NO312963B1 - Ureaderivater som inhibitorer av IMPDH-enzym - Google Patents

Ureaderivater som inhibitorer av IMPDH-enzym Download PDF

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Publication number
NO312963B1
NO312963B1 NO19984917A NO984917A NO312963B1 NO 312963 B1 NO312963 B1 NO 312963B1 NO 19984917 A NO19984917 A NO 19984917A NO 984917 A NO984917 A NO 984917A NO 312963 B1 NO312963 B1 NO 312963B1
Authority
NO
Norway
Prior art keywords
alkyl
agent
impdh
compound according
compound
Prior art date
Application number
NO19984917A
Other languages
English (en)
Norwegian (no)
Other versions
NO984917L (no
NO984917D0 (no
Inventor
David M Armistead
Michael C Badia
Guy W Bemis
Radny S Bethiel
Catharine A Frank
Perry M Novak
Steven M Ronkin
Jeffrey O 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 NO984917D0 publication Critical patent/NO984917D0/no
Publication of NO984917L publication Critical patent/NO984917L/no
Publication of NO312963B1 publication Critical patent/NO312963B1/no

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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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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)
  • Transplantation (AREA)
  • Biotechnology (AREA)
  • Molecular Biology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Enzymes And Modification Thereof (AREA)
NO19984917A 1996-04-23 1998-10-22 Ureaderivater som inhibitorer av IMPDH-enzym NO312963B1 (no)

Applications Claiming Priority (4)

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
PCT/US1997/006623 WO1997040028A1 (fr) 1996-04-23 1997-04-21 Derives d'uree agissant comme inhibiteurs de l'enzyme impdh

Publications (3)

Publication Number Publication Date
NO984917D0 NO984917D0 (no) 1998-10-22
NO984917L NO984917L (no) 1998-12-23
NO312963B1 true NO312963B1 (no) 2002-07-22

Family

ID=27417590

Family Applications (1)

Application Number Title Priority Date Filing Date
NO19984917A NO312963B1 (no) 1996-04-23 1998-10-22 Ureaderivater som inhibitorer av IMPDH-enzym

Country Status (21)

