ATE207889T1 - Trizyclische verbindungen mit wirkung auf integrine, besonders auf das alphavbeta3-integrin,verfahren zur ihrer herstellung und zwischenprodukte des verfahrens, ihre verwendung als arzneimittel und sie enthaltende pharmazeutische zusammensetzungen - Google Patents

Trizyclische verbindungen mit wirkung auf integrine, besonders auf das alphavbeta3-integrin,verfahren zur ihrer herstellung und zwischenprodukte des verfahrens, ihre verwendung als arzneimittel und sie enthaltende pharmazeutische zusammensetzungen

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Publication number
ATE207889T1
ATE207889T1 AT97915519T AT97915519T ATE207889T1 AT E207889 T1 ATE207889 T1 AT E207889T1 AT 97915519 T AT97915519 T AT 97915519T AT 97915519 T AT97915519 T AT 97915519T AT E207889 T1 ATE207889 T1 AT E207889T1
Authority
AT
Austria
Prior art keywords
trizyclic
integrins
integrin
products
production
Prior art date
Application number
AT97915519T
Other languages
English (en)
Inventor
Serge Bernard
Denis Carniato
Jean-Francois Gourvest
Jean-Georges Teutsch
Jochen Knolle
Hans-Ulrich Stilz
Volkmar Wehner
Sarah C Bodary
Thomas R Gadek
Robert S Mcdowell
Robert M Pitti
Original Assignee
Aventis Pharma Sa
Genentech 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
Priority claimed from FR9603437A external-priority patent/FR2746394B1/fr
Application filed by Aventis Pharma Sa, Genentech Inc filed Critical Aventis Pharma Sa
Application granted granted Critical
Publication of ATE207889T1 publication Critical patent/ATE207889T1/de

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    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C281/00Derivatives of carbonic acid containing functional groups covered by groups C07C269/00 - C07C279/00 in which at least one nitrogen atom of these functional groups is further bound to another nitrogen atom not being part of a nitro or nitroso group
    • C07C281/06Compounds containing any of the groups, e.g. semicarbazides
    • C07C281/08Compounds containing any of the groups, e.g. semicarbazides the other nitrogen atom being further doubly-bound to a carbon atom, e.g. semicarbazones
    • C07C281/12Compounds containing any of the groups, e.g. semicarbazides the other nitrogen atom being further doubly-bound to a carbon atom, e.g. semicarbazones the carbon atom being part of a ring other than a six-membered aromatic ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/06Heterocyclic 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
    • C07D239/08Heterocyclic 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
    • C07D239/12Nitrogen atoms not forming part of a nitro radical
    • C07D239/18Nitrogen atoms not forming part of a nitro radical with hetero atoms attached to said nitrogen atoms, except nitro radicals, e.g. hydrazine radicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/06Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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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    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C281/00Derivatives of carbonic acid containing functional groups covered by groups C07C269/00 - C07C279/00 in which at least one nitrogen atom of these functional groups is further bound to another nitrogen atom not being part of a nitro or nitroso group
    • C07C281/16Compounds containing any of the groups, e.g. aminoguanidine
    • C07C281/18Compounds containing any of the groups, e.g. aminoguanidine the other nitrogen atom being further doubly-bound to a carbon atom, e.g. guanylhydrazones
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C331/00Derivatives of thiocyanic acid or of isothiocyanic acid
    • C07C331/02Thiocyanates
    • C07C331/04Thiocyanates having sulfur atoms of thiocyanate groups bound to acyclic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C331/00Derivatives of thiocyanic acid or of isothiocyanic acid
    • C07C331/02Thiocyanates
    • C07C331/10Thiocyanates having sulfur atoms of thiocyanate groups bound to carbon atoms of hydrocarbon radicals substituted by singly-bound oxygen atoms
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    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C331/00Derivatives of thiocyanic acid or of isothiocyanic acid
    • C07C331/02Thiocyanates
    • C07C331/12Thiocyanates having sulfur atoms of thiocyanate groups bound to carbon atoms of hydrocarbon radicals substituted by nitrogen atoms, not being part of nitro or nitroso groups
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    • C07C331/00Derivatives of thiocyanic acid or of isothiocyanic acid
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    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C337/00Derivatives of thiocarbonic acids containing functional groups covered by groups C07C333/00 or C07C335/00 in which at least one nitrogen atom of these functional groups is further bound to another nitrogen atom not being part of a nitro or nitroso group
    • C07C337/06Compounds containing any of the groups, e.g. thiosemicarbazides
    • C07C337/08Compounds containing any of the groups, e.g. thiosemicarbazides the other nitrogen atom being further doubly-bound to a carbon atom, e.g. thiosemicarbazones
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    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/51Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by pyrolysis, rearrangement or decomposition
    • C07C45/516Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by pyrolysis, rearrangement or decomposition involving transformation of nitrogen-containing compounds to >C = O groups
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    • C07C45/63Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by introduction of halogen; by substitution of halogen atoms by other halogen atoms
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    • C07C45/673Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by change of size of the carbon skeleton
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    • C07C45/61Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups
    • C07C45/67Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton
    • C07C45/68Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms
    • C07C45/70Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms by reaction with functional groups containing oxygen only in singly bound form
    • C07C45/71Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms by reaction with functional groups containing oxygen only in singly bound form being hydroxy groups
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    • C07C49/00Ketones; Ketenes; Dimeric ketenes; Ketonic chelates
    • C07C49/587Unsaturated compounds containing a keto groups being part of a ring
    • C07C49/703Unsaturated compounds containing a keto groups being part of a ring containing hydroxy groups
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    • C07C49/753Unsaturated compounds containing a keto groups being part of a ring containing ether groups, groups, groups, or groups
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    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
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    • C07D233/28Heterocyclic 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
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    • YGENERAL 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
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
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    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
AT97915519T 1996-03-20 1997-03-20 Trizyclische verbindungen mit wirkung auf integrine, besonders auf das alphavbeta3-integrin,verfahren zur ihrer herstellung und zwischenprodukte des verfahrens, ihre verwendung als arzneimittel und sie enthaltende pharmazeutische zusammensetzungen ATE207889T1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
FR9603437A FR2746394B1 (fr) 1996-03-20 1996-03-20 Nouveaux composes tricycliques, leur procede de preparation, et les intermediaires de ce procede, leur application a titre de medicaments et les compositions pharmaceutiques les renfermant
PCT/FR1997/000487 WO1997034865A1 (fr) 1996-03-20 1997-03-20 COMPOSES TRICYCLIQUES AYANT UNE ACTIVITE VIS-A-VIS DES INTEGRINES NOTAMMENT VIS-A-VIS DE L'INTEGRINE ALPHA vBETA3, LEUR PROCEDE DE PREPARATION ET LES INTERMEDIAIRES DE CE PROCEDE, LEUR APPLICATION A TITRE DE MEDICAMENTS ET LES COMPOSITIONS PHARMACEUTIQUES LES RENFERMANT

