ES2111288T3 - Nuevos 3,4-diaril tiofenos y analogos de los mismos utiles como agentes antiinflamatorios. - Google Patents

Nuevos 3,4-diaril tiofenos y analogos de los mismos utiles como agentes antiinflamatorios.

Info

Publication number
ES2111288T3
ES2111288T3 ES94906625T ES94906625T ES2111288T3 ES 2111288 T3 ES2111288 T3 ES 2111288T3 ES 94906625 T ES94906625 T ES 94906625T ES 94906625 T ES94906625 T ES 94906625T ES 2111288 T3 ES2111288 T3 ES 2111288T3
Authority
ES
Spain
Prior art keywords
sup
analogs
sulfamyl
new
inflammatory agents
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Lifetime
Application number
ES94906625T
Other languages
English (en)
Inventor
Stephen R Bertenshaw
Paul W Collins
Thomas D Penning
David B Reitz
Roland S Rogers
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Monsanto Co
GD Searle LLC
Original Assignee
Monsanto Co
GD Searle LLC
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=21712697&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ES2111288(T3) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Monsanto Co, GD Searle LLC filed Critical Monsanto Co
Application granted granted Critical
Publication of ES2111288T3 publication Critical patent/ES2111288T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/341—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365—Lactones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/38—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/56—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom 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
    • C07D307/58—One oxygen atom, e.g. butenolide
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/06—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
    • C07D333/14—Radicals substituted by singly bound hetero atoms other than halogen
    • C07D333/16—Radicals substituted by singly bound hetero atoms other than halogen by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/06—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
    • C07D333/14—Radicals substituted by singly bound hetero atoms other than halogen
    • C07D333/18—Radicals substituted by singly bound hetero atoms other than halogen by sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom 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
    • C07D333/28—Halogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom 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
    • C07D333/38—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals

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)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

UNA CLASE DE DERIVADOS DE TIOFENO SUSTITUIDO 3,4-DIARILO, FURANO Y PIRROLO Y ANALOGOS DE LOS MISMOS, COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN Y METODOS PARA UTILIZARLOS PARA TRATAR INFLAMACION Y DESORDENES RELACIONADOS CON LA INFLAMACION. COMPUESTOS DE INTERES PARTICULAR SON DEFINIDOS POR LA FORMULA (I), EN DONDE Y SE SELECCIONA DE O, S Y NR{SUP,1}; EN DONDE R{SUP,1} SE SELECCIONA DE HIDRURO Y ALKILO BAJO; EN DONDE X ES UNO O DOS SUSTITUYENTES SELECCIONADOS DE HIDRURO, HALO, ALCOXICARBONILO BAJO Y CARBONILO; EN DONDE R{SUP,2} Y R{SUP,3} SON INDEPENDIENTEMENTE ARILO O HETEROARILO; Y EN DONDE R{SUP,2} Y R{SUP,3} SON OPCIONALMENTE SUSTITUIDOS EN UNA POSICION SUSTITUIBLE CON UNO O MAS RADICALES SELECCIONADOS DE SULFAMILO, ALKILSULFONILO, HALO, ALCOXI BAJO Y ALKILO BAJO; O UNA SAL FARMACEUTICAMENTE ACEPTABLE DE LOS MISMOS.
ES94906625T 1993-01-15 1994-01-14 Nuevos 3,4-diaril tiofenos y analogos de los mismos utiles como agentes antiinflamatorios. Expired - Lifetime ES2111288T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US482293A 1993-01-15 1993-01-15

Publications (1)

Publication Number Publication Date
ES2111288T3 true ES2111288T3 (es) 1998-03-01

Family

ID=21712697

Family Applications (1)

Application Number Title Priority Date Filing Date
ES94906625T Expired - Lifetime ES2111288T3 (es) 1993-01-15 1994-01-14 Nuevos 3,4-diaril tiofenos y analogos de los mismos utiles como agentes antiinflamatorios.

