[go: up one dir, main page]

AR057109A1 - Benzimidazoles sustituidos y metodos para usarlos como inhibidores de las quinasas asociadas con la tumorigenesis - Google Patents

Benzimidazoles sustituidos y metodos para usarlos como inhibidores de las quinasas asociadas con la tumorigenesis

Info

Publication number
AR057109A1
AR057109A1 ARP060103801A ARP060103801A AR057109A1 AR 057109 A1 AR057109 A1 AR 057109A1 AR P060103801 A ARP060103801 A AR P060103801A AR P060103801 A ARP060103801 A AR P060103801A AR 057109 A1 AR057109 A1 AR 057109A1
Authority
AR
Argentina
Prior art keywords
alkyl
halo
alkoxy
independently selected
hydroxy
Prior art date
Application number
ARP060103801A
Other languages
English (en)
Inventor
Mina E Aikawa
P Amiri
Jeffrey H Dove
Barry H Levine
Christopher Mcbride
Teresa Pick
Daniel J Poon
Savithri Ramurthy
Paul A Renhowe
Original Assignee
Novartis Ag
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 Novartis Ag filed Critical Novartis Ag
Publication of AR057109A1 publication Critical patent/AR057109A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • 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
    • 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
    • C07D403/14Heterocyclic 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
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

En algunas realizaciones, los compuestos y composiciones son eficaces para inhibir la actividad de al menos una serina/treonina quinasa o tirosina quinasa de receptores. Los compuestos y composiciones se pueden usar solos o en combinacion con al menos un agente adicional para el tratamiento de un trastorno mediado por una serina/treonina quinasa -o tirosina quinasa de receptores- tal como el cáncer. Reivindicacion 1: Un compuesto caracterizado porque responde un la formula (1), en donde, cada R1 se selecciona en forma independiente entre hidroxi, halo, alquilo C1-6, alcoxi C1-6, (alquil C1-6)sulfanilo, (alquil C1-6)sulfonilo, cicloalquilo, heterocicloalquilo, fenilo, y heteroarilo; R2 es alquilo C1-6 o halo(alquilo C1-6); cada R3 se selecciona en forma independiente entre halo, alquilo C1-6, y alcoxi C1-6; cada R4 se selecciona en forma independiente entre hidroxi, alquilo C1-6, alcoxi C1-6, halo, carboxilo, (alcoxi C1-6)carbonilo, aminocarbonilo, alquilaminocarbonilo C1-6, carbonitrilo, cicloalquilo, heterocicloalquilo, heterocicloalquilcarbonilo, fenilo, y heteroarilo; en donde R1, R2, R3, y R4 pueden estar opcionalmente sustituidos con uno o más sustituyentes seleccionados en forma independiente entre hidroxi, halo, alquilo C1-6, halo(alquil C1-6), alcoxi C1-6, y halo(alcoxi C1-6); un es 1, 2, 3, 4, o 5; b es 0, 1, 2, o 3; y c es 1 o 2; o un tautomero, estereoisomero, polimorfo, éster, metabolito, o prodroga del mismo o una sal aceptable para uso farmacéutico del compuesto, tautomero, estereoisomero, polimorfo, éster, metabolito, o prodroga.
ARP060103801A 2005-08-30 2006-08-30 Benzimidazoles sustituidos y metodos para usarlos como inhibidores de las quinasas asociadas con la tumorigenesis AR057109A1 (es)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US71253905P 2005-08-30 2005-08-30
US71310805P 2005-08-30 2005-08-30
US73159105P 2005-10-27 2005-10-27
US77468406P 2006-02-17 2006-02-17

Publications (1)

Publication Number Publication Date
AR057109A1 true AR057109A1 (es) 2007-11-14

Family

ID=37434025

Family Applications (2)

Application Number Title Priority Date Filing Date
ARP060103802A AR055622A1 (es) 2005-08-30 2006-08-30 Metodos de preparacion de benzimidazoles sustituidos y compuestos derivados de los mismos.
ARP060103801A AR057109A1 (es) 2005-08-30 2006-08-30 Benzimidazoles sustituidos y metodos para usarlos como inhibidores de las quinasas asociadas con la tumorigenesis

Family Applications Before (1)

Application Number Title Priority Date Filing Date
ARP060103802A AR055622A1 (es) 2005-08-30 2006-08-30 Metodos de preparacion de benzimidazoles sustituidos y compuestos derivados de los mismos.

Country Status (36)

Country Link
US (6) US7482367B2 (es)
EP (2) EP1924577B1 (es)
JP (4) JP5210867B2 (es)
KR (2) KR20080039965A (es)
AR (2) AR055622A1 (es)
AT (2) ATE526325T1 (es)
AU (2) AU2006287688B2 (es)
BR (2) BRPI0615314A2 (es)
CA (2) CA2619966A1 (es)
CR (1) CR9716A (es)
CU (1) CU23784B7 (es)
CY (2) CY1111871T1 (es)
DE (1) DE602006021036D1 (es)
DK (2) DK1924577T3 (es)
EA (1) EA014230B1 (es)
EC (2) ECSP088210A (es)
ES (1) ES2374451T3 (es)
GE (1) GEP20105004B (es)
GT (1) GT200600394A (es)
HN (1) HN2008000317A (es)
HR (2) HRP20110312T1 (es)
IL (2) IL189080A (es)
MA (2) MA29915B1 (es)
MY (2) MY163886A (es)
NI (1) NI200800060A (es)
NO (1) NO20081476L (es)
NZ (2) NZ565450A (es)
PE (2) PE20070427A1 (es)
PL (2) PL1926722T3 (es)
PT (2) PT1924577E (es)
RS (1) RS52099B (es)
SI (2) SI1924577T1 (es)
SM (1) SMAP200800022A (es)
TN (2) TNSN08088A1 (es)
TW (2) TWI387592B (es)
WO (2) WO2007027950A1 (es)

