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SK2862003A3 - Spiroheterocyclic nitriles useful as reversible inhibitors of cysteine proteases - Google Patents

Spiroheterocyclic nitriles useful as reversible inhibitors of cysteine proteases Download PDF

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Publication number
SK2862003A3
SK2862003A3 SK286-2003A SK2862003A SK2862003A3 SK 2862003 A3 SK2862003 A3 SK 2862003A3 SK 2862003 A SK2862003 A SK 2862003A SK 2862003 A3 SK2862003 A3 SK 2862003A3
Authority
SK
Slovakia
Prior art keywords
cyano
piperidin
methyl
cyclohexyl
carbamoyl
Prior art date
Application number
SK286-2003A
Other languages
English (en)
Slovak (sk)
Inventor
Younes Bekkali
Eugene Richard Hickey
Weimin Liu
Usha R Patel
Denice Mary Spero
Sanxing Sun
David S Thomson
Yancey David Ward
Erick Richard Roush Young
Original Assignee
Boehringer Ingelheim 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
Application filed by Boehringer Ingelheim Pharma filed Critical Boehringer Ingelheim Pharma
Publication of SK2862003A3 publication Critical patent/SK2862003A3/sk

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • 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
    • A61P25/28—Drugs 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
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
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    • 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
    • C04—CEMENTS; CONCRETE; ARTIFICIAL STONE; CERAMICS; REFRACTORIES
    • C04B—LIME, MAGNESIA; SLAG; CEMENTS; COMPOSITIONS THEREOF, e.g. MORTARS, CONCRETE OR LIKE BUILDING MATERIALS; ARTIFICIAL STONE; CERAMICS; REFRACTORIES; TREATMENT OF NATURAL STONE
    • C04B35/00—Shaped ceramic products characterised by their composition; Ceramics compositions; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
    • C04B35/622—Forming processes; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
    • C04B35/626—Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B
    • C04B35/63—Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B using additives specially adapted for forming the products, e.g.. binder binders
    • C04B35/632—Organic additives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic 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
    • C07D207/04—Heterocyclic 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
    • C07D207/10—Heterocyclic 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
    • C07D207/14—Nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic 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
    • C07D207/04—Heterocyclic 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
    • C07D207/10—Heterocyclic 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
    • C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
    • C07D211/56—Nitrogen atoms
    • C07D211/58—Nitrogen atoms attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
    • C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
    • C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D211/62—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
    • C07D211/66—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4 having a hetero atom as the second substituent in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D309/08—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings 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
    • C07D309/14—Nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D335/00—Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom
    • C07D335/02—Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D455/00—Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine
    • C07D455/02—Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing not further condensed quinolizine ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08—Bridged systems

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  • Chemical & Material Sciences (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
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  • General Chemical & Material Sciences (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Ceramic Engineering (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Manufacturing & Machinery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Neurology (AREA)
  • Materials Engineering (AREA)
  • Inorganic Chemistry (AREA)
  • Pulmonology (AREA)
  • Structural Engineering (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Emergency Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Transplantation (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
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SK286-2003A 2000-09-08 2001-03-14 Spiroheterocyclic nitriles useful as reversible inhibitors of cysteine proteases SK2862003A3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US09/655,351 US6420364B1 (en) 1999-09-13 2000-09-08 Compound useful as reversible inhibitors of cysteine proteases
PCT/US2001/008084 WO2002020485A1 (en) 2000-09-08 2001-03-14 Spiroheterocyclic nitriles useful as reversible inhibitors of cysteine proteases

Publications (1)

Publication Number Publication Date
SK2862003A3 true SK2862003A3 (en) 2003-08-05

Family

ID=24628539

Family Applications (1)

Application Number Title Priority Date Filing Date
SK286-2003A SK2862003A3 (en) 2000-09-08 2001-03-14 Spiroheterocyclic nitriles useful as reversible inhibitors of cysteine proteases

Country Status (25)

Country Link
US (10) US6420364B1 (pt)
EP (1) EP1322613A1 (pt)
JP (1) JP2004508356A (pt)
KR (1) KR20030051644A (pt)
CN (1) CN1303067C (pt)
AU (1) AU2001245694A1 (pt)
BG (1) BG107585A (pt)
BR (1) BR0113740A (pt)
CA (1) CA2417177A1 (pt)
CZ (1) CZ2003603A3 (pt)
EA (1) EA005203B1 (pt)
EE (1) EE200300093A (pt)
HK (1) HK1060565A1 (pt)
HR (1) HRP20030163A2 (pt)
HU (1) HUP0303934A2 (pt)
IL (1) IL154080A0 (pt)
MX (1) MXPA03001947A (pt)
NO (1) NO20031065L (pt)
NZ (1) NZ525169A (pt)
PL (1) PL361038A1 (pt)
SK (1) SK2862003A3 (pt)
UA (1) UA73378C2 (pt)
WO (1) WO2002020485A1 (pt)
YU (1) YU17003A (pt)
ZA (1) ZA200301032B (pt)

