HK1044527A1 - Para-substituted phenylene derivatives and their use as integrin antagonists - Google Patents

Para-substituted phenylene derivatives and their use as integrin antagonists Download PDF

Info

Publication number
HK1044527A1
HK1044527A1 HK02103989.5A HK02103989A HK1044527A1 HK 1044527 A1 HK1044527 A1 HK 1044527A1 HK 02103989 A HK02103989 A HK 02103989A HK 1044527 A1 HK1044527 A1 HK 1044527A1
Authority
HK
Hong Kong
Prior art keywords
amino
carbonyl
phenyl
aminoiminomethyl
aryl
Prior art date
Application number
HK02103989.5A
Other languages
English (en)
Chinese (zh)
Inventor
B. Chen Barbara
J. Chen Helen
J. Gesicki Glen
A. Haak Richard
W. Malecha James
D. Pfenning Thomas
G. Rico Joseph
E. Rogers Thomas
G. Ruminski Peter
A. Russel Mark
S. Yu Stella
Original Assignee
G.D. 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 G.D. Searle & Co. filed Critical G.D. Searle & Co.
Publication of HK1044527A1 publication Critical patent/HK1044527A1/en

Links

Classifications

    • 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
    • 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
    • C07C279/24—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
    • 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
    • C07C311/15—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
    • 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
    • C07D233/50—Nitrogen atoms not forming part of a nitro radical with carbocyclic radicals directly attached to said nitrogen atoms
    • 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
    • C07D233/54—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
    • 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
    • C07D233/54—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
    • 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
    • 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

Landscapes

  • 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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (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)
  • Peptides Or Proteins (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
HK02103989.5A 1996-03-29 2002-05-28 Para-substituted phenylene derivatives and their use as integrin antagonists HK1044527A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US1428896P 1996-03-29 1996-03-29
US14288P 1996-03-29

Publications (1)

Publication Number Publication Date
HK1044527A1 true HK1044527A1 (en) 2002-10-25

Family

ID=21764580

Family Applications (1)

Application Number Title Priority Date Filing Date
HK02103989.5A HK1044527A1 (en) 1996-03-29 2002-05-28 Para-substituted phenylene derivatives and their use as integrin antagonists

