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HRP20030163A2 - 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
HRP20030163A2
HRP20030163A2 HR20030163A HRP20030163A HRP20030163A2 HR P20030163 A2 HRP20030163 A2 HR P20030163A2 HR 20030163 A HR20030163 A HR 20030163A HR P20030163 A HRP20030163 A HR P20030163A HR P20030163 A2 HRP20030163 A2 HR P20030163A2
Authority
HR
Croatia
Prior art keywords
cyano
piperidin
methyl
cyclohexyl
ylcarbamoyl
Prior art date
Application number
HR20030163A
Other languages
English (en)
Croatian (hr)
Inventor
Bekkali Younes
R. Hickey Eugene
Liu Weimen
R. Patel Usha
M. Spero Denise
Sun Sanxing
S. Thomson David
D. Ward Yancey
R. R. Young Erick
Original Assignee
Boehringer Ingelheim Pharmaceuticals Inc.
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 Pharmaceuticals Inc. filed Critical Boehringer Ingelheim Pharmaceuticals Inc.
Publication of HRP20030163A2 publication Critical patent/HRP20030163A2/hr

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    • 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
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    • 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
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    • 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
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    • 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
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    • 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
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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
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    • 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
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    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
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    • 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
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    • 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
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    • 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
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    • 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
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    • 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
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    • 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
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    • 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
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    • 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
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    • 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
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    • 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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HR20030163A 2000-09-08 2001-03-14 Spiroheterocyclic nitriles useful as reversible inhibitors of cysteine proteases HRP20030163A2 (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
HRP20030163A2 true HRP20030163A2 (en) 2005-04-30

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ID=24628539

Family Applications (1)

Application Number Title Priority Date Filing Date
HR20030163A HRP20030163A2 (en) 2000-09-08 2001-03-14 Spiroheterocyclic nitriles useful as reversible inhibitors of cysteine proteases

Country Status (24)

Country Link
US (10) US6420364B1 (et)
EP (1) EP1322613A1 (et)
JP (1) JP2004508356A (et)
KR (1) KR20030051644A (et)
CN (1) CN1303067C (et)
AU (1) AU2001245694A1 (et)
BG (1) BG107585A (et)
BR (1) BR0113740A (et)
CA (1) CA2417177A1 (et)
CZ (1) CZ2003603A3 (et)
EA (1) EA005203B1 (et)
EE (1) EE200300093A (et)
HR (1) HRP20030163A2 (et)
HU (1) HUP0303934A2 (et)
IL (1) IL154080A0 (et)
MX (1) MXPA03001947A (et)
NO (1) NO20031065D0 (et)
NZ (1) NZ525169A (et)
PL (1) PL361038A1 (et)
SK (1) SK2862003A3 (et)
UA (1) UA73378C2 (et)
WO (1) WO2002020485A1 (et)
YU (1) YU17003A (et)
ZA (1) ZA200301032B (et)

Families Citing this family (74)