Families Citing this family (69)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PE20070427A1 (es) * 2005-08-30 2007-04-21 Novartis Ag Compuestos derivados de benzimidazoles sustituidos como inhibidores de tirosina quinasas
GB0609378D0 (en) * 2006-05-11 2006-06-21 Novartis Ag Organic compounds
DK2046292T3 (da) * 2006-07-21 2010-06-07 Novartis Ag Formuleringer for benzimidazolylpyridylethere
PE20080766A1 (es) * 2006-08-30 2008-06-15 Novartis Ag Sales de benzimidazolil piridil eteres y formulaciones que las contienen
RU2009114745A (ru) * 2006-09-19 2010-10-27 Новартис АГ (CH) Биомаркеры, предназначенные для выявления направленной модуляции, эффективности ингибиторов raf, применения с целью диагностики и/или прогнозирования
WO2008140850A1 (en) * 2007-03-02 2008-11-20 Novartis Ag Solid forms of a raf kinase inhibitor
WO2008147782A1 (en) * 2007-05-23 2008-12-04 Novartis Ag Raf inhibitors for the treatment of thyroid cancer
AR066845A1 (es) 2007-06-05 2009-09-16 Takeda Pharmaceutical Derivados de triazolopiridina e imidazopiridina una composicion farmaceutica que los comprende y su uso en la preparacion de un medicamento para el tratamiento del cancer
EP2181987B9 (en) 2007-08-23 2014-09-03 Takeda Pharmaceutical Company Limited 2-Carbonylaminobenzothiazoles and their use for the prophylaxis and treatment of cancer
EP2184285B1 (en) * 2007-08-29 2015-11-04 Takeda Pharmaceutical Company Limited Heterocyclic compound and use thereof
AU2009257487B2 (en) * 2008-06-13 2013-01-31 Novartis Ag Substituted benzimidazoles for neurofibromatosis
KR20110028651A (ko) * 2008-07-11 2011-03-21 노파르티스 아게 (a) 포스포이노시타이드 3-키나제 억제제 및 (b) ras/raf/mek 경로의 조절제의 조합물
CA2741300A1 (en) * 2008-10-29 2010-05-06 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
WO2010064611A1 (ja) 2008-12-01 2010-06-10 武田薬品工業株式会社 複素環化合物およびその用途
JO3101B1 (ar) 2008-12-02 2017-09-20 Takeda Pharmaceuticals Co مشتقات بنزوثيازول كعوامل مضادة للسرطان
JP2011020936A (ja) * 2009-07-14 2011-02-03 Lotte Co Ltd 口臭除去剤
JO3002B1 (ar) 2009-08-28 2016-09-05 Irm Llc مركبات و تركيبات كمثبطات كيناز بروتين
WO2011044072A1 (en) 2009-10-05 2011-04-14 Novartis Ag Combination of raf-265 and an activator of ampk for use in the treatment of a proliferative disease
WO2012068468A1 (en) * 2010-11-19 2012-05-24 Glaxosmithkline Llc Method of treatment with braf inhibitor
CA2828946C (en) 2011-04-18 2016-06-21 Eisai R&D Management Co., Ltd. Therapeutic agent for tumor
WO2012145503A1 (en) 2011-04-21 2012-10-26 Novartis Ag Pharmaceutical combinations
WO2013066483A1 (en) 2011-08-31 2013-05-10 Novartis Ag Synergistic combinations of pi3k- and mek-inhibitors
JP6073910B2 (ja) * 2011-11-09 2017-02-01 キャンサー・リサーチ・テクノロジー・リミテッド 5−(ピリジン−2−イル−アミノ)−ピラジン−2−カルボニトリル化合物及びその治療使用
WO2013070996A1 (en) 2011-11-11 2013-05-16 Novartis Ag Method of treating a proliferative disease
EP2782557B1 (en) 2011-11-23 2018-09-12 Array Biopharma, Inc. Pharmaceutical formulations
RU2659786C2 (ru) 2012-05-15 2018-07-04 Кансер Ресёрч Текнолоджи Лимитед 5-[[4-[[морфолин-2-ил]метиламино]-5-(трифторметил)-2-пиридил]амино]пиразин-2-карбонитрил, его терапевтические применения
UA115151C2 (uk) 2012-11-08 2017-09-25 Новартіс Аг Фармацевтична комбінація, що містить інгібітор b-raf та інгібітор деацетилази гістонів, та її застосування при лікуванні проліферативних захворювань
PT2976106T (pt) 2013-03-21 2021-05-26 Array Biopharma Inc Terapia de combinação que compreende um inibidor de b-raf e um segundo inibidor
EP3046557A1 (en) 2013-09-20 2016-07-27 Stichting Het Nederlands Kanker Instituut Rock in combination with mapk-pathway
WO2015041534A1 (en) 2013-09-20 2015-03-26 Stichting Het Nederlands Kanker Instituut P90rsk in combination with raf/erk/mek
JOP20200094A1 (ar) 2014-01-24 2017-06-16 Dana Farber Cancer Inst Inc جزيئات جسم مضاد لـ pd-1 واستخداماتها
JOP20200096A1 (ar) 2014-01-31 2017-06-16 Children’S Medical Center Corp جزيئات جسم مضاد لـ tim-3 واستخداماتها
ME03558B (me) 2014-03-14 2020-07-20 Novartis Ag Molekuli anti-lag-3 antiтela i njihove upotrebe
US20170027940A1 (en) 2014-04-10 2017-02-02 Stichting Het Nederlands Kanker Instituut Method for treating cancer
WO2015178770A1 (en) 2014-05-19 2015-11-26 Stichting Het Nederlands Kanker Instituut Compositions for cancer treatment
US20170114323A1 (en) 2014-06-19 2017-04-27 Whitehead Institute For Biomedical Research Uses of kinase inhibitors for inducing and maintaining pluripotency
MA41044A (fr) 2014-10-08 2017-08-15 Novartis Ag Compositions et procédés d'utilisation pour une réponse immunitaire accrue et traitement contre le cancer
MX389663B (es) 2014-10-14 2025-03-20 Novartis Ag Moleculas de anticuerpo que se unen a pd-l1 y usos de las mismas.
WO2016100882A1 (en) 2014-12-19 2016-06-23 Novartis Ag Combination therapies
US10449211B2 (en) 2015-03-10 2019-10-22 Aduro Biotech, Inc. Compositions and methods for activating “stimulator of interferon gene”—dependent signalling
US9890187B2 (en) 2015-06-26 2018-02-13 Epos-Iasis Research And Development, Ltd. Prototype systems of theranostic biomarkers for in vivo molecular management of cancer
DK3316857T3 (da) 2015-06-30 2021-10-18 Sequessome Tech Holdings Limited Multifasiske sammensætninger
EP3878465A1 (en) 2015-07-29 2021-09-15 Novartis AG Combination therapies comprising antibody molecules to tim-3
US20180222982A1 (en) 2015-07-29 2018-08-09 Novartis Ag Combination therapies comprising antibody molecules to pd-1
DK3317301T3 (da) 2015-07-29 2021-06-28 Immutep Sas Kombinationsterapier omfattende antistofmolekyler mod lag-3
SI3370768T1 (sl) 2015-11-03 2022-04-29 Janssen Biotech, Inc. Protitelesa, ki se specifično vežejo na PD-1, in njihove uporabe
CN105481944B (zh) * 2015-12-10 2019-01-08 华南农业大学 一种苯并咪唑衍生物二肽铜配合物及其制备方法和应用
EP3389712B1 (en) 2015-12-17 2024-04-10 Novartis AG Antibody molecules to pd-1 and uses thereof
US11098077B2 (en) 2016-07-05 2021-08-24 Chinook Therapeutics, Inc. Locked nucleic acid cyclic dinucleotide compounds and uses thereof
US11471538B2 (en) 2017-02-10 2022-10-18 INSERM (Institut National de la Santéet de la Recherche Medicale) Methods and pharmaceutical compositions for the treatment of cancers associated with activation of the MAPK pathway
WO2018168899A1 (ja) * 2017-03-15 2018-09-20 大日本住友製薬株式会社 ベンズイミダゾール誘導体の製造方法
HUE068023T2 (hu) 2017-04-18 2024-12-28 Lilly Co Eli Fenil-2-hidroxi-acetilamino-2-metil-fenil vegyületek
UY37695A (es) 2017-04-28 2018-11-30 Novartis Ag Compuesto dinucleótido cíclico bis 2’-5’-rr-(3’f-a)(3’f-a) y usos del mismo
EP3641812A1 (en) 2017-06-22 2020-04-29 Novartis AG Antibody molecules to cd73 and uses thereof
WO2018237173A1 (en) 2017-06-22 2018-12-27 Novartis Ag Antibody molecules to cd73 and uses thereof
EP3732285A1 (en) 2017-12-28 2020-11-04 Tract Pharmaceuticals, Inc. Stem cell culture systems for columnar epithelial stem cells, and uses related thereto
US12398209B2 (en) 2018-01-22 2025-08-26 Janssen Biotech, Inc. Methods of treating cancers with antagonistic anti-PD-1 antibodies
TWI869346B (zh) 2018-05-30 2025-01-11 瑞士商諾華公司 Entpd2抗體、組合療法、及使用該等抗體和組合療法之方法
US20210214459A1 (en) 2018-05-31 2021-07-15 Novartis Ag Antibody molecules to cd73 and uses thereof
WO2020097396A1 (en) * 2018-11-07 2020-05-14 Dana-Farber Cancer Institute, Inc. Benzimidazole derivatives and aza-benzimidazole derivatives as janus kinase 2 inhibitors and uses thereof
WO2020097398A1 (en) 2018-11-07 2020-05-14 Dana-Farber Cancer Institute, Inc. Benzothiazole derivatives and 7-aza-benzothiazole derivatives as janus kinase 2 inhibitors and uses thereof
JP7680955B2 (ja) 2019-01-11 2025-05-21 ネイジス ファーマシューティカルズ インコーポレイテッド ロイコトリエン合成阻害剤
AU2020340427A1 (en) 2019-08-29 2022-03-31 Hibercell, Inc. PERK inhibiting compounds
US20220348651A1 (en) 2019-09-18 2022-11-03 Novartis Ag Entpd2 antibodies, combination therapies, and methods of using the antibodies and combination therapies
CA3181537A1 (en) 2020-05-06 2021-11-11 Ajax Therapeutics, Inc. 6-heteroaryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors
WO2022140527A1 (en) 2020-12-23 2022-06-30 Ajax Therapeutics, Inc. 6-heteroaryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors
US12371667B2 (en) 2021-05-13 2025-07-29 Washington University Enhanced methods for inducing and maintaining naive human pluripotent stem cells
TW202325289A (zh) 2021-11-09 2023-07-01 美商雅捷可斯治療公司 Jak2抑制劑之形式及組合物
CA3234638A1 (en) 2021-11-09 2023-05-19 Ajax Therapeutics, Inc. 6-heteroaryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors

