HUP0303934A2 - Cisztein-proteázok reverzibilis inhibitoraiként alkalmazható spiroheterociklusos nitrilek és ezeket tartalmazó gyógyszerkészítmények - Google Patents

Cisztein-proteázok reverzibilis inhibitoraiként alkalmazható spiroheterociklusos nitrilek és ezeket tartalmazó gyógyszerkészítmények

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Publication number
HUP0303934A2
HUP0303934A2 HU0303934A HUP0303934A HUP0303934A2 HU P0303934 A2 HUP0303934 A2 HU P0303934A2 HU 0303934 A HU0303934 A HU 0303934A HU P0303934 A HUP0303934 A HU P0303934A HU P0303934 A2 HUP0303934 A2 HU P0303934A2
Authority
HU
Hungary
Prior art keywords
spiroheterocyclic
pharmaceutical compositions
compositions containing
cysteine proteases
reversible inhibitors
Prior art date
Application number
HU0303934A
Other languages
English (en)
Hungarian (hu)
Inventor
Younes Bekkali
Eugene R. Hickey
Weimin Liu
Usha R. Patel
Denice M. Spero
Sanxing Sun
David S. Thomson
Yancey D. Ward
Erick R. R. Young
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 HUP0303934A2 publication Critical patent/HUP0303934A2/hu

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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
    • 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
    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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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
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    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
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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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    • 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
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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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    • 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
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    • C07—ORGANIC CHEMISTRY
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    • 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
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    • 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
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    • C—CHEMISTRY; METALLURGY
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    • 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
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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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  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
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  • Hematology (AREA)
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HU0303934A 2000-09-08 2001-03-14 Cisztein-proteázok reverzibilis inhibitoraiként alkalmazható spiroheterociklusos nitrilek és ezeket tartalmazó gyógyszerkészítmények HUP0303934A2 (hu)

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
HUP0303934A2 true HUP0303934A2 (hu) 2004-04-28

Family

ID=24628539

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0303934A HUP0303934A2 (hu) 2000-09-08 2001-03-14 Cisztein-proteázok reverzibilis inhibitoraiként alkalmazható spiroheterociklusos nitrilek és ezeket tartalmazó gyógyszerkészítmények

Country Status (24)

