AP813A - Urea derivatives as inhibitors of IMPDH enzyme. - Google Patents

Urea derivatives as inhibitors of IMPDH enzyme. Download PDF

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Publication number
AP813A
AP813A APAP/P/1997/000973A AP9700973A AP813A AP 813 A AP813 A AP 813A AP 9700973 A AP9700973 A AP 9700973A AP 813 A AP813 A AP 813A
Authority
AP
ARIPO
Prior art keywords
compound
substituents
agent
present
formula
Prior art date
Application number
APAP/P/1997/000973A
Other languages
English (en)
Other versions
AP9700973A0 (en
Inventor
David Armistead
Michael C Badia
Guy Bemis
Randy S Bethiel
Cathrine A Frank
Perry M Novak
Steven M Ronkin
Jeffrey Saunders
Original Assignee
Vertex Pharma
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 Pharma filed Critical Vertex Pharma
Publication of AP9700973A0 publication Critical patent/AP9700973A0/xx
Application granted granted Critical
Publication of AP813A publication Critical patent/AP813A/en

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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)
  • Oncology (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biotechnology (AREA)
  • Molecular Biology (AREA)
  • Transplantation (AREA)
  • Cardiology (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)
APAP/P/1997/000973A 1996-04-23 1997-04-23 Urea derivatives as inhibitors of IMPDH enzyme. AP813A (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US08/636,361 US5807876A (en) 1996-04-23 1996-04-23 Inhibitors of IMPDH enzyme
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

Publications (2)

Publication Number Publication Date
AP9700973A0 AP9700973A0 (en) 1997-07-31
AP813A true AP813A (en) 2000-02-28

Family

ID=27417590

Family Applications (1)

Application Number Title Priority Date Filing Date
APAP/P/1997/000973A AP813A (en) 1996-04-23 1997-04-23 Urea derivatives as inhibitors of IMPDH enzyme.

Country Status (21)