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

Families Citing this family (160)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CZ298749B6 (cs) * 1996-10-18 2008-01-16 Vertex Pharmaceuticals Incorporated Inhibitory serinových proteáz a farmaceutické prostředky s jejich obsahem
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 (fr) * 1997-03-14 2003-12-03 Vertex Pharmaceuticals Incorporated Inhibiteurs de l'enzyme IMPDH
US6093742A (en) * 1997-06-27 2000-07-25 Vertex Pharmaceuticals, Inc. Inhibitors of p38
NZ503407A (en) * 1997-10-31 2002-08-28 Aventis Pharma Ltd Anilide derivatives useful for treating inflammatory diseases
US7329670B1 (en) 1997-12-22 2008-02-12 Bayer Pharmaceuticals Corporation Inhibition of RAF kinase using aryl and heteroaryl substituted heterocyclic ureas
HUP0101704A3 (en) * 1997-12-22 2002-12-28 Bayer Corp Pittsburgh Kinease substituted heterocyclic ureas with raf inhibition activity and pharmaceutical compositions containing them
WO1999032110A1 (fr) * 1997-12-22 1999-07-01 Bayer Corporation INHIBITION DE L'ACTIVITE DE p38 KINASE AU MOYEN D'UREES HETEROCYCLIQUES ARYLE ET HETEROARYLE SUBSTITUEES
US7517880B2 (en) 1997-12-22 2009-04-14 Bayer Pharmaceuticals Corporation Inhibition of p38 kinase using symmetrical and unsymmetrical diphenyl ureas
EP1076641A1 (fr) * 1998-04-29 2001-02-21 Vertex Pharmaceuticals Incorporated Inhibiteurs de l'enzyme impdh
EP1085010B1 (fr) * 1998-06-04 2004-03-10 Kumiai Chemical Industry Co., Ltd. Derives de phenylacetylene et bactericides a usage agricole ou horticole
SK5222001A3 (en) * 1998-10-22 2002-05-09 Neurosearch As Substituted phenyl derivatives, their preparation and use
JP2002528499A (ja) 1998-10-29 2002-09-03 ブリストル−マイヤーズ スクイブ カンパニー Impdh酵素のインヒビターであるアミノ核誘導化合物
JP2002528533A (ja) 1998-10-29 2002-09-03 ブリストル−マイヤーズ スクイブ カンパニー 酵素impdhの新規なインヒビター
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
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
US6166028A (en) 1998-12-09 2000-12-26 American Home Products Corporation Diaminopuridine-containing thiourea inhibitors of herpes viruses
AU1934600A (en) * 1998-12-09 2000-06-26 Wyeth Alpha-methylbenzyl-containing thiourea inhibitors of herpes viruses containing a phenylenediamine group
CZ20011957A3 (cs) * 1998-12-09 2001-10-17 American Home Products Corporation Thiomočoviny jako inhibitory herpes virů
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
US6337338B1 (en) 1998-12-15 2002-01-08 Telik, Inc. Heteroaryl-aryl ureas as IGF-1 receptor antagonists
EP1142868A4 (fr) * 1998-12-22 2004-09-29 Mitsubishi Chem Corp Derives d'amide
US8124630B2 (en) 1999-01-13 2012-02-28 Bayer Healthcare Llc ω-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
CA2359244C (fr) 1999-01-13 2013-10-08 Bayer Healthcare Llc Diphenyle urees a substitution .omega.-carboxy aryle en tant qu'inhibiteurs de la kinase p38
US7928239B2 (en) 1999-01-13 2011-04-19 Bayer Healthcare Llc Inhibition of RAF kinase using quinolyl, isoquinolyl or pyridyl ureas
EP1140840B1 (fr) 1999-01-13 2006-03-22 Bayer Pharmaceuticals Corp. Diphenylurees a substituants -g(v)-carboxyaryles, inhibitrices de kinase raf
US7351834B1 (en) 1999-01-13 2008-04-01 Bayer Pharmaceuticals Corporation 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
SK13332001A3 (sk) * 1999-03-19 2002-02-05 Vertex Pharmaceuticals Incorporated Inhibítory IMPDH enzýmu a ich použitie
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
DK1196414T3 (da) * 1999-06-25 2003-11-24 Vertex Pharma Prolægemiddel af carbamathæmmer for 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
AU2001255538B2 (en) * 2000-04-24 2006-03-30 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
EP2324825A1 (fr) 2002-02-11 2011-05-25 Bayer Healthcare LLC Arylurées dotées d'une activité d'inhibition de l'angiogenèse
SI1580188T1 (sl) 2002-02-11 2012-02-29 Bayer Healthcare Llc Aril sečnine kot kinazni inhibitorji
EP1402887A1 (fr) * 2002-09-18 2004-03-31 Jerini AG Nouvelles composés pour inhibiter la prolifération non-désirée des cellules, et leurs utilisation
