JP2005517640A - 置換2−アミノ−シクロアルカンカルボキサアミドならびにシステインプロテアーゼインヒビターとしてのその使用 - Google Patents

置換2−アミノ−シクロアルカンカルボキサアミドならびにシステインプロテアーゼインヒビターとしてのその使用 Download PDF

Info

Publication number
JP2005517640A
JP2005517640A JP2003549315A JP2003549315A JP2005517640A JP 2005517640 A JP2005517640 A JP 2005517640A JP 2003549315 A JP2003549315 A JP 2003549315A JP 2003549315 A JP2003549315 A JP 2003549315A JP 2005517640 A JP2005517640 A JP 2005517640A
Authority
JP
Japan
Prior art keywords
methyl
amino
lower alkyl
cyclohexyl
carbonyl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
JP2003549315A
Other languages
English (en)
Japanese (ja)
Other versions
JP2005517640A5 (enExample
Inventor
ガブリエル,トーマス
クラウス,ナンシー・エリザベス
ミアザデガン,タラネイ
パーマー,ワイリー・ソラング
スミス,デービッド・バーナード
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
F Hoffmann La Roche AG
Original Assignee
F Hoffmann La Roche AG
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 F Hoffmann La Roche AG filed Critical F Hoffmann La Roche AG
Publication of JP2005517640A publication Critical patent/JP2005517640A/ja
Publication of JP2005517640A5 publication Critical patent/JP2005517640A5/ja
Pending legal-status Critical Current

Links

Classifications

    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06—Antimalarials
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/06—Antiarrhythmics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/42—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
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/38—Nitrogen atoms
    • C07D215/40—Nitrogen atoms attached in position 8
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D215/54—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/58—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems with hetero atoms directly attached to the ring nitrogen atom
    • C07D215/60—N-oxides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/02—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/38—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/36—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
    • C07D241/38—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
    • C07D241/40—Benzopyrazines
    • C07D241/44—Benzopyrazines 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 carbon atoms of the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
    • 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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Cardiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Immunology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Molecular Biology (AREA)
  • Communicable Diseases (AREA)
  • AIDS & HIV (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Ophthalmology & Optometry (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Indole Compounds (AREA)
  • Quinoline Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
JP2003549315A 2001-12-04 2002-11-25 置換2−アミノ−シクロアルカンカルボキサアミドならびにシステインプロテアーゼインヒビターとしてのその使用 Pending JP2005517640A (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US33675001P 2001-12-04 2001-12-04
PCT/EP2002/013221 WO2003048123A1 (en) 2001-12-04 2002-11-25 Substituted 2-amino-cycloalkanecarboxamides and their use as cysteine protease inhibitors

Publications (2)

Publication Number Publication Date
JP2005517640A true JP2005517640A (ja) 2005-06-16
JP2005517640A5 JP2005517640A5 (enExample) 2005-12-22

Family

ID=23317485

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2003549315A Pending JP2005517640A (ja) 2001-12-04 2002-11-25 置換2−アミノ−シクロアルカンカルボキサアミドならびにシステインプロテアーゼインヒビターとしてのその使用

Country Status (25)

Country Link
US (1) US6747053B2 (enExample)
EP (1) EP1453801B1 (enExample)
JP (1) JP2005517640A (enExample)
KR (1) KR20050044660A (enExample)
CN (1) CN1315806C (enExample)
AR (1) AR037683A1 (enExample)
AT (1) ATE357432T1 (enExample)
AU (1) AU2002352126A1 (enExample)
BR (1) BR0214642A (enExample)
CA (1) CA2467435A1 (enExample)
DE (1) DE60219068T2 (enExample)
ES (1) ES2282497T3 (enExample)
GT (1) GT200200253A (enExample)
HU (1) HUP0402344A2 (enExample)
IL (1) IL161992A0 (enExample)
MX (1) MXPA04005263A (enExample)
NO (1) NO20042719L (enExample)
PA (1) PA8559701A1 (enExample)
PE (1) PE20030723A1 (enExample)
PL (1) PL370766A1 (enExample)
RU (1) RU2004120784A (enExample)
TW (1) TW200303861A (enExample)
UY (1) UY27561A1 (enExample)
WO (1) WO2003048123A1 (enExample)
ZA (1) ZA200404343B (enExample)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007080882A1 (ja) * 2006-01-11 2007-07-19 Seikagaku Corporation オキサゾロン誘導体
JP2010531344A (ja) * 2007-06-26 2010-09-24 アストラゼネカ アクチボラグ カテプシンk阻害剤としての1−シアノシクロプロピル誘導体
JP2017031199A (ja) * 2011-07-26 2017-02-09 サノフイ 3−ヘテロアロイルアミノ−プロピオン酸誘導体及び医薬としてのそれらの使用

