JP4958784B2 - ステアロイル−CoAデサチュラーゼ酵素によって媒介される疾患の処置のための複素環誘導体 - Google Patents

ステアロイル−CoAデサチュラーゼ酵素によって媒介される疾患の処置のための複素環誘導体 Download PDF

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Publication number
JP4958784B2
JP4958784B2 JP2007532631A JP2007532631A JP4958784B2 JP 4958784 B2 JP4958784 B2 JP 4958784B2 JP 2007532631 A JP2007532631 A JP 2007532631A JP 2007532631 A JP2007532631 A JP 2007532631A JP 4958784 B2 JP4958784 B2 JP 4958784B2
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piperazin
carboxylic acid
thiadiazole
trifluoromethyl
benzoyl
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Expired - Fee Related
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Japanese (ja)
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JP2008513499A (ja
JP2008513499A5 (enExample
Inventor
ラジェンダー カンボジ,
ザイホイ チャン,
チーアン−ミン フ,
ビシュヌマーシー コドゥムル,
シーフェン リュー,
シャオイー サン,
ナガスリー チャッカ,
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Xenon Pharmaceuticals Inc
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Xenon Pharmaceuticals Inc
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/22Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D277/28Radicals substituted by nitrogen atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/38Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381Heterocyclic compounds having sulfur as a ring hetero atom having five-membered 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/38Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D271/00Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/101,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles
    • C07D271/1131,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D285/00Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01Five-membered rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
JP2007532631A 2004-09-20 2005-09-20 ステアロイル−CoAデサチュラーゼ酵素によって媒介される疾患の処置のための複素環誘導体 Expired - Fee Related JP4958784B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US61135704P 2004-09-20 2004-09-20
US60/611,357 2004-09-20
PCT/US2005/033744 WO2006034315A2 (en) 2004-09-20 2005-09-20 Heterocyclic derivatives for the treatment of diseases mediated by stearoyl-coa desaturase enzymes

Publications (3)

Publication Number Publication Date
JP2008513499A JP2008513499A (ja) 2008-05-01
JP2008513499A5 JP2008513499A5 (enExample) 2008-10-16
JP4958784B2 true JP4958784B2 (ja) 2012-06-20

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ID=36090635

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JP2007532631A Expired - Fee Related JP4958784B2 (ja) 2004-09-20 2005-09-20 ステアロイル−CoAデサチュラーゼ酵素によって媒介される疾患の処置のための複素環誘導体

Country Status (11)

Country Link
US (1) US7919496B2 (enExample)
EP (2) EP1830837B1 (enExample)
JP (1) JP4958784B2 (enExample)
CN (1) CN101083982A (enExample)
AR (1) AR051026A1 (enExample)
AU (1) AU2005286793A1 (enExample)
BR (1) BRPI0515483A (enExample)
CA (1) CA2580787A1 (enExample)
MX (1) MX2007003318A (enExample)
TW (1) TW200626592A (enExample)
WO (1) WO2006034315A2 (enExample)

Families Citing this family (57)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7517884B2 (en) 1998-03-30 2009-04-14 Kalypsys Inc. Sulfonyl-substituted bicyclic compounds as modulators of PPAR
US20050119251A1 (en) * 2001-12-21 2005-06-02 Jian-Min Fu Nicotinamide derivatives and their use as therapeutic agents
WO2006034312A1 (en) 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Bicyclic heterocyclic derivatives and their use as inhibitors of stearoyl-coa-desaturase (scd)
AR051094A1 (es) * 2004-09-20 2006-12-20 Xenon Pharmaceuticals Inc Derivados heterociclicos y su uso como inhibidores de la estearoil-coa desaturasa
MX2007003327A (es) 2004-09-20 2007-06-05 Xenon Pharmaceuticals Inc Derivados heterociclicos, y su uso como mediadores de estearoil-coa desaturasa.
TW200626153A (en) * 2004-09-20 2006-08-01 Xenon Pharmaceuticals Inc Heterocyclic derivatives and their use as therapeutic agents
CN101084207A (zh) * 2004-09-20 2007-12-05 泽农医药公司 杂环衍生物及其作为硬脂酰CoA去饱和酶抑制剂的用途
EP1807085B1 (en) 2004-09-20 2013-08-21 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors
EP1804799B1 (en) 2004-09-20 2013-08-21 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors
MX2007003321A (es) 2004-09-20 2007-06-05 Xenon Pharmaceuticals Inc Derivados heterociclicos y su uso como agentes terapeuticos.
CN101083982A (zh) 2004-09-20 2007-12-05 泽农医药公司 用于治疗硬脂酰CoA去饱和酶介导的疾病的杂环衍生物
HUE039584T2 (hu) 2004-10-29 2019-01-28 Kalypsys Inc PPAR-modulátor szulfonil-szubsztituált biciklusos vegyületek
GT200600046A (es) * 2005-02-09 2006-09-25 Terapia de combinacion
BRPI0611187A2 (pt) 2005-06-03 2010-08-24 Xenon Pharmaceuticals Inc derivados aminotiazàis como inibidores da estearoil-coa desaturase humana
US7541359B2 (en) * 2005-06-30 2009-06-02 Janssen Pharmaceutica N.V. N-heteroarylpiperazinyl ureas as modulators of fatty acid amide hydrolase
WO2007051095A1 (en) 2005-10-25 2007-05-03 Kalypsys, Inc. Salts of modulators of ppar and methods of treating metabolic disorders
MX2008015229A (es) 2006-06-05 2008-12-12 Novartis Ag Compuestos organicos.
