JP2002536438A5 - - Google Patents
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- Publication number
- JP2002536438A5 JP2002536438A5 JP2000598485A JP2000598485A JP2002536438A5 JP 2002536438 A5 JP2002536438 A5 JP 2002536438A5 JP 2000598485 A JP2000598485 A JP 2000598485A JP 2000598485 A JP2000598485 A JP 2000598485A JP 2002536438 A5 JP2002536438 A5 JP 2002536438A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- residue
- aryl
- cycloalkyl
- alkoxy
- 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.)
- Granted
Links
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 description 9
- 150000001875 compounds Chemical class 0.000 description 9
- 125000000217 alkyl group Chemical group 0.000 description 8
- 125000005915 C6-C14 aryl group Chemical group 0.000 description 7
- 125000003118 aryl group Chemical group 0.000 description 7
- 125000000753 cycloalkyl group Chemical group 0.000 description 7
- 229910052736 halogen Inorganic materials 0.000 description 7
- 150000002367 halogens Chemical class 0.000 description 7
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 7
- 150000003839 salts Chemical class 0.000 description 7
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 description 6
- 125000006652 (C3-C12) cycloalkyl group Chemical group 0.000 description 6
- -1 (C 1 -C 8 ) -alkoxy Chemical group 0.000 description 5
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 description 5
- 229910052739 hydrogen Inorganic materials 0.000 description 5
- 239000001257 hydrogen Substances 0.000 description 5
- 239000000203 mixture Substances 0.000 description 5
- 125000001072 heteroaryl group Chemical group 0.000 description 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 4
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 description 3
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 description 3
- 125000001140 1,4-phenylene group Chemical group [H]C1=C([H])C([*:2])=C([H])C([H])=C1[*:1] 0.000 description 3
- 125000003545 alkoxy group Chemical group 0.000 description 3
- 150000002431 hydrogen Chemical class 0.000 description 3
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 description 2
- 206010003210 Arteriosclerosis Diseases 0.000 description 2
- 208000006386 Bone Resorption Diseases 0.000 description 2
- 208000024172 Cardiovascular disease Diseases 0.000 description 2
- ZRALSGWEFCBTJO-UHFFFAOYSA-N Guanidine Chemical compound NC(N)=N ZRALSGWEFCBTJO-UHFFFAOYSA-N 0.000 description 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 2
- 102100022337 Integrin alpha-V Human genes 0.000 description 2
- 208000001132 Osteoporosis Diseases 0.000 description 2
- 208000017442 Retinal disease Diseases 0.000 description 2
- 206010038923 Retinopathy Diseases 0.000 description 2
- 108010048673 Vitronectin Receptors Proteins 0.000 description 2
- 230000003042 antagnostic effect Effects 0.000 description 2
- 230000003110 anti-inflammatory effect Effects 0.000 description 2
- 208000011775 arteriosclerosis disease Diseases 0.000 description 2
- 230000024279 bone resorption Effects 0.000 description 2
- 150000001732 carboxylic acid derivatives Chemical class 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 2
- 239000003937 drug carrier Substances 0.000 description 2
- 230000002401 inhibitory effect Effects 0.000 description 2
- 208000017169 kidney disease Diseases 0.000 description 2
- 125000002950 monocyclic group Chemical group 0.000 description 2
- 125000004043 oxo group Chemical group O=* 0.000 description 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 2
- 208000037803 restenosis Diseases 0.000 description 2
- 206010039073 rheumatoid arthritis Diseases 0.000 description 2
- 229910052717 sulfur Inorganic materials 0.000 description 2
