CN1116288C - 用作肌苷－5'－一磷酸脱氢酶抑制剂的脲衍生物 - Google Patents

用作肌苷－5'－一磷酸脱氢酶抑制剂的脲衍生物 Download PDF

Info

Publication number
CN1116288C
CN1116288C CN97194856A CN97194856A CN1116288C CN 1116288 C CN1116288 C CN 1116288C CN 97194856 A CN97194856 A CN 97194856A CN 97194856 A CN97194856 A CN 97194856A CN 1116288 C CN1116288 C CN 1116288C
Authority
CN
China
Prior art keywords
compound
medicine
agent
alkyl
impdh
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
CN97194856A
Other languages
English (en)
Chinese (zh)
Other versions
CN1219929A (zh
Inventor
D·M·阿米斯泰德
M·C·巴迪阿
G·W·比米斯
R·S·伯希尔
C·A·法兰克
P·M·诺瓦克
S·M·隆金
J·O·桑德斯
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
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 CN1219929A publication Critical patent/CN1219929A/zh
Application granted granted Critical
Publication of CN1116288C publication Critical patent/CN1116288C/zh
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/12—Heterocyclic 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
    • 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
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic 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
    • A61K31/403—Heterocyclic 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
    • A61K31/404—Indoles, e.g. pindolol
    • 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
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic 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
    • A61K31/42—Oxazoles
    • 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
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic 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
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
    • 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
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/30—Heterocyclic 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
    • C07D263/32—Heterocyclic 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
    • Y—GENERAL 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
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design 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)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Virology (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Molecular Biology (AREA)
  • Biotechnology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Transplantation (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Enzymes And Modification Thereof (AREA)
CN97194856A 1996-04-23 1997-04-21 用作肌苷－5'－一磷酸脱氢酶抑制剂的脲衍生物 Expired - Fee Related CN1116288C (zh)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US08/636,361 US5807876A (en) 1996-04-23 1996-04-23 Inhibitors of IMPDH enzyme
US08/636,361 1996-04-23
US08/801,780 US6344465B1 (en) 1996-04-23 1997-02-14 Inhibitors of IMPDH enzyme
US08/801,780 1997-02-14
US08/832,165 1997-04-02
US08/832,165 US6054472A (en) 1996-04-23 1997-04-02 Inhibitors of IMPDH enzyme

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CNA031002366A Division CN1515248A (zh) 1996-04-23 1997-04-21 用作肌苷-5'-一磷酸脱氢酶抑制剂的脲衍生物

Publications (2)

Publication Number Publication Date
CN1219929A CN1219929A (zh) 1999-06-16
CN1116288C true CN1116288C (zh) 2003-07-30

Family

ID=27417590

Family Applications (2)

Application Number Title Priority Date Filing Date
CN97194856A Expired - Fee Related CN1116288C (zh) 1996-04-23 1997-04-21 用作肌苷－5'－一磷酸脱氢酶抑制剂的脲衍生物
CNA031002366A Pending CN1515248A (zh) 1996-04-23 1997-04-21 用作肌苷-5'-一磷酸脱氢酶抑制剂的脲衍生物

Family Applications After (1)

Application Number Title Priority Date Filing Date
CNA031002366A Pending CN1515248A (zh) 1996-04-23 1997-04-21 用作肌苷-5'-一磷酸脱氢酶抑制剂的脲衍生物

Country Status (21)