DE60326488D1 (de) * 2002-12-06 2009-04-16 Vertex Pharma Zusammensetzungen die eine kombination von diphenylharnstoff impdh-hemmern und apoptose-induzierenden antikrebsmitteln enthalten
US20040225077A1 (en) 2002-12-30 2004-11-11 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
DE602004007382T2 (de) 2003-05-20 2008-04-17 Bayer Pharmaceuticals Corp., West Haven Diaryl-harnstoffe für durch pdgfr vermittelte krankheiten
DK1663978T3 (da) 2003-07-23 2008-04-07 Bayer Pharmaceuticals Corp Fluorsubstitueret omega-carboxyaryl-diphenylurinstof til behandling og forebyggelse af sygdomme og lidelser
PE20050374A1 (es) * 2003-09-05 2005-05-30 Vertex Pharma Inhibidores de proteasas de serina, en particular proteasa ns3-ns4a del vhc
CA2541634A1 (fr) 2003-10-10 2005-04-28 Vertex Pharmaceuticals Incorporated Inhibiteurs de serine proteases, en particulier la ns3-ns4a protease du hcv
AR045870A1 (es) * 2003-10-11 2005-11-16 Vertex Pharma Terapia de combinacion para la infeccion de virus de hepatitis c
EP1944042A1 (fr) 2003-10-27 2008-07-16 Vertex Pharmceuticals Incorporated Combinaisons pour le traitement HCV
JP4890254B2 (ja) 2003-10-27 2012-03-07 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 Hcvns3−ns4aプロテアーゼ耐性突然変異体
EP2311851A3 (fr) 2004-02-04 2011-05-25 Vertex Pharmaceuticals Incorporated Inhibitoren der Serinproteasen, insbesondere der HCV-NS3-NS4A-Protease
US7317030B2 (en) 2004-02-26 2008-01-08 4Sc Ag Compounds as inhibitors of cell proliferation and viral infections
EP1568696A1 (fr) * 2004-02-26 2005-08-31 4Sc Ag Composés comme inhibiteurs de prolifération de cellules et d'infections virales
WO2006115509A2 (fr) 2004-06-24 2006-11-02 Novartis Vaccines And Diagnostics Inc. Immuno-potentialisateurs a petites molecules et analyses visant a detecter leur presence
DE602005010714D1 (de) 2004-08-12 2008-12-11 Pfizer Der p38-map-kinase
CA2583472A1 (fr) * 2004-10-01 2006-04-13 Chao Lin Inhibition de la protease ns3-ns4a du vhc
MY141025A (en) 2004-10-29 2010-02-25 Vertex Pharma Dose forms
TWI378925B (en) * 2005-01-14 2012-12-11 Gilead Connenticut Inc Certain 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
US20060235070A1 (en) * 2005-02-08 2006-10-19 Hayden Michael R Compositions and methods for treating vascular, autoimmune, and inflammatory diseases
WO2006086498A2 (fr) * 2005-02-08 2006-08-17 Aspreva Pharmaceuticals Sa Traitement de maladies vasculaires, auto-immunes et inflammatoires, a l'aide de faibles doses d'inhibiteurs de l'impdh
KR101335932B1 (ko) 2005-03-07 2013-12-04 바이엘 헬스케어 엘엘씨 암의 치료를 위한 오메가-카르복시아릴 치환된 디페닐우레아를 포함하는 제약 조성물
WO2007024294A2 (fr) * 2005-05-03 2007-03-01 Cgi Pharmaceuticals, Inc. Certains urees substitues, modulateurs de l'activite des kinases
CA2606507A1 (fr) * 2005-05-09 2006-11-16 Vertex Pharmaceuticals Incorporated Formes polymorphiques de (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
PE20070211A1 (es) 2005-07-29 2007-05-12 Medivir Ab 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
DK1919904T3 (da) 2005-07-29 2014-04-07 Janssen R & D Ireland Makrocykliske inhibitorer af hepatitis-c-virus
US20100120855A1 (en) 2005-07-29 2010-05-13 Tibotec Pharmaceuticals Ltd. Macrocylic 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
ES2373685T3 (es) 2005-07-29 2012-02-07 Tibotec Pharmaceuticals Inhibidores macrocíclicos del virus de la hepatitis c.
PL1919898T3 (pl) 2005-07-29 2011-06-30 Tibotec Pharm Ltd Makrocykliczne inhibitory wirusa zapalenia wątroby typu C
DK1919899T3 (da) 2005-07-29 2011-08-01 Tibotec Pharm Ltd Makrocykliske inhibitorer af hepatitis C virus
TWI412535B (zh) 2005-07-29 2013-10-21 Tibotec Pharm Ltd C型肝炎病毒之大環抑制劑(五)
CA2617679A1 (fr) * 2005-08-02 2007-02-08 Steve Lyons Inhibiteurs des serines 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
US7964624B1 (en) * 2005-08-26 2011-06-21 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases
AU2006315438A1 (en) 2005-11-11 2007-05-24 Vertex Pharmaceuticals Incorporated Hepatitis C virus variants
US7705138B2 (en) 2005-11-11 2010-04-27 Vertex Pharmaceuticals Incorporated Hepatitis C virus variants
