EA200300018A1 - PROTEAS INHIBITORS - Google Patents

PROTEAS INHIBITORS

Info

Publication number
EA200300018A1
EA200300018A1 EA200300018A EA200300018A EA200300018A1 EA 200300018 A1 EA200300018 A1 EA 200300018A1 EA 200300018 A EA200300018 A EA 200300018A EA 200300018 A EA200300018 A EA 200300018A EA 200300018 A1 EA200300018 A1 EA 200300018A1
Authority
EA
Eurasian Patent Office
Prior art keywords
compounds
cartilage
matrix
disease
bone loss
Prior art date
Application number
EA200300018A
Other languages
Russian (ru)
Inventor
Роберт В. мл. Маркьюс
Ю. Ру
Дэниел Ф. Вебер
Максвелл Д. Каммингз
Скотт К. Томпсон
Деннис Ямасита
Original Assignee
Смитклайн Бичам Корпорейшн
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 Смитклайн Бичам Корпорейшн filed Critical Смитклайн Бичам Корпорейшн
Publication of EA200300018A1 publication Critical patent/EA200300018A1/en

Links

Classifications

    • 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
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • 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
    • A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • 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
    • 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
    • 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
    • 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
    • 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
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/08—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis for Pneumocystis carinii
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/10—Anthelmintics
    • A61P33/12—Schistosomicides
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/02—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D223/06—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings 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
    • C07D223/12—Nitrogen atoms not forming part of a nitro radical
    • 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
    • C07D405/14—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 three or more hetero rings
    • 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

Abstract

Данное изобретение относится к 4-аминоазепан-3-онсодержащим ингибиторам протеаз и их фармацевтически приемлемым солям, гидратам и сольватам, которые ингибируют протеазы, в том числе катепсин К, фармацевтическим композициям таких соединений, новым промежуточным соединениям для получения таких соединений и способам лечения заболеваний излишней потери костной ткани или деградации хряща или матрикса, в том числе остеопороза; заболевания десен, в том числе гингивита и периодонтита; артрита, более конкретно остеоартрита и ревматоидного артрита; болезни Педжета; гиперкальциемии злокачественности и метаболического заболевания кости, предусматривающим ингибирование указанной рарефикации кости или избыточной деградации хряща или матрикса введением пациенту, нуждающемуся в этом, соединения данного изобретения.Международная заявка была опубликована вместе с отчетом о международном поиске.This invention relates to 4-aminoazepan-3-oncontaining protease inhibitors and their pharmaceutically acceptable salts, hydrates and solvates that inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, new intermediate compounds for the preparation of such compounds and methods for treating diseases of the excess bone loss or degradation of cartilage or matrix, including osteoporosis; gum diseases, including gingivitis and periodontitis; arthritis, more specifically osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy and metabolic bone disease, which involves inhibiting the indicated bone loss or excessive degradation of cartilage or matrix by administering to a patient in need this a compound of this invention. The international application was published together with an international search report.

EA200300018A 2000-06-14 2001-06-14 PROTEAS INHIBITORS EA200300018A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US59384500A 2000-06-14 2000-06-14
PCT/US2001/019062 WO2001095911A1 (en) 2000-06-14 2001-06-14 Protease inhibitors

Publications (1)

Publication Number Publication Date
EA200300018A1 true EA200300018A1 (en) 2003-06-26

Family

ID=24376433

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200300018A EA200300018A1 (en) 2000-06-14 2001-06-14 PROTEAS INHIBITORS

Country Status (25)

