DE69637307D1 - Aus d-aminosäuren abgeleitete cystein- und serinproteasehemmer - Google Patents

Aus d-aminosäuren abgeleitete cystein- und serinproteasehemmer

Info

Publication number
DE69637307D1
DE69637307D1 DE69637307T DE69637307T DE69637307D1 DE 69637307 D1 DE69637307 D1 DE 69637307D1 DE 69637307 T DE69637307 T DE 69637307T DE 69637307 T DE69637307 T DE 69637307T DE 69637307 D1 DE69637307 D1 DE 69637307D1
Authority
DE
Germany
Prior art keywords
cystein
protease inhibitors
amino acids
serine protease
inhibitors derived
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
DE69637307T
Other languages
English (en)
Other versions
DE69637307T2 (de
Inventor
Sankar Chatterjee
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.)
Cephalon LLC
Original Assignee
Cephalon LLC
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 Cephalon LLC filed Critical Cephalon LLC
Publication of DE69637307D1 publication Critical patent/DE69637307D1/de
Application granted granted Critical
Publication of DE69637307T2 publication Critical patent/DE69637307T2/de
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/44Iso-indoles; Hydrogenated iso-indoles
    • C07D209/48Iso-indoles; Hydrogenated iso-indoles with oxygen atoms in positions 1 and 3, e.g. phthalimide
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • 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
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/12Drugs for disorders of the metabolism for electrolyte homeostasis
    • A61P3/14Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
    • 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
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/22Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C307/00Amides of sulfuric acids, i.e. compounds having singly-bound oxygen atoms of sulfate groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C307/04Diamides of sulfuric acids
    • C07C307/06Diamides of sulfuric acids having nitrogen atoms of the sulfamide groups bound to acyclic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/01Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
    • C07C311/02Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C311/03Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the sulfonamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C311/06Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the sulfonamide groups bound to hydrogen atoms or to acyclic carbon atoms to acyclic carbon atoms of hydrocarbon radicals substituted by carboxyl groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/15Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/16Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
    • C07C311/18Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms, not being part of nitro or nitroso groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/15Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/16Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
    • C07C311/19Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/30Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/45Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups at least one of the singly-bound nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom, e.g. N-acylaminosulfonamides
    • C07C311/46Y being a hydrogen or a carbon atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00Sulfones; Sulfoxides
    • C07C317/44Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
    • C07C317/48Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/50Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton
    • C07C323/51Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C323/60Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton with the carbon atom of at least one of the carboxyl groups bound to nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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
    • C07D207/16Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/10Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D209/20Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals substituted additionally by nitrogen atoms, e.g. tryptophane
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D215/36Sulfur atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/02Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines
    • C07D217/08Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines with a hetero atom directly attached to the ring nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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
    • C07D231/18One oxygen or sulfur atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members 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
    • C07D233/84Sulfur atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D261/00Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/10Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/22Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with hetero atoms directly attached to ring nitrogen atoms
    • C07D295/26Sulfur atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/06Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
    • C07D333/24Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom 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
    • C07D333/30Hetero atoms other than halogen
    • C07D333/34Sulfur atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Neurology (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hematology (AREA)
  • Psychiatry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Peptides Or Proteins (AREA)
DE69637307T 1995-11-28 1996-11-27 Aus d-aminosäuren abgeleitete cystein-und serinproteasehemmer Expired - Fee Related DE69637307T2 (de)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US765195P 1995-11-28 1995-11-28
US7651P 1995-11-28
US75583996A 1996-11-26 1996-11-26
US755839 1996-11-26
PCT/US1996/018992 WO1997021690A1 (en) 1995-11-28 1996-11-27 D-amino acid derived inhibitors of cysteine and serine proteases

Publications (2)

Publication Number Publication Date
DE69637307D1 true DE69637307D1 (de) 2007-12-13
DE69637307T2 DE69637307T2 (de) 2008-02-28

Family

ID=26677244

Family Applications (1)

Application Number Title Priority Date Filing Date
DE69637307T Expired - Fee Related DE69637307T2 (de) 1995-11-28 1996-11-27 Aus d-aminosäuren abgeleitete cystein-und serinproteasehemmer

Country Status (11)