Families Citing this family (72)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9723407D0 (en) * 1997-11-05 1998-01-07 Ciba Geigy Ag Organic compounds
US7704958B1 (en) * 1999-03-05 2010-04-27 Bio Holding, Inc. Methods and compositions for inhibiting apoptosis using serine protease inhibitors
US6420364B1 (en) * 1999-09-13 2002-07-16 Boehringer Ingelheim Pharmaceuticals, Inc. Compound useful as reversible inhibitors of cysteine proteases
US6773704B1 (en) * 1999-10-28 2004-08-10 The Brigham And Women's Hospital, Inc. Methods of treating vascular disease associated with cystatin C deficiency
GB0003111D0 (en) * 2000-02-10 2000-03-29 Novartis Ag Organic compounds
US7030116B2 (en) 2000-12-22 2006-04-18 Aventis Pharmaceuticals Inc. Compounds and compositions as cathepsin inhibitors
CA2433520A1 (en) 2000-12-22 2002-07-04 Axys Pharmaceuticals, Inc. Novel compounds and compositions as cathepsin inhibitors
EP1372655B1 (en) * 2001-03-02 2008-10-01 Merck Frosst Canada Ltd. Cathepsin cysteine protease inhibitors
US6982263B2 (en) * 2001-06-08 2006-01-03 Boehringer Ingelheim Pharmaceuticals, Inc. Nitriles useful as reversible inhibitors of cysteine proteases
DE10141650C1 (de) * 2001-08-24 2002-11-28 Lohmann Therapie Syst Lts Transdermales Therapeutisches System mit Fentanyl bzw. verwandten Substanzen
PL369312A1 (en) 2001-09-14 2005-04-18 Aventis Pharmaceuticals Inc. Novel compounds and compositions as cathepsin inhibitors
EP1434769A2 (en) * 2001-10-02 2004-07-07 Boehringer Ingelheim Pharmaceuticals Inc. Compounds useful as reversible inhibitors of cysteine proteases
JP2005508979A (ja) * 2001-10-29 2005-04-07 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 システインプロテアーゼの可逆性インヒビターとして有用な化合物
CA2467391A1 (en) 2001-11-14 2003-05-22 Aventis Pharmaceuticals Inc. Oligopeptides and compositions containing them as cathepsin s inhibitors
AU2003256305A1 (en) * 2002-06-24 2004-01-06 Axys Pharmaceuticals, Inc. Peptidic compounds as cysteine protease inhibitors
US7326690B2 (en) * 2002-10-30 2008-02-05 Bach Pharma, Inc. Modulation of cell fates and activities by phthalazinediones
US7465745B2 (en) * 2003-03-13 2008-12-16 Boehringer Ingelheim Pharmaceuticals, Inc. Cathepsin S inhibitors
US7326719B2 (en) * 2003-03-13 2008-02-05 Boehringer Ingelheim Pharmaceuticals, Inc. Cathepsin S inhibitors
US7109243B2 (en) * 2003-03-24 2006-09-19 Irm Llc Inhibitors of cathepsin S
US7384970B2 (en) * 2003-03-24 2008-06-10 Irm Llc Inhibitors of cathepsin S
WO2004089395A2 (en) * 2003-04-01 2004-10-21 Aventis Pharmaceuticals Inc. Use of an inhibitor of cathepsin-s or -b to treat or prevent chronic obstructive pulmonary disease
CA2526694A1 (en) * 2003-06-04 2004-12-16 John W. Patterson Amidino compounds as cysteine protease inhibitors
US7173051B2 (en) * 2003-06-13 2007-02-06 Irm, Llc Inhibitors of cathepsin S
US7256207B2 (en) 2003-08-20 2007-08-14 Irm Llc Inhibitors of cathepsin S
EA011855B1 (ru) * 2003-09-18 2009-06-30 Вайробей, Инк. Соединения, содержащие галоидалкил, как ингибиторы цистеиновых протеаз
JP2007509961A (ja) * 2003-10-30 2007-04-19 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 ジペプチド類似体合成
AR046784A1 (es) * 2003-12-03 2005-12-21 Glaxo Group Ltd Compuesto de amina ciclica composicion farmaceutica que lo comprende y su uso para preparar esta ultima
JP2007513972A (ja) * 2003-12-11 2007-05-31 アクシス・ファーマシューティカルズ・インコーポレイテッド 低分子治療剤または生物製剤の投与によって引き起こされる免疫応答を治療するためのカテプシンｓインヒビターの使用
EP1694647B1 (en) * 2003-12-12 2016-11-09 Merck Canada Inc. Cathepsin cysteine protease inhibitors
JP2007516295A (ja) * 2003-12-23 2007-06-21 アクシス・ファーマシューティカルズ・インコーポレイテッド システインプロテアーゼインヒビターとしてのアミジノ化合物
WO2006060810A1 (en) * 2004-12-02 2006-06-08 Schering Aktiengesellschaft Sulfonamide compounds as cysteine protease inhibitors
WO2006076797A1 (en) * 2005-01-19 2006-07-27 Merck Frosst Canada Ltd. Cathepsin k inhibitors and atherosclerosis
EA201201550A1 (ru) * 2005-03-21 2013-08-30 Вайробей, Инк. Производные альфа-кетоамидов в качестве ингибиторов цистеинпротеаз
JP5215167B2 (ja) * 2005-03-22 2013-06-19 ビロベイ，インコーポレイティド システインプロテアーゼ阻害剤としてのスルホニル基含有化合物
US7282964B2 (en) * 2005-05-25 2007-10-16 Texas Instruments Incorporated Circuit for detecting transitions on either of two signal lines referenced at different power supply levels
