[go: up one dir, main page]

EA199700280A1 - Ингибиторы протеинкиназы с - Google Patents

Ингибиторы протеинкиназы с

Info

Publication number
EA199700280A1
EA199700280A1 EA199700280A EA199700280A EA199700280A1 EA 199700280 A1 EA199700280 A1 EA 199700280A1 EA 199700280 A EA199700280 A EA 199700280A EA 199700280 A EA199700280 A EA 199700280A EA 199700280 A1 EA199700280 A1 EA 199700280A1
Authority
EA
Eurasian Patent Office
Prior art keywords
proteinkinase
inhibitors
provides
indol
maleimide
Prior art date
Application number
EA199700280A
Other languages
English (en)
Other versions
EA000598B1 (ru
Inventor
Уильям Ф. мл. Хит
Майкл Р. Джироусек
Джон Х. МакДональд III
Кристофер Дж. Рито
Original Assignee
Эли Лилли Энд Компани
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 Эли Лилли Энд Компани filed Critical Эли Лилли Энд Компани
Publication of EA199700280A1 publication Critical patent/EA199700280A1/ru
Publication of EA000598B1 publication Critical patent/EA000598B1/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
    • C07D487/22Heterocyclic 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 four or more hetero rings
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • 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
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/08Vasodilators for multiple indications
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C43/00Ethers; Compounds having groups, groups or groups
    • C07C43/02Ethers
    • C07C43/03Ethers having all ether-oxygen atoms bound to acyclic carbon atoms
    • C07C43/14Unsaturated ethers
    • C07C43/17Unsaturated ethers containing halogen
    • C07C43/174Unsaturated ethers containing halogen containing six-membered aromatic rings
    • C07C43/1745Unsaturated ethers containing halogen containing six-membered aromatic rings having more than one ether bound
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C43/00Ethers; Compounds having groups, groups or groups
    • C07C43/02Ethers
    • C07C43/03Ethers having all ether-oxygen atoms bound to acyclic carbon atoms
    • C07C43/14Unsaturated ethers
    • C07C43/178Unsaturated ethers containing hydroxy or O-metal groups
    • C07C43/1785Unsaturated ethers containing hydroxy or O-metal groups having more than one ether bound
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/22Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains four or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02Silicon compounds
    • C07F7/08Compounds having one or more C—Si linkages
    • C07F7/18Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804Compounds having Si-O-C linkages

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Emergency Medicine (AREA)
  • Obesity (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Данное изобретение обеспечивает новые макроциклические производные бис-индолмалеимида формулы (I). Кроме того, данное изобретение обеспечивает получение этих соединений, фармацевтические препараты и способы применения их для ингибирования протеинкиназы C в млекопитающих.Международная заявка была опубликована вместе с отчетом о международном поиске.
EA199700280A 1995-03-30 1996-03-28 Ингибиторы протеинкиназы c EA000598B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US08/413,735 US5624949A (en) 1993-12-07 1995-03-30 Protein kinase C inhibitors
PCT/US1996/004245 WO1996030048A1 (en) 1995-03-30 1996-03-28 Protein kinase c inhibitors

Publications (2)

Publication Number Publication Date
EA199700280A1 true EA199700280A1 (ru) 1998-02-26
EA000598B1 EA000598B1 (ru) 1999-12-29

Family

ID=23638401

Family Applications (1)

Application Number Title Priority Date Filing Date
EA199700280A EA000598B1 (ru) 1995-03-30 1996-03-28 Ингибиторы протеинкиназы c

Country Status (16)

Country Link
US (10) US5624949A (ru)
EP (1) EP0735038A1 (ru)
JP (1) JPH11507327A (ru)
KR (1) KR100319945B1 (ru)
CN (1) CN1093767C (ru)
AU (1) AU701988B2 (ru)
CA (1) CA2216535C (ru)
CZ (1) CZ286301B6 (ru)
EA (1) EA000598B1 (ru)
HU (1) HUP9801250A3 (ru)
MX (1) MX9707431A (ru)
NO (1) NO309271B1 (ru)
NZ (1) NZ305276A (ru)
PL (1) PL183600B1 (ru)
TR (1) TR199701073T1 (ru)
WO (1) WO1996030048A1 (ru)

