WO2002066463A1 - 3-(4-amidopyrrol-2-ylmethlidene)-2-indolinone derivatives as protein kinase inhibitors - Google Patents

3-(4-amidopyrrol-2-ylmethlidene)-2-indolinone derivatives as protein kinase inhibitors Download PDF

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Publication number
WO2002066463A1
WO2002066463A1 PCT/US2002/004407 US0204407W WO02066463A1 WO 2002066463 A1 WO2002066463 A1 WO 2002066463A1 US 0204407 W US0204407 W US 0204407W WO 02066463 A1 WO02066463 A1 WO 02066463A1
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WO
WIPO (PCT)
Prior art keywords
oxo
dihydro
hydroxy
pyrrole
dimethyl
Prior art date
Application number
PCT/US2002/004407
Other languages
English (en)
French (fr)
Inventor
Huiping Guan
Congxin Liang
Li Sun
Peng Cho Tang
Chung Chen Wei
Michael A. Mauragis
Tomas Vojkovsky
Qingwu Jin
Paul Matthew Herrinton
Original Assignee
Pharmacia & Upjohn Company
Sugen, Inc.
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
Priority to AU2002247133A priority Critical patent/AU2002247133B2/en
Priority to MXPA03007367A priority patent/MXPA03007367A/es
Priority to UA2003087745A priority patent/UA75635C2/uk
Priority to EP02714897A priority patent/EP1370554B1/en
Priority to JP2002565978A priority patent/JP3677501B2/ja
Priority to SI200230238T priority patent/SI1370554T1/sl
Priority to DE60206736T priority patent/DE60206736T2/de
Priority to CNB028066804A priority patent/CN100338059C/zh
Priority to PL02364176A priority patent/PL364176A1/xx
Priority to AT02714897T priority patent/ATE307128T1/de
Application filed by Pharmacia & Upjohn Company, Sugen, Inc. filed Critical Pharmacia & Upjohn Company
Priority to EA200300793A priority patent/EA007186B1/ru
Priority to SK1133-2003A priority patent/SK11332003A3/sk
Priority to APAP/P/2003/002836A priority patent/AP1718A/en
Priority to NZ527572A priority patent/NZ527572A/en
Priority to BR0207494-0A priority patent/BR0207494A/pt
Priority to KR1020037010772A priority patent/KR100884858B1/ko
Priority to IL15741802A priority patent/IL157418A0/xx
Priority to EEP200300385A priority patent/EE200300385A/xx
Priority to HU0303146A priority patent/HUP0303146A3/hu
Priority to CA2438314A priority patent/CA2438314C/en
Publication of WO2002066463A1 publication Critical patent/WO2002066463A1/en
Priority to JP2003569632A priority patent/JP2005528344A/ja
Priority to US10/367,008 priority patent/US7119209B2/en
Priority to PCT/US2003/004520 priority patent/WO2003070725A2/en
Priority to YU70904A priority patent/RS70904A/sr
Priority to KR1020047012598A priority patent/KR100657110B1/ko
Priority to CNB038039885A priority patent/CN1308326C/zh
Priority to BR0307721-7A priority patent/BR0307721A/pt
Priority to PL03372302A priority patent/PL372302A1/xx
Priority to CA002475455A priority patent/CA2475455A1/en
Priority to AU2003216282A priority patent/AU2003216282A1/en
Priority to RU2004124711/04A priority patent/RU2299209C2/ru
Priority to MXPA04006992A priority patent/MXPA04006992A/es
Priority to EP03742760A priority patent/EP1476443A2/en
Priority to IL157418A priority patent/IL157418A/en
Priority to ZA2003/06335A priority patent/ZA200306335B/en
Priority to NO20033608A priority patent/NO326604B1/no
Priority to HR20030657A priority patent/HRP20030657B1/xx
Priority to IS6913A priority patent/IS2411B/is
Priority to HK04102229A priority patent/HK1059621A1/xx
Priority to ZA200405615A priority patent/ZA200405615B/en
Priority to US11/095,433 priority patent/US20050171357A1/en
Priority to HK05109991A priority patent/HK1078075A1/xx

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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
PCT/US2002/004407 2001-02-15 2002-02-15 3-(4-amidopyrrol-2-ylmethlidene)-2-indolinone derivatives as protein kinase inhibitors WO2002066463A1 (en)

Priority Applications (42)

