[go: up one dir, main page]

AR018408A1 - Compuesto pirrol sustituido 2-indolinona, composicion farmaceutica que lo comprende, uso de dicho compuesto en un metodo ''in vivo'' y su uso para lapreparacion de dicha composicion - Google Patents

Compuesto pirrol sustituido 2-indolinona, composicion farmaceutica que lo comprende, uso de dicho compuesto en un metodo ''in vivo'' y su uso para lapreparacion de dicha composicion

Info

Publication number
AR018408A1
AR018408A1 ARP990102526A ARP990102526A AR018408A1 AR 018408 A1 AR018408 A1 AR 018408A1 AR P990102526 A ARP990102526 A AR P990102526A AR P990102526 A ARP990102526 A AR P990102526A AR 018408 A1 AR018408 A1 AR 018408A1
Authority
AR
Argentina
Prior art keywords
group
carboxyl
alkyl
amido
cycloalkyl
Prior art date
Application number
ARP990102526A
Other languages
English (en)
Original Assignee
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
Application filed by Sugen Inc filed Critical Sugen Inc
Publication of AR018408A1 publication Critical patent/AR018408A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/06Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/30Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/32Oxygen atoms
    • C07D209/34Oxygen atoms in position 2

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
  • Pulmonology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Un compuesto pirrol sustituido 2-indolinona, que tiene la estructura química de la formula (I) en la cual R1 se selecciona del grupo que consiste enhidrogeno, alquilo, alquenilo, alquinilo, cicloalquilo, arilo, oxhidrilo, alcoxilo, C-carboxilo, O-carboxilo, acetilo, C-amido, C-tioamido, sulfonilo ytrihalometanosulfonilo, R2 se selecciona del grupo que consiste en hidrogeno, halogeno, alquilo, cicloalquilo, arilo, heteroarilo y heteroalicíclico. R3, R4,R5y R6 se seleccionan independientemente delgrupo que consiste en hidrogeno, alquilo, trihaloalquilo, cicloalquilo, alquenilo, alquinilo, arilo, heteroarilo,heteroalicíclico, oxhidrilo, alcoxilo, ariloxilo, mercapto, alquiltio, ariltio, sulfinilo, sulfonilo, S-sulfonamido, N-sulfonamido, triohalometanosulfonamido,carbonilo, C-carboxilo, O-carboxilo, C-amido, N-amido, ciano, nitro, halo, O-carbamilo, N-carbamilo, O-tiocarbamilo, N-tiocarbamilo, amino NR11R12, R11 y R12se seleccionan independientemente del grupo que consiste en hidrogeno,alquilo, cicloalquilo, arilo, carbonilo, acetilo, sulfonilo, trifluorometanosulfonilo, ycuando está combinado, es un anillo heteroalicíclico de cinco o seis miembros, R3 y R4, R4 y R5 o R4 y R5 se pueden combinar para formar un anillo de seismiembros, un grupo metilendioxi o un grupo etilendioxi, R7 se selecciona del grupo que consiste en hidrogeno, alquilo, cicloalquilo, alquenilo, alquinilo,arilo, heteroarilo, heteroalicíclico, oxhidrilo, alcoxilo, ariloxilo, carbonilo, acetilo,C-amido,C-tioamido, amidino, C-carboxilo,O-carboxilo, sulfonilo ytrihalometanosulfonilo; R8,R9 y R10se seleccionan independientemente del grupo formado de H, alquilo, trihaloalquilo, cicloalquilo, alquenilo, alquinilo,arilo,heteroarilo,heterolalicíclico, oxhidrilo,alcoxilo, ariloxilo, mercapto, alquiltio, ariltio, sulfinilo, sulfonilo, S-sulfonamido, N-sulfonamido, carbonilo, C-carboxilo, O-carboxilo,ciano, nitro, halo, O-carbamilo, N-carbamilo, O-tiocarbamilo, N-tiocarbamilo, C-amido, N-amido, amino y NR11R12, con la condicion de quepor lo menos uno de R8,R9 y R10 sea un grupo que tiene la formula: (alqu1)Z en la cual Alqu1 se selecciona del grupo formado de alquilo, alquenilo, o alquinilo
ARP990102526A 1998-05-29 1999-05-28 Compuesto pirrol sustituido 2-indolinona, composicion farmaceutica que lo comprende, uso de dicho compuesto en un metodo ''in vivo'' y su uso para lapreparacion de dicha composicion AR018408A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US8731098P 1998-05-29 1998-05-29
US11610699P 1999-01-15 1999-01-15

Publications (1)

Publication Number Publication Date
AR018408A1 true AR018408A1 (es) 2001-11-14

Family

ID=26776832

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP990102526A AR018408A1 (es) 1998-05-29 1999-05-28 Compuesto pirrol sustituido 2-indolinona, composicion farmaceutica que lo comprende, uso de dicho compuesto en un metodo ''in vivo'' y su uso para lapreparacion de dicha composicion

Country Status (23)

Country Link
US (2) US6395734B1 (es)
EP (2) EP1082305A4 (es)
JP (1) JP4528440B2 (es)
KR (1) KR100743287B1 (es)
CN (1) CN1250526C (es)
AR (1) AR018408A1 (es)
AU (1) AU759226B2 (es)
BR (1) BR9910792A (es)
CA (1) CA2314156C (es)
CO (1) CO5031249A1 (es)
DK (1) DK2020408T3 (es)
EA (1) EA005032B1 (es)
ES (1) ES2429573T3 (es)
HU (1) HUP0103617A2 (es)
IL (2) IL139934A (es)
NO (1) NO318083B1 (es)
NZ (1) NZ508815A (es)
PL (1) PL344477A1 (es)
PT (1) PT2020408E (es)
SK (1) SK287132B6 (es)
TR (1) TR200003514T2 (es)
TW (1) TWI229073B (es)
WO (1) WO1999061422A1 (es)

