BRPI0518509A2 - pirrolopirazàis, inibidores de cinase potentes - Google Patents

pirrolopirazàis, inibidores de cinase potentes

Info

Publication number
BRPI0518509A2
BRPI0518509A2 BRPI0518509-2A BRPI0518509A BRPI0518509A2 BR PI0518509 A2 BRPI0518509 A2 BR PI0518509A2 BR PI0518509 A BRPI0518509 A BR PI0518509A BR PI0518509 A2 BRPI0518509 A2 BR PI0518509A2
Authority
BR
Brazil
Prior art keywords
kinase inhibitors
pyrrolopyrazines
potent kinase
compounds
formula
Prior art date
Application number
BRPI0518509-2A
Other languages
English (en)
Inventor
Djalma Bouzida
Liming Dong
Chuangxing Guo
Yufeng Hong
Haitao Li
Joseph Timothy Marakovits
Anle Yang
Junhu Zhang
Original Assignee
Pfizer
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 Pfizer filed Critical Pfizer
Publication of BRPI0518509A2 publication Critical patent/BRPI0518509A2/pt

Links

Classifications

    • 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
    • A61K31/435—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
    • A61P35/00—Antineoplastic 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Coloring Foods And Improving Nutritive Qualities (AREA)

Abstract

PIRROLOPIRAZàIS, INIBIDORES DE CINASE POTENTES. Proporcionam-se compostos de pirrol pirazol de fórmula (I), composições que incluem estes compostos e métodos de seu uso. Os. compostos preferidos de fórmula I têm atividade como inibidores de proteína cinase, incluindo como inibidores de PAK4.
BRPI0518509-2A 2005-01-10 2005-12-28 pirrolopirazàis, inibidores de cinase potentes BRPI0518509A2 (pt)

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 (1)

Publication Number Publication Date
BRPI0518509A2 true BRPI0518509A2 (pt) 2008-11-25

Family

ID=36463340

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0518509-2A BRPI0518509A2 (pt) 2005-01-10 2005-12-28 pirrolopirazàis, inibidores de cinase potentes

Country Status (29)

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

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MY151455A (en) * 2005-12-21 2014-05-30 Pfizer Prod Inc Carbonylamino pyrrolopyrazoles, potent kinase inhibitors
CN101646673B (zh) * 2007-02-07 2014-06-25 辉瑞大药厂 作为pkc抑制剂的3-氨基-吡咯并[3,4-c]吡唑-5(1h,4h,6h)甲醛衍生物
EA017937B1 (ru) 2007-02-07 2013-04-30 Пфайзер Инк. ПРОИЗВОДНЫЕ 3-АМИНОПИРРОЛО[3,4-c]ПИРАЗОЛ-5(1H,4H,6H)-КАРБАЛЬДЕГИДА В КАЧЕСТВЕ ИНГИБИТОРОВ РКС
CN101675052A (zh) * 2007-04-12 2010-03-17 辉瑞大药厂 作为蛋白酶c抑制剂的3-酰氨基-吡咯并[3,4-c]吡唑-5(1h,4h,6h)甲醛衍生物
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
JPWO2009130900A1 (ja) * 2008-04-24 2011-08-11 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
WO2011044264A2 (en) * 2009-10-06 2011-04-14 Afraxis, Inc. Pyrrolopyrazoles for treating cns disorders
KR101483215B1 (ko) * 2010-01-29 2015-01-16 한미약품 주식회사 단백질 키나아제 저해활성을 갖는 비시클릭 헤테로아릴 유도체
BR112013012175A2 (pt) 2010-11-17 2019-09-24 Hoffmann La Roche combinação, coadministração, uso e método
US9056877B2 (en) 2011-07-19 2015-06-16 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
CA2862354A1 (en) 2012-02-03 2013-08-08 Basf Se Fungicidal pyrimidine compounds
WO2013113778A1 (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
WO2013113776A1 (en) 2012-02-03 2013-08-08 Basf Se Fungicidal pyrimidine compounds
IN2014DN07224A (pt) 2012-02-03 2015-04-24 Basf Se
WO2013113773A1 (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
WO2013113720A1 (en) 2012-02-03 2013-08-08 Basf Se Fungicidal pyrimidine compounds
WO2013113791A1 (en) 2012-02-03 2013-08-08 Basf Se Fungicidal pyrimidine compounds
WO2013135672A1 (en) 2012-03-13 2013-09-19 Basf Se Fungicidal pyrimidine compounds
IN2014DN07954A (pt) 2012-03-13 2015-05-01 Basf Se
HK1200093A1 (en) 2012-03-16 2015-07-31 霍夫曼-拉罗奇有限公司 Methods of treating melanoma with pak1 inhibitors
CA2882410A1 (en) 2012-09-19 2014-03-27 Novartis Ag Dihydropyrrolidino-pyrimidines as kinase inhibitors
US9388167B2 (en) * 2012-10-15 2016-07-12 Pfizer Ireland Pharmaceuticals Process for the preparation of voriconazole and analogues thereof
CA2923101A1 (en) 2013-09-16 2015-03-19 Basf Se Fungicidal pyrimidine compounds
WO2015036059A1 (en) 2013-09-16 2015-03-19 Basf Se Fungicidal pyrimidine compounds
US10870651B2 (en) 2014-12-23 2020-12-22 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
CN107427521B (zh) 2015-03-27 2021-08-03 达纳-法伯癌症研究所股份有限公司 细胞周期蛋白依赖性激酶的抑制剂
AU2016281225B2 (en) * 2015-06-15 2020-10-15 Ube Corporation Substituted dihydropyrrolopyrazole derivative
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
WO2017112777A1 (en) 2015-12-22 2017-06-29 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
JP7258748B2 (ja) 2016-11-22 2023-04-17 ダナ－ファーバー キャンサー インスティテュート， インコーポレイテッド サイクリン依存性キナーゼ１２（ｃｄｋ１２）の阻害剤およびその使用
KR102736865B1 (ko) 2017-06-21 2024-12-03 샤이 테라퓨틱스 엘엘씨 암, 염증성 질환, 신경발달질환 및 섬유증 질환의 치료를 위하여 Ras 수퍼패밀리와 상호작용하는 화합물
CA3097543A1 (en) * 2018-04-16 2019-10-24 The Regents Of The University Of California Pak4 inhibitors and methods of use
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CN113164477A (zh) 2018-12-14 2021-07-23 达纳-法伯癌症研究所股份有限公司 C-jun-n-末端激酶的吡唑并吡啶抑制剂及其用途
JP7407461B2 (ja) 2018-12-19 2024-01-04 シャイ・セラピューティクス・エルエルシー がん、炎症性疾患、ｒａｓ病、及び線維性疾患の処置のためのｒａｓスーパーファミリーと相互作用する化合物
EP3902542A4 (en) * 2018-12-28 2022-09-07 Dana-Farber Cancer Institute, Inc. CYCLIN DEPENDENT KINASE 7 INHIBITORS AND USES THEREOF
WO2020212484A1 (en) 2019-04-17 2020-10-22 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and compositions for treatment of nlrp3 inflammasome mediated il-1beta dependent disorders
CN114981298B (zh) 2019-12-12 2024-08-20 听治疗有限责任公司 用于预防和治疗听力损失的组合物和方法
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
CN121248675A (zh) * 2020-12-31 2026-01-02 赛诺哈勃药业（成都）有限公司 一种纤溶酶抑制剂、其制备方法及应用
WO2024261302A1 (en) 2023-06-22 2024-12-26 Institut National de la Santé et de la Recherche Médicale Nlrp3 inhibitors, pak1/2 inhibitors and/or caspase 1 inhibitors for use in the treatment of rac2 monogenic disorders
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Also Published As

