AP797A - Inhibitors of interleukin-1B converting enzyme. - Google Patents

Inhibitors of interleukin-1B converting enzyme. Download PDF

Info

Publication number
AP797A
AP797A APAP/P/1997/000960A AP9700960A AP797A AP 797 A AP797 A AP 797A AP 9700960 A AP9700960 A AP 9700960A AP 797 A AP797 A AP 797A
Authority
AP
ARIPO
Prior art keywords
ice
inhibitors
group
binding pocket
compounds
Prior art date
Application number
APAP/P/1997/000960A
Other languages
English (en)
Other versions
AP9700960A0 (en
Inventor
Guy Bemis
Julian M Golec
David J Lauffer
Michael D Mullican
Mark A Murcko
David J Livingstone
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 US08/261,452 external-priority patent/US5756466A/en
Priority claimed from US08/440,898 external-priority patent/US5847135A/en
Application filed by Vertex Pharma filed Critical Vertex Pharma
Publication of AP9700960A0 publication Critical patent/AP9700960A0/xx
Application granted granted Critical
Publication of AP797A publication Critical patent/AP797A/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0202Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • 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
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Peptides Or Proteins (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Paper (AREA)
APAP/P/1997/000960A 1994-06-17 1995-06-16 Inhibitors of interleukin-1B converting enzyme. AP797A (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US08/261,452 US5756466A (en) 1994-06-17 1994-06-17 Inhibitors of interleukin-1β converting enzyme
US08/405,581 US5656627A (en) 1994-06-17 1995-03-17 Inhibitors of interleukin-1β converting enzyme
US08/440,898 US5847135A (en) 1994-06-17 1995-05-25 Inhibitors of interleukin-1β converting enzyme
PCT/US1995/007617 WO1995035308A1 (en) 1994-06-17 1995-06-16 INHIBITORS OF INTERLEUKIN-1β CONVERTING ENZYME

Publications (2)

Publication Number Publication Date
AP9700960A0 AP9700960A0 (en) 1997-04-30
AP797A true AP797A (en) 2000-01-07

Family

ID=27401408

Family Applications (1)

Application Number Title Priority Date Filing Date
APAP/P/1997/000960A AP797A (en) 1994-06-17 1995-06-16 Inhibitors of interleukin-1B converting enzyme.

Country Status (22)

Country Link
US (2) US5716929A (pl)
EP (1) EP0784628A1 (pl)
JP (1) JP4190029B2 (pl)
CN (1) CN1192035C (pl)
AP (1) AP797A (pl)
AU (1) AU709114B2 (pl)
BG (1) BG63634B1 (pl)
BR (1) BR9508051A (pl)
CA (1) CA2192089C (pl)
CZ (1) CZ298625B6 (pl)
FI (1) FI965036A7 (pl)
GE (1) GEP20012446B (pl)
HU (1) HUT76622A (pl)
IL (1) IL114015A0 (pl)
IS (1) IS4399A (pl)
MA (1) MA24511A1 (pl)
MX (1) MX9606546A (pl)
NZ (1) NZ289560A (pl)
PL (1) PL185693B1 (pl)
SK (1) SK287422B6 (pl)
TW (1) TW509698B (pl)
WO (1) WO1995035308A1 (pl)