Family Cites Families (212)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3894037A (en) 1971-05-24 1975-07-08 Ciba Geigy Corp Certain isothiocyanobenzimidazoles
CH634306A5 (de) 1977-04-12 1983-01-31 Ciba Geigy Ag Benzimidazolderivate, verfahren zu ihrer herstellung und anthelmintische mittel enthaltend diese verbindungen als wirkstoffe.
US4319039A (en) 1979-06-15 1982-03-09 Merck & Co., Inc. Preparation of ammonium salt of hypocholesteremic fermentation product
US4294926A (en) 1979-06-15 1981-10-13 Merck & Co., Inc. Hypocholesteremic fermentation products and process of preparation
US4231938A (en) 1979-06-15 1980-11-04 Merck & Co., Inc. Hypocholesteremic fermentation products and process of preparation
US4444784A (en) 1980-08-05 1984-04-24 Merck & Co., Inc. Antihypercholesterolemic compounds
DK149080C (da) 1980-06-06 1986-07-28 Sankyo Co Fremgangsmaade til fremstilling af derivater af ml-236b-carboxylsyre
JPS5889191A (ja) 1981-11-20 1983-05-27 Sankyo Co Ltd 3−ヒドロキシ−ml−236b誘導体の製造法
US4430502A (en) 1982-08-13 1984-02-07 The Upjohn Company Pyridinyl substituted benzimidazoles and quinoxalines
US5354772A (en) 1982-11-22 1994-10-11 Sandoz Pharm. Corp. Indole analogs of mevalonolactone and derivatives thereof
WO1984002131A1 (fr) 1982-11-22 1984-06-07 Sandoz Ag Produits analogues de mevalolactone et leurs derives, leurs procedes de production, compositions pharmaceutiques les contenant ainsi que leur utilisation en tant que produits pharmaceutiques
US4911165A (en) 1983-01-12 1990-03-27 Ethicon, Inc. Pliabilized polypropylene surgical filaments
GB8307865D0 (en) 1983-03-22 1983-04-27 Fujisawa Pharmaceutical Co Benzimidazole derivatives
US4681893A (en) 1986-05-30 1987-07-21 Warner-Lambert Company Trans-6-[2-(3- or 4-carboxamido-substituted pyrrol-1-yl)alkyl]-4-hydroxypyran-2-one inhibitors of cholesterol synthesis
US4782084A (en) 1987-06-29 1988-11-01 Merck & Co., Inc. HMG-COA reductase inhibitors
US4885314A (en) 1987-06-29 1989-12-05 Merck & Co., Inc. Novel HMG-CoA reductase inhibitors
US4820850A (en) 1987-07-10 1989-04-11 Merck & Co., Inc. Process for α-C-alkylation of the 8-acyl group on mevinolin and analogs thereof
US5030447A (en) 1988-03-31 1991-07-09 E. R. Squibb & Sons, Inc. Pharmaceutical compositions having good stability
US5180589A (en) 1988-03-31 1993-01-19 E. R. Squibb & Sons, Inc. Pravastatin pharmaceuatical compositions having good stability
US4916239A (en) 1988-07-19 1990-04-10 Merck & Co., Inc. Process for the lactonization of mevinic acids and analogs thereof
US5290946A (en) 1988-10-13 1994-03-01 Sandoz Ltd. Processes for the synthesis of 3-(substituted indolyl-2-yl)propenaldehydes
US5118853A (en) 1988-10-13 1992-06-02 Sandoz Ltd. Processes for the synthesis of 3-disubstituted aminoacroleins
US4929437A (en) 1989-02-02 1990-05-29 Merck & Co., Inc. Coenzyme Q10 with HMG-CoA reductase inhibitors
US5189164A (en) 1989-05-22 1993-02-23 Sandoz Ltd. Processes for the synthesis of syn-(E)-3,5-dihydroxy-7-substituted hept-6-enoic and heptanoic acids and derivatives and intermediates thereof
FI94339C (fi) 1989-07-21 1995-08-25 Warner Lambert Co Menetelmä farmaseuttisesti käyttökelpoisen /R-(R*,R*)/-2-(4-fluorifenyyli)- , -dihydroksi-5-(1-metyylietyyli)-3-fenyyli-4-/(fenyyliamino)karbonyyli/-1H-pyrroli-1-heptaanihapon ja sen farmaseuttisesti hyväksyttävien suolojen valmistamiseksi
PH27357A (en) 1989-09-22 1993-06-21 Fujisawa Pharmaceutical Co Pyrazole derivatives and pharmaceutical compositions comprising the same
JPH06759B2 (ja) 1989-09-22 1994-01-05 ファイザー製薬株式会社 新規なベンゾイミダゾール化合物
US5420245A (en) 1990-04-18 1995-05-30 Board Of Regents, The University Of Texas Tetrapeptide-based inhibitors of farnesyl transferase
US5041453A (en) 1990-05-30 1991-08-20 Rhone-Poulenc Rorer Pharmaceuticals Inc. Quinolinyl-benzoheterobicyclic derivatives as antagonists of leukotriene D4
FR2677020B1 (fr) 1991-05-31 1993-08-27 Cird Galderma Composes derives de benzimidazole, leur procede de preparation et leur utilisation dans les domaines therapeutique et cosmetique.
HU9203780D0 (en) 1991-12-12 1993-03-29 Sandoz Ag Stabilized pharmaceutical products of hmg-coa reductase inhibitor and method for producing them
US5612360A (en) 1992-06-03 1997-03-18 Eli Lilly And Company Angiotensin II antagonists
US5604260A (en) 1992-12-11 1997-02-18 Merck Frosst Canada Inc. 5-methanesulfonamido-1-indanones as an inhibitor of cyclooxygenase-2
CA2111902A1 (en) 1992-12-21 1994-06-22 Jack Beuford Campbell Antitumor compositions and methods of treatment
CA2152792C (en) 1993-01-15 2000-02-15 Stephen R. Bertenshaw Novel 3,4-diaryl thiophenes and analogs thereof having use as antiinflammatory agents
WO1994019357A1 (en) 1993-02-23 1994-09-01 Merrell Dow Pharmaceuticals Inc. Farnesyl:protein transferase inhibitors as anticancer agents
US5298627A (en) 1993-03-03 1994-03-29 Warner-Lambert Company Process for trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-one inhibitors of cholesterol synthesis
US5409944A (en) 1993-03-12 1995-04-25 Merck Frosst Canada, Inc. Alkanesulfonamido-1-indanone derivatives as inhibitors of cyclooxygenase
CA2118985A1 (en) 1993-04-02 1994-10-03 Dinesh V. Patel Heterocyclic inhibitors of farnesyl protein transferase
WO1994026723A2 (en) 1993-05-14 1994-11-24 Genentech, Inc. ras FARNESYL TRANSFERASE INHIBITORS
US5602098A (en) 1993-05-18 1997-02-11 University Of Pittsburgh Inhibition of farnesyltransferase