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
NZ318926A (en) * 1995-08-30 1999-04-29 Searle & Co Alpha v beta 3 integrin (vitronectin) inhibitors or anatagonists derived from benzoic acid for treating diseases of cell adhesion
US6245809B1 (en) 1996-12-09 2001-06-12 Cor Therapeutics Inc. Integrin antagonists
DE69720062D1 (de) * 1996-12-09 2003-04-24 Lilly Co Eli Integrin antagonisten
WO1998057173A1 (en) * 1997-06-10 1998-12-17 Eli Lilly And Company Combinatorial process for preparing substituted phenylalanine libraries
RU2220950C2 (ru) * 1997-08-22 2004-01-10 Ф.Хоффманн-Ля Рош Аг N-алканоилфенилаланиновые производные
EP1403247A1 (en) * 1997-08-22 2004-03-31 F.Hoffmann-La Roche Ag N-Alkanoylphenylalanine derivatives
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
US6740682B2 (en) 1997-08-29 2004-05-25 Tularik Limited Meta-benzamidine derivatives as serine protease inhibitors
EP1009758B1 (en) * 1997-08-29 2005-06-01 Tularik Limited Meta-benzamidine derivatives as serine protease inhibitors
CA2303848C (en) 1997-10-31 2008-09-30 Rhone-Poulenc Rorer Limited Substituted anilides
EP1042279B1 (en) * 1997-12-23 2005-03-02 Aventis Pharma Limited Substituted beta-alanines
US6329372B1 (en) 1998-01-27 2001-12-11 Celltech Therapeutics Limited Phenylalanine derivatives
AU3260399A (en) * 1998-02-26 1999-09-15 Celltech Therapeutics Limited Phenylalanine derivatives as inhibitors of alpha4 integrins
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
NZ507222A (en) 1998-04-09 2003-05-30 Meiji Seika Kaisha Aminopiperidine derivatives useful as integrin antagonists
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
JP2002532465A (ja) * 1998-12-16 2002-10-02 バイエル アクチェンゲゼルシャフト インテグリンアンタゴニストとしての新規なビフェニル及びビフェニル−類似化合物
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
JP2002533404A (ja) 1998-12-23 2002-10-08 ジー・ディー・サール・アンド・カンパニー 新生物形成の治療における組合わせ療法としてインテグリン拮抗剤及び放射線治療を使用する方法
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
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
SI1154993T1 (en) * 1999-02-18 2004-12-31 F. Hoffmann-La Roche Ag Thioamide derivatives
YU58601A (sh) * 1999-02-18 2004-05-12 F.Hoffmann-La Roche Ag. Derivati fenilalaninola
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
AU6316900A (en) 1999-08-05 2001-03-05 Meiji Seika Kaisha Ltd. Omega-amino-alpha-hydroxycarboxylic acid derivatives having integrin alphavbeta3antagonism
US6534513B1 (en) 1999-09-29 2003-03-18 Celltech R&D Limited Phenylalkanoic acid derivatives
DE60021521T4 (de) 1999-09-29 2006-09-21 Ortho-Mcneil Pharmaceutical, Inc. Isonipecotamide zur behandlung von integrin vermittelten störungen
AU7961200A (en) * 1999-10-29 2001-05-14 Kaken Pharmaceutical Co., Ltd. Urea derivative, process for producing the same, and medicine containing the urea derivative
AU1733701A (en) 1999-12-16 2001-06-25 Sumitomo Pharmaceuticals Company, Limited Substituted guanidine derivatives
US6455539B2 (en) 1999-12-23 2002-09-24 Celltech R&D Limited Squaric acid derivates
US20030040531A1 (en) * 2000-01-25 2003-02-27 Kazuyuki Fujishima Remedies for reperfusion injury containing integrin alphanubeta 3 antagonist
ES2341843T3 (es) * 2000-02-03 2010-06-29 EISAI R&D MANAGEMENT CO., LTD. Inhibidores de la expresion de integrina.
JP2003531141A (ja) * 2000-04-17 2003-10-21 セルテック アール アンド ディ リミテッド エナミン誘導体
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
EP1301488A1 (en) 2000-07-07 2003-04-16 Celltech R&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
AU2001275724A1 (en) 2000-08-02 2002-02-13 Celltech R&D Limited 3-substituted isoquinolin-1-yl derivatives
WO2002009688A1 (en) * 2000-08-02 2002-02-07 Smithkline Beecham Corporation Fatty acid synthase inhibitors
US7288390B2 (en) 2000-08-07 2007-10-30 Centocor, Inc. Anti-dual integrin antibodies, compositions, methods and uses
US7163681B2 (en) 2000-08-07 2007-01-16 Centocor, Inc. Anti-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
WO2002014272A1 (en) * 2000-08-09 2002-02-21 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.
US6855722B2 (en) 2001-01-29 2005-02-15 Dimensional Pharmaceuticals, 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.
US7081460B2 (en) 2001-04-09 2006-07-25 Ortho-Mcneil Pharmaceutical, Inc. Quinazoline and quinazoline-like compounds for the treatment of integrin-mediated disorders
DK1385823T3 (da) 2001-04-09 2007-03-26 Novartis Vaccines & Diagnostic Guanidinoforbindelser som melanocortin-4-receptor- (MC4-R) -agonister
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
KR20040058229A (ko) 2001-10-22 2004-07-03 더 스크립스 리서치 인스티튜트 항체 표적화 화합물
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
DE60333937D1 (de) * 2002-05-23 2010-10-07 Novartis Vaccines & Diagnostic Substituierte quinazolinone verbindungen
WO2004112793A1 (en) * 2003-05-23 2004-12-29 Chiron Corporation Guanidino-substituted quinazolinone compounds as mc4-r agonists
ES2332135T3 (es) * 2003-06-03 2010-01-27 Novartis Ag Inhibidores p-38 basados en heterociclo de 5 miembros.
AU2004293012A1 (en) * 2003-11-19 2005-06-09 Rustum S. Boyce Quinazolinone compounds with reduced bioaccumulation
CA2630415A1 (en) * 2005-10-20 2007-04-26 The Scripps Research Institute Fc labeling for immunostaining and immunotargeting
WO2007147763A1 (en) 2006-06-20 2007-12-27 F. Hoffmann-La Roche Ag Arylsulfonyl naphthalene derivatives and uses thereof
EP2395992A2 (en) 2009-02-10 2011-12-21 The Scripps Research Institute Chemically programmed vaccination
US20140010783A1 (en) * 2012-07-06 2014-01-09 Hoffmann-La Roche Inc. Antiviral compounds
MX2015000794A (es) 2012-07-18 2015-10-12 Univ Saint Louis Derivados de aminoácido beta como antagonistas de integrina.
US8716226B2 (en) 2012-07-18 2014-05-06 Saint Louis University 3,5 phenyl-substituted beta amino acid derivatives as integrin antagonists
RU2729518C2 (ru) 2015-12-30 2020-08-07 Сент-Луис Юниверсити Мета-азациклические производные аминобензойной кислоты в качестве антагонистов пан-интегрина
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
CA2117282A1 (en) * 1991-11-22 1993-05-27 Ofer Lider Non-peptidic surrogates of the arg-gly-asp sequence and pharmaceutical compositions comprosing them
ES2186720T3 (es) * 1994-05-27 2003-05-16 Merck & Co Inc Composiciones para inhibir la reabsorcion osea mediada por osteoclastos.