Families Citing this family (91)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5843935A (en) * 1993-12-07 1998-12-01 Eli Lilly And Company Protein kinase C inhibitors
US5723456A (en) * 1993-12-07 1998-03-03 Eli Lilly & Company Therapeutic treatment for cardiovascular diseases
HU219709B (hu) * 1993-12-07 2001-06-28 Eli Lilly And Co. Proteinkináz C gátló hatású kondenzált indolszármazékok, eljárás előállításukra, és az ezeket tartalmazó gyógyászati készítmények
TW371661B (en) * 1995-11-20 1999-10-11 Lilly Co Eli Novel intermediates and their use to prepare N,N'-bridged bisindolylmaleimides
RO120074B1 (ro) * 1995-11-20 2005-08-30 Eli Lilly And Company Sare a unui derivat macrociclic de bis-indolmaleinimidă, ca inhibitor al protein kinazei c
EA001779B1 (ru) * 1996-05-01 2001-08-27 Эли Лилли Энд Компани Способ лечения заболеваний, связанных с фактором роста сосудистого эндотелия
US6232299B1 (en) 1996-05-01 2001-05-15 Eli Lilly And Company Use of protein kinase C inhibitors to enhance the clinical efficacy of oncolytic agents and radiation therapy
UA54427C2 (ru) * 1996-05-01 2003-03-17 Елі Ліллі Енд Компані Способ лечения заболеваний глаз, связанных с фактором роста эндотелия сосудов
EA001450B1 (ru) * 1996-05-01 2001-04-23 Эли Лилли Энд Компани Галогензамещенные ингибиторы протеинкиназы с
US6093709A (en) * 1996-08-22 2000-07-25 Eli Lilly And Company Therapeutic treatment for sexual dysfunctions
YU9499A (sh) * 1996-08-23 2000-03-21 Eli Lilly And Company Sinteza bisindolilmalimida
US6107327A (en) * 1996-08-30 2000-08-22 Eli Lilly And Company Therapeutic treatment for HIV infection
US5962446A (en) * 1996-08-30 1999-10-05 Eli Lilly And Company Therapetutic treatment for human T cell lymphotrophic virus type 1 infection
US6040152A (en) * 1996-12-31 2000-03-21 National Jewish Medical And Research Center Method and assay for regulation of T cell proliferation
US6093740A (en) * 1997-04-30 2000-07-25 Eli Lilly And Company Therapeutic treatment for skin disorders
JPH1180026A (ja) * 1997-09-02 1999-03-23 Yoshitomi Pharmaceut Ind Ltd 新規免疫抑制剤、その使用方法およびその同定方法
JP2001523707A (ja) * 1997-11-26 2001-11-27 イーライ・リリー・アンド・カンパニー 慢性骨髄性白血病および急性リンパ性白血病のための治療的処置
CA2227688C (en) 1998-01-16 2007-07-31 James W. Critchfield Methods and compositions for inhibition of viral replication
US6225301B1 (en) * 1998-03-05 2001-05-01 Eli Lilly And Company Therapeutic treatment for renal dysfunction
US6103713A (en) * 1998-03-05 2000-08-15 Eli Lilly And Company Therapeutic treatment for autoimmune diseases
US6291446B1 (en) * 1998-03-05 2001-09-18 Eli Lilly And Company Therapeutic treatment for cytomegalovirus infection
US6103712A (en) * 1998-03-05 2000-08-15 Eli Lilly And Company Therapeutic treatment for asthma
ATE251624T1 (de) * 1998-03-13 2003-10-15 Univ British Columbia Granulatimide-derivate zur behandlung von krebs
