118 aryl group Chemical group 0.000 claims abstract 7
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims abstract 7
229920006395 saturated elastomer Polymers 0.000 claims abstract 7
125000001624 naphthyl group Chemical group 0.000 claims abstract 4
125000002618 bicyclic heterocycle group Chemical group 0.000 claims abstract 2
150000002367 halogens Chemical class 0.000 claims 14
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
238000000034 method Methods 0.000 claims 5
125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 3
101000934996 Homo sapiens Tyrosine-protein kinase JAK3 Proteins 0.000 claims 3
102100025387 Tyrosine-protein kinase JAK3 Human genes 0.000 claims 3
201000010099 disease Diseases 0.000 claims 3
125000004043 oxo group Chemical group O=* 0.000 claims 3
229910052760 oxygen Inorganic materials 0.000 claims 3
229910052717 sulfur Inorganic materials 0.000 claims 3
YBYIRNPNPLQARY-UHFFFAOYSA-N 1H-indene Natural products C1=CC=C2CC=CC2=C1 YBYIRNPNPLQARY-UHFFFAOYSA-N 0.000 claims 2
-1 3 - ((6 - ((1-methyl-1H-pyrazol-4-yl) amino) -1H-pyrazolo [3,4-d] pyrimidin-1-yl) methyl) phenyl Chemical group 0.000 claims 2
ZCQWOFVYLHDMMC-UHFFFAOYSA-N Oxazole Chemical group C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 claims 2
WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical group C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 claims 2
208000037765 diseases and disorders Diseases 0.000 claims 2
208000035475 disorder Diseases 0.000 claims 2
239000003814 drug Substances 0.000 claims 2
125000003392 indanyl group Chemical group C1(CCC2=CC=CC=C12)* 0.000 claims 2
125000003454 indenyl group Chemical group C1(C=CC2=CC=CC=C12)* 0.000 claims 2
CTAPFRYPJLPFDF-UHFFFAOYSA-N isoxazole Chemical group C=1C=NOC=1 CTAPFRYPJLPFDF-UHFFFAOYSA-N 0.000 claims 2
239000008194 pharmaceutical composition Substances 0.000 claims 2
125000004076 pyridyl group Chemical group 0.000 claims 2
150000003852 triazoles Chemical group 0.000 claims 2
QEKADNOVOXTAIF-UHFFFAOYSA-N 2-methyl-n-[3-[[6-[(1-methylpyrazol-4-yl)amino]pyrazolo[3,4-d]pyrimidin-1-yl]methyl]phenyl]prop-2-enamide Chemical compound CC(=C)C(=O)NC1=CC=CC(CN2C3=NC(NC4=CN(C)N=C4)=NC=C3C=N2)=C1 QEKADNOVOXTAIF-UHFFFAOYSA-N 0.000 claims 1
206010052779 Transplant rejections Diseases 0.000 claims 1
230000000172 allergic effect Effects 0.000 claims 1
208000010668 atopic eczema Diseases 0.000 claims 1
230000001363 autoimmune Effects 0.000 claims 1
230000006806 disease prevention Effects 0.000 claims 1
239000003937 drug carrier Substances 0.000 claims 1
208000024908 graft versus host disease Diseases 0.000 claims 1
230000001900 immune effect Effects 0.000 claims 1
230000002757 inflammatory effect Effects 0.000 claims 1
238000004519 manufacturing process Methods 0.000 claims 1
DIQANUOZZBWOIF-UHFFFAOYSA-N n-[2-fluoro-5-[[6-[(1-methylpyrazol-4-yl)amino]pyrazolo[3,4-d]pyrimidin-1-yl]methyl]phenyl]prop-2-enamide Chemical compound C1=NN(C)C=C1NC1=NC=C(C=NN2CC=3C=C(NC(=O)C=C)C(F)=CC=3)C2=N1 DIQANUOZZBWOIF-UHFFFAOYSA-N 0.000 claims 1
KSHMJJCPYXRKEN-UHFFFAOYSA-N n-[3-[[2-[(1-methylpyrazol-4-yl)amino]pyrrolo[2,3-d]pyrimidin-7-yl]methyl]phenyl]prop-2-enamide Chemical compound C1=NN(C)C=C1NC1=NC=C(C=CN2CC=3C=C(NC(=O)C=C)C=CC=3)C2=N1 KSHMJJCPYXRKEN-UHFFFAOYSA-N 0.000 claims 1
PRKZDXYTQMDRPI-UHFFFAOYSA-N n-[3-[[6-[(1-methylpyrazol-3-yl)amino]pyrazolo[4,3-c]pyridin-1-yl]methyl]phenyl]prop-2-enamide Chemical compound CN1C=CC(NC=2N=CC=3C=NN(CC=4C=C(NC(=O)C=C)C=CC=4)C=3C=2)=N1 PRKZDXYTQMDRPI-UHFFFAOYSA-N 0.000 claims 1
OVIYRHXLFVAREZ-UHFFFAOYSA-N n-[3-[[6-[(1-methylpyrazol-4-yl)amino]pyrazolo[3,4-d]pyrimidin-1-yl]methyl]phenyl]prop-2-enamide Chemical compound C1=NN(C)C=C1NC1=NC=C(C=NN2CC=3C=C(NC(=O)C=C)C=CC=3)C2=N1 OVIYRHXLFVAREZ-UHFFFAOYSA-N 0.000 claims 1
RZLULRDRCUAUKD-UHFFFAOYSA-N n-[3-[[6-[(1-methylpyrazol-4-yl)amino]pyrazolo[3,4-d]pyrimidin-1-yl]methyl]phenyl]prop-2-ynamide Chemical compound C1=NN(C)C=C1NC1=NC=C(C=NN2CC=3C=C(NC(=O)C#C)C=CC=3)C2=N1 RZLULRDRCUAUKD-UHFFFAOYSA-N 0.000 claims 1
ZYRCGZXXJZYGPD-UHFFFAOYSA-N n-[3-[[6-[(1-methylpyrazol-4-yl)amino]pyrazolo[4,3-c]pyridin-1-yl]methyl]phenyl]prop-2-enamide Chemical compound C1=NN(C)C=C1NC(N=C1)=CC2=C1C=NN2CC1=CC=CC(NC(=O)C=C)=C1 ZYRCGZXXJZYGPD-UHFFFAOYSA-N 0.000 claims 1
230000001575 pathological effect Effects 0.000 claims 1
230000002265 prevention Effects 0.000 claims 1
230000002062 proliferating effect Effects 0.000 claims 1
125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 3
125000003342 alkenyl group Chemical group 0.000 abstract 1