Application Number Priority Date Filing Date Title
EA200300793A EA007186B1 (ru) 2001-02-15 2002-02-15 Производные 3-(4-амидопиррол-2-илметилиден)-2-индолинона в качестве ингибиторов протеинкиназ
MXPA03007367A MXPA03007367A (es) 2001-02-15 2002-02-15 Derivados de 3-(4-amidopirrol-2-ilmetilideno)-2-indolinona como inhibidores de proteina cinasa.
EP02714897A EP1370554B1 (en) 2001-02-15 2002-02-15 3-(4-amidopyrrol-2-ylmethylidene)-2-indolinone derivatives as protein kinase inhibitors
JP2002565978A JP3677501B2 (ja) 2001-02-15 2002-02-15 蛋白質キナーゼ阻害剤としての３−（４−アミドピロール−２−イルメチリデン）−２−インドリノン誘導体
SI200230238T SI1370554T1 (sl) 2001-02-15 2002-02-15 3-(4-amidopirol-2-ilmetiliden)-2-indolinonski derivati kot inhibitorji protein kinaze
DE60206736T DE60206736T2 (de) 2001-02-15 2002-02-15 3-(4-amidopyrrol-2-ylmethylidene)-2-indolinon-derivative als protein-kinase inhibitoren
CNB028066804A CN100338059C (zh) 2001-02-15 2002-02-15 作为蛋白激酶抑制剂的3－(4－酰氨基吡咯－2－基亚甲基)－2－二氢吲哚酮衍生物
SK1133-2003A SK11332003A3 (sk) 2001-02-15 2002-02-15 Deriváty 3-(4-amidopyrol-2-ylmetylidén)-2-indolinónu ako inhibítory proteínkinázy
AT02714897T ATE307128T1 (de) 2001-02-15 2002-02-15 3-(4-amidopyrrol-2-ylmethylidene)-2-indolinon- derivative als protein-kinase inhibitoren
AU2002247133A AU2002247133B2 (en) 2001-02-15 2002-02-15 3-(4-amidopyrrol-2-ylmethlidene)-2-indolinone derivatives as protein kinase inhibitors
UA2003087745A UA75635C2 (en) 2001-02-15 2002-02-15 Derivatives of 3-(4-amidopyrol-2-ylmethyliden)-2-indolinone as inhibitors of protein kinase
PL02364176A PL364176A1 (en) 2001-02-15 2002-02-15 3-(4-amidopyrrol-2-ylmethlidene)-2-indolinone derivatives as protein kinase inhibitors
APAP/P/2003/002836A AP1718A (en) 2001-02-15 2002-02-15 3-(4-amidopyrrol-2-ylmethlidene)-2-indolinone derivatives as protein kinase inhibitors
NZ527572A NZ527572A (en) 2001-02-15 2002-02-15 3-(4-amidopyrrol-2-ylmethlidene)-2-indolinone derivatives as protein kinase inhibitors
BR0207494-0A BR0207494A (pt) 2001-02-15 2002-02-15 Derivados de 3-(4-amidopirrol-2-ilmetilideno)-2-indolinona como inibidores de proteìna quinase
KR1020037010772A KR100884858B1 (ko) 2001-02-15 2002-02-15 단백질 키나제 억제제로서의3-(4-아미도피롤-2-일메틸리덴)-2-인돌리논 유도체
IL15741802A IL157418A0 (en) 2001-02-15 2002-02-15 3-(4-amidopyrrol-2-ylmethylidene)-2-indolinone derivatives as protein kinase inhibitors
EEP200300385A EE200300385A (et) 2001-02-15 2002-02-15 3-(4-amidopürrool-2-üülmetülideen)-2-indolinooni derivaadid kui proteiini kinaasi inhibiitorid
HU0303146A HUP0303146A3 (en) 2001-02-15 2002-02-15 3-(4-amidopyrrol-2-ylmethlidene)-2-indolinone derivatives as protein kinase inhibitors and pharmaceutical compositions containing them
CA2438314A CA2438314C (en) 2001-02-15 2002-02-15 3-(4-amidopyrrol-2-ylmethylidene)-2-indolinone derivatives as protein kinase inhibitors