CA2610828A1 (en) * 2005-06-14 2006-12-28 Schering Corporation Heterocyclic aspartyl protease inhibitors, preparation and use thereof
US8067415B2 (en) * 2005-11-01 2011-11-29 Millennium Pharmaceuticals, Inc. Compounds useful as antagonists of CCR2
EP1951706A1 (en) 2005-11-01 2008-08-06 Janssen Pharmaceutica N.V. Dihydroisoindolones as allosteric modulators of glucokinase
WO2007053495A2 (en) * 2005-11-01 2007-05-10 Millennium Pharmaceuticals, Inc. Compounds useful as antagonists of ccr2
WO2007053498A1 (en) * 2005-11-01 2007-05-10 Millennium Pharmaceuticals, Inc. Compounds useful as antagonists of ccr2
MY156425A (en) 2006-06-01 2016-02-26 Sanofi Aventis Spirocyclic nitriles as protease inhibitors
US8652844B2 (en) 2006-06-13 2014-02-18 The Curators Of The University Of Missouri Methods for the cryopreservation of animal cells that contain high levels of intracellular lipids
US8063082B2 (en) * 2006-08-02 2011-11-22 Cytokinetics, Inc. Certain chemical entities, compositions, and methods
US8071625B2 (en) * 2006-08-02 2011-12-06 Cytokinetics, Inc. Certain chemical entities, compositions, and methods
NZ576105A (en) * 2006-10-04 2012-01-12 Virobay Inc Di-fluoro containing compounds as cysteine protease inhibitors
US7893112B2 (en) 2006-10-04 2011-02-22 Virobay, Inc. Di-fluoro containing compounds as cysteine protease inhibitors
KR100877394B1 (ko) 2007-07-11 2009-01-07 한국화학연구원 카보니트릴 화합물을 포함하는 골다공증 및 치은 질환의치료 및 예방을 위한 약제학적 조성물
CA2692713A1 (en) 2007-07-17 2009-01-22 Amgen Inc. Heterocyclic modulators of pkb
AU2008276512A1 (en) * 2007-07-17 2009-01-22 Amgen Inc. Thiadiazole modulators of PKB
US8088793B2 (en) 2007-08-15 2012-01-03 Cytokinetics, Inc. Certain chemical entities, compositions, and methods
US8354446B2 (en) 2007-12-21 2013-01-15 Ligand Pharmaceuticals Incorporated Selective androgen receptor modulators (SARMs) and uses thereof
JP5587790B2 (ja) 2008-01-09 2014-09-10 アミュラ セラピューティクス リミティド 化合物
WO2010028236A1 (en) * 2008-09-05 2010-03-11 Avila Therapeutics, Inc. Algorithm for designing irreversible inhibitors
US20120088791A1 (en) * 2009-02-19 2012-04-12 Vanderbilt University Amidobipiperidinecarboxylate m1 allosteric agonists, analogs and derivatives thereof, and methods of making and using same
US8324417B2 (en) 2009-08-19 2012-12-04 Virobay, Inc. Process for the preparation of (S)-2-amino-5-cyclopropyl-4,4-difluoropentanoic acid and alkyl esters and acid salts thereof
SG179172A1 (en) 2009-09-16 2012-04-27 Avila Therapeutics Inc Protein kinase conjugates and inhibitors
MX2012007684A (es) 2009-12-30 2012-10-05 Avila Therapeutics Inc Modificacion covalente ligando dirigida de proteina.
WO2012151319A1 (en) 2011-05-02 2012-11-08 Virobay, Inc. Cathepsin inhibitors for the treatment of bone cancer and bone cancer pain
CN104744315A (zh) 2011-06-07 2015-07-01 株式会社吴羽 氧杂环丁烷化合物的制造方法、唑甲基环戊醇化合物的制造方法、以及中间体化合物
EP2537532A1 (en) 2011-06-22 2012-12-26 J. Stefan Institute Cathepsin-binding compounds bound to a nanodevice and their diagnostic and therapeutic use
DK2780015T3 (en) 2011-11-18 2017-03-27 Heptares Therapeutics Ltd M1 MUSCARINRECEPTORAGONISTER
ES2785313T3 (es) 2013-01-15 2020-10-06 Merck Patent Gmbh Acilguanidinas para el tratamiento de la artrosis
EP3094323A4 (en) 2014-01-17 2017-10-11 Ligand Pharmaceuticals Incorporated Methods and compositions for modulating hormone levels
GB201404922D0 (en) 2014-03-19 2014-04-30 Heptares Therapeutics Ltd Pharmaceutical compounds
GB201513743D0 (en) 2015-08-03 2015-09-16 Heptares Therapeutics Ltd Muscarinic agonists
US10259787B2 (en) 2016-10-14 2019-04-16 Heptares Therapeutics Limited Substituted cyclohexanes as muscarinic M1 receptor and/or M4 receptor agonists
GB201617454D0 (en) 2016-10-14 2016-11-30 Heptares Therapeutics Limited Pharmaceutical compounds
GB201810239D0 (en) 2018-06-22 2018-08-08 Heptares Therapeutics Ltd Pharmaceutical compounds
GB201819961D0 (en) 2018-12-07 2019-01-23 Heptares Therapeutics Ltd Pharmaceutical compounds
GB201819960D0 (en) 2018-12-07 2019-01-23 Heptares Therapeutics Ltd Pharmaceutical compounds
GB202020191D0 (en) 2020-12-18 2021-02-03 Heptares Therapeutics Ltd Pharmaceutical compounds
CN111943848B (zh) * 2020-08-19 2023-05-05 苏州旺山旺水生物医药有限公司 一种elexacaftor中间体的制备方法及其应用