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1147214B1 (en) * 1999-01-13 2011-01-05 The Research Foundation Of State University Of New York A novel method for designing protein kinase inhibitors
US7005445B2 (en) * 2001-10-22 2006-02-28 The Research Foundation Of State University Of New York Protein kinase and phosphatase inhibitors and methods for designing them
GB0128996D0 (en) 2001-12-04 2002-01-23 Novartis Ag Organic compounds
DE60305446T4 (de) * 2002-01-07 2009-07-09 Eisai R&D Management Co., Ltd. Desazapurine und deren verwendung
SE0203712D0 (sv) 2002-12-13 2002-12-13 Astrazeneca Ab Novel compounds
GB0403038D0 (en) 2004-02-11 2004-03-17 Novartis Ag Organic compounds
US20090226552A1 (en) * 2004-07-22 2009-09-10 Colorado State University Research Foundation Agents and methods for diagnosing osteoarthritis
AU2006261954A1 (en) * 2005-06-28 2007-01-04 Merck & Co., Inc. Non-nucleoside reverse transcriptase inhibitors
EP1749822B1 (en) * 2005-08-05 2008-10-15 Hybrigenics S.A. Novel cysteine protease inhibitors and their therapeutic applications
RU2424234C2 (ru) * 2005-08-05 2011-07-20 Ибриженикс Са Новые ингибиторы цистеиновых протеаз и их терапевтическое применение
WO2007041775A1 (en) * 2005-10-10 2007-04-19 The University Of Queensland Cysteine protease inhibitors incorporating azide groups
WO2007081530A2 (en) * 2006-01-03 2007-07-19 Med Institute, Inc. Endoluminal medical device for local delivery of cathepsin inhibitors
US7838542B2 (en) * 2006-06-29 2010-11-23 Kinex Pharmaceuticals, Llc Bicyclic compositions and methods for modulating a kinase cascade
CN101591327B (zh) * 2008-05-26 2012-07-25 华东理工大学 苯烷酰胺类化合物及其用途
BR112015004666B1 (pt) 2012-09-07 2022-04-26 Novartis Ag Derivados de indol carboxamida, seu uso, e composição farmacêutica
NO2699580T3 (enExample) 2014-01-24 2018-02-24
CA2939491A1 (en) * 2014-02-14 2015-08-20 Toa Eiyo Ltd. Cyclic hydrocarbon compound
KR20200035035A (ko) 2017-07-31 2020-04-01 노파르티스 아게 코카인 사용 감소 또는 코카인 사용 재발 예방에 있어서 마보글루란트의 용도
PT3758708T (pt) 2018-03-01 2025-02-13 Astrazeneca Ab Composições farmacêuticas compreendendo (2s)-{(1,s)-1-ciano-2-[4-(3-metil-2-oxo-2,3-di-hidro-1,3-benzoxazol-5-il)fenil]etil}-1,4-oxazepano-2-carboxamida
CA3106269A1 (en) 2018-07-17 2020-01-23 Insmed Incorporated Certain (2s)-n-[(1s)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides for treating lupus nephritis
PL4129989T3 (pl) 2020-08-26 2025-02-24 Haisco Pharmaceuticals Pte. Ltd. Pochodna nitrilu działająca jako inhibitor dipeptydylopeptydazy 1 i jej zastosowanie
KR20230117738A (ko) 2020-12-04 2023-08-09 레이스톤 바이오파마 컴퍼니 리미티드 카텝신 c의 소분자 억제제 및 이의 의약적 용도
US20250361226A1 (en) 2022-06-07 2025-11-27 Reistone Biopharma Company Limited Pharmaceutically acceptable salt of benzo[c]chroman compound and polymorphic form and use of pharmaceutically acceptable salt
TW202404960A (zh) 2022-06-07 2024-02-01 大陸商瑞石生物醫藥有限公司 苯并[c]色滿化合物的多晶型及其製備方法和用途
JP2026503035A (ja) 2023-01-06 2026-01-27 インスメッド インコーポレイテッド 新規な可逆性dpp1阻害剤及びその用途
WO2025162472A1 (en) 2024-01-31 2025-08-07 Insmed Incorporated Linear dipeptidyl peptidase 1 inhibitors and uses thereof

