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1. 发明申请

WO2004082637A3 COMBINATION OF AN ALDOSTERONE RECEPTOR ANTAGONIST AND AN ENDOTHELIN RECEPTOR ANTAGONIST AND/OR ENDOTHELIN CONVERTING ENZYME INHIBITOR 审中-公开
标题翻译：阿托品酮受体拮抗剂和内皮素受体拮抗剂和/或内皮素转化酶抑制剂的组合
公开(公告)号：WO2004082637A3
公开(公告)日：2007-05-10
申请号：PCT/US2004008250
申请日：2004-03-18
申请人： PHARMACIA CORP , MCMAHON ELLEN G , RUDOLPH AMY E
发明人： MCMAHON ELLEN G , RUDOLPH AMY E
IPC分类号： A61K31/56 , A61K31/41 , A61K31/415 , A61K31/55 , A61K45/06
CPC分类号： A61K45/06 , A61K31/56 , A61K2300/00
摘要： Novel combinations, compositions, and therapeutic methods of treatment and/or prophylaxis of a hypertension, cardiovascular disease, renal dysfunction, edema, cerebrovascular disease, or insulinopathy pathological conditions in a subject, wherein the methods comprise the administration of a combination of one or more aldosterone receptor antagonists and one or more endothelin receptor antagonist and/or ECE inhibitors selected from a specific group of compounds described herein.
摘要翻译：用于治疗和/或预防受试者的高血压，心血管疾病，肾功能障碍，水肿，脑血管疾病或胰岛素病变病症的新型组合，组合物和治疗方法，其中所述方法包括施用一种或多种醛固酮受体拮抗剂和选自本文所述的特定化合物组的一种或多种内皮素受体拮抗剂和/或ECE抑制剂。

2. 发明申请

WO2003068153A2 CARDIAC-SPECIFIC 11β HYDROXYSTEROID DEHYDROGENASE TYPE 2 TRANSGENIC MICE 审中-公开
标题翻译： CARDIAC-SPECIFIC 11beta羟虫类脱氢酶2型转基因小鼠
公开(公告)号：WO2003068153A2
公开(公告)日：2003-08-21
申请号：PCT/US2003/004054
申请日：2003-02-12
申请人： PHARMACIA CORPORATION , MCMAHON, Ellen, G. , WENNING, Qin , GOELLNER, Joseph , RUDOLPH, Amy, E.
发明人： MCMAHON, Ellen, G. , WENNING, Qin , GOELLNER, Joseph , RUDOLPH, Amy, E.
IPC分类号： A61K
CPC分类号： C12N9/0006
摘要： Five independent transgenic founder lines were created which have all developed cardiac hypertrophy and heart failure. The line with the most severe phenotype was analyzed in detail. Transgenic cardiac 11β3HSD2 mRNA expression is increased 4,000 fold over non-transgenic mice and the expressed enzyme was found to possess catalytic activity. At five months of age transgenic mice had developed severe myocardial hypertrophy in the absence of an increase in blood pressure. Interstitial fibrosis in the left ventricle of transgenic mice was revealed by picrosirius red staining. The hearts of the mice were severely dilated and cardiomyocyte size was increased.
摘要翻译：创建了五个独立的转基因创始人系，其中全部发展为心脏肥大和心力衰竭。详细分析了最严重表型的行。转基因心脏11beta3HSD2 mRNA表达比非转基因小鼠增加了4000倍，发现表达的酶具有催化活性。在五个月龄时，转基因小鼠在没有血压升高的情况下发展为严重的心肌肥大。转染小鼠左心室间质纤维化通过微血管红染色显示。小鼠心脏严重扩张，心肌细胞数量增加。