Family Cites Families (172)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3467691A (en) 1964-04-22 1969-09-16 Tsutomu Irikura N-(n-acylaminoacyl)-aminoacetonitriles
US6204261B1 (en) 1995-12-20 2001-03-20 Vertex Pharmaceuticals Incorporated Inhibitors of interleukin-1β Converting enzyme inhibitors
JPS4310619Y1 (pt) 1967-02-16 1968-05-09
EP0115472A3 (de) 1983-01-27 1985-10-02 Ciba-Geigy Ag Pyrrolidinonderivate und Verfahren zu ihrer Herstellung
US4767202A (en) * 1984-01-20 1988-08-30 Minolta Camera Kabushiki Kaisha Objective lens system for optical recording type disks
JPS61502124A (ja) * 1984-05-09 1986-09-25 ジ　オ−ストラリアン　ナシヨナル　ユニヴア−シテイ− 免疫応答の調節方法
US4797202A (en) 1984-09-13 1989-01-10 The Dow Chemical Company Froth flotation method
US4737425A (en) * 1986-06-10 1988-04-12 International Business Machines Corporation Patterned resist and process
JPS6358346A (ja) 1986-08-29 1988-03-14 Fuji Photo Film Co Ltd カラ−写真現像液組成物及びハロゲン化銀写真感光材料の処理方法
US4734425A (en) 1986-10-17 1988-03-29 E. R. Squibb & Sons, Inc. 7-oxabicycloheptane substituted hydroxamic acid prostaglandin analogs
US4749715A (en) 1987-03-02 1988-06-07 E. R. Squibb & Sons, Inc. 7-oxabicycloheptane substituted amino prostaglandin analogs
FR2615104B1 (fr) 1987-05-14 1989-08-18 Centre Nat Rech Scient Nouvelle protease de plasmodium falciparum, anticorps diriges contre cette protease, substrats peptidiques specifiques de ladite protease, et leur utilisation comme medicament contre le paludisme
JPS63301868A (ja) 1987-06-01 1988-12-08 Nippon Kayaku Co Ltd Ｎ−（２−クロロイソニコチノイル）アミノ酸誘導体およびそれを有効成分とする農園芸用殺菌剤
DE3719226A1 (de) 1987-06-09 1988-12-22 Bayer Ag (2-cyan-2-oximinoacetyl)-aminosaeure-derivate
US4971978A (en) 1987-09-21 1990-11-20 Nadzan Alex M Derivatives of D-glutamic acid and D-aspartic acid
KR890701619A (ko) 1987-10-26 1989-12-22 크리스틴 에이.트러트웨인 레닌 억제제, 그의 제조 방법, 그 사용 방법 및 이들을 함유한 조성물
CA1322005C (en) 1987-11-25 1993-09-07 Robert N. Young Benzoheterazoles
US4962117A (en) 1987-11-25 1990-10-09 Merck Frosst Canada, Inc. Heterazole dialkanoic acids
US5004743A (en) 1987-11-25 1991-04-02 Merck Frosst Canada, Inc. Pyridyl styrene dialkanoic acids as anti-leukotriene agents
US5346907A (en) 1988-04-05 1994-09-13 Abbott Laboratories Amino acid analog CCK antagonists
WO1989010355A1 (en) 1988-04-05 1989-11-02 Abbott Laboratories Derivatives of tryptophan as cck antagonists
EP0413750A1 (en) 1988-05-03 1991-02-27 The Upjohn Company Renin inhibitory peptides containing a substituted phenoxyacetyle group
DE3827727A1 (de) 1988-08-16 1990-02-22 Boehringer Ingelheim Kg Anellierte tetrahydropyridinessigsaeurederivate, verfahren zu deren herstellung und verwendung solcher verbindungen zur kardioprotektion
EP0374098A3 (de) 1988-12-15 1991-05-02 Ciba-Geigy Ag Retrovirale Proteasehemmer
US5270302A (en) 1988-12-21 1993-12-14 Abbott Laboratories Derivatives of tetrapeptides as CCK agonists
GB8909836D0 (en) 1989-04-28 1989-06-14 Boots Co Plc Therapeutic agent
US5504109A (en) 1989-05-13 1996-04-02 Bayer Aktiengesellschaft Susbstituted amino acid amide derivatives their preparation and use
DE3915755A1 (de) 1989-05-13 1990-11-29 Bayer Ag Fungizide mittel sowie substituierte aminosaeureamid-derivate und deren herstellung
US5196291A (en) 1989-05-24 1993-03-23 Fuji Photo Film Co., Ltd. Silver halide photographic material
JP2658004B2 (ja) 1989-05-31 1997-09-30 キヤノン株式会社 電子写真感光体
JPH0462788A (ja) 1990-06-30 1992-02-27 Toshiba Corp 電子レンジ
FR2665159B1 (fr) 1990-07-24 1992-11-13 Rhone Poulenc Sante Nouveaux derives de la pyridine et de la quinoleine, leur preparation et les compositions pharmaceutiques qui les contiennent.
JPH06145173A (ja) 1990-08-21 1994-05-24 Fujisawa Pharmaceut Co Ltd １−アザビシクロ［３．２．０］ヘプト−２−エン−２−カルボン酸化合物
JPH0511439A (ja) 1990-09-13 1993-01-22 Fuji Photo Film Co Ltd 光重合性組成物
DE4035961A1 (de) 1990-11-02 1992-05-07 Thomae Gmbh Dr K Cyclische iminoderivate, diese verbindungen enthaltende arzneimittel und verfahren zu ihrer herstellung
WO1992010675A1 (en) 1990-12-07 1992-06-25 Dyno Industrier A.S System for utilization of wave energy