Families Citing this family (266)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6906093B2 (en) * 1995-06-07 2005-06-14 Sugen, Inc. Indolinone combinatorial libraries and related products and methods for the treatment of disease
US5880141A (en) 1995-06-07 1999-03-09 Sugen, Inc. Benzylidene-Z-indoline compounds for the treatment of disease
US6316429B1 (en) * 1997-05-07 2001-11-13 Sugen, Inc. Bicyclic protein kinase inhibitors
US6051593A (en) * 1997-06-20 2000-04-18 Sugen, Inc. 3-(cycloalkanoheteroarylidenyl)-2- indolinone protein tyrosine kinase inhibitors
US6569868B2 (en) 1998-04-16 2003-05-27 Sugen, Inc. 2-indolinone derivatives as modulators of protein kinase activity
EP1082305A4 (en) 1998-05-29 2001-09-26 Sugen Inc PYRROL SUBSTITUTED 2-INDOLINONE EFFECTIVE AS A PROTEIN KINASE INHIBITOR
CA2354591A1 (en) 1998-12-17 2000-06-22 F. Hoffmann-La Roche Ag 4-aryloxindoles as inhibitors of jnk protein kinases
AU770375B2 (en) * 1998-12-17 2004-02-19 F. Hoffmann-La Roche Ag 4-alkenyl (and alkynyl) oxindoles as inhibitors of cyclin-dependent kinases, in particular CDK2
US6153634A (en) * 1998-12-17 2000-11-28 Hoffmann-La Roche Inc. 4,5-azolo-oxindoles
US20030119895A1 (en) * 1998-12-23 2003-06-26 Pharmacia Corporation Methods using a combination of a 3-heteroaryl-2-indolinone and a cyclooxygenase-2 inhibitor for the treatment of neoplasia
US6689806B1 (en) * 1999-03-24 2004-02-10 Sugen, Inc. Indolinone compounds as kinase inhibitors
UA74803C2 (uk) 1999-11-11 2006-02-15 Осі Фармасьютікалз, Інк. Стійкий поліморф гідрохлориду n-(3-етинілфеніл)-6,7-біс(2-метоксіетокси)-4-хіназолінаміну, спосіб його одержання (варіанти) та фармацевтичне застосування
US6878733B1 (en) 1999-11-24 2005-04-12 Sugen, Inc. Formulations for pharmaceutical agents ionizable as free acids or free bases
JP5336686B2 (ja) * 1999-11-24 2013-11-06 スージェン, インク. 遊離酸または遊離塩基としてイオン化可能な医薬品のための処方
US6313310B1 (en) 1999-12-15 2001-11-06 Hoffmann-La Roche Inc. 4-and 5-alkynyloxindoles and 4-and 5-alkenyloxindoles
EP1255536B1 (en) * 1999-12-22 2006-06-28 Sugen, Inc. Indolinone derivatives for modulation of c-kit tyrosine protein kinase
US6339100B1 (en) 1999-12-29 2002-01-15 The Trustees Of Columbia University In The City Of New York Methods for inhibiting mastocytosis
ES2269156T3 (es) * 1999-12-30 2007-04-01 Sugen, Inc. Compuestos de heteroarilidenil-3-indolinona para modular la actividad de proteina-quinasas y para el uso en quimioterapia del cancer.
MY130363A (en) * 2000-02-15 2007-06-29 Sugen Inc "pyrrole substituted 2-indolinone protein kinase inhibitors"
MXPA02010759A (es) 2000-05-02 2004-07-30 Sugen Inc Derivados del acido (2-oxindol-3-ilidenil) acetico y su uso como inhibidores de la proteina quinasa.
MY128450A (en) 2000-05-24 2007-02-28 Upjohn Co 1-(pyrrolidin-1-ylmethyl)-3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives
US6706709B2 (en) 2000-06-02 2004-03-16 Sugen, Inc. Indolinone derivatives as protein kinase/phosphatase inhibitors
CA2414468A1 (en) * 2000-06-30 2002-01-10 Sugen, Inc. 4-heteroaryl-3-heteroarylidenyl-2-indolinones and their use as protein kinase inhibitors
CA2432114A1 (en) 2000-12-20 2002-07-18 Sugen, Inc. 4-(hetero)aryl substituted indolinones
MX349009B (es) 2001-01-05 2017-07-06 Pfizer Anticuerpos contra el receptor del factor de crecimiento similar a insulina.
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
US7186745B2 (en) 2001-03-06 2007-03-06 Astrazeneca Ab Indolone derivatives having vascular damaging activity
US6797725B2 (en) 2001-04-09 2004-09-28 Sugen, Inc. Prodrugs of a 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives
KR20040000507A (ko) * 2001-05-24 2004-01-03 야마노우치세이야쿠 가부시키가이샤 3-퀴놀린-2(1h)-일리덴인돌린-2-온 유도체
AU2002303892A1 (en) * 2001-05-30 2002-12-09 Jingrong Cui 5-aralkylsulfonyl-3- (pyrrol-2-ylmethylidene)-2-indolinone derivatives as kinase inhibitors
WO2003000194A2 (en) 2001-06-21 2003-01-03 Pfizer Inc. Thienopyridine and thienopyrimidine anticancer agents
JP2004537536A (ja) 2001-06-29 2004-12-16 アブ サイエンス アレルギー疾患を治療するためのチロシンキナーゼ阻害剤の使用方法
DK1401415T3 (da) 2001-06-29 2006-10-16 Ab Science Anvendelse af N-phenyl-2-pyrimidinamin-derivater til behandling af inflammatoriske sygdomme
EP1401411A2 (en) * 2001-06-29 2004-03-31 AB Science Use of tyrosine kinase inhibitors for treating bone loss
DK1401416T5 (da) 2001-06-29 2007-03-19 Ab Science Anvendelse af C-kit-inhibitorer til behandling af inflammatorisk tarmsygdom
ATE376182T1 (de) 2001-06-29 2007-11-15 Ab Science C-kit inhibitoren
AR038957A1 (es) 2001-08-15 2005-02-02 Pharmacia Corp Terapia de combinacion para el tratamiento del cancer
MXPA04003385A (es) 2001-10-10 2005-04-11 Sugen Inc Derivados de 3-?4-substituido con heterociclilo)-pirrol-2-ilmetilidene?-2-indolinona como inhibidores de cinasa.
TWI259081B (en) * 2001-10-26 2006-08-01 Sugen Inc Treatment of acute myeloid leukemia with indolinone compounds
AR039067A1 (es) 2001-11-09 2005-02-09 Pfizer Prod Inc Anticuerpos para cd40
US20030187026A1 (en) 2001-12-13 2003-10-02 Qun Li Kinase inhibitors
US6797825B2 (en) 2001-12-13 2004-09-28 Abbott Laboratories Protein kinase inhibitors
RU2316554C2 (ru) 2001-12-27 2008-02-10 Тереванс, Инк. Производные индолина, используемые как ингибиторы протеинкиназы
WO2003074529A2 (en) 2002-03-01 2003-09-12 Pfizer Inc. iNDOLYL-UREA DERIVATIVES OF THIENOPYRIDINES USEFUL AS ANTI-ANGIOGENIC AGENTS
CA2483142A1 (en) * 2002-05-06 2003-11-20 Genentech, Inc. Use of vegf for treating bone defects
UA77303C2 (en) 2002-06-14 2006-11-15 Pfizer Derivatives of thienopyridines substituted by benzocondensed heteroarylamide useful as therapeutic agents, pharmaceutical compositions and methods for their use
AU2003249366A1 (en) 2002-06-24 2004-01-06 Tufts University Silk biomaterials and methods of use thereof
US20050032871A1 (en) * 2002-09-03 2005-02-10 Sugen, Inc. Sulfonylated pyrrole-2-indolinone derivatives as kinase inhibitors
AR042042A1 (es) * 2002-11-15 2005-06-08 Sugen Inc Administracion combinada de una indolinona con un agente quimioterapeutico para trastornos de proliferacion celular
EP1581309A4 (en) 2002-11-15 2009-07-29 Exelixis Inc KINASE MODULATORS