* 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
AU3731400A (en) * 1999-03-05 2000-09-21 Trustees Of University Technology Corporation, The Methods and compositions useful in inhibiting apoptosis
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
WO2002051983A2 (en) 2000-12-22 2002-07-04 Axys Pharmaceuticals, Inc. Novel compounds and compositions as cathepsin inhibitors
ATE409482T1 (de) * 2001-03-02 2008-10-15 Merck Frosst Canada Ltd Cathepsincystein-proteasehemmer
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
KR20040044920A (ko) 2001-09-14 2004-05-31 아벤티스 파마슈티칼스 인크. 카뎁신 억제제로서 신규한 화합물 및 조성물
CA2459825A1 (en) * 2001-10-02 2003-04-10 Boehringer Ingelheim Pharmaceuticals, Inc. Compounds useful as reversible inhibitors of cysteine proteases
CA2463770A1 (en) * 2001-10-29 2003-05-08 Boehringer Ingelheim Pharmaceuticals, Inc. Compounds useful as reversible inhibitors of cysteine proteases
CA2467391A1 (en) 2001-11-14 2003-05-22 Aventis Pharmaceuticals Inc. Oligopeptides and compositions containing them as cathepsin s inhibitors
US7101880B2 (en) * 2002-06-24 2006-09-05 Schering Aktiengesellschaft 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
US7384970B2 (en) * 2003-03-24 2008-06-10 Irm Llc Inhibitors of cathepsin S
US7109243B2 (en) * 2003-03-24 2006-09-19 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
US7662849B2 (en) * 2003-06-04 2010-02-16 Virobay, Inc. 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
SG146658A1 (en) * 2003-09-18 2008-10-30 Schering Ag Haloalkyl containing compounds as cysteine protease inhibitors
US7186827B2 (en) * 2003-10-30 2007-03-06 Boehringer Ingelheim Pharmaceuticals, Inc. Dipeptide synthesis
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
EP1694357A1 (en) * 2003-12-11 2006-08-30 Axys Pharmaceuticals, Inc. Use of cathepsin s inhibitors for treating an immune response caused by administration of a small molecule therapeutic or biologic
CA2548600A1 (en) * 2003-12-12 2005-06-23 Merck Frosst Canada & Co. 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
US20080125442A1 (en) * 2005-01-19 2008-05-29 Michael David Percival Cathepsin K Inhibitors and Atherosclerosis
NZ561681A (en) * 2005-03-21 2011-01-28 Virobay Inc Alpha ketoamide compounds as cysteine protease inhibitors
WO2006102535A2 (en) * 2005-03-22 2006-09-28 Celera Genomics Sulfonyl containing compounds as cysteine protease inhibitors
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
US20100016289A1 (en) * 2005-11-01 2010-01-21 Kevin Sprott Compounds Useful as Antagonists of CCR2
EP1951706A1 (en) 2005-11-01 2008-08-06 Janssen Pharmaceutica N.V. Dihydroisoindolones as allosteric modulators of glucokinase
US8067415B2 (en) * 2005-11-01 2011-11-29 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
MX2008014800A (es) * 2006-06-01 2008-12-02 Sanofi Aventis Nitrilos espirociclicos como inhibidores de proteasa.
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
US8071625B2 (en) * 2006-08-02 2011-12-06 Cytokinetics, Inc. Certain chemical entities, compositions, and methods
US8063082B2 (en) * 2006-08-02 2011-11-22 Cytokinetics, Inc. Certain chemical entities, compositions, and methods
US7893112B2 (en) 2006-10-04 2011-02-22 Virobay, Inc. Di-fluoro containing compounds as cysteine protease inhibitors
NZ576105A (en) * 2006-10-04 2012-01-12 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
NZ583351A (en) 2007-08-15 2012-05-25 Cytokinetics Inc Modulate smooth muscle myosin and/or non-muscle myosin
DK2222636T3 (da) 2007-12-21 2013-06-03 Ligand Pharm Inc Selektive androgenreceptormodulatorer (SARMS) og anvendelser deraf
EP2240491B1 (en) 2008-01-09 2015-07-15 Amura Therapeutics Limited TETRAHYDROFURO(2,3-b)PYRROL-3-ONE DERIVATIVES AS INHIBITORS OF CYSTEINE PROTEINASES
WO2010028236A1 (en) * 2008-09-05 2010-03-11 Avila Therapeutics, Inc. Algorithm for designing irreversible inhibitors
EP2398320A4 (en) * 2009-02-19 2012-09-19 Univ Vanderbilt ALLOSTERIC ANTAGONISTS OF AMIDOBIPIPERIDINECARBOXYLATE M1, ANALOGUES AND DERIVATIVES THEREOF, AND METHODS FOR THEIR MANUFACTURE AND USE
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
NZ620174A (en) * 2009-09-16 2016-08-26 Celgene Avilomics Res Inc Protein kinase conjugates and inhibitors
WO2011082285A1 (en) 2009-12-30 2011-07-07 Avila Therapeutics, Inc. Ligand-directed covalent modification of protein
WO2012151319A1 (en) 2011-05-02 2012-11-08 Virobay, Inc. Cathepsin inhibitors for the treatment of bone cancer and bone cancer pain
CN103764636A (zh) 2011-06-07 2014-04-30 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
SG11201402405QA (en) 2011-11-18 2014-09-26 Heptares Therapeutics Ltd Muscarinic m1 receptor agonists
CA2898077C (en) 2013-01-15 2021-10-19 Merck Patent Gmbh Acylguanidines for treating osteoarthritis
WO2015108988A2 (en) 2014-01-17 2015-07-23 Ligand Pharmaceuticals, Inc. 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
GB201519352D0 (en) 2015-11-02 2015-12-16 Heptares Therapeutics Ltd Pharmaceutical compounds
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
CN114096522A (zh) 2019-04-19 2022-02-25 利亘制药公司 化合物的晶型和制备化合物的晶型的方法
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 (171)