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

Families Citing this family (159)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA001915B1 (ru) * 1996-10-18 2001-10-22 Вертекс Фармасьютикалз Инкорпорейтед Ингибиторы серин-протеаз, в частности ns3 протеазы вируса гепатита c (hvc)
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
TR200001179T2 (tr) 1997-10-31 2000-11-21 Aventis Pharma Ltd. Değiştirilmiş anilidler
WO1999032110A1 (en) * 1997-12-22 1999-07-01 Bayer Corporation 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
US7517880B2 (en) 1997-12-22 2009-04-14 Bayer Pharmaceuticals Corporation Inhibition of p38 kinase using symmetrical and unsymmetrical diphenyl ureas
NZ505844A (en) * 1997-12-22 2003-10-31 Bayer Ag Inhibition of raf kinase using substituted heterocyclic ureas
WO1999055663A1 (en) * 1998-04-29 1999-11-04 Vertex Pharmaceuticals Incorporated Inhibitors of impdh enzyme
DE69915472T2 (de) * 1998-06-04 2004-08-19 Kumiai Chemical Industry Co., Ltd. Phenylacetylenderivate und bakterizide für landwirtschaft und gartenbau
CA2342626A1 (en) * 1998-10-22 2000-05-04 Neurosearch A/S Substituted phenyl derivatives, their preparation and use
US6596747B2 (en) 1998-10-29 2003-07-22 Bristol-Myers Squibb Company Compounds derived from an amine nucleus and pharmaceutical compositions comprising same
CA2348234A1 (en) 1998-10-29 2000-05-11 Chunjian Liu Compounds derived from an amine nucleus that are inhibitors of impdh enzyme
EP1127054A4 (en) * 1998-10-29 2006-11-02 Bristol Myers Squibb Co INHIBITORS OF IMPDH ENZYME
US6420403B1 (en) 1998-10-29 2002-07-16 Edwin J. Iwanowicz 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
US6166028A (en) 1998-12-09 2000-12-26 American Home Products Corporation Diaminopuridine-containing thiourea inhibitors of herpes viruses
EP1137632B1 (en) * 1998-12-09 2004-07-28 Wyeth 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
US6262090B1 (en) 1998-12-09 2001-07-17 American Home Products Corporation Aminopyridine-containing thiourea inhibitors of herpes viruses
US6337338B1 (en) 1998-12-15 2002-01-08 Telik, Inc. Heteroaryl-aryl ureas as IGF-1 receptor antagonists
CN1337941A (zh) * 1998-12-22 2002-02-27 三菱化学株式会社 酰胺衍生物
US7928239B2 (en) 1999-01-13 2011-04-19 Bayer Healthcare Llc Inhibition of RAF kinase using quinolyl, isoquinolyl or pyridyl ureas
AU2725000A (en) 1999-01-13 2000-08-01 Bayer Corporation Omega-carboxy aryl substituted diphenyl ureas as p38 kinase inhibitors
ME00275B (me) 1999-01-13 2011-02-10 Bayer Corp ω-KARBOKSIARIL SUPSTITUISANI DIFENIL KARBAMIDI KAO INHIBITORI RAF KINAZE
EP1140840B1 (en) 1999-01-13 2006-03-22 Bayer Pharmaceuticals Corp. -g(v)-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
US8124630B2 (en) 1999-01-13 2012-02-28 Bayer Healthcare Llc ω-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
HUP0202248A3 (en) * 1999-03-12 2006-06-28 Boehringer Ingelheim Pharma Compounds useful as anti-inflammatory agents
PL211562B1 (pl) 1999-03-19 2012-05-31 Vertex Pharma Związki, zawierające je kompozycje oraz ich zastosowania
US6653309B1 (en) 1999-04-26 2003-11-25 Vertex Pharmaceuticals Incorporated Inhibitors of IMPDH enzyme technical field of the invention
WO2000073288A1 (en) * 1999-05-28 2000-12-07 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
DK1196414T3 (da) * 1999-06-25 2003-11-24 Vertex Pharma Prolægemiddel af carbamathæmmer for 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
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
CN1318404C (zh) 2002-02-11 2007-05-30 拜耳制药公司 作为激酶抑制剂的芳基脲类化合物
CA2475703C (en) 2002-02-11 2016-12-20 Bayer Pharmaceuticals Corporation Aryl ureas with angiogenesis inhibiting activity
EP1402887A1 (en) * 2002-09-18 2004-03-31 Jerini AG New compounds for the inhibition of undesired cell proliferation and use thereof
CA2510006C (en) 2002-12-06 2012-02-07 Vertex Pharmaceuticals Incorporated Compositions comprising a combination of diphenyl urea impdh inhibitors and apoptosis-inducing anti-cancer agents
DE60331367D1 (de) 2002-12-30 2010-04-01 Angiotech Int Ag Wirkstofffreisetzung von schnell gelierender polymerzusammensetzung
US7220768B2 (en) * 2003-02-11 2007-05-22 Wyeth Holdings Corp. Isoxazole-containing thiourea inhibitors useful for treatment of varicella zoster virus
DK1636585T3 (da) 2003-05-20 2008-05-26 Bayer Pharmaceuticals Corp Diarylurinstoffer med kinasehæmmende aktivitet