EP03742760A EP1476443A2 (en) 2002-02-15 2003-02-14 Process for preparing indolinone derivatives
JP2003569632A JP2005528344A (ja) 2002-02-15 2003-02-14 インドリノン誘導体の製造法
MXPA04006992A MXPA04006992A (es) 2002-02-15 2003-02-14 Procedimiento para preparar derivados de indolinona.
PCT/US2003/004520 WO2003070725A2 (en) 2002-02-15 2003-02-14 Process for preparing indolinone derivatives
YU70904A RS70904A (en) 2002-02-15 2003-02-14 Process for preparing indolinone derivatives
KR1020047012598A KR100657110B1 (ko) 2002-02-15 2003-02-14 인돌리논 유도체의 제조방법
CNB038039885A CN1308326C (zh) 2002-02-15 2003-02-14 吲哚满酮衍生物的制备方法
BR0307721-7A BR0307721A (pt) 2002-02-15 2003-02-14 Processo para preparação de derivados de indolinona
PL03372302A PL372302A1 (en) 2002-02-15 2003-02-14 Process for preparing indolinone derivatives
CA002475455A CA2475455A1 (en) 2002-02-15 2003-02-14 Process for preparing indolinone derivatives
AU2003216282A AU2003216282A1 (en) 2002-02-15 2003-02-14 Process for preparing indolinone derivatives
RU2004124711/04A RU2299209C2 (ru) 2002-02-15 2003-02-14 Способ получения производных индолинона
US10/367,008 US7119209B2 (en) 2002-02-15 2003-02-14 Process for preparing indolinone derivatives
IS6913A IS2411B (is) 2001-02-15 2003-08-14 3-(4-amídópýrról-2-ýlmetýlíden)-2-indólínon afleiður sem prótein kínasa hindrar
IL157418A IL157418A (en) 2001-02-15 2003-08-14 Derivatives of 3- (4-amidopyrol-2-ylmethylidene) -2-indolinone The pharmaceutical compositions containing them and their use in the preparation of medicinal preparations for preventive treatment or medical treatment of protein-related kinase diseases
ZA2003/06335A ZA200306335B (en) 2001-02-15 2003-08-14 3-(4-amidopyrrol-2-ylmethlidene)-2-indolinone derivatives as protein kinase inhibitors
NO20033608A NO326604B1 (no) 2001-02-15 2003-08-14 3-(4-amidopyrrol-2-ylmetliden)-2-indolinonderivater, fremstilling av slike, farmasoytiske preparater inneholdende slike, metode for a modulere den katalytiske aktiviteten til en proteinkinase in vitro med slike forbindelser samt anvendelse av slike forbindelser for fremstilling av medikament for behandling av sykdommer hos pattedyr
HR20030657A HRP20030657B1 (en) 2001-02-15 2003-08-14 3-(4-amidopyrrol-2-ylmethylidene)-2-indolinone derivatives as protein kinase inhibitors
HK04102229A HK1059621A1 (en) 2001-02-15 2004-03-25 3-(4-Amidopyrrol-2-ylmethylidene)-2-indolinone derivatives as protein kinase inhibitors
ZA200405615A ZA200405615B (en) 2001-02-15 2004-07-14 Process for preparing indoline derivatives.
US11/095,433 US20050171357A1 (en) 2002-02-15 2005-03-30 Process for preparing indolinone derivatives
HK05109991A HK1078075A1 (en) 2002-02-15 2005-11-09 Process for preparing indolinone derivatives