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

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
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
WO2002051983A2 (en) 2000-12-22 2002-07-04 Axys Pharmaceuticals, Inc. Novel compounds and compositions as cathepsin inhibitors
US7030116B2 (en) 2000-12-22 2006-04-18 Aventis Pharmaceuticals Inc. Compounds and compositions as cathepsin inhibitors
JP4365094B2 (ja) * 2001-03-02 2009-11-18 メルク フロスト カナダ リミテツド カテプシンシステインプロテアーゼ阻害薬
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
JP2005504078A (ja) 2001-09-14 2005-02-10 アベンティス・ファーマスーティカルズ・インコーポレイテツド カテプシン阻害剤としての新規化合物および組成物
WO2003029200A2 (en) * 2001-10-02 2003-04-10 Boehringer Ingelheim Pharmaceuticals, Inc. Compounds useful as reversible inhibitors of cysteine proteases
US6841571B2 (en) * 2001-10-29 2005-01-11 Boehringer Ingelheim Pharmaceuticals, Inc. Compounds useful as reversible inhibitors of cysteine proteases
IL161950A0 (en) 2001-11-14 2005-11-20 Axys Pharm 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
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
KR20060079143A (ko) * 2003-09-18 2006-07-05 액시스 파마슈티컬스 인코포레이티드 시스테인 프로테아제 억제제로서의 할로알킬 함유 화합물
US7186827B2 (en) * 2003-10-30 2007-03-06 Boehringer Ingelheim Pharmaceuticals, Inc. Dipeptide synthesis
PE20050897A1 (es) * 2003-12-03 2005-11-06 Glaxo Group Ltd Nuevos antagonistas del receptor muscarinico m3 de acetilcolina
US20070141059A1 (en) * 2003-12-11 2007-06-21 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
JP5154944B2 (ja) * 2004-12-02 2013-02-27 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インヒビターとしてのスルホンアミド含有化合物
WO2006076797A1 (en) * 2005-01-19 2006-07-27 Merck Frosst Canada Ltd. Cathepsin k inhibitors and atherosclerosis
US7488848B2 (en) * 2005-03-21 2009-02-10 Virobay, Inc. Alpha ketoamide compounds as cysteine protease inhibitors
US7893093B2 (en) * 2005-03-22 2011-02-22 Virobay, Inc. 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
WO2007053662A1 (en) * 2005-11-01 2007-05-10 Janssen Pharmaceutica N.V. Dihydroisoindolones as allosteric modulators of glucokinase
WO2007053498A1 (en) * 2005-11-01 2007-05-10 Millennium Pharmaceuticals, Inc. Compounds useful as antagonists of ccr2
WO2007053499A2 (en) * 2005-11-01 2007-05-10 Millennium Pharmaceuticals, Inc. Compounds useful as antagonists of ccr2
RU2478620C2 (ru) * 2006-06-01 2013-04-10 Санофи-Авентис Спироциклические нитрилы в качестве ингибиторов протеазы
WO2007146253A2 (en) 2006-06-13 2007-12-21 Critser John K 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
ZA200902477B (en) * 2006-10-04 2010-08-25 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
CA2693473A1 (en) * 2007-07-17 2009-01-22 Amgen Inc. Thiadiazole modulators of pkb
CA2692713A1 (en) 2007-07-17 2009-01-22 Amgen Inc. Heterocyclic modulators of pkb
AU2008287435B2 (en) 2007-08-15 2013-05-16 Cytokinetics, Incorporated Certain chemical entities, compositions, and methods
DK2222636T3 (da) 2007-12-21 2013-06-03 Ligand Pharm Inc Selektive androgenreceptormodulatorer (SARMS) og anvendelser deraf
EP2719700A1 (en) 2008-01-09 2014-04-16 Amura Therapeutics Limited Tetrahydrofuro(3,2-b)pyrrol-3-one derivatives as inhibitors of cysteine proteinases
CN102405284B (zh) * 2008-09-05 2016-01-20 新基阿维罗米克斯研究公司 设计不可逆抑制剂的算法
CA2753205A1 (en) * 2009-02-19 2010-08-26 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
RU2012114902A (ru) * 2009-09-16 2013-10-27 Авила Терапьютикс, Инк. Конъюгаты и ингибиторы протеинкиназы
SG181965A1 (en) 2009-12-30 2012-08-30 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
WO2012169555A1 (ja) 2011-06-07 2012-12-13 株式会社クレハ オキセタン化合物の製造方法、アゾリルメチルシクロペンタノール化合物の製造方法、および中間体化合物
EP2537532A1 (en) 2011-06-22 2012-12-26 J. Stefan Institute Cathepsin-binding compounds bound to a nanodevice and their diagnostic and therapeutic use
CN106831541B (zh) 2011-11-18 2019-09-06 赫普泰雅治疗有限公司 毒蕈碱性m1受体激动剂
CA2898077C (en) * 2013-01-15 2021-10-19 Merck Patent Gmbh Acylguanidines for treating osteoarthritis
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
GB201519352D0 (en) 2015-11-02 2015-12-16 Heptares Therapeutics Ltd Pharmaceutical compounds
GB201617454D0 (en) 2016-10-14 2016-11-30 Heptares Therapeutics Limited Pharmaceutical compounds
US10259787B2 (en) 2016-10-14 2019-04-16 Heptares Therapeutics Limited Substituted cyclohexanes as muscarinic M1 receptor and/or M4 receptor agonists
GB201810239D0 (en) 2018-06-22 2018-08-08 Heptares Therapeutics Ltd Pharmaceutical compounds