Country Link
US (3) US6541496B1 (cg-RX-API-DMAC7.html)
EP (1) EP0902782A1 (cg-RX-API-DMAC7.html)
CN (2) CN1116288C (cg-RX-API-DMAC7.html)
AP (1) AP813A (cg-RX-API-DMAC7.html)
AU (1) AU723730B2 (cg-RX-API-DMAC7.html)
BG (1) BG64507B1 (cg-RX-API-DMAC7.html)
BR (1) BR9708735A (cg-RX-API-DMAC7.html)
CA (1) CA2252465C (cg-RX-API-DMAC7.html)
CZ (1) CZ298463B6 (cg-RX-API-DMAC7.html)
EA (1) EA004771B1 (cg-RX-API-DMAC7.html)
HU (1) HUP0004421A3 (cg-RX-API-DMAC7.html)
ID (1) ID16664A (cg-RX-API-DMAC7.html)
IL (1) IL126674A (cg-RX-API-DMAC7.html)
IN (1) IN190508B (cg-RX-API-DMAC7.html)
NO (1) NO312963B1 (cg-RX-API-DMAC7.html)
NZ (1) NZ332405A (cg-RX-API-DMAC7.html)
OA (1) OA10902A (cg-RX-API-DMAC7.html)
PL (1) PL192628B1 (cg-RX-API-DMAC7.html)
SK (1) SK286662B6 (cg-RX-API-DMAC7.html)
TR (1) TR199802136T2 (cg-RX-API-DMAC7.html)
WO (1) WO1997040028A1 (cg-RX-API-DMAC7.html)

