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DE69830404D1 - P38-inhibitoren - Google Patents

P38-inhibitoren

Info

Publication number
DE69830404D1
DE69830404D1 DE69830404T DE69830404T DE69830404D1 DE 69830404 D1 DE69830404 D1 DE 69830404D1 DE 69830404 T DE69830404 T DE 69830404T DE 69830404 T DE69830404 T DE 69830404T DE 69830404 D1 DE69830404 D1 DE 69830404D1
Authority
DE
Germany
Prior art keywords
inhibitors
methods
relates
prevention
producing
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 - Fee Related
Application number
DE69830404T
Other languages
English (en)
Other versions
DE69830404T2 (de
Inventor
Gerald Salituro
W Bemis
Jeremy Green
L Kofron
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.)
Vertex Pharmaceuticals Inc
Original Assignee
Vertex Pharmaceuticals Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Vertex Pharmaceuticals Inc filed Critical Vertex Pharmaceuticals Inc
Publication of DE69830404D1 publication Critical patent/DE69830404D1/de
Application granted granted Critical
Publication of DE69830404T2 publication Critical patent/DE69830404T2/de
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D319/00—Heterocyclic compounds containing six-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D319/10—1,4-Dioxanes; Hydrogenated 1,4-dioxanes
    • C07D319/14—1,4-Dioxanes; Hydrogenated 1,4-dioxanes condensed with carbocyclic rings or ring systems
    • C07D319/16—1,4-Dioxanes; Hydrogenated 1,4-dioxanes condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D319/18—Ethylenedioxybenzenes, not substituted on the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C275/00—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C275/28—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C275/00—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C275/28—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C275/30—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by halogen atoms, or by nitro or nitroso groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C275/00—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C275/28—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C275/32—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by singly-bound oxygen atoms
    • C07C275/34—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by singly-bound oxygen atoms having nitrogen atoms of urea groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C275/00—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C275/28—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C275/38—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by doubly-bound oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C275/00—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C275/28—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C275/40—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by nitrogen atoms not being part of nitro or nitroso groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C275/00—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C275/28—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C275/42—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by carboxyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/30—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/45—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups at least one of the singly-bound nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom, e.g. N-acylaminosulfonamides
    • C07C311/47—Y being a hetero atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen 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
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen 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
    • C07D215/38—Nitrogen atoms
    • C07D215/40—Nitrogen atoms attached in position 8
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
    • C07D277/64—Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
    • C07D277/68—Benzothiazoles 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 in position 2
    • C07D277/82—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
    • C07D295/135—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • 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
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/91—Dibenzofurans; Hydrogenated dibenzofurans
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D317/00—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/44—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D317/46—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D317/48—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring
    • C07D317/62—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring 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 atoms of the carbocyclic ring
    • C07D317/66—Nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2602/00—Systems containing two condensed rings
    • C07C2602/02—Systems containing two condensed rings the rings having only two atoms in common
    • C07C2602/04—One of the condensed rings being a six-membered aromatic ring
    • C07C2602/08—One of the condensed rings being a six-membered aromatic ring the other ring being five-membered, e.g. indane

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
DE69830404T 1997-06-27 1998-06-29 P38-inhibitoren Expired - Fee Related DE69830404T2 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US08/884,160 US6093742A (en) 1997-06-27 1997-06-27 Inhibitors of p38
US884160 1997-06-27
PCT/US1998/013496 WO1999000357A1 (en) 1997-06-27 1998-06-29 INHIBITORS OF p38

Publications (2)

Publication Number Publication Date
DE69830404D1 true DE69830404D1 (de) 2005-07-07
DE69830404T2 DE69830404T2 (de) 2006-01-26

Family

ID=25384090

Family Applications (1)

Application Number Title Priority Date Filing Date
DE69830404T Expired - Fee Related DE69830404T2 (de) 1997-06-27 1998-06-29 P38-inhibitoren