Publication number Publication date
CN101115760A (zh) 2008-01-30
MX2007008385A (es) 2007-08-21
GEP20094785B (en) 2009-09-25
WO2006072831A1 (en) 2006-07-13
HRP20110485T1 (hr) 2011-07-31
JP4250195B2 (ja) 2009-04-08
CN101115760B (zh) 2010-11-03
ES2365245T3 (es) 2011-09-27
US8067591B2 (en) 2011-11-29
EP1838718B1 (en) 2011-06-15
SI1838718T1 (sl) 2011-08-31
PT1838718E (pt) 2011-08-17
ATE512972T1 (de) 2011-07-15
NO20073859L (no) 2007-10-03
CA2593428A1 (en) 2006-07-13
AP2007004061A0 (en) 2007-08-31
AU2005323797B2 (en) 2009-07-09
CU23778B7 (es) 2012-02-15
TNSN07254A1 (en) 2008-12-31
ZA200705628B (en) 2008-11-26
KR20070096007A (ko) 2007-10-01
AU2005323797A1 (en) 2006-07-13
CA2593428C (en) 2012-04-17
HK1114380A1 (en) 2008-10-31
US20100222342A1 (en) 2010-09-02
EA200701257A1 (ru) 2007-12-28
IL184275A0 (en) 2007-10-31
NZ556273A (en) 2010-01-29
RS51891B (sr) 2012-02-29
DK1838718T3 (da) 2011-07-25
EA011815B1 (ru) 2009-06-30
US20120264751A1 (en) 2012-10-18
MA29141B1 (fr) 2008-01-02
CU20070160A7 (es) 2009-03-16
EP1838718A1 (en) 2007-10-03
US8530652B2 (en) 2013-09-10
CY1111752T1 (el) 2015-10-07
JP2008526826A (ja) 2008-07-24
KR100919343B1 (ko) 2009-09-25
PL1838718T3 (pl) 2011-10-31

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Legal Events

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B11A Dismissal acc. art.33 of ipl - examination not requested within 36 months of filing
B11Y Definitive dismissal - extension of time limit for request of examination expired [chapter 11.1.1 patent gazette]