Publications (1)

Publication Number Publication Date
ATE207889T1 true ATE207889T1 (de) 2001-11-15

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AT97915519T ATE207889T1 (de) 1996-03-20 1997-03-20 Trizyclische verbindungen mit wirkung auf integrine, besonders auf das alphavbeta3-integrin,verfahren zur ihrer herstellung und zwischenprodukte des verfahrens, ihre verwendung als arzneimittel und sie enthaltende pharmazeutische zusammensetzungen

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US (1) US6221907B1 (de)
EP (1) EP0888292B1 (de)
JP (1) JP4091983B2 (de)
KR (1) KR20000064710A (de)
AP (1) AP806A (de)
AT (1) ATE207889T1 (de)
AU (1) AU728852B2 (de)
BG (1) BG63569B1 (de)
BR (1) BR9708231A (de)
CA (1) CA2249471A1 (de)
DE (1) DE69707843T2 (de)
DK (1) DK0888292T3 (de)
EA (1) EA002271B1 (de)
EE (1) EE9800317A (de)
GE (1) GEP20012516B (de)
LV (1) LV12207B (de)
NO (1) NO312459B1 (de)
NZ (1) NZ331778A (de)
SI (1) SI9720021A (de)
SK (1) SK282894B6 (de)
WO (1) WO1997034865A1 (de)