WO2008024390A2 (en) 2006-08-24 2008-02-28 Novartis Ag 2- (pyrazin-2-yl) -thiazole and 2- (1h-pyraz0l-3-yl) -thiazole derivatives as well as related compounds as stearoyl-coa desaturase (scd) inhibitors for the treatment of metabolic, cardiovascular and other disorders
JP5351025B2 (ja) * 2006-09-22 2013-11-27 ノバルティス アーゲー ヘテロ環式有機化合物
AU2007312866A1 (en) * 2006-10-20 2008-04-24 Merck Frosst Canada Ltd. Azacycloalkane derivatives as inhibitors of stearoyl-coenzyme A delta-9 desaturase
TW200826936A (en) 2006-12-01 2008-07-01 Merck Frosst Canada Ltd Azacycloalkane derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase
US8680012B2 (en) 2006-12-14 2014-03-25 Syngenta Crop Protection Llc 4-phenyl-pyrane-3,5-diones,4-phenyl-thiopyrane-3,6-diones and cyclohexanetriones as novel herbicides
US8258160B2 (en) 2006-12-20 2012-09-04 Novartis Ag SCD1 inhibitors triazole and tetrazole compounds
WO2008091863A1 (en) 2007-01-23 2008-07-31 Kalypsys, Inc. Sulfonyl-substituted bicyclic compounds as ppar modulators for the treatment of non-alcoholic steatohepatitis
AR064965A1 (es) 2007-01-26 2009-05-06 Merck Frosst Canada Inc Derivados de azacicloalcanos como inhibidores de estearoil - coenzima a delta -9 desaturasa
JP2010524987A (ja) 2007-04-27 2010-07-22 サノフィ−アベンティス 2−ヘテロアリール−ピロロ[3,4−c]ピロール誘導体及びscd阻害剤としてのそれらの使用
GB0710223D0 (en) 2007-05-29 2007-07-11 Syngenta Ltd Novel Herbicides
WO2008157844A1 (en) 2007-06-21 2008-12-24 Forest Laboratories Holdings Limited Novel piperazine derivatives as inhibitors of stearoyl-coa desaturase
GB0712653D0 (en) 2007-06-28 2007-08-08 Syngenta Ltd Novel herbicides
JP2011500767A (ja) 2007-10-26 2011-01-06 グラクソ グループ リミテッド P2x7モジュレータとしての4−ベンゾイル−1−置換ピペラジン−2−オン誘導体
AP2010005287A0 (en) 2007-12-13 2010-06-30 Syngenta Participations Ag 4-phenylpyrane-3,5-diones,4-phenylthiopyrane-3,5-diones and 2-phenylcyclohexane-1,3,5-triones as herbicides
JP2011525478A (ja) * 2008-03-20 2011-09-22 フォレスト・ラボラトリーズ・ホールディングス・リミテッド ステアロイル−CoAデサチュラーゼの阻害剤としての新規ピペラジン誘導体
GB0900641D0 (en) 2009-01-15 2009-02-25 Syngenta Ltd Novel herbicides
GB0901086D0 (en) 2009-01-22 2009-03-11 Syngenta Ltd Novel herbicides
GB0901835D0 (en) 2009-02-04 2009-03-11 Syngenta Ltd Novel herbicides
GB0901834D0 (en) 2009-02-04 2009-03-11 Syngenta Ltd Novel herbicides
US9168248B2 (en) 2009-02-17 2015-10-27 Merck Canada Inc. Spiro compounds useful as inhibitors of stearoyl-coenzyme A delta-9 desaturase
EP2459568A4 (en) 2009-07-28 2013-02-27 Merck Frosst Canada Ltd NEW SPIRO COMPOUNDS AS AN INHIBITORS OF STEAROYL COENZYME A DELTA 9 DESATURASE
WO2011030312A1 (en) 2009-09-10 2011-03-17 Institut National De La Sante Et De La Recherche Medicale (Inserm) NOVEL INHIBITORS OF STEAROYL-CoA-DESATURASE-1 AND THEIR USES
CN102574841A (zh) * 2009-10-01 2012-07-11 诺瓦提斯公司 调节硬脂酰-coa去饱和酶的吡唑衍生物
KR20130087002A (ko) 2010-06-04 2013-08-05 알바니 몰레큘라 리써치, 인크. 글리신 수송체-1 저해제, 그의 제조 방법 및 그의 용도
KR20140084164A (ko) 2011-10-15 2014-07-04 제넨테크, 인크. 암의 치료를 위한 scd1 길항제
WO2013175474A2 (en) 2012-05-22 2013-11-28 Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. Selective inhibitors of undifferentiated cells
US9290465B2 (en) * 2012-12-03 2016-03-22 Hoffmann-La Roche Inc. Substituted isoxazole amine compounds as inhibitors of SCD1
PE20151979A1 (es) 2013-01-23 2016-01-15 Astrazeneca Ab Compuestos quimicos
MA46589A (fr) 2016-10-24 2019-08-28 Yumanity Therapeutics Inc Composés et utilisations de ces derniers
MA47212A (fr) 2017-01-06 2019-11-13 Yumanity Therapeutics Inc Méthodes de traitement de troubles neurologiques
SMT201900517T1 (it) 2017-03-20 2019-11-13 Forma Therapeutics Inc Composizioni di pirrolopirrolo come attivatori di piruvato chinasi (pkr)
WO2019084157A1 (en) 2017-10-24 2019-05-02 Yumanity Therapeutics, Inc. COMPOUNDS AND USES THEREOF
CN112312913B (zh) 2018-03-23 2024-03-08 詹森药业有限公司 化合物和其用途
US11001588B2 (en) 2018-09-19 2021-05-11 Forma Therapeutics, Inc. Activating pyruvate kinase R and mutants thereof
CN113166060B (zh) 2018-09-19 2024-01-09 诺沃挪第克健康护理股份公司 用丙酮酸激酶激活化合物治疗镰状细胞病
MX2021008903A (es) 2019-01-24 2021-11-04 Yumanity Therapeutics Inc Compuestos y usos de los mismos.
JP2022526890A (ja) * 2019-03-22 2022-05-27 ユマニティ セラピューティクス,インコーポレーテッド 化合物及びその使用
CA3151612A1 (en) 2019-09-19 2021-03-25 George P. Luke Pyruvate kinase r (pkr) activating compositions
EA202192047A1 (ru) 2019-11-13 2021-12-08 Юманити Терапьютикс, Инк. Соединения и их применение
US12128035B2 (en) 2021-03-19 2024-10-29 Novo Nordisk Health Care Ag Activating pyruvate kinase R

Family Cites Families (279)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL237878A (enExample) * 1958-04-07
US2985657A (en) 1959-10-12 1961-05-23 Paul A J Janssen 1-(aroylalkyl)-4-heterocyclylpiperazines
US3830924A (en) * 1966-12-23 1974-08-20 American Cyanamid Co Substituted nitroimidazolyl-thiadiazoles as growth promoting agents
AT340933B (de) 1973-08-20 1978-01-10 Thomae Gmbh Dr K Verfahren zur herstellung neuer pyrimidinderivate und ihrer saureadditionssalze
DE2341925A1 (de) 1973-08-20 1975-03-06 Thomae Gmbh Dr K Neue pyrimidinderivate und verfahren zu ihrer herstellung
GB1432660A (en) * 1973-10-30 1976-04-22 Science Union & Cie Piperazine derivatives processes for their preparation and and pharamacueitcal compositions containing them
DE2427943C2 (de) 1974-06-10 1984-08-02 Dr. Karl Thomae Gmbh, 7950 Biberach Benzimidazole, Verfahren zu deren Herstellung und diese enthaltende Arzneimittel
DE2516040C2 (de) 1974-06-10 1984-12-20 Dr. Karl Thomae Gmbh, 7950 Biberach Benzimidazole, Verfahren zu deren Herstellung und diese enthaltende Arzneimittel
NL171985C (nl) 1976-02-10 1983-06-16 Rhone Poulenc Ind Werkwijze voor het bereiden van preparaten met werking tegen schistosomiasis, de aldus verkregen gevormde preparaten en werkwijze voor het bereiden van 1,2-dithioolverbindingen.
DE2965377D1 (en) 1978-10-02 1983-06-16 Lepetit Spa 6-amino substituted n-pyrrolyl-3-pyridazine amines, their preparation, and pharmaceutically antihypertensive compositions containing them
US4247551A (en) 1979-09-17 1981-01-27 Gruppo Lepetit S.P.A. N-Pyrrolyl-pyridazineamines and their use as antihypertensive agents
FI70411C (fi) 1980-12-29 1986-09-19 Pfizer Foerfarande foer framstaellning av nya antihypertensiva 4-amino-6,7-dimetoxi-2-piperazinokinazolin derivat
US4439606A (en) * 1982-05-06 1984-03-27 American Cyanamid Company Antiatherosclerotic 1-piperazinecarbonyl compounds
CH655103A5 (de) 1983-03-11 1986-03-27 Sandoz Ag Azolderivate, verfahren zu ihrer herstellung und ihre verwendung.