US5380738A (en) 1993-05-21 1995-01-10 Monsanto Company 2-substituted oxazoles further substituted by 4-fluorophenyl and 4-methylsulfonylphenyl as antiinflammatory agents
GB9602877D0 (en) 1996-02-13 1996-04-10 Merck Frosst Canada Inc 3,4-Diaryl-2-hydroxy-2,5- dihydrofurans as prodrugs to cox-2 inhibitors
US5436265A (en) 1993-11-12 1995-07-25 Merck Frosst Canada, Inc. 1-aroyl-3-indolyl alkanoic acids and derivatives thereof useful as anti-inflammatory agents
US5474995A (en) 1993-06-24 1995-12-12 Merck Frosst Canada, Inc. Phenyl heterocycles as cox-2 inhibitors
US5852046A (en) 1993-08-03 1998-12-22 Hoechst Aktiengesellschaft Benzo-fused heterocyclic compounds having a 5-membered ring processes for their preparation their use as medicaments their use as diagnostic agents and medicaments containing them
EP0639573A1 (de) 1993-08-03 1995-02-22 Hoechst Aktiengesellschaft Benzokondensierte 5-Ringheterocyclen, Verfahren zu ihrer Herstellung, ihre Verwendung als Medikament, ihre Verwendung als Diagnostikum, sowie sie enthaltendes Medikament
WO1995008542A1 (en) 1993-09-22 1995-03-30 Kyowa Hakko Kogyo Co., Ltd. Farnesyltransferase inhibitor
IL111235A (en) 1993-10-15 2001-03-19 Schering Plough Corp Medicinal preparations for inhibiting protein G activity and for the treatment of malignant diseases, containing tricyclic compounds, some such new compounds and a process for the preparation of some of them
US5661152A (en) 1993-10-15 1997-08-26 Schering Corporation Tricyclic sulfonamide compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
ATE210652T1 (de) 1993-10-15 2001-12-15 Schering Corp Tricyclische carbamat-derivate zur inhibierung der g-protein funktion und für die behandlung von proliferativen erkrankungen
US5719148A (en) 1993-10-15 1998-02-17 Schering Corporation Tricyclic amide and urea compounds useful for inhibition of g-protein function and for treatment of proliferative diseases
ES2164717T3 (es) 1993-10-15 2002-03-01 Schering Corp Compuestos triciclicos de sulfonamida utiles para inhibir la funcion de la proteina-g y para el tratamiento de enfermedades proliferativas.
US5721236A (en) 1993-10-15 1998-02-24 Schering Corporation Tricyclic carbamate compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
KR100378615B1 (ko) 1993-10-25 2003-10-10 파크데이비스앤드캄파니 단백질:파르네실트랜스퍼라제의치환된테트라및펜타펩티드억제제
US5344991A (en) 1993-10-29 1994-09-06 G.D. Searle & Co. 1,2 diarylcyclopentenyl compounds for the treatment of inflammation
US5783593A (en) 1993-11-04 1998-07-21 Abbott Laboratories Inhibitors of squalene synthetase and protein farnesyltransferase
WO1995012572A1 (en) 1993-11-04 1995-05-11 Abbott Laboratories Cyclobutane derivatives as inhibitors of squalene synthetase and protein farnesyltransferase
KR100362338B1 (ko) 1993-11-05 2003-04-08 워너-램버트 캄파니 단백질:파르네실트랜스퍼라아제의치환디-및트리펩티드억제제
US5466823A (en) 1993-11-30 1995-11-14 G.D. Searle & Co. Substituted pyrazolyl benzenesulfonamides
US5484799A (en) 1993-12-09 1996-01-16 Abbott Laboratories Antifungal dorrigocin derivatives
US5393790A (en) 1994-02-10 1995-02-28 G.D. Searle & Co. Substituted spiro compounds for the treatment of inflammation
FI963597L (fi) 1994-03-15 1996-11-14 Eisai Co Ltd Isoprenyylitransferaasi-inhibiittoreita
HUT72440A (en) 1994-03-31 1996-04-29 Bristol Myers Squibb Co Imidazole-containing inhibitors of farnesyl protein transferase and pharmaceutical compositions containing them
US5523430A (en) 1994-04-14 1996-06-04 Bristol-Myers Squibb Company Protein farnesyl transferase inhibitors
US5510510A (en) 1994-05-10 1996-04-23 Bristol-Meyers Squibb Company Inhibitors of farnesyl protein transferase
US5563255A (en) 1994-05-31 1996-10-08 Isis Pharmaceuticals, Inc. Antisense oligonucleotide modulation of raf gene expression
US6391636B1 (en) 1994-05-31 2002-05-21 Isis Pharmaceuticals, Inc. Antisense oligonucleotide modulation of raf gene expression
US6358932B1 (en) 1994-05-31 2002-03-19 Isis Pharmaceticals, Inc. Antisense oligonucleotide inhibition of raf gene expression
CN1150419A (zh) 1994-06-10 1997-05-21 罗纳-布朗克罗莱尔股份有限公司 新的法呢基转移酶抑制剂、其制法及其药物组合物
US5571792A (en) 1994-06-30 1996-11-05 Warner-Lambert Company Histidine and homohistidine derivatives as inhibitors of protein farnesyltransferase
WO1996005529A1 (en) 1994-08-09 1996-02-22 Micron Optics, Inc. Temperature compensated fiber fabry-perot filters
CA2155448A1 (en) 1994-08-11 1996-02-12 Katerina Leftheris Inhibitors of farnesyl protein transferase
WO1996005168A1 (en) 1994-08-11 1996-02-22 Banyu Pharmaceutical Co., Ltd. Substituted amide derivative
WO1996005169A1 (en) 1994-08-12 1996-02-22 Banyu Pharmaceutical Co., Ltd. N,n-disubstituted amic acid derivative
DE4429506B4 (de) 1994-08-19 2007-09-13 Degussa Gmbh Verfahren zur Extraktion natürlicher Carotinoid-Farbstoffe
DE4429653C2 (de) 1994-08-20 1997-04-03 Anton Dr More Konverter und Verfahren zum Frischen von Metallschmelzen insbesondere von Roheisen zu Stahl
EP0701907A1 (en) 1994-09-13 1996-03-20 Agfa-Gevaert N.V. A dye donor element for use in a thermal dye transfer process
US6037136A (en) 1994-10-24 2000-03-14 Cold Spring Harbor Laboratory Interactions between RaF proto-oncogenes and CDC25 phosphatases, and uses related thereto
WO1996016443A1 (en) 1994-11-22 1996-05-30 Philips Electronics N.V. Semiconductor device with a carrier body on which a substrate with a semiconductor element is fastened by means of a glue layer and on which a pattern of conductor tracks is fastened