Families Citing this family (159)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ335276A (en) * 1996-10-18 2000-09-29 Vertex Pharma Inhibitors of serine proteases, particularly hepatitis C virus (HCV) NS3 (Non Structural Protein 3) 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
DK1027328T3 (da) * 1997-10-31 2006-11-13 Aventis Pharma Ltd Substituerede anilider
US7517880B2 (en) 1997-12-22 2009-04-14 Bayer Pharmaceuticals Corporation Inhibition of p38 kinase using symmetrical and unsymmetrical diphenyl ureas
IL136768A0 (en) * 1997-12-22 2001-06-14 Bayer Ag INHIBITION OF p38 KINASE ACTIVITY USING ARYL AND HETEROARYL SUBSTITUTED HETEROCYCLIC UREAS
US7329670B1 (en) 1997-12-22 2008-02-12 Bayer Pharmaceuticals Corporation Inhibition of RAF kinase using aryl and heteroaryl substituted heterocyclic ureas
JP4437270B2 (ja) * 1997-12-22 2010-03-24 バイエル コーポレイション 置換複素環式尿素を用いたｒａｆキナーゼの阻害
EP1076641A1 (en) * 1998-04-29 2001-02-21 Vertex Pharmaceuticals Incorporated Inhibitors of impdh enzyme
AU4059199A (en) * 1998-06-04 1999-12-20 Ihara Chemical Industry Co. Ltd. Phenylacetylene derivatives and agricultural/horticultural bactericides
EP1514867A3 (en) * 1998-10-22 2005-03-23 NeuroSearch A/S Substituted phenyl derivatives, their preparation and use
AU764479B2 (en) 1998-10-29 2003-08-21 Bristol-Myers Squibb Company Compounds derived from an amine nucleus that are inhibitors of IMPDH enzyme
US6420403B1 (en) 1998-10-29 2002-07-16 Edwin J. Iwanowicz 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
WO2000026197A1 (en) 1998-10-29 2000-05-11 Bristol-Myers Squibb Company Novel 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
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
ATE267824T1 (de) * 1998-12-09 2004-06-15 Wyeth Corp Alpha-methylbenzyl-enthaltende thioharnstoffe als inhibitoren von herpes-viren mit einer phenylenediamingruppe
EP1137632B1 (en) * 1998-12-09 2004-07-28 Wyeth Thiourea inhibitors of herpes viruses
US6262090B1 (en) 1998-12-09 2001-07-17 American Home Products Corporation Aminopyridine-containing thiourea inhibitors of herpes viruses
US6166028A (en) 1998-12-09 2000-12-26 American Home Products Corporation Diaminopuridine-containing 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
EP2298311B1 (en) 1999-01-13 2012-05-09 Bayer HealthCare LLC w-Carboxy aryl substituted diphenyl ureas as p38 kinase inhibitors
EP1140840B1 (en) 1999-01-13 2006-03-22 Bayer Pharmaceuticals Corp. -g(v)-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
US8124630B2 (en) 1999-01-13 2012-02-28 Bayer Healthcare Llc ω-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
TR200102817T2 (tr) * 1999-03-12 2002-05-21 Boehringer Ingelheim Pharmaceuticals, Inc. Antiinflamatuar ajanlar olarak faydalı bileşikler
CZ301802B6 (cs) 1999-03-19 2010-06-30 Vertex Pharmaceuticals Incorporated Deriváty mocoviny jako inhibitory IMPDH a farmaceutické prostredky s jejich obsahem
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
PT1196414E (pt) * 1999-06-25 2003-12-31 Vertex Pharma Pro-farmacos de inibidores carbamato de impdh
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
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
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
WO2001081340A2 (en) 2000-04-24 2001-11-01 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
DK1478358T3 (da) 2002-02-11 2013-10-07 Bayer Healthcare Llc Sorafenibtosylat til behandling af sygdomme kendetegnet ved unormal angiogenese
ATE529406T1 (de) 2002-02-11 2011-11-15 Bayer Healthcare Llc Aryl-harnstoffe als kinase inhibitoren