DE4104257A1 (de) 1991-02-13 1992-08-20 Boehringer Ingelheim Kg Verwendung von anellierten tetrahydropyridinessigsaeurederivaten fuer die behandlung neurologischer erkrankungen
US5206249A (en) 1991-03-27 1993-04-27 Du Pont Merck Pharmaceutical Company Bis-naphthalimides containing amino-acid derived linkers as anticancer agents
US5461176A (en) 1991-03-27 1995-10-24 The Du Pont Merck Pharmaceutical Company Processes for preparing bis-naphthalimides containing amino-acid derived linkers
US5190922A (en) 1991-06-04 1993-03-02 Abbott Laboratories Terminally modified tri-, tetra- and pentapeptide anaphylatoxin receptor ligands
EP0668870A1 (en) 1991-06-14 1995-08-30 Chiron Corporation Inhibitors of picornavirus proteases
US5250732A (en) 1991-07-18 1993-10-05 Genentech, Inc. Ketamine analogues for treatment of thrombocytopenia
US5298377A (en) 1991-08-28 1994-03-29 Eastman Kodak Company Photographic element with 2-equivalent magenta dye-forming coupler and filter dye
US5215876A (en) 1991-08-29 1993-06-01 Eastman Kodak Company Radiographic element with uv absorbation compound in polyester support
US5204349A (en) 1991-09-16 1993-04-20 Merck & Co., Inc. Amide-substituted derivatives of spiroindanylcamphorsulfonyl oxytocin antagonists
JP2947539B2 (ja) 1991-11-12 1999-09-13 コニカ株式会社 ハロゲン化銀写真感光材料
KR100236806B1 (ko) 1991-12-10 2000-01-15 시오노 요시히코 방향족 설폰아미드계 하이드록삼산 유도체
EP0547699A1 (en) 1991-12-19 1993-06-23 Merck & Co. Inc. Peptidyl derivatives as inhibitors of interleukin-1B converting enzyme
GB9200209D0 (en) 1992-01-07 1992-02-26 British Bio Technology Compounds
US5218123A (en) 1992-02-18 1993-06-08 Warner-Lambert Company Didehydrotryptophan derivatives and pharmaceutical use thereof
US5831002A (en) 1992-05-20 1998-11-03 Basf Aktiengesellschaft Antitumor peptides
JPH063787A (ja) 1992-06-18 1994-01-14 Konica Corp ハロゲン化銀写真感光材料用固形発色現像処理剤及び該固形発色現像処理剤を用いた処理方法
WO1994000435A1 (de) 1992-06-22 1994-01-06 Boehringer Ingelheim Kg Anellierte dihydropyridine und deren verwendung für die herstellung von pharmazeutischen zubereitungen
FR2694006A1 (fr) 1992-07-22 1994-01-28 Esteve Labor Dr Amides dérivés de benzohétérocyles.
DE4225487A1 (de) 1992-07-30 1994-02-03 Schering Ag Interphenylen-bicyclo(3.3.0)octan-Derivate, Verfahren zu ihrer Herstellung und ihre pharmazeutische Verwendung
JPH0651451A (ja) 1992-07-31 1994-02-25 Konica Corp ハロゲン化銀写真感光材料用固形処理剤
JP3168547B2 (ja) 1992-08-18 2001-05-21 日本製粉株式会社 ポテト生地用ミックス、ポテト生地の製造法およびポテト生地を用いたフライ食品
JP3283114B2 (ja) 1992-09-07 2002-05-20 クミアイ化学工業株式会社 縮合ヘテロ環誘導体及び農園芸用殺菌剤
US5389682A (en) 1992-09-18 1995-02-14 Warner-Lambert Company Agents acting at cholecystokinin receptors
DE4232505A1 (de) 1992-09-29 1994-03-31 Degussa Verfahren zur Reduktion von Carbonsäuren oder Carbonsäurederivaten sowie neue Verbindungen
DE69329544T2 (de) 1992-12-22 2001-05-31 Eli Lilly And Co., Indianapolis HIV Protease hemmende Verbindungen
DE4303145A1 (de) 1993-01-30 1994-08-04 Schering Ag Interphenylen-2-Oxabicyclo(2.2.1)heptan-Derivate, Verfahren zu ihrer Herstellung und ihre pharmazeutische Verwendung
JP2848232B2 (ja) 1993-02-19 1999-01-20 武田薬品工業株式会社 アルデヒド誘導体
AU6019794A (en) 1993-03-18 1994-10-11 Pfizer Inc. Antibacterial 16-membered ring macrolides containing olefins at c-20
WO1994022911A2 (en) 1993-03-29 1994-10-13 The Du Pont Merck Pharmaceutical Company A PROCESS AND INTERMEDIATE COMPOUNDS USEFUL FOR THE PREPARATION OF PLATELET GLYCOPROTEIN IIb/IIIa INHIBITORS CONTAINING Nα-METHYLARGININE
JPH06340643A (ja) 1993-04-04 1994-12-13 Nippon Nohyaku Co Ltd オキサゾ−ル又はチアゾ−ル誘導体及びその製造方法並びに除草剤
JP3165760B2 (ja) 1993-04-12 2001-05-14 株式会社トクヤマ 新規化合物
US5658885A (en) 1993-04-27 1997-08-19 The Dupont Merck Pharmaceutical Company Amidino and guanidino substituted boronic acid inhibitors of trypsin-like enzymes
WO1994025432A1 (en) 1993-04-28 1994-11-10 Kumiai Chemical Industry Co., Ltd. Amino acid amide derivative, agrohorticultural bactericide, and production process
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
DE4321897A1 (de) 1993-07-01 1995-01-12 Hoechst Schering Agrevo Gmbh Substituierte Aminosäureamid-Derivate, Verfahren zu ihrer Herstellung, diese enthaltende Mittel und ihre Verwendung