- 125000003837 (C1-C20) alkyl group Chemical group 0.000 description 1
- IXYNDHRYWPYGLR-UHFFFAOYSA-N CC1=CC=C(C=C1)S(=O)(=O)NC2=C(C=CC3=C2C(=C(C(=C3NS(=O)(=O)C4=CC=CC5=CC=CC=C54)NS(=O)(=O)C6=CC=C(C=C6)C(F)(F)F)NS(=O)(=O)C7=CC=C(C=C7)Br)NS(=O)(=O)C8=CC=C(C=C8)Cl)NS(=O)(=O)C9=CC=CC=C9 Chemical compound CC1=CC=C(C=C1)S(=O)(=O)NC2=C(C=CC3=C2C(=C(C(=C3NS(=O)(=O)C4=CC=CC5=CC=CC=C54)NS(=O)(=O)C6=CC=C(C=C6)C(F)(F)F)NS(=O)(=O)C7=CC=C(C=C7)Br)NS(=O)(=O)C8=CC=C(C=C8)Cl)NS(=O)(=O)C9=CC=CC=C9 IXYNDHRYWPYGLR-UHFFFAOYSA-N 0.000 description 1
- CHJJGSNFBQVOTG-UHFFFAOYSA-N N-methyl-guanidine Natural products CNC(N)=N CHJJGSNFBQVOTG-UHFFFAOYSA-N 0.000 description 1
- 125000000539 amino acid group Chemical group 0.000 description 1
- 125000003277 amino group Chemical group 0.000 description 1
- 150000001450 anions Chemical class 0.000 description 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 1
- SWSQBOPZIKWTGO-UHFFFAOYSA-N dimethylaminoamidine Natural products CN(C)C(N)=N SWSQBOPZIKWTGO-UHFFFAOYSA-N 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 125000000524 functional group Chemical group 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 125000000896 monocarboxylic acid group Chemical group 0.000 description 1
- 125000004433 nitrogen atom Chemical group N* 0.000 description 1
- 238000010534 nucleophilic substitution reaction Methods 0.000 description 1
- 229910052760 oxygen Inorganic materials 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 239000002243 precursor Substances 0.000 description 1
- 125000001424 substituent group Chemical group 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP99102916A EP1028114A1 (en) | 1999-02-13 | 1999-02-13 | Novel guanidine derivatives as inhibitors of cell adhesion |
| EP99102916.6 | 1999-02-13 | ||
| PCT/EP2000/000895 WO2000047564A1 (en) | 1999-02-13 | 2000-02-04 | Novel guanidine derivatives as inhibitors of cell adhesion |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2002536438A JP2002536438A (ja) | 2002-10-29 |
| JP2002536438A5 true JP2002536438A5 (https=) | 2007-01-11 |
| JP4642242B2 JP4642242B2 (ja) | 2011-03-02 |
Family
ID=8237555
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2000598485A Expired - Lifetime JP4642242B2 (ja) | 1999-02-13 | 2000-02-04 | 細胞接着の阻害剤としての新規のグアニジン誘導体 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US6340679B1 (https=) |
| EP (2) | EP1028114A1 (https=) |
| JP (1) | JP4642242B2 (https=) |
| AT (1) | ATE273285T1 (https=) |
| AU (1) | AU768206B2 (https=) |
| CA (1) | CA2371789C (https=) |
| DE (1) | DE60012890T2 (https=) |
| ES (1) | ES2225086T3 (https=) |
| IL (1) | IL144725A0 (https=) |
| MX (1) | MXPA01008072A (https=) |
| WO (1) | WO2000047564A1 (https=) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE19629816A1 (de) * | 1996-07-24 | 1998-01-29 | Hoechst Ag | Neue Cycloalkyl-Derivate als Inhibitoren der Knochenresorption und Vitronectinrezeptor-Antagonisten |
| US6972296B2 (en) | 1999-05-07 | 2005-12-06 | Encysive Pharmaceuticals Inc. | Carboxylic acid derivatives that inhibit the binding of integrins to their receptors |
| GEP20053477B (en) | 1999-08-13 | 2005-03-25 | Biogen Inc | Cell Adhesion Inhibitors and Pharmaceutical Compositions Containing Them |
| EP1443963B1 (en) | 2001-10-22 | 2014-05-21 | The Scripps Research Institute | Antibody targeting compounds |
| AU2004287875B2 (en) * | 2003-11-05 | 2011-06-02 | Bausch + Lomb Ireland Limited | Modulators of cellular adhesion |
| US7196112B2 (en) | 2004-07-16 | 2007-03-27 | Biogen Idec Ma Inc. | Cell adhesion inhibitors |
| DK2444079T3 (en) | 2005-05-17 | 2017-01-30 | Sarcode Bioscience Inc | Compositions and Methods for the Treatment of Eye Diseases |