US5001125A (en) 1984-03-26 1991-03-19 Janssen Pharmaceutica N.V. Anti-virally active pyridazinamines
EP0200024B1 (de) 1985-04-30 1992-07-01 ARZNEIMITTELWERK DRESDEN GmbH 3-Cyan-pyridine, Verfahren zu ihrer Herstellung und ihre pharmazeutische Verwendung
ES8802151A1 (es) 1985-07-31 1988-04-01 Janssen Pharmaceutica Nv Un procedimiento para la preparacion de nuevos piridazinaminas.
DE3536030A1 (de) 1985-10-09 1987-04-09 Thomae Gmbh Dr K Verwendung von benzimidazolen zur behandlung der migraene
WO1988007527A1 (en) 1987-04-03 1988-10-06 The Upjohn Company Amino-9,10-secosteroids
CA1338012C (en) 1987-04-27 1996-01-30 John Michael Mccall Pharmaceutically active amines
NZ225045A (en) 1987-07-01 1990-06-26 Janssen Pharmaceutica Nv Antiviral pharmaceutical compositions containing cyclodextrin and an antiviral agent
MY104343A (en) 1987-11-23 1994-03-31 Janssen Pharmaceutica Nv Novel pyridizinamine deravatives
DE3827599A1 (de) 1988-08-13 1990-02-15 Hoechst Ag Verwendung von optisch aktiven tetrahydrofuran-2-carbonsaeureestern als dotierstoffe in fluessigkristallmischungen, diese enthaltende fluessigkristallmischungen und neue optisch aktive tetrahydrofuran-2-carbonsaeureester
US4994456A (en) 1989-03-01 1991-02-19 Nisshin Flour Milling Co., Ltd. Pyridinecarboxylic acid amide derivatives and pharmaceutical compositions comprising same
CA2071529C (en) 1989-12-28 2001-03-20 Donna Lee Romero Diaromatic substituted anti-aids compounds
EP0507863A4 (en) 1989-12-28 1993-07-07 Virginia Commonwealth University Sigma receptor ligands and the use thereof
IL96891A0 (en) 1990-01-17 1992-03-29 Merck Sharp & Dohme Indole-substituted five-membered heteroaromatic compounds,their preparation and pharmaceutical compositions containing them
US5166147A (en) 1990-07-09 1992-11-24 The Du Pont Merck Pharmaceutical Company 4-heteroaryl-and 4-aryl-1,4-dihydropyridine, derivatives with calcium agonist and alpha1 -antagonist activity
EP0471201A1 (de) 1990-07-21 1992-02-19 Hoechst Aktiengesellschaft Neue Oxazolidinon-Derivate und ihre Verwendung als Dotierstoffe in Flüssigkristallmischungen
DE4031000A1 (de) 1990-10-01 1992-04-09 Hoechst Ag 4- oder 5-substituierte pyridin-2-carbonsaeuren, verfahren zu deren herstellung sowie deren verwendung als arzneimittel
IT1245712B (it) 1991-04-09 1994-10-14 Boehringer Mannheim Italia Ammine eterocicliche utili terapia dell'asma e dell'infiammazione delle vie aeree
EP0520292A1 (de) 1991-06-19 1992-12-30 Hoechst Aktiengesellschaft Chirale Azetidinon-Derivate und ihre Verwendung als Dotierstoffe in Flüssigkristallmischungen
PT100639A (pt) 1991-06-27 1993-09-30 Univ Virginia Commonwealth Metodo para o tratamento terapeutico com compostos que sao ligandos ao receptor sigma e compostos ai utilizados, nomeadamente derivados fenilalquil-amina, aminotetralina,piperazina e piperidina
EP0594702B1 (en) 1991-07-03 1997-01-29 PHARMACIA & UPJOHN COMPANY Substituted indoles as anti-aids pharmaceuticals
EP0524146A1 (de) 1991-07-19 1993-01-20 Ciba-Geigy Ag Aminosubstituierte Piperazinderivate
DE4124942A1 (de) 1991-07-27 1993-01-28 Thomae Gmbh Dr K 5-gliedrige heterocyclen, verfahren zu ihrer herstellung und diese verbindungen enthaltende arzneimittel
GB9117639D0 (en) 1991-08-15 1991-10-02 Ici Plc Therapeutic compounds
JPH05255089A (ja) 1991-12-18 1993-10-05 Sanwa Kagaku Kenkyusho Co Ltd 抗ウイルス剤
JPH05345780A (ja) 1991-12-24 1993-12-27 Kumiai Chem Ind Co Ltd ピリミジンまたはトリアジン誘導体及び除草剤
AU3351293A (en) 1992-01-21 1993-08-03 Glaxo Group Limited Piperidineacetic acid derivatives as inhibitors of fibrinogen-dependent blood platelet aggregation
EP0630370A1 (en) 1992-03-11 1994-12-28 E.I. Du Pont De Nemours And Company Fungicidal oxazolidinones
HU209678B (en) 1992-06-09 1994-10-28 Richter Gedeon Vegyeszet Process for producing biologically active eburnamenin-14-carbonyl-amino derivatives and pharmaceutical compositions containing them
IT1255704B (it) 1992-09-30 1995-11-10 Boehringer Mannheim Italia Ammine eterocicliche utili nella terapia dell'asma e dell'infiammazione delle vie aeree
DE4236106A1 (de) 1992-10-26 1994-04-28 Hoechst Ag Azaaromatische Verbindungen, Verfahren zu ihrer Herstellung und ihre Verwendung in flüssigkristallinen Mischungen
US5494908A (en) 1992-11-23 1996-02-27 Hoechst-Roussel Pharmaceutical Incorporated Substituted 3-(aminoalkylamino)-1,2-benzisoxazoles and related compounds
US5380726A (en) 1993-01-15 1995-01-10 Ciba-Geigy Corporation Substituted dialkylthio ethers
DE4302051A1 (de) 1993-01-26 1994-07-28 Thomae Gmbh Dr K 5-gliedrige Heterocyclen, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel
US5547605A (en) 1993-12-15 1996-08-20 Hoechst Aktiengesellschaft 2-Aryloxytetrafluoropropionic esters, process for their preparation, and their use in liquid-crystalline mixtures
DE4343286A1 (de) 1993-12-17 1995-06-22 Hoechst Ag Heteroaromatische Verbindungen und ihre Verwendung in flüssigkristallinen Mischungen
DE19502178A1 (de) 1994-01-27 1995-08-03 Hoechst Ag Thiadiazolderivate, Verfahren zu ihrer Herstellung und ihre Verwendung als Vorprodukte zur Herstellung von Flüssigkristallen
US5464788A (en) 1994-03-24 1995-11-07 Merck & Co., Inc. Tocolytic oxytocin receptor antagonists
DE4423044A1 (de) 1994-07-01 1996-01-04 Hoechst Ag 1-(3-Alkyloxiran-2-yl)alkylester mesogener Carbonsäuren und ihre Verwendung in flüssigkristallinen Mischungen
US5571811A (en) 1994-07-12 1996-11-05 Janssen Pharmaceutica N.V. Sulfonamide derivatives of azolones
US5637592A (en) 1994-07-12 1997-06-10 Janssen Pharmaceutica N.V. Acyl derivatives of azolones
US5607932A (en) 1994-07-12 1997-03-04 Janssen Pharmaceutica N.V. Heterocyclic derivatives of azolones
RU2165423C2 (ru) 1994-10-07 2001-04-20 Фудзисава Фармасьютикал Ко., Лтд. Полипептидное соединение, способ его получения и фармацевтическая композиция
US5702637A (en) 1995-04-19 1997-12-30 Minnesota Mining And Manufacturing Company Liquid crystal compounds having a chiral fluorinated terminal portion
US5668148A (en) 1995-04-20 1997-09-16 Merck & Co., Inc. Alpha1a adrenergic receptor antagonists
DE19517056A1 (de) 1995-05-10 1996-11-14 Hoechst Ag 1-Fluor-5,6,7,8-tetrahydroisochinolin-Derivate und ihre Verwendung in flüssigkristallinen Mischungen
DE19517025A1 (de) 1995-05-10 1996-11-14 Hoechst Ag Trifluortetrahydroisochinolin-Derivate und ihre Verwendung in flüssigkristallinen Mischungen
DE19517038A1 (de) 1995-05-10 1996-11-14 Hoechst Ag 1,8-Difluorisochinolinderivate und ihre Verwendung in flüssigkristallinen Mischungen
DE19517060A1 (de) 1995-05-10 1996-11-14 Hoechst Ag 1-Fluorisochinolinderivate und ihre Verwendung in flüssigkristallinen Mischungen
DE19517051A1 (de) 1995-05-10 1996-11-14 Hoechst Ag 1-Fluor-6,7-dihydro-5H-isochinolin-8-on-Derivate und ihre Verwendung in flüssigkristallinen Mischungen
TW357143B (en) 1995-07-07 1999-05-01 Novartis Ag Benzo[g]quinoline derivatives
ZA969622B (en) 1995-12-13 1998-05-15 Upjohn Co Oxazolidinone antibacterial agents having a six-membered heteroaromatic ring.
