AU723730B2 - Urea derivatives as inhibitors of IMPDH enzyme - Google Patents

Urea derivatives as inhibitors of IMPDH enzyme Download PDF

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Publication number
AU723730B2
AU723730B2 AU26785/97A AU2678597A AU723730B2 AU 723730 B2 AU723730 B2 AU 723730B2 AU 26785/97 A AU26785/97 A AU 26785/97A AU 2678597 A AU2678597 A AU 2678597A AU 723730 B2 AU723730 B2 AU 723730B2
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AU
Australia
Prior art keywords
compound
agent
compound according
aug
substituents
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.)
Ceased
Application number
AU26785/97A
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English (en)
Other versions
AU2678597A (en
Inventor
David M Armistead
Michael C. Badia
Guy W Bemis
Randy S. Bethiel
Catharine A. Frank
Perry M. Novak
Steven M. Ronkin
Jeffrey O. Saunders
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Vertex Pharmaceuticals Inc
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Vertex Pharmaceuticals Inc
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Filing date
Publication date
Priority claimed from US08/636,361 external-priority patent/US5807876A/en
Priority claimed from US08/832,165 external-priority patent/US6054472A/en
Application filed by Vertex Pharmaceuticals Inc filed Critical Vertex Pharmaceuticals Inc
Publication of AU2678597A publication Critical patent/AU2678597A/en
Application granted granted Critical
Publication of AU723730B2 publication Critical patent/AU723730B2/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404Indoles, e.g. pindolol
    • 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
    • A61K31/42Oxazoles
    • 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
    • A61K31/42Oxazoles
    • A61K31/422Oxazoles not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/20Antivirals for DNA viruses
    • A61P31/22Antivirals for DNA viruses for herpes viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/14Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C275/00Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C275/28Derivatives 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
    • C07C275/42Derivatives 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D263/00Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/30Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D263/32Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole 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
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Molecular Biology (AREA)
  • Biotechnology (AREA)
  • Vascular Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Enzymes And Modification Thereof (AREA)
AU26785/97A 1996-04-23 1997-04-21 Urea derivatives as inhibitors of IMPDH enzyme Ceased AU723730B2 (en)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US08/636,361 US5807876A (en) 1996-04-23 1996-04-23 Inhibitors of IMPDH enzyme
US08636361 1996-04-23
US08801780 1997-02-14
US08/801,780 US6344465B1 (en) 1996-04-23 1997-02-14 Inhibitors of IMPDH enzyme
US08/832,165 US6054472A (en) 1996-04-23 1997-04-02 Inhibitors of IMPDH enzyme
US08832165 1997-04-02
PCT/US1997/006623 WO1997040028A1 (en) 1996-04-23 1997-04-21 Urea derivatives as inhibitors of impdh enzyme

