DK0891325T3 - Para-substituerede phenylpropansyrederivater som integrinantagonister - Google Patents

Para-substituerede phenylpropansyrederivater som integrinantagonister

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Publication number
DK0891325T3
DK0891325T3 DK97916852T DK97916852T DK0891325T3 DK 0891325 T3 DK0891325 T3 DK 0891325T3 DK 97916852 T DK97916852 T DK 97916852T DK 97916852 T DK97916852 T DK 97916852T DK 0891325 T3 DK0891325 T3 DK 0891325T3
Authority
DK
Denmark
Prior art keywords
para
acid derivatives
phenylpropanoic acid
integrin antagonists
substituted phenylpropanoic
Prior art date
Application number
DK97916852T
Other languages
Danish (da)
English (en)
Inventor
Barbara B Chen
Helen Y Chen
Glen J Gesicki
Richard A Haack
James W Malecha
Thomas D Penning
Joseph G Rico
Thomas E Rogers
Peter G Ruminski
Mark A Russell
Stella S Yu
Original Assignee
Searle & Co
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 Searle & Co filed Critical Searle & Co
Application granted granted Critical
Publication of DK0891325T3 publication Critical patent/DK0891325T3/da

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/06—1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
    • C07D271/07—1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
    • 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
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C275/00—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C275/28—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C275/42—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by carboxyl groups
    • 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
    • C07C279/18—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to carbon atoms of six-membered aromatic rings
    • 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
    • C07C279/22—Y being a hydrogen or a carbon atom, e.g. benzoylguanidines
    • C—CHEMISTRY; METALLURGY
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    • 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
    • C07C279/24—Y being a hetero atom
    • 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
    • C07C279/28—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to cyano groups, e.g. cyanoguanidines, dicyandiamides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/01—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
    • C07C311/02—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C311/03—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the sulfonamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C311/06—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the sulfonamide groups bound to hydrogen atoms or to acyclic carbon atoms to acyclic carbon atoms of hydrocarbon radicals substituted by carboxyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/01—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
    • C07C311/12—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings
    • C07C311/13—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings the carbon skeleton containing six-membered aromatic rings
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    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/16—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
    • C07C311/19—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/50—Compounds containing any of the groups, X being a hetero atom, Y being any atom
    • C07C311/52—Y being a hetero atom
    • C07C311/64—X and Y being nitrogen atoms, e.g. N-sulfonylguanidine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/44—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/50—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton
    • C07C323/51—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C323/52—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
    • 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
    • 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
    • C07D231/12—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 only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • 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
    • C07D233/50—Nitrogen atoms not forming part of a nitro radical with carbocyclic radicals directly attached to said nitrogen atoms
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    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two 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
    • C07D233/88—Nitrogen atoms, e.g. allantoin
    • 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
    • C07D239/14—Nitrogen atoms not forming part of a nitro radical with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to said nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
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    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C07D249/10—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles 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
    • C07D249/14—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/20—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof
    • C07D295/215—Radicals derived from nitrogen analogues of carbonic acid

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Epidemiology (AREA)
  • Vascular Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Peptides Or Proteins (AREA)
DK97916852T 1996-03-29 1997-03-26 Para-substituerede phenylpropansyrederivater som integrinantagonister DK0891325T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US1428896P 1996-03-29 1996-03-29
PCT/US1997/004460 WO1997036859A1 (en) 1996-03-29 1997-03-26 Para-substituted phenylpropanoic acid derivatives as integrin antagonists

Publications (1)

Publication Number Publication Date
DK0891325T3 true DK0891325T3 (da) 2002-05-21

Family

ID=21764580

Family Applications (1)

Application Number Title Priority Date Filing Date
DK97916852T DK0891325T3 (da) 1996-03-29 1997-03-26 Para-substituerede phenylpropansyrederivater som integrinantagonister

Country Status (12)

Country Link
US (2) US5952381A (enExample)
EP (1) EP0891325B1 (enExample)
JP (1) JP2000515493A (enExample)
AT (1) ATE212978T1 (enExample)
AU (1) AU2536097A (enExample)
CA (1) CA2250698A1 (enExample)
DE (1) DE69710319T2 (enExample)
DK (1) DK0891325T3 (enExample)
ES (1) ES2172780T3 (enExample)
HK (1) HK1044527A1 (enExample)
PT (1) PT891325E (enExample)
WO (1) WO1997036859A1 (enExample)