Families Citing this family (144)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5874424A (en) * 1995-12-20 1999-02-23 Vertex Pharmaceuticals Incorporated Inhibitors of interleukin-1β converting enzyme
US6204261B1 (en) * 1995-12-20 2001-03-20 Vertex Pharmaceuticals Incorporated Inhibitors of interleukin-1β Converting enzyme inhibitors
US5846981A (en) * 1993-05-28 1998-12-08 Gpi Nil Holdings Inc. Inhibitors of rotamase enzyme activity
US5798355A (en) * 1995-06-07 1998-08-25 Gpi Nil Holdings, Inc. Inhibitors of rotamase enzyme activity
US6420522B1 (en) * 1995-06-05 2002-07-16 Vertex Pharmaceuticals Incorporated Inhibitors of interleukin-1β converting enzyme
US6245764B1 (en) 1995-03-24 2001-06-12 Molecumetics Ltd. β-sheet mimetics and use thereof as inhibitors of biologically active peptides or proteins
US6699869B1 (en) 1995-03-24 2004-03-02 Myriad Genetics Inc. β-sheet mimetics and use thereof as inhibitors of biologically active peptides or proteins
US6020331A (en) * 1995-03-24 2000-02-01 Molecumetics, Ltd. β-sheet mimetics and use thereof as protease inhibitors
EP0820464A2 (en) * 1995-03-31 1998-01-28 Takeda Chemical Industries, Ltd. Cysteine protease inhibitor
US5696135A (en) * 1995-06-07 1997-12-09 Gpi Nil Holdings, Inc. Inhibitors of rotamase enzyme activity effective at stimulating neuronal growth
US5859031A (en) * 1995-06-07 1999-01-12 Gpi Nil Holdings, Inc. Small molecule inhibitors of rotamase enzyme activity
US5744451A (en) * 1995-09-12 1998-04-28 Warner-Lambert Company N-substituted glutamic acid derivatives with interleukin-1 β converting enzyme inhibitory activity
US5801197A (en) * 1995-10-31 1998-09-01 Gpi Nil Holdings, Inc. Rotamase enzyme activity inhibitors
US5843904A (en) * 1995-12-20 1998-12-01 Vertex Pharmaceuticals, Inc. Inhibitors of interleukin-1βconverting enzyme
US5834457A (en) * 1996-01-26 1998-11-10 The Regents Of The University Of California Method of modulating radical formation by mutant cuznsod enzymes
US6117896A (en) * 1997-02-10 2000-09-12 Molecumetics Ltd. Methods for regulating transcription factors
KR20000029838A (ko) * 1996-08-05 2000-05-25 몰레큐메틱스 리미티드 프로테아제및키나제억제제로서그리고전사인자억제제로서의베타-시트유사체의용도
EP1661566A3 (en) * 1996-08-05 2008-04-16 Myriad Genetics, Inc. Use of beta-sheet mimetics as protease and kinase inhibitors and as inhibitors of transcription factors
US5869519A (en) * 1996-12-16 1999-02-09 Idun Pharmaceuticals, Inc. C-terminal modified (n-substituted)-2-indolyl dipeptides as inhibitors of the ICE/ced-3 family of cysteine proteases
US5801187A (en) 1996-09-25 1998-09-01 Gpi-Nil Holdings, Inc. Heterocyclic esters and amides
US6218424B1 (en) 1996-09-25 2001-04-17 Gpi Nil Holdings, Inc. Heterocyclic ketone and thioester compounds and uses
US5786378A (en) * 1996-09-25 1998-07-28 Gpi Nil Holdings, Inc. Heterocyclic thioesters
US5919790A (en) * 1996-10-11 1999-07-06 Warner-Lambert Company Hydroxamate inhibitors of interleukin-1β converting enzyme
US6262047B1 (en) 1996-10-11 2001-07-17 Cor Therapeutics, Inc. Selective factor Xa inhibitors
EP0932600B1 (en) * 1996-10-11 2006-02-08 Warner-Lambert Company Llc Sulfonamide substituted aspartic acid interleukin-1beta converting enzyme inhibitors
US6063794A (en) 1996-10-11 2000-05-16 Cor Therapeutics Inc. Selective factor Xa inhibitors
US6369080B2 (en) 1996-10-11 2002-04-09 Cor Therapeutics, Inc. Selective factor Xa inhibitors
US6194435B1 (en) 1996-10-11 2001-02-27 Cor Therapeutics, Inc. Lactams as selective factor Xa inhibitors
KR20000049047A (ko) 1996-10-11 2000-07-25 로즈 암스트롱, 크리스틴 에이. 트러트웨인 술폰아미드 인터루킨-1β 전환 효소 억제제