Publications (2)

Publication Number Publication Date
AU2678597A AU2678597A (en) 1997-11-12
AU723730B2 true AU723730B2 (en) 2000-09-07

Family

ID=27417590

Family Applications (1)

Application Number Title Priority Date Filing Date
AU26785/97A Ceased AU723730B2 (en) 1996-04-23 1997-04-21 Urea derivatives as inhibitors of IMPDH enzyme

Country Status (21)

Country Link
US (3) US6541496B1 (enExample)
EP (1) EP0902782A1 (enExample)
CN (2) CN1116288C (enExample)
AP (1) AP813A (enExample)
AU (1) AU723730B2 (enExample)
BG (1) BG64507B1 (enExample)
BR (1) BR9708735A (enExample)
CA (1) CA2252465C (enExample)
CZ (1) CZ298463B6 (enExample)
EA (1) EA004771B1 (enExample)
HU (1) HUP0004421A3 (enExample)
ID (1) ID16664A (enExample)
IL (1) IL126674A (enExample)
IN (1) IN190508B (enExample)
NO (1) NO312963B1 (enExample)
NZ (1) NZ332405A (enExample)
OA (1) OA10902A (enExample)
PL (1) PL192628B1 (enExample)
SK (1) SK286662B6 (enExample)
TR (1) TR199802136T2 (enExample)
WO (1) WO1997040028A1 (enExample)

Families Citing this family (159)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HU227742B1 (en) * 1996-10-18 2012-02-28 Vertex Pharma Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease
JP2001508767A (ja) * 1996-12-02 2001-07-03 藤沢薬品工業株式会社 5―ht拮抗作用を有するインドール―ウレア誘導体
EP1366766A1 (en) * 1997-03-14 2003-12-03 Vertex Pharmaceuticals Incorporated Inhibitors of IMPDH enzyme
US6093742A (en) * 1997-06-27 2000-07-25 Vertex Pharmaceuticals, Inc. Inhibitors of p38
JP4555468B2 (ja) * 1997-10-31 2010-09-29 アベンテイス・フアルマ・リミテツド 置換アニリド
DE69836563T2 (de) * 1997-12-22 2007-05-16 Bayer Pharmaceuticals Corp., West Haven INHIBIERUNG DER p38 KINASE-AKTIVITÄT DURCH DIE VERWENDUNG VON ARYL- UND HETEROARYL-SUBSTITUIERTEN HARNSTOFFEN
PL205321B1 (pl) * 1997-12-22 2010-04-30 Bayer Corp Zastosowanie podstawionych heterocyklicznych moczników do wytwarzania leku do hamowania kinazy raf, podstawione heterocykliczne moczniki oraz kompozycja farmaceutyczna je zawierająca
US7517880B2 (en) 1997-12-22 2009-04-14 Bayer Pharmaceuticals Corporation Inhibition of p38 kinase using symmetrical and unsymmetrical diphenyl ureas
US7329670B1 (en) 1997-12-22 2008-02-12 Bayer Pharmaceuticals Corporation Inhibition of RAF kinase using aryl and heteroaryl substituted heterocyclic ureas
JP2002512997A (ja) * 1998-04-29 2002-05-08 バーテックス ファーマシューティカルズ インコーポレイテッド Impdh酵素のインヒビター
EP1085010B1 (en) * 1998-06-04 2004-03-10 Kumiai Chemical Industry Co., Ltd. Phenylacetylene derivatives and agricultural/horticultural bactericides
EP1123274B1 (en) * 1998-10-22 2004-12-29 Neurosearch A/S Substituted phenyl derivatives, their preparation and use
AU1707700A (en) 1998-10-29 2000-05-22 Bristol-Myers Squibb Company Novel inhibitors of impdh enzyme
US6596747B2 (en) 1998-10-29 2003-07-22 Bristol-Myers Squibb Company Compounds derived from an amine nucleus and pharmaceutical compositions comprising same
US6420403B1 (en) 1998-10-29 2002-07-16 Edwin J. Iwanowicz Inhibitors of IMPDH enzyme
CA2348234A1 (en) 1998-10-29 2000-05-11 Chunjian Liu Compounds derived from an amine nucleus that are inhibitors of impdh enzyme
GB9823873D0 (en) 1998-10-30 1998-12-30 Pharmacia & Upjohn Spa 2-ureido-thiazole derivatives,process for their preparation,and their use as antitumour agents