JP4777887B2 (ja) 2003-07-23 2011-09-21 バイエル、ファーマシューテイカルズ、コーポレイション 病気および状態の処置および防止のためのフロロ置換オメガカルボキシアリールジフェニル尿素
UY28500A1 (es) * 2003-09-05 2005-04-29 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
EP1678202B1 (en) 2003-10-27 2012-06-13 Vertex Pharmaceuticals Incorporated Hcv ns3-ns4a protease resistance mutants
EP1944042A1 (en) 2003-10-27 2008-07-16 Vertex Pharmceuticals Incorporated Combinations for HCV treatment
AU2005212257A1 (en) 2004-02-04 2005-08-25 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
US7317030B2 (en) 2004-02-26 2008-01-08 4Sc Ag Compounds as inhibitors of cell proliferation and viral infections
EP1568696A1 (en) * 2004-02-26 2005-08-31 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
WO2006018718A2 (en) 2004-08-12 2006-02-23 Pfizer Limited Triazolopyridinylsulfanyl derivatives as p38 map kinase inhibitors
KR20070061570A (ko) 2004-10-01 2007-06-13 버텍스 파마슈티칼스 인코포레이티드 Ｈｃｖ ｎｓ3-ｎｓ4ａ 프로테아제 저해
TW201424733A (zh) 2004-10-29 2014-07-01 Vertex Pharma 劑量型式
WO2006076592A1 (en) * 2005-01-14 2006-07-20 Cgi Pharmaceuticals, Inc. 1,3 substituted diaryl ureas as modulators of kinase activity
JP2008526988A (ja) * 2005-01-14 2008-07-24 シージーアイ ファーマシューティカルズ，インコーポレーテッド キナーゼ活性モジュレーターとしての１，３−ジアリール置換尿素
US20060235009A1 (en) * 2005-02-08 2006-10-19 Richard Glickman Treatment of vascular, autoimmune and inflammatory diseases using low dosages of IMPDH inhibitors
WO2006086500A2 (en) * 2005-02-08 2006-08-17 Aspreva Pharmaceuticals Sa Compositions and methods for treating vascular, autoimmune and inflammatory diseases
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
EP1891062A2 (en) * 2005-05-09 2008-02-27 Vertex Pharmaceuticals, Inc. Polymorphic forms of (s)- tetrahydrofuran-3-yl-3-(3-(3-methoxy-4-(oxazol-5-yl) phenyl) ureido) benzylcarbamate
US7544810B2 (en) 2005-05-09 2009-06-09 Vertex Pharmaceuticals Incorporated Processes for preparing biaryl ureas and analogs thereof
KR101381176B1 (ko) 2005-07-29 2014-04-11 메디비르 아베 Ｃ형 간염 바이러스의 마크로사이클릭 억제제
PE20070211A1 (es) 2005-07-29 2007-05-12 Medivir Ab Compuestos macrociclicos como inhibidores del virus de hepatitis c
PL1919898T3 (pl) 2005-07-29 2011-06-30 Tibotec Pharm Ltd Makrocykliczne inhibitory wirusa zapalenia wątroby typu C
PE20070210A1 (es) 2005-07-29 2007-04-16 Tibotec Pharm Ltd Compuestos macrociclicos como inhibidores del virus de hepatitis c
JO2768B1 (en) 2005-07-29 2014-03-15 تيبوتيك فارماسيوتيكالز ليمتد Large cyclic inhibitors of hepatitis C virus
TWI383980B (zh) 2005-07-29 2013-02-01 Tibotec Pharm Ltd Ｃ型肝炎病毒之大環抑制劑
EP1913015B1 (en) 2005-07-29 2013-12-11 Janssen R&D Ireland Macrocyclic inhibitors of hepatitis c virus
WO2007014925A1 (en) 2005-07-29 2007-02-08 Tibotec Pharmaceuticals Ltd. Macrocylic inhibitors of hepatitis c virus
MY139988A (en) 2005-07-29 2009-11-30 Tibotec Pharm Ltd Macrocylic inhibitors of hepatitis c virus
EP1910341B1 (en) * 2005-08-02 2013-01-02 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases
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
CN101405295A (zh) 2005-11-11 2009-04-08 沃泰克斯药物股份有限公司 丙型肝炎病毒变种
CN101489557B (zh) 2006-02-27 2013-12-18 弗特克斯药品有限公司 包含vx-950的共晶体和包含所述共晶体的药物组合物
AU2007227544B2 (en) 2006-03-16 2012-11-01 Vertex Pharmaceuticals Incorporated Deuterated hepatitis C protease inhibitors
KR101059593B1 (ko) 2006-04-11 2011-08-25 노파르티스 아게 Ｈｃｖ/ｈｉｖ 억제제 및 이들의 용도
US20080076770A1 (en) * 2006-09-25 2008-03-27 Arete Therapeutics, Inc. Soluble epoxide hydrolase inhibitors
WO2008040778A2 (en) 2006-10-04 2008-04-10 Tibotec Pharmaceuticals Ltd. Carboxamide 4-[(4-pyridyl)amino] pyrimidines for the treatment of hepatitis c
AR064258A1 (es) 2006-11-17 2009-03-25 Tibotec Pharm Ltd Inhibidores macrociclicos del virus de hepatitis c
WO2008106151A2 (en) * 2007-02-27 2008-09-04 Vertex Pharmaceuticals Incorporated Co-crystals and pharmaceutical compositions comprising the same
EP2134717A2 (en) * 2007-02-27 2009-12-23 Vertex Pharmceuticals Incorporated Inhibitors of serine proteases
KR20100014811A (ko) * 2007-04-20 2010-02-11 데시페라 파마슈티칼스, 엘엘씨. 골수증식성 질환 및 기타 증식성 질환의 치료에 유용한 키나제 억제제
JP2010526143A (ja) 2007-05-04 2010-07-29 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 Ｈｃｖ感染の処置のための併用療法
EP2436682A1 (en) * 2007-08-30 2012-04-04 Vertex Pharmceuticals Incorporated Co-crystals and pharmaceutical compositions comprising the same