CA2245029A1 (en) 1998-03-13 1999-09-13 University Of British Columbia Granulatimide compounds as g2 checkpoint inhibitors
US6127401A (en) 1998-06-05 2000-10-03 Cephalon, Inc. Bridged indenopyrrolocarbazoles
US6013646A (en) 1998-07-02 2000-01-11 Bayer Corporation Indolocarbazole derivatives useful for the treatment of neurodegenerative diseases and cancer
US6841567B1 (en) 1999-02-12 2005-01-11 Cephalon, Inc. Cyclic substituted fused pyrrolocarbazoles and isoindolones
US6284783B1 (en) 1999-06-09 2001-09-04 The Uab Research Foundation Use of bisindolylmaleimide compounds to induce Fas-mediated apoptosis
US6399780B1 (en) 1999-08-20 2002-06-04 Cephalon, Inc. Isomeric fused pyrrolocarbazoles and isoindolones
US6852688B2 (en) 2000-03-10 2005-02-08 University Of Florida Compositions for treating diabetic retinopathy and methods of using same
WO2001081375A2 (en) * 2000-04-24 2001-11-01 Yale University Dna & protein binding miniature proteins
US20020048581A1 (en) * 2000-07-18 2002-04-25 King George L. Modulation of nitric oxide synthase by PKC
US7425537B2 (en) 2000-08-22 2008-09-16 The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services SH2 domain binding inhibitors
DE60112611T2 (de) * 2000-12-08 2006-06-14 Ortho Mcneil Pharm Inc Makroheterocyclische verbindungen als kinase inhibitoren
AU2002230727A1 (en) * 2000-12-08 2002-06-18 Ortho-Mcneil Pharmaceutical, Inc. Indazolyl-substituted pyrroline compounds as kinase inhibitors
DE10109280A1 (de) * 2001-02-26 2002-09-05 Peter Mayser Indolderivate mit inhibitorischer Wirkung auf Proteinkinasen
US6559299B2 (en) * 2001-03-29 2003-05-06 Merck & Co., Inc. Preparation and isolation of indolocarbazole glycosides
GB0125658D0 (en) * 2001-10-25 2001-12-19 Ssl Int Plc Medicaments
GB0125659D0 (en) * 2001-10-25 2001-12-19 Ssl Int Plc Spermicides
ATE352312T1 (de) * 2001-12-29 2007-02-15 Novo Nordisk As Kombinierte verwendung einer glp-1-verbindung und eines aldose reduktase inhibitors
US20030232741A1 (en) * 2002-05-06 2003-12-18 Washington University Methods of treatment of glaucoma and other conditions mediated by NOS-2 expression via inhibition of the EGFR pathway
CA2488798A1 (en) * 2002-06-05 2003-12-18 Janssen Pharmaceutica N.V. Substituted pyrrolines as kinase inhibitors
KR20050008787A (ko) 2002-06-05 2005-01-21 얀센 파마슈티카 엔.브이. 키나제 저해제로서의 비스인돌릴-말레이미드 유도체
CA2393720C (en) * 2002-07-12 2010-09-14 Eli Lilly And Company Crystalline 2,5-dione-3-(1-methyl-1h-indol-3-yl)-4-[1-(pyridin-2-ylmethyl)piperidin-4-yl]-1h-indol-3-yl]-1h-pyrrole mono-hydrochloride
US20040175384A1 (en) * 2003-12-12 2004-09-09 Mohapatra Shyam S. Protein kinase C as a target for the treatment of respiratory syncytial virus