Country Link
US (1) US5852007A (de)
EP (1) EP0910564B1 (de)
JP (1) JP2002515860A (de)
KR (1) KR100490807B1 (de)
AT (1) ATE377006T1 (de)
AU (1) AU714324B2 (de)
CA (1) CA2238175A1 (de)
DE (1) DE69637307T2 (de)
ES (1) ES2293651T3 (de)
MX (1) MX9804262A (de)
WO (1) WO1997021690A1 (de)

Families Citing this family (49)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2193615T3 (es) 1995-10-25 2003-11-01 Senju Pharma Co .nhibidor de la angiogenesis.
US6214800B1 (en) 1995-10-25 2001-04-10 Senju Pharmaceutical Co., Ltd. Angiogenesis inhibitor
WO1998053814A1 (en) * 1997-05-29 1998-12-03 Merck & Co., Inc. Heterocyclic amide compounds as cell adhesion inhibitors
EP1504760B1 (de) * 1998-03-05 2008-07-09 Senju Pharmaceutical Co., Ltd. Pharmazeutische Zusammenstellung zur Vorbeugung und Behandlung von mit Zellkrankheiten des Augenhintergrundes zusammenhängenden Krankheiten
DE19817459A1 (de) * 1998-04-20 1999-10-21 Basf Ag Neue heterozyklische substituierte Amide, Herstellung und Anwendung
DE19818614A1 (de) 1998-04-20 1999-10-21 Basf Ag Neue substituierte Amide, deren Herstellung und Anwendung
US6902721B1 (en) * 1998-07-10 2005-06-07 Osteoscreen, Inc. Inhibitors of proteasomal activity for stimulating bone growth
US6333340B1 (en) * 1998-08-14 2001-12-25 Gpi Nil Holdings, Inc. Small molecule sulfonamides 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
US6307049B1 (en) 1998-09-30 2001-10-23 The Procter & Gamble Co. Heterocyclic 2-substituted ketoamides
US6300341B1 (en) 1998-09-30 2001-10-09 The Procter & Gamble Co. 2-substituted heterocyclic sulfonamides
AU3511500A (en) 1999-03-05 2000-09-21 Trustees Of University Technology Corporation, The Inhibitors of serine protease activity, methods and compositions for treatment of nitric oxide-induced clinical conditions
AU3731400A (en) 1999-03-05 2000-09-21 Trustees Of University Technology Corporation, The Methods and compositions useful in inhibiting apoptosis
WO2001019808A1 (en) * 1999-09-16 2001-03-22 Axys Pharmaceuticals, Inc. Chemical compounds and compositions and their use as cathepsin s inhibitors
CA2384544A1 (en) * 1999-10-08 2001-04-19 Bristol-Myers Squibb Pharma Company Amino lactam sulfonamides as inhibitors of a.beta. protein production
KR20020056923A (ko) 1999-11-18 2002-07-10 코르바스 인터내셔날, 인코포레이티드 엔도텔리아제를 암호화하는 핵산, 엔도텔리아제 및 이의용도
US6358928B1 (en) 1999-11-22 2002-03-19 Enzyme Systems Products Peptidyl sulfonyl imidazolides as selective inhibitors of serine proteases
US7700341B2 (en) 2000-02-03 2010-04-20 Dendreon Corporation Nucleic acid molecules encoding transmembrane serine proteases, the encoded proteins and methods based thereon
EP1334718A4 (de) * 2000-10-26 2007-07-18 Senju Pharma Co Arzneimittelzusammensetzung mit einem dipeptydylaldehydderivat
AU2002232558A1 (en) * 2000-12-12 2002-06-24 Corvas International, Inc. Compounds, compositions and methods for treatment of parasitic infections
SI1341779T1 (sl) 2000-12-13 2006-12-31 Wyeth Corp Heterociklicni sulfonamidni inhibitorji produkcije beta amiloida
US6657070B2 (en) 2000-12-13 2003-12-02 Wyeth Production of chirally pure α-amino acids and N-sulfonyl α-amino acids
US7030116B2 (en) * 2000-12-22 2006-04-18 Aventis Pharmaceuticals Inc. Compounds and compositions as cathepsin inhibitors