WO2004048366A1 (ja) * 2002-11-22 2004-06-10 Yamanouchi Pharmaceutical Co., Ltd. 2−オキソインドリン誘導体
JP4879492B2 (ja) * 2002-11-27 2012-02-22 アラーガン、インコーポレイテッド 疾患の治療のためのキナーゼ阻害剤
RS20050430A (sr) 2002-12-19 2007-08-03 Pfizer Inc., Jedinjenja 2-(1h-indazol-6-ilamino)- benzamida kao inhibitori protein kinaza, korisni u tretmanu oftalmoloških bolesti
US7230098B2 (en) 2003-02-26 2007-06-12 Sugen, Inc. Aminoheteroaryl compounds as protein kinase inhibitors
US20040266843A1 (en) * 2003-03-07 2004-12-30 Sugen, Inc. Sulfonamide substituted indolinones as inhibitors of DNA dependent protein kinase (DNA-PK)
US7157577B2 (en) * 2003-03-07 2007-01-02 Sugen Inc. 5-sulfonamido-substituted indolinone compounds as protein kinase inhibitors
JP4698596B2 (ja) 2003-04-10 2011-06-08 タフツ ユニバーシティー 濃縮された水性シルクフィブロイン溶液およびそれらの使用
AR042955A1 (es) 2003-07-18 2005-07-13 Amgen Inc Agentes de union especifica al factor de crecimiento de hepatocitos
HN2004000285A (es) 2003-08-04 2006-04-27 Pfizer Prod Inc ANTICUERPOS DIRIGIDOS A c-MET
JP2007501229A (ja) * 2003-08-06 2007-01-25 スゲン,インコーポレイティド 強力なプロテインキナーゼ阻害剤としての幾何学的に束縛された3−シクロペンチリデン−1,3−ジヒドロインドール−2−オン類
JP2007504122A (ja) 2003-08-29 2007-03-01 ファイザー・インク 新規抗血管形成剤として有用なチエノピリジン−フェニルアセトアミドおよびその誘導体
AR045563A1 (es) 2003-09-10 2005-11-02 Warner Lambert Co Anticuerpos dirigidos a m-csf
BRPI0415773A (pt) 2003-10-24 2006-12-26 Schering Ag derivados de indolinona e sua aplicação no tratamento de estados de doença tais como cáncer
DK1689721T3 (da) * 2003-11-26 2010-09-20 Pfizer Prod Inc Aminopyrazolderivater som GSK-3-ihibitorer
GEP20084572B (en) 2003-12-23 2008-12-25 Pfizer Novel quinoline derivatives
JP2008504292A (ja) 2004-06-24 2008-02-14 ノバルティス ヴァクシンズ アンド ダイアグノスティクス, インコーポレイテッド 免疫増強用の化合物
CN101014365B (zh) 2004-07-16 2011-04-13 辉瑞产品公司 使用抗-igf-1r抗体联合治疗非血液的恶性肿瘤
CA2578066C (en) 2004-08-26 2011-10-11 Pfizer Inc. Enantiomerically pure aminoheteroaryl compounds as protein kinase inhibitors
GT200500321A (es) * 2004-11-09 2006-09-04 Compuestos y composiciones como inhibidores de proteina kinase.
EP1827434B1 (en) 2004-11-30 2014-01-15 Amgen Inc. Quinolines and quinazoline analogs and their use as medicaments for treating cancer
US8093011B2 (en) 2005-03-16 2012-01-10 Haley John D Biological markers predictive of anti-cancer response to epidermal growth factor receptor kinase inhibitors
WO2006105488A2 (en) 2005-03-31 2006-10-05 Agensys, Inc. Antibodies and related molecules that bind to 161p2f10b proteins
KR100990027B1 (ko) 2005-04-26 2010-10-26 화이자 인코포레이티드 P-카드헤린 항체
WO2006119148A2 (en) * 2005-04-29 2006-11-09 The Ohio State University Research Foundation Keratinocyte growth factor receptor - tyrosine specific inhibitors for the prevention of cancer metastatis
DOP2006000195A (es) 2005-09-07 2017-08-15 Amgen Fremont Inc Anticuerpos monoclonales humanos para la quinasa-1 tipo receptor de activina
ATE533057T1 (de) 2005-09-20 2011-11-15 Osi Pharm Inc Biologische marker als prädiktoren der antikrebsreaktion auf insulinähnlichen wachstumsfaktor-1-rezeptor-kinaseinhibitoren
US20080108664A1 (en) 2005-12-23 2008-05-08 Liu Belle B Solid-state form of AMG 706 and pharmaceutical compositions thereof
JO2660B1 (en) 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
DK1973910T3 (da) 2006-01-27 2013-08-12 Shanghai Hengrui Pharm Co Ltd Pyrrolo[3,2-c]pyridin-4-on-2-indolinon-proteinkinaseinhibitorer
AR059066A1 (es) * 2006-01-27 2008-03-12 Amgen Inc Combinaciones del inhibidor de la angiopoyetina -2 (ang2) y el inhibidor del factor de crecimiento endotelial vascular (vegf)
ATE489380T1 (de) 2006-02-10 2010-12-15 Amgen Inc Hydratformen von amg706
KR100647350B1 (ko) * 2006-04-03 2006-11-23 김상민 시밍장치
AR060358A1 (es) 2006-04-06 2008-06-11 Novartis Vaccines & Diagnostic Quinazolinas para la inhibicion de pdk 1
KR20080110912A (ko) 2006-04-19 2008-12-19 노파르티스 아게 인다졸 화합물 및 cdc7의 억제 방법
BRPI0711358A2 (pt) 2006-05-09 2011-09-27 Pfizer Prod Inc derivados do ácido cicloalquilamino e suas composições farmacêuticas
US8217177B2 (en) 2006-07-14 2012-07-10 Amgen Inc. Fused heterocyclic derivatives and methods of use
PE20121506A1 (es) 2006-07-14 2012-11-26 Amgen Inc Compuestos triazolopiridinas como inhibidores de c-met
US20100028451A1 (en) 2006-09-26 2010-02-04 Trustees Of Tufts College Silk microspheres for encapsulation and controlled release
JP2010505834A (ja) * 2006-10-06 2010-02-25 メルク エンド カムパニー インコーポレーテッド 非ヌクレオシド系逆転写酵素阻害剤
CA2672438A1 (en) 2006-12-20 2008-07-03 Amgen Inc. Substituted heterocycles and methods of use
AU2008205252B2 (en) 2007-01-09 2013-02-21 Amgen Inc. Bis-aryl amide derivatives useful for the treatment of cancer
MX2009008531A (es) 2007-02-16 2009-08-26 Amgen Inc Cetonas de heterociclilo que contienen nitrogeno y su uso como inhibidores de c-met.
US9102916B2 (en) 2007-02-27 2015-08-11 Trustees Of Tufts College Tissue-engineered silk organs
US8642067B2 (en) 2007-04-02 2014-02-04 Allergen, Inc. Methods and compositions for intraocular administration to treat ocular conditions
AU2008239594B2 (en) 2007-04-13 2013-10-24 Beth Israel Deaconess Medical Center Methods for treating cancer resistant to ErbB therapeutics
WO2009023615A1 (en) 2007-08-10 2009-02-19 Trustees Of Tufts College Tubular silk compositions and methods of use thereof
EP2592093A1 (en) 2007-08-21 2013-05-15 Amgen, Inc Human c-fms antigen binding proteins
WO2009030270A1 (en) * 2007-09-03 2009-03-12 Novartis Ag Dihydroindole derivatives useful in parkinson's disease
BRPI0820722A2 (pt) 2007-12-20 2015-06-16 Novartis Ag Derivados de tiazol usados como inibidores de pi 3 cinases
US8993615B2 (en) * 2008-08-08 2015-03-31 The Johns Hopkins University Compositions and methods for treatment of neurodegenerative disease
EP2334701A4 (en) 2008-10-16 2014-01-08 Univ Pittsburgh FULLY HUMAN ANTIBODIES AGAINST ANTIGENES ASSOCIATED WITH MELANOMA OF HIGH MOLECULAR WEIGHT AND USES THEREOF
CN101397295B (zh) * 2008-11-12 2012-04-25 深圳微芯生物科技有限责任公司 作为组蛋白去乙酰化酶抑制剂的2-吲哚满酮衍生物、其制法和用途
CA2748943A1 (en) 2009-02-09 2010-08-12 Supergen, Inc. Pyrrolopyrimidinyl axl kinase inhibitors