RU2233269C2 (ru) * 1998-11-02 2004-07-27 Авентис Фарма Лимитед Замещенные анилиды, фармацевтическая композиция и способ лечения
US6262090B1 (en) 1998-12-09 2001-07-17 American Home Products Corporation Aminopyridine-containing thiourea inhibitors of herpes viruses
US6201013B1 (en) 1998-12-09 2001-03-13 American Home Products Corporation Heterocyclic carboxamide-containing thiourea inhibitors of herpes viruses containing a substituted phenylenediamine group
IL143183A0 (en) * 1998-12-09 2002-04-21 American Home Prod Alpha-methylbenzyl-containing thiourea inhibitors of herpres viruses containing a phenylenediamine group
US6166028A (en) 1998-12-09 2000-12-26 American Home Products Corporation Diaminopuridine-containing thiourea inhibitors of herpes viruses
WO2000034238A1 (en) * 1998-12-09 2000-06-15 American Home Products Corporation Thiourea inhibitors of herpes viruses
WO2000035455A1 (en) * 1998-12-15 2000-06-22 Telik, Inc. Heteroaryl-aryl ureas as igf-1 receptor antagonists
EP1142868A4 (en) * 1998-12-22 2004-09-29 Mitsubishi Chem Corp AMIDE DERIVATIVES
US7928239B2 (en) 1999-01-13 2011-04-19 Bayer Healthcare Llc Inhibition of RAF kinase using quinolyl, isoquinolyl or pyridyl ureas
US8124630B2 (en) 1999-01-13 2012-02-28 Bayer Healthcare Llc ω-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
ATE556713T1 (de) 1999-01-13 2012-05-15 Bayer Healthcare Llc Omega-carboxyarylsubstituierte-diphenyl- harnstoffe als p38-kinasehemmer
EP1140840B1 (en) 1999-01-13 2006-03-22 Bayer Pharmaceuticals Corp. -g(v)-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
US7351834B1 (en) 1999-01-13 2008-04-01 Bayer Pharmaceuticals Corporation ω-Carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
EE04799B1 (et) * 1999-03-12 2007-04-16 Boehringer Ingelheim Pharmaceuticals, Inc. Ühendid, mis on kasulikud põletikuvastaste vahenditena, nende ühendite valmistamise meetodid ja neid sisaldavad farmatseutilised kompositsioonid
WO2000056331A1 (en) 1999-03-19 2000-09-28 Vertex Pharmaceuticals Incorporated Inhibitors of impdh enzyme
US6653309B1 (en) 1999-04-26 2003-11-25 Vertex Pharmaceuticals Incorporated Inhibitors of IMPDH enzyme technical field of the invention
AU5031200A (en) * 1999-05-28 2000-12-18 Vertex Pharmaceuticals Incorporated Method for preparing 5-substituted oxazoles
US6107052A (en) * 1999-06-09 2000-08-22 Roche Diagnostics Corporation Enzymatic measurement of mycophenolic acid
US6395763B1 (en) * 1999-06-25 2002-05-28 Vertex Pharmaceuticals Incorporated Prodrugs of carbamate inhibitors of IMPDH
JP2001011060A (ja) * 1999-06-28 2001-01-16 Nippon Synthetic Chem Ind Co Ltd:The 新規オキサゾール化合物及びその製造方法
JP2001011059A (ja) * 1999-06-28 2001-01-16 Nippon Synthetic Chem Ind Co Ltd:The 5−(2−置換−4−ニトロフェニル)−オキサゾールの製造方法
TWI262185B (en) * 1999-10-01 2006-09-21 Eisai Co Ltd Carboxylic acid derivatives having anti-hyperglycemia and anti-hyperlipemia action, and pharmaceutical composition containing the derivatives
US6867299B2 (en) 2000-02-24 2005-03-15 Hoffmann-La Roche Inc. Oxamide IMPDH inhibitors
EP1276739A2 (en) 2000-04-24 2003-01-22 Bristol-Myers Squibb Company Heterocycles that are inhibitors of impdh enzyme
SV2003000617A (es) * 2000-08-31 2003-01-13 Lilly Co Eli Inhibidores de la proteasa peptidomimetica ref. x-14912m
