DE69809594T2 - Acylguanidin derivate als inhibitoren von knochenresorption und als vitronectin rezeptor antagonisten - Google Patents

Acylguanidin derivate als inhibitoren von knochenresorption und als vitronectin rezeptor antagonisten

Info

Publication number
DE69809594T2
DE69809594T2 DE69809594T DE69809594T DE69809594T2 DE 69809594 T2 DE69809594 T2 DE 69809594T2 DE 69809594 T DE69809594 T DE 69809594T DE 69809594 T DE69809594 T DE 69809594T DE 69809594 T2 DE69809594 T2 DE 69809594T2
Authority
DE
Germany
Prior art keywords
alkyl
radical
formula
unsubstituted
aryl
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.)
Expired - Fee Related
Application number
DE69809594T
Other languages
German (de)
English (en)
Other versions
DE69809594D1 (de
Inventor
Catherine Bodary
Gerhard Breipohl
Denis Carniato
Andrew Cuthbertson
Napoleane Ferrara
Thomas Gadek
Jean-Francois Gourvest
Jochen Knolle
Robert Mcdowell
Anuschirwan Peyman
Karl-Heinz Scheunemann
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.)
Sanofi Aventis Deutschland GmbH
Genentech Inc
Original Assignee
Aventis Pharma Deutschland GmbH
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
Application filed by Aventis Pharma Deutschland GmbH, Genentech Inc filed Critical Aventis Pharma Deutschland GmbH
Publication of DE69809594D1 publication Critical patent/DE69809594D1/de
Application granted granted Critical
Publication of DE69809594T2 publication Critical patent/DE69809594T2/de
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C279/00Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
    • C07C279/20Derivatives 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/13Amines
    • A61K31/155Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/41641,3-Diazoles
    • A61K31/41681,3-Diazoles having a nitrogen attached in position 2, e.g. clonidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • 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
    • A61P19/08Drugs 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
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04Heterocyclic 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
    • C07D233/28Heterocyclic 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
    • C07D233/44Nitrogen atoms not forming part of a nitro radical
    • C07D233/48Nitrogen atoms not forming part of a nitro radical with acyclic hydrocarbon or substituted acyclic hydrocarbon radicals, attached to said nitrogen atoms
    • 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
    • C07D239/16Nitrogen atoms not forming part of a nitro radical acylated on said nitrogen atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (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)
  • Indole Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
DE69809594T 1997-12-19 1998-12-10 Acylguanidin derivate als inhibitoren von knochenresorption und als vitronectin rezeptor antagonisten Expired - Fee Related DE69809594T2 (de)

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
DE69809594D1 DE69809594D1 (de) 2003-01-02
DE69809594T2 true DE69809594T2 (de) 2003-04-24

Family

ID=8227841

Family Applications (1)

Application Number Title Priority Date Filing Date
DE69809594T Expired - Fee Related DE69809594T2 (de) 1997-12-19 1998-12-10 Acylguanidin derivate als inhibitoren von knochenresorption und als vitronectin rezeptor antagonisten

Country Status (33)

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

Families Citing this family (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6313119B1 (en) 1998-01-23 2001-11-06 Adventis Pharma Deutschland Gmbh Sulfonamide derivatives as inhibitors of bone resorption and as inhibitors of cell adhesion
GB9805655D0 (en) 1998-03-16 1998-05-13 Celltech Therapeutics Ltd Chemical compounds
US6521626B1 (en) 1998-03-24 2003-02-18 Celltech R&D Limited Thiocarboxamide derivatives
GB9814414D0 (en) 1998-07-03 1998-09-02 Celltech Therapeutics Ltd Chemical compounds
AU747784B2 (en) * 1998-07-29 2002-05-23 Merck & Co., Inc. Integrin receptor antagonists
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
EP1028114A1 (en) 1999-02-13 2000-08-16 Aventis Pharma Deutschland GmbH Novel guanidine derivatives as inhibitors of cell adhesion
US6518283B1 (en) 1999-05-28 2003-02-11 Celltech R&D Limited Squaric acid derivatives
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
US6849639B2 (en) 1999-12-14 2005-02-01 Amgen Inc. Integrin inhibitors and their methods of use
US6455539B2 (en) 1999-12-23 2002-09-24 Celltech R&D Limited Squaric acid derivates
AU2001248553A1 (en) 2000-04-17 2001-10-30 Celltech R And D Limited Enamine derivatives as cell adhesion molecules
FR2808798A1 (fr) * 2000-05-09 2001-11-16 Hoechst Marion Roussel Inc Nouveaux derives antagonistes du recepteur de la vitronectine
US6403608B1 (en) 2000-05-30 2002-06-11 Celltech R&D, Ltd. 3-Substituted isoquinolin-1-yl derivatives
US6545013B2 (en) 2000-05-30 2003-04-08 Celltech R&D Limited 2,7-naphthyridine derivatives
WO2002004426A1 (en) 2000-07-07 2002-01-17 Celltech R & D Limited Squaric acid derivatives containing a bicyclic heteroaromatic ring as integrin antagonists
EP1176145A1 (en) 2000-07-28 2002-01-30 Aventis Pharma Deutschland GmbH Novel guanidino derivatives as inhibitors of cell adhesion
EP1305291A1 (en) 2000-08-02 2003-05-02 Celltech R&D Limited 3-substituted isoquinolin-1-yl derivatives
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
FR2847254B1 (fr) * 2002-11-19 2005-01-28 Aventis Pharma Sa Nouveaux derives antagonistes du recepteur de la vitronectine, leur procede de preparation, leur application comme medicaments et les compositions pharmaceutiques les refermant
FR2870541B1 (fr) 2004-05-18 2006-07-14 Proskelia Sas Derives de pyrimidines antigonistes du recepteur de la vitronectine
UA87854C2 (en) 2004-06-07 2009-08-25 Мерк Энд Ко., Инк. N-(2-benzyl)-2-phenylbutanamides as androgen receptor modulators
FR2873585B1 (fr) * 2004-07-27 2006-11-17 Aventis Pharma Sa Nouvelles formulations galeniques de principes actifs
US20060039949A1 (en) * 2004-08-20 2006-02-23 Nycz Jeffrey H Acetabular cup with controlled release of an osteoinductive formulation
US20060057184A1 (en) * 2004-09-16 2006-03-16 Nycz Jeffrey H Process to treat avascular necrosis (AVN) with osteoinductive materials
US8414907B2 (en) 2005-04-28 2013-04-09 Warsaw Orthopedic, Inc. Coatings on medical implants to guide soft tissue healing
US9119901B2 (en) * 2005-04-28 2015-09-01 Warsaw Orthopedic, Inc. Surface treatments for promoting selective tissue attachment to medical impants
US20070077267A1 (en) * 2005-10-03 2007-04-05 Sdgi Holdings, Inc. Bioactive composite implants
US20070280986A1 (en) * 2006-06-01 2007-12-06 Carlos Gil Intra-operative coating of implants
US8133553B2 (en) 2007-06-18 2012-03-13 Zimmer, Inc. Process for forming a ceramic layer
US8309521B2 (en) 2007-06-19 2012-11-13 Zimmer, Inc. Spacer with a coating thereon for use with an implant device
US8608049B2 (en) 2007-10-10 2013-12-17 Zimmer, Inc. Method for bonding a tantalum structure to a cobalt-alloy substrate
US20090192609A1 (en) * 2008-01-29 2009-07-30 Zimmer, Inc. Implant device for use in an implant system
SG11201609050UA (en) 2014-05-30 2016-12-29 Pfizer Carbonitrile derivatives as selective androgen receptor modulators
US11020160B2 (en) 2016-03-21 2021-06-01 Warsaw Orthopedic, Inc. Surgical injection system and method
US10709814B2 (en) 2016-04-22 2020-07-14 Warsaw Orthopedic, Inc. Osteoimplant comprising an insoluble fibrous polymer
WO2023275715A1 (en) 2021-06-30 2023-01-05 Pfizer Inc. Metabolites of selective androgen receptor modulators