BRPI0411366A (pt) * 2003-06-13 2006-07-25 Janssen Pharmaceutica Nv derivados de indazolil (indolil) maleimida substituìdos como inibidores de cinase
DK1633774T3 (da) * 2003-06-18 2010-05-25 Tranzyme Pharma Inc Makrocykliske motilinreceptorantagonister
EP2322547A1 (en) 2003-06-25 2011-05-18 Crucell Holland B.V. Myeloid cell-specific lectin
GB0407315D0 (en) * 2003-07-15 2004-05-05 Cambridge Antibody Tech Human antibody molecules
WO2005012360A2 (en) * 2003-07-22 2005-02-10 Crucell Holland B.V. Binding molecules against sars-coronavirus and uses thereof
US7491794B2 (en) * 2003-10-14 2009-02-17 Intermune, Inc. Macrocyclic compounds as inhibitors of viral replication
US8592368B2 (en) 2003-12-19 2013-11-26 University Of South Florida JAK/STAT inhibitors and MAPK/ERK inhibitors for RSV infection
CA2601278C (en) * 2004-03-17 2014-06-10 Lars Michael Larsen Prevention of retinopathy by inhibition of the visual cycle
RS51847B (en) 2004-05-27 2012-02-29 Crucell Holland Bv. BINDING MOLECULES WHICH MAY NEUTRALIZE FRAGILE VIRUS AND USE
EP1765313A2 (en) 2004-06-24 2007-03-28 Novartis Vaccines and Diagnostics, Inc. Compounds for immunopotentiation
WO2006019851A1 (en) * 2004-07-23 2006-02-23 Eli Lilly And Company Methods for diagnosing and treating diabetic microvascular complications
JP4852046B2 (ja) 2004-10-12 2012-01-11 クルセル ホランド ベー ヴェー 癌の治療及び検出に用いる結合分子
SG159542A1 (en) 2004-11-11 2010-03-30 Crucell Holland Bv Compositions against sars-coronavirus and uses thereof
WO2006068988A1 (en) * 2004-12-20 2006-06-29 Eli Lilly And Company Combination therapy for vascular complications associated with hyperglycemia
US8158586B2 (en) * 2005-04-11 2012-04-17 Pharmagap Inc. Inhibitors of protein kinases and uses thereof
ATE507242T1 (de) 2005-05-12 2011-05-15 Crucell Holland Bv Wirtszellenspezifische bindungsmoleküle, die dazu in der lage sind, viren zu neutralisieren, und anwendungen davon
SG166791A1 (en) * 2005-07-25 2010-12-29 Intermune Inc Novel macrocyclic inhibitors of hepatitis c virus replication
US20070112053A1 (en) 2005-09-16 2007-05-17 Pickett Cecil B Pharmaceutical compositions and methods using temozolomide and a protein kinase inhibitor
EP1940411A4 (en) * 2005-09-29 2008-10-29 Janssen Pharmaceutica Nv MACROHETEROCYCLIC COMPOUNDS AS KINASE INHIBITORS
KR20080056295A (ko) 2005-10-11 2008-06-20 인터뮨, 인크. C형 간염 바이러스 복제를 억제하기 위한 화합물 및 방법
JP2009529575A (ja) * 2006-03-10 2009-08-20 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ キナーゼ阻害剤としてのピリジン−含有大複素環式化合物
CA2646316C (en) 2006-03-15 2016-05-24 Theralogics, Inc. Methods of treating muscular wasting diseases using nf-kb activation inhibitors
AU2007255388B2 (en) * 2006-06-06 2013-07-04 Crucell Holland B.V. Human binding molecules having killing activity against enterococci and staphylococcus aureus and uses thereof
KR101508390B1 (ko) * 2006-06-06 2015-04-08 크루셀 홀란드 비.브이. 포도상구균에 대한 사멸활성을 갖는 인간결합분자 및 그것의 용도