US6423849B1 (en) * 2000-09-01 2002-07-23 The Nippon Synthetic Chemical Industry Co., Ltd. Process of preparing 5-(2-substituted-4-nitrophenyl)-oxazole, novel oxazole compound, and process of preparing the same
US7235576B1 (en) 2001-01-12 2007-06-26 Bayer Pharmaceuticals Corporation Omega-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
US7371763B2 (en) 2001-04-20 2008-05-13 Bayer Pharmaceuticals Corporation Inhibition of raf kinase using quinolyl, isoquinolyl or pyridyl ureas
US6593362B2 (en) * 2001-05-21 2003-07-15 Guilford Pharmaceuticals Inc. Non-peptidic cyclophilin binding compounds and their use
TW200301698A (en) 2001-12-21 2003-07-16 Bristol Myers Squibb Co Acridone inhibitors of IMPDH enzyme
AU2003209116A1 (en) 2002-02-11 2003-09-04 Bayer Pharmaceuticals Corporation Aryl ureas with angiogenesis inhibiting activity
EP1474393A1 (en) 2002-02-11 2004-11-10 Bayer Pharmaceuticals Corporation Aryl ureas as kinase inhibitors
EP1402887A1 (en) * 2002-09-18 2004-03-31 Jerini AG New compounds for the inhibition of undesired cell proliferation and use thereof
DE60326488D1 (de) 2002-12-06 2009-04-16 Vertex Pharma Zusammensetzungen die eine kombination von diphenylharnstoff impdh-hemmern und apoptose-induzierenden antikrebsmitteln enthalten
JP2006516548A (ja) 2002-12-30 2006-07-06 アンジオテック インターナショナル アクツィエン ゲゼルシャフト 迅速ゲル化ポリマー組成物からの薬物送達法
US7220768B2 (en) * 2003-02-11 2007-05-22 Wyeth Holdings Corp. Isoxazole-containing thiourea inhibitors useful for treatment of varicella zoster virus
PT1636585E (pt) 2003-05-20 2008-03-27 Bayer Pharmaceuticals Corp Diarilureias com actividade inibidora de cinase
NZ544920A (en) 2003-07-23 2009-11-27 Bayer Healthcare Llc 4{4-[3-(4-chloro-3-trifluoromethylphenyl)-ureido]-3-fluorophenoxy}-pyridine-2-carboxylic acid methylamide and metabolites for the treatment and prevention of diseases and conditions
PE20050374A1 (es) * 2003-09-05 2005-05-30 Vertex Pharma Inhibidores de proteasas de serina, en particular proteasa ns3-ns4a del vhc
EP1692157B1 (en) 2003-10-10 2013-04-17 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
AR045870A1 (es) * 2003-10-11 2005-11-16 Vertex Pharma Terapia de combinacion para la infeccion de virus de hepatitis c
EP1944042A1 (en) 2003-10-27 2008-07-16 Vertex Pharmceuticals Incorporated Combinations for HCV treatment
CN1894276B (zh) 2003-10-27 2010-06-16 威特克斯医药股份有限公司 Hcv ns3-ns4a蛋白酶抗药性突变体
CN1938332B (zh) 2004-02-04 2011-10-19 沃泰克斯药物股份有限公司 丝氨酸蛋白酶、特别是hcv ns3-ns4a蛋白酶的抑制剂
EP1568696A1 (en) * 2004-02-26 2005-08-31 4Sc Ag Compounds as inhibitors of cell proliferation and viral infections
US7317030B2 (en) 2004-02-26 2008-01-08 4Sc Ag Compounds as inhibitors of cell proliferation and viral infections
CA2571710A1 (en) 2004-06-24 2006-11-02 Nicholas Valiante Small molecule immunopotentiators and assays for their detection
PT1778686E (pt) 2004-08-12 2008-12-26 Pfizer Derivados de triazolopiridinilsufanilo como inibidores da p38 map-cinase
CN102160891A (zh) * 2004-10-01 2011-08-24 威特克斯医药股份有限公司 Hcv ns3-ns4a蛋白酶抑制
TWI437990B (zh) 2004-10-29 2014-05-21 Vertex Pharma Vx-950之醫藥用途
NZ556433A (en) * 2005-01-14 2010-10-29 Cgi Pharmaceuticals Inc 1, 3-diaryl substituted ureas as modulators of kinase activity