* 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 (et) 1967-02-16 1968-05-09
FI840260A7 (fi) 1983-01-27 1984-07-28 Ciba Geigy Ag Pyrrolidinonijohdannaiset ja menetelmä niiden valmistamiseksi.
US4767202A (en) * 1984-01-20 1988-08-30 Minolta Camera Kabushiki Kaisha Objective lens system for optical recording type disks
EP0181351A4 (en) * 1984-05-09 1989-06-21 Univ Australian METHOD FOR MODULATING IMMUNE REACTION.
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
EP0389535A1 (en) 1987-10-26 1990-10-03 Warner-Lambert Company Renin inhibitors, processes for preparing them, methods for using them, and compositions containing them
US5004743A (en) 1987-11-25 1991-04-02 Merck Frosst Canada, Inc. Pyridyl styrene dialkanoic acids as anti-leukotriene agents
US4962117A (en) 1987-11-25 1990-10-09 Merck Frosst Canada, Inc. Heterazole dialkanoic acids
US4957932A (en) 1987-11-25 1990-09-18 Merck Frosst Canada, Inc. Benzoheterazoles
EP0336356A3 (en) 1988-04-05 1991-09-25 Abbott Laboratories Derivatives of tryptophan as cck antagonists
US5346907A (en) 1988-04-05 1994-09-13 Abbott Laboratories Amino acid analog 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
DE3915755A1 (de) 1989-05-13 1990-11-29 Bayer Ag Fungizide mittel sowie substituierte aminosaeureamid-derivate und deren herstellung
US5504109A (en) 1989-05-13 1996-04-02 Bayer Aktiengesellschaft Susbstituted amino acid amide derivatives their preparation and use
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
AU9042191A (en) 1990-12-07 1992-07-08 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
CA2111471A1 (en) 1991-06-14 1992-12-23 Bruce Malcolm 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
EP0570594B1 (en) 1991-12-10 1997-07-30 Shionogi & Co., Ltd. Hydroxamic acid derivative based on aromatic sulfonamide
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
EP0604182B1 (en) 1992-12-22 2000-10-11 Eli Lilly And Company Inhibitors of HIV protease useful for the treatment of Aids
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
AU6697694A (en) 1993-03-29 1994-10-24 Du Pont Merck Pharmaceutical Company, The A process and intermediate compounds useful for the preparation of platelet glycoprotein IIb/IIIa inhibitors containing N alpha--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
BR9405281A (pt) 1993-04-28 1999-08-31 Kumiai Chemical Industry Co Derivados de amida de amino ácido, fungicidas para agricultura ou horticultura, e método para produção dos mesmos
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
HU221629B1 (hu) 1993-10-01 2002-12-28 Merrell Pharmaceuticals Inc. Béta-amiloid fehérje képződést gátló peptidek, eljárás előállításukra és ezeket tartalmazó gyógyszerkészítmények
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
JPH09504302A (ja) 1993-11-01 1997-04-28 日本チバガイギー株式会社 エンドセリン・レセプター・アンタゴニスト
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
ATE195933T1 (de) 1994-03-10 2000-09-15 Searle & Co L-n6-(1-iminoethyl)lysin - derivate und ihre verwendung als no-synthase - inhibitoren
ES2108504T3 (es) 1994-03-19 1997-12-16 Basf Ag Amidas del acido carbamoiloximcarboxilico fungicidas.
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