EP1402887A1 (en) * 2002-09-18 2004-03-31 Jerini AG New compounds for the inhibition of undesired cell proliferation and use thereof
US7943593B2 (en) 2002-12-06 2011-05-17 Vertex Pharmaceuticals Incorporated Compositions comprising inhibitors of IMPDH enzyme
WO2004060346A2 (en) 2002-12-30 2004-07-22 Angiotech International Ag Drug delivery from rapid gelling polymer composition
US7220768B2 (en) * 2003-02-11 2007-05-22 Wyeth Holdings Corp. Isoxazole-containing thiourea inhibitors useful for treatment of varicella zoster virus
EP1636585B2 (en) 2003-05-20 2012-06-13 Bayer HealthCare LLC Diaryl ureas with kinase inhibiting activity
PL1663978T3 (pl) 2003-07-23 2008-04-30 Bayer Healthcare Llc Fluoropodstawiony omega-karboksyarylodifenylomocznik do leczenia i profilaktyki chorób i stanów
MY148123A (en) 2003-09-05 2013-02-28 Vertex Pharma Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
NZ546663A (en) 2003-10-10 2010-01-29 Vertex Pharma 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
ES2389201T3 (es) 2003-10-27 2012-10-24 Vertex Pharmaceuticals Incorporated Mutantes de resistencia de la proteasa NS3/4A de HCV
EP1711515A2 (en) 2004-02-04 2006-10-18 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
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
EP1768662A2 (en) 2004-06-24 2007-04-04 Novartis Vaccines and Diagnostics, Inc. Small molecule immunopotentiators and assays for their detection
AU2005273612B2 (en) 2004-08-12 2010-10-14 Pfizer Inc. Triazolopyridinylsulfanyl derivatives as p38 map kinase inhibitors
US20080267915A1 (en) 2004-10-01 2008-10-30 Vertex Pharmaceuticals Hcv Ns3-Ns4a Protease Inhibition
MY141025A (en) 2004-10-29 2010-02-25 Vertex Pharma Dose forms
EP2397478A1 (en) * 2005-01-14 2011-12-21 CGI Pharmaceuticals, Inc. 1,3-diaryl substituted ureas as modulators of kinase activity.
ES2465469T3 (es) * 2005-01-14 2014-06-05 Gilead Connecticut, Inc. Diaril ureas 1,3-sustituidas como moduladores de la actividad quinasa
EP1917010A2 (en) * 2005-02-08 2008-05-07 Aspreva Pharmaceuticals SA Compositions and methods for treating vascular, autoimmune and inflammatory diseases
WO2006086498A2 (en) * 2005-02-08 2006-08-17 Aspreva Pharmaceuticals Sa Treatment of vascular, autoimmune and inflammatory diseases using low dosages of impdh inhibitors
DE602006017188D1 (de) 2005-03-07 2010-11-11 Bayer Schering Pharma Ag Pharmazeutische zusammensetzung mit einem omega-carboxyaryl-substituierten diphenylharnstoff zur behandlung von krebs
US7777040B2 (en) * 2005-05-03 2010-08-17 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
EP1919904B1 (en) 2005-07-29 2014-01-08 Janssen R&D Ireland Macrocyclic inhibitors of hepatitis c virus
ATE496042T1 (de) 2005-07-29 2011-02-15 Tibotec Pharm Ltd Makrocyclische inhibitoren des hepatitis-c-virus
WO2007014922A1 (en) 2005-07-29 2007-02-08 Tibotec Pharmaceuticals Ltd. Macrocyclic inhibitors of hepatitis c virus
PE20070210A1 (es) 2005-07-29 2007-04-16 Tibotec Pharm Ltd Compuestos macrociclicos como inhibidores del virus de hepatitis c
BRPI0614637A2 (pt) 2005-07-29 2011-04-12 Tibotec Pharm Ltd inibidores macrocìclicos do vìrus da hepatite c
AR055105A1 (es) 2005-07-29 2007-08-08 Tibotec Pharm Ltd Inhibidores macrociclicos del virus de la hepatitis c
JO2768B1 (en) 2005-07-29 2014-03-15 تيبوتيك فارماسيوتيكالز ليمتد Large cyclic inhibitors of hepatitis C virus
RU2436787C2 (ru) 2005-07-29 2011-12-20 Тиботек Фармасьютикалз Лтд. Макроциклические ингибиторы вируса гепатита с
ES2401661T3 (es) * 2005-08-02 2013-04-23 Vertex Pharmaceuticals Incorporated Inhibidores de serina proteasas