CN1104430C (zh) 1996-01-15 2003-04-02 詹森药业有限公司 抑制血管生成的哒嗪胺
US6313127B1 (en) 1996-02-02 2001-11-06 Zeneca Limited Heterocyclic compounds useful as pharmaceutical agents
DE19614204A1 (de) 1996-04-10 1997-10-16 Thomae Gmbh Dr K Carbonsäurederivate, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
JPH107572A (ja) 1996-06-17 1998-01-13 Sumitomo Pharmaceut Co Ltd 腫瘍壊死因子産生阻害剤
GB9614238D0 (en) 1996-07-06 1996-09-04 Zeneca Ltd Chemical compounds
DE19630068A1 (de) 1996-07-25 1998-01-29 Basf Ag Neue flüssigkristalline Verbindungen und deren Vorprodukte
EP0929553B1 (en) * 1996-10-02 2005-03-16 Novartis AG Pyrimidine derivatives and processes for the preparation thereof
DE59707681D1 (de) 1996-10-28 2002-08-14 Rolic Ag Zug Vernetzbare, photoaktive Silanderivate
ZA98376B (en) 1997-01-23 1998-07-23 Hoffmann La Roche Sulfamide-metalloprotease inhibitors
AU8096798A (en) 1997-06-27 1999-01-19 Resolution Pharmaceuticals Inc. Dopamine d4 receptor ligands
CN1239570A (zh) 1997-07-17 1999-12-22 索尼公司 磁记录介质和使用该介质的磁记录/再现装置
ES2125206B1 (es) 1997-07-21 1999-11-16 Esteve Labor Dr Derivados de acil-piperazinil-pirimidinas, su preparacion y su aplicacion como medicamentos.
SE9703377D0 (sv) 1997-09-18 1997-09-18 Astra Ab New compounds
AR013693A1 (es) 1997-10-23 2001-01-10 Uriach & Cia Sa J Nuevas piperidinas y piperazinas como inhibidores de la agregacion plaquetaria
CZ299499B6 (cs) 1997-10-27 2008-08-13 Neurosearch A/S Homopiperazinový derivát, farmaceutická kompoziceho obsahující a jeho použití
WO1999033805A1 (en) 1997-12-26 1999-07-08 Mochida Pharmaceutical Co., Ltd. Aromatic compounds having cyclic amino or salts thereof
DK1054874T3 (da) 1998-02-13 2002-12-30 Upjohn Co Substituerede aminophenylisoxazolinderivater, der er anvendelige som antimokrobielle midler
EP1060179A1 (en) 1998-02-25 2000-12-20 PHARMACIA & UPJOHN COMPANY Substituted aminomethyl isoxazoline derivatives useful as antimicrobials
DK1064273T3 (da) * 1998-03-19 2003-03-31 Upjohn Co 1,3,4-Thiadiazoler, som er nyttige til behandling af CMV-infektioner
DE59914996D1 (en) 1998-04-20 2009-05-14 Abbott Gmbh & Co Kg Heterocyclisch substituierte amide als calpainhemmer
WO1999055675A1 (de) 1998-04-29 1999-11-04 Axiva Gmbh Verfahren zur katalytischen herstellung von substituierten bipyridylderivaten
KR100579792B1 (ko) 1998-05-13 2006-05-12 동화약품공업주식회사 신규 2,5-피리딘디카복실산 유도체
GB9812019D0 (en) 1998-06-05 1998-07-29 Zeneca Ltd Chemical compounds
NZ508174A (en) 1998-06-05 2003-10-31 Astrazeneca Ab Oxazolidinone derivatives, process for their preparation and pharmaceutical compositions containing them
JP2000119253A (ja) * 1998-08-11 2000-04-25 Dai Ichi Seiyaku Co Ltd 新規なスルホニル誘導体
ATE259803T1 (de) 1998-10-09 2004-03-15 Janssen Pharmaceutica Nv 4,5-dehydroisoxazole derivate und ihre pharmazeutische verwendung
DE69913558T2 (de) 1998-10-21 2004-11-04 Takeda Chemical Industries, Ltd. Kondensierte pyridazinderivate, verfahren zu ihrer herstellung und ihre anwendung
AU1549500A (en) 1998-12-02 2000-06-19 Novo Nordisk A/S Use of n-substituted azaheterocyclic compounds for the manufacture of a pharmaceutical composition for the treatment of indications related to angiogenesis
GB9826412D0 (en) 1998-12-03 1999-01-27 Glaxo Group Ltd Chemical compounds
EP1156045A4 (en) 1999-01-28 2002-04-17 Nippon Shinyaku Co Ltd AMID DERIVATIVES AND DRUG COMPOSITIONS
EP1359152B1 (en) 1999-01-29 2008-05-07 Abbott Laboratories Diazabicyclic derivatives as nicotinic acetylcholine receptor ligands
ES2226622T3 (es) 1999-02-24 2005-04-01 F. Hoffmann-La Roche Ag Derivados de 4-fenil piridina y su empleo como antagonistas del receptor nk-1.