CA2204144A1 (en) 1994-12-09 1996-06-13 Francis J. Tinney Substituted tetra- and pentapeptide inhibitors of protein:farnesyl transferase
WO1996021701A2 (en) 1995-01-09 1996-07-18 Magla International Ltd. Wear resistant image printing on latex surfaces
AU4915796A (en) 1995-01-12 1996-07-31 University Of Pittsburgh Inhibitors of prenyl transferases
US5741789A (en) 1995-01-17 1998-04-21 Eli Lilly And Company Compounds having effects on serotonin-related systems
FR2729390A1 (fr) 1995-01-18 1996-07-19 Rhone Poulenc Rorer Sa Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent
FR2730492B1 (fr) 1995-02-09 1997-03-14 Rhone Poulenc Rorer Sa Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent
FR2730491B1 (fr) 1995-02-09 1997-03-14 Rhone Poulenc Rorer Sa Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent
US5633272A (en) 1995-02-13 1997-05-27 Talley; John J. Substituted isoxazoles for the treatment of inflammation
US5684013A (en) 1995-03-24 1997-11-04 Schering Corporation Tricyclic compounds useful for inhibition of g-protein function and for treatment of proliferative diseases
US5700806A (en) 1995-03-24 1997-12-23 Schering Corporation Tricyclic amide and urea compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
IL117580A0 (en) 1995-03-29 1996-07-23 Merck & Co Inc Inhibitors of farnesyl-protein transferase and pharmaceutical compositions containing them
IL117798A (en) 1995-04-07 2001-11-25 Schering Plough Corp Tricyclic compounds useful for inhibiting the function of protein - G and for the treatment of malignant diseases, and pharmaceutical preparations containing them
US5891872A (en) 1995-04-07 1999-04-06 Schering Corporation Tricyclic compounds
CA2217351C (en) 1995-04-07 2003-03-18 Schering Corporation Carbonyl-piperazinyl and piperidinyl compounds which inhibit farnesyl protein transferase
US5712280A (en) 1995-04-07 1998-01-27 Schering Corporation Tricyclic compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
US5831115A (en) 1995-04-21 1998-11-03 Abbott Laboratories Inhibitors of squalene synthase and protein farnesyltransferase
IL118101A0 (en) 1995-05-03 1996-09-12 Abbott Lab Inhibitors of farnesyltransferase
WO1997000252A1 (en) 1995-06-16 1997-01-03 Warner-Lambert Company Tricyclic inhibitors of protein farnesyltransferase
FR2736641B1 (fr) 1995-07-10 1997-08-22 Rhone Poulenc Rorer Sa Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent
AT402617B (de) 1995-07-11 1997-07-25 Datacon Schweitzer & Zeindl Gm Anlage zum automatisierten, hermetischen anlage zum automatisierten, hermetischen verschliessen von gehäusen verschliessen von gehäusen
FR2736638B1 (fr) 1995-07-12 1997-08-22 Rhone Poulenc Rorer Sa Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent
GB9514265D0 (en) 1995-07-13 1995-09-13 Wellcome Found Hetrocyclic compounds
CH690163A5 (fr) 1995-07-28 2000-05-31 Symphar Sa Dérivés gem-diphosphonates substitués utiles en tant qu'agents anti-cancers.
US6001866A (en) 1995-10-05 1999-12-14 Warner-Lambert Company Method for treating and preventing inflammation and atherosclerosis
WO1997012613A1 (en) 1995-10-05 1997-04-10 Warner-Lambert Company Method for treating and preventing inflammation and atherosclerosis
US5717100A (en) 1995-10-06 1998-02-10 Merck & Co., Inc. Substituted imidazoles having anti-cancer and cytokine inhibitory activity
US6020343A (en) 1995-10-13 2000-02-01 Merck Frosst Canada, Inc. (Methylsulfonyl)phenyl-2-(5H)-furanones as COX-2 inhibitors
CA2235986C (en) 1995-11-06 2006-09-12 University Of Pittsburgh Inhibitors of protein isoprenyl transferases
US6288237B1 (en) 1995-11-17 2001-09-11 Gesellschaft Fur Biotechnologische Forschung Mbh (Gbf) Epothilons C and D, preparation and compositions
EP0862435A4 (en) 1995-11-22 1999-02-03 Merck & Co Inc Inhibitors of farnesyl-protein transferase
EE03484B1 (et) 1995-12-08 2001-08-15 Janssen Pharmaceutica N.V. Farnesüülproteiintransferaasi inhibeerivad (5-imidasolüül)metüül-2-kinolinooni derivaadid ja nende kasutamine
EP1380581A1 (en) 1995-12-22 2004-01-14 Schering Corporation Tricyclic amides useful for inhibition of G-protein function and for treatment of proliferative diseases
EA002357B1 (ru) 1995-12-28 2002-04-25 Фудзисава Фармасьютикал Ко., Лтд. Производные бензимидазола
WO1997026246A1 (en) 1996-01-16 1997-07-24 Warner-Lambert Company Substituted histidine inhibitors of protein farnesyltransferase
GB9602029D0 (en) 1996-02-01 1996-04-03 Fujisawa Pharmaceutical Co New heterocyclic compounds
US6673927B2 (en) 1996-02-16 2004-01-06 Societe De Conseils De Recherches Et D'applications Scientifiques, S.A.S. Farnesyl transferase inhibitors
CA2249601A1 (en) 1996-04-03 1997-10-23 Thorsten E. Fisher Inhibitors of farnesyl-protein transferase
BR9708574A (pt) 1996-04-12 1999-08-03 Searle & Co Derivados benzeno sulfonamida substituídos como pródrogas de inibidores cox-2
EP0938494A1 (en) 1996-05-22 1999-09-01 Warner-Lambert Company Inhibitors of protein farnesyl transferase
CA2256109A1 (en) 1996-05-23 1997-11-27 Applied Research Systems Ars Holding N.V. Compounds that inhibit the binding of raf-1 or 14-3-3 proteins to the beta chain of il-2 receptor, and pharmaceutical compositions containing same
HRP970371A2 (en) 1996-07-13 1998-08-31 Kathryn Jane Smith Heterocyclic compounds
EP0918771A4 (en) 1996-07-15 2001-02-07 Bristol Myers Squibb Co THIADIOXOBENZODIAZEPINES FOR USE AS FARNESYL PROTEIN TRANSFERASE INHIBITORS