US20120189641A1 (en) 2009-02-25 2012-07-26 OSI Pharmaceuticals, LLC Combination anti-cancer therapy
WO2010099137A2 (en) 2009-02-26 2010-09-02 Osi Pharmaceuticals, Inc. In situ methods for monitoring the emt status of tumor cells in vivo
EP2401613A2 (en) 2009-02-27 2012-01-04 OSI Pharmaceuticals, LLC Methods for the identification of agents that inhibit mesenchymal-like tumor cells or their formation
WO2010099138A2 (en) 2009-02-27 2010-09-02 Osi Pharmaceuticals, Inc. Methods for the identification of agents that inhibit mesenchymal-like tumor cells or their formation
TW201035088A (en) 2009-02-27 2010-10-01 Supergen Inc Cyclopentathiophene/cyclohexathiophene DNA methyltransferase inhibitors
US8642834B2 (en) 2009-02-27 2014-02-04 OSI Pharmaceuticals, LLC Methods for the identification of agents that inhibit mesenchymal-like tumor cells or their formation
US8293753B2 (en) 2009-07-02 2012-10-23 Novartis Ag Substituted 2-carboxamide cycloamino ureas
AU2010273585B2 (en) 2009-07-13 2015-04-23 Genentech, Inc. Diagnostic methods and compositions for treatment of cancer
US20120128670A1 (en) 2009-07-31 2012-05-24 OSI Pharmaceuticals, LLC mTOR INHIBITOR AND ANGIOGENESIS INHIBITOR COMBINATION THERAPY
WO2011027249A2 (en) 2009-09-01 2011-03-10 Pfizer Inc. Benzimidazole derivatives
KR20120105423A (ko) 2009-09-11 2012-09-25 제넨테크, 인크. 항암제에 반응할 증가된 가능성을 갖는 환자를 확인하는 방법
MX2012002909A (es) 2009-09-17 2012-04-19 Hoffmann La Roche Metodos y composiciones para su uso en diagnostico de pacientes con cancer.
WO2011073521A1 (en) 2009-12-15 2011-06-23 Petri Salven Methods for enriching adult-derived endothelial progenitor cells and uses thereof
US20120264803A1 (en) 2009-12-25 2012-10-18 Toshinori Oka Method for predicting therapeutic effects of chemotherapy on hepatocellular carcinoma patients
CA2785389A1 (en) 2009-12-25 2011-06-30 Taiho Pharmaceutical Co., Ltd. Antitumor agent or postoperative adjuvant chemotherapeutic agent for hepatocellular carcinoma treatment
KR20120127495A (ko) 2010-02-12 2012-11-21 화이자 인코포레이티드 8-플루오로-2-{4-[(메틸아미노)메틸]페닐}-1,3,4,5-테트라하이드로-6h-아제피노[5,4,3-cd]인돌-6-온의 염 및 다형체
EP2542893A2 (en) 2010-03-03 2013-01-09 OSI Pharmaceuticals, LLC Biological markers predictive of anti-cancer response to insulin-like growth factor-1 receptor kinase inhibitors
JP2013527748A (ja) 2010-03-03 2013-07-04 オーエスアイ・ファーマシューティカルズ,エルエルシー インスリン様増殖因子1受容体キナーゼ阻害剤に対する抗癌反応の予測に役立つ生物学的マーカー
WO2011153224A2 (en) 2010-06-02 2011-12-08 Genentech, Inc. Diagnostic methods and compositions for treatment of cancer
CA2802857C (en) 2010-06-16 2018-09-11 University Of Pittsburgh-Of The Commonwealth System Of Higher Education Antibodies to endoplasmin and their use
WO2011161217A2 (en) 2010-06-23 2011-12-29 Palacký University in Olomouc Targeting of vegfr2
WO2012010550A1 (en) 2010-07-19 2012-01-26 F. Hoffmann-La Roche Ag Method to identify a patient with an increased likelihood of responding to an anti-cancer therapy
KR20130126576A (ko) 2010-07-19 2013-11-20 에프. 호프만-라 로슈 아게 항암요법에 반응할 가능성이 증가된 환자를 확인하는 방법
EP3696195B1 (en) 2010-07-23 2024-02-14 Trustees of Boston University Anti-despr inhibitors as therapeutics for inhibition of pathological angiogenesis and tumor cell invasiveness and for molecular imaging and targeted delivery
AR082418A1 (es) 2010-08-02 2012-12-05 Novartis Ag Formas cristalinas de 1-(4-metil-5-[2-(2,2,2-trifluoro-1,1-dimetil-etil)-piridin-4-il]-tiazol-2-il)-amida de 2-amida del acido (s)-pirrolidin-1,2-dicarboxilico
WO2012042421A1 (en) 2010-09-29 2012-04-05 Pfizer Inc. Method of treating abnormal cell growth
US9056865B2 (en) 2010-10-20 2015-06-16 Pfizer Inc. Pyridine-2-derivatives as smoothened receptor modulators
US8987257B2 (en) 2011-01-31 2015-03-24 Novartis Ag Heterocyclic derivatives
WO2012116040A1 (en) 2011-02-22 2012-08-30 OSI Pharmaceuticals, LLC Biological markers predictive of anti-cancer response to insulin-like growth factor-1 receptor kinase inhibitors in hepatocellular carcinoma
WO2012129344A1 (en) 2011-03-23 2012-09-27 Amgen Inc. Fused tricyclic dual inhibitors of cdk 4/6 and flt3
WO2012142164A1 (en) 2011-04-12 2012-10-18 The United States Of America, As Represented By The Secretary, Department Of Health & Human Services Human monoclonal antibodies that bind insulin-like growth factor (igf) i and ii
TR201905909T4 (tr) 2011-04-19 2019-05-21 Pfizer Kanser tedavisi için anti-4-1bb antikorlarının ve adcc indükleyici antikorların kombinasyonları.
WO2012145652A1 (en) 2011-04-20 2012-10-26 Trustees Of Tufts College Dynamic silk coatings for implantable devices
JP2014519813A (ja) 2011-04-25 2014-08-21 オーエスアイ・ファーマシューティカルズ,エルエルシー 癌薬剤発見、診断、および治療におけるemt遺伝子シグネチャーの使用
PT3409278T (pt) 2011-07-21 2020-12-18 Sumitomo Dainippon Pharma Oncology Inc Inibidores de proteína cinase heterocíclicos
US9745288B2 (en) 2011-08-16 2017-08-29 Indiana University Research And Technology Corporation Compounds and methods for treating cancer by inhibiting the urokinase receptor
JP5914667B2 (ja) 2011-09-22 2016-05-11 ファイザー・インク ピロロピリミジンおよびプリン誘導体
US9783613B2 (en) 2011-10-04 2017-10-10 Igem Therapeutics Limited IgE anti-HMW-MAA antibody
PT2771342T (pt) 2011-10-28 2016-08-17 Novartis Ag Derivados de purina e o seu uso no tratamento de doença
US20140286959A1 (en) 2011-11-08 2014-09-25 Pfizer Inc. Methods of Treating Inflammatory Disorders Using Anti-M-CSF Antibodies
AR090263A1 (es) 2012-03-08 2014-10-29 Hoffmann La Roche Terapia combinada de anticuerpos contra el csf-1r humano y las utilizaciones de la misma
HK1205953A1 (en) 2012-03-20 2015-12-31 Trustees Of Tufts College Silk reservoirs for drug delivery
WO2013152252A1 (en) 2012-04-06 2013-10-10 OSI Pharmaceuticals, LLC Combination anti-cancer therapy
CA2869967A1 (en) 2012-04-13 2013-10-17 Trustees Of Tufts College Methods and compositions for preparing a silk microsphere
JP6177879B2 (ja) 2012-04-20 2017-08-09 アンジー ファーマスーティカル カンパニー リミテッドAnnji Pharamaceutical Co., Ltd. プリンアナログのシクロプロパンカルボキシレートエステル
EP2849756A1 (en) 2012-05-16 2015-03-25 Novartis AG Dosage regimen for a pi-3 kinase inhibitor
US10034945B2 (en) 2012-07-13 2018-07-31 Trustees Of Tufts College Silk powder compaction for production of constructs with high mechanical strength and stiffness