Country Status (11)

Country Link
US (1) US7012094B1 (es)
EP (4) EP0764644A1 (es)
JP (1) JP3137648B2 (es)
AT (1) ATE160345T1 (es)
AU (1) AU6027694A (es)
CA (4) CA2152792C (es)
DE (2) DE9422447U1 (es)
DK (1) DK0679157T3 (es)
ES (1) ES2111288T3 (es)
GR (1) GR3025762T3 (es)
WO (1) WO1994015932A1 (es)

Families Citing this family (145)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6492413B2 (en) 1993-01-15 2002-12-10 G.D. Searle & Co. 3.4-diaryl thiophenes and analogs thereof having use as antiinflammatory agents
CA2152792C (en) 1993-01-15 2000-02-15 Stephen R. Bertenshaw Novel 3,4-diaryl thiophenes and analogs thereof having use as antiinflammatory agents
GB9420616D0 (en) * 1994-10-12 1994-11-30 Merck Sharp & Dohme Method, compositions and use
CA2161789A1 (en) * 1993-05-13 1994-11-24 Jacques Yves Gauthier 2-substituted-3,4-diarylthiophene derivatives as inhibitors of cyclooxygenase
US6090834A (en) * 1993-05-21 2000-07-18 G.D. Searle & Co. Substituted oxazoles for the treatment of inflammation
US5380738A (en) * 1993-05-21 1995-01-10 Monsanto Company 2-substituted oxazoles further substituted by 4-fluorophenyl and 4-methylsulfonylphenyl as antiinflammatory agents
US5474995A (en) * 1993-06-24 1995-12-12 Merck Frosst Canada, Inc. Phenyl heterocycles as cox-2 inhibitors
US5840746A (en) * 1993-06-24 1998-11-24 Merck Frosst Canada, Inc. Use of inhibitors of cyclooxygenase in the treatment of neurodegenerative diseases
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
CA2180651A1 (en) * 1994-01-10 1995-07-13 Yves Ducharme Phenyl heterocycles as cox-2 inhibitors
US5620999A (en) * 1994-07-28 1997-04-15 Weier; Richard M. Benzenesulfonamide subtituted imidazolyl compounds for the treatment of inflammation
US6426360B1 (en) * 1994-07-28 2002-07-30 G D Searle & Co. 4,5-substituted imidazolyl compounds for the treatment of inflammation
US5521213A (en) * 1994-08-29 1996-05-28 Merck Frosst Canada, Inc. Diaryl bicyclic heterocycles as inhibitors of cyclooxygenase-2
US5585504A (en) * 1994-09-16 1996-12-17 Merck & Co., Inc. Process of making cox-2 inhibitors having a lactone bridge
US5696143A (en) * 1994-09-20 1997-12-09 Talley; John J. Benz G! indazolyl derivatives for the treatment of inflammation
US5593994A (en) * 1994-09-29 1997-01-14 The Dupont Merck Pharmaceutical Company Prostaglandin synthase inhibitors
GB2294879A (en) * 1994-10-19 1996-05-15 Merck & Co Inc Cylcooxygenase-2 Inhibitors
US5739166A (en) * 1994-11-29 1998-04-14 G.D. Searle & Co. Substituted terphenyl compounds for the treatment of inflammation
JP2636819B2 (ja) 1994-12-20 1997-07-30 日本たばこ産業株式会社 オキサゾール系複素環式芳香族化合物
DE69529690T2 (de) * 1994-12-21 2003-11-13 Merck Frosst Canada Inc Diaryl-2(5h)-fuaranone als cox-2-inhibitoren
US5571825A (en) * 1995-03-31 1996-11-05 Warner-Lambert Company Method of selectively inhibiting prostaglandin G/H synthase-2
US5691374A (en) * 1995-05-18 1997-11-25 Merck Frosst Canada Inc. Diaryl-5-oxygenated-2-(5H) -furanones as COX-2 inhibitors
US6512121B2 (en) 1998-09-14 2003-01-28 G.D. Searle & Co. Heterocyclo substituted hydroxamic acid derivatives as cyclooxygenase-2 and 5-lipoxygenase inhibitors