RU2008152171A (ru) * 2006-07-05 2010-08-10 Интермьюн, Инк. (Us) Новые ингибиторы вирусной репликации гепатита с
US8445437B2 (en) * 2006-07-27 2013-05-21 The Brigham And Women's Hospital, Inc. Treatment and prevention of cardiovascular disease using mast cell stabilizers
DK2059532T3 (da) 2006-09-07 2013-03-18 Crucell Holland Bv Humane bindingsmolekyler, der er i stand til at neutralisere influenzavirus H5N1, og anvendelser deraf
KR101485197B1 (ko) 2006-09-07 2015-01-23 크루셀 홀란드 비.브이. 인플루엔자 바이러스 h5n1을 중화시킬 수 있는 인간 결합분자 및 그것의 용도
MX2009011867A (es) * 2007-05-03 2010-03-22 Array Biopharma Inc Nuevos inhibidores macrociclicos de la replicacion del virus de hepatitis c.
BRPI0811447A2 (pt) * 2007-05-10 2014-10-29 Intermune Inc Compostos, composição farmacêutica e métodos de inibição da atividade da protease ns3/ns4, de tratamento da fibrose hepática e de intensificação da função hepática num indivíduo tendo infecção de vírus da hepatite c.
CN101808642B (zh) * 2007-09-28 2012-05-02 布里格海姆妇女医院公司 肥大细胞稳定剂治疗肥胖症
US20090130195A1 (en) 2007-10-17 2009-05-21 Mildred Acevedo-Duncan Prostate carcinogenesis predictor
US8419332B2 (en) * 2007-10-19 2013-04-16 Atlas Bolt & Screw Company Llc Non-dimpling fastener
BRPI0911260A2 (pt) * 2008-04-15 2015-09-29 Intermune Inc composto, composição farmacêutica, método de inibição de atividade da protease de ns3/ns4 in, vitro e usos de compostos
EP2181999A1 (en) 2008-11-03 2010-05-05 Zentiva, A.S. Method of manufacturing ruboxistarin
AR075584A1 (es) * 2009-02-27 2011-04-20 Intermune Inc COMPOSICIONES TERAPEUTICAS QUE COMPRENDEN beta-D-2'-DESOXI-2'-FLUORO-2'-C-METILCITIDINA Y UN DERIVADO DE ACIDO ISOINDOL CARBOXILICO Y SUS USOS. COMPUESTO.
CN105418757B (zh) 2009-05-11 2019-07-09 扬森疫苗与预防公司 能中和流感病毒h3n2的人结合分子及其应用
CN105001302A (zh) * 2009-09-28 2015-10-28 英特穆恩公司 C型肝炎病毒复制的环肽抑制剂
ES2385157B1 (es) * 2010-02-25 2013-07-08 Universidad Del País Vasco Compuestos para el tratamiento de alzheimer.
US8785648B1 (en) 2010-08-10 2014-07-22 The Regents Of The University Of California PKC-epsilon inhibitors
EP3180003B1 (en) 2014-07-01 2022-01-12 The Regents of the University of California Pkc-epsilon inhibitors
BR112019012383A2 (pt) 2016-12-19 2020-02-27 Chromaderm, Inc. Métodos de tratamento de distúrbios de hiperpigmentação
WO2019000224A1 (zh) * 2017-06-27 2019-01-03 中国海洋大学 双吲哚马来酰亚胺衍生物及其制备方法和用途
CA3071114A1 (en) 2017-07-28 2019-01-31 Applied Therapeutics Inc. Compositions and methods for treating galactosemia
JP2023524504A (ja) 2020-05-01 2023-06-12 アプライド セラピューティクス, インコーポレイテッド ソルビトールデヒドロゲナーゼ欠乏症を処置するためのアルドースレダクターゼ阻害剤
EP4525862A1 (en) 2022-05-20 2025-03-26 Dermbiont, Inc. Compositions and formulations for use of a pk inhibitor for the prevention, treatment, and improvement of skin diseases, conditions, and disorders