US9505749B2 (en) 2012-08-29 2016-11-29 Amgen Inc. Quinazolinone compounds and derivatives thereof
EP2909181B1 (en) 2012-10-16 2017-08-09 Tolero Pharmaceuticals, Inc. Pkm2 modulators and methods for their use
CN102887851B (zh) * 2012-11-02 2014-03-19 天津希恩思生化科技有限公司 化合物3,5-二甲基-1h-吡咯-2,4-二甲醛及其制备方法
US9260426B2 (en) 2012-12-14 2016-02-16 Arrien Pharmaceuticals Llc Substituted 1H-pyrrolo [2, 3-b] pyridine and 1H-pyrazolo [3, 4-b] pyridine derivatives as salt inducible kinase 2 (SIK2) inhibitors
US10202356B2 (en) 2013-03-14 2019-02-12 Tolero Pharmaceuticals, Inc. JAK2 and ALK2 inhibitors and methods for their use
KR102774944B1 (ko) 2013-03-15 2025-02-27 트러스티즈 오브 터프츠 칼리지 저분자량 실크 조성물 및 안정화 실크 조성물
US11376329B2 (en) 2013-03-15 2022-07-05 Trustees Of Tufts College Low molecular weight silk compositions and stabilizing silk compositions
US9206188B2 (en) 2013-04-18 2015-12-08 Arrien Pharmaceuticals Llc Substituted pyrrolo[2,3-b]pyridines as ITK and JAK inhibitors
US10285702B2 (en) 2013-04-24 2019-05-14 Trustees Of Tufts College Bioresorbable biopolymer anastomosis devices
KR20160058960A (ko) 2013-10-04 2016-05-25 압토스 바이오사이언시스 인코포레이티드 암을 치료하기 위한 조성물과 방법
UA115388C2 (uk) 2013-11-21 2017-10-25 Пфайзер Інк. 2,6-заміщені пуринові похідні та їх застосування в лікуванні проліферативних захворювань
WO2015083101A1 (en) 2013-12-06 2015-06-11 Novartis Ag Dosage regimen for an alpha-isoform selective phosphatidylinositol 3-kinase inhibitor
EP4012049A3 (en) 2014-04-04 2022-08-24 Crown Bioscience, Inc. (Taicang) Methods for determining responsiveness to mek/erk inhibitors
WO2015155624A1 (en) 2014-04-10 2015-10-15 Pfizer Inc. Dihydropyrrolopyrimidine derivatives
GEP20186879B (en) 2014-04-30 2018-07-10 Pfizer Cycloalkyl-linked diheterocycle derivatives
WO2016001789A1 (en) 2014-06-30 2016-01-07 Pfizer Inc. Pyrimidine derivatives as pi3k inhibitors for use in the treatment of cancer
JP6811706B2 (ja) 2014-07-31 2021-01-13 ザ ホンコン ユニヴァーシティ オブ サイエンス アンド テクノロジー Epha4に対するヒトモノクローナル抗体及びそれらの使用
WO2016100721A1 (en) 2014-12-17 2016-06-23 Tufts University Injectable, flexible hydroxyapatite-silk foams for osteochondral and dental repair
JP6621477B2 (ja) 2014-12-18 2019-12-18 ファイザー・インク ピリミジンおよびトリアジン誘導体ならびにaxl阻害薬としてのそれらの使用
HK1247955A1 (zh) 2015-01-08 2018-10-05 小利兰.斯坦福大学托管委员会 提供骨、骨髓及软骨的诱导的因子和细胞
HK1251655A1 (zh) 2015-04-20 2019-02-01 Tolero Pharmaceuticals, Inc. 通过线粒体分析预测对阿伏西地的应答
MX382566B (es) 2015-05-01 2025-03-13 Univ Emory Analogos de nucleosidos para el tratamiento de la familia de virus flaviviridae y cancer
TR201911032T4 (tr) 2015-05-18 2019-08-21 Tolero Pharmaceuticals Inc Artırılmış biyoyararlanıma sahip alvocıdıb ön ilaçları.
WO2017009751A1 (en) 2015-07-15 2017-01-19 Pfizer Inc. Pyrimidine derivatives
AU2016296984B2 (en) 2015-07-20 2021-08-26 Massachusetts Eye And Ear Infirmary Biodegradable silk ear tubes
CN108289861B (zh) 2015-08-03 2021-11-02 大日本住友制药肿瘤公司 用于治疗癌症的组合疗法
AU2016347881A1 (en) 2015-11-02 2018-05-10 Novartis Ag Dosage regimen for a phosphatidylinositol 3-kinase inhibitor
AU2016364855B2 (en) 2015-12-03 2019-08-29 Les Laboratoires Servier MAT2A inhibitors for treating MTAP null cancer
WO2017189832A1 (en) 2016-04-29 2017-11-02 Trustees Of Tufts College An artificial silk based innervated cornea
WO2018006037A1 (en) 2016-07-01 2018-01-04 Trustees Of Tufts College Innervated artificial skin
US11248313B2 (en) 2016-08-01 2022-02-15 Trustees Of Tufts College Biomimetic mechanical tension driven fabrication of nanofibrillar architecture
WO2018060833A1 (en) 2016-09-27 2018-04-05 Novartis Ag Dosage regimen for alpha-isoform selective phosphatidylinositol 3-kinase inhibitor alpelisib
WO2018094275A1 (en) 2016-11-18 2018-05-24 Tolero Pharmaceuticals, Inc. Alvocidib prodrugs and their use as protein kinase inhibitors
US10132797B2 (en) 2016-12-19 2018-11-20 Tolero Pharmaceuticals, Inc. Profiling peptides and methods for sensitivity profiling
CN110366550A (zh) 2016-12-22 2019-10-22 美国安进公司 作为用于治疗肺癌、胰腺癌或结直肠癌的KRAS G12C抑制剂的苯并异噻唑、异噻唑并[3,4-b]吡啶、喹唑啉、酞嗪、吡啶并[2,3-d]哒嗪和吡啶并[2,3-d]嘧啶衍生物
US20200000713A1 (en) 2017-01-20 2020-01-02 Massachusetts Institute Of Technology Injectable polymer micro-depots for controlled local drug delivery
JOP20190272A1 (ar) 2017-05-22 2019-11-21 Amgen Inc مثبطات kras g12c وطرق لاستخدامها
EP3679040B1 (en) 2017-09-08 2022-08-03 Amgen Inc. Inhibitors of kras g12c and methods of using the same
US11497756B2 (en) 2017-09-12 2022-11-15 Sumitomo Pharma Oncology, Inc. Treatment regimen for cancers that are insensitive to BCL-2 inhibitors using the MCL-1 inhibitor alvocidib
US20200237766A1 (en) 2017-10-13 2020-07-30 Tolero Pharmaceuticals, Inc. Pkm2 activators in combination with reactive oxygen species for treatment of cancer
WO2019089567A1 (en) 2017-10-30 2019-05-09 Massachusetts Institute Of Technology Layer-by-layer nanoparticles for cytokine therapy in cancer treatment
US20210236644A1 (en) 2017-11-10 2021-08-05 Cocoon Biotech Inc. Ocular applications of silk-based products
US11090304B2 (en) 2018-05-04 2021-08-17 Amgen Inc. KRAS G12C inhibitors and methods of using the same
MA52496A (fr) 2018-05-04 2021-03-10 Amgen Inc Inhibiteurs de kras g12c et leurs procédés d'utilisation
WO2019217691A1 (en) 2018-05-10 2019-11-14 Amgen Inc. Kras g12c inhibitors for the treatment of cancer
US11096939B2 (en) 2018-06-01 2021-08-24 Amgen Inc. KRAS G12C inhibitors and methods of using the same
JP7357644B2 (ja) 2018-06-11 2023-10-06 アムジエン・インコーポレーテツド がんを処置するためのkras g12c阻害剤
EP3807276B1 (en) 2018-06-12 2025-12-10 Amgen Inc. Kras g12c inhibitors encompassing a piperazine ring and use thereof in the treatment of cancer
JP2021530554A (ja) 2018-07-26 2021-11-11 スミトモ ダイニッポン ファーマ オンコロジー, インコーポレイテッド 異常なacvr1発現を伴う疾患を処置するための方法およびそこで使用するためのacvr1阻害剤
JP7516029B2 (ja) 2018-11-16 2024-07-16 アムジエン・インコーポレーテツド Kras g12c阻害剤化合物の重要な中間体の改良合成法
AU2019384118B2 (en) 2018-11-19 2025-06-12 Amgen Inc. KRAS G12C inhibitors and methods of using the same
JP7377679B2 (ja) 2018-11-19 2023-11-10 アムジエン・インコーポレーテツド がん治療のためのkrasg12c阻害剤及び1種以上の薬学的に活性な追加の薬剤を含む併用療法