EP1383748A2 (de) * 2000-12-22 2004-01-28 Axys Pharmaceuticals, Inc. Neue verbindungen und zusammensetzungen als cathepsin-inhibitoren
MXPA03010766A (es) * 2001-06-01 2005-03-07 Axys Pharm Inc Nuevos compuestos y composiciones como inhibicores de las catepsinas.
US20040147503A1 (en) * 2002-06-04 2004-07-29 Sheila Zipfeil Novel compounds and compositions as cathepsin inhibitors
MXPA04002282A (es) * 2001-09-14 2005-03-07 Axis Pharmaceutical Inc Nuevos compuestos y preparaciones como inhibidores de la catepsina.
GB0125594D0 (en) * 2001-10-25 2001-12-19 Univ Sheffield Inhibitors for inactivating allergens
MXPA04004450A (es) * 2001-11-14 2004-08-11 Aventis Pharma Inc Nuevos compuestos y composiciones como inhibidores de catepsina s.
IL165265A0 (en) * 2002-06-11 2005-12-18 Wyeth Corp Substituted phenylsulfonamide inhibitors of beta amyloid production
WO2004007464A1 (ja) * 2002-07-10 2004-01-22 Sumitomo Pharmaceuticals Co., Ltd. イミダゾール誘導体
NZ542468A (en) * 2003-03-31 2009-01-31 Wyeth Corp Fluoro- and trifluoroalkyl-containing heterocyclic sulfonamide inhibitors of beta amyloid production and derivatives thereof
EP1660094A4 (de) 2003-08-26 2009-09-16 Univ Colorado Hemmer der serinprotease-aktivität und ihre verwendung bei verfahren und zusammensetzungen zur behandlung von bakterieninfektionen
EP1677745A4 (de) * 2003-10-14 2008-10-22 Renovis Inc Nitron-verbindungs-prodrugs und pharmazeutische zusammensetzung daraus zur behandlung von menschlichen erkrankungen
US7078447B2 (en) * 2003-11-21 2006-07-18 General Electric Company Ionizing radiation stable polyarylestercarbonate compositions
CA2547651C (en) * 2003-12-01 2015-06-23 Cambridge University Technical Services Limited Anti-inflammatory agents
ES2330451T3 (es) * 2004-01-16 2009-12-10 Wyeth Inhibidores a base de sulfonamidas heterociclicas de la produccion de beta-amiloides que contienen un azol.
US20070093492A1 (en) * 2004-03-09 2007-04-26 Weir-Torn Jiaang Pyrrolidine derivatives
CA2559611C (en) * 2004-03-09 2012-01-17 National Health Research Institutes Pyrrolidine compounds
RU2436768C2 (ru) 2005-07-11 2011-12-20 Вайет Глютаматы в качестве ингибиторов аггреканазы
EP1752467A1 (de) * 2005-08-10 2007-02-14 4Sc Ag Krebszellen-, t-Zellen- und Keratinocyte-Proliferation-Inhibitoren
BRPI0617348A2 (pt) 2005-10-13 2011-07-26 Wyeth Corp mÉtodos para a preparaÇço de derivados de Ácido glutÂmico; e compostos preparados por esses mÉtodos
MY155630A (en) * 2008-03-05 2015-11-13 Nat Health Research Institutes Pyrrolidine derivatives
WO2012178102A2 (en) 2011-06-24 2012-12-27 The Regents Of The Unversity Of Colorado, A Body Corporate Compositions, methods and uses for alpha-1 antitrypsin fusion molecules
WO2013106589A1 (en) 2012-01-10 2013-07-18 The Regents Of The University Of Colorado, A Body Corporate Compositions, methods and uses for alpha-1 antitrypsin fusion molecules
WO2017156071A1 (en) 2016-03-09 2017-09-14 Blade Therapeutics, Inc. Cyclic keto-amide compounds as calpain modulators and methods of production and use thereof
WO2018009417A1 (en) 2016-07-05 2018-01-11 Blade Therapeutics, Inc. Calpain modulators and therapeutic uses thereof
WO2018064119A1 (en) 2016-09-28 2018-04-05 Blade Therapeutics, Inc. Calpain modulators and therapeutic uses thereof
CN110511147B (zh) * 2019-09-16 2022-06-17 武汉嘉诺康医药技术有限公司 一种硝基烯烃的还原方法