CA2223154A1 (en) 1995-06-02 1996-12-05 G.D. Searle & Co. Heterocyclo substituted hydroxamic acid derivatives as cyclooxygenase-2 and 5-lipoxygenase inhibitors
US5643933A (en) * 1995-06-02 1997-07-01 G. D. Searle & Co. Substituted sulfonylphenylheterocycles as cyclooxygenase-2 and 5-lipoxygenase inhibitors
US6515014B2 (en) 1995-06-02 2003-02-04 G. D. Searle & Co. Thiophene substituted hydroxamic acid derivatives as cyclooxygenase-2 and 5-lipoxygenase inhibitors
JPH11507669A (ja) * 1995-06-12 1999-07-06 ジー．ディー．サール アンド カンパニー シクロオキシゲナーゼ−２インヒビターとロイコトリエンｂ▲下４▼受容体アンタゴニストの組合せによる炎症と炎症関連疾患の治療
JPH11507670A (ja) * 1995-06-12 1999-07-06 ジー．ディー．サール アンド カンパニー シクロオキシゲナーゼ−２インヒビターと５−リポキシゲナーゼインヒビターの組合せによる炎症と炎症関連疾患の治療
US5700816A (en) * 1995-06-12 1997-12-23 Isakson; Peter C. Treatment of inflammation and inflammation-related disorders with a combination of a cyclooxygenase-2 inhibitor and a leukotriene A4 hydrolase inhibitor
US6593361B2 (en) 1995-07-19 2003-07-15 Merck & Co Inc Method of treating colonic adenomas
US5968974A (en) 1995-07-19 1999-10-19 Merck & Co., Inc. Method of treating colonic adenomas
US5792778A (en) * 1995-08-10 1998-08-11 Merck & Co., Inc. 2-substituted aryl pyrroles, compositions containing such compounds and methods of use
US5837719A (en) * 1995-08-10 1998-11-17 Merck & Co., Inc. 2,5-substituted aryl pyrroles, compositions containing such compounds and methods of use
JP2000510816A (ja) * 1995-10-17 2000-08-22 ジー．ディー．サール アンド カンパニー シクロオキシゲナーゼ−２の検出法
ES2169351T3 (es) 1996-02-13 2002-07-01 Searle & Co Combinaciones que tienen efectos inmunosupresores, que contienen inhibidores de ciclooxigenasa-2 y 5-lipoxigenasa.
DK0880363T3 (da) 1996-02-13 2003-01-20 Searle & Co Kombinationer der omfatter en cyclooxygenase-2 hæmmer samt en leukotrien A4 hydrolasehæmmer, som har immunsuppressive virkninger
ATE296114T1 (de) 1996-02-13 2005-06-15 Searle & Co Zubereitungen, enthaltend einen cyclooxygenase-2- inhibitor und einen leukotrien-b4-rezeptor- antagonisten
JP3338876B2 (ja) * 1996-03-28 2002-10-28 住友精化株式会社 α−ハロアセトフェノン誘導体の製造方法
FR2747123B1 (fr) * 1996-04-04 1998-06-26 Union Pharma Scient Appl Nouveaux derives diarylmethylidene tetrahydrofurane, leurs procedes de preparation, et leurs utilisations en therapeutique
US6180651B1 (en) 1996-04-04 2001-01-30 Bristol-Myers Squibb Diarylmethylidenefuran derivatives, processes for their preparation and their uses in therapeutics
US5807873A (en) * 1996-04-04 1998-09-15 Laboratories Upsa Diarylmethylidenefuran derivatives and their uses in therapeutics
US5908858A (en) * 1996-04-05 1999-06-01 Sankyo Company, Limited 1,2-diphenylpyrrole derivatives, their preparation and their therapeutic uses
TR199802049T2 (xx) 1996-04-12 1999-01-18 G.D.Searle & Co. COX-2 Inhibit�rlerinin �nilac� olarak s�bstit�e edilmi� benzens�lfonamid t�revleri.
US6677364B2 (en) 1998-04-20 2004-01-13 G.D. Searle & Co. Substituted sulfonylphenylheterocycles as cyclooxygenase-2 and 5-lipoxygenase inhibitors
