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1. 发明授权

US06353099B1 Substituted ureas as cell adhesion inhibitors 失效
标题翻译：取代尿素作为细胞粘附抑制剂
公开(公告)号：US06353099B1
公开(公告)日：2002-03-05
申请号：US09641408
申请日：2000-08-17
申请人： Stephen E. DeLaszlo , William K. Hagmann , Theodore M. Kamenecka
发明人： Stephen E. DeLaszlo , William K. Hagmann , Theodore M. Kamenecka
IPC分类号： C07D26702
CPC分类号： C07D207/08 , A61K9/0019 , A61K9/008 , A61K9/2054 , A61K9/4858 , C07C275/24 , C07C275/26 , C07C275/28 , C07C275/30 , C07C275/34 , C07C275/42 , C07C2601/14 , C07D207/09 , C07D207/16 , C07D209/02 , C07D211/16 , C07D211/32 , C07D211/34 , C07D211/58 , C07D211/60 , C07D211/64 , C07D215/08 , C07D215/18 , C07D217/06 , C07D221/20 , C07D223/16 , C07D295/215 , C07D307/14 , C07D307/68 , C07D317/58 , C07D471/10
摘要： Compounds of Formula I are antagonists of VLA-4 and/or &agr;4&bgr;7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.
摘要翻译：式I的化合物是VLA-4和/或α4β7的拮抗剂，因此可用于抑制或预防细胞粘附和细胞粘附介导的病理学。这些化合物可以配制成药物组合物，适用于治疗AIDS相关的痴呆，过敏性结膜炎，过敏性鼻炎，阿尔茨海默病，哮喘，动脉粥样硬化，自体骨髓移植，某些类型的毒性和免疫性肾炎，接触皮肤过敏，包括溃疡性结肠炎和克罗恩病的炎性肠病，炎症性肺病，病毒感染的炎症后遗症，脑膜炎，多发性硬化，多发性骨髓瘤，心肌炎，器官移植，牛皮癣，肺纤维化，再狭窄，视网膜炎，类风湿性关节炎，败血症关节炎，中风，肿瘤转移，葡萄膜炎和I型糖尿病。

2. 发明授权

US06734311B2 Substituted amidine derivatives as inhibitors of cell adhesion 失效
标题翻译：取代的脒衍生物作为细胞粘附的抑制剂
公开(公告)号：US06734311B2
公开(公告)日：2004-05-11
申请号：US09862151
申请日：2001-05-21
申请人： William K. Hagmann , Stephen E. DeLaszlo , Theodore Kamenecka , Malcolm MacCoss
发明人： William K. Hagmann , Stephen E. DeLaszlo , Theodore Kamenecka , Malcolm MacCoss
IPC分类号： C07D20704
CPC分类号： C07D207/48 , C07D205/04
摘要： Compounds of Formula I are antagonists of VLA-4 and/or &agr;4&bgr;7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.
摘要翻译：式I的化合物是VLA-4和/或α4β7的拮抗剂，因此可用于抑制或预防细胞粘附和细胞粘附介导的病理学。这些化合物可以配制成药物组合物，适用于治疗AIDS相关的痴呆，过敏性结膜炎，过敏性鼻炎，阿尔茨海默病，哮喘，动脉粥样硬化，自体骨髓移植，某些类型的毒性和免疫性肾炎，接触皮肤过敏，包括溃疡性结肠炎和克罗恩病的炎性肠病，炎症性肺病，病毒感染的炎症后遗症，脑膜炎，多发性硬化，多发性骨髓瘤，心肌炎，器官移植，牛皮癣，肺纤维化，再狭窄，视网膜炎，类风湿性关节炎，败血症关节炎，中风，肿瘤转移，葡萄膜炎和I型糖尿病。

3. 发明授权

US06191171B1 Para-aminomethylaryl carboxamide derivatives 失效
标题翻译：对氨基甲基芳基甲酰胺衍生物
公开(公告)号：US06191171B1
公开(公告)日：2001-02-20
申请号：US09191489
申请日：1998-11-13
申请人： Stephen E. DeLaszlo , William K. Hagmann
发明人： Stephen E. DeLaszlo , William K. Hagmann
IPC分类号： A61K31165
CPC分类号： C07D333/34 , C07C233/87 , C07C275/42 , C07C311/19 , C07C311/29 , C07D233/84
摘要： para-Aminomethylaryl carboxamides of Formula I are antagonists of VLA-4 and/or &agr;4&bgr;7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of asthma, allergies, inflammation, multiple sclerosis, and other inflammatory and autoimmune disorders.
摘要翻译：式I的对氨基甲基芳基甲酰胺是VLA-4和/或α4β7的拮抗剂，因此可用于抑制或预防细胞粘附和细胞粘附介导的病理学。这些化合物可以配制成药物组合物，并且适用于治疗哮喘，过敏，炎症，多发性硬化以及其它炎性和自身免疫性疾病。

4. 发明授权

US6020347A 4-substituted-4-piperidine carboxamide derivatives 失效
标题翻译： 4-取代-4-哌啶甲酰胺衍生物
公开(公告)号：US6020347A
公开(公告)日：2000-02-01
申请号：US191902
申请日：1998-11-13
申请人： Stephen E. DeLaszlo , William K. Hagmann
发明人： Stephen E. DeLaszlo , William K. Hagmann
IPC分类号： C07D211/62 , C07D211/64 , C07D211/96 , A01N43/40 , C07D211/26 , C07D211/30 , C07D211/60
CPC分类号： C07D211/62 , C07D211/64 , C07D211/96
摘要： 4-Substituted-4-piperidinecarboxamides of Formula I are antagonists of VLA-4 and/or .alpha..sub.4 .beta..sub.7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of asthma, allergies, inflammation, multiple sclerosis, and other inflammatory and autoimmune disorders.
摘要翻译：式I的4-取代-4-哌啶甲酰胺是VLA-4和/或α4β7的拮抗剂，因此可用于抑制或预防细胞粘附和细胞粘附介导的病理。这些化合物可以配制成药物组合物，并且适用于治疗哮喘，过敏，炎症，多发性硬化以及其它炎性和自身免疫性疾病。

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