Country Link
EP (1) EP1307204A4 (en)
JP (1) JP2004503502A (en)
KR (1) KR20030008220A (en)
CN (1) CN1444481A (en)
AP (1) AP2002002671A0 (en)
AR (1) AR032622A1 (en)
AU (1) AU2001268407A1 (en)
BG (1) BG107327A (en)
BR (1) BR0111693A (en)
CA (1) CA2412353A1 (en)
CZ (1) CZ20024086A3 (en)
EA (1) EA200300018A1 (en)
EC (1) ECSP024388A (en)
HU (1) HUP0301231A2 (en)
IL (1) IL153421A0 (en)
MA (1) MA25758A1 (en)
MX (1) MXPA02012442A (en)
NO (1) NO20025786L (en)
NZ (1) NZ522965A (en)
OA (1) OA12288A (en)
PE (1) PE20011374A1 (en)
PL (1) PL360508A1 (en)
SK (1) SK17592002A3 (en)
WO (1) WO2001095911A1 (en)
ZA (1) ZA200209808B (en)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001034159A1 (en) * 1999-11-10 2001-05-17 Smithkline Beecham Corporation Protease inhibitors
JP2003513926A (en) * 1999-11-10 2003-04-15 スミスクライン・ビーチャム・コーポレイション Protease inhibitor
EP1392657A4 (en) * 2000-11-22 2004-03-10 Smithkline Beecham Corp Protease inhibitors
MXPA03007441A (en) 2001-02-20 2004-10-15 Chugai Pharmaceutical Co Ltd Azoles as malonyl-coa decarboxylase inhibitors useful as metabolic modulators.
US7709510B2 (en) 2001-02-20 2010-05-04 Chugai Seiyaku Kabushiki Kaisha Azoles as malonyl-CoA decarboxylase inhibitors useful as metabolic modulators
JP2004527575A (en) * 2001-05-17 2004-09-09 スミスクライン・ビーチャム・コーポレイション Protease inhibitor
DE602004014937D1 (en) 2003-08-01 2008-08-21 Chugai Pharmaceutical Co Ltd PIPERIDINE COMPOUNDS AS MALONYL-COA DECARBOXYLASE HEMMER
EP1653944B1 (en) 2003-08-01 2010-11-10 Chugai Seiyaku Kabushiki Kaisha Heterocyclic compounds useful as malonyl-coa decarboxylase inhibitors
JP4773960B2 (en) 2003-08-01 2011-09-14 中外製薬株式会社 Cyanoguanidine-type azole compounds useful as malonyl-CoA decarboxylase inhibitors
JP5587790B2 (en) 2008-01-09 2014-09-10 アミュラ セラピューティクス リミティド Compound
CN103275070A (en) * 2013-05-10 2013-09-04 郑彪 Tetracyclic compound for adjusting proliferation of mononuclear cells and application of tetracyclic compound
US9427441B2 (en) 2014-02-19 2016-08-30 Indiana University Research And Technology Corporation Targeting primary cilia to treat glaucoma

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DZ2285A1 (en) * 1996-08-08 2002-12-25 Smithkline Beecham Corp Cysteine protease inhibitors.
HUP0104768A3 (en) * 1998-12-23 2002-05-28 Smithkline Beecham Corp 4-amino-3-oxo-azepanes as protease inhibitors and pharmaceutical compositions containing the same
WO2001034565A2 (en) * 1999-11-10 2001-05-17 Smithkline Beecham Corporation Protease inhibitors
JP2003513926A (en) * 1999-11-10 2003-04-15 スミスクライン・ビーチャム・コーポレイション Protease inhibitor
EP1320370A4 (en) * 2000-09-01 2008-10-22 Smithkline Beecham Corp Method of treatment
EP1392657A4 (en) * 2000-11-22 2004-03-10 Smithkline Beecham Corp Protease inhibitors
JP2004527575A (en) * 2001-05-17 2004-09-09 スミスクライン・ビーチャム・コーポレイション Protease inhibitor

Also Published As

Publication number Publication date
PL360508A1 (en) 2004-09-06
MA25758A1 (en) 2003-04-01
WO2001095911A1 (en) 2001-12-20
MXPA02012442A (en) 2003-04-25
PE20011374A1 (en) 2002-04-07
ZA200209808B (en) 2004-07-09
SK17592002A3 (en) 2003-05-02
BR0111693A (en) 2004-04-06
AR032622A1 (en) 2003-11-19
KR20030008220A (en) 2003-01-24
CA2412353A1 (en) 2001-12-20
EP1307204A4 (en) 2004-06-02
NO20025786D0 (en) 2002-12-02
AP2002002671A0 (en) 2002-12-31
CZ20024086A3 (en) 2003-05-14
IL153421A0 (en) 2003-07-06
NO20025786L (en) 2003-02-12
EP1307204A1 (en) 2003-05-07
ECSP024388A (en) 2003-02-06
HUP0301231A2 (en) 2003-08-28
CN1444481A (en) 2003-09-24
JP2004503502A (en) 2004-02-05
BG107327A (en) 2003-07-31
OA12288A (en) 2003-12-12
AU2001268407A1 (en) 2001-12-24
NZ522965A (en) 2004-06-25

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