Family Cites Families (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4808613A (en) * 1986-11-21 1989-02-28 Bristol-Myers Company Rebeccamycin derivative containing pharmaceutical composition
US4785085A (en) * 1986-11-21 1988-11-15 Bristol-Myers Company Rebeccamycin analogs
DE3752123T2 (de) * 1987-03-09 1998-05-14 Kyowa Hakko Kogyo Kk Derivate des physiologisch aktiven mittels k-252
JPH07113027B2 (ja) * 1987-12-24 1995-12-06 協和醗酵工業株式会社 K−252誘導体
DE3803620A1 (de) * 1988-02-06 1989-08-17 Goedecke Ag Indolocarbazol-derivate, verfahren zu deren herstellung und diese enthaltende arzneimittel
US5438050A (en) * 1988-02-06 1995-08-01 Godecke Aktiengesellschaft Indolocarbazole derivatives, processes for their preparation and compositions containing them
NZ227850A (en) * 1988-02-10 1991-11-26 Hoffmann La Roche Indole substituted pyrrole derivatives; preparatory process and medicaments for use against inflammatory immunological, bronchopulmonary or vascular disorders
MC2096A1 (fr) * 1989-02-23 1991-02-15 Hoffmann La Roche Pyrroles substitues
DE3914764A1 (de) * 1989-05-05 1990-11-08 Goedecke Ag Maleinimid-derivate und deren verwendung als arzneimittel
IL94274A0 (en) * 1989-05-05 1991-03-10 Goedecke Ag Maleinimide derivatives,process for the preparation thereof and pharmaceutical compositions containing the same
US5380746A (en) * 1989-05-05 1995-01-10 Goedecke Aktiengesellschaft Bis-(1H-indol-3-YL)-maleinimide derivatives, processes for the preparation thereof and pharmaceutical compositions containing them
DE3924538A1 (de) * 1989-07-25 1991-01-31 Goedecke Ag Indolocarbazol und dessen verwendung
DE3942296A1 (de) * 1989-12-21 1991-06-27 Goedecke Ag Indolocarbazol-derivate, verfahren zu deren herstellung und deren verwendung
DE4005970A1 (de) * 1990-02-26 1991-08-29 Boehringer Mannheim Gmbh Neue trisubstituierte maleinimide, verfahren zu ihrer herstellung sowie arzneimittel, die diese verbindungen enthalten
DE4005969A1 (de) * 1990-02-26 1991-08-29 Boehringer Mannheim Gmbh Neue trisubstituierte pyrrole, verfahren zu ihrer herstellung sowie arzneimittel, die diese verbindungen enthalten
US5292747A (en) * 1990-08-07 1994-03-08 Hoffman-La Roche Inc. Substituted pyrroles
CA2046801C (en) * 1990-08-07 2002-02-26 Peter D. Davis Substituted pyrroles
FI934461L (fi) * 1991-04-11 1993-10-11 Schering Corp Antitumoer- och antipsoriasismedel
GB9123396D0 (en) * 1991-11-04 1991-12-18 Hoffmann La Roche A process for the manufacture of substituted maleimides
DE69326388T2 (de) * 1992-06-22 1999-12-30 Kyowa Hakko Kogyo Co., Ltd. Verfahren zur Herstellung von Staurosporin-Derivaten
US5461146A (en) * 1992-07-24 1995-10-24 Cephalon, Inc. Selected protein kinase inhibitors for the treatment of neurological disorders
WO1994007895A1 (en) * 1992-09-25 1994-04-14 Schering Corporation Diindolo compounds and pharmaceutical compositions containing them
DE4243321A1 (de) * 1992-12-21 1994-06-23 Goedecke Ag Aminosäurederivate von Heterocyclen als PKC-Inhibitoren
PH30300A (en) * 1993-05-07 1997-01-20 Ciba Geigy Ag Polycyclic compounds and processes for the preparation thereof
AU678435B2 (en) * 1993-05-10 1997-05-29 F. Hoffmann-La Roche Ag Substituted pyrroles
HU219709B (hu) * 1993-12-07 2001-06-28 Eli Lilly And Co. Proteinkináz C gátló hatású kondenzált indolszármazékok, eljárás előállításukra, és az ezeket tartalmazó gyógyászati készítmények
DE69418978T2 (de) * 1993-12-07 1999-10-28 Eli Lilly And Co., Indianapolis Synthese von Bisindolylmaleimiden
US5481003A (en) * 1994-06-22 1996-01-02 Eli Lilly And Company Protein kinase C inhibitors
RO120074B1 (ro) * 1995-11-20 2005-08-30 Eli Lilly And Company Sare a unui derivat macrociclic de bis-indolmaleinimidă, ca inhibitor al protein kinazei c