US5861419A (en) 1996-07-18 1999-01-19 Merck Frosst Canad, Inc. Substituted pyridines as selective cyclooxygenase-2 inhibitors
FR2751649B1 (fr) 1996-07-26 1998-08-28 Adir Nouveaux derives de benzimidazole, de benzoxazole et de benzothiazole, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
US6242469B1 (en) 1996-12-03 2001-06-05 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto, analogues and uses thereof
CA2276150A1 (en) 1996-12-30 1998-07-09 Steven D. Young Inhibitors of farnesyl-protein transferase
JP2002511054A (ja) 1996-12-30 2002-04-09 メルク エンド カンパニー インコーポレーテッド ファルネシル蛋白トランスフェラーゼ阻害薬
US6127380A (en) 1997-02-18 2000-10-03 American Home Products Corporation 4-aminoalkoxy-1H-benzoimidazoles
US5932600A (en) 1997-03-14 1999-08-03 Vertex Pharmaceuticals Incorporated Inhibitors of IMPDH enzyme
ATE244717T1 (de) 1997-03-14 2003-07-15 Vertex Pharma Inhibitoren des impdh-enzyms
AR012634A1 (es) 1997-05-02 2000-11-08 Sugen Inc Compuesto basado en quinazolina, composicion famaceutica que lo comprende, metodo para sintetizarlo, su uso, metodos de modulacion de la funcion deserina/treonina proteinaquinasa con dicho compuesto y metodo in vitro para identificar compuestos que modulan dicha funcion
US6187799B1 (en) 1997-05-23 2001-02-13 Onyx Pharmaceuticals Inhibition of raf kinase activity using aryl ureas
CA2294898A1 (en) 1997-07-03 1999-01-14 Neurogen Corporation Certain diarylimidazole derivatives; a new class of npy specific ligands
SI9700186B (sl) 1997-07-14 2006-10-31 Lek, Tovarna Farmacevtskih In Kemicnih Izdelkov, D.D. Nova farmacevtska oblika z nadzorovanim sproscanjem zdravilnih ucinkovin
FR2766822B1 (fr) 1997-07-30 2001-02-23 Adir Nouveaux derives de benzimidazole, de benzoxazole et de benzothiazole, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
GB9716557D0 (en) 1997-08-06 1997-10-08 Glaxo Group Ltd Benzylidene-1,3-dihydro-indol-2-one derivatives having anti-cancer activity
US6022884A (en) 1997-11-07 2000-02-08 Amgen Inc. Substituted pyridine compounds and methods of use
US6204467B1 (en) 1998-03-24 2001-03-20 Ford Global Technologies, Inc. Method and apparatus for resistive welding
KR20010025087A (ko) 1998-05-22 2001-03-26 스튜어트 알. 수터 신규한 2-알킬 치환된 이미다졸 화합물
US6420555B1 (en) 1998-06-16 2002-07-16 Societe De Conseils De Recherches Et D'applications Scientifiques, S.A.S. Imidazolyl derivatives
FR2780973B1 (fr) 1998-07-09 2001-10-05 Hoechst Marion Roussel Inc Procede de preparation du 4-(3-pyridinyl)-1h-imidazole, et les intermediaires mis en oeuvre
DE19834751A1 (de) 1998-08-01 2000-02-03 Boehringer Ingelheim Pharma Disubstituierte bicyclische Heterocyclen, ihre Herstellung und ihre Verwendung als Arzneimittel
HUP0104171A3 (en) 1998-11-17 2002-04-29 Ihara Chemical Ind Co Pyrimidinylbenzimidazole and triatinylbenzimidazole derivatives, intermediates and use as agricultura/horticultural fungicides
US6211177B1 (en) 1998-11-24 2001-04-03 Cell Pathways, Inc. Method for treating neoplasia by exposure to substituted 2-aryl-benzimidazole derivatives
US6339083B1 (en) 1998-12-14 2002-01-15 Bayer Aktiengesellschaft Multiheterocyclic pharmAceuticals
US7351834B1 (en) 1999-01-13 2008-04-01 Bayer Pharmaceuticals Corporation ω-Carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
CA2361553A1 (en) 1999-01-29 2000-08-03 Zhenping Zhu Antibodies specific to kdr and uses thereof
GB9904387D0 (en) 1999-02-25 1999-04-21 Pharmacia & Upjohn Spa Antitumour synergistic composition
AU4972900A (en) 1999-04-08 2000-11-14 Arch Development Corporation Use of anti-vegf antibody to enhance radiation in cancer therapy
NZ514602A (en) 1999-04-12 2003-06-30 Aventis Pharma Ltd Substituted bicyclic heteroaryl compounds as integrin antagonists
EP1196167B1 (en) 1999-07-02 2006-04-19 Stuart A. Lipton Use of p38 MAPK inhibitors in the treatment of ophthalmic conditions
US6545004B1 (en) 1999-10-27 2003-04-08 Cytokinetics, Inc. Methods and compositions utilizing quinazolinones
EP1686120A3 (en) 1999-10-27 2007-05-30 Cytokinetics, Inc. Methods and compositions utilizing quinazolinones
JP2003525936A (ja) 2000-03-06 2003-09-02 スミスクライン ビーチャム パブリック リミテッド カンパニー Rafキナーゼ阻害物質としてのイミダゾール誘導体
US6548517B2 (en) 2000-03-24 2003-04-15 Millennium Pharmaceuticals, Inc. Oxindole inhibitors of factor Xa
US6469026B2 (en) 2000-03-24 2002-10-22 Millennium Pharmaceuticals, Inc. Isoquinolone inhibitors of factor Xa
JP2001322903A (ja) 2000-05-15 2001-11-20 Kumiai Chem Ind Co Ltd 農園芸用殺菌剤組成物
AU7804501A (en) * 2000-07-27 2002-02-13 Pharmacia Corp Epoxy-steroidal aldosterone antagonist and calcium channel blocker combination therapy for treatment of congestive heart failure
WO2002018654A1 (en) 2000-08-30 2002-03-07 The Board Of Trustees Of The University Of Arkansas Induction of ldl receptor expression by extracellular-signal regulated kinase, erk-1/2
JP4734705B2 (ja) 2000-10-31 2011-07-27 三菱化学株式会社 リチウム二次電池用正極材料、リチウム二次電池用正極及びリチウム二次電池
DE10060292A1 (de) 2000-12-05 2002-06-20 Aventis Pharma Gmbh Verwendung substituierter Benzimidazole zur Herstellung eines Medikaments zur Behandlung von Krankheiten, welche durch Inhibierung des Na+/H+-Austauschers beeinflusst werden können und sie enthaltendes Medikament
DE60139964D1 (de) 2000-12-15 2009-10-29 Vertex Pharma Bakterielle Gyrase-Hemmer sowie deren Verwendung
TW593278B (en) 2001-01-23 2004-06-21 Wyeth Corp 1-aryl-or 1-alkylsulfonylbenzazole derivatives as 5-hydroxytryptamine-6 ligands
IL157031A0 (en) 2001-02-08 2004-02-08 Karobio Ab Thyroid receptor ligands