Country Status (8)

Country Link
US (1) US6093742A (de)
EP (1) EP0993441B1 (de)
AT (1) ATE296799T1 (de)
AU (1) AU8377698A (de)
CA (1) CA2294463A1 (de)
DE (1) DE69830404T2 (de)
ES (1) ES2244071T3 (de)
WO (1) WO1999000357A1 (de)

Families Citing this family (144)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6608060B1 (en) * 1996-12-18 2003-08-19 Vertex Pharmaceuticals Incorporated Inhibitors of p38
US6187799B1 (en) 1997-05-23 2001-02-13 Onyx Pharmaceuticals Inhibition of raf kinase activity using aryl ureas
CA2294057A1 (en) 1997-06-13 1998-12-17 Smithkline Beecham Corporation Novel pyrazole and pyrazoline substituted compounds
DE69829412T2 (de) * 1997-12-22 2005-07-28 Bayer Pharmaceuticals Corp., West Haven Hemmung der raf-kinase unter verwendung von symmetrisch und unsymmetrisch substituierten harnstoffen
US7329670B1 (en) 1997-12-22 2008-02-12 Bayer Pharmaceuticals Corporation Inhibition of RAF kinase using aryl and heteroaryl substituted heterocyclic ureas
US20080300281A1 (en) * 1997-12-22 2008-12-04 Jacques Dumas Inhibition of p38 Kinase Activity Using Aryl and Heteroaryl Substituted Heterocyclic Ureas
US7517880B2 (en) 1997-12-22 2009-04-14 Bayer Pharmaceuticals Corporation Inhibition of p38 kinase using symmetrical and unsymmetrical diphenyl ureas
WO1999061039A2 (en) * 1998-05-22 1999-12-02 MAX-PLANCK-Gesellschaft zur Förderung der Wissenschaften e.V. Novel composition for modulating ischemic cell death
US6867209B1 (en) 1998-05-22 2005-03-15 Scios, Inc. Indole-type derivatives as inhibitors of p38 kinase
US6858617B2 (en) 1998-05-26 2005-02-22 Smithkline Beecham Corporation Substituted imidazole compounds
NZ510098A (en) * 1998-10-22 2003-09-26 Neurosearch As Substituted phenyl derivatives, pharmaceuticals thereof and their use as blockers of the chloride channel
JP2002528506A (ja) 1998-11-04 2002-09-03 スミスクライン・ビーチャム・コーポレイション ピリジン−４−イルまたはピリミジン−４−イル置換ピラジン
US6326391B1 (en) * 1998-12-04 2001-12-04 Influx, Inc. Inhibitors of multidrug transporters
WO2000035455A1 (en) * 1998-12-15 2000-06-22 Telik, Inc. Heteroaryl-aryl ureas as igf-1 receptor antagonists
US20080269265A1 (en) * 1998-12-22 2008-10-30 Scott Miller Inhibition Of Raf Kinase Using Symmetrical And Unsymmetrical Substituted Diphenyl Ureas
EP1140840B1 (de) 1999-01-13 2006-03-22 Bayer Pharmaceuticals Corp. -g(v)-carboxyaryl substituierte diphenyl harnstoffe als raf kinase inhibitoren
US8124630B2 (en) 1999-01-13 2012-02-28 Bayer Healthcare Llc ω-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
US7928239B2 (en) 1999-01-13 2011-04-19 Bayer Healthcare Llc Inhibition of RAF kinase using quinolyl, isoquinolyl or pyridyl ureas
US20020065296A1 (en) * 1999-01-13 2002-05-30 Bayer Corporation Heteroaryl ureas containing nitrogen hetero-atoms as p38 kinase inhibitors
ME00275B (me) * 1999-01-13 2011-02-10 Bayer Corp ω-KARBOKSIARIL SUPSTITUISANI DIFENIL KARBAMIDI KAO INHIBITORI RAF KINAZE