HUP0202248A3 (en) 1999-03-12 2006-06-28 Boehringer Ingelheim Pharma Compounds useful as anti-inflammatory agents
WO2000061556A1 (en) 1999-04-09 2000-10-19 Meiji Seika Kaisha, Ltd. Nitrogen-containing heterocyclic compounds and benamide compounds and drugs containing the same
FR2792314B1 (fr) 1999-04-15 2001-06-01 Adir Nouveaux composes aminotriazoles, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
AU2935200A (en) 1999-04-30 2000-11-17 Pfizer Products Inc. Compounds for the treatment of obesity
DE19922723A1 (de) 1999-05-18 2000-11-23 Clariant Gmbh Aktivmatrix-Displays mit hohem Kontrast
WO2000071536A1 (en) 1999-05-20 2000-11-30 E.I. Du Pont De Nemours And Company Heteroaryloxypyrimidine insecticides and acaricides
WO2001007409A1 (en) 1999-07-23 2001-02-01 Astrazeneca Uk Limited Carbazole derivatives and their use as neuropeptide y5 receptor ligands
DE19934799B4 (de) 1999-07-28 2008-01-24 Az Electronic Materials (Germany) Gmbh Chiral-smektische Flüssigkristallmischung und ihre Verwendung in Aktivmatrix-Displays mit hohen Kontrastwerten
US6127382A (en) 1999-08-16 2000-10-03 Allergan Sales, Inc. Amines substituted with a tetrahydroquinolinyl group an aryl or heteroaryl group and an alkyl group, having retinoid-like biological activity
DE60039359D1 (de) 1999-09-04 2008-08-14 Astrazeneca Ab Amide als pyruvatdehydrogenaseinhibitoren
US6156758A (en) 1999-09-08 2000-12-05 Isis Pharmaceuticals, Inc. Antibacterial quinazoline compounds
AUPQ288499A0 (en) 1999-09-16 1999-10-07 Biota Scientific Management Pty Ltd Antiviral agents
MX228790B (es) 1999-09-17 2005-06-30 Millennium Pharm Inc Inhibidores del factor xa.
SK285240B6 (sk) 1999-09-24 2006-09-07 Janssen Pharmaceutica N. V. Antivírusové prostriedky
US6677452B1 (en) 1999-09-30 2004-01-13 Lion Bioscience Ag Pyridine carboxamide or sulfonamide derivatives and combinatorial libraries thereof
WO2001032628A1 (en) 1999-11-03 2001-05-10 Bristol-Myers Squibb Pharma Company Cyano compounds as factor xa inhibitors
WO2001043746A1 (en) 1999-12-14 2001-06-21 Nippon Shinyaku Co., Ltd. Medicinal composition
SE9904652D0 (sv) 1999-12-17 1999-12-17 Astra Pharma Prod Novel Compounds
US6518285B2 (en) 1999-12-21 2003-02-11 Ortho Mcneil Pharmaceutical, Inc. Piperidinyloxy and pyrrolidinyloxy oxazolidinone antibacterials
JP2003519143A (ja) 1999-12-28 2003-06-17 ファーマコピーア,インコーポレーティッド ピリミジン及びトリアジン系キナーゼ阻害剤
US6515124B2 (en) * 2000-02-09 2003-02-04 Hoffman-La Roche Inc. Dehydroamino acids
ATE475718T1 (de) 2000-02-24 2010-08-15 Xenon Pharmaceuticals Inc Stearoyl-coa-desaturase zur identifizierung von triglyceridreduktionstherapeutika
HUP0300029A2 (en) 2000-02-25 2003-05-28 Hoffmann La Roche Adenosine receptor modulators, pharmaceutical compositions containing them and their use
US6605615B2 (en) 2000-03-01 2003-08-12 Tularik Inc. Hydrazones and analogs as cholesterol lowering agents
WO2001068619A1 (en) 2000-03-15 2001-09-20 Warner-Lambert Company 5-amide substituted diarylamines as mex inhibitors
EP1339702A1 (en) * 2000-03-15 2003-09-03 Warner-Lambert Company 5-amide substituted diarylamines as mek inhibitors
US6613917B1 (en) 2000-03-23 2003-09-02 Allergan, Inc. Amines substituted with a dihydronaphthalenyl, chromenyl, or thiochromenyl group, an aryl or heteroaryl group and an alkyl group, having retinoid-like biological activity
US20020045613A1 (en) 2000-04-27 2002-04-18 Heinz Pauls 1-aroyl-piperidinyl benzamidines
AU4114201A (en) 2000-04-28 2001-11-12 Tanabe Seiyaku Co Cyclic compounds
CZ20023562A3 (cs) 2000-04-28 2003-03-12 Sankyo Company, Limited PPAR gama modulátory
GB0010757D0 (en) * 2000-05-05 2000-06-28 Astrazeneca Ab Chemical compounds
GB0013378D0 (en) 2000-06-01 2000-07-26 Glaxo Group Ltd Use of therapeutic benzamide derivatives
GB0013383D0 (en) 2000-06-01 2000-07-26 Glaxo Group Ltd Therapeutic benzamide derivatives
GB0030304D0 (en) * 2000-12-13 2001-01-24 Lilly Co Eli Compounds
EP1307444B1 (en) 2000-07-27 2007-10-03 Eli Lilly And Company Substituted heterocyclic amides
HRP20030081A2 (en) 2000-08-08 2005-02-28 Sanofi-Aventis Benzimidazole derivatives, preparation and therapeutic use thereof
EP1184442A1 (en) 2000-08-30 2002-03-06 Clariant International Ltd. Liquid crystal mixture
FR2815032B1 (fr) 2000-10-10 2003-08-08 Pf Medicament Nouveaux derives d'aminophenyle piperazine ou d'amino phenyle piperide inhibiteurs de proteines prenyl transferase ainsi que leurs preparations
MXPA03003264A (es) 2000-10-13 2003-06-06 Neurosearch As Tratamiento de trastornos afectivos mediante la accion combinada de un agonista del receptor nicotinico y una sustancia monoaminergica.
JP4170753B2 (ja) 2000-10-17 2008-10-22 ファルマシア・アンド・アップジョン・カンパニー・エルエルシー オキサゾリジノン化合物の製造方法
DE10060412A1 (de) 2000-12-05 2002-06-06 Bayer Ag DELTA1-Pyrroline
US7129242B2 (en) 2000-12-06 2006-10-31 Signal Pharmaceuticals, Llc Anilinopyrimidine derivatives as JNK pathway inhibitors and compositions and methods related thereto
WO2002055496A1 (en) 2001-01-15 2002-07-18 Glaxo Group Limited Aryl piperidine and piperazine derivatives as inducers of ldl-receptor expression
JP4280068B2 (ja) 2001-01-16 2009-06-17 アストラゼネカ・アクチエボラーグ 治療用クロマン化合物
US7026314B2 (en) 2001-01-16 2006-04-11 Astrazeneca Ab Therapeutic chromone compounds
EP1353913A2 (en) 2001-01-16 2003-10-22 AstraZeneca AB Therapeutic heterocyclic compounds
ES2317116T3 (es) * 2001-02-16 2009-04-16 Aventis Pharmaceuticals Inc. Derivados de carbonilos sustituidos heterociclicos y su uso como ligandos del receptor de dopamina d3.
