EA200701257A1 - Пирролопиразолы в качестве сильнодействующих ингибиторов киназы - Google Patents

Пирролопиразолы в качестве сильнодействующих ингибиторов киназы

Info

Publication number
EA200701257A1
EA200701257A1 EA200701257A EA200701257A EA200701257A1 EA 200701257 A1 EA200701257 A1 EA 200701257A1 EA 200701257 A EA200701257 A EA 200701257A EA 200701257 A EA200701257 A EA 200701257A EA 200701257 A1 EA200701257 A1 EA 200701257A1
Authority
EA
Eurasian Patent Office
Prior art keywords
pyrrophorasoles
strongly
kinase inhibitors
acting
compounds
Prior art date
Application number
EA200701257A
Other languages
English (en)
Other versions
EA011815B1 (ru
Inventor
Джамал Бузида
Лимин Дун
Чуансин Го
Юйфын Хун
Хайтао Ли
Джозеф Тимоти Мараковиц
Аньлэ Ян
Цзюньху Чжан
Original Assignee
Пфайзер Инк.
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 Пфайзер Инк. filed Critical Пфайзер Инк.
Publication of EA200701257A1 publication Critical patent/EA200701257A1/ru
Publication of EA011815B1 publication Critical patent/EA011815B1/ru

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Abstract

Предложены соединения пирролпиразола формулы (I), композиции, содержащие эти соединения, и способы их применения. Предпочтительные соединения формулы I обладают активностью ингибиторов протеинкиназы, в том числе активностью ингибиторов PAK4.
EA200701257A 2005-01-10 2005-12-28 Пирролопиразолы в качестве сильнодействующих ингибиторов киназы EA011815B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US64290005P 2005-01-10 2005-01-10
US73377005P 2005-11-04 2005-11-04
PCT/IB2005/003975 WO2006072831A1 (en) 2005-01-10 2005-12-28 Pyrrolopyrazoles, potent kinase inhibitors

Publications (2)

Publication Number Publication Date
EA200701257A1 true EA200701257A1 (ru) 2007-12-28
EA011815B1 EA011815B1 (ru) 2009-06-30

Family

ID=36463340

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200701257A EA011815B1 (ru) 2005-01-10 2005-12-28 Пирролопиразолы в качестве сильнодействующих ингибиторов киназы

Country Status (30)

Country Link
US (2) US8067591B2 (ru)
EP (1) EP1838718B1 (ru)
JP (1) JP4250195B2 (ru)
KR (1) KR100919343B1 (ru)
CN (1) CN101115760B (ru)
AP (1) AP2007004061A0 (ru)
AT (1) ATE512972T1 (ru)
AU (1) AU2005323797B2 (ru)
BR (1) BRPI0518509A2 (ru)
CA (1) CA2593428C (ru)
CU (1) CU23778B7 (ru)
CY (1) CY1111752T1 (ru)
DK (1) DK1838718T3 (ru)
EA (1) EA011815B1 (ru)
ES (1) ES2365245T3 (ru)
GE (1) GEP20094785B (ru)
HK (1) HK1114380A1 (ru)
HR (1) HRP20110485T1 (ru)
IL (1) IL184275A0 (ru)
MA (1) MA29141B1 (ru)
MX (1) MX2007008385A (ru)
NO (1) NO20073859L (ru)
NZ (1) NZ556273A (ru)
PL (1) PL1838718T3 (ru)
PT (1) PT1838718E (ru)
RS (1) RS51891B (ru)
SI (1) SI1838718T1 (ru)
TN (1) TNSN07254A1 (ru)
WO (1) WO2006072831A1 (ru)
ZA (1) ZA200705628B (ru)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10894798B2 (en) 2015-06-15 2021-01-19 Ube Industries, Ltd. Substituted dihydropyrrolopyrazole derivative