JP2002534468A (ja) 1999-01-13 2002-10-15 バイエル コーポレイション ｐ３８キナーゼ阻害剤としてのω−カルボキシアリール置換ジフェニル尿素
UA73492C2 (en) 1999-01-19 2005-08-15 Aromatic heterocyclic compounds as antiinflammatory agents
JP2002537397A (ja) 1999-02-22 2002-11-05 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド 抗炎症剤としての多環ヘテロ環式誘導体
WO2000055152A1 (en) 1999-03-12 2000-09-21 Boehringer Ingelheim Pharmaceuticals, Inc. Aromatic heterocyclic compounds as anti-inflammatory agents
CN1156452C (zh) 1999-03-12 2004-07-07 贝林格尔·英格海姆药物公司 作为消炎剂的化合物
JP2000281588A (ja) * 1999-03-30 2000-10-10 Sankyo Co Ltd ガンの予防又は治療薬及びそのスクリーニング方法
US7125875B2 (en) 1999-04-15 2006-10-24 Bristol-Myers Squibb Company Cyclic protein tyrosine kinase inhibitors
ES2391550T3 (es) 1999-04-15 2012-11-27 Bristol-Myers Squibb Company Inhibidores cíclicos de la proteína tirosina quinasa
CA2372567A1 (en) * 1999-05-21 2000-11-30 Scios Inc. Indole-type derivatives as inhibitors of p38 kinase
IL146309A (en) 1999-05-21 2008-03-20 Scios Inc Derivatives of the indole type and pharmaceutical preparations containing them as inhibitors of kinase p38
US6365617B1 (en) 1999-06-29 2002-04-02 Ortho-Mcneil Pharmaceutical, Inc. Indole and indazole urea-peptoids as thrombin receptor antagonists
US6630451B1 (en) 1999-06-29 2003-10-07 Orthomcneil Pharmaceutical, Inc. Benzimidazolone peptidometics as thrombin receptor antagonist
US6858577B1 (en) 1999-06-29 2005-02-22 Ortho-Mcneil Pharmaceutical, Inc. Indole peptidomimetics as thrombin receptor antagonists
AU5895500A (en) 1999-06-29 2001-01-31 Cor Therapeutics, Inc. Novel indazole peptidomimetics as thrombin receptor antagonists
ATE323482T1 (de) * 1999-07-02 2006-05-15 Stuart A Lipton Verwendung von p38 mapk inhibitoren in der behandlung von augenkrankheiten
WO2001004115A2 (en) 1999-07-09 2001-01-18 Boehringer Ingelheim Pharmaceuticals, Inc. Novel process for synthesis of heteroaryl-substituted urea compounds
US6451837B1 (en) 1999-09-01 2002-09-17 Andrius Baskys Neuroprotective effects of mitogen-activated protein kinase (MAPK) cascade inhibitors
WO2001017953A1 (en) 1999-09-08 2001-03-15 Guilford Pharmaceuticals Inc. Non-peptidic cyclophilin binding compounds and their use
ATE281439T1 (de) 1999-11-23 2004-11-15 Smithkline Beecham Corp 3,4-dihydro-(1h)chinazolin-2-on-verbindungen als csbp/p38-kinase-inhibitoren
AU1782301A (en) 1999-11-23 2001-06-04 Smithkline Beecham Corporation 3,4-dihydro-(1h)quinazolin-2-one compounds as csbp/p39 kinase inhibitors
AU1783201A (en) 1999-11-23 2001-06-04 Smithkline Beecham Corporation 3,4-dihydro-(1h)quinazolin-2-one compounds as csbp/p38 kinase inhibitors
US6525046B1 (en) 2000-01-18 2003-02-25 Boehringer Ingelheim Pharmaceuticals, Inc. Aromatic heterocyclic compounds as antiinflammatory agents
US6515023B2 (en) * 2000-01-31 2003-02-04 Merck & Co., Inc. Thrombin receptor antagonists