US20050038022A1 (en) 2001-03-26 2005-02-17 Unisearch Limited Method for treatment of cancer and compositions for use therein
ATE400274T1 (de) 2001-04-10 2008-07-15 Merck & Co Inc Hemmstoffe der akt aktivität
WO2002083064A2 (en) 2001-04-10 2002-10-24 Merck & Co., Inc. A method of treating cancer
WO2002083139A1 (en) 2001-04-10 2002-10-24 Merck & Co., Inc. Inhibitors of akt activity
WO2002083140A1 (en) 2001-04-10 2002-10-24 Merck & Co., Inc. Inhibitors of akt activity
NZ529043A (en) 2001-04-16 2006-11-30 Tanabe Seiyaku Co Large conductance calcium-activated K channel opener
US6855714B2 (en) 2001-07-06 2005-02-15 Schering Aktiengesellschaft 1-alkyl-2-aryl-benzimidazole derivatives, their use for the production of pharmaceutical agents as well as pharmaceutical preparations that contain these derivatives
WO2003013526A1 (en) 2001-08-08 2003-02-20 Merck & Co. Inc. Anticoagulant compounds
AU2002341715A1 (en) 2001-09-17 2003-04-01 Bristol-Myers Squibb Company Cyclic hydroxamic acids as inhibitors of matrix metalloproteinases and/or tnf-alpha converting enzyme (tace)
ATE511840T1 (de) 2001-10-09 2011-06-15 Amgen Inc Imidazolderivate als entzündungshemmende mittel
US7039413B2 (en) * 2001-10-24 2006-05-02 Ntt Docomo, Inc. Mobile station transfer control system, cell transfer control method, mobile station, cell transfer control method at mobile station, cell transfer control program, control apparatus, and allocating method of communication resources
US7060705B2 (en) 2001-11-07 2006-06-13 Merck & Co., Inc. Mitotic kinesin inhibitors
TW200300140A (en) 2001-11-14 2003-05-16 Novartis Ag Organic compounds
TW200303742A (en) 2001-11-21 2003-09-16 Novartis Ag Organic compounds
UA83620C2 (ru) 2001-12-05 2008-08-11 Уайт Замещенные бензоксазолы и их аналоги как эстрогенные агенты
CA2467916A1 (en) 2001-12-06 2003-06-19 Merck & Co., Inc. Mitotic kinesin inhibitors
US7378411B2 (en) 2001-12-06 2008-05-27 Merck & Co., Inc. Substituted thienopyrimidinones as a mitotic kinesin inhibitor
EP1481077B1 (en) 2001-12-06 2009-11-04 Merck & Co., Inc. Mitotic kinesin inhibitors
US7244723B2 (en) 2001-12-06 2007-07-17 Merck & Co., Inc. Substituted furopyrimidinones as a mitotic kinesin inhibitors
JP4391825B2 (ja) 2001-12-06 2009-12-24 メルク エンド カムパニー インコーポレーテッド 有糸分裂キネシン阻害剤
JP4136395B2 (ja) 2002-02-22 2008-08-20 クミアイ化学工業株式会社 農園芸用殺菌剤組成物
CA2478068C (en) 2002-03-08 2011-02-08 Merck & Co., Inc. Dihydropyrazole compounds useful for treating or preventing cancer
US8299108B2 (en) 2002-03-29 2012-10-30 Novartis Ag Substituted benzazoles and methods of their use as inhibitors of raf kinase
JP4628678B2 (ja) * 2002-03-29 2011-02-09 ノバルティス バクシンズ アンド ダイアグノスティックス,インコーポレーテッド 置換ベンズアゾールおよびRafキナーゼ阻害剤としてのそれらの使用
AU2003231359B2 (en) 2002-04-16 2009-04-30 Teijin Limited Piperidine derivatives having CCR3 antagonism
US7524841B2 (en) 2002-04-25 2009-04-28 Teijin Limited 4,4-disubstituted piperidine derivatives having CCR3 antagonism
AU2003231799A1 (en) 2002-05-23 2003-12-12 Merck & Co., Inc. Mitotic kinesin inhibitors
CA2485343A1 (en) 2002-05-23 2004-05-13 Merck & Co., Inc. Mitotic kinesin inhibitors
JP4377323B2 (ja) 2002-06-14 2009-12-02 メルク エンド カムパニー インコーポレーテッド 有糸分裂キネシン阻害剤
JP4463679B2 (ja) 2002-06-14 2010-05-19 メルク エンド カムパニー インコーポレーテッド 有糸分裂キネシン阻害剤
TW200400816A (en) * 2002-06-26 2004-01-16 Lilly Co Eli Tricyclic steroid hormone nuclear receptor modulators
CN1894241A (zh) 2002-08-09 2007-01-10 阿斯利康(瑞典)有限公司 作为代谢型谷氨酸受体-5调节剂的“1,2,4” 噁二唑
WO2004026859A1 (en) 2002-09-18 2004-04-01 Pfizer Products Inc. Novel imidazole compounds as transforming growth factor (tgf) inhibitors
AU2003271548A1 (en) 2002-10-13 2004-05-04 Neurosearch A/S Use of skca channel blocking drugs for combating parkinson's disease
US7122665B2 (en) 2002-10-15 2006-10-17 Synta Pharmaceuticals Corp. Heterocyclic compounds
US20050054705A1 (en) 2003-02-04 2005-03-10 Aventis Pharma Deutschland Gmbh N-substituted (benzoimidazol-2-yl) phenylamines, process for their preparation, their use as medicament or diagnostic aid, and medicament comprising them
US7531553B2 (en) 2003-03-21 2009-05-12 Amgen Inc. Heterocyclic compounds and methods of use
US7893096B2 (en) 2003-03-28 2011-02-22 Novartis Vaccines And Diagnostics, Inc. Use of small molecule compounds for immunopotentiation
US7652061B2 (en) 2003-05-20 2010-01-26 Novartis A.G. N-acyl nitrogen heterocycles as ligands of peroxisome proliferator-activated receptors
TW200510394A (en) 2003-05-29 2005-03-16 Synta Pharmaceuticals Corp Heterocyclic compounds for preventing and treating disorders associated with excessive bone loss
US7538135B2 (en) 2003-07-08 2009-05-26 Novartis Ag Benzenesulfonylamino compounds and pharmaceutical compositions containing these compounds
JP2007502298A (ja) 2003-08-14 2007-02-08 スミスクライン ビーチャム コーポレーション 化合物
WO2005030140A2 (en) 2003-09-26 2005-04-07 Exelixis, Inc. C-met modulators and methods of use
CA2542653A1 (en) 2003-10-16 2005-04-28 Chiron Corporation Substituted benzazoles and use thereof as inhibitors of raf kinase
US7470712B2 (en) 2004-01-21 2008-12-30 Bristol-Myers Squibb Company Amino-benzazoles as P2Y1 receptor inhibitors
JP2007518823A (ja) 2004-01-23 2007-07-12 アムゲン インコーポレイテッド キノリン、キナゾリン、ピリジン、及びピリミジン化合物と炎症、血管新生、及び癌に対する治療におけるそれら化合物の用途
PE20070427A1 (es) * 2005-08-30 2007-04-21 Novartis Ag Compuestos derivados de benzimidazoles sustituidos como inhibidores de tirosina quinasas
DK2046292T3 (da) * 2006-07-21 2010-06-07 Novartis Ag Formuleringer for benzimidazolylpyridylethere