CA2643688A1 (fr) 2006-02-27 2007-08-30 Vertex Pharmaceuticals Incorporated Co-cristaux et compositions pharmaceutiques les comprenant
WO2007109080A2 (fr) 2006-03-16 2007-09-27 Vertex Pharmaceuticals Incorporated Inhibiteurs de protéase de l'hépatite c deutérés
CA2643680A1 (fr) 2006-04-11 2007-11-22 Novartis Ag Composes organiques et leurs utilisations
EP2066642A1 (fr) * 2006-09-25 2009-06-10 Arete Therapeutics, INC. Inhibiteurs d'époxyde hydrolase soluble
EP2097084B1 (fr) 2006-10-04 2015-01-28 Janssen R&D Ireland Carboxamide 4-[(4-pyridyl)amino] pyrimidines pour le traitement de l'hépatite c
CA2661338C (fr) 2006-11-17 2015-05-12 Tibotec Pharmaceuticals Ltd. Inhibiteurs macrocycliques du virus de l'hepatite c
WO2008106058A2 (fr) * 2007-02-27 2008-09-04 Vertex Pharmaceuticals Incorporated Inhibiteurs de sérine protéases
GEP20125645B (en) * 2007-02-27 2012-09-25 Vertex Pharma Co-crystals and pharmaceutical compositions comprising the same
CA2684950A1 (fr) * 2007-04-20 2008-10-30 Deciphera Pharmaceuticals, Llc Inhibiteurs de kinases utiles pour le traitement des maladies myeloproliferatives et d'autres maladies proliferatives
ES2381410T3 (es) 2007-05-04 2012-05-28 Vertex Pharmceuticals Incorporated Terapia de combinación paa el tratamiento de infecciones por VHC
WO2009032198A1 (fr) * 2007-08-30 2009-03-12 Vertex Pharmaceuticals Incorporated Co-cristaux et compositions pharmaceutiques les comportant
US8524716B2 (en) 2007-12-24 2013-09-03 Janssen R&D Ireland Macrocyclic indoles as hepatitis C virus inhibitors
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
PL2331554T3 (pl) 2008-08-14 2013-08-30 Janssen R&D Ireland Makrocykliczne pochodne indolu użyteczne jako inhibitory wirusa zapalenia wątroby typu C
BRPI0922366B8 (pt) 2008-12-03 2021-05-25 Presidio Pharmaceuticals Inc composto, composição farmacêutica e uso de um composto
EP2774927A1 (fr) 2008-12-03 2014-09-10 Presidio Pharmaceuticals, Inc. Inhibiteurs du virus de l'hépatite C de type NS5A
EP2396028A2 (fr) 2009-02-12 2011-12-21 Vertex Pharmceuticals Incorporated Polythérapie contre le hcv comprenant de l'interféron pégylé, de la ribavirine et de la telaprevir
EP2408753A4 (fr) * 2009-03-20 2012-11-07 Univ Brandeis Composés et procédés pour traiter les infections microbiennes gastro-intestinales mammaliennes
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
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
CN102844030A (zh) 2010-01-29 2012-12-26 沃泰克斯药物股份有限公司 用于治疗丙型肝炎病毒感染的疗法
WO2011112516A1 (fr) 2010-03-08 2011-09-15 Ico Therapeutics Inc. Traitement et prévention de l'infection par le virus de l'hépatite c en utilisant des oligonucléotides antisens de la kinase c-raf
EP2575866A4 (fr) 2010-05-24 2013-10-16 Presidio Pharmaceuticals Inc Inhibiteurs de ns5a du vhc
NZ772688A (en) 2010-06-03 2022-09-30 Pharmacyclics Llc The use of inhibitors of bruton’s tyrosine kinase (btk)
WO2011156545A1 (fr) 2010-06-09 2011-12-15 Vertex Pharmaceuticals Incorporated Modèle dynamique viral pour une polythérapie contre le vhc
WO2011161232A1 (fr) 2010-06-24 2011-12-29 Tibotec Pharmaceuticals Préparation d'acide 13-cyclohexyl-3-méthoxy-6-[méthyl-(2-{2-[méthyl-(sulfamoyl)-amino]- éthoxy}-éthyl)-carbamoyl]-7h-indolo-[2,1-a]-[2]-benzazépine-10- carboxylique
EP2593105A1 (fr) 2010-07-14 2013-05-22 Vertex Pharmaceuticals Incorporated Composition pharmaceutique au goût agréable comprenant vx-950
WO2012020036A1 (fr) 2010-08-13 2012-02-16 F. Hoffmann-La Roche Ag Inhibiteurs du virus de l'hépatite c
WO2012109646A1 (fr) 2011-02-11 2012-08-16 Vertex Pharmaceuticals Incorporated Traitement du vhc chez des patients infectés par le vih
WO2012116370A1 (fr) 2011-02-25 2012-08-30 Medtronic, Inc. Procédés et systèmes utilisant des profils pharmacocinétiques et pharmacodynamiques dans régimes thérapeutiques d'interféron-alpha
WO2012123298A1 (fr) 2011-03-11 2012-09-20 F. Hoffmann-La Roche Ag Composés antiviraux
WO2012175700A1 (fr) 2011-06-23 2012-12-27 Digna Biotech, S. L. Traitement de l'hépatite c chronique avec ifn-a5 en combinaison avec ifn-a2b dans une cohorte de patients