US7217722B2 (en) * 2000-02-01 2007-05-15 Kirin Beer Kabushiki Kaisha Nitrogen-containing compounds having kinase inhibitory activity and drugs containing the same
WO2001057008A1 (en) 2000-02-07 2001-08-09 Abbott Gesellschaft Mit Beschrankter Haftung & Company Kommanditgesellschaft 2-benzothiazolyl urea derivatives and their use as protein kinase inhibitors
US6608052B2 (en) 2000-02-16 2003-08-19 Boehringer Ingelheim Pharmaceuticals, Inc. Compounds useful as anti-inflammatory agents
US7235551B2 (en) 2000-03-02 2007-06-26 Smithkline Beecham Corporation 1,5-disubstituted-3,4-dihydro-1h-pyrimido[4,5-d]pyrimidin-2-one compounds and their use in treating csbp/p38 kinase mediated diseases
US6645990B2 (en) 2000-08-15 2003-11-11 Amgen Inc. Thiazolyl urea compounds and methods of uses
DE60134679D1 (de) 2000-10-20 2008-08-14 Eisai R&D Man Co Ltd Stickstoff enthaltende aromatische Heterozyklen
WO2002038157A2 (en) * 2000-11-09 2002-05-16 The Hospital For Sick Children Inhibitors of thromboxane formation and action
WO2002058695A1 (en) 2000-12-20 2002-08-01 Merck & Co., Inc. (halo-benzo carbonyl)heterocyclo fused phenyl p38 kinase inhibiting agents
WO2002050071A1 (en) 2000-12-21 2002-06-27 Bristol-Myers Squibb Company Thiazolyl inhibitors of tec family tyrosine kinases
US7235576B1 (en) 2001-01-12 2007-06-26 Bayer Pharmaceuticals Corporation Omega-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
WO2002059080A2 (en) 2001-01-25 2002-08-01 Guilford Pharmaceuticals Inc. Trisubstituted carbocyclic cyclophilin binding compounds and their use
DE10105077A1 (de) * 2001-02-05 2002-08-08 Febit Ferrarius Biotech Gmbh Hybrid-Schutzgruppe
UA76977C2 (en) * 2001-03-02 2006-10-16 Icos Corp Aryl- and heteroaryl substituted chk1 inhibitors and their use as radiosensitizers and chemosensitizers
ES2286267T3 (es) * 2001-03-07 2007-12-01 Telik, Inc. Diarilureas sustituidas como estimuladoras de mediada por fas.
US7371763B2 (en) * 2001-04-20 2008-05-13 Bayer Pharmaceuticals Corporation Inhibition of raf kinase using quinolyl, isoquinolyl or pyridyl ureas
ATE415162T1 (de) 2001-06-11 2008-12-15 Vertex Pharma Isochinolin-inhibitoren von p38
AU2002317377A1 (en) * 2001-07-20 2003-03-03 Cancer Research Technology Limited Biphenyl apurinic/apyrimidinic site endonuclease inhibitors to treat cancer
RU2299877C2 (ru) 2001-09-18 2007-05-27 Ф.Хоффманн-Ля Рош Аг Производные алкилмочевины, обладающие свойствами ретиноидных агонистов (i), фармацевтическая композиция и лекарственное средство
CA2458266C (en) * 2001-09-18 2011-03-15 F. Hoffmann-La Roche Ag Substituted urea retinoid agonists ii
RU2316326C2 (ru) * 2001-12-03 2008-02-10 Байер Фамэсьютиклс Копэрейшн Способ и композиция для лечения ракового заболевания, тозилат и фармацевтически приемлемые соли n-(4-хлор-3-(трифторметил)фенил)-n'-(4-(2-(n-метилкарбамоил)-4-пиридилокси)фенил)мочевины