Families Citing this family (81)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL186370B1 (pl) * 1995-08-30 2003-12-31 Searle & Co Związki, pochodne kwasu aminobenzoesowego, zawierające je kompozycje farmaceutyczne oraz zastosowanie tych związków
EP0963370B1 (en) * 1996-12-09 2003-03-19 Eli Lilly And Company Integrin antagonists
US6245809B1 (en) 1996-12-09 2001-06-12 Cor Therapeutics Inc. Integrin antagonists
WO1998057173A1 (en) * 1997-06-10 1998-12-17 Eli Lilly And Company Combinatorial process for preparing substituted phenylalanine libraries
NZ502813A (en) * 1997-08-22 2002-10-25 F N-aroylphenylalanine derivatives as inhibitors of the interaction between a4 containing integrins and VCAM-1
US6229011B1 (en) 1997-08-22 2001-05-08 Hoffman-La Roche Inc. N-aroylphenylalanine derivative VCAM-1 inhibitors
US6455550B1 (en) 1997-08-22 2002-09-24 Hoffmann-La Roche Inc. N-alkanoylphenylalanine derivatives
SI1005445T1 (en) * 1997-08-22 2004-12-31 F. Hoffmann-La Roche Ag N-alkanoylphenylalanine derivatives
DE69830410T2 (de) * 1997-08-29 2006-01-26 Tularik Ltd. Meta-benzamidinderivate als serinprotease-inhibitoren
US6740682B2 (en) 1997-08-29 2004-05-25 Tularik Limited Meta-benzamidine derivatives as serine protease inhibitors
CA2303848C (en) 1997-10-31 2008-09-30 Rhone-Poulenc Rorer Limited Substituted anilides
CA2316235A1 (en) * 1997-12-23 1999-07-08 Aventis Pharma Limited Substituted .beta.-alanines
US6329372B1 (en) 1998-01-27 2001-12-11 Celltech Therapeutics Limited Phenylalanine derivatives
JP2002504534A (ja) * 1998-02-26 2002-02-12 セルテック・セラピューティクス・リミテッド α４インテグリンの阻害剤としてのフェニルアラニン誘導体
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
JP4064059B2 (ja) 1998-04-09 2008-03-19 明治製菓株式会社 インテグリンαＶβ３拮抗剤としてのアミノピペリジン誘導体
GB9811159D0 (en) 1998-05-22 1998-07-22 Celltech Therapeutics Ltd Chemical compounds
GB9811969D0 (en) 1998-06-03 1998-07-29 Celltech Therapeutics Ltd Chemical compounds
GB9812088D0 (en) 1998-06-05 1998-08-05 Celltech Therapeutics Ltd Chemical compounds
GB9814414D0 (en) 1998-07-03 1998-09-02 Celltech Therapeutics Ltd Chemical compounds
US6352977B1 (en) 1998-07-13 2002-03-05 Aventis Pharma Limited Substituted β-alanines
GB9821061D0 (en) * 1998-09-28 1998-11-18 Celltech Therapeutics Ltd Chemical compounds
GB9821222D0 (en) 1998-09-30 1998-11-25 Celltech Therapeutics Ltd Chemical compounds
GB9825652D0 (en) 1998-11-23 1999-01-13 Celltech Therapeutics Ltd Chemical compounds
GB9826174D0 (en) * 1998-11-30 1999-01-20 Celltech Therapeutics Ltd Chemical compounds
US6677360B2 (en) 1998-12-16 2004-01-13 Bayer Aktiengesellschaft Biphenyl and biphenyl-analogous compounds as integrin antagonists
IL143484A0 (en) * 1998-12-16 2002-04-21 Bayer Ag New biphenyl and biphenyl-analogous compounds as integrin antagonists
US6858598B1 (en) 1998-12-23 2005-02-22 G. D. Searle & Co. Method of using a matrix metalloproteinase inhibitor and one or more antineoplastic agents as a combination therapy in the treatment of neoplasia
US6833373B1 (en) 1998-12-23 2004-12-21 G.D. Searle & Co. Method of using an integrin antagonist and one or more antineoplastic agents as a combination therapy in the treatment of neoplasia
EA006294B1 (ru) 1998-12-23 2005-10-27 Дж.Д.Сирл Энд Ко. Применение комбинации целекоксиба и гемцитабина в комбинированном способе лечебного воздействия при лечении рака поджелудочной железы
US6291503B1 (en) 1999-01-15 2001-09-18 Bayer Aktiengesellschaft β-phenylalanine derivatives as integrin antagonists
US6344484B1 (en) 1999-02-12 2002-02-05 3-Dimensional Pharmaceuticals, Inc. Tyrosine alkoxyguanidines as integrin inhibitors
WO2000048994A1 (en) 1999-02-18 2000-08-24 F. Hoffmann-La Roche Ag Thioamide derivatives
DK1154987T3 (da) * 1999-02-18 2004-08-09 Hoffmann La Roche Phenylalaninolderivater
FR2792314B1 (fr) * 1999-04-15 2001-06-01 Adir Nouveaux composes aminotriazoles, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
US6518283B1 (en) 1999-05-28 2003-02-11 Celltech R&D Limited Squaric acid derivatives
WO2001010844A1 (fr) 1999-08-05 2001-02-15 Meiji Seika Kaisha, Ltd. DERIVES D'ACIDE φ-AMINO-α-HYDROXYCARBOXYLIQUE POSSEDANT UN ANTAGONISME αvβ3 D'INTEGRINE
US6534513B1 (en) 1999-09-29 2003-03-18 Celltech R&D Limited Phenylalkanoic acid derivatives
CA2352957A1 (en) 1999-09-29 2001-04-05 Ortho-Mcneil Pharmaceutical, Inc. Isonipecotamides for the treatment of integrin-mediated disorders
WO2001032610A1 (en) * 1999-10-29 2001-05-10 Kaken Pharmaceutical Co., Ltd. Urea derivative, process for producing the same, and medicine containing the urea derivative