JP2022511029A (ja) 2018-12-04 2022-01-28 スミトモ ダイニッポン ファーマ オンコロジー, インコーポレイテッド がんの処置のための薬剤としての使用のためのcdk9インヒビターおよびその多形
IL283639B2 (en) 2018-12-20 2024-06-01 Amgen Inc Kif18a inhibitors
US12459932B2 (en) 2018-12-20 2025-11-04 Amgen Inc. KIF18A inhibitors
ES2997190T3 (en) 2018-12-20 2025-02-14 Amgen Inc Heteroaryl amides useful as kif18a inhibitors
EP3898616B1 (en) 2018-12-20 2024-10-02 Amgen Inc. Heteroaryl amides useful as kif18a inhibitors
CA3127502A1 (en) 2019-02-12 2020-08-20 Sumitomo Dainippon Pharma Oncology, Inc. Formulations comprising heterocyclic protein kinase inhibitors
AU2020232616A1 (en) 2019-03-01 2021-09-09 Revolution Medicines, Inc. Bicyclic heterocyclyl compounds and uses thereof
WO2020180768A1 (en) 2019-03-01 2020-09-10 Revolution Medicines, Inc. Bicyclic heteroaryl compounds and uses thereof
JP2022525149A (ja) 2019-03-20 2022-05-11 スミトモ ダイニッポン ファーマ オンコロジー, インコーポレイテッド ベネトクラクスが失敗した急性骨髄性白血病(aml)の処置
CN113747895A (zh) 2019-03-22 2021-12-03 大日本住友制药肿瘤公司 包含pkm2调节剂的组合物和用其治疗的方法
EP3738593A1 (en) 2019-05-14 2020-11-18 Amgen, Inc Dosing of kras inhibitor for treatment of cancers
JP7092935B2 (ja) 2019-05-21 2022-06-28 アムジエン・インコーポレーテツド 固体形態
EP3975841A1 (en) 2019-05-30 2022-04-06 Massachusetts Institute of Technology Peptide nucleic acid functionalized hydrogel microneedles for sampling and detection of interstitial fluid nucleic acids
US20240352079A1 (en) 2019-06-04 2024-10-24 Cocoon Biotech Inc. Silk-Based Products, Formulations, and Methods of Use
CA3147451A1 (en) 2019-08-02 2021-02-11 Amgen Inc. Kif18a inhibitors
EP4007753B1 (en) 2019-08-02 2025-09-24 Amgen Inc. Kif18a inhibitors
CA3147276A1 (en) 2019-08-02 2021-02-11 Amgen Inc. Kif18a inhibitors
CA3146693A1 (en) 2019-08-02 2021-02-11 Amgen Inc. Kif18a inhibitors
AU2020369569A1 (en) 2019-10-24 2022-04-14 Amgen Inc. Pyridopyrimidine derivatives useful as KRAS G12C and KRAS G12D inhibitors in the treatment of cancer
IL320513A (en) 2019-11-04 2025-06-01 Revolution Medicines Inc RAS inhibitors
CR20220240A (es) 2019-11-04 2022-08-03 Revolution Medicines Inc Inhibidores de ras
US11608346B2 (en) 2019-11-04 2023-03-21 Revolution Medicines, Inc. Ras inhibitors
CN114901662A (zh) 2019-11-08 2022-08-12 锐新医药公司 双环杂芳基化合物及其用途
TW202132271A (zh) 2019-11-14 2021-09-01 美商安進公司 Kras g12c抑制劑化合物之改善的合成
BR112022009390A2 (pt) 2019-11-14 2022-08-09 Amgen Inc Síntese melhorada de composto inibidor de kras g12c
CN114980976A (zh) 2019-11-27 2022-08-30 锐新医药公司 共价ras抑制剂及其用途
WO2021142026A1 (en) 2020-01-07 2021-07-15 Revolution Medicines, Inc. Shp2 inhibitor dosing and methods of treating cancer
WO2021155006A1 (en) 2020-01-31 2021-08-05 Les Laboratoires Servier Sas Inhibitors of cyclin-dependent kinases and uses thereof
EP4168002A1 (en) 2020-06-18 2023-04-26 Revolution Medicines, Inc. Methods for delaying, preventing, and treating acquired resistance to ras inhibitors
CA3187757A1 (en) 2020-09-03 2022-03-24 Ethan AHLER Use of sos1 inhibitors to treat malignancies with shp2 mutations
US11690915B2 (en) 2020-09-15 2023-07-04 Revolution Medicines, Inc. Ras inhibitors
CN112661639A (zh) * 2020-12-07 2021-04-16 浙江工业大学 一种4-乙酰丁酸酯类化合物合成方法
US20240051956A1 (en) 2020-12-22 2024-02-15 Qilu Regor Therapeutics Inc. Sos1 inhibitors and uses thereof
US12161693B2 (en) 2021-04-14 2024-12-10 Cocoon Biotech Inc. Methods of making stable silk fibroin formulations
CN117500811A (zh) 2021-05-05 2024-02-02 锐新医药公司 共价ras抑制剂及其用途
CN118561952A (zh) 2021-05-05 2024-08-30 锐新医药公司 Ras抑制剂
CR20230558A (es) 2021-05-05 2024-01-24 Revolution Medicines Inc Inhibidores de ras para el tratamiento del cáncer
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
KR20240115979A (ko) 2021-11-08 2024-07-26 프로젠토스 테라퓨틱스, 인크. 혈소판-유래 성장 인자 수용체(pdgfr) 알파 억제제 및 이의 용도
US20250282782A1 (en) 2021-12-17 2025-09-11 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
EP4227307A1 (en) 2022-02-11 2023-08-16 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
AU2023230882A1 (en) 2022-03-07 2024-08-22 Amgen Inc. A process for preparing 4-methyl-2-propan-2-yl-pyridine-3-carbonitrile.
CN119136806A (zh) 2022-03-08 2024-12-13 锐新医药公司 用于治疗免疫难治性肺癌的方法
EP4536364A1 (en) 2022-06-10 2025-04-16 Revolution Medicines, Inc. Macrocyclic ras inhibitors
US20230399313A1 (en) * 2022-06-10 2023-12-14 Advenchen Pharmaceuticals, LLC Biological activities of 5-(2-(4-(4-fluoro-2-methyl-1h-indol-5-yloxy)-6-methoxyquinolin-7-yloxy)ethyl)-5-azaspiro[2.4]-heptan-7-ol crystalline, phosphoric acid salt and its enantiomers
EP4601644A1 (en) 2022-10-14 2025-08-20 Black Diamond Therapeutics, Inc. Methods of treating cancers using isoquinoline or 6-aza-quinoline derivatives
CR20250458A (es) 2023-03-30 2025-11-21 Revolution Medicines Inc Composiciones para inducir la hidrólisis de ras gtp y sus usos
WO2024211712A1 (en) 2023-04-07 2024-10-10 Revolution Medicines, Inc. Condensed macrocyclic compounds as ras inhibitors
KR20260005904A (ko) 2023-04-07 2026-01-12 레볼루션 메디슨즈, 인크. 매크로사이클릭 ras 억제제
AU2024252105A1 (en) 2023-04-14 2025-10-16 Revolution Medicines, Inc. Crystalline forms of ras inhibitors, compositions containing the same, and methods of use thereof
AU2024251341A1 (en) 2023-04-14 2025-10-16 Revolution Medicines, Inc. Crystalline forms of a ras inhibitor
AU2024265078A1 (en) 2023-05-04 2025-12-11 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
US20250049810A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
US20250154171A1 (en) 2023-10-12 2025-05-15 Revolution Medicines, Inc. Ras inhibitors
WO2025137507A1 (en) 2023-12-22 2025-06-26 Regor Pharmaceuticals, Inc. Sos1 inhibitors and uses thereof
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors
WO2025255438A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025265060A1 (en) 2024-06-21 2025-12-26 Revolution Medicines, Inc. Therapeutic compositions and methods for managing treatment-related effects
WO2026006747A1 (en) 2024-06-28 2026-01-02 Revolution Medicines, Inc. Ras inhibitors
WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015790A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015796A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer

Family Cites Families (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3308134A (en) 1965-10-22 1967-03-07 Mcneilab Inc Spiro(indan-2, 3'-indoline)-1, 2'-diones
US3859693A (en) 1973-06-12 1975-01-14 Charles P Breed Sliding snap shackle
US4002749A (en) 1975-08-12 1977-01-11 E. R. Squibb & Sons, Inc. Substituted indolinones
US4053613A (en) 1975-09-17 1977-10-11 E. R. Squibb & Sons, Inc. 1,3,thiazolinyl and 1,3 thiazinyl substituted indolinones
US4966849A (en) 1985-09-20 1990-10-30 President And Fellows Of Harvard College CDNA and genes for human angiogenin (angiogenesis factor) and methods of expression
CA1284681C (en) 1986-07-09 1991-06-04 Alcan International Limited Methods and apparatus for the detection and correction of roll eccentricity in rolling mills
US5217999A (en) 1987-12-24 1993-06-08 Yissum Research Development Company Of The Hebrew University Of Jerusalem Styryl compounds which inhibit EGF receptor protein tyrosine kinase
GB9004483D0 (en) 1990-02-28 1990-04-25 Erba Carlo Spa New aryl-and heteroarylethenylene derivatives and process for their preparation
EP0526488B1 (en) 1990-04-02 1994-11-30 Pfizer Inc. Benzylphosphonic acid tyrosine kinase inhibitors
US5302606A (en) 1990-04-16 1994-04-12 Rhone-Poulenc Rorer Pharmaceuticals Inc. Styryl-substituted pyridyl compounds which inhibit EGF receptor tyrosine kinase
WO1992007830A2 (en) 1990-10-29 1992-05-14 Pfizer Inc. Oxindole peptide antagonists
EP0584222B1 (en) 1991-05-10 1997-10-08 Rhone-Poulenc Rorer International (Holdings) Inc. Bis mono-and bicyclic aryl and heteroaryl compounds which inhibit egf and/or pdgf receptor tyrosine kinase
US5480883A (en) 1991-05-10 1996-01-02 Rhone-Poulenc Rorer Pharmaceuticals Inc. Bis mono- and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
CA2108889A1 (en) 1991-05-29 1992-11-30 Robert Lee Dow Tricyclic polyhydroxylic tyrosine kinase inhibitors
GB9300059D0 (en) 1992-01-20 1993-03-03 Zeneca Ltd Quinazoline derivatives
WO1993023040A1 (en) 1992-05-20 1993-11-25 Merck & Co., Inc. 17-ethers and thioethers of 4-aza-steroids
WO1994003427A1 (en) 1992-08-06 1994-02-17 Warner-Lambert Company 2-thioindoles (selenoindoles) and related disulfides (selenides) which inhibit protein tyrosine kinases and which have antitumor properties
US5330992A (en) 1992-10-23 1994-07-19 Sterling Winthrop Inc. 1-cyclopropyl-4-pyridyl-quinolinones
DK1975181T3 (da) 1992-10-28 2011-06-06 Genentech Inc Anvendelse af vaskulære endothelcelle-vækstfaktor-antagonister
US6177401B1 (en) 1992-11-13 2001-01-23 Max-Planck-Gesellschaft Zur Forderung Der Wissenschaften Use of organic compounds for the inhibition of Flk-1 mediated vasculogenesis and angiogenesis
GB9226855D0 (en) 1992-12-23 1993-02-17 Erba Carlo Spa Vinylene-azaindole derivatives and process for their preparation
AU2096895A (en) 1994-03-07 1995-09-25 Sugen, Incorporated Receptor tyrosine kinase inhibitors for inhibiting cell proliferative disorders and compositions thereof
GB9412719D0 (en) 1994-06-24 1994-08-17 Erba Carlo Spa Substituted azaindolylidene compounds and process for their preparation
GB9423997D0 (en) * 1994-11-28 1995-01-11 Erba Carlo Spa Substituted 3-arylidene-7-azaoxindole compounds and process for their preparation
GB9501567D0 (en) 1995-01-26 1995-03-15 Pharmacia Spa Hydrosoluble 3-arylidene-2-oxindole derivatives as tyrosine kinase inhibitors
US5880141A (en) 1995-06-07 1999-03-09 Sugen, Inc. Benzylidene-Z-indoline compounds for the treatment of disease
US5786488A (en) 1996-11-13 1998-07-28 Sugen, Inc. Synthetic methods for the preparation of indolyquinones
EP0931152A2 (en) * 1996-08-21 1999-07-28 Sugen, Inc. Crystal structures of a protein tyrosine kinase
ATE308520T1 (de) 1996-08-23 2005-11-15 Sugen Inc Kombinatorische bibliotheken von indolinone und verwandte produkte und verfahren zur behandlung von krankheiten
WO1998024432A2 (en) 1996-12-05 1998-06-11 Sugen, Inc. Use of indolinone compounds as modulators of protein kinases
WO1998038984A2 (en) * 1997-03-05 1998-09-11 Sugen, Inc. Formulations for hydrophobic pharmaceutical agents
WO1998045708A1 (en) 1997-04-08 1998-10-15 Sugen, Inc. Study and treatment of diseases related to specific cellular functions of receptor protein tyrosine kinases
WO1998050356A1 (en) * 1997-05-07 1998-11-12 Sugen, Inc. 2-indolinone derivatives as modulators of protein kinase activity
WO1998056376A1 (en) 1997-06-13 1998-12-17 Sugen, Inc. Novel heteroaryl compounds for the modulation of protein tyrosine enzyme related cellular signal transduction
GB9716557D0 (en) 1997-08-06 1997-10-08 Glaxo Group Ltd Benzylidene-1,3-dihydro-indol-2-one derivatives having anti-cancer activity
AU3363599A (en) 1998-03-26 1999-10-18 Max-Planck Institut Fur Biochemie Heterocyclic families of compounds for the modulation of tyrosine protein kinase
EP1082305A4 (en) * 1998-05-29 2001-09-26 Sugen Inc PYRROL SUBSTITUTED 2-INDOLINONE EFFECTIVE AS A PROTEIN KINASE INHIBITOR