US7126003B2 (en) 2001-03-07 2006-10-24 Daiichi Pharmaceutical Co., Ltd. Method for producing 2-azetidinone derivative
US20020169166A1 (en) 2001-03-09 2002-11-14 Cowart Marlon D. Benzimidazoles that are useful in treating sexual dysfunction
EP1373204B1 (en) 2001-03-09 2016-10-26 Janssen Pharmaceuticals, Inc. Heterocyclic compounds
SE0100902D0 (sv) * 2001-03-15 2001-03-15 Astrazeneca Ab Compounds
CN1509275A (zh) * 2001-03-15 2004-06-30 金属蛋白酶抑制剂
FR2823209B1 (fr) 2001-04-04 2003-12-12 Fournier Lab Sa Nouvelles thiohydantoines et leur utilisation en therapeutique
US20040106794A1 (en) 2001-04-16 2004-06-03 Schering Corporation 3,4-Di-substituted cyclobutene-1,2-diones as CXC-chemokine receptor ligands
CZ20032831A3 (cs) 2001-04-16 2004-03-17 Schering Corporation 3,4-Disubstituované cyklobuten-1,2-diony
US6911447B2 (en) 2001-04-25 2005-06-28 The Procter & Gamble Company Melanocortin receptor ligands
US20050009834A1 (en) 2001-05-09 2005-01-13 Shigeyuki Itoh Azole compounds, process for preparation of the same and use thereof
PL367205A1 (en) 2001-06-15 2005-02-21 Yamanouchi Pharmaceutical Co, Ltd. Phenylpyridine carbonyl piperazine derivative
WO2003003008A1 (en) 2001-06-29 2003-01-09 7Tm Pharma A/S Chemical libraries useful for drug discovery processes
US7115607B2 (en) 2001-07-25 2006-10-03 Amgen Inc. Substituted piperazinyl amides and methods of use
JO3429B1 (ar) 2001-08-13 2019-10-20 Janssen Pharmaceutica Nv مشتقات برميدينات مثبطة فيروس الايدز
WO2003018563A1 (en) 2001-08-31 2003-03-06 Northwestern University Anti-inflammatory and protein kinase inhibitor composition and method of use
JP2005504789A (ja) 2001-09-13 2005-02-17 シンタ ファーマスーティカルズ コーポレイション 癌治療のための2−アロイルイミダゾール化合物
FR2829926B1 (fr) 2001-09-26 2004-10-01 Oreal Composition pour la teinture des fibres keratiniques comprenant un colorant diazoique dicationique particulier
US6916812B2 (en) 2001-10-09 2005-07-12 Bristol-Myers Squibb Company Alpha-aminoamide derivatives as melanocortin agonists
US6824707B2 (en) 2001-10-23 2004-11-30 Clariant International Ltd. Active matrix liquid crystal device and smectic liquid crystal mixture
WO2003035602A1 (en) 2001-10-25 2003-05-01 Sankyo Company, Limited Lipid modulators
WO2003037862A1 (en) 2001-10-30 2003-05-08 Nippon Shinyaku Co., Ltd. Amide derivatives and drugs
SE0103649D0 (sv) 2001-11-01 2001-11-01 Astrazeneca Ab Therapeutic quinoline compounds
SE0103648D0 (sv) 2001-11-01 2001-11-01 Astrazeneca Ab Therapeutic quinolone compounds
GB0127008D0 (en) 2001-11-09 2002-01-02 Novartis Ag Organic compounds
US6620811B2 (en) 2001-11-19 2003-09-16 Hoffmann-La Roche Inc. Isonicotin- and nicotinamide derivatives of benzothiazoles
JP2005510564A (ja) 2001-11-28 2005-04-21 藤沢薬品工業株式会社 アポリポタンパク質b阻害剤としての複素環式アミド化合物
US7163952B2 (en) 2001-12-03 2007-01-16 Japan Tobacco Inc. Azole compound and medicinal use thereof
FR2833261B1 (fr) 2001-12-06 2004-07-02 Yang Ji Chemical Company Ltd Nouveaux composes inhibiteurs specifiques de la phospholipase a2 secretee non pancreatique humaine du groupe ii
AU2002350172A1 (en) 2001-12-07 2003-06-23 Eli Lilly And Company Substituted heterocyclic carboxamides with antithrombotic activity
US6806279B2 (en) * 2001-12-17 2004-10-19 Sunesis Pharmaceuticals, Inc. Small-molecule inhibitors of interleukin-2
US20050119251A1 (en) 2001-12-21 2005-06-02 Jian-Min Fu Nicotinamide derivatives and their use as therapeutic agents
US20030166932A1 (en) 2002-01-04 2003-09-04 Beard Richard L. Amines substituted with a dihydronaphthalenyl, chromenyl, or thiochromenyl group, an aryl or heteroaryl group and an alkyl group, having retinoid-like biological activity
IL162859A0 (en) 2002-02-05 2005-11-20 Novo Nordisk As Novel aryl-and heteroarylpiperazines
EP1485354B1 (en) 2002-03-13 2008-05-28 Janssen Pharmaceutica N.V. Sulfonylamino-derivatives as novel inhibitors of histone deacetylase
CA2476586C (en) 2002-03-13 2011-11-01 Janssen Pharmaceutica N.V. Sulfonyl-derivatives as novel inhibitors of histone deacetylase
BR0307607A (pt) 2002-03-13 2004-12-21 Janssen Pharmaceutica Nv Derivados de carbonilamino como inibidores de histona desacetilase
JP4725944B2 (ja) 2002-03-13 2011-07-13 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 ヒストンデアセチラーゼの阻害剤
AR038966A1 (es) 2002-03-18 2005-02-02 Solvay Pharm Bv Derivados de tiazol que tienen actividad antagonista, agonista o agonista parcial de cb1
WO2003080060A1 (en) 2002-03-20 2003-10-02 Schering Aktiengesellschaft Substituted piperazine antithrombotic pai-1 inhibitors
DE10217006A1 (de) 2002-04-16 2003-11-06 Merck Patent Gmbh Substituierte Indole
WO2003091247A2 (en) 2002-04-25 2003-11-06 Pharmacia Corporation Piperidinyl-and piperazinyl-sulfonylmethyl hydroxamic acids and their use as protease inhibitors
GB0209715D0 (en) 2002-04-27 2002-06-05 Astrazeneca Ab Chemical compounds
US6982259B2 (en) 2002-04-30 2006-01-03 Schering Aktiengesellschaft N-heterocyclic derivatives as NOS inhibitors
UA77526C2 (en) * 2002-06-07 2006-12-15 Sanofi Aventis Substituted derivatives of 1-piperazineacylpiperidine, a method for the preparation thereof and their use in therapy
HUP0202001A2 (hu) 2002-06-14 2005-08-29 Sanofi-Aventis DDP-IV gátló hatású azabiciklooktán- és nonánszármazékok
US20040082627A1 (en) 2002-06-21 2004-04-29 Darrow James W. Certain aromatic monocycles as kinase modulators
WO2004000318A2 (en) 2002-06-21 2003-12-31 Cellular Genomics, Inc. Certain amino-substituted monocycles as kinase modulators