EP1858877B1 (en) * 2005-01-14 2014-03-12 Gilead Connecticut, Inc. 1,3 substituted diaryl ureas as modulators of kinase activity
US20060235009A1 (en) * 2005-02-08 2006-10-19 Richard Glickman Treatment of vascular, autoimmune and inflammatory diseases using low dosages of IMPDH inhibitors
EP1917010A2 (en) * 2005-02-08 2008-05-07 Aspreva Pharmaceuticals SA Compositions and methods for treating vascular, autoimmune and inflammatory diseases
NZ561178A (en) 2005-03-07 2010-11-26 Bayer Schering Pharma Ag Pharmaceutical composition comprising an omega-carboxyaryl substituted diphenyl urea for the treatment of cancer
WO2007024294A2 (en) * 2005-05-03 2007-03-01 Cgi Pharmaceuticals, Inc. Certain substituted ureas, as modulators of kinase activity
JP2008540538A (ja) * 2005-05-09 2008-11-20 バーテックス ファーマシューティカルズ インコーポレイテッド (s)−3−(3−(3−メトキシ−4−(オキサゾール−5−イル)フェニル)ウレイド)ベンジルカルバミン酸テトラヒドロフラン−3−イルの多形形態
WO2006122072A2 (en) * 2005-05-09 2006-11-16 Vertex Pharmaceuticals Incorporated Processes for preparing biaryl ureas and analogs thereof
PE20070211A1 (es) 2005-07-29 2007-05-12 Medivir Ab Compuestos macrociclicos como inhibidores del virus de hepatitis c
JP5426164B2 (ja) 2005-07-29 2014-02-26 ヤンセン・アールアンドデイ・アイルランド C型肝炎ウイルスの大環式インヒビター
JO2768B1 (en) 2005-07-29 2014-03-15 تيبوتيك فارماسيوتيكالز ليمتد Large cyclic inhibitors of hepatitis C virus
BRPI0614696A2 (pt) 2005-07-29 2011-04-12 Tibotec Pharm Ltd inibidores macrocìclicos de vìrus da hepatite c
DE602006019883D1 (de) 2005-07-29 2011-03-10 Medivir Ab Makrocyclische inhibitoren des hepatitis-c-virus
AR055361A1 (es) 2005-07-29 2007-08-22 Medivir Ab Inhibidores macrociclicos del virus de la hepatitis c
CN101273030B (zh) 2005-07-29 2012-07-18 泰博特克药品有限公司 丙型肝炎病毒的大环抑制剂
PE20070210A1 (es) 2005-07-29 2007-04-16 Tibotec Pharm Ltd Compuestos macrociclicos como inhibidores del virus de hepatitis c
MY141245A (en) 2005-07-29 2010-03-31 Tibotec Pharm Ltd Macrocylic inhibitors of hepatitis c virus
RU2441020C2 (ru) 2005-08-02 2012-01-27 Вертекс Фармасьютикалз Инкорпорейтед Ингибиторы серинпротеазы
US7964624B1 (en) * 2005-08-26 2011-06-21 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases
AR055395A1 (es) * 2005-08-26 2007-08-22 Vertex Pharma Compuestos inhibidores de la actividad de la serina proteasa ns3-ns4a del virus de la hepatitis c
US7705138B2 (en) 2005-11-11 2010-04-27 Vertex Pharmaceuticals Incorporated Hepatitis C virus variants
JP5409008B2 (ja) 2005-11-11 2014-02-05 バーテックス ファーマシューティカルズ インコーポレイテッド C型肝炎ウイルス改変体
EP1991229A2 (en) 2006-02-27 2008-11-19 Vertex Pharmaceuticals Incorporated Co-crystals and pharmaceutical compositions comprising the same
EP2194039A1 (en) 2006-03-16 2010-06-09 Vertex Pharmceuticals Incorporated Process for preparing optically enriched compounds
WO2007133865A2 (en) 2006-04-11 2007-11-22 Novartis Ag Hcv/hiv inhibitors an their uses
JP2010504362A (ja) * 2006-09-25 2010-02-12 アレテ セラピューティクス, インコーポレイテッド 可溶性エポキシドヒドロラーゼ阻害剤
JP5616063B2 (ja) 2006-10-04 2014-10-29 ヤンセン・アールアンドデイ・アイルランド Hcv阻害剤として有用なカルボキシアミド4−[(4−ピリジル)アミノ]ピリミジン
ES2470568T3 (es) 2006-11-17 2014-06-24 Janssen R&D Ireland Inhibidores macroc�clicos del virus de la hepatitis C
CN101903392A (zh) * 2007-02-27 2010-12-01 弗特克斯药品有限公司 丝氨酸蛋白酶的抑制剂
BRPI0807907A2 (pt) * 2007-02-27 2017-05-16 Vertex Pharma co-cristais e composições farmacêuticas compreendendo os mesmos.