US5883267A (en) * 1996-05-31 1999-03-16 Merck & Co., Inc. Process for making phenyl heterocycles useful as cox-2 inhibitors
HRP970289A2 (en) * 1996-05-31 1998-04-30 Merck & Co Inc Process for preparing phenyl heterocycles useful as cox-2 inhibitors
KR100483736B1 (ko) * 1996-07-03 2007-03-30 머크 앤드 캄파니 인코포레이티드 사이클로옥시게나제-2억제제로서유용한페닐헤테로사이클의제조방법
GB9615867D0 (en) * 1996-07-03 1996-09-11 Merck & Co Inc Process of preparing phenyl heterocycles useful as cox-2 inhibitors
DE69729946T2 (de) 1996-10-15 2005-01-20 G.D. Searle Llc Verwendung von cyclooxygenase-2 inhibitoren zur behandlung und verbeugung von neoplasia
US5776954A (en) * 1996-10-30 1998-07-07 Merck & Co., Inc. Substituted pyridyl pyrroles, compositions containing such compounds and methods of use
UA70294C2 (en) * 1996-11-19 2004-10-15 Use of cyclooxygenase-2 inhibitors as anti-angiogeuse of cyclooxygenase-2 inhibitors as anti-angiogenic agents nic agents
PT946507E (pt) * 1996-12-10 2004-02-27 Searle & Co Compostos de pirrolilo substituidos para o tratamento da inflamacao
US6034089A (en) * 1997-10-03 2000-03-07 Merck & Co., Inc. Aryl thiophene derivatives as PDE IV inhibitors
US6025353A (en) * 1997-11-19 2000-02-15 G.D. Searle & Co. Method of using cyclooxygenase-2 inhibitors as anti-angiogenic agents
NZ333399A (en) 1997-12-24 2000-05-26 Sankyo Co Cyclooxygenase-2 inhibitors (COX-2) for the prevention and treatment of tumors, cachexia and tumor-metastasis
US6180629B1 (en) 1998-08-14 2001-01-30 Cell Pathways, Inc. [4,5]-Fused-1,3-disubstituted-1,2-diazine-6-one derivatives with nitrogen containing substitutents in position one for the treatment of neoplasia
US6649645B1 (en) 1998-12-23 2003-11-18 Pharmacia Corporation Combination therapy of radiation and a COX-2 inhibitor for treatment of neoplasia
US7122666B2 (en) 1999-07-21 2006-10-17 Sankyo Company, Limited Heteroaryl-substituted pyrrole derivatives, their preparation and their therapeutic uses
WO2001045703A1 (en) 1999-12-23 2001-06-28 Nitromed, Inc. Nitrosated and nitrosylated cyclooxygenase-2 inhibitors, compositions and methods of use
DE10001166A1 (de) 2000-01-13 2001-07-19 Merckle Gmbh Anellierte Pyrrolverbindungen, diese enthaltende pharmazeutische Mittel und deren Verwendung
JP2003531202A (ja) * 2000-04-25 2003-10-21 ファルマシア・コーポレーション ３，４−ジ（カルボシクリルまたはヘテロシクリル）チオフェンの位置選択的合成
JP2004510705A (ja) 2000-07-20 2004-04-08 ラウラス　エイエス 方法
US6716829B2 (en) 2000-07-27 2004-04-06 Pharmacia Corporation Aldosterone antagonist and cyclooxygenase-2 inhibitor combination therapy to prevent or treat inflammation-related cardiovascular disorders
EP1377290B1 (en) 2001-01-26 2006-10-04 Chugai Seiyaku Kabushiki Kaisha Malonyl-coa decarboxylase inhibitors useful as metabolic modulators
WO2002058698A2 (en) 2001-01-26 2002-08-01 Chugai Seiyaku Kabushiki Kaisha Malonyl-coa decarboxylase inhibitors useful as metabolic modulators
EP1353662B1 (en) 2001-01-26 2007-04-18 Chugai Seiyaku Kabushiki Kaisha Methods for the treatment of diseases using malonyl-coa decarbox ylase inhibitors
US7709510B2 (en) 2001-02-20 2010-05-04 Chugai Seiyaku Kabushiki Kaisha Azoles as malonyl-CoA decarboxylase inhibitors useful as metabolic modulators