CN1133649C (zh) * 1996-10-18 2004-01-07 沃泰克斯药物股份有限公司 丝氨酸蛋白酶、特别是丙型肝炎病毒ns3蛋白酶的抑制剂
EP1136498A1 (en) * 1996-10-18 2001-09-26 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hepatitis c virus NS3 protease
US6080738A (en) * 1996-10-25 2000-06-27 Yoshitomi Pharmaceuticals Industries, Ltd. Heterocyclic amide compounds and medicinal uses thereof
JP4094066B2 (ja) * 1996-12-06 2008-06-04 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 インターロイキン−1β変換酵素のインヒビター
EP1466921A1 (en) * 1996-12-06 2004-10-13 Vertex Pharmaceuticals Incorporated Inhibitors of interleukin-1 beta converting enzyme
PT944645E (pt) * 1996-12-06 2005-06-30 Vertex Pharma Inibidores da enzima conversora de interleucina 1beta
US6184244B1 (en) 1996-12-16 2001-02-06 Idun Pharmaceuticals, Inc. C-terminal modified (N-substituted)-2-indolyl dipeptides as inhibitors of the ICE/ced-3 family of cysteine proteases
US5877197A (en) * 1996-12-16 1999-03-02 Karanewsky; Donald S. C-terminal modified (N-substituted)-2-indolyl dipeptides as inhibitors of the ICE/ced-3 family of cysteine proteases
US5846979A (en) 1997-02-28 1998-12-08 Gpi Nil Holdings, Inc. N-oxides of heterocyclic esters, amides, thioesters, and ketones
US6054487A (en) * 1997-03-18 2000-04-25 Basf Aktiengesellschaft Methods and compositions for modulating responsiveness to corticosteroids
CA2285705A1 (en) * 1997-04-14 1998-10-22 Cor Therapeutics, Inc. Selective factor xa inhibitors
AU6896398A (en) 1997-04-14 1998-11-11 Cor Therapeutics, Inc. Selective factor xa inhibitors
EP0977772A1 (en) 1997-04-14 2000-02-09 Cor Therapeutics, Inc. SELECTIVE FACTOR Xa INHIBITORS
HUP9700816A3 (en) * 1997-04-28 1999-06-28 Gyogyszerkutato Intezet 3(r)-3-amino-4-carboxy-butiraldehyde derivatives inhibiting release of interleukin-1-beta
US20010049381A1 (en) 1997-06-04 2001-12-06 Gpl Nil Holdings, Inc., Pyrrolidine derivative hair growth compositions and uses
FR2766188B1 (fr) * 1997-07-15 2000-02-11 Hoechst Marion Roussel Inc Nouveau procede de preparation de derives amines d'alkyloxy furanone, composes issus de ce procede et utilisation de ces composes
US6218382B1 (en) 1997-08-11 2001-04-17 Cor Therapeutics, Inc Selective factor Xa inhibitors
US6333321B1 (en) 1997-08-11 2001-12-25 Cor Therapeutics, Inc. Selective factor Xa inhibitors
US6228854B1 (en) 1997-08-11 2001-05-08 Cor Therapeutics, Inc. Selective factor Xa inhibitors
ATE267168T1 (de) * 1997-11-24 2004-06-15 Merck & Co Inc Beta-alanin-derivate als zell-adhäsions- inhibitoren
US6645939B1 (en) 1997-11-24 2003-11-11 Merck & Co., Inc. Substituted β-alanine derivatives as cell adhesion inhibitors
DE69839221T2 (de) * 1997-12-18 2009-04-30 Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield Pyridone als hemmer der sh2-domäne der src-familie
DE69925581T2 (de) 1998-03-09 2006-04-27 Vertex Pharmaceuticals Inc., Cambridge 1,2-diazepanderivate als inhibitoren des interleukin-1beta umwandelnden enzyms
TR200103406T2 (tr) * 1998-03-19 2002-06-21 Vertex Pharmaceuticals Incorporated Kaspaz inhibitörleri.
GB9809664D0 (en) * 1998-05-06 1998-07-01 Hoffmann La Roche a-Ketoamide derivatives
US6331537B1 (en) 1998-06-03 2001-12-18 Gpi Nil Holdings, Inc. Carboxylic acids and carboxylic acid isosteres of N-heterocyclic compounds
CN1295561A (zh) 1998-06-03 2001-05-16 Gpinil控股公司 N-杂环羧酸或羧酸等排物的n-结合氨磺酰
US6337340B1 (en) 1998-08-14 2002-01-08 Gpi Nil Holdings, Inc. Carboxylic acids and isosteres of heterocyclic ring compounds having multiple heteroatoms for vision and memory disorders