3. 发明申请

WO2004075857A3 COMPOSITIONS, COMBINATIONS, AND METHODS FOR TREATING CARDIOVASCULAR CONDITIONS AND OTHER ASSOCIATED CONDITIONS 审中-公开
标题翻译：用于治疗心血管病和其他相关条件的组合物，组合和方法
公开(公告)号：WO2004075857A3
公开(公告)日：2005-08-18
申请号：PCT/US2004005799
申请日：2004-02-26
申请人： PHARMACIA CORP , RUDOLPH AMY E , ROCHA RICARDO
发明人： RUDOLPH AMY E , ROCHA RICARDO
IPC分类号： A61K31/415 , A61K31/56 , A61K45/06 , A61K31/675 , A61K31/497 , A61K31/505 , A61K31/535
CPC分类号： A61K45/06
摘要： This invention is directed generally to a method for treating a pathological condition (particularly a cardiovascular condition (e.g., hypertension or heart failure) or a condition associated with a cardiovascular condition) using a p38-kinase inhibitor (e.g., a p38-kinase-inhibiting substituted pyrazole), and specifically a combination comprising a p38-kinase inhibitor with an aldosterone antagonist or diuretic for treating a cardiovascular condition. This invention also is directed generally to combinations comprising a p38-kinase inhibitor, and specifically to combinations comprising a p38-kinase inhibitor with an aldosterone antagonist or diuretic. This invention is further directed generally to pharmaceutical compositions comprising a p38-kinase inhibitor, and more specifically to compositions comprising the above-described combinations.
摘要翻译：本发明一般涉及使用p38-激酶抑制剂（例如，p38-激酶抑制剂）治疗病理状况（特别是心血管病症（例如高血压或心力衰竭）或与心血管疾病相关的病症）的方法取代的吡唑），特别是包含p38-激酶抑制剂与醛固酮拮抗剂或利尿剂治疗心血管病症的组合。本发明还通常涉及包含p38-激酶抑制剂的组合，特别涉及包含p38-激酶抑制剂与醛固酮拮抗剂或利尿剂的组合。本发明进一步涉及包含p38-激酶抑制剂的药物组合物，更具体地涉及包含上述组合的组合物。

4. 发明申请

WO2004100871A2 COMBINATION OF AN ALDOSTERONE RECEPTOR ANTAGONIST AND A RENIN INHIBITOR 审中-公开
标题翻译： ALDOSTERONE受体拮抗剂和RININ抑制剂的组合
公开(公告)号：WO2004100871A2
公开(公告)日：2004-11-25
申请号：PCT/US2004/013673
申请日：2004-04-29
申请人： PHARMACIA CORPORATION , MCMAHON, Ellen, G. , RUDOLPH, Amy, E.
发明人： MCMAHON, Ellen, G. , RUDOLPH, Amy, E.
IPC分类号： A61K
CPC分类号： A61K45/06
摘要： Novel combinations, compositions, and therapeutic methods of treatment of a hypertension, cardiovascular disease, renal dysfunction, edema, cerebrovascular disease, or insulinopathy pathological condition in a subject, wherein the methods comprise the administration of a combination of one or more aldosterone receptor antagonists and one or more renin inhibitors.
摘要翻译：治疗受试者中的高血压，心血管疾病，肾功能障碍，水肿，脑血管疾病或胰岛素病变病症的新型组合，组合物和治疗方法，其中所述方法包括施用一种或多种醛固酮受体拮抗剂和一种或多种肾素抑制剂。

5. 发明申请

WO2004082636A3 COMBINATION OF AN ALDOSTERONE RECEPTOR ANTAGONIST AND A NEUTRAL ENDOPEPTIDASE INHIBITOR 审中-公开
公开(公告)号：WO2004082636A3
公开(公告)日：2004-09-30
申请号：PCT/US2004/008220
申请日：2004-03-18
申请人： PHARMACIA CORPORATION , MCMAHON, Ellen, G. , RUDOLPH, Amy, E.
发明人： MCMAHON, Ellen, G. , RUDOLPH, Amy, E.
IPC分类号： A61K31/55
摘要： Novel combinations, compositions, and therapeutic methods of treatment and/or prophylaxis of a hypertension, cardiovascular disease, renal dysfunction, edema, cerebrovascular disease, or insulinopathy pathological condition in a subject, wherein the methods comprise the administration of a combination of one or more aldosterone receptor antagonists and one or more NEP inhibitors; a combination of one or more aldosterone receptor antagonists, one or more NEP inhibitors, and one or more ACE inhibitors; or a combination of one or more aldosterone receptor antagonists and one or more vasopeptidase inhibitors selected from a specific group of compounds described herein.