US5514778A (en) 1993-07-01 1996-05-07 Eli Lilly And Company Anti-picornaviral agents
DE4322067A1 (de) 1993-07-02 1995-01-12 Hoechst Schering Agrevo Gmbh Acylierte Aminophenylsulfonylharnstoffe; Darstellung und Verwendung als Herbizide und Wachstumsregulatoren
CH686479A5 (fr) 1993-08-11 1996-04-15 Nestle Sa Produit alimentaire a rehydratation rapide et son procede de preparation.
US5554753A (en) 1993-08-25 1996-09-10 Indiana University Foundation Catalytic enantioselective synthesis of α-amino acid derivatives by phase-transfer catalysis
JPH07101959A (ja) 1993-09-30 1995-04-18 Sankyo Co Ltd １−メチルカルバペネム誘導体
DK0721449T3 (da) 1993-10-01 2002-04-22 Merrell Pharma Inc Inhibitorer af beta-amyloidproteinproduktion
IT1270882B (it) 1993-10-05 1997-05-13 Isagro Srl Oligopeptidi ad attivita' fungicida
JP3075657B2 (ja) 1993-10-15 2000-08-14 富士写真フイルム株式会社 写真用処理組成物及び処理方法
US5780498A (en) 1993-11-01 1998-07-14 Ciba-Geigy Japan Limited Endothelin receptor antagonists
US5486623A (en) 1993-12-08 1996-01-23 Prototek, Inc. Cysteine protease inhibitors containing heterocyclic leaving groups
US5714484A (en) 1993-12-08 1998-02-03 Prototek, Inc. α-(1,3-dicarbonylenol ether) methyl ketones as cysteine protease inhibitors
DE4343528A1 (de) 1993-12-16 1995-06-22 Schering Ag Zweifach heterocyclisch substituierte Benzole und Pyridine, Verfahren zu ihrer Herstellung und ihre Verwendung als Schädlingsbekämpfungsmittel
IL112759A0 (en) 1994-02-25 1995-05-26 Khepri Pharmaceuticals Inc Novel cysteine protease inhibitors
EP0749418B1 (en) 1994-03-10 2000-08-30 G.D. Searle & Co. L-n6 -(1-iminoethyl)lysine derivatives useful as nitric oxide synthase inhibitors
DK0672654T3 (da) 1994-03-19 1997-10-13 Basf Ag Fungicide carbamoyloximcarboxylsyreamider
JPH07285931A (ja) 1994-04-19 1995-10-31 Tokuyama Corp 新規化合物
DE4415049A1 (de) 1994-04-29 1995-11-02 Hoechst Schering Agrevo Gmbh Acylierte Aminophenylsulfonylharnstoffe, Verfahren zu deren Herstellung und Verwendung als Herbizide und Wachstumsregulatoren
DE4419517A1 (de) 1994-06-03 1995-12-07 Basf Ag Substituierte 3-Phenylpyrazole
US5847135A (en) 1994-06-17 1998-12-08 Vertex Pharmaceuticals, Incorporated Inhibitors of interleukin-1β converting enzyme
US5716929A (en) 1994-06-17 1998-02-10 Vertex Pharmaceuticals, Inc. Inhibitors of interleukin-1β converting enzyme
DE4431467A1 (de) 1994-09-03 1996-03-07 Basf Ag Caramoylcarbonsäureamide
CA2200981A1 (en) 1994-10-04 1996-04-11 Hisashi Takasugi Urea derivatives and their use as acat-inhibitors
CA2200433C (en) 1994-10-26 2006-02-07 Douglas K. Hutchinson Phenyloxazolidinone antimicrobials
CA2163325A1 (en) 1994-11-21 1996-05-22 Kaneyoshi Kato Amine compounds, their production and use
ES2193202T3 (es) 1994-12-02 2003-11-01 Yamanouchi Pharma Co Ltd Nuevo derivado de amidinonaftilo o sal de este.
US5872101A (en) 1995-01-06 1999-02-16 Sibia Neurosciences, Inc. Methods of treating neurodegenerative disorders using protease inhibitors
US5804560A (en) 1995-01-06 1998-09-08 Sibia Neurosciences, Inc. Peptide and peptide analog protease inhibitors
US5691368A (en) 1995-01-11 1997-11-25 Hoechst Marion Roussel, Inc. Substituted oxazolidine calpain and/or cathepsin B inhibitors
DE19501841A1 (de) 1995-01-23 1996-07-25 Bayer Ag Aminosäureamide
DE19505932B4 (de) 1995-02-21 2005-06-23 Degussa Ag Verfahren zur Herstellung von Oxazolidinonen, neue Oxazolidinone sowie Verwendung von Oxazolidinonen
US5710129A (en) 1995-02-23 1998-01-20 Ariad Pharmaceuticals, Inc. Inhibitors of SH2-mediated processes
JPH08248579A (ja) 1995-03-14 1996-09-27 Mitsubishi Paper Mills Ltd ハロゲン化銀写真感光材料及びその処理方法
US5776718A (en) * 1995-03-24 1998-07-07 Arris Pharmaceutical Corporation Reversible protease inhibitors
CA2216151A1 (en) 1995-03-24 1996-10-03 Arris Pharmaceutical Corporation Reversible protease inhibitors
IN186549B (pt) 1995-04-19 2001-09-29 Kumiai Chemical Co Ltd
GB9508195D0 (en) 1995-04-20 1995-06-07 Univ British Columbia Novel biologically active compounds and compositions,their use and derivation
JPH11505522A (ja) 1995-04-21 1999-05-21 ノバルティス・アクチエンゲゼルシャフト エンドセリン阻害剤としてのｎ−アロイルアミノ酸アミド
JPH08319291A (ja) 1995-05-25 1996-12-03 Meiji Seika Kaisha Ltd 新規セフェム誘導体