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HU177576B (en) 1975-06-02 1981-11-28 Chinoin Gyogyszer Es Vegyeszet Process for preparing 2-amino-cyclohexane carboxylic acid,its amides and similar compounds
DE4417163A1 (de) 1994-05-17 1995-11-23 Hoechst Schering Agrevo Gmbh Heterocyclylamino- und Heterocyclyloxy-cycloalkyl-Derivate, ihre Herstellung und ihre Verwendung als Schädlingsbekämpfungsmittel und Fungizide
IT1283467B1 (it) 1996-07-19 1998-04-21 Menarini Farma Ind Derivati di cicloalcani 1,2 sostituiti come inibitori della trombina, procedimento per la loro preparazione e loro impiego in formulazioni
HUP0004400A3 (en) 1997-11-05 2002-10-28 Novartis Ag Dipeptide nitriles, process for their preparation, pharmaceutical compositions comprising thereof and their use
ATE339404T1 (de) * 1999-12-24 2006-10-15 Hoffmann La Roche Nitrilderivate als cathepsin k hemmer
DE60132975T2 (de) 2000-01-06 2009-02-26 Merck Frosst Canada Inc., Kirkland Neue substanzen und verbindungen als protease-inhibitoren
US6462076B2 (en) * 2000-06-14 2002-10-08 Hoffmann-La Roche Inc. Beta-amino acid nitrile derivatives as cathepsin K inhibitors
DE60225316T2 (de) 2001-11-13 2009-02-26 AXYS Pharmaceuticals, Inc., South San Francisco Cyanoalkylamino-derivate als protease-hemmer

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007080882A1 (ja) * 2006-01-11 2007-07-19 Seikagaku Corporation オキサゾロン誘導体
US8785631B2 (en) 2006-01-11 2014-07-22 Seikagaku Corporation Oxazolone derivative compounds having a 3-oxa-1-azaspiro[4.5] core
JP2010531344A (ja) * 2007-06-26 2010-09-24 アストラゼネカ アクチボラグ カテプシンk阻害剤としての1−シアノシクロプロピル誘導体
JP2017031199A (ja) * 2011-07-26 2017-02-09 サノフイ 3−ヘテロアロイルアミノ−プロピオン酸誘導体及び医薬としてのそれらの使用

Also Published As

Publication number Publication date
CA2467435A1 (en) 2003-06-12
PA8559701A1 (es) 2003-07-28
ZA200404343B (en) 2006-07-26
PE20030723A1 (es) 2003-08-29
KR20050044660A (ko) 2005-05-12
US20030212097A1 (en) 2003-11-13
NO20042719L (no) 2004-06-28
DE60219068T2 (de) 2007-12-13
IL161992A0 (en) 2005-11-20
RU2004120784A (ru) 2005-08-10
EP1453801A1 (en) 2004-09-08
GT200200253A (es) 2003-07-03
BR0214642A (pt) 2004-11-03
ES2282497T3 (es) 2007-10-16
PL370766A1 (en) 2005-05-30
EP1453801B1 (en) 2007-03-21
US6747053B2 (en) 2004-06-08
WO2003048123A1 (en) 2003-06-12
ATE357432T1 (de) 2007-04-15
CN1639119A (zh) 2005-07-13
AU2002352126A1 (en) 2003-06-17
CN1315806C (zh) 2007-05-16
DE60219068D1 (de) 2007-05-03
TW200303861A (en) 2003-09-16
MXPA04005263A (es) 2004-10-11
UY27561A1 (es) 2003-06-30
HUP0402344A2 (hu) 2005-02-28
AR037683A1 (es) 2004-12-01

Similar Documents

Publication Publication Date Title
CN1315806C (zh) 取代的2-氨基-环烷烃甲酰胺和它们作为半胱氨酸蛋白酶抑制剂的用途
US9079880B2 (en) Rho kinase inhibitors
CA2264556C (en) Substituted n-[(aminoiminomethyl or aminomethyl)phenyl]propyl amides
US20080176870A1 (en) Heterobicyclic metalloprotease inhibitors
EP2518067B1 (fr) Dérives de n-[(1h-pyrazol-1-yl)aryl]-1h-indole ou 1h- indazole-3-carboxamide et leurs applications en thérapeutique comme antagonistes de p2y12.
JP2004002368A (ja) 医薬組成物
JP2011511018A (ja) Par1阻害剤としてのsf5誘導体、その製造、及び薬剤としての使用
JP2010150275A (ja) ピラジノントロンビン阻害剤
US20090012087A1 (en) New Aza-Bicyclohexane Compounds Useful As Inhibitors Of Thrombin
US8097758B2 (en) Isoserine derivatives for use as coagulation factor IXa inhibitors
EP2733144B1 (en) Novel compound having parp inhibitory activity
JP2008524210A (ja) メタロプロテイナーゼ阻害剤としての新規ヒダントイン誘導体
CA2712701A1 (en) Cyclic azaindole-3-carboxamides, their preparation and their use as pharmaceuticals
US6759428B2 (en) Indole nitriles
JP5570434B2 (ja) Par1阻害剤としてのイミダゾピリダジン類、その製造、及び薬剤としての使用
CN115353508A (zh) 5-吡啶-1h-吲唑类化合物、药物组合物和应用
WO2003048155A1 (en) Thrombin inhibitors
CN107459491A (zh) 含1,2,3‑三氮唑结构的苯甲酰胺类化合物及其用途
CN102344402A (zh) 苯并氮杂环羟乙基胺类化合物、其制备方法和用途

Legal Events

Date Code Title Description
A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20080430

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20081021