US20120328565A1 (en) 2011-06-24 2012-12-27 Brinkman John A Antiviral compounds
CA2847083A1 (fr) 2011-10-10 2013-04-18 F. Hoffmann-La Roche Ag Composes antiviraux
US9133170B2 (en) 2011-12-16 2015-09-15 Hoffmann-La Roche Inc. Inhibitors of HCV NS5A
UA111761C2 (uk) 2011-12-20 2016-06-10 Рібосаєнс Ллс 2',4'-дифтор-2'-метилзаміщені нуклеозидні похідні як інгібітори реплікації phk вірусу гепатиту c
US9708357B2 (en) 2011-12-20 2017-07-18 Riboscience, LLC 4′-azido, 3′-fluoro substituted nucleoside derivatives as inhibitors of HCV RNA replication
BR112014016157A8 (pt) 2011-12-28 2017-07-04 Janssen R&D Ireland derivados heterobicíclicos como inibidores de vhc
US20130195797A1 (en) 2012-01-31 2013-08-01 Vertex Pharmaceuticals Incorporated High potency formulations of vx-950
EP2817291A1 (fr) 2012-02-24 2014-12-31 F. Hoffmann-La Roche AG Composés antiviraux
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
AU2013293087B2 (en) 2012-07-24 2017-08-31 Pharmacyclics Llc Mutations associated with resistance to inhibitors of Bruton's tyrosine kinase (BTK)
US9447134B2 (en) 2012-08-17 2016-09-20 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
WO2014135422A1 (fr) 2013-03-05 2014-09-12 F. Hoffmann-La Roche Ag Composés antiviraux
US20180200280A1 (en) 2013-05-16 2018-07-19 Riboscience Llc 4'-Fluoro-2'-Methyl Substituted Nucleoside Derivatives as Inhibitors of HCV RNA Replication
HK1219901A1 (zh) 2013-05-16 2017-04-21 Riboscience Llc 4’-叠氮基,3’-脱氧基-3’-氟取代的核苷衍生物
MA46490A1 (fr) 2013-05-16 2021-04-30 Riboscience Llc Dérivés de nucléosides 4'- fluoro-2' - méthyle substitués
TWI617309B (zh) 2013-10-25 2018-03-11 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 (fr) 2014-03-20 2015-09-24 Pharmacyclics Inc. Mutations de phospholipase c gamma 2 et associees aux resistances
AU2018335411B2 (en) 2017-09-21 2024-06-27 Riboscience Llc 4'-fluoro-2'-methyl substituted nucleoside derivatives as inhibitors of HCV RNA replication
EP3746059B1 (fr) 2018-01-31 2026-03-04 Deciphera Pharmaceuticals, LLC Polythérapie pour le traitement de tumeurs stromales gastro-intestinales
AU2019216351B2 (en) 2018-01-31 2024-07-25 Deciphera Pharmaceuticals, Llc Combination therapy for the treatment of mastocytosis
JP2021519334A (ja) 2018-03-26 2021-08-10 クリア クリーク バイオ, インコーポレイテッド ジヒドロオロト酸デヒドロゲナーゼを阻害するための組成物および方法
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
EA202190046A1 (ru) 2018-06-19 2021-03-24 Новартис Аг N-замещенные производные тетрагидротиенопиридина и их применение
EP3894392A4 (fr) * 2018-12-11 2022-08-24 Duke University Compositions et procédés pour le traitement du cancer
WO2020185812A1 (fr) 2019-03-11 2020-09-17 Teva Pharmaceuticals International Gmbh Formes à l'état solide de riprétinib
FI4013412T3 (fi) 2019-08-12 2026-03-24 Deciphera Pharmaceuticals Llc Ripretinibi ruoansulatuskanavan stroomakasvaimien hoitoon
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
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
PL4084779T3 (pl) 2019-12-30 2025-02-24 Deciphera Pharmaceuticals, Llc Kompozycje 1-(4-bromo-5-(1-etylo-7-(metyloamino)-2-okso-1,2-dihydro-1,6-naftyrydyn-3-ylo)-2-fluorofenylo)-3-fenylomocznika
AU2020419197B2 (en) 2019-12-30 2023-08-31 Deciphera Pharmaceuticals, Llc Amorphous kinase inhibitor formulations and methods of use thereof
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

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
CA985286A (en) 1971-05-04 1976-03-09 Charles J. Paget (Jr.) (substituted anilino) benzoxazoles useful in the prophylaxis of mareks disease
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 (fr) 1992-11-24 1994-06-09 Syntex (U.S.A.) Inc. Utilisation d'acide mycophenolique, de mofetile de mycophenolate ou d'un derive de ceux-ci pour inhiber la stenose
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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US6967214B2 (en) 2005-11-22
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US7329681B2 (en) 2008-02-12
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AP813A (en) 2000-02-28
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