EA200000682A1 - Новые ацилгуанидиновые производные в качестве ингибиторов резорбции костной ткани и антагонистов витронектиновых рецепторов - Google Patents

Новые ацилгуанидиновые производные в качестве ингибиторов резорбции костной ткани и антагонистов витронектиновых рецепторов

Info

Publication number
EA200000682A1
EA200000682A1 EA200000682A EA200000682A EA200000682A1 EA 200000682 A1 EA200000682 A1 EA 200000682A1 EA 200000682 A EA200000682 A EA 200000682A EA 200000682 A EA200000682 A EA 200000682A EA 200000682 A1 EA200000682 A1 EA 200000682A1
Authority
EA
Eurasian Patent Office
Prior art keywords
compounds
inhibitors
bone tissue
formula
new
Prior art date
Application number
EA200000682A
Other languages
English (en)
Other versions
EA002921B1 (ru
Inventor
Ануширван Пейман
Йохен Кнолле
Герхард Брайполь
Карл-Хайнц Шойнеманн
Дени Карниато
Жан-Франсуа Гурве
Томас Гейдек
Роберт Макдауэлл
Сара Кэтрин Бодари
Роберт Эндрю Катбертсон
Наполиэйн Феррара
Original Assignee
Авентис Фарма Дойчланд Гмбх
Генентек, Инк.
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 Авентис Фарма Дойчланд Гмбх, Генентек, Инк. filed Critical Авентис Фарма Дойчланд Гмбх
Publication of EA200000682A1 publication Critical patent/EA200000682A1/ru
Publication of EA002921B1 publication Critical patent/EA002921B1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C279/00—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
    • C07C279/20—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups containing any of the groups, X being a hetero atom, Y being any atom, e.g. acylguanidines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/13—Amines
    • A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4168—1,3-Diazoles having a nitrogen attached in position 2, e.g. clonidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • 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
    • A61P19/08—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
    • A61P35/00—Antineoplastic agents
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/28—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D233/44—Nitrogen atoms not forming part of a nitro radical
    • C07D233/48—Nitrogen atoms not forming part of a nitro radical with acyclic hydrocarbon or substituted acyclic hydrocarbon radicals, attached to said nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/06—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D239/08—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms directly attached in position 2
    • C07D239/12—Nitrogen atoms not forming part of a nitro radical
    • C07D239/16—Nitrogen atoms not forming part of a nitro radical acylated on said nitrogen atoms

Abstract

(57) Настоящее изобретение относится к ацилгуанидиновым производным формулы I, где R, R, R, R, R, A, m и n имеют значения, указанные в формуле изобретения, их физиологически переносимым солям и их пролекарствам. Соединения формулы I являются ценными фармацевтически активными соединениями. Данные соединения являются антагонистами витронектиновых рецепторов и ингибиторами резорбции костной ткани остеокластами и применимы, например, для терапии и профилактики заболеваний, вызванных, по крайней мере частично, нежелательной активностью резорбции костной ткани, например остеопороза. Настоящее изобретение также относится к способам получения соединений формулы I, их применению, в частности, в качестве фармацевтически активных ингредиентов и фармацевтическим препаратам, содержащим данные соединения.Международная заявка была опубликована вместе с отчетом о международном поиске.
EA200000682A 1997-12-19 1998-12-10 Новые ацилгуанидиновые производные в качестве ингибиторов резорбции костной ткани и антагонистов витронектиновых рецепторов EA002921B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP97122520A EP0933367A1 (en) 1997-12-19 1997-12-19 Novel acylguanidine derivates as inhibitors of bone resorption and as vitronectin receptor antagonists
PCT/EP1998/008051 WO1999032457A1 (en) 1997-12-19 1998-12-10 Novel acylguanidine derivatives as inhibitors of bone resorption and as vitronectin receptor antagonists

Publications (2)

Publication Number Publication Date
EA200000682A1 true EA200000682A1 (ru) 2000-12-25
EA002921B1 EA002921B1 (ru) 2002-10-31

Family

ID=8227841

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200000682A EA002921B1 (ru) 1997-12-19 1998-12-10 Новые ацилгуанидиновые производные в качестве ингибиторов резорбции костной ткани и антагонистов витронектиновых рецепторов

Country Status (34)