CA2684950A1 (en) * 2007-04-20 2008-10-30 Deciphera Pharmaceuticals, Llc Kinase inhibitors useful for the treatment of myleoproliferative diseases and other proliferative diseases
CN102872461A (zh) 2007-05-04 2013-01-16 弗特克斯药品有限公司 用于治疗hcv感染的组合治疗
TW200922933A (en) * 2007-08-30 2009-06-01 Vertex Pharma Co-crystals and pharmaceutical compositions comprising the same
PL2238142T3 (pl) 2007-12-24 2012-11-30 Janssen R&D Ireland Makrocykliczne indole jako inhibitory wirusa zapalenia wątroby typu C
TWI454476B (zh) 2008-07-08 2014-10-01 Tibotec Pharm Ltd 用作c型肝炎病毒抑制劑之巨環吲哚衍生物
EP2331554B1 (en) 2008-08-14 2013-03-06 Janssen R&D Ireland Macrocyclic indole derivatives useful as hepatitis c virus inhibitors
JP2012510523A (ja) 2008-12-03 2012-05-10 プレシディオ ファーマシューティカルズ インコーポレイテッド Hcvns5aの阻害剤
HK1203929A1 (en) 2008-12-03 2015-11-06 普雷西迪奥制药公司 Inhibitors of hcv ns5a
WO2010093843A2 (en) 2009-02-12 2010-08-19 Vertex Pharmaceuticals Incorporated Hcv combination therapies
WO2010108187A2 (en) * 2009-03-20 2010-09-23 Brandeis University Compounds and methods for treating mammalian gastrointestinal microbial infections
CA2755658A1 (en) 2009-03-27 2010-09-30 Presidio Pharmaceuticals, Inc. Fused ring inhibitors of hepatitis c
US8512690B2 (en) 2009-04-10 2013-08-20 Novartis Ag Derivatised proline containing peptide compounds as protease inhibitors
US20110182850A1 (en) 2009-04-10 2011-07-28 Trixi Brandl Organic compounds and their uses
US20110027229A1 (en) 2009-07-31 2011-02-03 Medtronic, Inc. Continuous subcutaneous administration of interferon-alpha to hepatitis c infected patients
UA108211C2 (uk) 2009-11-04 2015-04-10 Янссен Рід Айрленд Бензімідазолімідазольні похідні
EP2528605A1 (en) 2010-01-29 2012-12-05 Vertex Pharmaceuticals Incorporated Therapies for treating hepatitis c virus infection
WO2011112516A1 (en) 2010-03-08 2011-09-15 Ico Therapeutics Inc. Treating and preventing hepatitis c virus infection using c-raf kinase antisense oligonucleotides
EP2575866A4 (en) 2010-05-24 2013-10-16 Presidio Pharmaceuticals Inc HCV NS5A INHIBITORS
EA201890869A3 (ru) 2010-06-03 2019-03-29 Фармасайкликс, Инк. Применение ингибиторов тирозинкиназы брутона (btk)
WO2011156545A1 (en) 2010-06-09 2011-12-15 Vertex Pharmaceuticals Incorporated Viral dynamic model for hcv combination therapy
CA2801517C (en) 2010-06-24 2017-12-12 Janssen R&D Ireland Preparation of 13-cyclohexyl-3-methoxy-6-[methyl-(2-{2-[methyl-(sulphamoyl)-amino]-ethoxy}-ethyl)-carbamoyl]-7h-indolo-[2,1-.alpha.]-[2]-benzazepine-10-carboxylic acid
AR082215A1 (es) 2010-07-14 2012-11-21 Vertex Pharma Composicion farmaceutica agradable al paladar
WO2012020036A1 (en) 2010-08-13 2012-02-16 F. Hoffmann-La Roche Ag Hepatitis c virus inhibitors