Classifications

- 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
- A61K31/435—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
- A61K31/437—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 five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic 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
- 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
- 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

Landscapes

Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Health & Medical Sciences (AREA)
Animal Behavior & Ethology (AREA)
Veterinary Medicine (AREA)
Public Health (AREA)
General Health & Medical Sciences (AREA)
Pharmacology & Pharmacy (AREA)
Medicinal Chemistry (AREA)
Life Sciences & Earth Sciences (AREA)
General Chemical & Material Sciences (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Chemical Kinetics & Catalysis (AREA)
Engineering & Computer Science (AREA)
Immunology (AREA)
Bioinformatics & Cheminformatics (AREA)
Epidemiology (AREA)
Pulmonology (AREA)
Transplantation (AREA)
Pain & Pain Management (AREA)
Rheumatology (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Nitrogen Condensed Heterocyclic Rings (AREA)

RU2014115476/04A 2011-09-20 2012-09-20 Производные пиразоло[4, 3-с]птридина в качестве ингибиторов киназ RU2014115476A (ru)

Applications Claiming Priority (3)

Application Number	Priority Date	Filing Date	Title
EP11182020		2011-09-20
EP11182020.5		2011-09-20
PCT/EP2012/068504 WO2013041605A1 (en)	2011-09-20	2012-09-20	Pyrazolo[4,3-c]pyridine derivatives as kinase inhibitors

Publications (1)

Publication Number	Publication Date
RU2014115476A true RU2014115476A (ru)	2015-10-27

Family

ID=46924422

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
RU2014115476/04A RU2014115476A (ru)	2011-09-20	2012-09-20	Производные пиразоло[4, 3-с]птридина в качестве ингибиторов киназ

Country Status (9)

Country	Link
US (1)	US20140323504A1 (2)
EP (1)	EP2760863A1 (2)
JP (1)	JP2014531449A (2)
KR (1)	KR20140063700A (2)
CN (1)	CN103874699A (2)
AU (1)	AU2012311504B2 (2)
CA (1)	CA2849340A1 (2)
RU (1)	RU2014115476A (2)
WO (1)	WO2013041605A1 (2)