GB201819960D0 (en) 2018-12-07 2019-01-23 Heptares Therapeutics Ltd Pharmaceutical compounds
GB201819961D0 (en) 2018-12-07 2019-01-23 Heptares Therapeutics Ltd Pharmaceutical compounds
EP3956309A4 (en) 2019-04-19 2023-06-07 Ligand Pharmaceuticals Inc. CRYSTALLINE FORMS AND METHODS FOR PRODUCING CRYSTALLINE FORMS OF A COMPOUND
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 (enExample) 1967-02-16 1968-05-09
FI840260L (fi) 1983-01-27 1984-07-28 Ciba Geigy Ag Pyrrolidinonderivat och foerfarande foer deras framstaellning.
US4767202A (en) * 1984-01-20 1988-08-30 Minolta Camera Kabushiki Kaisha Objective lens system for optical recording type disks
WO1985005031A1 (en) * 1984-05-09 1985-11-21 The Australian National University A method for the modulation of the immune response
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
JPH03500880A (ja) 1987-10-26 1991-02-28 ワーナー‐ランバート・コンパニー レニン阻害剤、その製造方法、その使用のための方法およびそれを含有する組成物
US4962117A (en) 1987-11-25 1990-10-09 Merck Frosst Canada, Inc. Heterazole dialkanoic acids
CA1322005C (en) 1987-11-25 1993-09-07 Robert N. Young Benzoheterazoles
CA1322004C (en) 1987-11-25 1993-09-07 Merck Frosst Canada Incorporated Pyridyl styrene dialkanoic acids
US5346907A (en) 1988-04-05 1994-09-13 Abbott Laboratories Amino acid analog CCK antagonists
EP0442878A4 (en) 1988-04-05 1991-10-23 Abbott Laboratories Derivatives of tryptophan as cck antagonists
AU3570089A (en) 1988-05-03 1989-11-29 Upjohn Company, The 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
AU2251892A (en) 1991-06-14 1993-01-12 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
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
EP0957092A1 (de) 1992-06-22 1999-11-17 Boehringer Ingelheim Pharma 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
CA2159069A1 (en) 1993-03-29 1994-10-13 William Frank Degrado A process and intermediate compounds useful for the preparation of platelet glycoprotein iib/iiia inhibitors containing n -a- 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
US5574064A (en) 1993-04-28 1996-11-12 Kumiai Chemical Industry Co., Ltd. Amino-acid amide derivatives, agricultural or horticultural fungicides, and method for producing the same
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
CN1078886C (zh) 1993-10-01 2002-02-06 默里尔药物公司 抑制β－淀粉样蛋白产生的抑制剂
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
EP0728145A1 (en) 1993-11-01 1996-08-28 Ciba-Geigy Japan Limited Endothelin receptor antagonists
US5714484A (en) 1993-12-08 1998-02-03 Prototek, Inc. α-(1,3-dicarbonylenol ether) methyl ketones as cysteine protease inhibitors
US5486623A (en) 1993-12-08 1996-01-23 Prototek, Inc. Cysteine protease inhibitors containing heterocyclic leaving groups
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
WO1995024382A1 (en) 1994-03-10 1995-09-14 G.D. Searle & Co. L-n6-(1-iminoethyl)lysine derivatives useful as nitric oxide synthase inhibitors
ATE157965T1 (de) 1994-03-19 1997-09-15 Basf Ag Fungizide carbamoyloximcarbonsäureamide
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
US5716929A (en) 1994-06-17 1998-02-10 Vertex Pharmaceuticals, Inc. Inhibitors of interleukin-1β converting enzyme
US5847135A (en) 1994-06-17 1998-12-08 Vertex Pharmaceuticals, Incorporated 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
WO1996013502A1 (en) 1994-10-26 1996-05-09 Pharmacia & Upjohn Company Phenyloxazolidinone antimicrobials
CA2163325A1 (en) 1994-11-21 1996-05-22 Kaneyoshi Kato Amine compounds, their production and use
ATE233240T1 (de) 1994-12-02 2003-03-15 Yamanouchi Pharma Co Ltd Neues amidinonaphthylderivat oder dessen salz
US5804560A (en) 1995-01-06 1998-09-08 Sibia Neurosciences, Inc. Peptide and peptide analog protease inhibitors
US5863902A (en) 1995-01-06 1999-01-26 Sibia Neurosciences, Inc. Methods of treating neurodegenerative disorders using 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
CZ298197A3 (cs) 1995-03-24 1998-03-18 Arris Pharmaceutical Corporation Reverzibilní inhibitory proteas
US5776718A (en) 1995-03-24 1998-07-07 Arris Pharmaceutical Corporation Reversible protease inhibitors
MY114302A (en) 1995-04-19 2002-09-30 Ihara Chemical Ind Co Benzylsulfide derivative, process for its production and pesticide
GB9508195D0 (en) 1995-04-20 1995-06-07 Univ British Columbia Novel biologically active compounds and compositions,their use and derivation
AU5687396A (en) 1995-04-21 1996-11-07 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