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
NZ568324A (en) 2005-11-11 2012-01-12 Vertex Pharma Hepatitis C virus variants
US7705138B2 (en) 2005-11-11 2010-04-27 Vertex Pharmaceuticals Incorporated Hepatitis C virus variants
EP1991229A2 (en) 2006-02-27 2008-11-19 Vertex Pharmaceuticals Incorporated Co-crystals and pharmaceutical compositions comprising the same
JP2009531315A (ja) 2006-03-16 2009-09-03 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 重水素化ｃ型肝炎プロテアーゼインヒビター
EP2518079A3 (en) 2006-04-11 2012-12-12 Novartis AG HCV/HIV inhibitors and their uses
EP2066642A1 (en) * 2006-09-25 2009-06-10 Arete Therapeutics, INC. Soluble epoxide hydrolase inhibitors
US9987277B2 (en) 2006-10-04 2018-06-05 Janssen Sciences Ireland Uc Carboxamide 4-[(4-pyridyl)amino] pryimidines for the treatment of hepatitis C
WO2008059046A1 (en) 2006-11-17 2008-05-22 Tibotec Pharmaceuticals Ltd. Macrocyclic inhibitors of hepatitis c virus
US8575208B2 (en) * 2007-02-27 2013-11-05 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases
EA200970806A1 (ru) * 2007-02-27 2010-08-30 Вертекс Фармасьютикалз Инкорпорейтед Сокристаллы и содержащие их фармацевтические композиции
WO2008140895A1 (en) * 2007-04-20 2008-11-20 Deciphera Pharmaceuticals, Llc Kinase inhibitors useful for the treatment of myleoproliferative diseases and other proliferative diseases
MX2009011930A (es) 2007-05-04 2009-11-18 Vertex Pharma Terapia de combinacion para el tratamiento de infeccion de virus de hepatitis c.
EP2436682A1 (en) * 2007-08-30 2012-04-04 Vertex Pharmceuticals Incorporated Co-crystals and pharmaceutical compositions comprising the same
CN101910177B (zh) 2007-12-24 2013-08-28 泰博特克药品公司 作为丙型肝炎病毒抑制剂的大环吲哚
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
RU2518471C2 (ru) 2008-08-14 2014-06-10 Тиботек Фармасьютикалз Макроциклические индольные производные, применимые в качестве ингибиторов вируса гепатита с
WO2010065668A1 (en) 2008-12-03 2010-06-10 Presidio Pharmaceuticals, Inc. Inhibitors of hcv ns5a
AU2009322393B2 (en) 2008-12-03 2017-02-02 Presidio Pharmaceuticals, Inc. Inhibitors of HCV NS5A
EP2396028A2 (en) 2009-02-12 2011-12-21 Vertex Pharmceuticals Incorporated Hcv combination therapies comprising pegylated interferon, ribavirin and telaprevir
US8969342B2 (en) 2009-03-20 2015-03-03 Brandeis University Compounds and methods for treating mammalian gastrointestinal microbial infections
EA201190224A1 (ru) 2009-03-27 2012-03-30 Пресидио Фармасьютикалс, Инк. Ингибиторы гепатита c, содержащие конденсированные кольца
US20110182850A1 (en) 2009-04-10 2011-07-28 Trixi Brandl Organic compounds and their uses
US8512690B2 (en) 2009-04-10 2013-08-20 Novartis Ag Derivatised proline containing peptide compounds as protease inhibitors
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
AU2011210795A1 (en) 2010-01-29 2012-08-02 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
CA2800509A1 (en) 2010-05-24 2011-12-01 Presidio Pharmaceuticals, Inc. Inhibitors of hcv ns5a
MX380504B (es) 2010-06-03 2025-03-12 Pharmacyclics Llc El uso de inhibidores de la tirosina quinasa de bruton (btk).
WO2011156545A1 (en) 2010-06-09 2011-12-15 Vertex Pharmaceuticals Incorporated Viral dynamic model for hcv combination therapy
EP2585438B1 (en) 2010-06-24 2014-08-20 Janssen R&D Ireland PREPARATION OF 13-CYCLOHEXYL-3-METHOXY-6-[METHYL-(2-{2-[METHYL-(SULPHAMOYL)-AMINO]-ETHOXY}-ETHYL)-CARBAMOYL]-7H-INDOLO-[2,1-a]-[2]-BENZAZEPINE-10-CARBOXYLIC ACID
EP2593105A1 (en) 2010-07-14 2013-05-22 Vertex Pharmaceuticals Incorporated Palatable pharmaceutical composition comprising vx-950