| WO2007048127A2 (en) * | 2005-10-20 | 2007-04-26 | The Scripps Research Institute | Fc labeling for immunostaining and immunotargeting |
| ES2630406T3 (es) * | 2007-10-19 | 2017-08-21 | Sarcode Bioscience Inc. | Composición y procedimientos para el tratamiento de la retinopatía diabética |
| US8080562B2 (en) | 2008-04-15 | 2011-12-20 | Sarcode Bioscience Inc. | Crystalline pharmaceutical and methods of preparation and use thereof |
| EP2276508A4 (en) * | 2008-04-15 | 2011-12-28 | Sarcode Bioscience Inc | ADMINISTRATION OF LFA-1 ANTAGONISTS TO THE GASTROINTESTINAL SYSTEM |
| WO2009128934A1 (en) * | 2008-04-15 | 2009-10-22 | Sarcode Corporation | Topical lfa-1 antagonists for use in localized treatment of immune related disorders |
| EP2265124A4 (en) * | 2008-04-15 | 2011-12-28 | Sarcode Bioscience Inc | AEROSOLISED LFA-1 ANTAGONISTS FOR THE USE IN THE LOCAL TREATMENT OF IMMUNE DISEASES |
| EP2395992A2 (en) | 2009-02-10 | 2011-12-21 | The Scripps Research Institute | Chemically programmed vaccination |
| US8378105B2 (en) * | 2009-10-21 | 2013-02-19 | Sarcode Bioscience Inc. | Crystalline pharmaceutical and methods of preparation and use thereof |
| CA2879982C (en) | 2012-07-25 | 2020-09-01 | Sarcode Bioscience Inc. | Lfa-1 inhibitor and polymorph thereof |
Family Cites Families (14)
| 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 |
| US5250679A (en) | 1991-10-18 | 1993-10-05 | Genentech, Inc. | Nonpeptidyl platelet aggregation inhibitors having specificity for the GPIIb III.sub. receptor |
| 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 |
| JPH10501222A (ja) | 1994-05-27 | 1998-02-03 | メルク エンド カンパニー インコーポレーテッド | 破骨細胞仲介骨吸収を抑制するための化合物 |
| EP0767792A4 (en) | 1994-06-29 | 2002-11-20 | Smithkline Beecham Corp | VITRONECTIN RECEPTOR ANTAGONISTS |
| EP0762882A4 (en) | 1994-06-29 | 2002-09-11 | Smithkline Beecham Corp | Vibronectin Receptor Antagonists |
| HUP9802675A3 (en) | 1995-08-14 | 2000-09-28 | Scripps Research Inst | Methods and compositions useful for inhibition of alfa-v beta-5 mediated angiogenesis |
| DE19548709A1 (de) * | 1995-12-23 | 1997-07-03 | Merck Patent Gmbh | Tyrosinderivate |
| KR20000022190A (ko) * | 1996-06-28 | 2000-04-25 | 플레믹 크리스티안 | 인테그린 저해제로서의 페닐알라닌 유도체 |
| DE19629816A1 (de) * | 1996-07-24 | 1998-01-29 | Hoechst Ag | Neue Cycloalkyl-Derivate als Inhibitoren der Knochenresorption und Vitronectinrezeptor-Antagonisten |
| EP0933367A1 (en) | 1997-12-19 | 1999-08-04 | Hoechst Marion Roussel Deutschland GmbH | Novel acylguanidine derivates as inhibitors of bone resorption and as vitronectin receptor antagonists |
| IL137423A0 (en) | 1998-01-23 | 2001-07-24 | Aventis Pharma Gmbh | Novel sulfonamide derivatives as inhibitors of bone resorption and as inhibitors of cell adhesion |
-
1999
- 1999-02-13 EP EP99102916A patent/EP1028114A1/en not_active Withdrawn
-
2000
- 2000-02-04 AU AU26699/00A patent/AU768206B2/en not_active Ceased
- 2000-02-04 MX MXPA01008072A patent/MXPA01008072A/es not_active IP Right Cessation
- 2000-02-04 CA CA002371789A patent/CA2371789C/en not_active Expired - Lifetime
- 2000-02-04 DE DE60012890T patent/DE60012890T2/de not_active Expired - Lifetime
- 2000-02-04 AT AT00905022T patent/ATE273285T1/de not_active IP Right Cessation
- 2000-02-04 ES ES00905022T patent/ES2225086T3/es not_active Expired - Lifetime
- 2000-02-04 IL IL14472500A patent/IL144725A0/xx unknown
- 2000-02-04 JP JP2000598485A patent/JP4642242B2/ja not_active Expired - Lifetime
- 2000-02-04 WO PCT/EP2000/000895 patent/WO2000047564A1/en not_active Ceased
- 2000-02-04 EP EP00905022A patent/EP1155003B1/en not_active Expired - Lifetime
- 2000-02-11 US US09/502,577 patent/US6340679B1/en not_active Expired - Lifetime
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