AU2001280642A1 - Lactam compounds and their use as inhibitors of serine proteases and method - Google Patents

Lactam compounds and their use as inhibitors of serine proteases and method

Info

Publication number
AU2001280642A1
AU2001280642A1 AU2001280642A AU8064201A AU2001280642A1 AU 2001280642 A1 AU2001280642 A1 AU 2001280642A1 AU 2001280642 A AU2001280642 A AU 2001280642A AU 8064201 A AU8064201 A AU 8064201A AU 2001280642 A1 AU2001280642 A1 AU 2001280642A1
Authority
AU
Australia
Prior art keywords
alkyl
compound
cycloheteroalkyl
aryl
heteroaryl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Abandoned
Application number
AU2001280642A
Other languages
English (en)
Inventor
Gregory S. Bisacchi
R. Michael Lawrence
Steven M. Seiler
William A. Slusarchyk
James C. Sutton
Guohua Zhao
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bristol Myers Squibb Co
Original Assignee
Bristol Myers Squibb Co
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
Application filed by Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of AU2001280642A1 publication Critical patent/AU2001280642A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/02—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D223/06—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D223/08—Oxygen atoms
    • C07D223/10—Oxygen atoms attached in position 2
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • 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
    • A61P37/08—Antiallergic agents
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Molecular Biology (AREA)
  • Epidemiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Immunology (AREA)
  • Dermatology (AREA)
  • Neurology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Neurosurgery (AREA)
  • Urology & Nephrology (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Vascular Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Otolaryngology (AREA)
  • Gastroenterology & Hepatology (AREA)
AU2001280642A 2000-08-07 2001-07-20 Lactam compounds and their use as inhibitors of serine proteases and method Abandoned AU2001280642A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US09/633,751 2000-08-07
US09/633,751 US6344450B1 (en) 1999-02-09 2000-08-07 Lactam compounds and their use as inhibitors of serine proteases and method
PCT/US2001/022829 WO2002012196A2 (en) 2000-08-07 2001-07-20 Lactam compounds and their use as inhibitors of serine proteases and method

Publications (1)

Publication Number Publication Date
AU2001280642A1 true AU2001280642A1 (en) 2002-02-18

Family

ID=24540977

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2001280642A Abandoned AU2001280642A1 (en) 2000-08-07 2001-07-20 Lactam compounds and their use as inhibitors of serine proteases and method

Country Status (7)

Country Link
US (1) US6344450B1 (hu)
EP (1) EP1309609A2 (hu)
JP (1) JP2004521071A (hu)
AU (1) AU2001280642A1 (hu)
CA (1) CA2418995A1 (hu)
HU (1) HUP0303662A2 (hu)
WO (1) WO2002012196A2 (hu)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1127054A4 (en) * 1998-10-29 2006-11-02 Bristol Myers Squibb Co INHIBITORS OF IMPDH ENZYME
JP2005537247A (ja) * 2002-06-27 2005-12-08 シエーリング アクチエンゲゼルシャフト 置換されたキノリンｃｃｒ５受容体アンタゴニスト
WO2004011019A1 (de) * 2002-07-25 2004-02-05 Charite-Universitäts Medizin Berlin Verwendung eines proteasom-inhibitors zur behandlung fibrotischer erkrankungen
DE10238002A1 (de) * 2002-08-20 2004-03-04 Merck Patent Gmbh Benzimidazolderivate
AU2002951912A0 (en) 2002-10-08 2002-10-24 Unisearch Limited Tryptase polypeptide and uses thereof
US20040180855A1 (en) * 2003-02-19 2004-09-16 Schumacher William A. Methods of treating thrombosis with reduced risk of increased bleeding times
CA2547651C (en) * 2003-12-01 2015-06-23 Cambridge University Technical Services Limited Anti-inflammatory agents
BRPI0507971A (pt) * 2004-02-23 2007-07-24 Tufts College composto, composição farmacêutica, uso de um composto,método para inibir a atividade proteolìtica de uma enzima de clivagem pós-prolina e remédio empacotado
CA2558766A1 (en) 2004-03-05 2005-09-22 The Trustees Of The University Of Pennsylvania The use of mtp inhibitors for treating disorders or diseases associated with hyperlipidemia and hypercholesterolemia while minimizing side effects
US7361672B2 (en) * 2004-12-23 2008-04-22 Hoffmann-La Roche Inc. Heteroarylacetamide inhibitors of factor Xa
CA2648522A1 (en) * 2005-04-04 2006-10-12 Daiamed, Inc. Substituted azetidinones
EP1951224A2 (en) * 2005-10-18 2008-08-06 Aegerion Pharmaceuticals Methods for treating disorders associated with hyperlipidemia in a mammal
JP2010513534A (ja) * 2006-12-21 2010-04-30 エージェリオン ファーマシューティカルズ， インコーポレイテッド Ｍｔｐインヒビターおよびコレステロール吸収インヒビターを含む組み合わせを用いて肥満症を処置する方法
WO2018002673A1 (en) 2016-07-01 2018-01-04 N4 Pharma Uk Limited Novel formulations of angiotensin ii receptor antagonists