Country Link
US (1) US6492356B1 (ru)
EP (2) EP0933367A1 (ru)
JP (1) JP2001526271A (ru)
KR (1) KR20010033281A (ru)
CN (1) CN1205191C (ru)
AP (1) AP2000001842A0 (ru)
AR (1) AR016437A1 (ru)
AT (1) ATE228112T1 (ru)
AU (1) AU753109B2 (ru)
BG (1) BG64754B1 (ru)
BR (1) BR9814308A (ru)
CA (1) CA2312712A1 (ru)
CU (1) CU23032A3 (ru)
DE (1) DE69809594T2 (ru)
DK (1) DK1042301T3 (ru)
EA (1) EA002921B1 (ru)
ES (1) ES2186251T3 (ru)
HK (1) HK1034974A1 (ru)
HR (1) HRP20000412A2 (ru)
HU (1) HUP0104912A3 (ru)
ID (1) ID26248A (ru)
IL (1) IL136858A0 (ru)
MY (1) MY122269A (ru)
NO (1) NO317420B1 (ru)
NZ (1) NZ504954A (ru)
PL (1) PL341216A1 (ru)
PT (1) PT1042301E (ru)
SI (1) SI1042301T1 (ru)
SK (1) SK9032000A3 (ru)
TR (1) TR200001964T2 (ru)
TW (1) TW446705B (ru)
WO (1) WO1999032457A1 (ru)
YU (1) YU39000A (ru)
ZA (1) ZA9811571B (ru)

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GB9821061D0 (en) 1998-09-28 1998-11-18 Celltech Therapeutics Ltd Chemical compounds
GB9826174D0 (en) 1998-11-30 1999-01-20 Celltech Therapeutics Ltd Chemical compounds
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EP1065207A1 (en) * 1999-07-02 2001-01-03 Aventis Pharma Deutschland GmbH Naphthyridine derivatives, processes for their preparation, their use, and pharmaceutical compositions comprising them
EP1070707A1 (en) 1999-07-21 2001-01-24 Aventis Pharma Deutschland GmbH 1,4,5,6-tetrahydropyrimidine derivative as a vitronectin inhibitor
US6534513B1 (en) 1999-09-29 2003-03-18 Celltech R&D Limited Phenylalkanoic acid derivatives
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FR2808798A1 (fr) * 2000-05-09 2001-11-16 Hoechst Marion Roussel Inc Nouveaux derives antagonistes du recepteur de la vitronectine
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US6545013B2 (en) 2000-05-30 2003-04-08 Celltech R&D Limited 2,7-naphthyridine derivatives
JP2004502762A (ja) 2000-07-07 2004-01-29 セルテック　アール　アンド　ディ　リミテッド 二環性ヘテロ芳香環を含有するインテグリンアンタゴニストとしてのスクエア酸誘導体
EP1176145A1 (en) * 2000-07-28 2002-01-30 Aventis Pharma Deutschland GmbH Novel guanidino derivatives as inhibitors of cell adhesion
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EP1197488A1 (en) 2000-10-10 2002-04-17 Aventis Pharma Deutschland GmbH (2S)-2-(Adamantan-1-ylmethoxycarbonylamino)-3-(4-(2-(1,4,5,6-tetrahydropyrimidin-2-ylcarbamoyl)ethyl)benzoylamino)propionic acid isopropyl ester, its preparation and its use
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Also Published As

Publication number Publication date
CA2312712A1 (en) 1999-07-01
HUP0104912A3 (en) 2002-09-30
AU753109B2 (en) 2002-10-10
YU39000A (sh) 2002-11-15
EP1042301A1 (en) 2000-10-11
AP2000001842A0 (en) 2000-06-30
NO20003118D0 (no) 2000-06-16
AR016437A1 (es) 2001-07-04
SI1042301T1 (en) 2003-04-30
WO1999032457A1 (en) 1999-07-01
TW446705B (en) 2001-07-21
NO317420B1 (no) 2004-10-25
ID26248A (id) 2000-12-07
EP0933367A1 (en) 1999-08-04
ES2186251T3 (es) 2003-05-01
HRP20000412A2 (en) 2000-10-31
ATE228112T1 (de) 2002-12-15
EA002921B1 (ru) 2002-10-31
DK1042301T3 (da) 2003-03-17
KR20010033281A (ko) 2001-04-25
HK1034974A1 (en) 2001-11-09
TR200001964T2 (tr) 2000-11-21
ZA9811571B (en) 1999-06-21
DE69809594D1 (de) 2003-01-02
PL341216A1 (en) 2001-03-26
AU2270099A (en) 1999-07-12
US6492356B1 (en) 2002-12-10
DE69809594T2 (de) 2003-04-24
JP2001526271A (ja) 2001-12-18
PT1042301E (pt) 2003-04-30
NZ504954A (en) 2002-05-31
NO20003118L (no) 2000-08-21
EP1042301B1 (en) 2002-11-20
BG104544A (en) 2001-03-30
SK9032000A3 (en) 2001-04-09
CU23032A3 (es) 2005-03-22
HUP0104912A1 (hu) 2002-07-29
CN1205191C (zh) 2005-06-08
IL136858A0 (en) 2001-06-14
CN1284950A (zh) 2001-02-21
MY122269A (en) 2006-03-31
BR9814308A (pt) 2000-10-10
BG64754B1 (bg) 2006-02-28

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