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70 条记录 (耗时 0.061 秒)

    SUBSTITUTED ESTERS AS CANNABINOID-1 RECEPTOR MODULATORS
    51.
    发明申请
    SUBSTITUTED ESTERS AS CANNABINOID-1 RECEPTOR MODULATORS 审中-公开
    作为CANNABINOID-1受体调节剂的替代品

    公开(公告)号：US20090137529A1

    公开(公告)日：2009-05-28

    申请号：US12226934

    申请日：2007-05-11

    申请人： William K. Hagmann ,  Milton L. Hammond

    发明人： William K. Hagmann ,  Milton L. Hammond

    IPC分类号： A61K31/675 ,  C07D211/72 ,  A61K31/44 ,  C07F9/06

    CPC分类号： C07D213/64

    摘要： The compounds of the present invention are prodrugs of modulators of the Cannabinoid-1 (CB 1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the Cannabinoid-1 (CB 1) receptor. In particular, compounds of the present invention are 5 prodrugs of antagonists or inverse agonists of the CB 1 receptor. The invention is concerned with the use of these compounds to be converted to compounds that modulate the Cannabinoid-1 (CB 1) receptor. As such, the compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer's disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-10 Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia.

    摘要翻译： 本发明的化合物是大麻素-1（CB 1）受体的调节剂的前药，可用于治疗，预防和抑制由大麻素-1（CB 1）受体介导的疾病。 特别地，本发明的化合物是CB 1受体的5种前药拮抗剂或反向激动剂。 本发明涉及将这些化合物转化为调节大麻素-1（CB 1）受体的化合物的用途。 因此，本发明的化合物可用作治疗精神病，记忆缺陷，认知障碍，阿尔茨海默氏病，偏头痛，神经病，包括多发性硬化症和神经炎症性障碍的神经炎症症状和Guillain-10 Barre综合征和炎性反应的中枢作用药物 病毒性脑炎，脑血管意外，头部创伤，焦虑障碍，压力，癫痫，帕金森病，运动障碍和精神分裂症的后遗症。

    Substituted nipecotyl derivatives as inhibitors of cell adhesion
    52.
    发明授权
    Substituted nipecotyl derivatives as inhibitors of cell adhesion 失效
    取代的nipecotyl衍生物作为细胞粘附的抑制剂

    公开(公告)号：US06403584B1

    公开(公告)日：2002-06-11

    申请号：US09882319

    申请日：2001-06-15

    申请人： Stephen E. de Laszlo ,  Clare E. Gutteridge ,  William K. Hagmann ,  Theodore M. Kamenecka

    发明人： Stephen E. de Laszlo ,  Clare E. Gutteridge ,  William K. Hagmann ,  Theodore M. Kamenecka

    IPC分类号： C07D21112

    CPC分类号： C07D401/12 ,  C07D211/60 ,  C07D417/12

    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。

    Para-aminomethylaryl carboxamide derivatives
    55.
    发明授权
    Para-aminomethylaryl carboxamide derivatives 失效
    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-substituted-4-piperidine carboxamide derivatives
    56.
    发明授权
    4-substituted-4-piperidine carboxamide derivatives 失效
    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。

    Preparation of carboxyalkyl derivatives as inhibitors of matrix metalloproteinases
    57.
    发明授权
    Preparation of carboxyalkyl derivatives as inhibitors of matrix metalloproteinases 失效
    羧基烷基衍生物作为基质金属蛋白酶抑制剂的制备

    公开(公告)号：US5684152A

    公开(公告)日：1997-11-04

    申请号：US716042

    申请日：1996-09-19

    申请人： Mitree M. Ponpipom ,  William K. Hagmann

    发明人： Mitree M. Ponpipom ,  William K. Hagmann

    IPC分类号： C07C231/18 ,  C07C237/22 ,  C07C39/225 ,  C07D207/00 ,  C07D209/02 ,  C07D263/04 ,  C07D277/04 ,  C07D279/00 ,  C07D307/00 ,  C07D413/08

    CPC分类号： C07C231/18 ,  C07C237/22

    摘要： Carboxy-peptidyl compounds of Formula I are found to be useful inhibitors of matrix metalloendoproteinase-mediated diseases including osteoarthritis, rheumatoid arthritis, septic arthritis, tumor invasion in certain cancers, periodontal disease, corneal ulceration, proteinuria, dystrophobic epidermolysis bullosa, coronary thrombosis associated with atherosclerotic plaque rupture, and aneurysmal aortic disease. This invention relates to a process of making the carboxy-peptidyl compounds of formula I. ##STR1##

    摘要翻译： 发现式I的羧基肽基化合物是有用的基质金属蛋白酶介导的疾病的抑制剂，包括骨关节炎，类风湿性关节炎，脓毒性关节炎，某些癌症中的肿瘤侵袭，牙周病，角膜溃疡，蛋白尿，疏水性表皮松解性大疱性肿瘤，冠状动脉血栓形成相关 动脉粥样硬化斑块破裂和动脉瘤性主动脉疾病。 本发明涉及制备式I的羧基肽基化合物的方法

    Substituted amidine derivatives as inhibitors of cell adhesion
    60.
    发明授权
    Substituted amidine derivatives as inhibitors of cell adhesion 失效
    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。