JPH10510512A (ja) 1994-10-04 1998-10-13 藤沢薬品工業株式会社 尿素誘導体とａｃａｔ阻害剤としての用途
EP0788498B1 (en) 1994-10-26 2001-08-16 PHARMACIA & UPJOHN COMPANY Phenyloxazolidinone antimicrobials
CA2163325A1 (en) 1994-11-21 1996-05-22 Kaneyoshi Kato Amine compounds, their production and use
TW300888B (et) 1994-12-02 1997-03-21 Yamanouchi Pharma Co Ltd
US5804560A (en) 1995-01-06 1998-09-08 Sibia Neurosciences, Inc. Peptide and peptide analog protease inhibitors
US6017887A (en) 1995-01-06 2000-01-25 Sibia Neurosciences, Inc. Peptide, peptide analog and amino acid 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
CA2216151A1 (en) 1995-03-24 1996-10-03 Arris Pharmaceutical Corporation Reversible protease inhibitors
US5776718A (en) * 1995-03-24 1998-07-07 Arris Pharmaceutical Corporation Reversible protease inhibitors
IN186549B (et) 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
WO1996033170A1 (en) 1995-04-21 1996-10-24 Novarits Ag N-aroylamino acid amides as endothelin inhibitors
JPH08319291A (ja) 1995-05-25 1996-12-03 Meiji Seika Kaisha Ltd 新規セフェム誘導体
CA2342471C (en) 1995-06-06 2002-10-29 Judith L. Treadway Heterocyclecarbonylmethyl amine intermediates
US5756528A (en) 1995-06-06 1998-05-26 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5827866A (en) 1995-06-07 1998-10-27 Ortho Pharmaceutical Corporation Peptidyl heterocycles useful in the treatment of thrombin related disorders
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
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
US6069130A (en) 1995-06-07 2000-05-30 Cor Therapeutics, Inc. Ketoheterocyclic inhibitors of factor Xa
EP0836383A1 (en) 1995-06-29 1998-04-22 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
PL327582A1 (en) 1995-12-29 1998-12-21 Boehringer Ingelheim Pharma Derivatives of phenylthiazole exhibiting antiviral properties against herpes virues
AU1529997A (en) 1996-01-16 1997-08-11 Warner-Lambert Company Substituted histidine inhibitors of protein farnesyltransferase
WO1997027200A1 (en) 1996-01-26 1997-07-31 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
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
DE19621522A1 (de) 1996-05-29 1997-12-04 Hoechst Schering Agrevo Gmbh Neue N-Acylsulfonamide, neue Mischungen aus Herbiziden und Antidots und deren Verwendung
US6124345A (en) 1996-05-31 2000-09-26 Basf Aktiengesellschaft Carbamoyl carboxylic acid amide oximes
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
EP0929553B1 (en) 1996-10-02 2005-03-16 Novartis AG Pyrimidine derivatives and processes for the preparation thereof
BR9712544B1 (pt) 1996-10-18 2013-10-22 Inibidores de proteases de serina, composição farmacêutica compreendendo os mesmos e seus usos
EP0844248B1 (de) 1996-10-28 2002-07-10 Rolic AG Vernetzbare, photoaktive Silanderivate
KR20000053201A (ko) 1996-11-12 2000-08-25 한스 루돌프 하우스, 헨리테 브룬너, 베아트리체 귄터 제초제로서 유용한 피라졸 유도체
CA2272065A1 (en) 1996-11-22 1998-05-28 Thomas E. Mabry N-(aryl/heteroaryl/alkylacetyl) amino acid amides, pharmaceutical compositions comprising same, and methods for inhibiting .beta.-amyloid peptide release and/or its synthesis by use of 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
WO1998025617A1 (en) 1996-12-13 1998-06-18 Merck & Co., Inc. Substituted aryl piperazines as modulators of chemokine receptor activity