WO2004009587A1 (en) 2002-07-22 2004-01-29 Orchid Chemicals & Pharmaceuticals Ltd Oxazolidinone derivatives as antibacterial agents
WO2004010927A2 (en) 2002-07-25 2004-02-05 Wisconsin Alumni Research Foundation Method for increasing insulin sensitivity and for treating and preventing type 2 diabetes
AU2003257637A1 (en) * 2002-08-23 2004-03-11 Dainippon Pharmaceutical Co., Ltd. Proline derivatives
JP2006501260A (ja) 2002-09-04 2006-01-12 シェーリング コーポレイション サイクリン依存性キナーゼインヒビターとしてのピラゾロピリミジン
KR20050057226A (ko) 2002-09-06 2005-06-16 얀센 파마슈티카 엔.브이. 알레르기성 비염 치료용 약제를 제조하기 위한 인돌릴 유도체의 용도
JP2004123732A (ja) * 2002-09-10 2004-04-22 Takeda Chem Ind Ltd 5員複素環化合物
JP2006506443A (ja) 2002-09-18 2006-02-23 ファイザー・プロダクツ・インク 形質転換成長因子(tgf)阻害剤としての新規なイソチアゾール及びイソキサゾール化合物
AU2003256003A1 (en) 2002-09-18 2004-04-08 Pfizer Products Inc. Novel oxazole and thiazole compounds as transforming growth factor (TGF) inhibitors
US7582761B2 (en) 2002-10-17 2009-09-01 Amgen Inc. Vanilloid receptor ligands and their use in treatments
US7084145B2 (en) 2002-10-25 2006-08-01 Pfizer Inc. Triazole compounds useful in therapy
DE10250708A1 (de) 2002-10-31 2004-05-19 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Alkin-Verbindungen mit MCH-antagonistischer Wirkung und diese Verbindungen enthaltende Arzneimittel
US20040097492A1 (en) 2002-11-01 2004-05-20 Pratt John K Anti-infective agents
FR2847253B1 (fr) 2002-11-19 2007-05-18 Aventis Pharma Sa Nouveaux derives de pyridazinones a titre de medicaments et compositions pharmaceutiques les renfermant
DE10254875A1 (de) 2002-11-25 2004-06-03 Bayer Healthcare Ag Phenylsulfoxid und -sulfon-Derivate
JP2004203871A (ja) 2002-12-13 2004-07-22 Yamanouchi Pharmaceut Co Ltd 医薬組成物
DE10259382A1 (de) * 2002-12-18 2004-07-01 Abbott Gmbh & Co. Kg 3-Substituierte 3,4-Dihydro-thieno[2,3-d]pyrimidin-4-on-Derivate, ihre Herstellung und Verwendung
AU2003299791A1 (en) * 2002-12-20 2004-07-22 Bayer Pharmaceuticals Corporation Substituted 3,5-dihydro-4h-imidazol-4-ones for the treatment of obesity
CN102558155A (zh) 2003-01-14 2012-07-11 阿伦纳药品公司 作为代谢调节剂的芳基和杂芳基衍生物及其所涉及的疾病如糖尿病和高血糖症的预防和治疗
EP1590341B1 (en) 2003-01-17 2009-06-17 Warner-Lambert Company LLC 2-aminopyridine substituted heterocycles as inhibitors of cellular proliferation
US20050130989A1 (en) 2003-01-28 2005-06-16 Aventis Pharma S. A. N-arylheteroaromatic products compositions containing them and use thereof
ATE551324T1 (de) 2003-02-03 2012-04-15 Janssen Pharmaceutica Nv Chinolin-amid-derivate als modulatoren von vanilloid-vr1-rezeptoren
GB0302671D0 (en) 2003-02-06 2003-03-12 Astrazeneca Ab Pharmaceutical formulations
HRP20050688B1 (hr) 2003-02-07 2017-03-24 Janssen Pharmaceutica N.V. Derivati pirimidina za sprječavanje hiv infekcije
DE602004015254D1 (de) 2003-02-07 2008-09-04 Janssen Pharmaceutica Nv Hiv-inhibierende1,2,4-triazine
US7223788B2 (en) 2003-02-14 2007-05-29 Sanofi-Aventis Deutschland Gmbh Substituted N-aryl heterocycles, process for their preparation and their use as medicaments
CN1753873A (zh) 2003-02-22 2006-03-29 默克专利股份有限公司 作为液晶的氰基吡啶酮衍生物
DK1606282T3 (da) 2003-02-24 2009-03-16 Arena Pharm Inc Phenyl- og pyridylpipereidinye-derivater som modulatorer af glucosemetabolisme
US6861422B2 (en) 2003-02-26 2005-03-01 Boehringer Ingelheim Pharma Gmbh & Co. Kg Dihydropteridinones, processes for preparing them and their use as pharmaceutical compositions
WO2004078716A1 (en) 2003-03-03 2004-09-16 Merck & Co. Inc. Acylated piperazine derivatives as melanocortin-4 receptor agonists
JP2006522750A (ja) * 2003-04-11 2006-10-05 ノボ ノルディスク アクティーゼルスカブ 代謝性症候群ならびに関連の疾患および障害を治療するために、11β−ヒドロキシステロイドデヒドロゲナーゼ1型阻害剤および抗高血圧剤を使用する併用療法
CA2523831C (en) 2003-04-29 2008-11-18 Pfizer Inc. 5,7-diaminopyrazolo[4,3-d]pyrimidines useful in the treatment of hypertension
WO2004110350A2 (en) 2003-05-14 2004-12-23 Torreypines Therapeutics, Inc. Compouds and uses thereof in modulating amyloid beta
DE10322408A1 (de) 2003-05-16 2004-12-02 Degussa Ag Stickstoffhaltige monodentate Phosphine und deren Verwendung in der Katalyse
GB0312832D0 (en) 2003-06-04 2003-07-09 Pfizer Ltd 2-amino-pyridine derivatives useful for the treatment of diseases
PE20050226A1 (es) 2003-06-04 2005-05-18 Aventis Pharma Sa Productos aril-heteroaromaticos y composiciones que los contienen
US7610411B2 (en) * 2003-06-23 2009-10-27 Sharp Kabushiki Kaisha Information processing device, line concentrator, network information processing system having the line concentrator, information processing program and storage medium
WO2005003087A2 (en) 2003-07-01 2005-01-13 Orchid Chemicals And Pharmaceuticals Ltd. Oxazole derivatives as antibacterial agents
KR20060120393A (ko) 2003-07-16 2006-11-27 얀센 파마슈티카 엔.브이. 글리코겐 신타아제 키나제 3 저해제로서의트리아졸로피리미딘 유도체
CN100549014C (zh) 2003-07-16 2009-10-14 詹森药业有限公司 作为糖原合酶激酶3抑制剂的三唑并嘧啶衍生物
CA2533397A1 (en) 2003-07-22 2005-02-03 Neurogen Corporation Substituted pyridin-2-ylamine analogues
FR2857966A1 (fr) 2003-07-24 2005-01-28 Aventis Pharma Sa Produits aryl-heteroaromatiques, compositions les contenant et utilisation
TW200523262A (en) 2003-07-29 2005-07-16 Smithkline Beecham Corp Inhibitors of AKT activity
CA2533898A1 (en) 2003-07-29 2005-02-10 Xenon Pharmaceuticals Inc. Pyridyl derivatives and their use as therapeutic agents
ES2342605T3 (es) 2003-07-29 2010-07-09 High Point Pharmaceuticals, Llc Piridazinil-piperazinas y su uso como ligandos del receptor histaminico h3.