WO2001044186A1 (en) * 1999-12-16 2001-06-21 Sumitomo Pharmaceuticals Company, Limited Substituted guanidine derivatives
US6455539B2 (en) 1999-12-23 2002-09-24 Celltech R&D Limited Squaric acid derivates
EP1250935A1 (en) * 2000-01-25 2002-10-23 Meiji Seika Kaisha Ltd. REMEDIES FOR REPERFUSION INJURY CONTAINING INTEGRIN ALPHAvBETA3 ANTAGONIST
RU2240826C2 (ru) * 2000-02-03 2004-11-27 Эйсай Ко., Лтд. Ингибитор экспрессии интегрина
EP1332132B1 (en) 2000-04-17 2007-10-10 UCB Pharma, S.A. Enamine derivatives as cell adhesion molecules
GB0011817D0 (en) * 2000-05-16 2000-07-05 Pharmacia & Upjohn Spa Antagonists of integrin receptors
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
DE10032256C2 (de) * 2000-07-03 2003-06-05 Infineon Technologies Ag Chip-ID-Register-Anordnung
AU2001267753A1 (en) 2000-07-07 2002-01-21 Celltech R And D Limited Squaric acid derivatives containing a bicyclic heteroaromatic ring as integrin antagonists
US7015216B2 (en) * 2000-07-21 2006-03-21 Elan Pharmaceuticals, Inc. Heteroaryl-β-alanine derivatives as alpha 4 integrin inhibitors
EP1318803A1 (en) * 2000-08-02 2003-06-18 SmithKline Beecham Corporation Fatty acid synthase inhibitors
EP1305291A1 (en) 2000-08-02 2003-05-02 Celltech R&D Limited 3-substituted isoquinolin-1-yl derivatives
US7163681B2 (en) 2000-08-07 2007-01-16 Centocor, Inc. Anti-integrin antibodies, compositions, methods and uses
US7288390B2 (en) 2000-08-07 2007-10-30 Centocor, Inc. Anti-dual integrin antibodies, compositions, methods and uses
US6486174B2 (en) 2000-08-07 2002-11-26 3-Dimensional Pharmaceuticals, Inc. Tetrahydroisoquinoline-3-carboxylic acid alkoxyguanidines as integrin antagonists
AU2001277720A1 (en) * 2000-08-09 2002-02-25 Kaken Pharmaceutical Co., Ltd. (thio)urea derivatives, process for their production and medicines containing the derivatives
DZ3415A1 (fr) 2000-08-31 2002-03-07 Chiron Corp Guanidinobenzamides comme mc4-r agonistes.
NZ539682A (en) * 2001-01-29 2006-03-31 Dimensional Pharm Inc Substituted indoles and their use as integrin antagonists
ITTO20010110A1 (it) * 2001-02-08 2002-08-08 Rotta Research Lab Nuovi derivati benzamidinici dotati di attivita' anti-infiammatoria ed immunosoppressiva.
DK1385823T3 (da) * 2001-04-09 2007-03-26 Novartis Vaccines & Diagnostic Guanidinoforbindelser som melanocortin-4-receptor- (MC4-R) -agonister
EP1389205B1 (en) 2001-04-09 2005-12-21 Ortho-McNeil Pharmaceutical Research Inc. Quinazoline and quinazoline-like compounds for the treatment of integrin-mediated disorders
US6872730B2 (en) 2001-04-27 2005-03-29 3-Dimensional Pharmaceuticals, Inc. Substituted benzofurans and benzothiophenes, methods of making and methods of use as integrin antagonists
US8252902B2 (en) 2001-10-22 2012-08-28 The Scripps Research Institute Antibody targeting compounds
US20030207814A1 (en) * 2002-02-04 2003-11-06 Chiron Corporation Novel guanidinyl derivatives
US20050124652A1 (en) * 2002-02-04 2005-06-09 Rustum Boyce Guanidino compounds
US20030195187A1 (en) * 2002-02-04 2003-10-16 Chiron Corporation Guanidino compounds
JP2005524649A (ja) * 2002-02-25 2005-08-18 カイロン コーポレーション Ｍｃ４−ｒアゴニストの鼻腔内投与
EP1551834B1 (en) * 2002-05-23 2010-08-25 Novartis Vaccines and Diagnostics, Inc. Substituted quinazolinone compounds
KR20060018217A (ko) * 2003-05-23 2006-02-28 카이론 코포레이션 Ｍｃ4-ｒ 작용제로서 구아니디노-치환된 퀴나졸리논 화합물
AU2004251668B2 (en) * 2003-06-03 2008-03-20 Triad Therapeutics, Inc 5-membered heterocycle-based p-38 inhibitors
WO2005051391A1 (en) * 2003-11-19 2005-06-09 Chiron Corporation Quinazolinone compounds with reduced bioaccumulation
WO2007048127A2 (en) * 2005-10-20 2007-04-26 The Scripps Research Institute Fc labeling for immunostaining and immunotargeting
AU2007263076A1 (en) 2006-06-20 2007-12-27 F. Hoffmann-La Roche Ag Arylsulfonyl naphthalene derivatives and uses thereof
WO2010093706A2 (en) 2009-02-10 2010-08-19 The Scripps Research Institute Chemically programmed vaccination
US20140010783A1 (en) * 2012-07-06 2014-01-09 Hoffmann-La Roche Inc. Antiviral compounds
IN2015DN00099A (enExample) 2012-07-18 2015-05-29 Univ Saint Louis
US8716226B2 (en) 2012-07-18 2014-05-06 Saint Louis University 3,5 phenyl-substituted beta amino acid derivatives as integrin antagonists
EP3294716B1 (en) 2015-12-30 2020-04-15 Saint Louis University Meta-azacyclic amino benzoic acid derivatives as pan integrin antagonists
CN107652210B (zh) * 2017-09-30 2021-01-01 瑞阳（上海）新药研发有限公司 一种胍类化合物或其药学上可接受的盐、其制备方法和应用