Also Published As

Publication number Publication date
US6251944B1 (en) 2001-06-26
PT891325E (pt) 2002-07-31
CA2250698A1 (en) 1997-10-09
JP2000515493A (ja) 2000-11-21
WO1997036859A1 (en) 1997-10-09
DK0891325T3 (da) 2002-05-21
US5952381A (en) 1999-09-14
ES2172780T3 (es) 2002-10-01
DE69710319T2 (de) 2002-08-14
DE69710319D1 (de) 2002-03-21
AU2536097A (en) 1997-10-22
EP0891325B1 (en) 2002-02-06
EP0891325A1 (en) 1999-01-20
ATE212978T1 (de) 2002-02-15

Similar Documents

Publication Publication Date Title
EP0891325B1 (en) Para-substituted phenylpropanoic acid derivatives as integrin antagonists
EP0889877B1 (en) META-SUBSTITUTED PHENYLENE DERIVATIVES AND THEIR USE AS ALPHAvBETA3 INTEGRIN ANTAGONISTS OR INHIBITORS
EP0889875B1 (en) Cyclopropyl alkanoic acid derivatives
EP0889876B1 (en) Meta-substituted phenylene sulphonamide derivatives
EP0894084B1 (en) Cinnamic acid derivatives and their use as integrin antagonists
US6831199B1 (en) Pyrimidine compounds and derivatives thereof
AU3294799A (en) Meta-azacyclic amino benzoic acid compounds and derivatives thereof being integrin antagonists
EP0804418B1 (en) Platelet aggregation inhibitors
US6013651A (en) Meta-azacyclic amino benzoic acid compounds and derivatives thereof
US5639765A (en) Guanidinoalkyl glycine β-amino acids useful for inhibiting bone loss
EP1157985A1 (en) Para- substituted phenylene derivatives and their use as integrin antagonists
HK1021532B (en) Meta-guanidine, urea, thiourea or azacyclic amino benzoic acid derivatives as integrin antagonists
HK1021532A1 (en) Meta-guanidine, urea, thiourea or azacyclic amino benzoic acid derivatives as integrin antagonists
MXPA00008427A (en) Meta-azacyclic amino benzoic acid compounds and derivatives thereof being integrin antagonists