Also Published As

Publication number Publication date
JP2013060458A (ja) 2013-04-04
HK1117523A1 (en) 2009-01-16
PL1924577T3 (pl) 2011-09-30
US20080287682A1 (en) 2008-11-20
HK1117519A1 (en) 2009-01-16
AU2006284666A1 (en) 2007-03-08
NZ565450A (en) 2011-04-29
AR055622A1 (es) 2007-08-29
US7732465B2 (en) 2010-06-08
TW200804345A (en) 2008-01-16
KR20080039964A (ko) 2008-05-07
TWI387592B (zh) 2013-03-01
DE602006021036D1 (de) 2011-05-12
US20090170904A1 (en) 2009-07-02
PE20070427A1 (es) 2007-04-21
BRPI0615314A2 (pt) 2011-05-17
AU2006284666B2 (en) 2011-04-28
DK1926722T3 (da) 2011-12-19
JP2009507794A (ja) 2009-02-26
JP5210867B2 (ja) 2013-06-12
SMP200800022B (it) 2008-04-02
MA29915B1 (fr) 2008-11-03
CA2619966A1 (en) 2007-03-08
EP1926722A1 (en) 2008-06-04
US20100234394A1 (en) 2010-09-16
DK1924577T3 (da) 2011-05-16
US20070161680A1 (en) 2007-07-12
IL189080A (en) 2013-05-30
GEP20105004B (en) 2010-06-10
MY163886A (en) 2017-11-15
EP1926722B1 (en) 2011-09-28
JP5210866B2 (ja) 2013-06-12
CU23784B7 (es) 2012-02-15
MY148694A (en) 2013-05-31
SI1926722T1 (sl) 2012-01-31
ECSP088210A (es) 2008-03-26
NI200800060A (es) 2009-03-03
PT1926722E (pt) 2012-01-11
PL1926722T3 (pl) 2012-02-29
US20070049622A1 (en) 2007-03-01
EP1924577A1 (en) 2008-05-28
US8592459B2 (en) 2013-11-26
EP1924577B1 (en) 2011-03-30
IL189194A (en) 2013-09-30
PT1924577E (pt) 2011-07-04
KR20080039965A (ko) 2008-05-07
CA2620472C (en) 2013-12-24
CY1112157T1 (el) 2015-12-09
US20100256375A1 (en) 2010-10-07
BRPI0615309B1 (pt) 2021-07-27
ES2374451T3 (es) 2012-02-16
RS52099B (sr) 2012-06-30
WO2007030377A1 (en) 2007-03-15
AU2006287688A1 (en) 2007-03-15
JP2013060457A (ja) 2013-04-04
GT200600394A (es) 2008-03-17
IL189080A0 (en) 2008-08-07
SI1924577T1 (sl) 2011-07-29
TNSN08088A1 (en) 2009-07-14
ECSP088218A (es) 2008-03-26
US7767820B2 (en) 2010-08-03
CY1111871T1 (el) 2015-11-04
ATE526325T1 (de) 2011-10-15
NZ565451A (en) 2011-05-27
HRP20110939T1 (hr) 2012-01-31
US7482367B2 (en) 2009-01-27
BRPI0615309A2 (pt) 2011-05-17
PE20070335A1 (es) 2007-04-21
EA200800441A1 (ru) 2008-08-29
HN2008000317A (es) 2011-02-16
AU2006287688B2 (en) 2010-08-19
TNSN08089A1 (en) 2009-07-14
CR9716A (es) 2008-04-16
ATE503751T1 (de) 2011-04-15
CU20080027A7 (es) 2010-12-08
EA014230B1 (ru) 2010-10-29
IL189194A0 (en) 2008-06-05
CA2620472A1 (en) 2007-03-15
MA29772B1 (fr) 2008-09-01
HRP20110312T1 (hr) 2011-08-31
WO2007027950A1 (en) 2007-03-08
SMAP200800022A (it) 2008-04-02
NO20081476L (no) 2008-03-26
JP2009507026A (ja) 2009-02-19
TW200804346A (en) 2008-01-16

Similar Documents

Publication Publication Date Title
AR057109A1 (es) Benzimidazoles sustituidos y metodos para usarlos como inhibidores de las quinasas asociadas con la tumorigenesis
AR073369A1 (es) Derivados de 2-carboxamida-cicloamino-urea como inhibidores de pi-3
PE20141167A1 (es) Piridopirazinas sustituidas como inhibidores novedosos de ptk
PE20191755A1 (es) Derivados de pirazol como inhibidores de malt 1
BRPI0612072A2 (pt) inibidores da aspartil protease
PE20140192A1 (es) Derivados de bencimidazol como inhibidores de cinasa pi3
PE20110062A1 (es) N-(3-(3,5-dimetoxifenetil)-1h-pirazol-5-il)-4-(3,4-dimetilpiperazin-1-il)benzamida y sales del mismo
AR072952A1 (es) Compuestos de 2-imino-3-metilpirrolopirimidinona fenilo-sustituida como inhibidores de bace-1, composiciones y su uso
AR047076A1 (es) Compuestos de pirrolotriazina como inhibidores de tirosina quinasas, composiciones farmaceuticas
AR070828A1 (es) Derivados de azetidina y ciclobutano como inhibidores de jak
AR053569A1 (es) Derivados de pirazol
AR081058A1 (es) Derivados de arilmetoxi isoindolina, composiciones que los comprenden y su uso en el tratamiento del cancer.
AR083542A1 (es) Piperidin-4-il-azetidin diamidas como inhibidores de monoacilglicerol lipasa
AR092269A1 (es) Sulfamoilarilamidas y su uso como medicamentos para el tratamiento de la hepatitis b
AR059249A1 (es) Compuesto amina trisustituido
PE20141075A1 (es) 4-aril-n-fenil-1,3,5-triazin-2-aminas que contienen un grupo sulfoximina
ECSP12011645A (es) Compuestos y métodos inhibidores de jak de pirazolopirimidina
PE20121509A1 (es) Compuestos de triazolopiridinas como inhibidores de quinasa mps-1
ES2587304T3 (es) Derivados de diaminopirimidina y procedimientos para la preparación de los mismos
PE20081530A1 (es) Nuevos compuestos 617
NZ607794A (en) N-acylsulfonamide apoptosis promoters
CR9214A (es) 2-fenilindoles como antagonistas del receptor de la prostaglandina d2
PE20070832A1 (es) Derivados de piridazinona como inhibidores de la tirosina quinasa
AR058569A1 (es) Inhibidores de histona desacetilasa para mejorar la actividad de agentes antifungicos
IN2014DN07283A (es)

Legal Events

Date Code Title Description
FB Suspension of granting procedure