US6399648B1 (en) 1998-08-14 2002-06-04 Gpi Nil Holdings, Inc. N-oxides of heterocyclic ester, amide, thioester, or ketone for vision and memory disorders
US6506788B1 (en) 1998-08-14 2003-01-14 Gpi Nil Holdings, Inc. N-linked urea or carbamate of heterocyclic thioesters for vision and memory disorders
US6376517B1 (en) 1998-08-14 2002-04-23 Gpi Nil Holdings, Inc. Pipecolic acid derivatives for vision and memory disorders
US7338976B1 (en) 1998-08-14 2008-03-04 Gpi Nil Holdings, Inc. Heterocyclic esters or amides for vision and memory disorders
US6333340B1 (en) 1998-08-14 2001-12-25 Gpi Nil Holdings, Inc. Small molecule sulfonamides for vision and memory disorders
US6384056B1 (en) 1998-08-14 2002-05-07 Gpi Nil Holdings, Inc. Heterocyclic thioesters or ketones for vision and memory disorders
US6395758B1 (en) 1998-08-14 2002-05-28 Gpi Nil Holdings, Inc. Small molecule carbamates or ureas for vision and memory disorders
US6335348B1 (en) 1998-08-14 2002-01-01 Gpi Nil Holdings, Inc. Nitrogen-containing linear and azepinyl/ compositions and uses for vision and memory disorders
US6218423B1 (en) 1998-08-14 2001-04-17 Gpi Nil Holdings, Inc. Pyrrolidine derivatives for vision and memory disorders
US6339101B1 (en) 1998-08-14 2002-01-15 Gpi Nil Holdings, Inc. N-linked sulfonamides of N-heterocyclic carboxylic acids or isosteres for vision and memory disorders
US6177565B1 (en) * 1998-08-19 2001-01-23 Vertex Pharmaceuticals Inc. Process for synthesizing piperazic acid
US6559304B1 (en) * 1998-08-19 2003-05-06 Vertex Pharmaceuticals Incorporated Method for synthesizing caspase inhibitors
US6201118B1 (en) 1998-08-19 2001-03-13 Vertex Pharmaceuticals Inc. Process for forming an N-acylated, N,N-containing bicyclic ring from piperazic acid or an ester thereof especially useful as an intermediate in the manufacture of a caspase inhibitor
US6462072B1 (en) 1998-09-21 2002-10-08 Gpi Nil Holdings, Inc. Cyclic ester or amide derivatives
JP2003524603A (ja) * 1998-10-06 2003-08-19 スミスクライン・ビーチャム・コーポレイション カスパーゼおよびアポトーシス
WO2000032620A1 (en) * 1998-12-02 2000-06-08 Merck Frosst Canada & Co. Gamma-ketoacid tetrapeptides as inhibitors of caspase-3
JP2002538151A (ja) 1999-03-02 2002-11-12 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド カテプシンの可逆的インヒビターとして有用な化合物
TW200404789A (en) * 1999-03-15 2004-04-01 Axys Pharm Inc Novel compounds and compositions as protease inhibitors
US6724942B1 (en) 1999-05-24 2004-04-20 Fuji Photo Film Co., Ltd. Image processing method and system
ATE344249T1 (de) * 1999-07-19 2006-11-15 Merck Frosst Canada Ltd Pyrazinone, diese verbindungen enthaltende zusammenstellungen
US6420364B1 (en) 1999-09-13 2002-07-16 Boehringer Ingelheim Pharmaceuticals, Inc. Compound useful as reversible inhibitors of cysteine proteases
US7253169B2 (en) 1999-11-12 2007-08-07 Gliamed, Inc. Aza compounds, pharmaceutical compositions and methods of use
US6417189B1 (en) 1999-11-12 2002-07-09 Gpi Nil Holdings, Inc. AZA compounds, pharmaceutical compositions and methods of use
US6358928B1 (en) 1999-11-22 2002-03-19 Enzyme Systems Products Peptidyl sulfonyl imidazolides as selective inhibitors of serine proteases
CA2393466C (en) 1999-12-21 2010-01-19 Gpi Nil Holdings, Inc. Hydantoin derivative compounds, pharmaceutical compositions, and methods of using same
AU2001257006A1 (en) 2000-04-11 2001-10-23 Du Pont Pharmaceuticals Company Substituted lactams as inhibitors of abeta protein production
EP1712239A3 (en) * 2000-05-12 2007-08-22 Immunex Corporation Interleukin-1 inhibitors in the treatment of diseases