AU5756798A (en) 1996-12-19 1998-07-15 Isagro S.P.A. Fungicidal compositions based on (n-phenylacetyl-n-2,6-xylyl)methyl alaninate
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
HRP980093A2 (en) 1997-02-28 1998-12-31 Lilly Co Eli Heterocyclic compounds, pharmaceutical compositions comprising same, and methods for inhibiting "beta"-amyloid peptide release and/or its synthesis by use of such compounds
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
JP2002502380A (ja) 1997-05-22 2002-01-22 ジー．ディー．サール アンド カンパニー ｐ３８キナーゼ阻害剤としてのピラゾール誘導体
AU7585598A (en) 1997-05-23 1998-12-11 Bayer Corporation Raf kinase inhibitors
WO1998052558A1 (en) 1997-05-23 1998-11-26 Bayer Corporation INHIBITION OF p38 KINASE ACTIVITY BY ARYL UREAS
BR9810151A (pt) 1997-06-19 2000-08-08 Du Pont Pharm Co Composto, composição farmacêutica e método para tratamento ou prevenção de uma desordem tromoboembólica
ZA985247B (en) 1997-06-19 1999-12-17 Du Pont Merck Pharma Guanidine mimics as factor Xa inhibitors.
EP0897908A1 (de) 1997-08-19 1999-02-24 Roche Diagnostics GmbH 3-Aryl-Succinamido-Hydroxamsäuren, Prozesse zu ihrer Herstellung und diese Substanzen enthaltende Medikamente
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
CN1327443A (zh) 1997-10-31 2001-12-19 艾文蒂斯药品有限公司 取代的酰苯胺化合物
BR9813197A (pt) 1997-11-05 2000-08-29 Novartis Ag Dipeptìdeo nitrilas
TR200002617T2 (tr) 1997-12-22 2000-11-21 Bayer Corporation Aril ve heteroaril sübstitüentli heterosiklik üreler kullanılarak RAF kinazın inhibe edilmesi
CA2315717C (en) 1997-12-22 2011-02-01 Bayer Corporation Inhibition of raf kinase using substituted heterocyclic ureas
SK16732000A3 (sk) 1998-05-05 2001-06-11 Warner-Lambert Company Sukcínamidové inhibítory konverzného enzýmu interleukínu-1beta
WO1999063115A2 (en) 1998-06-04 1999-12-09 Reprogen, Inc. Use of cathepsin s in the diagnosis and treatment of endometriosis
EP1159273A1 (en) 1999-03-02 2001-12-05 Boehringer Ingelheim Pharmaceuticals Inc. Compounds useful as reversible inhibitors of cathepsin s
US6455502B1 (en) 1999-03-15 2002-09-24 Axys Pharmaceuticals, Inc. Compounds and compositions as protease inhibitors
EP1136575A4 (en) * 1999-08-10 2008-04-23 Jfe Steel Corp PROCESS FOR PRODUCING COLD LAMINATED STEEL STRIPS
EP1218372B1 (en) 1999-09-13 2003-07-02 Boehringer Ingelheim Pharmaceuticals, Inc. Novel heterocyclic compounds useful as reversible inhibitors of cysteine proteases
US6420364B1 (en) * 1999-09-13 2002-07-16 Boehringer Ingelheim Pharmaceuticals, Inc. Compound useful as reversible inhibitors of cysteine proteases
EP2166121A1 (en) * 1999-09-16 2010-03-24 JFE Steel Corporation High strength steel sheet and method for manufacturing the same
WO2001023632A1 (fr) * 1999-09-28 2001-04-05 Nkk Corporation Tole d'acier laminee a chaud et possedant une resistance elevee a la traction, et procede de production associe
EP1149925B1 (en) * 1999-09-29 2010-12-01 JFE Steel Corporation Sheet steel and method for producing sheet steel
WO2001023624A1 (fr) * 1999-09-29 2001-04-05 Nkk Corporation Tole d'acier et son procede de fabrication
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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