JP2003192587A (ja) * 2001-12-26 2003-07-09 Bayer Ag 尿素誘導体
PT1580188E (pt) * 2002-02-11 2012-01-25 Bayer Healthcare Llc Aril-ureias como inibidores de cinases
US20030216396A1 (en) * 2002-02-11 2003-11-20 Bayer Corporation Pyridine, quinoline, and isoquinoline N-oxides as kinase inhibitors
WO2003068223A1 (en) * 2002-02-11 2003-08-21 Bayer Corporation Aryl ureas with raf kinase and angiogenesis inhibiting activity
PT1478358E (pt) 2002-02-11 2013-09-11 Bayer Healthcare Llc Tosilato de sorafenib para o tratamento de doenças caracterizadas por angiogénese anormal
DE60319066T2 (de) 2002-02-25 2009-02-26 Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield 1,4-disubstituierte benzokondensierte cycloalkyl-harnstoffverbindungen zur behandlung von zytokinvermittelten erkrankungen
US20030236287A1 (en) * 2002-05-03 2003-12-25 Piotrowski David W. Positive allosteric modulators of the nicotinic acetylcholine receptor
PE20040522A1 (es) * 2002-05-29 2004-09-28 Novartis Ag Derivados de diarilurea dependientes de la cinasa de proteina
ES2278170T3 (es) 2002-07-09 2007-08-01 BOEHRINGER INGELHEIM PHARMA GMBH & CO.KG Composiciones farmaceuticas de anticolinergicos e inhibidores de la quinasa p38 en el tratamiento de enfermedades respiratorias.
JP2006503025A (ja) * 2002-09-05 2006-01-26 サイオス インク． ｐ３８ＭＡＰキナーゼの抑制による疼痛治療
US20080039461A1 (en) * 2002-09-05 2008-02-14 Protter Andrew A Treatment of pain by inhibition of p38 map kinase
EP1402888A1 (de) * 2002-09-18 2004-03-31 Jerini AG Verwendung von substituierte carbozyclische Verbindungen als rotamase inhibitoren
EA200500846A1 (ru) * 2002-11-19 2005-12-29 Ачиллион Фармасьютикалз, Инк. Замещенные арилтиомочевины и родственные соединения; ингибиторы вирусной репликации
ES2327834T3 (es) 2002-11-21 2009-11-04 Neurosearch A/S Derivados de diarilureido y su uso medico.
WO2004050023A2 (en) * 2002-11-27 2004-06-17 Dmi Biosciences, Inc. Treatment of diseases and conditions mediated by increased phosphorylation
CL2004000366A1 (es) * 2003-02-26 2005-01-07 Pharmacia Corp Sa Organizada B USO DE UNA COMBINACION DE UN COMPUESTO DERIVADO DE PIRAZOL INHIBIDOR DE QUINASA p38, Y UN INHIBIDOR DE ACE PARA TRATAR DISFUNCION RENAL, ENFERMEDAD CARDIOVASCULAR Y VASCULAR, RETINOPATIA, NEUROPATIA, EDEMA, DISFUNCION ENDOTELIAL O INSULINOPATIA.
UY28213A1 (es) 2003-02-28 2004-09-30 Bayer Pharmaceuticals Corp Nuevos derivados de cianopiridina útiles en el tratamiento de cáncer y otros trastornos.
RU2357957C2 (ru) * 2003-03-03 2009-06-10 Эррэй Биофарма, Инк. Ингибиторы р38 и способы их применения
US7135575B2 (en) * 2003-03-03 2006-11-14 Array Biopharma, Inc. P38 inhibitors and methods of use thereof
EP1611128A2 (de) * 2003-03-28 2006-01-04 Pharmacia & Upjohn Company LLC Positive allosterische modulatoren des nikotinischen acetylcholin-rezeptors