PE20011350A1 (es) 2000-05-19 2002-01-15 Vertex Pharma PROFARMACO DE UN INHIBIDOR DE ENZIMA CONVERTIDORA DE INTERLEUCINA-1ß (ICE)
AU783857B2 (en) 2000-06-01 2005-12-15 Bristol-Myers Squibb Pharma Company Lactams substituted by cyclic succinates as inhibitors of a beta protein production
EP1289993B9 (en) 2000-06-07 2008-08-20 Vertex Pharmaceuticals Incorporated Caspase inhibitors and uses thereof
SV2003000617A (es) 2000-08-31 2003-01-13 Lilly Co Eli Inhibidores de la proteasa peptidomimetica ref. x-14912m
NZ526420A (en) * 2000-11-21 2005-08-26 Vertex Pharma Imidazole and benzimidazole caspase inhibitors and uses thereof
AU2002230763A1 (en) * 2000-12-13 2008-01-03 Bristol-Myers Squibb Pharma Company Inhibitors of hepatitis c virus ns3 protease
US6653295B2 (en) 2000-12-13 2003-11-25 Bristol-Myers Squibb Company Inhibitors of hepatitis C virus NS3 protease
AUPR215700A0 (en) * 2000-12-19 2001-01-25 Fujisawa Pharmaceutical Co., Ltd. Carboxylic acid compound having cyclopropane ring
US20050192228A1 (en) * 2001-02-05 2005-09-01 Jean Rapin Tripeptide derivatives for the treatment of neurodegenerative diseases
DE10105040A1 (de) * 2001-02-05 2002-08-14 Tell Pharm Ag Hergiswil Tripeptid-Derivate für die Behandlung von postläsionalen Krankheiten des Nervensystems
DE10105041A1 (de) * 2001-02-05 2002-08-14 Tell Pharm Ag Hergiswil Tripeptide und Tripeptid-Derivate für die Behandlung neurodegenerativer Krankheiten
DE10105038B4 (de) * 2001-02-05 2005-07-07 Neurotell Ag Tripeptid-Derivate für die Behandlung von postläsionalen Krankheiten des Nervensystems
DE10105039A1 (de) * 2001-02-05 2002-08-08 Tell Pharm Ag Hergiswil Tripeptid-Derivate für die Behandlung neurodegenerativer Krankheiten
WO2002094787A1 (en) * 2001-05-23 2002-11-28 Ucb, S.A. 2-oxo-piperidinyl- and 2-oxo-azepanyl alkanoic acid derivativ es for the treatment of epilepsy and other neurological disorders
GB0129260D0 (en) 2001-12-06 2002-01-23 Eisai London Res Lab Ltd Pharmaceutical compositions and their uses
JP2005170790A (ja) * 2002-01-09 2005-06-30 Ajinomoto Co Inc N−アルキルスルフォニル置換アミド誘導体
AU2003211052A1 (en) * 2002-02-11 2003-09-04 Vertex Pharmaceuticals Incorporated Phospholipids as caspase inhibitor prodrugs
WO2003068237A1 (en) 2002-02-14 2003-08-21 Myriad Genetics, Inc. Beta-sheet mimetics and composition and methods relating thereto
AU2003231012B2 (en) * 2002-04-22 2008-05-08 University Of Maryland, Baltimore County Antiviral inhibitions of capsid proteins
US7138395B2 (en) * 2002-06-10 2006-11-21 The Procter & Gamble Company Interleukin-1β converting enzyme inhibitors
US7001899B2 (en) * 2002-06-10 2006-02-21 The Procter & Gamble Company Interleukin converting enzyme inhibitors
US7094783B2 (en) * 2002-06-26 2006-08-22 Bristol-Myers Squibb Company Bicyclic pyrimidinones as coagulation cascade inhibitors
WO2004002405A2 (en) 2002-06-26 2004-01-08 Bristol-Myers Squibb Company Amino-bicyclic pyrazinones and pyridinones
BR0312232A (pt) * 2002-06-28 2005-05-10 Vertex Pharma Inibidores de caspases e seus usos
JP4675628B2 (ja) * 2002-12-20 2011-04-27 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 4−オキソ−3−(1−オキソ−1h−イソキノリン−2−イルアセチルアミノ)−ペンタン酸のエステル誘導体およびアミド誘導体、ならびにカスパーゼインヒビターとしてのそれらの使用
PE20050159A1 (es) 2003-05-27 2005-04-19 Vertex Pharma Derivados de acido 3-[2-(3-amino-2-oxo-2h-piridin-1-il)-acetilamino]-4-oxo-pentanoico como inhibidores de caspasa
MY148123A (en) 2003-09-05 2013-02-28 Vertex Pharma Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
AU2011226946B2 (en) * 2004-02-27 2012-05-03 Vertex Pharmaceuticals Incoporated Caspase Inhibitors and Uses Thereof
