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公开(公告)号：US20070093485A1
公开(公告)日：2007-04-26
申请号：US10527384
申请日：2003-12-18
申请人： Francine Farouz , Michael Dappen , Ying-Zi Xu , Sarah Bartulis , Ryan Holcomb , Ramesh Kasar , Michael Pleiss , Eugene Thorsett , Xiaocong Ye , Andrei Konradi
发明人： Francine Farouz , Michael Dappen , Ying-Zi Xu , Sarah Bartulis , Ryan Holcomb , Ramesh Kasar , Michael Pleiss , Eugene Thorsett , Xiaocong Ye , Andrei Konradi
IPC分类号： A61K31/5377 , A61K31/497 , A61K31/4965 , A61K31/496 , A61K31/4545 , A61K31/454 , A61K31/4439 , A61K31/427 , A61K31/22 , C07D417/02 , C07D403/02
CPC分类号： C07D213/40 , C07C311/21 , C07D207/337 , C07D211/26 , C07D211/34 , C07D213/56 , C07D213/74 , C07D239/26 , C07D243/24 , C07D295/13 , C07D295/185 , C07D401/04 , C07D471/04
摘要： Disclosed are certain substituted N-phenylsulfonamide derivatives and related compounds. These compounds are useful as bradykinin antagonists to relieve adverse symptoms in mammals mediated, at least in part, by bradykinin including pain, inflammation, bronchoconstriction, cerebral edema, etc.
摘要翻译： 公开了某些取代的N-苯基磺酰胺衍生物和相关化合物。 这些化合物可用作缓激肽拮抗剂，以缓解哺乳动物的不良反应，至少部分由缓激肽介导，包括疼痛，炎症，支气管收缩，脑水肿等。
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12.发明申请Polyethylene glycol conjugates of heterocycloalkyl carboxamido propanoic acids 有权杂环烷基甲酰氨基丙酸的聚乙二醇缀合物公开(公告)号：US20050238614A1
公开(公告)日：2005-10-27
申请号：US11042734
申请日：2005-01-24
IPC分类号： A61K31/765 , A61K47/48 , C07D277/06 , C07D295/205 , C07D401/12 , C07D417/12 , C07D417/14 , C08G63/91
CPC分类号： C08G63/91 , A61K47/60 , C07D295/205 , C07D417/12 , C07D417/14
摘要： Disclosed are conjugates which bind VLA-4. Certain of these conjugates also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such conjugates are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The conjugates can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
摘要翻译： 公开了结合VLA-4的缀合物。 这些缀合物中的某些也抑制白细胞粘附，特别是由VLA-4介导的白细胞粘附。 这样的缀合物可用于治疗哺乳动物患者（例如人，例如哮喘，阿尔茨海默氏病，动脉粥样硬化，艾滋病痴呆，糖尿病，炎性肠病，类风湿性关节炎，组织移植，肿瘤转移和心肌缺血）中的炎性疾病。 也可以将缀合物用于治疗炎性脑疾病如多发性硬化症。
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13.发明申请Pyrimidine hydantoin analogues which inhibit leukocyte adhesion mediated by VLA-4 失效抑制VLA-4介导的白细胞粘附的嘧啶乙内酰脲类似物公开(公告)号：US20050261324A1
公开(公告)日：2005-11-24
申请号：US11118862
申请日：2005-04-29
IPC分类号： A61K31/506 , C07D403/00 , C07D403/10 , C07D403/12 , C07D405/14 , C07D487/04 , C07D43/02
CPC分类号： C07D487/04 , C07D403/10 , C07D403/12 , C07D405/14
摘要： Disclosed are compounds which bind VLA-4 and/or LPAM-1. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4 and/or LPAM-1. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
摘要翻译： 公开了结合VLA-4和/或LPAM-1的化合物。 这些化合物中的某些也抑制白细胞粘附，特别是由VLA-4和/或LPAM-1介导的白细胞粘附。 这样的化合物可用于治疗哺乳动物患者，例如人类例如哮喘，阿尔茨海默氏病，动脉粥样硬化，艾滋病痴呆，糖尿病，炎性肠病，类风湿性关节炎，组织移植，肿瘤转移和心肌缺血等炎性疾病。 化合物也可以用于治疗炎性脑疾病如多发性硬化症。
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公开(公告)号：US20060013799A1
公开(公告)日：2006-01-19
申请号：US11177748
申请日：2005-07-08
IPC分类号： A61K31/785
CPC分类号： A61K45/06 , A61K31/785 , A61K47/60 , A61Q5/00