DK1636585T3 (da) 2003-05-20 2008-05-26 Bayer Pharmaceuticals Corp Diarylurinstoffer med kinasehæmmende aktivitet
US7297709B2 (en) 2003-05-22 2007-11-20 Abbott Laboratories Indazole, benzisoxazole, and benzisothiazole kinase inhibitors
PT1663978E (pt) 2003-07-23 2008-02-15 Bayer Pharmaceuticals Corp Omega-carboxiaril difenil ureia substituída por flúor para o tratamento e a prevenção de doenças e estados patológicos
GB0322016D0 (en) * 2003-09-19 2003-10-22 Merck Sharp & Dohme New compounds
JP4303726B2 (ja) 2003-11-11 2009-07-29 エーザイ・アール・アンド・ディー・マネジメント株式会社 ウレア誘導体およびその製造方法
TW200530236A (en) 2004-02-23 2005-09-16 Chugai Pharmaceutical Co Ltd Heteroaryl phenylurea
US7454007B2 (en) * 2004-03-26 2008-11-18 Samsung Electronics Co., Ltd. Telecommunication switch using generic API to support multiple protocol-specific signal control functions
MXPA06012394A (es) * 2004-04-30 2007-01-31 Bayer Pharmaceuticals Corp Derivados de pirazolilurea sustituidos utiles en el tratamiento de cancer.
DE602005019874D1 (de) * 2004-05-12 2010-04-22 Bristol Myers Squibb Co Für die behandlung von thrombotischen leiden geeignete harnstoffantagonisten des p2y1-rezeptors
TW200600492A (en) * 2004-05-18 2006-01-01 Achillion Pharmaceuticals Inc Substituted aryl acylthioureas and related compounds; inhibitors of viral replication
US20060035893A1 (en) 2004-08-07 2006-02-16 Boehringer Ingelheim International Gmbh Pharmaceutical compositions for treatment of respiratory and gastrointestinal disorders
ES2322175T3 (es) 2004-09-17 2009-06-17 EISAI R&D MANAGEMENT CO., LTD. Composicion medicinal con estabilidad mejorada y gelificacion reducida.
MX2007005590A (es) * 2004-11-09 2007-05-24 Smithkline Beecham Corp Compuestos del inhibidor glicogeno fosforilasa y sus composiciones farmaceuticas.
AR051780A1 (es) * 2004-11-29 2007-02-07 Japan Tobacco Inc Compuestos en anillo fusionados que contienen nitrogeno y utilizacion de los mismos
PE20060777A1 (es) 2004-12-24 2006-10-06 Boehringer Ingelheim Int Derivados de indolinona para el tratamiento o la prevencion de enfermedades fibroticas
WO2006118914A2 (en) * 2005-04-29 2006-11-09 Children's Medical Center Corporation Methods of increasing proliferation of adult mammalian cardiomyocytes through p38 map kinase inhibition
US9006240B2 (en) 2005-08-02 2015-04-14 Eisai R&D Management Co., Ltd. Method for assay on the effect of vascularization inhibitor
PL1981851T3 (pl) * 2006-01-31 2012-07-31 Array Biopharma Inc Inhibitory kinazy i sposoby ich stosowania
CA2652442C (en) 2006-05-18 2014-12-09 Eisai R & D Management Co., Ltd. Antitumor agent for thyroid cancer
EP2065372B1 (de) 2006-08-28 2012-11-28 Eisai R&D Management Co., Ltd. Antitumormittel gegen undifferenzierten magenkrebs
JP5319306B2 (ja) 2007-01-29 2013-10-16 エーザイ・アール・アンド・ディー・マネジメント株式会社 未分化型胃癌治療用組成物
EP2131858A4 (de) * 2007-03-20 2011-11-23 Cadila Pharmaceuticals Ltd P38-hemmer