Families Citing this family (41)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2634381C (en) * 2005-12-21 2011-03-08 Pfizer Products Inc. Carbonylamino pyrrolopyrazoles, potent kinase inhibitors
MX2009008546A (es) 2007-02-07 2009-10-08 Pfizer Derivados de 3-amino-pirrolo[3,4-c]pirazol-5(1h,4h,6h)carbaldehido como inhibidores de la proteina quinasa c.
UA96618C2 (en) * 2007-02-07 2011-11-25 Пфайзер Инк. 3-amino-pyrrolo[3,4-c] pyrazole- 5 (1h, 4h, 6h) carbaldehyde derivatives as pkc inhibitors
US8114871B2 (en) * 2007-04-12 2012-02-14 Pfizer Inc. 3-amido-pyrrolo[3,4-C]pyrazole-5(1H,4H,6H) carbaldehyde derivatives
US8415340B2 (en) 2007-07-25 2013-04-09 Bristol-Myers Squibb Company Triazine kinase inhibitors
FR2928150A1 (fr) 2008-02-29 2009-09-04 Vetoquinol Sa Sa Nouveaux derives 7-substitues de 3-carboxy-oxadiazino-quinolones, leur preparation et leur application comme anti-bacteriens
WO2009130900A1 (ja) * 2008-04-24 2009-10-29 日本曹達株式会社 オキシム誘導体、中間体化合物および植物病害防除剤
EP2145891A1 (en) 2008-07-09 2010-01-20 Vetoquinol S.A. 9-substituted-5-carboxy-oxadiazino-quinolone derivatives, their preparation and their application as anti-bacterials
EP2485727A4 (en) * 2009-10-06 2013-05-01 Afraxis Inc PYRROLOPYRAZOLE FOR THE TREATMENT OF CNS DISEASES
KR101483215B1 (ko) 2010-01-29 2015-01-16 한미약품 주식회사 단백질 키나아제 저해활성을 갖는 비시클릭 헤테로아릴 유도체
RU2013126036A (ru) 2010-11-17 2014-12-27 Ф. Хоффманн-Ля Рош Аг Способ лечения опухолей
AR088218A1 (es) 2011-07-19 2014-05-21 Infinity Pharmaceuticals Inc Compuestos heterociclicos utiles como inhibidores de pi3k
WO2013113776A1 (en) 2012-02-03 2013-08-08 Basf Se Fungicidal pyrimidine compounds
WO2013113719A1 (en) 2012-02-03 2013-08-08 Basf Se Fungicidal pyrimidine compounds ii
WO2013113716A1 (en) 2012-02-03 2013-08-08 Basf Se Fungicidal pyrimidine compounds
WO2013113782A1 (en) 2012-02-03 2013-08-08 Basf Se Fungicidal pyrimidine compounds
WO2013113720A1 (en) 2012-02-03 2013-08-08 Basf Se Fungicidal pyrimidine compounds
CN104220427A (zh) 2012-02-03 2014-12-17 巴斯夫欧洲公司 杀真菌嘧啶化合物
WO2013113773A1 (en) 2012-02-03 2013-08-08 Basf Se Fungicidal pyrimidine compounds
CN104220428A (zh) 2012-02-03 2014-12-17 巴斯夫欧洲公司 杀真菌嘧啶化合物
WO2013113778A1 (en) 2012-02-03 2013-08-08 Basf Se Fungicidal pyrimidine compounds
WO2013113781A1 (en) 2012-02-03 2013-08-08 Basf Se Fungicidal pyrimidine compounds i
WO2013113787A1 (en) 2012-02-03 2013-08-08 Basf Se Fungicidal pyrimidine compounds
WO2013135671A1 (en) 2012-03-13 2013-09-19 Basf Se Fungicidal pyrimidine compounds
WO2013135672A1 (en) 2012-03-13 2013-09-19 Basf Se Fungicidal pyrimidine compounds
MX2014010953A (es) * 2012-03-16 2014-10-13 Hoffmann La Roche Metodos para tratamiento de melanoma con inhibidores pak1.
JP6186440B2 (ja) 2012-09-19 2017-08-23 ノバルティス アーゲー キナーゼ阻害剤としてのジヒドロピロリジノピリミジン
BR112015007821B1 (pt) * 2012-10-15 2022-02-15 Pfizer Ireland Pharmaceuticals Processo para a preparação de voriconazol e análogos do mesmo
US20160221964A1 (en) 2013-09-16 2016-08-04 Basf Se Fungicidal pyrimidine compounds
WO2015036059A1 (en) 2013-09-16 2015-03-19 Basf Se Fungicidal pyrimidine compounds
CN104926735A (zh) * 2015-06-16 2015-09-23 上海合全药物研发有限公司 4-氯-5-氟-2-甲基嘧啶的工业化制备方法
SG11201804901WA (en) 2015-12-22 2018-07-30 SHY Therapeutics LLC Compounds for the treatment of cancer and inflammatory disease
WO2017144546A1 (en) 2016-02-23 2017-08-31 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and pharmaceutical compositions for the treatment of nasopharyngeal carcinoma
WO2018098361A1 (en) 2016-11-22 2018-05-31 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 12 (cdk12) and uses thereof
EA201992780A1 (ru) 2017-06-21 2020-06-02 ШАЙ ТЕРАПЬЮТИКС ЭлЭлСи Соединения, которые взаимодействуют с суперсемейством ras, для лечения рака, воспалительных заболеваний, ras-опатий и фиброзного заболевания
CA3097543A1 (en) * 2018-04-16 2019-10-24 The Regents Of The University Of California Pak4 inhibitors and methods of use
EP3956446A1 (en) 2019-04-17 2022-02-23 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and compositions for treatment of nlrp3 inflammasome mediated il-1beta dependent disorders
WO2021198511A1 (en) 2020-04-03 2021-10-07 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and compositions for treatment of sars-cov-2 infection
CN111454278B (zh) * 2020-05-15 2021-03-19 四川大学 Pak1抑制剂及其合成和在制备抗肿瘤药物中的应用
WO2022008597A1 (en) 2020-07-08 2022-01-13 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and pharmaceutical composition for the treatment of infectious diseases
KR20230128085A (ko) * 2020-12-31 2023-09-01 시노허브 파마슈티컬 씨오., 엘티디 플라스민 억제제, 이를 제조하는 방법 및 이의 용도