BRPI0821836A2 (pt) 2007-12-24 2015-06-16 Tibotec Pharm Ltd Indóis macrocíclicos como inibidores do vírus da hepatite 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
DK2331554T3 (da) 2008-08-14 2013-05-27 Janssen R & D Ireland Makrocykliske indolderivater, der er anvendelige som hepatitis c-virusinhibitorer
US9120779B2 (en) 2008-12-03 2015-09-01 Presidio Pharmaceuticals, Inc. Inhibitors of HCV NS5A
CA2746004C (en) 2008-12-03 2017-06-06 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
MX2011010132A (es) 2009-03-27 2011-10-14 Presidio Pharmaceuticals Inc Inhibidores de anillo fusionado de hepatitis c.
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
EP2459211A1 (en) 2009-07-31 2012-06-06 Medtronic, Inc. Continuous subcutaneous administration of interferon- 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
AU2011261185A1 (en) 2010-06-03 2013-01-10 Pharmacyclics, Inc. The use of inhibitors of Bruton's tyrosine kinase (Btk)
WO2011156545A1 (en) 2010-06-09 2011-12-15 Vertex Pharmaceuticals Incorporated Viral dynamic model for hcv combination therapy
AU2011268922B2 (en) 2010-06-24 2014-06-12 Janssen Sciences Ireland Uc 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
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
CN103732242A (zh) 2011-06-23 2014-04-16 迪格纳生物技术公司 用与IFN-α2b组合的IFN-α5在患者群体中治疗慢性丙型肝炎
US20120328565A1 (en) 2011-06-24 2012-12-27 Brinkman John A Antiviral compounds
WO2013053657A1 (en) 2011-10-10 2013-04-18 F. Hoffmann-La Roche Ag Antiviral compounds
EP2791161B1 (en) 2011-12-16 2016-02-10 F.Hoffmann-La Roche Ag Inhibitors of hcv ns5a
RS56212B1 (sr) 2011-12-20 2017-11-30 Riboscience Llc 2',4'-difluoro-2'-metilom supstituisani nukleozidni derivati kao inhibitori replikacije rna hcv-a
CN108409820A (zh) 2011-12-20 2018-08-17 里博科学有限责任公司 作为hcv rna复制抑制剂的4′-叠氮基，3′-氟取代的核苷衍生物
BR112014016157A8 (pt) 2011-12-28 2017-07-04 Janssen R&D Ireland derivados heterobicíclicos como inibidores de vhc
WO2013116339A1 (en) 2012-01-31 2013-08-08 Vertex Pharmaceuticals Incorporated High potency formulations of vx-950
CA2857262A1 (en) 2012-02-24 2013-08-29 F. Hoffmann-La Roche Ag Antiviral compounds
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
CN104704129A (zh) 2012-07-24 2015-06-10 药品循环公司 与对布鲁顿酪氨酸激酶(btk)抑制剂的抗性相关的突变
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
KR20150109451A (ko) 2013-01-23 2015-10-01 에프. 호프만-라 로슈 아게 항바이러스성 트라이아졸 유도체
BR112015021429A2 (pt) 2013-03-05 2017-07-18 Hoffmann La Roche compostos antivirais
US20180200280A1 (en) 2013-05-16 2018-07-19 Riboscience Llc 4'-Fluoro-2'-Methyl Substituted Nucleoside Derivatives as Inhibitors of HCV RNA Replication
KR20160039154A (ko) 2013-05-16 2016-04-08 리보사이언스 엘엘씨 4''-아자이도-3''-데옥시-3''-플루오로 치환된 뉴클레오시드 유도체
MY186547A (en) 2013-05-16 2021-07-26 Riboscience Llc 4?-fluoro-2?-methyl substituted nucleoside derivatives
CN105848680A (zh) 2013-10-25 2016-08-10 药品循环有限责任公司 使用布鲁顿酪氨酸激酶抑制剂和免疫疗法的治疗
EP3119910A4 (en) 2014-03-20 2018-02-21 Pharmacyclics LLC Phospholipase c gamma 2 and resistance associated mutations
JP7299897B2 (ja) 2017-09-21 2023-06-28 リボサイエンス リミティド ライアビリティ カンパニー Ｈｃｖのｒｎａ複製阻害剤としての４’－フルオロ－２’－メチル置換ヌクレオシド誘導体
CA3089630A1 (en) 2018-01-31 2019-08-08 Deciphera Pharmaceuticals, Llc Combination therapy for the treatment of mastocytosis
JP2021512105A (ja) 2018-01-31 2021-05-13 デシフェラ・ファーマシューティカルズ，エルエルシー 消化管間質腫瘍の治療のための併用療法
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
US12012417B2 (en) 2018-06-19 2024-06-18 Novartis Ag N-substituted tetrahydrothienopyridine derivatives and uses thereof
EP3894392A4 (en) * 2018-12-11 2022-08-24 Duke University COMPOSITIONS AND METHODS FOR THE TREATMENT OF CANCER
EP4013412A1 (en) 2019-08-12 2022-06-22 Deciphera Pharmaceuticals, LLC Ripretinib for treating gastrointestinal stromal tumors
WO2021030405A1 (en) 2019-08-12 2021-02-18 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
SI4084778T1 (sl) 2019-12-30 2024-01-31 Deciphera Pharmaceuticals, Llc Formulacije inhibitorja amorfne kinaze in načini njihove uporabe
EP4084779B1 (en) 2019-12-30 2024-10-09 Deciphera Pharmaceuticals, LLC Compositions of 1-(4-bromo-5-(1-ethyl-7-(methylamino)-2-oxo-1,2-dihydro-1,6-naphthyridin-3-yl)-2-fluorophenyl)-3-phenylurea
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
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

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

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