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FR2768736B1 (fr) * 1997-09-24 2000-05-26 Roussel Uclaf Nouveaux composes tricycliques, leur procede de preparation et les intermediaires de ce procede, leur application a titre de medicaments et les compositions pharmaceutiques les renfermant
FR2768734B1 (fr) * 1997-09-24 2000-01-28 Roussel Uclaf Nouveaux composes tricycliques, leur procede de preparation et les intermediaires de ce procede, leur application a titre de medicaments et les compositions pharmaceutiques les renfermant
TW538046B (en) 1998-01-08 2003-06-21 Hoechst Marion Roussel Inc Aromatic amides having antiobiotic activities and the preparation processes, intermediates and pharmaceutical composition thereof
FR2786181B1 (fr) 1998-11-24 2001-10-26 Hoechst Marion Roussel Inc Nouveaux derives d'iminoguanidines, leur procede de preparation, leur application comme medicaments et les compositions pharmaceutiques les renfermant
DE19916837A1 (de) * 1999-04-14 2000-10-19 Merck Patent Gmbh Dibenzoazulenderivate
WO2001038297A1 (en) * 1999-11-18 2001-05-31 Ajinomoto Co., Inc. Novel intermediate for sweetener with high sweetness and process for producing the same
KR100523119B1 (ko) * 2000-03-16 2005-10-20 에프. 호프만-라 로슈 아게 Ip 길항제로서의 카복실산 유도체
JP4660067B2 (ja) 2001-04-24 2011-03-30 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング 抗血管新生剤とTNFαとを用いる組合せ療法
UA87854C2 (en) 2004-06-07 2009-08-25 Мерк Энд Ко., Инк. N-(2-benzyl)-2-phenylbutanamides as androgen receptor modulators
BRPI0706540A2 (pt) 2006-01-18 2011-03-29 Merck Patent Gmbh terapia especìfica usando ligantes de integrina para tratar cáncer
KR101482956B1 (ko) * 2006-12-26 2015-01-15 센트로 데 인뮤놀러지아 모레큘러 류마티스 관절염의 진단 및 치료에 사용되는 항-cd6 단일클론성 항체를 포함하는 약학 조성물
EP2441464B1 (de) 2007-01-18 2014-04-09 Merck Patent GmbH Integrin-liganden zur verwendung in der behandlung von darmkrebs
WO2009113083A1 (en) 2008-03-14 2009-09-17 Biocon Limited A monoclonal antibody and a method thereof
CN102448497A (zh) 2009-05-25 2012-05-09 默克专利有限公司 在癌症治疗中的西仑吉肽的持续给药
CN102603743B (zh) * 2012-02-24 2014-05-28 南京天易生物科技有限公司 抗肿瘤的氮杂苯并[f]薁衍生物其制备方法及其用途
EP3024485B1 (de) 2013-07-23 2020-11-18 Biocon Limited Verwendung eines cd6-bindungspartners und verfahren damit
ES2864079T3 (es) 2014-05-30 2021-10-13 Pfizer Derivados de carbonitrilo como moduladores selectivos del receptor de andrógenos
ES2991182T3 (es) 2016-10-21 2024-12-02 Biocon Ltd Un anticuerpo monoclonal y un método de uso para el tratamiento del lupus
WO2023275715A1 (en) 2021-06-30 2023-01-05 Pfizer Inc. Metabolites of selective androgen receptor modulators

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JPH10504825A (ja) 1994-08-22 1998-05-12 スミスクライン・ビーチャム・コーポレイション 二環式化合物
FR2731217B1 (fr) * 1995-03-03 1997-06-13 Roussel Uclaf Nouveaux derives tricycliques, leur preparation, leur application a la preparation de la colchicine et de la thiocolchicine optiquement actives ou racemiques et d'analogues ou derives et intermediaires

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JP4091983B2 (ja) 2008-05-28
EP0888292B1 (de) 2001-10-31
NO984352L (no) 1998-11-19
DE69707843D1 (de) 2001-12-06
DE69707843T2 (de) 2002-05-16
GEP20012516B (en) 2001-08-27
NO984352D0 (no) 1998-09-18
LV12207B (lv) 1999-03-20
CA2249471A1 (fr) 1997-09-25
SK282894B6 (sk) 2003-01-09
SK124998A3 (en) 1999-08-06
BR9708231A (pt) 1999-08-03
AU2296697A (en) 1997-10-10
NZ331778A (en) 2000-02-28
EP0888292A1 (de) 1999-01-07
SI9720021A (sl) 1999-04-30
US6221907B1 (en) 2001-04-24
WO1997034865A1 (fr) 1997-09-25
AP806A (en) 2000-01-28
EE9800317A (et) 1999-04-15
DK0888292T3 (da) 2002-02-18
EA002271B1 (ru) 2002-02-28
JP2000506879A (ja) 2000-06-06
NO312459B1 (no) 2002-05-13
BG63569B1 (bg) 2002-05-31
LV12207A (lv) 1999-01-20
AU728852B2 (en) 2001-01-18
KR20000064710A (ko) 2000-11-06
EA199800837A1 (ru) 1999-06-24
BG102778A (en) 1999-05-31
AP9801342A0 (en) 1998-09-30

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