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WO2015038417A1 (en) *	2013-09-10	2015-03-19	Asana Biosciences, Llc	Compounds for regulating fak and/or src pathways
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CN106831779B (zh) *	2015-11-28	2019-07-19	南昌弘益药业有限公司	一类jak激酶抑制剂的新化合物
CN115054586B (zh)	2016-06-29	2024-08-02	普林斯匹亚生物制药公司	改性的释放制剂
WO2018011681A1 (en)	2016-07-14	2018-01-18	Pfizer Inc.	Novel pyrimidine carboxamides as inhibitors of vanin-1 enzyme
KR20190043437A (ko)	2017-10-18	2019-04-26	씨제이헬스케어 주식회사	단백질 키나제 억제제로서의 헤테로고리 화합물
CN110885331B (zh) *	2018-09-11	2021-07-09	中国药科大学	一种6-氨基-1H-吡唑并[3，4-d]嘧啶类JAK激酶抑制剂的制备与应用
KR102195348B1 (ko)	2018-11-15	2020-12-24	에이치케이이노엔 주식회사	단백질 키나제 억제제로서의 신규 화합물 및 이를 포함하는 약제학적 조성물
CA3139277A1 (en) *	2019-05-08	2020-11-12	Vimalan Biosciences, Inc.	Jak inhibitors
TWI899080B (zh) *	2019-05-27	2025-10-01	大陸商迪哲（江蘇）醫藥股份有限公司	Ｄｎａ依賴性蛋白激酶抑制劑
US20210106584A1 (en)	2019-10-14	2021-04-15	Principia Biopharma Inc.	Methods for treating immune thrombocytopenia by administering (r)-2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile
US11697648B2 (en)	2019-11-26	2023-07-11	Theravance Biopharma R&D Ip, Llc	Fused pyrimidine pyridinone compounds as JAK inhibitors
WO2021147953A1 (zh) *	2020-01-21	2021-07-29	江苏先声药业有限公司	嘧啶并五元环类衍生物及其应用
US11814390B2 (en)	2020-01-22	2023-11-14	Principia Biopharma Inc.	Crystalline forms of 2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)-1H-pyrazolo[3,4-D]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile
WO2022237844A1 (zh) *	2021-05-12	2022-11-17	微境生物医药科技(上海)有限公司	含吡嗪结构的吡咯并嘧啶衍生物
US12084453B2 (en)	2021-12-10	2024-09-10	Incyte Corporation	Bicyclic amines as CDK12 inhibitors

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2012
- 2012-09-20 CN CN201280049382.6A patent/CN103874699A/zh active Pending
- 2012-09-20 RU RU2014115476/04A patent/RU2014115476A/ru not_active Application Discontinuation
- 2012-09-20 CA CA2849340A patent/CA2849340A1/en not_active Abandoned
- 2012-09-20 JP JP2014531222A patent/JP2014531449A/ja active Pending
- 2012-09-20 US US14/345,512 patent/US20140323504A1/en not_active Abandoned
- 2012-09-20 EP EP12762577.0A patent/EP2760863A1/en not_active Withdrawn
- 2012-09-20 AU AU2012311504A patent/AU2012311504B2/en not_active Expired - Fee Related
- 2012-09-20 WO PCT/EP2012/068504 patent/WO2013041605A1/en not_active Ceased
- 2012-09-20 KR KR1020147006956A patent/KR20140063700A/ko not_active Withdrawn

Also Published As

Publication number	Publication date
US20140323504A1 (en)	2014-10-30
WO2013041605A1 (en)	2013-03-28
AU2012311504B2 (en)	2016-03-24
CN103874699A (zh)	2014-06-18
AU2012311504A1 (en)	2014-04-10
CA2849340A1 (en)	2013-03-28
KR20140063700A (ko)	2014-05-27
JP2014531449A (ja)	2014-11-27
EP2760863A1 (en)	2014-08-06

Legal Events

Date	Code	Title	Description
2017-01-20	FA92	Acknowledgement of application withdrawn (lack of supplementary materials submitted)	Effective date: 20170110

Publication	Publication Date	Title
RU2014115476A (ru)	2015-10-27	Производные пиразоло[4, 3-с]птридина в качестве ингибиторов киназ
JP2014531449A5 (2)	2015-11-05
PE20230161A1 (es)	2023-02-01	Inhibidores de proteinas kras mutantes
RU2011151835A (ru)	2013-06-27	Пиразолопиримидины и родственные гетероциклы как ингибиторы киназ
RU2014141579A (ru)	2016-05-27	Гетероциклические соединения в качестве ингибиторов бета-лактамаз
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