US5756528A (en) 1995-06-06 1998-05-26 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
FI974436A7 (fi) 1995-06-06 1998-01-27 Pfizer Substituoituja N-(indoli-2-karbonyyli)-glysiiniamideja ja -johdannaisi a glykogeenifosforylaasi-inhibiittoreina
US5827860A (en) 1995-06-07 1998-10-27 Ortho Pharmaceutical Corporation Peptidyl heterocycles useful in the treatment of thrombin related disorders
WO1996040753A1 (en) 1995-06-07 1996-12-19 G.D. Searle & Co. Pipecolic acid derivatives of proline threonine amides useful for the treatment of rheumatoid arthritis
US6069130A (en) 1995-06-07 2000-05-30 Cor Therapeutics, Inc. Ketoheterocyclic inhibitors of factor Xa
TW438591B (en) 1995-06-07 2001-06-07 Arris Pharm Corp Reversible cysteine protease inhibitors
US5827866A (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
WO1997019908A1 (en) 1995-11-29 1997-06-05 Nihon Nohyaku Co., Ltd. Phenylalanine derivatives, optically active substances, salts or coordination compounds thereof, and their use as fungicides
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
DE69624728T2 (de) 1995-12-29 2003-07-10 Boehringer Ingelheim (Canada) Ltd., Laval Phenyl thiazol derivate mit antiherpesvirus eigenschaften
WO1997026246A1 (en) 1996-01-16 1997-07-24 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
WO1997031016A2 (en) 1996-02-23 1997-08-28 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
EP0906271B1 (de) 1996-05-31 2002-02-06 Basf Aktiengesellschaft 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
JP4205168B2 (ja) 1996-10-02 2009-01-07 ノバルティス アクチエンゲゼルシヤフト ピリミジン誘導体およびその製造法
JP4080541B2 (ja) 1996-10-18 2008-04-23 バーテックス ファーマシューティカルズ インコーポレイテッド セリンプロテアーゼ、特にｃ型肝炎ウイルスｎｓ３プロテアーゼの阻害因子
EP0844248B1 (de) 1996-10-28 2002-07-10 Rolic AG Vernetzbare, photoaktive Silanderivate
JP2001503762A (ja) 1996-11-12 2001-03-21 ノバルティス アクチェンゲゼルシャフト 除草剤として有用なピラゾール誘導体
CN1238760A (zh) 1996-11-22 1999-12-15 伊兰药品公司 N－(芳基/杂芳基/烷基乙酰基)氨基酸酰胺类，含有这类化合物的药物组合物，及用这类化合物抑制β－淀粉样肽释放和或合成的方法
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
EP0946093B1 (en) 1996-12-19 2002-08-28 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
HUP0000735A3 (en) 1996-12-23 2002-03-28 Bristol Myers Squibb Pharma Co Nitrogen containing heteroaromatics as factor xa inhibitors
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
AU7726898A (en) 1997-05-22 1998-12-11 G.D. Searle & Co. Pyrazole derivatives as p38 kinase inhibitors
EP1019040B1 (en) 1997-05-23 2004-09-29 Bayer Corporation Aryl ureas for the treatment of inflammatory or immunomodulatory diseases
ATE399007T1 (de) 1997-05-23 2008-07-15 Bayer Pharmaceuticals Corp Raf kinase hemmer
HRP980334A2 (en) 1997-06-19 1999-04-30 Mimi Lifen Quan INHIBITORS OF FACTOR Xa WITH A NEUTRAL P1 SPECIFICITY GROUP
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
HUP0100699A3 (en) 1997-10-31 2002-11-28 Aventis Pharma Ltd West Mallin Substituted anilides and pharmaceuticals comprising them
CN1273444C (zh) 1997-11-05 2006-09-06 诺瓦提斯公司 二肽腈
PL205321B1 (pl) 1997-12-22 2010-04-30 Bayer Corp Zastosowanie podstawionych heterocyklicznych moczników do wytwarzania leku do hamowania kinazy raf, podstawione heterocykliczne moczniki oraz kompozycja farmaceutyczna je zawierająca
DK1056725T3 (da) 1997-12-22 2006-10-02 Bayer Pharmaceuticals Corp Inhibering af raf-kinase ved hjælp af aryl- og heteroaryl-substituerede heterocykliske urinstoffer
WO1999056765A1 (en) 1998-05-05 1999-11-11 Warner-Lambert Company SUCCINAMIDE INHIBITORS OF INTERLEUKIN-1β CONVERTING ENZYME
US6387629B1 (en) 1998-06-04 2002-05-14 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
KR100688740B1 (ko) 1999-03-15 2007-02-28 액시스 파마슈티컬스 인코포레이티드 프로테아제 억제제로서의 ｎ-시아노메틸 아미드
KR100430981B1 (ko) * 1999-08-10 2004-05-14 제이에프이 엔지니어링 가부시키가이샤 디프 드로잉성이 우수한 냉연강판의 제조방법
US6420364B1 (en) * 1999-09-13 2002-07-16 Boehringer Ingelheim Pharmaceuticals, Inc. Compound useful as reversible inhibitors of cysteine proteases
AU782246B2 (en) * 1999-09-13 2005-07-14 Boehringer Ingelheim Pharmaceuticals, Inc. Novel spiroheterocyclic compounds useful as reversible inhibitors of cysteine proteases
EP1143022B1 (en) * 1999-09-16 2010-04-14 JFE Steel Corporation Method for producing a thin steel plate having high strength
WO2001023625A1 (en) * 1999-09-29 2001-04-05 Nkk Corporation Sheet steel and method for producing sheet steel
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
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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