Family Cites Families (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4804782A (en) * 1980-01-21 1989-02-14 Pfizer, Inc. Branched amides of L-aspartyl-D-amino acid dipeptides
EP0124317B1 (de) * 1983-04-27 1990-04-11 Ici Americas Inc. Prolin-Derivate
US4518528A (en) * 1983-05-19 1985-05-21 Rasnick David W α Amino fluoro ketones
US4792555A (en) * 1987-03-20 1988-12-20 American Home Products Corporation Phospholipase A2 inhibitors
US5187157A (en) * 1987-06-05 1993-02-16 Du Pont Merck Pharmaceutical Company Peptide boronic acid inhibitors of trypsin-like proteases
ZA897515B (en) * 1988-10-07 1990-06-27 Merrell Dow Pharma Novel peptidase inhibitors
CA2012306A1 (en) * 1989-03-28 1990-09-28 Werner Neidhart Amino acid derivatives
DE4014421A1 (de) * 1990-05-05 1991-11-07 Merck Patent Gmbh Aminosaeurederivate
US5444042A (en) * 1990-12-28 1995-08-22 Cortex Pharmaceuticals Method of treatment of neurodegeneration with calpain inhibitors
AU667463B2 (en) * 1990-12-28 1996-03-28 Cortex Pharmaceuticals, Inc. Use of calpain inhibitors in the inhibition and treatment of neurodegeneration
WO1992012140A1 (en) * 1990-12-28 1992-07-23 Georgia Tech Research Corporation Peptides ketoamides, ketoacids, and ketoesters
ZA921279B (en) * 1991-02-22 1993-08-23 Du Pont Merck Pharma Substituted alpha-aminoaldehydes and derivatives
CA2071621C (en) * 1991-06-19 1996-08-06 Ahihiko Hosoda Aldehyde derivatives
TW223629B (de) * 1992-03-06 1994-05-11 Hoffmann La Roche
GB9211707D0 (en) * 1992-06-03 1992-07-15 Celltech Ltd Peptidyl derivatives
ATE178650T1 (de) * 1992-06-05 1999-04-15 Scripps Research Inst D-enzymzusammensetzungen und verfahren zu deren verwendung
WO1994000488A1 (en) * 1992-06-23 1994-01-06 Sumitomo Pharmaceuticals Company, Limited Anti-hiv peptide or peptide derivative
WO1994000095A2 (en) * 1992-06-24 1994-01-06 Cortex Pharmaceuticals, Inc. Use of calpain inhibitors in the inhibition and treatment of medical conditions associated with increased calpain activity
US5514694A (en) * 1992-09-21 1996-05-07 Georgia Tech Research Corp Peptidyl ketoamides
US5554653A (en) * 1992-12-22 1996-09-10 Eli Lilly And Company Inhibitors of HIV protease useful for the treatment of AIDS
MX9308016A (es) * 1992-12-22 1994-08-31 Lilly Co Eli Compuestos inhibidores de la proteasa del virus de la inmunodeficiencia humana, procedimiento para su preparacion y formulacion farmaceutica que los contiene.
US5434265A (en) * 1992-12-22 1995-07-18 Eli Lilly And Company Inhibitors of HIV protease
US5491166A (en) * 1992-12-22 1996-02-13 Eli Lilly And Company Inhibitors of HIV protease useful for the treatment of AIDS
DE69329544T2 (de) * 1992-12-22 2001-05-31 Eli Lilly And Co., Indianapolis HIV Protease hemmende Verbindungen
JP3599287B2 (ja) * 1993-04-28 2004-12-08 三菱化学株式会社 スルホンアミド誘導体
FR2706895A1 (en) * 1993-06-22 1994-12-30 Synthelabo Tetrahydroisoquinoline derivatives, their preparation and their application in therapeutics
US5541290A (en) * 1993-06-24 1996-07-30 Harbeson; Scott L. Optically pure calpain inhibitor compounds
US5455262A (en) * 1993-10-06 1995-10-03 Florida State University Mercaptosulfide metalloproteinase inhibitors
US5436229A (en) * 1994-03-04 1995-07-25 Eli Lilly And Company Bisulfite adducts of arginine aldehydes
US5693617A (en) * 1994-03-15 1997-12-02 Proscript, Inc. Inhibitors of the 26s proteolytic complex and the 20s proteasome contained therein
US5536639A (en) * 1994-03-25 1996-07-16 Cephalon, Inc. Methods for detecting calpain activation by detection of calpain activated spectrin breakdown products
US5550262A (en) * 1994-11-14 1996-08-27 Cephalon, Inc. Multicatalytic protease inhibitors
JPH11506923A (ja) * 1995-06-06 1999-06-22 アセナ ニューロサイエンシーズ,インコーポレイテッド 新しいカテプシンならびにその阻害のための方法および組成物