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US26868301P 2001-02-15 2001-02-15
US60/268,683 2001-02-15
US31236101P 2001-08-15 2001-08-15
US60/312,361 2001-08-15

Related Child Applications (1)

Application Number Title Priority Date Filing Date
US10/367,008 Continuation-In-Part US7119209B2 (en) 2002-02-15 2003-02-14 Process for preparing indolinone derivatives

Publications (1)

Publication Number Publication Date
WO2002066463A1 true WO2002066463A1 (en) 2002-08-29

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PCT/US2002/004407 WO2002066463A1 (en) 2001-02-15 2002-02-15 3-(4-amidopyrrol-2-ylmethlidene)-2-indolinone derivatives as protein kinase inhibitors

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WO2003070725A2 (en) * 2002-02-15 2003-08-28 Pharmacia & Upjohn Company Process for preparing indolinone derivatives
EP1446117A2 (en) * 2001-10-26 2004-08-18 Sugen, Inc. Treatment of acute myeloid leukemia with indolinone compounds
WO2005033098A1 (en) * 2003-10-02 2005-04-14 Pharmacia & Upjohn Company Llc Salts and polymorphs of a pyrrole-substituted indolinone compound
US7105563B2 (en) 2003-10-24 2006-09-12 Schering Aktiengesellschaft Indolinone derivatives and their use in treating disease-states such as cancer
JP2007500137A (ja) * 2003-07-28 2007-01-11 ビーエーエスエフ　アクチェンゲゼルシャフト 無水マレイン酸の製造方法
JP2007512353A (ja) * 2003-11-26 2007-05-17 ザ スクリプス リサーチ インスティテュート 高機能インドリノン系プロテインキナーゼ阻害剤
EP1893194A1 (en) * 2005-05-26 2008-03-05 The Scripps Research Institute Enhanced indolinone based protein kinase inhibitors
CN100430060C (zh) * 2002-11-15 2008-11-05 苏根公司 用于细胞增殖性障碍的二氢吲哚酮与化疗剂的联合的制药用途
WO2008145398A1 (en) * 2007-06-01 2008-12-04 Pfizer Italia S.R.L. 4-arylpyrrole substituted 2-indoline derivatives active as protein kinase inhibitors
US7683057B2 (en) 2006-09-15 2010-03-23 Tyrogenex, Inc. Kinase inhibitor compounds
JP2011516488A (ja) * 2008-03-31 2011-05-26 テバ ファーマシューティカル インダストリーズ リミティド スニチニブ及びその塩の調製方法
WO2012158810A1 (en) * 2011-05-17 2012-11-22 Principia Biopharma Inc. Tyrosine kinase inhibitors
EA019481B1 (ru) * 2009-08-04 2014-04-30 Ле Лаборатуар Сервье Новые дигидроиндолоновые соединения, способ их получения и фармацевтические композиции, содержащие их
US8829039B2 (en) 2008-05-23 2014-09-09 Shanghai Institute Of Pharmaceutical Industry Dihydroindolinone derivatives
CN104592143A (zh) * 2015-01-23 2015-05-06 四川大学 一种噁唑烷酮类化合物的制备方法
MD4507C1 (ro) * 2013-07-12 2018-03-31 Les Laboratoires Servier Metansulfonat de 3-[((3Z)-3-{[4-(4-morfolinilmetil)-1H-pirol-2-il]metilen}-2-oxo-2,3-dihidro-1H-indol-5-il)metil]-1,3-tiazolidin-2,4-dionă, procedeu de obţinere a lui şi forme preparative care îl conţin
US10456403B2 (en) 2014-02-21 2019-10-29 Principia Biopharma Inc. Salts and solid form of a BTK inhibitor
US10485797B2 (en) 2014-12-18 2019-11-26 Principia Biopharma Inc. Treatment of pemphigus
US10533013B2 (en) 2012-09-10 2020-01-14 Principia Biopharma Inc. Substituted pyrazolo[3,4-d]pyrimidines as kinase inhibitors
US10947215B2 (en) 2015-08-31 2021-03-16 Dong-A Socio Holdings Co., Ltd. Heteroaryl compounds and their use as therapeutic drugs
US11155544B2 (en) 2015-06-24 2021-10-26 Principia Biopharma Inc. Heterocycle comprising tyrosine kinase inhibitors
US11872229B2 (en) 2016-06-29 2024-01-16 Principia Biopharma Inc. Modified release formulations of 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

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US6861442B1 (en) * 1998-12-30 2005-03-01 Sugen, Inc. PYK2 and inflammation
AR042586A1 (es) * 2001-02-15 2005-06-29 Sugen Inc 3-(4-amidopirrol-2-ilmetiliden)-2-indolinona como inhibidores de la protein quinasa; sus composiciones farmaceuticas; un metodo para la modulacion de la actividad catalitica de la proteinquinasa; un metodo para tratar o prevenir una afeccion relacionada con la proteinquinasa
AU2003233576A1 (en) * 2002-05-17 2003-12-02 Sugen, Inc. Novel biomarkers of tyrosine kinase inhibitor exposure and activity in mammals
US20040209937A1 (en) * 2003-02-24 2004-10-21 Sugen, Inc. Treatment of excessive osteolysis with indolinone compounds
CN102127058A (zh) 2004-05-14 2011-07-20 辉瑞产品有限公司 治疗异常细胞生长的嘧啶衍生物
US20060009510A1 (en) * 2004-07-09 2006-01-12 Pharmacia & Upjohn Company Llc Method of synthesizing indolinone compounds
CN102886045A (zh) * 2005-02-03 2013-01-23 综合医院公司 治疗吉非替尼耐药性癌症的方法
MX2007011767A (es) * 2005-03-23 2007-10-18 Pfizer Prod Inc Terapia de combinacion de anticuerpo anti-ctla4 e indolinona para el tratamiento del cancer.
AP2552A (en) 2005-04-26 2013-01-08 Pfizer P-cadherin antibodies
PL2960253T3 (pl) 2005-09-07 2018-11-30 Amgen Fremont Inc. Ludzkie przeciwciała monoklonalne przeciwko kinazie podobnej do receptora aktywiny-1
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