AR082619A1 (es) 2010-08-13 2012-12-19 Hoffmann La Roche Inhibidores del virus de la hepatitis c
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
BR112013032188A2 (pt) 2011-06-23 2016-12-20 Digna Biotech Sl composição, produto e método para tratar pacientes com hepatite c crônica
WO2012175581A1 (en) 2011-06-24 2012-12-27 F. Hoffmann-La Roche Ag Antiviral compounds
KR101621181B1 (ko) 2011-10-10 2016-05-13 에프. 호프만-라 로슈 아게 항바이러스성 화합물
CN103987723B (zh) 2011-12-16 2017-03-01 弗·哈夫曼-拉罗切有限公司 Hcv ns5a 的抑制剂
EA024297B1 (ru) 2011-12-20 2016-09-30 Рибосайенс Ллк 2',4'-дифтор-2'-метилзамещенные нуклеозидные производные в качестве ингибиторов репликации рнк вируса гепатита с
IN2014CN04530A (cg-RX-API-DMAC7.html) 2011-12-20 2015-09-11 Hoffmann La Roche
MX340033B (es) 2011-12-28 2016-06-21 Janssen Sciences Ireland Uc Derivados heterobiciclicos como inhibidores del virus de la hepatitis c.
US20130195797A1 (en) 2012-01-31 2013-08-01 Vertex Pharmaceuticals Incorporated High potency formulations of vx-950
CN104185624B (zh) 2012-02-24 2016-10-12 弗·哈夫曼-拉罗切有限公司 抗病毒化合物
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
HK1206073A1 (en) 2012-07-24 2015-12-31 药品循环有限责任公司 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
MX2015009176A (es) 2013-01-23 2015-11-09 Hoffmann La Roche Derivados de triazola antivirales.
WO2014135422A1 (en) 2013-03-05 2014-09-12 F. Hoffmann-La Roche Ag Antiviral compounds
MX2015015781A (es) 2013-05-16 2016-06-02 Riboscience Llc Derivados de nucleósido 4'-azido, 3'-deoxi-3'-fluoro sustituido.
AU2014265293B2 (en) 2013-05-16 2019-07-18 Riboscience Llc 4'-Fluoro-2'-methyl substituted nucleoside derivatives
US20180200280A1 (en) 2013-05-16 2018-07-19 Riboscience Llc 4'-Fluoro-2'-Methyl Substituted Nucleoside Derivatives as Inhibitors of HCV RNA Replication
WO2015061752A1 (en) 2013-10-25 2015-04-30 Pharmacyclics, Inc. Treatment using bruton's tyrosine kinase inhibitors and immunotherapy
US9885086B2 (en) 2014-03-20 2018-02-06 Pharmacyclics Llc Phospholipase C gamma 2 and resistance associated mutations
EP3684374B1 (en) 2017-09-21 2025-07-30 Riboscience LLC 4'-fluoro-2'-methyl substituted nucleoside derivatives as inhibitors of hcv rna replication
KR102708177B1 (ko) 2018-01-31 2024-09-23 데시페라 파마슈티칼스, 엘엘씨. 위장관 기질 종양의 치료를 위한 병용 요법
CN118903436A (zh) 2018-01-31 2024-11-08 德西费拉制药有限责任公司 治疗肥大细胞增多症的组合疗法
EP3773579A4 (en) 2018-03-26 2022-03-09 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
PE20210097A1 (es) 2018-06-19 2021-01-12 Novartis Ag Derivados de tetrahidrotienopiridina n-sustituidos y sus usos
US12098117B2 (en) * 2018-12-11 2024-09-24 Duke University Compositions and methods for the treatment of cancer
IL330104A (en) 2019-03-11 2026-08-01 Deciphera Pharmaceuticals Llc Crystalline forms of rifatinib
US12691108B2 (en) 2019-08-12 2026-07-28 Deciphera Pharmaceuticals, Llc Methods for treating vascular malformations
HRP20260411T1 (hr) 2019-08-12 2026-05-08 Deciphera Pharmaceuticals, Llc Ripretinib za liječenje gastrointestinalnih stromalnih tumora
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
FI4084779T3 (fi) 2019-12-30 2024-12-16 Deciphera Pharmaceuticals Llc 1-(4-bromi-5-(1-etyyli-7-(metyyliamino)-2-okso-1,2-dihydro-1,6-naftyridin-3-yyli)-2-fluorifenyyli)-3-fenyyliurean koostumuksia
US12076315B2 (en) 2020-03-20 2024-09-03 Clear Creek Bio, Inc. Stable polymorphic compositions of brequinar sodium and methods of use and manufacture thereof
WO2021209563A1 (en) 2020-04-16 2021-10-21 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