EP0832065B1 (en) 1995-06-06 2001-10-10 Pfizer Inc. Substituted n-(indole-2-carbonyl)-glycinamides and derivatives as glycogen phosphorylase inhibitors
US5756528A (en) 1995-06-06 1998-05-26 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
AU6099496A (en) 1995-06-07 1996-12-30 G.D. Searle & Co. Pipecolic acid derivatives of proline threonine amides usefu l for the treatment of rheumatoid arthritis
US6069130A (en) 1995-06-07 2000-05-30 Cor Therapeutics, Inc. Ketoheterocyclic inhibitors of factor Xa
US5827866A (en) 1995-06-07 1998-10-27 Ortho Pharmaceutical Corporation Peptidyl heterocycles useful in the treatment of thrombin related disorders
TW438591B (en) 1995-06-07 2001-06-07 Arris Pharm Corp Reversible cysteine protease inhibitors
US5827860A (en) 1995-06-07 1998-10-27 Ortho Pharmaceutical Corporation Peptidyl heterocycles useful in the treatment of thrombin related disorders
CA2225255A1 (en) 1995-06-29 1997-01-16 Merck & Co., Inc. Combinations of inhibitors of farnesyl-protein transferase
CA2226303A1 (en) 1995-07-07 1997-01-30 Sagami Chemical Research Center Peptide derivatives and angiotensin iv receptor agonist
GB9518552D0 (en) 1995-09-11 1995-11-08 Fujisawa Pharmaceutical Co New heterocyclic compounds
US5744451A (en) 1995-09-12 1998-04-28 Warner-Lambert Company N-substituted glutamic acid derivatives with interleukin-1 β converting enzyme inhibitory activity
AR004980A1 (es) 1995-11-29 1999-04-07 Nihon Nohyaku Co Ltd Fungicida para la fruta de cultivo, derivado de fenilalanina comprendido como ingrediente activo en el mismo y metodo para controlar enfermedades enplantas aplicando dicho fungicida.
TW474946B (en) 1995-12-15 2002-02-01 Basf Ag Novel compounds, the preparation and use thereof
US5843904A (en) 1995-12-20 1998-12-01 Vertex Pharmaceuticals, Inc. Inhibitors of interleukin-1βconverting enzyme
IL124436A0 (en) 1995-12-29 1998-12-06 Boehringer Ingelheim Phaarmace Phenyl thiazole derivatives with anti herpes virus properties
AU1529997A (en) 1996-01-16 1997-08-11 Warner-Lambert Company Substituted histidine inhibitors of protein farnesyltransferase
AU1595997A (en) 1996-01-26 1997-08-20 Smithkline Beecham Plc Thienoxazinone derivatives useful as antiviral agents
US6288037B1 (en) 1996-01-29 2001-09-11 Basf Aktiengesellschaft Substrates and inhibitors for cysteine protease ICH-1
AU2277597A (en) 1996-02-23 1997-09-10 Ariad Pharmaceuticals, Inc. New inhibitors of sh2-mediated processes
DE19609955A1 (de) 1996-03-14 1997-09-18 Basf Ag Amidonitrile, Verfahren zu ihrer Herstellung, ihre Verwendung als Kaltbleichaktivatoren oder optische Aufheller in Wasch-, Reinigungs- und Bleichmitteln sowie ihre Verwendung als Ausgangsmaterial bei der Herstellung von Amidocarbonsäuren und Amidocarbonsäure-Derivaten
CA2204082A1 (en) 1996-05-03 1997-11-03 Michael William John Urquhart Pharmaceutical compounds
DE19621522A1 (de) 1996-05-29 1997-12-04 Hoechst Schering Agrevo Gmbh Neue N-Acylsulfonamide, neue Mischungen aus Herbiziden und Antidots und deren Verwendung
DE19621483A1 (de) 1996-05-29 1997-12-04 Hoechst Ag Substituierte 2-Naphthoylguanidine, Verfahren zur ihrer Herstellung, ihre Verwendung als Medikament oder Diagnostikum sowie sie enthaltendes Medikament
DE59706319D1 (de) 1996-05-31 2002-03-21 Basf Ag Carbamoylcarbonsäureamidoxime
DE19629717C1 (de) 1996-07-25 1998-02-12 Hoechst Ag Verfahren zur katalytischen Herstellung von N-Acylglycinderivaten
US5939527A (en) 1996-07-30 1999-08-17 Basf Aktiengesellschaft Tetrapeptides as antitumor agents
US6251911B1 (en) 1996-10-02 2001-06-26 Novartis Ag Pyrimidine derivatives and processes for the preparation thereof
EE04023B1 (et) 1996-10-18 2003-04-15 Vertex Pharmaceuticals Incorporated Seriinproteaaside, eriti C-hepatiidi viiruse NS3-proteaasi inhibiitorid
EP0844248B1 (de) 1996-10-28 2002-07-10 Rolic AG Vernetzbare, photoaktive Silanderivate
US6204221B1 (en) 1996-11-12 2001-03-20 Syngenta Crop Protection, Inc. Herbicides
PL334516A1 (en) 1996-11-22 2000-02-28 Elan Pharm Inc N-(aryl/heteroaryl/alkylacetyl)amino cid amides, pharmaceutic agent containing them and method of inhibiting eduction and/or synthesis of beta-amyloid peptide using such compounds