摘要： Disclosed are conjugates which bind VLA-4. Certain of these conjugates also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such conjugates are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The conjugates can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
摘要翻译： 公开了结合VLA-4的缀合物。 这些缀合物中的某些也抑制白细胞粘附，特别是由VLA-4介导的白细胞粘附。 这样的缀合物可用于治疗哺乳动物患者（例如人，例如哮喘，阿尔茨海默氏病，动脉粥样硬化，艾滋病痴呆，糖尿病，炎性肠病，类风湿性关节炎，组织移植，肿瘤转移和心肌缺血）中的炎性疾病。 也可以将缀合物用于治疗炎性脑疾病如多发性硬化症。
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公开(公告)号：US20060074110A1
公开(公告)日：2006-04-06
申请号：US11285889
申请日：2005-11-22
IPC分类号： A61K31/455 , A61K31/401 , C07C237/24 , A61K31/215
CPC分类号： C07C233/84 , C07C233/63 , C07C233/85 , C07C233/87 , C07C237/22 , C07C255/60 , C07C271/22 , C07C271/34 , C07C271/42 , C07C271/44 , C07C275/16 , C07C275/18 , C07C275/20 , C07C275/24 , C07C2601/14 , C07C2603/74 , C07D213/55 , C07D213/64 , C07D213/80 , C07D213/89 , C07D239/52 , C07D239/54 , C07D261/08 , C07D277/48 , C07D295/15 , C07D295/205 , C07D453/02
摘要： Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
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公开(公告)号：US20060293332A1
公开(公告)日：2006-12-28
申请号：US11429656
申请日：2006-05-05
申请人： Francine Grant , Sarah Bartulis , Louis Brogley , Michael Dappen , Ramesh Kasar , Mohammed Khan , Martin Neitzel , Michael Pleiss , Eugene Thorsett , John Tucker , Michael Ye , Jon Hawkinson
发明人： Francine Grant , Sarah Bartulis , Louis Brogley , Michael Dappen , Ramesh Kasar , Mohammed Khan , Martin Neitzel , Michael Pleiss , Eugene Thorsett , John Tucker , Michael Ye , Jon Hawkinson
IPC分类号： A61K31/498 , C07D241/36
CPC分类号： C07D401/14 , C07D241/44 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： Disclosed are sulfonylquinoxalone acetamide derivatives useful as bradykinin antagonists.
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17.发明申请4-Bromo-5-(2-chloro-benzoylamino)-1h-pyrazole-3-carboxylic acid (phenyl) amide derivatives and related compounds as bradykinin b1 receptor antagonists for the treatment of inflammatory diseases 审中-公开4-溴-5-（2-氯 - 苯甲酰基氨基）-1 - 吡唑-3-羧酸（苯基）酰胺衍生物和相关化合物作为缓激肽b1受体拮抗剂，用于治疗炎性疾病公开(公告)号：US20070123531A1
公开(公告)日：2007-05-31
申请号：US10555508
申请日：2004-04-30
申请人： Albert Garofalo , Jay Tung , Michael Pleiss , Jing Wu , David Wone , Ashley Guinn , Darren Dressen , Jennifer Marugg , Martin Neitzel
发明人： Albert Garofalo , Jay Tung , Michael Pleiss , Jing Wu , David Wone , Ashley Guinn , Darren Dressen , Jennifer Marugg , Martin Neitzel
IPC分类号： A61K31/5377 , A61K31/4709 , A61K31/4439 , A61K31/416 , A61K31/4178 , A61K31/427 , A61K31/423 , C07D413/02 , C07D417/02 , C07D405/02 , C07D403/02
CPC分类号： C07D401/12 , C07D231/16 , C07D231/40 , C07D403/12 , C07D417/12
摘要： Disclosed are compounds that are bradykinin B1 receptor antagonists and are useful for treating diseases, or relieving adverse symptoms associated with disease conditions, in mammals mediated by bradykinin B1 receptor. Certain of the compounds exhibit increased potency and are also expected to exhibit increased duration of action.