WO2005011653A2 (en) 2003-07-30 2005-02-10 Xenon Pharmaceuticals Inc. Pyridazine derivatives and their use as therapeutic agents
US7754711B2 (en) 2003-07-30 2010-07-13 Xenon Pharmaceuticals Inc. Pyridazine derivatives and their use as therapeutic agents
EP2316825A1 (en) 2003-07-30 2011-05-04 Xenon Pharmaceuticals Inc. Pyridyl derivatives and their use as therapeutic agents
US7456180B2 (en) 2003-07-30 2008-11-25 Xenon Pharmaceuticals Inc. Piperazine derivatives and their use as therapeutic agents
HRP20110974T1 (hr) 2003-07-30 2012-01-31 Xenon Pharmaceuticals Inc. Derivati piperazina i njihova uporaba kao terapeutskih sredstava
CN1867554B (zh) 2003-08-11 2011-07-06 弗·哈夫曼-拉罗切有限公司 具有邻-取代的苯基的哌嗪及其作为glyt1抑制剂的用途
EP1657240A4 (en) 2003-08-18 2009-04-08 Fujifilm Finechemicals Co Ltd PYRIDYLTETRAHYDROPYRIDINE, PYRIDYLPIPERIDINE AND METHOD FOR THE PRODUCTION THEREOF
CN101851238B (zh) 2003-08-25 2012-07-18 卓维斯医药品有限责任公司 取代的8-杂芳基黄嘌呤
EP1659123A1 (en) 2003-08-29 2006-05-24 Dainippon Sumitomo Pharma Co., Ltd. Bicyclic pyrazole derivative
RU2355683C2 (ru) 2003-09-09 2009-05-20 Ф.Хоффманн-Ля Рош Аг Производные 1-бензоилпиперазина в качестве ингибиторов поглощения глицина для лечения психозов
WO2005023260A1 (en) 2003-09-09 2005-03-17 F. Hoffmann-La Roche Ag 1- (2-amino-benzol) -piperazine derivatives as glycine uptake inhibitors for the treatment of psychoses
US20050065178A1 (en) 2003-09-19 2005-03-24 Anwer Basha Substituted diazabicycloakane derivatives
US7399765B2 (en) 2003-09-19 2008-07-15 Abbott Laboratories Substituted diazabicycloalkane derivatives
CA2535313C (en) 2003-09-25 2012-07-17 Janssen Pharmaceutica N.V. Hiv replication inhibiting purine derivatives
AR047759A1 (es) 2003-09-26 2006-02-22 Vertex Pharma Derivados de fenil - piperazina como moduladores de receptores muscarnicos
PL2392565T3 (pl) 2003-09-26 2014-08-29 Exelixis Inc Modulatory c-Met i sposoby stosowania
US7199149B2 (en) 2003-10-01 2007-04-03 Bristol Myers Squibb Company Monocyclic and bicyclic lactams as factor Xa inhibitors
WO2005034952A2 (en) 2003-10-07 2005-04-21 The Feinstein Institute For Medical Research Isoxazole and isothiazole compounds useful in the treatment of inflammation
FR2860793A1 (fr) 2003-10-14 2005-04-15 Entomed Composes derives de norcantharidine, leurs procedes de preparation, les compositions les contenant et leurs utilisations
US20050124625A1 (en) 2003-10-21 2005-06-09 Salvati Mark E. Piperazine derivatives and their use as modulators of nuclear hormone receptor function
WO2005040109A1 (en) 2003-10-22 2005-05-06 Neurocrine Biosciences, Inc. Ligands of melanocortin receptors and compositions and methods related thereto
AU2004283056A1 (en) 2003-10-24 2005-05-06 Solvay Pharmaceuticals Gmbh Novel medical uses of compounds showing CB1-antagonistic activity and combination treatment involving said compounds
US20050124660A1 (en) 2003-10-27 2005-06-09 Jochen Antel Novel medical uses of compounds showing CB1-antagonistic activity and combination treatment involving said compounds
US7683059B2 (en) * 2003-10-28 2010-03-23 Amgen Inc. Triazole compounds and uses related thereto
GB0327323D0 (en) 2003-11-24 2003-12-31 Pfizer Ltd Novel pharmaceuticals
GB0327319D0 (en) 2003-11-24 2003-12-24 Pfizer Ltd Novel pharmaceuticals
KR20080052683A (ko) 2003-12-18 2008-06-11 인사이트 코포레이션 케모킨 수용체의 조절제로서의3-사이클로알킬아미노피롤리딘 유도체
CA2551038C (en) 2003-12-22 2010-04-27 Pfizer Inc. Triazole derivatives as vasopressin antagonists
US7345043B2 (en) 2004-04-01 2008-03-18 Miikana Therapeutics Inhibitors of histone deacetylase
AR048523A1 (es) 2004-04-07 2006-05-03 Kalypsys Inc Compuestos con estructura de aril sulfonamida y sulfonilo como moduladores de ppar y metodos para tratar trastornos metabolicos
ATE537830T1 (de) 2004-07-06 2012-01-15 Xenon Pharmaceuticals Inc Nicotinamid derivate und ihre verwendung als therapeutika
CN101084207A (zh) 2004-09-20 2007-12-05 泽农医药公司 杂环衍生物及其作为硬脂酰CoA去饱和酶抑制剂的用途
EP1807085B1 (en) 2004-09-20 2013-08-21 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors
CN101083982A (zh) 2004-09-20 2007-12-05 泽农医药公司 用于治疗硬脂酰CoA去饱和酶介导的疾病的杂环衍生物
EP1804799B1 (en) 2004-09-20 2013-08-21 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors
WO2006034312A1 (en) 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Bicyclic heterocyclic derivatives and their use as inhibitors of stearoyl-coa-desaturase (scd)
MX2007003321A (es) 2004-09-20 2007-06-05 Xenon Pharmaceuticals Inc Derivados heterociclicos y su uso como agentes terapeuticos.
AR051094A1 (es) 2004-09-20 2006-12-20 Xenon Pharmaceuticals Inc Derivados heterociclicos y su uso como inhibidores de la estearoil-coa desaturasa
TW200626153A (en) 2004-09-20 2006-08-01 Xenon Pharmaceuticals Inc Heterocyclic derivatives and their use as therapeutic agents
MX2007003327A (es) 2004-09-20 2007-06-05 Xenon Pharmaceuticals Inc Derivados heterociclicos, y su uso como mediadores de estearoil-coa desaturasa.
ATE472327T1 (de) * 2005-01-07 2010-07-15 Hoffmann La Roche Ä4-(heteroaryl)piperazin-1-ylü-(2,5-substituier e phenyl)methanon-derivate als glycin-transporter 1 (glyt-1) hemmer zur behandlung von neurologischen und neuropsychiatrischen erkrankungen
WO2006106423A2 (en) 2005-04-07 2006-10-12 Pfizer Inc. Amino sulfonyl derivatives as inhibitors of human 11-.beta.-hydrosysteroid dehydrogenase
BRPI0611187A2 (pt) 2005-06-03 2010-08-24 Xenon Pharmaceuticals Inc derivados aminotiazàis como inibidores da estearoil-coa desaturase humana
WO2006130986A1 (en) * 2005-06-09 2006-12-14 Merck Frosst Canada Ltd. Azacyclohexane derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase

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CN101083982A (zh) 2007-12-05
WO2006034315A2 (en) 2006-03-30
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AR051026A1 (es) 2006-12-13
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