EP1992344A1 (de) 2007-05-18 2008-11-19 Institut Curie P38 Alpha als therapeutisches Target für Erkrankungen, die mit einer FGFR3- Mutation assoziiert sind
WO2009035951A2 (en) * 2007-09-11 2009-03-19 Arete Therapeutics, Inc. Soluble epoxide hydrolase inhibitors
CN101848895B (zh) 2007-11-09 2013-10-23 卫材R&D管理有限公司 血管新生抑制物质和抗肿瘤性铂络合物的组合使用
EP3312269A1 (de) 2008-12-17 2018-04-25 The Scripps Research Institute Erzeugung und erhaltung von stammzellen
KR101064258B1 (ko) 2008-12-29 2011-09-14 한국과학기술연구원 벤조아릴우레이도 화합물, 및 이를 함유하는 퇴행성 뇌질환예방 또는 치료용 조성물
CA2763589A1 (en) * 2009-05-28 2010-12-02 President And Fellows Of Harvard College N,n'-diarylurea compounds and n,n'-diarylthiourea compounds as inhibitors of translation initiation
AU2010285740C1 (en) 2009-08-19 2016-03-17 Eisai R&D Management Co., Ltd. Quinoline derivative-containing pharmaceutical composition
WO2011040509A1 (ja) 2009-09-30 2011-04-07 東レ株式会社 ２，３－ジヒドロ－１ｈ－インデン－２－イルウレア誘導体及びその医薬用途
WO2011103016A2 (en) * 2010-02-19 2011-08-25 The Regents Of The University Of Michigan Compositions and methods for inhibiting ezh2
ES2573515T3 (es) 2010-06-25 2016-06-08 Eisai R&D Management Co., Ltd. Agente antitumoral que emplea compuestos con efecto inhibitorio de cinasas combinados
BRPI1004176A2 (pt) * 2010-10-25 2015-08-11 Univ Rio De Janeiro Compostos aril e/ou hetero aril uréias funcionalizados; processo de síntese desses composto; composição farmacêutica contendo tais compostos e usos
JP6021805B2 (ja) 2011-04-18 2016-11-09 エーザイ・アール・アンド・ディー・マネジメント株式会社 腫瘍治療剤
EP3444363B1 (de) 2011-06-03 2020-11-25 Eisai R&D Management Co., Ltd. Biomarker zur vorhersage und beurteilung des ansprechens von schilddrüsen- und nierenkrebspatienten auf lenvatinibverbindungen
EP2843049B1 (de) 2012-04-27 2018-04-11 Keio University Promoter für neuronale differenzierung
ES2449640B1 (es) * 2012-09-19 2015-01-26 Universidad De Zaragoza Compuestos para su uso en el tratamiento de la enfermedad de alzheimer
BR112015009004A8 (pt) 2012-12-21 2021-07-20 Eisai R&D Man Co Ltd forma amorfa de derivado de quinolina e método de produção da mesma
EP2968322B1 (de) 2013-03-15 2018-12-26 The Trustees of Columbia University in the City of New York Map-kinasemodulatoren und verwendungen davon
US10517861B2 (en) 2013-05-14 2019-12-31 Eisai R&D Management Co., Ltd. Biomarkers for predicting and assessing responsiveness of endometrial cancer subjects to lenvatinib compounds
JP6659554B2 (ja) 2014-08-28 2020-03-04 エーザイ・アール・アンド・ディー・マネジメント株式会社 高純度キノリン誘導体およびその製造方法
LT3263106T (lt) 2015-02-25 2024-01-10 Eisai R&D Management Co., Ltd. Chinolino darinių kartumo sumažinimo būdas
AU2015384801B2 (en) 2015-03-04 2022-01-06 Eisai R&D Management Co., Ltd. Combination of a PD-1 antagonist and a VEGFR/FGFR/RET tyrosine kinase inhibitor for treating cancer