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5204350A (en) * 1991-08-09 1993-04-20 Merck & Co., Inc. Method of inhibiting osteoclast-mediated bone resorption by administration of n-heterocyclicalkyl-substituted phenyl derivatives
US5217994A (en) * 1991-08-09 1993-06-08 Merck & Co., Inc. Method of inhibiting osteoclast-mediated bone resorption by administration of aminoalkyl-substituted phenyl derivatives
AU674553B2 (en) * 1992-10-14 1997-01-02 Merck & Co., Inc. Fibrinogen receptor antagonists
JPH08504194A (ja) * 1992-12-01 1996-05-07 メルク エンド カンパニー インコーポレーテッド フィブリノーゲンレセプターアンタゴニスト
JP3895792B2 (ja) * 1995-12-08 2007-03-22 プロスケリア・エス・ア・エス 骨形成促進剤

Also Published As

Publication number Publication date
TR200001964T2 (tr) 2000-11-21
ZA9811571B (en) 1999-06-21
DE69809594D1 (de) 2003-01-02
AU2270099A (en) 1999-07-12
TW446705B (en) 2001-07-21
HUP0104912A3 (en) 2002-09-30
CN1284950A (zh) 2001-02-21
JP2001526271A (ja) 2001-12-18
HRP20000412A2 (en) 2000-10-31
PT1042301E (pt) 2003-04-30
KR20010033281A (ko) 2001-04-25
PL341216A1 (en) 2001-03-26
BG104544A (en) 2001-03-30
EA200000682A1 (ru) 2000-12-25
HK1034974A1 (en) 2001-11-09
DK1042301T3 (da) 2003-03-17
ID26248A (id) 2000-12-07
ES2186251T3 (es) 2003-05-01
NO20003118L (no) 2000-08-21
SK9032000A3 (en) 2001-04-09
AP2000001842A0 (en) 2000-06-30
EA002921B1 (ru) 2002-10-31
AU753109B2 (en) 2002-10-10
CU23032A3 (es) 2005-03-22
EP1042301B1 (en) 2002-11-20
EP1042301A1 (en) 2000-10-11
ATE228112T1 (de) 2002-12-15
NO20003118D0 (no) 2000-06-16
US6492356B1 (en) 2002-12-10
HUP0104912A1 (hu) 2002-07-29
MY122269A (en) 2006-03-31
NZ504954A (en) 2002-05-31
BG64754B1 (bg) 2006-02-28
IL136858A0 (en) 2001-06-14
BR9814308A (pt) 2000-10-10
WO1999032457A1 (en) 1999-07-01
AR016437A1 (es) 2001-07-04
SI1042301T1 (en) 2003-04-30
NO317420B1 (no) 2004-10-25
EP0933367A1 (en) 1999-08-04
CA2312712A1 (en) 1999-07-01
CN1205191C (zh) 2005-06-08
YU39000A (sh) 2002-11-15

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Legal Events

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8364 No opposition during term of opposition
8328 Change in the person/name/address of the agent

Representative=s name: PFENNING MEINIG & PARTNER GBR, 80339 MUENCHEN

8339 Ceased/non-payment of the annual fee