WO2012109646A1 (en) 2011-02-11 2012-08-16 Vertex Pharmaceuticals Incorporated Treatment of hcv in hiv infection patients
CN102985104A (zh) 2011-02-25 2013-03-20 麦德托尼克公司 在干扰素-α治疗方案中使用药代动力学分布和药效动力学分布的方法和系统
WO2012123298A1 (en) 2011-03-11 2012-09-20 F. Hoffmann-La Roche Ag Antiviral compounds
RU2014102102A (ru) 2011-06-23 2015-07-27 Дигна Байотек, С.Л. КОМПОЗИЦИЯ И КОМБИНИРОВАННЫЙ ПРЕПАРАТ ИНТЕРФЕРОНА-а5 С ИНТЕРФЕРОНОМ-а2 И СПОСОБ ЛЕЧЕНИЯ ХРОНИЧЕСКОГО ГЕПАТИТА С
US20120328565A1 (en) 2011-06-24 2012-12-27 Brinkman John A Antiviral compounds
US9180193B2 (en) 2011-10-10 2015-11-10 Hoffmann-La Roche Inc. Antiviral compounds
MX2014006745A (es) 2011-12-16 2014-10-15 Hoffmann La Roche Inhibidores de hcv ns5a.
LT2794628T (lt) 2011-12-20 2017-07-10 Riboscience Llc 4`-azido-3`-fluoro pakeistieji nukleozido dariniai kaip hcv replikacijos inhibitoriai
PE20141423A1 (es) 2011-12-20 2014-10-16 Hoffmann La Roche Derivados nucleosidos con sustitucion 2',4'-difluoro-2'-metilo como inhibidores de la replicacion del arn del vhc
WO2013098313A1 (en) 2011-12-28 2013-07-04 Janssen R&D Ireland Hetero-bicyclic derivatives as hcv inhibitors
US20130195797A1 (en) 2012-01-31 2013-08-01 Vertex Pharmaceuticals Incorporated High potency formulations of vx-950
BR112014015582A8 (pt) 2012-02-24 2017-07-04 Hoffmann La Roche compostos antivirais
US8461179B1 (en) 2012-06-07 2013-06-11 Deciphera Pharmaceuticals, Llc Dihydronaphthyridines and related compounds useful as kinase inhibitors for the treatment of proliferative diseases
US20140010783A1 (en) 2012-07-06 2014-01-09 Hoffmann-La Roche Inc. Antiviral compounds
WO2014018567A1 (en) 2012-07-24 2014-01-30 Pharmacyclics, Inc. Mutations associated with resistance to inhibitors of bruton's tyrosine kinase (btk)
WO2014028931A2 (en) 2012-08-17 2014-02-20 Brandeis University Compounds and methods for treating mammalian gastrointestinal microbial infections
US20140205566A1 (en) 2012-11-30 2014-07-24 Novartis Ag Cyclic nucleuoside derivatives and uses thereof
CN105073726B (zh) 2013-01-23 2017-05-31 弗·哈夫曼-拉罗切有限公司 抗病毒三唑衍生物
CA2900319A1 (en) 2013-03-05 2014-09-12 F. Hoffmann-La Roche Ag Antiviral compounds
MA38678A1 (fr) 2013-05-16 2017-07-31 Riboscience Llc Dérivés nucléosidiques 4'-azido, 3'désoxy-3'-fluoro substitués
US20180200280A1 (en) 2013-05-16 2018-07-19 Riboscience Llc 4'-Fluoro-2'-Methyl Substituted Nucleoside Derivatives as Inhibitors of HCV RNA Replication
CA2912682C (en) 2013-05-16 2021-07-06 Riboscience Llc 4'-fluoro-2'-methyl substituted nucleoside derivatives
TWI660739B (zh) 2013-10-25 2019-06-01 製藥公司 使用布魯頓氏酪胺酸激酶抑制劑之治療及免疫療法
CA2942528A1 (en) 2014-03-20 2015-09-24 Pharmacyclics Inc. Phospholipase c gamma 2 and resistance associated mutations