WO2002066035A2 (en) 2001-02-20 2002-08-29 Chugai Seiyaku Kabushiki Kaisha Azoles as malonyl-coa decarboxylase inhibitors useful as metabolic modulators
US7695736B2 (en) 2001-04-03 2010-04-13 Pfizer Inc. Reconstitutable parenteral composition
US20030105144A1 (en) 2001-04-17 2003-06-05 Ping Gao Stabilized oral pharmaceutical composition
US6673818B2 (en) 2001-04-20 2004-01-06 Pharmacia Corporation Fluoro-substituted benzenesulfonyl compounds for the treatment of inflammation
AR038957A1 (es) 2001-08-15 2005-02-02 Pharmacia Corp Terapia de combinacion para el tratamiento del cancer
ATE424388T1 (de) 2001-12-06 2009-03-15 Merck & Co Inc Mitotische kinesinhemmer
US7329401B2 (en) 2002-04-15 2008-02-12 The Regents Of The University Of California Cyclooxygenase-2 selective agents useful as imaging probes and related methods
US7211598B2 (en) 2002-06-28 2007-05-01 Nitromed, Inc. Oxime and/or hydrozone containing nitrosated and/or nitrosylated cyclooxygenase-2 selective inhibitors, compositions and methods of use
KR20090118994A (ko) 2002-12-13 2009-11-18 워너-램버트 캄파니 엘엘씨 하부요로증상을 치료하기 위한 알파-2-델타 리간드
US7772188B2 (en) 2003-01-28 2010-08-10 Ironwood Pharmaceuticals, Inc. Methods and compositions for the treatment of gastrointestinal disorders
US7790724B2 (en) 2003-04-25 2010-09-07 Janssen Pharmaceutica N.V. c-fms kinase inhibitors
US20050113566A1 (en) * 2003-04-25 2005-05-26 Player Mark R. Inhibitors of C-FMS kinase
MXPA05011503A (es) * 2003-04-25 2006-05-31 Johnson & Johnson Inhibidores de la c-fms cinasa.
US7427683B2 (en) * 2003-04-25 2008-09-23 Ortho-Mcneil Pharmaceutical, Inc. c-fms kinase inhibitors
ES2275218T3 (es) 2003-05-07 2007-06-01 Osteologix A/S Sales de estroncio hidrosolubles para el tratamiento de afecciones de cartilagos y/o huesos.
ATE375810T1 (de) 2003-08-01 2007-11-15 Chugai Pharmaceutical Co Ltd Cyanoamid-verbindungen als nützliche malonyl-coa decarboxylase-hemmer
ES2353306T3 (es) 2003-08-01 2011-03-01 Chugai Seiyaku Kabushiki Kaisha Compuestos heterocíclicos útiles como inhibidores de la malonil-coa-descarboxilasa.
ES2378418T3 (es) 2003-08-01 2012-04-12 Chugai Seiyaku Kabushiki Kaisha Compuestos de azol basados en cianoguanidina útiles como inhibidores de malonil-coadescarboxilasa
DE602004014937D1 (de) 2003-08-01 2008-08-21 Chugai Pharmaceutical Co Ltd Piperidin-verbindungen als malonyl-coa decarboxylase-hemmer
US7067159B2 (en) 2003-12-05 2006-06-27 New Chapter, Inc. Methods for treating prostate cancer with herbal compositions
US7070816B2 (en) 2003-12-05 2006-07-04 New Chapter, Inc. Methods for treating prostatic intraepithelial neoplasia with herbal compositions
KR101347830B1 (ko) 2004-05-23 2014-01-07 에이치엠아이, 인코포레이티드 테라뮤틴 조절물질
RU2007103816A (ru) 2004-07-01 2008-08-10 Мерк энд Ко., Инк. (US) Ингибиторы митотического кинезина
US7622142B2 (en) 2004-09-14 2009-11-24 New Chapter Inc. Methods for treating glioblastoma with herbal compositions
WO2006100557A1 (en) 2005-03-21 2006-09-28 Pfizer Limited Substituted triazole derivatives as oxytocin antagonists