6. 发明申请

WO2004075857A2 COMPOSITIONS, COMBINATIONS, AND METHODS FOR TREATING CARDIOVASCULAR CONDITIONS AND OTHER ASSOCIATED CONDITIONS 审中-公开
标题翻译：用于治疗心血管病和其他相关条件的组合物，组合和方法
公开(公告)号：WO2004075857A2
公开(公告)日：2004-09-10
申请号：PCT/US2004/005799
申请日：2004-02-26
申请人： PHARMACIA CORPORATION , RUDOLPH, Amy, E. , ROCHA, Ricardo
发明人： RUDOLPH, Amy, E. , ROCHA, Ricardo
IPC分类号： A61K
CPC分类号： A61K45/06
摘要： This invention is directed generally to a method for treating a pathological condition (particularly a cardiovascular condition (e.g., hypertension or heart failure) or a condition associated with a cardiovascular condition) using a p38-kinase inhibitor (e.g., a p38-kinase-inhibiting substituted pyrazole), and specifically a combination comprising a p38-kinase inhibitor with an aldosterone antagonist or diuretic for treating a cardiovascular condition. This invention also is directed generally to combinations comprising a p38-kinase inhibitor, and specifically to combinations comprising a p38-kinase inhibitor with an aldosterone antagonist or diuretic. This invention is further directed generally to pharmaceutical compositions comprising a p38-kinase inhibitor, and more specifically to compositions comprising the above-described combinations.
摘要翻译：本发明一般涉及使用p38-激酶抑制剂（例如，p38-激酶抑制剂）治疗病理状况（特别是心血管病症（例如高血压或心力衰竭）或与心血管疾病相关的病症）的方法取代的吡唑），特别是包含p38-激酶抑制剂与醛固酮拮抗剂或利尿剂治疗心血管病症的组合。本发明还通常涉及包含p38-激酶抑制剂的组合，特别涉及包含p38-激酶抑制剂与醛固酮拮抗剂或利尿剂的组合。本发明进一步涉及包含p38-激酶抑制剂的药物组合物，更具体地涉及包含上述组合的组合物。

7. 发明申请

WO2004075852A3 COMPOSITIONS, COMBINATIONS, AND METHODS FOR TREATING CARDIOVASCULAR CONDITIONS AND OTHER ASSOCIATED CONDITIONS 审中-公开
公开(公告)号：WO2004075852A3
公开(公告)日：2004-09-10
申请号：PCT/US2004/005609
申请日：2004-02-26
申请人： PHARMACIA CORPORATION , RUDOLPH, Amy, E. , ROCHA, Ricardo , CARRETERO, Oscar, A.
发明人： RUDOLPH, Amy, E. , ROCHA, Ricardo , CARRETERO, Oscar, A.
IPC分类号： A61K31/675
摘要： This invention is directed generally to a method for treating a pathological condition (particularly a cardiovascular condition ( e.g ., hypertension or heart failure) or a condition associated with a cardiovascular condition) using a p38-kinase inhibitor ( e.g ., a p38-kinase-inhibiting substituted pyrazole), and specifically a combination comprising a p38-kinase inhibitor with an angiotensin-converting-enzyme inhibitor (or "ACE inhibitor") for treating a cardiovascular condition. This invention also is directed generally to combinations comprising a p38-kinase inhibitor, and specifically to combinations comprising a p38-kinase inhibitor with an angiotensin-converting-enzyme inhibitor. This invention is further directed generally to pharmaceutical compositions comprising a p38-kinase inhibitor, and more specifically to compositions comprising the above-described combinations.