Also Published As

Publication number Publication date
HUP9801250A2 (hu) 1998-09-28
CA2216535A1 (en) 1996-10-03
CN1093767C (zh) 2002-11-06
PL183600B1 (pl) 2002-06-28
US5719175A (en) 1998-02-17
KR19980703380A (ko) 1998-10-15
EP0735038A1 (en) 1996-10-02
US5821365A (en) 1998-10-13
NZ305276A (en) 1999-02-25
CN1185742A (zh) 1998-06-24
EA000598B1 (ru) 1999-12-29
NO974453D0 (no) 1997-09-26
CA2216535C (en) 2002-05-07
JPH11507327A (ja) 1999-06-29
US5780461A (en) 1998-07-14
US6057440A (en) 2000-05-02
US5552396A (en) 1996-09-03
AU701988B2 (en) 1999-02-11
MX9707431A (es) 1997-12-31
KR100319945B1 (ko) 2002-03-08
PL322584A1 (en) 1998-02-02
NO309271B1 (no) 2001-01-08
US5674862A (en) 1997-10-07
TR199701073T1 (xx) 1998-02-21
NO974453L (no) 1997-11-19
AU5324996A (en) 1996-10-16
US5696108A (en) 1997-12-09
US5621098A (en) 1997-04-15
HUP9801250A3 (en) 1998-12-28
WO1996030048A1 (en) 1996-10-03
CZ286301B6 (cs) 2000-03-15
US5624949A (en) 1997-04-29
US5739322A (en) 1998-04-14
CZ305197A3 (cs) 1998-05-13

Similar Documents

Publication Publication Date Title
EA199700280A1 (ru) Ингибиторы протеинкиназы с
EA199800374A1 (ru) Ингибитор протеинкиназы с
DE69428025D1 (de) Proteinkinase C-Inhibitoren
EA200001176A1 (ru) Гетероциклические ингибиторы p38
EA200000047A1 (ru) НОВЫЕ МИМЕТИКИ ГУАНИДИНА В КАЧЕСТВЕ ИНГИБИТОРОВ ФАКТОРА Xa
EA200000920A1 (ru) Производные бициклических гидроксамовых кислот
EA199900620A1 (ru) Фталазиноны
EA200300248A1 (ru) Бициклопиразолы, активные в качестве ингибиторов киназы, способ их получения и включающие их фармацевтические композиции
DE69617273D1 (de) Heterocyclisch substituierte cyclopentanderivate.
EP0986382A4 (en) RAF KINASE HEMMER
EA199900494A1 (ru) Производные 2-(пурин-9-ил)-тетрагидрофуран-3,4-диола
EA199900021A1 (ru) Бициклические гетероароматические соединения в качестве ингибиторов протеинтирозинкиназы
EA200000098A1 (ru) 4-АМИНОПИРРОЛ(3,2-d)ПИРИМИДИНЫ В КАЧЕСТВЕ АНТАГОНИСТОВ РЕЦЕПТОРА НЕЙРОПЕПТИДА Y
DE69627179T2 (de) Substituierte 2-anilino-pyrimidines verwendbar als protein kinase inhibitoren
EA200100688A1 (ru) АЗОТСОДЕРЖАЩИЕ ГЕТЕРОБИЦИКЛЫ В КАЧЕСТВЕ ИНГИБИТОРОВ ФАКТОРА Xa
EA200200530A1 (ru) Гетероциклические замещенные пиразолоны
EA200000759A1 (ru) Производные 2-(пурин-9-ил)-тетрагидрофуран-3,4-диола
EA200201096A1 (ru) СОЕДИНЕНИЯ ПИРРОЛО[2,3-d]ПИРИМИДИНА В КАЧЕСТВЕ ИММУНОДЕПРЕССАНТОВ
EA200100589A1 (ru) Азабициклоалканы как модуляторы ccr5
EA199900083A1 (ru) Замещенные пиридо- или пиримидосодержащие 6,6 или 6,7-бициклические производные
EA199700087A1 (ru) Способ ингибирования катепсина к
EA199900421A1 (ru) Бензонафтиридины в качестве бронхиальных терапевтических средств
ATE214381T1 (de) Thiazole derivate als protein kinase c inhibitoren
EA199800773A1 (ru) Производные пирролопирролона в качестве ингибиторов нейтрофильной эластазы
EA199700160A1 (ru) Производные индола в качестве антагонистов eaa

Legal Events

Date Code Title Description
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