摘要翻译： 公开了缓激肽B1受体拮抗剂的化合物，可用于治疗由缓激肽B1受体介导的哺乳动物中疾病或与疾病状况相关的不良症状。 某些化合物表现出增加的效力，并且还预期表现出增加的作用持续时间。
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18.发明申请4-Bromo-5-(2-chloro-benzoylamino)-1h-pyrazole-3-carboxylic acid (1-aminocarbonyl)eth-1-yl) amide derivatives and related compounds as bradykinin b1 receptor antagonists for the treatment of inflammatory diseases 审中-公开4-溴-5-（2-氯 - 苯甲酰基氨基）-1 - 吡唑-3-羧酸（1-氨基羰基）乙-1-基）酰胺衍生物和相关化合物作为缓激肽b1受体拮抗剂，用于治疗炎性疾病公开(公告)号：US20070161633A1
公开(公告)日：2007-07-12
申请号：US10555515
申请日：2004-04-30
申请人： Jay Tung , Albert Garofalo , Michael Pleiss , Jing Wu , David Wone , Ashley Guinn , Darren Dressen , Jennifer Marugg , Martin Neitzel
发明人： Jay Tung , Albert Garofalo , Michael Pleiss , Jing Wu , David Wone , Ashley Guinn , Darren Dressen , Jennifer Marugg , Martin Neitzel
IPC分类号： A61K31/5377 , A61K31/496 , A61K31/454 , A61K31/4152 , C07D413/02 , C07D403/02
CPC分类号： C07D401/14 , C07D231/16 , C07D231/40 , C07D401/12 , C07D403/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D453/02 , C07D471/04 , C07D471/08 , C07D487/08
摘要： Disclosed are compounds of formulae (I) and (II) that are bradykinin B1 receptor antagonists and are useful for treating diseases, or relieving adverse symptoms associated with disease conditions, in mammals mediated by bradykinin B1 receptor. Certain of the compounds exhibit increased potency and are also expected to exhibit increased duration of action. Wherein Z is selected from O, S and NH; Q of formula (III) and the other substituents are as defined in claim 1.
摘要翻译： 公开了缓激肽B 1受体拮抗剂的式（I）和（II）化合物，并且可用于治疗由缓激肽B介导的哺乳动物中的疾病或减轻与疾病相关的不良症状B 1 受体。 某些化合物表现出增加的效力，并且还预期表现出增加的作用持续时间。 其中Z选自O，S和NH; 式（III）的Q和其它取代基如权利要求1中所定义。
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19.发明申请Substituted pyrazole derivatives and related compounds as bradykinin B1 receptor antagonists 审中-公开取代的吡唑衍生物和相关化合物作为缓激肽B1受体拮抗剂公开(公告)号：US20050038099A1
公开(公告)日：2005-02-17
申请号：US10836929
申请日：2004-04-30
申请人： Jay Tung , Albert Garofalo , Michael Pleiss , Jing Wu , David Wone , Ashley Guinn , Darren Dressen , Jennifer Marugg , Martin Neitzel
发明人： Jay Tung , Albert Garofalo , Michael Pleiss , Jing Wu , David Wone , Ashley Guinn , Darren Dressen , Jennifer Marugg , Martin Neitzel
IPC分类号： A61P29/00 , C07D231/16 , C07D231/40 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D453/02 , C07D471/04 , C07D471/08 , C07D487/08 , A61K31/416 , A61K31/4152
CPC分类号： C07D401/14 , C07D231/16 , C07D231/40 , C07D401/12 , C07D403/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D453/02 , C07D471/04 , C07D471/08 , C07D487/08
摘要： Disclosed are compounds that are bradykinin B1 receptor antagonists and are useful for treating diseases, or relieving adverse symptoms associated with disease conditions, in mammals mediated by bradykinin B1 receptor. Certain of the compounds exhibit increased potency and are also expected to exhibit increased duration of action.
摘要翻译： 公开了缓激肽B1受体拮抗剂的化合物，可用于治疗由缓激肽B1受体介导的哺乳动物中疾病或与疾病状况相关的不良症状。 某些化合物表现出增加的效力，并且还预期表现出增加的作用持续时间。
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20.发明申请Selected substituted pyrazole derivatives and related compounds as bradykinin B1 receptor antagonists 审中-公开所选取代的吡唑衍生物和相关化合物作为缓激肽B1受体拮抗剂公开(公告)号：US20050032868A1
公开(公告)日：2005-02-10
申请号：US10836903
申请日：2004-04-30
申请人： Albert Garofalo , Jay Tung , Michael Pleiss , Jing Wu , David Wone , Ashley Guinn , Darren Dressen , Jennifer Marugg , Martin Neitzel
发明人： Albert Garofalo , Jay Tung , Michael Pleiss , Jing Wu , David Wone , Ashley Guinn , Darren Dressen , Jennifer Marugg , Martin Neitzel
IPC分类号： A61K31/4152 , A61K31/416 , C07D231/16 , C07D231/40 , C07D401/12 , C07D403/12 , C07D417/12 , C07D43/02
CPC分类号： C07D401/12 , C07D231/16 , C07D231/40 , C07D403/12 , C07D417/12
摘要： Disclosed are compounds that are bradykinin B1 receptor antagonists and are useful for treating diseases, or relieving adverse symptoms associated with disease conditions, in mammals mediated by bradykinin B1 receptor. Certain of the compounds exhibit increased potency and are also expected to exhibit increased duration of action.
摘要翻译： 公开了缓激肽B1受体拮抗剂的化合物，可用于治疗由缓激肽B1受体介导的哺乳动物中疾病或与疾病状况相关的不良症状。 某些化合物表现出增加的效力，并且还预期表现出增加的作用持续时间。
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