8. 发明申请

WO2003063846A3 ALDOSTERONE RECEPTOR ANTAGONIST AND ALPHA-ADRENERGIC MODULATING AGENT COMBINATION THERAPY FOR PREVENTION OR TREATMENT OF CARDIOVASCULAR CONDITIONS 审中-公开
公开(公告)号：WO2003063846A3
公开(公告)日：2003-08-07
申请号：PCT/US2003/002723
申请日：2003-01-30
申请人： PHARMACIA CORPORATION , MCMAHON, Ellen, G. , RUDOLPH, Amy, E.
发明人： MCMAHON, Ellen, G. , RUDOLPH, Amy, E.
IPC分类号： A61K31/585
摘要： A combination therapy comprising a therapeutically-effective amount of an aldosterone receptor antagonist and a therapeutically-effective amount of an alpha-adrenergic modulating agent is described for treatment of circulatory disorders, including cardiovascular disorders such as hypertension, congestive heart failure, cirrhosis and ascites. Preferred alpha-adrenergic modulating agents are those compounds having high potency and bioavailability. Preferred aldosterone receptor antagonists are 20-spiroxane steroidal compounds characterized by the presence of a 9α, 11α-substituted epoxy moiety. A preferred combination therapy includes an alpha-1-adrenergic antagonist or an alpha-2-adrenergic agonist and the aldosterone receptor antagonist epoxymexrenone.

9. 发明申请

WO2004082637A2 COMBINATION OF AN ALDOSTERONE RECEPTOR ANTAGONIST AND AN ENDOTHELIN RECEPTOR ANTAGONIST AND/OR ENDOTHELIN CONVERTING ENZYME INHIBITOR 审中-公开
标题翻译：阿托品酮受体拮抗剂和内皮素受体拮抗剂和/或内皮素转化酶抑制剂的组合
公开(公告)号：WO2004082637A2
公开(公告)日：2004-09-30
申请号：PCT/US2004/008250
申请日：2004-03-18
申请人： PHARMACIA CORPORATION , MCMAHON, Ellen, G. , RUDOLPH, Amy, E.
发明人： MCMAHON, Ellen, G. , RUDOLPH, Amy, E.
IPC分类号： A61K
CPC分类号： A61K45/06 , A61K31/56 , A61K2300/00
摘要： Novel combinations, compositions, and therapeutic methods of treatment and/or prophylaxis of a hypertension, cardiovascular disease, renal dysfunction, edema, cerebrovascular disease, or insulinopathy pathological conditions in a subject, wherein the methods comprise the administration of a combination of one or more aldosterone receptor antagonists and one or more endothelin receptor antagonist and/or ECE inhibitors selected from a specific group of compounds described herein.
摘要翻译：用于治疗和/或预防受试者的高血压，心血管疾病，肾功能障碍，水肿，脑血管疾病或胰岛素性病理状况的新型组合，组合物和治疗方法，其中所述方法包括施用一种或多种醛固酮受体拮抗剂和选自本文所述的特定化合物组的一种或多种内皮素受体拮抗剂和/或ECE抑制剂。

10. 发明申请

WO2004017906A3 MODULATION OF MATRIX METALLOPROTEINASE (MMP) ACTIVITY WITH ALDOSTERONE BLOCKER(S) 审中-公开
标题翻译：基质金属蛋白酶（MMP）活性与阿托品酮阻滞剂的调节（S）
公开(公告)号：WO2004017906A3
公开(公告)日：2004-07-01
申请号：PCT/US0326251
申请日：2003-08-22
申请人： PHARMACIA CORP , RUDOLPH AMY E , MCMAHON ELLEN G
发明人： RUDOLPH AMY E , MCMAHON ELLEN G
IPC分类号： A61K45/00 , A61K31/00 , A61K31/56 , A61K31/585 , A61P3/10 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/12 , A61P13/12 , A61P21/00 , A61P25/00 , A61P43/00
CPC分类号： A61K31/00 , A61K31/56 , A61K31/585
摘要： The present invention is directed to a method for preventing an increase in matrix metalloproteinase (MMP) activity or reducing MMP activity in a subject in need thereof by administering to the subject a therapeutically effective amount of a selective aldosterone blocker. More particularly, the present invention is directed to attenuating or preventing an increase in MMP activity comprising administering eplerenone, or derivatives thereof.
摘要翻译：本发明涉及通过向受治疗者施用治疗有效量的选择性醛固酮阻断剂来防止基质金属蛋白酶（MMP）活性增加或降低有需要的受试者的MMP活性的方法。更具体地，本发明涉及减轻或预防MMP活性的增加，其包括给予依普利酮或其衍生物。

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