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5380879A (en) * 1994-02-18 1995-01-10 Syntex (U.S.A.) Inc. Derivatives of mycophenolic acid

Family Cites Families (6)

* 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
US5444072A (en) 1994-02-18 1995-08-22 Syntex (U.S.A.) Inc. 6-substituted mycophenolic acid and derivatives

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5380879A (en) * 1994-02-18 1995-01-10 Syntex (U.S.A.) Inc. Derivatives of mycophenolic acid

Also Published As

Publication number Publication date
CA2252465C (en) 2007-07-03
US7329681B2 (en) 2008-02-12
ID16664A (id) 1997-10-30
SK286662B6 (sk) 2009-03-05
NZ332405A (en) 2000-06-23
AP813A (en) 2000-02-28
IN190508B (cg-RX-API-DMAC7.html) 2003-08-02
NO984917D0 (no) 1998-10-22
EP0902782A1 (en) 1999-03-24
EA199800943A1 (ru) 1999-04-29
HUP0004421A2 (hu) 2001-04-28
CN1515248A (zh) 2004-07-28
CZ338098A3 (cs) 1999-02-17
NO312963B1 (no) 2002-07-22
OA10902A (en) 2001-10-11
CN1219929A (zh) 1999-06-16
US6967214B2 (en) 2005-11-22
HUP0004421A3 (en) 2002-10-28
US6541496B1 (en) 2003-04-01
US20030195202A1 (en) 2003-10-16
PL329639A1 (en) 1999-04-12
WO1997040028A1 (en) 1997-10-30
BG64507B1 (bg) 2005-05-31
IL126674A0 (en) 1999-08-17
PL192628B1 (pl) 2006-11-30
AU723730B2 (en) 2000-09-07
IL126674A (en) 2005-08-31
CZ298463B6 (cs) 2007-10-10
AP9700973A0 (en) 1997-07-31
EA004771B1 (ru) 2004-08-26
NO984917L (no) 1998-12-23
BG102945A (en) 1999-08-31
BR9708735A (pt) 1999-08-03
TR199802136T2 (xx) 2001-06-21
AU2678597A (en) 1997-11-12
US20050282876A1 (en) 2005-12-22
CA2252465A1 (en) 1997-10-30
SK146198A3 (en) 1999-07-12

Similar Documents

Publication Publication Date Title
CN1219929A (zh) 用作肌苷－5'－一磷酸脱氢酶抑制剂的脲衍生物
CN1196687C (zh) Impdh酶抑制剂
JP4782254B2 (ja) Ｉｍｐｄｈ酵素のインヒビターとしての尿素誘導体
JP4327910B2 (ja) Ｉｍｐｄｈ酵素のインヒビター
TWI249531B (en) Pharmaceutical compositions for treating or preventing HCV
CN1195515C (zh) 用于抗血管生成和/或抗肿瘤生成的酰胺衍生物
CN1317970A (zh) 用aP2抑制剂和组合剂治疗动脉粥样硬化的方法
CN1339025A (zh) 吲哚衍生物及其作为mcp－1拮抗剂的用途
CN1520290A (zh) 含铜胺氧化酶的碳环肼基抑制剂
CN1450998A (zh) 含铜的胺氧化酶的抑制剂
CN1348436A (zh) 新颖的核受体ppar配体
CN1032534C (zh) 二氨基三氟甲基吡啶衍生物的制备方法
CN1777576A (zh) 用于治疗代谢紊乱的化合物
CN1703207A (zh) GSK－3β抑制剂在制备增加骨生成的药物中的应用
CN1243746C (zh) 抑制血管生成的杂环化合物
CN1141940C (zh) 多环噻唑体系用于制备预防或治疗肥胖的药物的用途
CN1902184A (zh) 噻唑烷酮酰胺、噻唑烷羧酸酰胺、其制备方法及其用途
CN1257893C (zh) 具有优异降糖降酯活性的芳烷基氨基酸类ppar全激活剂
CN1657529A (zh) 2－取代亚胺噻唑烷衍生物，其制备工艺及药物组合物
CN1146552C (zh) 作为金属蛋白抑制剂的薁异羟肟酸衍生物
CN1243749C (zh) 苯并咪唑衍生物
CN1023478C (zh) 新化合物
KR20050044853A (ko) 카르복실산 유도체 화합물 및 이 화합물을 유효성분으로서함유하는 약제
CN1974554A (zh) 环酰亚胺类肽金属蛋白酶抑制剂及其应用
CN1816542A (zh) 2,4－二(三氟乙氧基)吡啶化合物以及含有该化合物的药物

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C14 Grant of patent or utility model
GR01 Patent grant
C17 Cessation of patent right
CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20030730

Termination date: 20130421