US5952322A (en) 1996-12-05 1999-09-14 Pfizer Inc. Method of reducing tissue damage associated with non-cardiac ischemia using glycogen phosphorylase inhibitors
AU5522498A (en) 1996-12-13 1998-07-03 Merck & Co., Inc. Substituted aryl piperazines as modulators of chemokine receptor activity
ES2190425T3 (es) 1996-12-19 2003-08-01 Isagro Spa Procedimiento para la preparacion de alaninato de (n-fenilacetil-n-2,6-xilil)metilo.
DE19653647A1 (de) 1996-12-20 1998-06-25 Hoechst Ag Vitronectin - Rezeptorantagonisten, deren Herstellung sowie deren Verwendung
KR20000062284A (ko) 1996-12-23 2000-10-25 블레어 큐. 퍼거슨 인자 Ｘａ 억제제로서의 질소 함유 헤테로방향족 화합물
AR011164A1 (es) 1997-02-28 2000-08-02 Lilly Co Eli Compuestos heterociclicos, composiciones farmaceuticas que los comprenden, y metodos para inhibir la liberacion del peptido beta-amiloide y/o su sintesismediante el uso de dichos compuestos
FR2762315B1 (fr) 1997-04-22 1999-05-28 Logeais Labor Jacques Derives d'amino-acides inhibiteurs des metalloproteases de la matrice extracellulaire et de la liberation du tnf alpha
AU7726898A (en) 1997-05-22 1998-12-11 G.D. Searle & Co. Pyrazole derivatives as p38 kinase inhibitors
CA2291065C (en) 1997-05-23 2010-02-09 Bayer Corporation Raf kinase inhibitors
ES2151467T3 (es) 1997-05-23 2005-03-01 Bayer Corporation Arilureas para el tratamiento de enfermedades inflamatorias o inmunomoduladoras.
ZA985247B (en) 1997-06-19 1999-12-17 Du Pont Merck Pharma Guanidine mimics as factor Xa inhibitors.
SI20208A (sl) 1997-06-19 2000-10-31 Dupont Pharmaceuticals Company INHIBITORJI FAKTORJA Xa Z NEVTRALNO P1 SPECIFIČNO SKUPINO
EP0897908A1 (de) 1997-08-19 1999-02-24 Roche Diagnostics GmbH 3-Aryl-Succinamido-Hydroxamsäuren, Prozesse zu ihrer Herstellung und diese Substanzen enthaltende Medikamente
JP3002872B2 (ja) 1997-09-05 2000-01-24 ヒエン電工株式会社 ケ−ブル吊り下げ用螺旋状支持具の引き紐通し具
JPH11100373A (ja) 1997-09-26 1999-04-13 Eisai Co Ltd 新規フェノチアジン誘導体及びその医薬
US5872122A (en) 1997-10-16 1999-02-16 Monsanto Company Pyrimidinylamidino β-amino acid derivatives useful as inhibitors of platelet aggregation
JP4555468B2 (ja) 1997-10-31 2010-09-29 アベンテイス・フアルマ・リミテツド 置換アニリド
HUP0004400A3 (en) 1997-11-05 2002-10-28 Novartis Ag Dipeptide nitriles, process for their preparation, pharmaceutical compositions comprising thereof and their use
IL136767A0 (en) 1997-12-22 2001-06-14 Bayer Ag Inhibition of raf kinase using substituted heterocyclic ureas
RU2265597C2 (ru) 1997-12-22 2005-12-10 Байер Копэрейшн Арил- и гетероарилзамещенные гетероциклические производные мочевины, способ ингибирования киназы raf и фармацевтическая композиция
IL139416A0 (en) 1998-05-05 2001-11-25 Warner Lambert Company Basf Ag Succinamide inhibitors of interleukin-1? converting enzyme
WO1999063115A2 (en) 1998-06-04 1999-12-09 Reprogen, Inc. Use of cathepsin s in the diagnosis and treatment of endometriosis
WO2000051998A1 (en) 1999-03-02 2000-09-08 Boehringer Ingelheim Pharmaceuticals, Inc. Compounds useful as reversible inhibitors of cathepsin s
UA76088C2 (en) 1999-03-15 2006-07-17 Axys Pharm Inc N-cyanomethyl amides as cysteine protease inhibitors
EP1136575A4 (en) * 1999-08-10 2008-04-23 Jfe Steel Corp PROCESS FOR PRODUCING COLD LAMINATED STEEL STRIPS
US6420364B1 (en) * 1999-09-13 2002-07-16 Boehringer Ingelheim Pharmaceuticals, Inc. Compound useful as reversible inhibitors of cysteine proteases
WO2001019816A1 (en) 1999-09-13 2001-03-22 Boehringer Ingelheim Pharmaceuticals, Inc. Novel spiroheterocyclic compounds useful as reversible inhibitors of cysteine proteases
ATE464402T1 (de) * 1999-09-16 2010-04-15 Jfe Steel Corp Verfahren zur herstellung einer dünnen stahlplatte mit hoher festigkeit
KR100419080B1 (ko) * 1999-09-28 2004-02-18 제이에프이 엔지니어링 가부시키가이샤 고장력 열연강판 및 그 제조방법
ATE490349T1 (de) * 1999-09-29 2010-12-15 Jfe Steel Corp Stahlblech und verfahren zu dessen herstellung
KR100401272B1 (ko) * 1999-09-29 2003-10-17 닛폰 고칸 가부시키가이샤 박강판 및 박강판의 제조방법
CN1331183A (zh) 2000-06-28 2002-01-16 上海博德基因开发有限公司 一种新的多肽——人dna修复蛋白10.23和编码这种多肽的多核苷酸

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