CA2820541A1 (en) * 2004-02-27 2005-09-15 Vertex Pharmaceuticals Incorporated Caspase inhibitors and uses thereof
CN102161656B (zh) 2004-02-27 2013-02-20 沃泰克斯药物股份有限公司 天冬氨酸特异性半胱氨酸蛋白酶抑制剂及其用途
CA2559303C (en) 2004-03-12 2013-09-10 Vertex Pharmaceuticals Incorporated Processes and intermediates for the preparation of aspartic acetal caspase inhibitors
CN102362867A (zh) 2004-05-15 2012-02-29 沃泰克斯药物股份有限公司 使用ice抑制剂治疗癫痫发作
GB0411056D0 (en) 2004-05-18 2004-06-23 Novartis Ag Organic compounds
EP1778221A2 (en) 2004-05-27 2007-05-02 Vertex Pharmaceuticals Incorporated Ice inhibitors for the treatment of autoinflammatory diseases
CN101098855B (zh) * 2004-11-24 2012-06-06 沃泰克斯药物股份有限公司 3-[2-(3-酰氨基-2-氧代-2h-吡啶-1-基)-乙酰氨基]-4-氧代-戊酸衍生物及其作为天冬氨酸特异性半胱氨酸蛋白酶抑制剂的用途
JPWO2006126730A1 (ja) * 2005-05-26 2008-12-25 味の素株式会社 二環式ピリミジン化合物及びその製造方法
JP2009502922A (ja) 2005-07-28 2009-01-29 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 カスパーゼ阻害剤プロドラッグ
EP2402331A1 (en) * 2005-08-02 2012-01-04 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
US8039475B2 (en) 2006-02-27 2011-10-18 Vertex Pharmaceuticals Incorporated Co-crystals and pharmaceutical compositions comprising the same
KR20080112303A (ko) * 2006-03-16 2008-12-24 버텍스 파마슈티칼스 인코포레이티드 중수소화 c형 간염 프로테아제 억제제
PT2114924E (pt) * 2007-02-27 2012-04-03 Vertex Pharma Co-cristais e composições farmacêuticas que compreendem os mesmos
EP2134717A2 (en) * 2007-02-27 2009-12-23 Vertex Pharmceuticals Incorporated Inhibitors of serine proteases
JP5443360B2 (ja) * 2007-08-30 2014-03-19 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 共結晶体およびそれを含む医薬組成物
TW200920355A (en) * 2007-09-06 2009-05-16 Lexicon Pharmaceuticals Inc Compositions and methods for treating immunological and inflammatory diseases and disorders
ES2700613T3 (es) * 2008-07-16 2019-02-18 Bitop Ag Síntesis de amidinas cíclicas
EP2635906A4 (en) 2010-11-05 2014-04-02 Univ Brandeis Ice inhibiting compounds and uses thereof
HU1000676D0 (en) * 2010-12-17 2011-02-28 Pharmahungary 2000 Kft Inhibitors of matrix metalloproteinase, pharmaceutical compositions thereof and use of them for preventing and treating diseases where the activation of mmp is involved
US9956260B1 (en) 2011-07-22 2018-05-01 The J. David Gladstone Institutes Treatment of HIV-1 infection and AIDS
BR112015003376A8 (pt) * 2012-08-23 2018-01-23 Alios Biopharma Inc composto ou sal farmaceuticamente aceitável do mesmo, composição farmacêutica e usos de quantidade eficiente de composto ou sal farmaceuticamente aceitável do mesmo ou composição farmacêutica
TWI770525B (zh) 2014-12-30 2022-07-11 美商瓦洛健康公司 作為泛素特異性蛋白酶7抑制劑之吡咯并及吡唑并嘧啶
MA41291A (fr) 2014-12-30 2017-11-07 Forma Therapeutics Inc Dérivés de la pyrrolotriazinone et de l'imidazotriazinone en tant qu'inhibiteurs de la protéase spécifique de l'ubiquitine n° 7 (usp7) pour le traitement d'un cancer
WO2016126929A1 (en) 2015-02-05 2016-08-11 Forma Therapeutics, Inc. Thienopyrimidinones as ubiquitin-specific protease 7 inhibitors
HK1248221A1 (zh) 2015-02-05 2018-10-12 Forma Therapeutics, Inc. 异噻唑啉酮类,吡唑并嘧啶酮类和吡咯并嘧啶酮作为泛蛋白特异性蛋白酶7抑制剂
HK1248220A1 (zh) 2015-02-05 2018-10-12 Forma Therapeutics, Inc. 喹唑啉酮和偶氮喹唑啉作为泛特丁胺蛋白酶7抑制剂
PH12022553378A1 (en) 2020-06-10 2024-03-25 Univ Leuven Kath Anti-viral compounds for treating coronavirus, picornavirus, and norovirus infections
EP4366831A4 (en) 2021-07-09 2025-06-11 Aligos Therapeutics, Inc. ANTI-VIRAL COMPOUNDS
US12065428B2 (en) 2021-09-17 2024-08-20 Aligos Therapeutics, Inc. Anti-viral compounds
CN119504546B (zh) * 2023-11-28 2025-12-05 成都地奥制药集团有限公司 内酰胺环类化合物及其用途