AU2016279474B2 (en) 2015-06-16 2021-09-09 Eisai R&D Management Co., Ltd. Anticancer agent
SG11201801083UA (en) 2015-08-20 2018-03-28 Eisai R&D Man Co Ltd Tumor therapeutic agent
DK3368052T3 (da) 2015-10-27 2022-03-14 Childrens Hospital Med Ct Anvendelse af mapk-hæmmere for at nedbringe tabet af hæmatopoietiske stamceller under ex vivo-dyrkning og -genmanipulation
CA3014395A1 (en) 2016-02-19 2017-08-24 Phoenix Molecular Designs Carboxamide derivatives useful as rsk inhibitors
ES2901164T3 (es) * 2016-05-30 2022-03-21 Univ Muenchen Tech Compuestos con motivo de urea y derivados de los mismos como fármacos antibacterianos
CN110072528B (zh) 2017-02-08 2022-04-26 卫材R&D管理有限公司 治疗肿瘤的药物组合物
CN116283668A (zh) 2017-05-12 2023-06-23 研究三角协会 作为cb1别构调节剂的二芳基脲
KR20200013644A (ko) 2017-05-16 2020-02-07 에자이 알앤드디 매니지먼트 가부시키가이샤 간세포 암종의 치료
KR20200067170A (ko) 2017-10-05 2020-06-11 풀크럼 쎄러퓨틱스, 인코포레이티드 FSHD의 치료를 위하여 DUX4 및 하류 유전자 발현을 저감시키는 p38 키나제 저해제
US10342786B2 (en) 2017-10-05 2019-07-09 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD
JP2021519334A (ja) 2018-03-26 2021-08-10 クリア クリーク バイオ， インコーポレイテッド ジヒドロオロト酸デヒドロゲナーゼを阻害するための組成物および方法
EP3894392A4 (de) * 2018-12-11 2022-08-24 Duke University Zusammensetzungen und verfahren zur behandlung von krebs
EP3924352A4 (de) 2019-02-11 2022-11-16 Phoenix Molecular Designs Kristalline formen eines rsk-hemmers
MA56193A (fr) * 2019-06-14 2022-04-20 Ifm Due Inc Composés et compositions pour traiter des états associés à une activité de sting
US20210300873A1 (en) 2020-03-20 2021-09-30 Clear Creek Bio, Inc. Stable polymorphic compositions of brequinar sodium and methods of use and manufacture thereof
CN111704714B (zh) * 2020-07-01 2023-08-04 浙江大学 一种苯并五元、六元环(硫)脲催化剂及其在开环聚合中的应用
CN112076185A (zh) * 2020-08-17 2020-12-15 西安交通大学 一类卤代二芳基脲类化合物及其在制备抗过敏药物中的应用
WO2022150585A1 (en) 2021-01-08 2022-07-14 Ifm Due, Inc. Heterobicyclic compounds having an urea or analogue and their compositions for treating conditions associated with sting activity

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5716972A (en) * 1993-01-13 1998-02-10 Smithkline Beecham Corporation Pyridyl substituted imidazoles
US5559137A (en) * 1994-05-16 1996-09-24 Smithkline Beecham Corp. Compounds
US5773459A (en) * 1995-06-07 1998-06-30 Sugen, Inc. Urea- and thiourea-type compounds
US5843904A (en) * 1995-12-20 1998-12-01 Vertex Pharmaceuticals, Inc. Inhibitors of interleukin-1βconverting enzyme
US5807876A (en) * 1996-04-23 1998-09-15 Vertex Pharmaceuticals Incorporated Inhibitors of IMPDH enzyme
PL192628B1 (pl) * 1996-04-23 2006-11-30 Vertex Pharma Pochodne mocznika, kompozycje farmaceutyczne i zastosowanie związku i kompozycji
JP2000513359A (ja) * 1996-06-27 2000-10-10 スミスクライン・ビーチャム・コーポレイション Ｉｌ―８受容体拮抗薬
WO1997049400A1 (en) * 1996-06-27 1997-12-31 Smithkline Beecham Corporation Il-8 receptor antagonists

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