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IT1247698B (it) 1990-06-21 1994-12-30 Sigma Tau Ind Farmaceuti 1-alchil-3-(acilammino)-e-caprolattami quali attivatori dei processi di apprendimento e della memoria e composizioni farmaceutiche comprendenti tali composti
GB9200535D0 (en) 1992-01-10 1992-02-26 Fujisawa Pharmaceutical Co New compound
US5484917A (en) 1993-06-16 1996-01-16 Pfizer Inc. Substituted tetrahydrobenzazepinones
US5618811A (en) 1993-07-26 1997-04-08 Pfizer Inc. Tetrahydro-1H-benzazepinones and hexahydroazepinones as selective cholecystokinin-B receptor antagonists
US5932733A (en) 1994-06-17 1999-08-03 Corvas International, Inc. 3-amino-2-oxo-1-piperidineacetic derivatives containing an arginine mimic as enzyme inhibitors
US5703208A (en) 1994-06-17 1997-12-30 Corvas International, Inc. 3-amino-2-oxo-1-piperidineacetic derivatives as enzyme inhibitors
WO1995035311A1 (en) 1994-06-17 1995-12-28 Corvas International, Inc. 3-amino-2-oxo-1-piperidineacetic derivatives as enzyme inhibitors
GB9420763D0 (en) 1994-10-14 1994-11-30 Glaxo Inc Acetamide derivatives
US5672598A (en) 1995-03-21 1997-09-30 The Procter & Gamble Company Lactam-containing hydroxamic acids
EP0761680A3 (en) 1995-09-12 1999-05-06 Ono Pharmaceutical Co., Ltd. Tetrazole compounds having Interleukin-1beta converting enzyme inhibitory activity
WO1997014417A1 (en) 1995-10-19 1997-04-24 Merck & Co., Inc. Fibrinogen receptor antagonists
AU7604196A (en) 1995-10-30 1997-05-22 Merck & Co., Inc. Novel inhibitors of peptide binding to mhc class ii proteins
IL119466A (en) * 1995-11-03 2001-08-26 Akzo Nobel Nv Thrombin inhibitors, their preparation and pharmaceutical compositions containing them
TR199801569T2 (xx) 1996-02-13 1998-10-21 Akzo Nobel N.V. Serin proteaz inhibit�rleri.
IL120311A (en) * 1996-03-01 2001-10-31 Akzo Nobel Nv Serine protease inhibitors and pharmaceuticals containing them
AU718055B2 (en) 1996-09-19 2000-04-06 Aventisub Ii Inc. 3-mercaptoacetylamino-1,5-substituted-2-oxo-azepan derivatives useful as inhibitors of matrix metalloproteinase
WO1998016523A2 (en) 1996-10-11 1998-04-23 Cor Therapeutics, Inc. Selective factor xa inhibitors
PL336589A1 (en) * 1997-05-02 2000-07-03 Akzo Nobel Nv Serinic protease inhibitors
FR2764511B1 (fr) 1997-06-13 2000-09-08 Sanofi Sa Compositions pour le traitement et la prevention de la thrombose arterielle et utilisation d'un inhibiteur du facteur xa seul et/ou en combinaison avec un antiagregant plaquettaire
EP1100782A1 (en) 1998-07-24 2001-05-23 Corvas International, Inc. Amino-aldehyde solid support, linker therefor and methods of preparation and use thereof
WO2000047563A1 (en) * 1999-02-09 2000-08-17 Bristol-Myers Squibb Co. LACTAM INHIBITORS OF FXa AND METHOD
AU766089B2 (en) 1999-03-11 2003-10-09 Du Pont Pharmaceuticals Company Treatment of thrombosis by combined use of a factor Xa inhibitor and aspirin, tissue plasminogen activator (TPA), a GPIIb/IIIa antagonist, low molecular weight heparin or heparin
AU2001255408A1 (en) * 2000-04-14 2001-10-30 Corvas International, Inc. Tetrahydro-azepinone derivatives as thrombin inhibitors

Also Published As

Publication number Publication date
WO2002012196A3 (en) 2003-01-16
CA2418995A1 (en) 2002-02-14
JP2004521071A (ja) 2004-07-15
US6344450B1 (en) 2002-02-05
HUP0303662A2 (hu) 2004-03-01
EP1309609A2 (en) 2003-05-14
WO2002012196A2 (en) 2002-02-14

Similar Documents

Publication Publication Date Title
US6875867B2 (en) Process for preparing chiral diol sulfones and dihydroxy acid HMG CoA reductase inhibitors
US6511977B1 (en) Potassium channel inhibitors and method
AU2008229725B2 (en) Beta-secretase inhibitors and methods of use
US4518528A (en) α Amino fluoro ketones
JP5385904B2 (ja) γ−セクレターゼ阻害剤
AU2001280642A1 (en) Lactam compounds and their use as inhibitors of serine proteases and method
AU648751B2 (en) Novel aminobenzoates
CZ20031715A3 (cs) Nové deriváty N- (fenylsulfonyl)glycinu a jejich terapeutické použití
US20040072881A1 (en) Heterocyclic aromatic compounds useful as growth hormone secreagogues
WO2002022563A1 (fr) Derive d'uree et inhibiteur de molecule adhesive contenant celui-ci en tant que substance active
EP1089973B1 (en) Amidino and guanidino azetidinone tryptase inhibitors
EP2906560B1 (en) Azaindolines having activity as inhibitors of iap
AU756174B2 (en) Lactam inhibitors of FXa and method
ES2208396T3 (es) Compuestos que inhiben la actividad de la triptasa.
CA2187449C (en) Anti-cancer compounds containing cyclopentaquinazoline ring
US20040147502A1 (en) Beta lactam compounds and their use as inhibitors of tryptase
ES2278928T3 (es) Inhibidores de triptasa.
JPH08512024A (ja) １，２−ジアシル化ヒドラジン誘導体および全接着阻害剤としてのそれらの使用
AU2002310261A1 (en) Process for preparing chiral diol sulfones and dihydroxy acid HMG COA reductase inhibitors

Legal Events

Date Code Title Description
MK5 Application lapsed section 142(2)(e) - patent request and compl. specification not accepted