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0519748A2 (en) * 1991-06-21 1992-12-23 Merck & Co. Inc. Peptidyl derivatives as inhibitors of interleukin-1B converting enzyme
EP0529713A1 (en) * 1991-08-16 1993-03-03 Merck & Co. Inc. Affinity chromatography matrix useful in purifying interleukin-1B converting enzyme
WO1993009135A1 (en) * 1991-11-04 1993-05-13 Sandoz Ltd. Peptides inhibiting il-1 beta release
WO1993014777A1 (en) * 1992-01-31 1993-08-05 Merck & Co., Inc. PEPTIDYL DERIVATIVES AS INHIBITORS OF INTERLEUKIN-1β CONVERTING ENZYME
WO1993016710A1 (en) * 1992-02-21 1993-09-02 Merck & Co., Inc. PEPTIDYL DERIVATIVES AS INHIBITORS OF INTERLEUKIN-1β CONVERTING ENZYME

Family Cites Families (45)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4276298A (en) * 1978-03-24 1981-06-30 Merck & Co., Inc. 2-Aryl-1,2-benzisothiazolinone-1,1-dioxides and their use as selective protease inhibitors
US4369183A (en) * 1979-09-06 1983-01-18 Merck & Co., Inc. 2-Pyridyl-1,2-benzisothiazolinone-1,1-dioxides and their use as selective protease inhibitors
US4584397A (en) * 1983-05-09 1986-04-22 G. D. Searle & Co. Protease inhibitors
US4499295A (en) * 1983-05-09 1985-02-12 G. D. Searle & Co. Protease inhibitors
US4551279A (en) * 1984-01-09 1985-11-05 G. D. Searle & Co. Protease inhibitors
US5055451A (en) * 1986-12-22 1991-10-08 Syntex Inc. Aryloxy and arylacyloxy methyl ketones as thiol protease inhibitors
US5158936A (en) * 1986-12-22 1992-10-27 Syntex (U.S.A.) Inc. Aryloxy and arylacyloxy methyl ketones as thiol protease inhibitors
NZ223148A (en) * 1987-01-16 1989-10-27 Merrell Dow Pharma Peptide derivatives having peptidase inhibition activity
WO1989004838A1 (en) * 1987-11-25 1989-06-01 Immunex Corporation Interleukin-1 receptors
US5081228A (en) * 1988-02-25 1992-01-14 Immunex Corporation Interleukin-1 receptors
US4968607A (en) * 1987-11-25 1990-11-06 Immunex Corporation Interleukin-1 receptors
US5008245A (en) * 1988-10-27 1991-04-16 University Of Kentucky Research Foundation Novel peptidyl carbamate inhibitors of the enzyme elastase
ZA905737B (en) * 1989-07-26 1991-05-29 Merrell Dow Pharma Novel peptidase inhibitors
NZ235155A (en) * 1989-09-11 1993-04-28 Merrell Dow Pharma Peptidase substrates in which the carboxy terminal group has been replaced by a tricarbonyl radical
WO1991015577A1 (en) * 1990-04-04 1991-10-17 Black, Roy, A. INTERLEUKIN 1'beta' PROTEASE
US5416013A (en) * 1990-04-04 1995-05-16 Sterling Winthrop Inc. Interleukin 1β protease and interleukin 1β protease inhibitors
IL99527A (en) * 1990-09-28 1997-08-14 Lilly Co Eli Tripeptide antithrombotic agents
EP0504938A3 (en) * 1991-03-22 1993-04-14 Suntory Limited Prophylactic and therapeutic agent for bone diseases comprising di- or tripeptide derivative as active ingredient
JP3190431B2 (ja) * 1991-07-01 2001-07-23 三菱化学株式会社 ケトン誘導体
EP0533226A3 (en) * 1991-08-16 1993-08-18 Merck & Co. Inc. Novel chromophore containing compounds
DE69229252T2 (de) * 1991-08-16 1999-12-16 Merck & Co., Inc. DNS, welche das Interleukin-1B-Vorläufer-Converting-Enzym kodiert
US6348570B1 (en) * 1991-08-16 2002-02-19 Merck & Co., Inc. Chromophore containing compounds and their use in determining interleukin-1β convertase activity
EP0600880B1 (en) * 1991-08-30 2004-01-07 Vertex Pharmaceuticals Incorporated Interleukin 1- beta protease and interleukin 1-beta protease inhibitors
EP0547699A1 (en) * 1991-12-19 1993-06-23 Merck & Co. Inc. Peptidyl derivatives as inhibitors of interleukin-1B converting enzyme
WO1993025683A1 (en) * 1992-06-12 1993-12-23 Massachusetts Institute Of Technology A gene which prevents programmed cell death
WO1993025685A1 (en) * 1992-06-12 1993-12-23 Massachusetts Institute Of Technology Cloning and characterization of the cell death genes ced-3 and ced-4
WO1993025694A1 (en) * 1992-06-12 1993-12-23 Massachusetts Institute Of Technology Inhibitors of ced-3 and related proteins
JPH08500242A (ja) * 1992-06-24 1996-01-16 メルク エンド カンパニー インコーポレーテッド インターロイキン1β前駆体の転換酵素をコードするDNA
ES2117133T3 (es) * 1992-07-31 1998-08-01 Pfizer Derivados peptidilicos del acido 4-amino-2,2-difluoro-3-oxo-1,6-hexanodioico como agentes antiinflamatorios.
US5374623A (en) * 1992-08-20 1994-12-20 Prototek, Inc. Cysteine protease inhibitors effective for in vivo use
CA2109646C (en) * 1992-11-24 2000-03-07 Gaston O. Daumy Para-nitroanilide peptides
EP0618223A3 (en) * 1993-03-08 1996-06-12 Sandoz Ltd Peptides, the release of Interleukin 1-Bêta, useful as anti-inflammatory agents.
CA2122227A1 (en) * 1993-04-29 1994-10-30 Roland E. Dolle Peptide analogs as irreversible interleukin-1.beta. protease inhibitors
US5462939A (en) * 1993-05-07 1995-10-31 Sterling Winthrop Inc. Peptidic ketones as interleukin-1β-converting enzyme inhibitors
US5411985A (en) * 1993-05-17 1995-05-02 Merck & Co., Inc. Gamma-pyrone-3-acetic acid as an inhibitor or interleukin-1 β inventory enzyme
JPH0789951A (ja) * 1993-06-03 1995-04-04 Sterling Winthrop Inc インターロイキン−1β転換酵素阻害剤
DK0644197T3 (da) * 1993-06-04 1999-06-07 Vertex Pharma Peptidphosphinyloxymethylketoner som inhibitorer af interleukin-1beta-konverterende enzymer
DK0628550T3 (da) * 1993-06-08 1998-09-28 Vertex Pharma Pyridazin som interleukin-1 beta-omdannede enzyminhibitorer
US6083735A (en) * 1993-06-24 2000-07-04 The General Hospital Corporation Programmed cell death genes and proteins
WO1995005192A1 (en) * 1993-08-13 1995-02-23 Merck & Co., Inc. SUBSTITUTED KETONE DERIVATIVES AS INHIBITORS OF INTERLEUKIN-1β CONVERTING ENZYME
US5486623A (en) * 1993-12-08 1996-01-23 Prototek, Inc. Cysteine protease inhibitors containing heterocyclic leaving groups
CN1504462A (zh) * 1994-03-31 2004-06-16 ������˹ҩƷ��˾ 作为白细胞介素抑制剂的嘧啶基衍生物
US5552400A (en) * 1994-06-08 1996-09-03 Sterling Winthrop Inc. Fused-bicyclic lactams as interleukin-1β converting enzyme inhibitors
US5565430A (en) * 1994-08-02 1996-10-15 Sterling Winthrop Inc. Azaaspartic acid analogs as interleukin-1β converting enzyme inhibitors
US5498616A (en) * 1994-11-04 1996-03-12 Cephalon, Inc. Cysteine protease and serine protease inhibitors