ATE550019T1 (de) 2005-05-17 2012-04-15 Merck Sharp & Dohme Cis-4-ä(4-chlorophenyl)sulfonylü-4-(2,5- difluorophenyl)cyclohexanepropansäure zur behandlug von krebs
US8431110B2 (en) 2005-05-23 2013-04-30 Hmi Medical Innovations, Llc. Compounds and method of identifying, synthesizing, optimizing and profiling protein modulators
US20090062302A1 (en) 2006-01-24 2009-03-05 Buser-Doepner Carolyn A Jak2 Tyrosine Kinase Inhibition
GB0603041D0 (en) 2006-02-15 2006-03-29 Angeletti P Ist Richerche Bio Therapeutic compounds
EP2010528B1 (en) 2006-04-19 2017-10-04 Novartis AG 6-o-substituted benzoxazole and benzothiazole compounds and methods of inhibiting csf-1r signaling
US8173629B2 (en) 2006-09-22 2012-05-08 Merck Sharp & Dohme Corp. Method of treatment using fatty acid synthesis inhibitors
US20110218176A1 (en) 2006-11-01 2011-09-08 Barbara Brooke Jennings-Spring Compounds, methods, and treatments for abnormal signaling pathways for prenatal and postnatal development
UA94979C2 (uk) 2006-12-22 2011-06-25 Рекордати Айеленд Лимитед КОМБІНОВАНА ТЕРАПІЯ ПОРУШЕНЬ НИЖНІХ СЕЧОВИВІДНИХ ШЛЯХІВ ЛІГАНДАМИ α2δ І НПЗП
RS58936B1 (sr) 2007-01-10 2019-08-30 Msd Italia Srl Indazoli supstituisani amidom kao inhibitori poli(adp-riboza)polimeraze (parp)
JP2010516679A (ja) * 2007-01-19 2010-05-20 マリンクロット インコーポレイテッド 診断用および治療用シクロオキシゲナーゼ−２結合リガンド
CA2679659C (en) 2007-03-01 2016-01-19 Novartis Ag Pim kinase inhibitors and methods of their use
EP2152700B1 (en) 2007-05-21 2013-12-11 Novartis AG Csf-1r inhibitors, compositions, and methods of use
JP2008303173A (ja) * 2007-06-07 2008-12-18 Daicel Chem Ind Ltd チオジグリコール酸ジメチルの製造方法
US8389553B2 (en) 2007-06-27 2013-03-05 Merck Sharp & Dohme Corp. 4-carboxybenzylamino derivatives as histone deacetylase inhibitors
MX2010002712A (es) 2007-09-10 2010-06-09 Calcimedica Inc Compuestos que modulan calcio intracelular.
US8598184B2 (en) 2008-03-03 2013-12-03 Tiger Pharmatech Protein kinase inhibitors
EP2321303B1 (en) 2008-08-27 2019-11-27 Calcimedica, Inc. Compounds that modulate intracellular calcium
CN101429189B (zh) * 2008-12-24 2014-07-23 沈阳药科大学 2，3-二取代芳基噻吩类衍生物及其用途
CN104945382B (zh) 2009-10-14 2020-02-07 默沙东公司 提高p53活性的取代的哌啶和其用途
CA2797533A1 (en) 2010-04-27 2011-11-10 Calcimedica, Inc. Compounds that modulate intracellular calcium
ES2591004T3 (es) 2010-04-27 2016-11-24 Calcimedica, Inc. Compuestos moduladores del calcio intracelular
WO2011163330A1 (en) 2010-06-24 2011-12-29 Merck Sharp & Dohme Corp. Novel heterocyclic compounds as erk inhibitors
WO2012018754A2 (en) 2010-08-02 2012-02-09 Merck Sharp & Dohme Corp. RNA INTERFERENCE MEDIATED INHIBITION OF CATENIN (CADHERIN-ASSOCIATED PROTEIN), BETA 1 (CTNNB1) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA)
US9029341B2 (en) 2010-08-17 2015-05-12 Sirna Therapeutics, Inc. RNA interference mediated inhibition of hepatitis B virus (HBV) gene expression using short interfering nucleic acid (siNA)
EP2608669B1 (en) 2010-08-23 2016-06-22 Merck Sharp & Dohme Corp. NOVEL PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVES AS mTOR INHIBITORS