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3423414A (en) * 1966-01-13 1969-01-21 Ciba Geigy Corp Pyrazolopyridines
US3526633A (en) * 1968-03-06 1970-09-01 American Cyanamid Co Substituted 2,4,5,6-tetrahydropyrrolo(3,4-c)pyrazoles
US3947467A (en) * 1973-08-02 1976-03-30 Eli Lilly And Company 3-(5-Nitro-2-imidazolyl) pyrazoles
JPS5163193A (ja) 1974-11-26 1976-06-01 Yoshitomi Pharmaceutical Tetorahidoropirazoropirijinkagobutsuno seizoho
US6013500A (en) * 1998-05-21 2000-01-11 The Trustees Of Columbia University In The City Of New York PAK4, a novel gene encoding a serine/threonine kinase
CA2416527C (en) 2000-08-10 2009-12-22 Pharmacia Italia S.P.A. Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
BR0312913A (pt) 2002-07-25 2005-07-12 Pharmacia Italia Spa Ativo de biciclo-pirazóis como inibidores de cinase, processo para sua preparação e composições farmacêuticas compreendendo o mesmo
UA81790C2 (ru) * 2002-12-19 2008-02-11 Фармация Италия С.П.А. Замещенные пиролопиразольные производные как ингибиторы киназы
US7141568B2 (en) * 2003-07-09 2006-11-28 Pfizer Italia S.R.L. Pyrrolo[3,4-c]pyrazole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10894798B2 (en) 2015-06-15 2021-01-19 Ube Industries, Ltd. Substituted dihydropyrrolopyrazole derivative
RU2765718C1 (ru) * 2015-06-15 2022-02-02 Убе Индастриз, Лтд. Замещенное производное дигидропирролопиразола

Also Published As

Publication number Publication date
CN101115760A (zh) 2008-01-30
US8530652B2 (en) 2013-09-10
NO20073859L (no) 2007-10-03
PT1838718E (pt) 2011-08-17
EP1838718A1 (en) 2007-10-03
RS51891B (en) 2012-02-29
MX2007008385A (es) 2007-08-21
ATE512972T1 (de) 2011-07-15
TNSN07254A1 (en) 2008-12-31
NZ556273A (en) 2010-01-29
AU2005323797A1 (en) 2006-07-13
CU20070160A7 (es) 2009-03-16
CA2593428A1 (en) 2006-07-13
SI1838718T1 (sl) 2011-08-31
US8067591B2 (en) 2011-11-29
ZA200705628B (en) 2008-11-26
BRPI0518509A2 (pt) 2008-11-25
DK1838718T3 (da) 2011-07-25
HRP20110485T1 (hr) 2011-07-31
EP1838718B1 (en) 2011-06-15
IL184275A0 (en) 2007-10-31
HK1114380A1 (en) 2008-10-31
CN101115760B (zh) 2010-11-03
EA011815B1 (ru) 2009-06-30
AU2005323797B2 (en) 2009-07-09
CU23778B7 (es) 2012-02-15
CA2593428C (en) 2012-04-17
ES2365245T3 (es) 2011-09-27
KR100919343B1 (ko) 2009-09-25
PL1838718T3 (pl) 2011-10-31
GEP20094785B (en) 2009-09-25
US20100222342A1 (en) 2010-09-02
US20120264751A1 (en) 2012-10-18
AP2007004061A0 (en) 2007-08-31
CY1111752T1 (el) 2015-10-07
MA29141B1 (fr) 2008-01-02
JP4250195B2 (ja) 2009-04-08
KR20070096007A (ko) 2007-10-01
JP2008526826A (ja) 2008-07-24
WO2006072831A1 (en) 2006-07-13

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Legal Events

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MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG MD TJ TM RU