Also Published As

Publication number Publication date
ATE377006T1 (de) 2007-11-15
EP0910564A1 (de) 1999-04-28
AU714324B2 (en) 2000-01-06
US5852007A (en) 1998-12-22
EP0910564B1 (de) 2007-10-31
JP2002515860A (ja) 2002-05-28
CA2238175A1 (en) 1997-06-19
KR19990071683A (ko) 1999-09-27
AU1025397A (en) 1997-07-03
EP0910564A4 (de) 1999-04-28
ES2293651T3 (es) 2008-03-16
MX9804262A (es) 1998-09-30
KR100490807B1 (ko) 2005-10-14
DE69637307T2 (de) 2008-02-28
WO1997021690A1 (en) 1997-06-19

Similar Documents

Publication Publication Date Title
DE69637307D1 (de) Aus d-aminosäuren abgeleitete cystein- und serinproteasehemmer
HK1025511A1 (en) Peptidyl-2-amino-1-hydroxyalkanesulfonic acid cysteine protease inhibitors
HK1016495A1 (en) Phosphorous-containing cysteine and serine protease inhibitors
NO964590L (no) Töyvaskemidler omfattende subtilisin BPN'-varianter
NO990548L (no) Inhibitorer for cystein-protease
ATE335485T1 (de) Quinolin-enthaltende alpha-ketoamid-basierte inhibitoren von cystein- und serin protease
ATE245185T1 (de) Proteasen enthaltende bleichmittelzusammensetzungen
IL111175A0 (en) Electrophilic peptide analogs as inhibitors of trypsin-like serine proteases and pharmaceutical compositions containing them
DE3485568D1 (de) Peptide aus alpha-aminoboronsaeuren.
ATE52518T1 (de) Peptid-derivate, pepstatin-analoga, renin- und saeureprotease hemmende mittel.
MY116539A (en) New amino acid derivatives
BR9815469A (pt) Inibidores de protease
HUP9901725A2 (hu) Szubtilizinváltozatok
DE69326077D1 (de) Sulfonylalkanoylaminohydroxyethylaminosulfaminsäuren verwendbar als inhibitoren retroviraler proteasen
GR3023577T3 (en) Peptide boronic acid derivatives having protease inhibiting activity
CA2342985A1 (en) Hydroxamate-containing cysteine and serine protease inhibitors
ATE154036T1 (de) Retrovirale protease-inhibitoren
DE59900730D1 (de) Korrosionsinhibitoren enthaltender Injektionszement
BR9711540A (pt) Inibidores de protease proteìnico estabilizados e variantes dos mesmos
DE59812724D1 (de) Serin-proteinase-inhibitoren
NO993394L (no) Fremgangsmåte for fremstilling av rhizoferrin
ATE152731T1 (de) Zytotoixisches t- lymphozyten antigen als cystein protease inhibitor
AU7257994A (en) Novel protein inhibitors of serine proteinases (e.g. furin) derived from turkey ovomucoid third domain
DK0534992T3 (da) Fremgangsmåde til fremstilling af peptider
ATE241383T1 (de) Behandlung von allergischen zuständen mit cystein-und serin-proteinase inhibitoren

Legal Events

Date Code Title Description
8364 No opposition during term of opposition
8339 Ceased/non-payment of the annual fee