EP2609095A4 (en) 2010-08-27 2014-06-18 Calcimedica Inc COMPOUNDS MODULATING INTRACELLULAR CALCIUM
EP2613782B1 (en) 2010-09-01 2016-11-02 Merck Sharp & Dohme Corp. Indazole derivatives useful as erk inhibitors
US9242981B2 (en) 2010-09-16 2016-01-26 Merck Sharp & Dohme Corp. Fused pyrazole derivatives as novel ERK inhibitors
US9260471B2 (en) 2010-10-29 2016-02-16 Sirna Therapeutics, Inc. RNA interference mediated inhibition of gene expression using short interfering nucleic acids (siNA)
WO2012087772A1 (en) 2010-12-21 2012-06-28 Schering Corporation Indazole derivatives useful as erk inhibitors
US20140045847A1 (en) 2011-04-21 2014-02-13 Piramal Enterprises Limited Crystalline form of a salt of a morpholino sulfonyl indole derivative and a process for its preparation
EP2770987B1 (en) 2011-10-27 2018-04-04 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
US9221809B2 (en) 2011-10-31 2015-12-29 Merck Sharp & Dohme Corp. Aminopyrimidinones as interleukin receptor-associated kinase inhibitors
EP3453762B1 (en) 2012-05-02 2021-04-21 Sirna Therapeutics, Inc. Short interfering nucleic acid (sina) compositions
MX2015004041A (es) 2012-09-28 2015-07-06 Merck Sharp & Dohme Compuestos novedosos que son inhibidores de erk.
WO2014059333A1 (en) 2012-10-12 2014-04-17 Calcimedica, Inc. Compounds that modulate intracellular calcium
WO2014085216A1 (en) 2012-11-28 2014-06-05 Merck Sharp & Dohme Corp. Compositions and methods for treating cancer
CA2895504A1 (en) 2012-12-20 2014-06-26 Merck Sharp & Dohme Corp. Substituted imidazopyridines as hdm2 inhibitors
EP2951180B1 (en) 2013-01-30 2018-05-02 Merck Sharp & Dohme Corp. 2,6,7,8 substituted purines as hdm2 inhibitors
WO2015006181A1 (en) 2013-07-11 2015-01-15 Merck Sharp & Dohme Corp. Substituted amidopyrazole inhibitors of interleukin receptor-associated kinases (irak-4)
EP3041938A1 (en) 2013-09-03 2016-07-13 Moderna Therapeutics, Inc. Circular polynucleotides
US9611263B2 (en) 2013-10-08 2017-04-04 Calcimedica, Inc. Compounds that modulate intracellular calcium
JO3589B1 (ar) 2014-08-06 2020-07-05 Novartis Ag مثبطات كيناز البروتين c وطرق استخداماتها
EP3267996B1 (en) 2015-03-12 2020-11-11 Merck Sharp & Dohme Corp. Pyrazolopyrimidine inhibitors of irak4 activity
US10040802B2 (en) 2015-03-12 2018-08-07 Merck Sharp & Dohme Corp. Thienopyrazine inhibitors of IRAK4 activity
EP3268367B8 (en) 2015-03-12 2022-11-16 Merck Sharp & Dohme LLC Carboxamide inhibitors of irak4 activity
EP3292213A1 (en) 2015-05-04 2018-03-14 Academisch Medisch Centrum Biomarkers for the detection of aspirin insensitivity
WO2018201146A1 (en) 2017-04-28 2018-11-01 Case Western Reserve University Compounds and methods of treating retinal degeneration
WO2019094311A1 (en) 2017-11-08 2019-05-16 Merck Sharp & Dohme Corp. Prmt5 inhibitors
US11981701B2 (en) 2018-08-07 2024-05-14 Merck Sharp & Dohme Llc PRMT5 inhibitors
EP3833668A4 (en) 2018-08-07 2022-05-11 Merck Sharp & Dohme Corp. PRMT5 INHIBITORS
JP2023507634A (ja) 2019-12-17 2023-02-24 メルク・シャープ・アンド・ドーム・エルエルシー Ｐｒｍｔ５阻害剤
CN114507251B (zh) * 2022-01-15 2023-08-22 南方科技大学 一种双硅中心手性杂芳基硅烷及其制备方法