AU2018335411B2 (en) 2017-09-21 2024-06-27 Riboscience Llc 4'-fluoro-2'-methyl substituted nucleoside derivatives as inhibitors of HCV RNA replication
AU2019216351B2 (en) 2018-01-31 2024-07-25 Deciphera Pharmaceuticals, Llc Combination therapy for the treatment of mastocytosis
CN111818915B (zh) 2018-01-31 2024-05-24 德西费拉制药有限责任公司 治疗胃肠道间质瘤的组合疗法
US10889548B2 (en) 2018-03-26 2021-01-12 Clear Creek Bio, Inc. Compositions and methods for inhibiting dihydroorotate dehydrogenase
CN109970675A (zh) * 2018-05-28 2019-07-05 中国医学科学院医药生物技术研究所 一组硫脲化合物及其制备方法和应用
JOP20200326A1 (ar) 2018-06-19 2020-12-14 Novartis Ag مشتقات تترا هيدرو ثينوبيريدين بها استبدال بـ n واستخداماتها
EP3894392A4 (en) * 2018-12-11 2022-08-24 Duke University COMPOSITIONS AND METHODS FOR THE TREATMENT OF CANCER
TWI878335B (zh) 2019-08-12 2025-04-01 美商迪賽孚爾製藥有限公司 治療胃腸道基質瘤方法
NZ784949A (en) 2019-08-12 2025-09-26 Deciphera Pharmaceuticals Llc Ripretinib for treating gastrointestinal stromal tumors
CN110590535A (zh) * 2019-10-12 2019-12-20 重庆医药高等专科学校 用二氧化硒氧化芳香乙酮制备芳香乙醛酸的方法
AU2020419197B2 (en) 2019-12-30 2023-08-31 Deciphera Pharmaceuticals, Llc Amorphous kinase inhibitor formulations and methods of use thereof
KR20250057151A (ko) 2019-12-30 2025-04-28 데시페라 파마슈티칼스, 엘엘씨 1-(4-브로모-5-(1-에틸-7-(메틸아미노)-2-옥소-1,2-디히드로-1,6-나프티리딘-3-일)-2-플루오로페닐)-3-페닐우레아의조성물
US20210315880A1 (en) 2020-03-20 2021-10-14 Clear Creek Bio, Inc. Methods of treating viral infections using inhibitors of nucleotide synthesis pathways
US20230218644A1 (en) 2020-04-16 2023-07-13 Som Innovation Biotech, S.A. Compounds for use in the treatment of viral infections by respiratory syndrome-related coronavirus
US11779572B1 (en) 2022-09-02 2023-10-10 Deciphera Pharmaceuticals, Llc Methods of treating gastrointestinal stromal tumors

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1171904A (en) 1965-10-21 1969-11-26 Unilever Ltd Anilinobenzimidazoles having Antibacterial Properties
IL39336A0 (en) 1971-05-04 1972-07-26 Lilly Co Eli Substituted 2-anilinobenzoxazoles
DE2928485A1 (de) * 1979-07-14 1981-01-29 Bayer Ag Verwendung von harnstoffderivaten als arzneimittel bei der behandlung von fettstoffwechselstoerungen
US5283257A (en) 1992-07-10 1994-02-01 The Board Of Trustees Of The Leland Stanford Junior University Method of treating hyperproliferative vascular disease
WO1994012184A1 (en) 1992-11-24 1994-06-09 Syntex (U.S.A.) Inc. Use of mycophenolic acid, mycophenolate mofetil or derivate thereof to inhibit stenosis
US5380879A (en) * 1994-02-18 1995-01-10 Syntex (U.S.A.) Inc. Derivatives of mycophenolic acid
US5444072A (en) 1994-02-18 1995-08-22 Syntex (U.S.A.) Inc. 6-substituted mycophenolic acid and derivatives

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