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FI890918A7 (fi) * 1988-03-11 1989-09-12 Eisai Co Ltd Polypeptider.
US5039805A (en) * 1988-12-08 1991-08-13 Hoffmann-La Roche Inc. Novel benzoic and phenylacetic acid derivatives
NZ239846A (en) * 1990-09-27 1994-11-25 Merck & Co Inc Sulphonamide derivatives and pharmaceutical compositions thereof
IL99537A (en) * 1990-09-27 1995-11-27 Merck & Co Inc Fibrinogen receptor antagonists and pharmaceutical compositions containing them
WO1992008464A1 (en) * 1990-11-15 1992-05-29 Tanabe Seiyaku Co. Ltd. Substituted urea and related cell adhesion modulation compounds
WO1993008823A1 (en) * 1991-11-06 1993-05-13 Tanabe Seiyaku Co., Ltd. Guanidinyl and related cell adhesion modulation compounds
US5352667A (en) * 1991-11-22 1994-10-04 Ofer Lider Non-peptidic surrogates of the Arg-Gly-Asp sequence and pharmaceutical compositions comprising them
WO1995032710A1 (en) * 1994-05-27 1995-12-07 Merck & Co., Inc. Compounds for inhibiting osteoclast-mediated bone resorption

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ATE212978T1 (de) 2002-02-15
US5952381A (en) 1999-09-14
EP0891325B1 (en) 2002-02-06
CA2250698A1 (en) 1997-10-09
US6251944B1 (en) 2001-06-26
ES2172780T3 (es) 2002-10-01
EP0891325A1 (en) 1999-01-20
JP2000515493A (ja) 2000-11-21
AU2536097A (en) 1997-10-22
DE69710319T2 (de) 2002-08-14
PT891325E (pt) 2002-07-31
WO1997036859A1 (en) 1997-10-09
DE69710319D1 (de) 2002-03-21

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