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0519748A2 (en) * 1991-06-21 1992-12-23 Merck & Co. Inc. Peptidyl derivatives as inhibitors of interleukin-1B converting enzyme
EP0529713A1 (en) * 1991-08-16 1993-03-03 Merck & Co. Inc. Affinity chromatography matrix useful in purifying interleukin-1B converting enzyme
WO1993009135A1 (en) * 1991-11-04 1993-05-13 Sandoz Ltd. Peptides inhibiting il-1 beta release
WO1993014777A1 (en) * 1992-01-31 1993-08-05 Merck & Co., Inc. PEPTIDYL DERIVATIVES AS INHIBITORS OF INTERLEUKIN-1β CONVERTING ENZYME
WO1993016710A1 (en) * 1992-02-21 1993-09-02 Merck & Co., Inc. PEPTIDYL DERIVATIVES AS INHIBITORS OF INTERLEUKIN-1β CONVERTING ENZYME

Also Published As

Publication number Publication date
BG101130A (bg) 1997-08-29
SK160996A3 (en) 1997-09-10
IS4399A (is) 1996-12-17
AU709114B2 (en) 1999-08-19
JP4190029B2 (ja) 2008-12-03
US5973111A (en) 1999-10-26
US5716929A (en) 1998-02-10
CZ369896A3 (en) 1997-06-11
HUT76622A (en) 1997-10-28
CA2192089C (en) 2010-01-12
EP0784628A1 (en) 1997-07-23
JPH10504285A (ja) 1998-04-28
WO1995035308A1 (en) 1995-12-28
CN1192035C (zh) 2005-03-09
GEP20012446B (en) 2001-05-25
TW509698B (en) 2002-11-11
HU9603475D0 (en) 1997-02-28
MA24511A1 (fr) 1998-12-31
FI965036L (fi) 1997-02-14
MX9606546A (es) 1997-03-29
SK287422B6 (sk) 2010-09-07
AP9700960A0 (en) 1997-04-30
NZ289560A (en) 1999-09-29
PL185693B1 (pl) 2003-07-31
BR9508051A (pt) 1997-10-21
BG63634B1 (bg) 2002-07-31
CA2192089A1 (en) 1995-12-28
IL114015A0 (en) 1995-10-31
FI965036A7 (fi) 1997-02-14
AU2944695A (en) 1996-01-15
CN1159196A (zh) 1997-09-10
CZ298625B6 (cs) 2007-11-28
PL318220A1 (en) 1997-05-26
FI965036A0 (fi) 1996-12-16

Similar Documents

Publication Publication Date Title
AP797A (en) Inhibitors of interleukin-1B converting enzyme.
US6025147A (en) Inhibitors of interleukin-1 β converting enzyme
US5847135A (en) Inhibitors of interleukin-1β converting enzyme
US7772366B2 (en) Inhibitors of interleukin-1β converting enzyme
Mattos et al. Locating and characterizing binding sites on proteins
Skidgel et al. Structure and function of human plasma carboxypeptidase N, the anaphylatoxin inactivator
Maryanoff Inhibitors of serine proteases as potential therapeutic agents: the road from thrombin to tryptase to cathepsin G
EP0765388A1 (en) CRYSTAL STRUCTURE AND MUTANTS OF INTERLEUKIN-1BETA(b) CONVERTING ENZYME
Muniz et al. The three-dimensional structure of bothropasin, the main hemorrhagic factor from Bothrops jararaca venom: insights for a new classification of snake venom metalloprotease subgroups
Kalupov et al. Structural characterization of mouse neutrophil serine proteases and identification of their substrate specificities
US20020183249A1 (en) Method of identifying inhibitors of CDC25
Dattagupta et al. Refined crystal structure (2.3 Å) of a double‐headed winged bean α‐chymotrypsin inhibitor and location of its second reactive site
Wells et al. Calpain inhibitors as potential treatment for stroke and other neurodegenerative diseases: recent trends and developments
Jalkute et al. Insight into molecular interactions of Aβ peptide and gelatinase from Enterococcus faecalis: a molecular modeling approach
Pedersen et al. Residue 182 influences the second step of protein-tyrosine phosphatase-mediated catalysis
CN102268069B (zh) 基质金属蛋白酶-9多肽抑制剂4及其应用
Rester et al. Structure of the complex of the antistasin-type inhibitor bdellastasin with trypsin and modelling of the bdellastasin-microplasmin system
Metz et al. Inhibitors of human neutrophil elastase as a potential treatment for inflammatory diseases
EP1797115A1 (en) A bacterial atp synthase binding domain
Eguchi et al. Chemogenomics with peptide secondary structure mimetics
JP2003508049A (ja) Cdc25の阻害物質を同定する方法
WO2003002729A1 (en) A crystallised catalytic domain of matrix metalloproteinase 9 (mmp9) and the use of its three dimensional structure to design mmp9 modulators
KR100478324B1 (ko) 인터류킨-1베타전환효소억제제
Law Structural insights into inhibitory mechanisms of cathepsin K
HK1062918A (en) Inhibitors of interleukin-1beta converting enzyme