Family Cites Families (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CH423473A (de) * 1963-01-19 1966-10-31 Ciba Geigy Verfahren zur Herstellung eines photographischen Farbenbildes unter Verwendung neuer Thiophenverbindungen als Farbstoffbildner für Purpurfarbstoffe
US3507648A (en) 1966-06-06 1970-04-21 Eastman Kodak Co 2(5h)-furanone dyes as sensitizers for organic photoconductors
US3743656A (en) * 1969-05-01 1973-07-03 Wyeth John & Brother Ltd Thiophene and furan lower alkanoic acids and derivatives
US3661899A (en) 1970-06-01 1972-05-09 Eastman Kodak Co 2(5h)-furanone compounds
JPS4891061A (es) * 1972-03-10 1973-11-27
JPS4891058A (es) * 1972-03-10 1973-11-27
JPS5127743B2 (es) 1973-05-25 1976-08-14
JPS50121261A (es) * 1974-03-12 1975-09-23
DE2817449A1 (de) 1978-04-21 1979-10-31 Bayer Ag Mittel zur regulierung des pflanzenwachstums
US4302461A (en) * 1979-08-09 1981-11-24 E. I. Du Pont De Nemours And Company Antiinflammatory 5-substituted-2,3-diarylthiophenes
US4381311A (en) * 1980-12-29 1983-04-26 E. I. Du Pont De Nemours And Company Antiinflammatory 4,5-diaryl-α-(polyhalomethyl)-2-thiophenemethanols
US4427693A (en) * 1981-08-05 1984-01-24 E. I. Du Pont De Nemours And Company Antiinflammatory 4,5-diaryl-α,α-bis (polyhalomethyl)-2-thiophenemethanamines
EP0087629B1 (en) * 1982-03-03 1986-01-15 E.I. Du Pont De Nemours And Company Antiinflammatory and/or analgesic 2,3-diaryl-5-halo thiophenes
US4432974A (en) * 1982-03-04 1984-02-21 E. I. Du Pont De Nemours And Company Antiinflammatory and/or analgesic 2,3-diaryl-5-silyl thiophenes
DE3817808A1 (de) * 1987-07-21 1989-02-02 Bayer Ag Verfahren zur herstellung von 2-substituierten pyrrolen
DE3739882A1 (de) * 1987-11-25 1989-06-08 Bayer Ag Substituierte hydroxylamine
DE3816120A1 (de) 1988-05-11 1989-11-23 Bayer Ag Verfahren zur herstellung von unsymmetrischen biarylverbindungen
US5196532A (en) 1989-02-08 1993-03-23 Basf Aktiengesellschaft Diaryl-substituted heterocyclic compounds, their preparation and drugs and cosmetics obtained therefrom
DE3903993A1 (de) * 1989-02-10 1990-08-16 Basf Ag Diarylsubstituierte heterocyclische verbindungen, ihre herstellung und arzneimittel daraus
DE3915450A1 (de) * 1989-05-11 1990-11-15 Gerd Prof Dr Dannhardt Substituierte pyrrolverbindungen und deren anwendung in der pharmazie
JPH04279672A (ja) * 1991-03-06 1992-10-05 Mita Ind Co Ltd フェニレンジアミン系化合物およびそれを用いた電子写真感光体
CA2152792C (en) 1993-01-15 2000-02-15 Stephen R. Bertenshaw Novel 3,4-diaryl thiophenes and analogs thereof having use as antiinflammatory agents
CA2161789A1 (en) * 1993-05-13 1994-11-24 Jacques Yves Gauthier 2-substituted-3,4-diarylthiophene derivatives as inhibitors of cyclooxygenase
US5474995A (en) 1993-06-24 1995-12-12 Merck Frosst Canada, Inc. Phenyl heterocycles as cox-2 inhibitors

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ATE160345T1 (de) 1997-12-15
GR3025762T3 (en) 1998-03-31
CA2243199A1 (en) 1994-07-21
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DE69406903D1 (de) 1998-01-02
DE9422447U1 (de) 2002-10-17
CA2152792A1 (en) 1994-07-21
JP3137648B2 (ja) 2001-02-26
EP0679157A1 (en) 1995-11-02
CA2152792C (en) 2000-02-15
CA2243199C (en) 2005-08-02
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EP0764644A1 (en) 1997-03-26
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CA2293952A1 (en) 1994-07-21
EP0764645A1 (en) 1997-03-26
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US7012094B1 (en) 2006-03-14
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