Also Published As

Publication number Publication date
US6395734B1 (en) 2002-05-28
CO5031249A1 (es) 2001-04-27
BR9910792A (pt) 2002-01-29
CA2314156C (en) 2010-05-25
EP1082305A1 (en) 2001-03-14
US20030105151A1 (en) 2003-06-05
SK18062000A3 (sk) 2001-06-11
NO20005916D0 (no) 2000-11-22
IL139934A (en) 2007-10-31
AU759226B2 (en) 2003-04-10
AU4410299A (en) 1999-12-13
NZ508815A (en) 2005-02-25
KR20010083039A (ko) 2001-08-31
PT2020408E (pt) 2013-09-13
TR200003514T2 (tr) 2002-05-21
NO318083B1 (no) 2005-01-31
US7119090B2 (en) 2006-10-10
EP2020408B1 (en) 2013-06-26
CN1250526C (zh) 2006-04-12
HK1126770A1 (en) 2009-09-11
EA200001258A1 (ru) 2001-08-27
IL139934A0 (en) 2002-02-10
JP2002516310A (ja) 2002-06-04
HUP0103617A2 (hu) 2002-02-28
EP1082305A4 (en) 2001-09-26
NO20005916L (no) 2001-01-29
SK287132B6 (sk) 2009-12-07
CN1311775A (zh) 2001-09-05
JP4528440B2 (ja) 2010-08-18
ES2429573T3 (es) 2013-11-15
TWI229073B (en) 2005-03-11
KR100743287B1 (ko) 2007-07-26
WO1999061422A1 (en) 1999-12-02
PL344477A1 (en) 2001-11-05
DK2020408T3 (da) 2013-09-30
CA2314156A1 (en) 1999-12-02
EA005032B1 (ru) 2004-10-28
EP2020408A1 (en) 2009-02-04

Similar Documents

Publication Publication Date Title
AR018408A1 (es) Compuesto pirrol sustituido 2-indolinona, composicion farmaceutica que lo comprende, uso de dicho compuesto en un metodo ''in vivo'' y su uso para lapreparacion de dicha composicion
CO5040216A1 (es) Agonistas de adenosina a 1, proceso para su preparacion y composiciones farmaceuticas que los contienen
EA200201179A1 (ru) Производные 2-аминокарбонил-9h-пурина
EA200101107A1 (ru) Пуриновые производные
EA200101177A1 (ru) Производные индола в качестве антагонистов прогестерона
TR200003256T2 (tr) P-38 mapkinaz engelleyicileri olan pirazol türevleri
NO20060154L (no) Imidazolyl-derivater
BR0112456A (pt) Compostos de piperidina para uso como inibidores de ccr-3
EA200201291A1 (ru) Производные пурина
DK0594702T3 (da) Substituerede indoler som midler mod AIDS
DE69942753D1 (de) Peptidantagonist von Zonulin und dessen Verwendung
EA200200360A1 (ru) Производные пурина
EA199800374A1 (ru) Ингибитор протеинкиназы с
EA200200770A1 (ru) Производные пурина
IS4863A (is) Staðgengnar bensensúlfonamíðafleiður sem forlyf fyrir COX-2 tálma
AR028164A1 (es) Componentes de formula mejaradores de estabilidad, composiciones y metodo de lavado que los emplea.
BR0017013A (pt) Composições de antibiótico azalìdeo
ATE249827T1 (de) Zusammensetzungen enhaltende 5-hydroxyindol als modulator eines nikotinischen rezeptors
AR010001A1 (es) Composiciones detergentes
IT8967757A0 (it) Uso di derivati di indolo per la tintura di sostanze cheratiniche composizioni tintorie nuovi compo sti e procedimento di tintura
EA200200417A1 (ru) Фармацевтически активные производные сульфонамида
GT200200069A (es) Derivados de mercaptoacetilamida, procedimiento para su preparacion y su uso
DK1254134T3 (da) Derivater af 1,3-dihydro-2H-indol-2-on og deres anvendelse som ligander for argininvasopressinreceptorerne V1B eller V1B og V1A
EA200001193A1 (ru) 2-фенил-1-[4-(2-аминоэтокси)бензил]индол в комбинации с эстрогенами
EA200300593A1 (ru) Соединения пиперазинилпиразинов в качестве агонистов или антагонистов серотонин 5-ht2 рецептора

Legal Events

Date Code Title Description
FG Grant, registration