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1. 发明申请

WO2009106471A2 NEW ANGIOTENSIN II RECEPTOR BLOCKER DERIVATIVES 审中-公开
标题翻译：新型血管紧张素II受体阻断剂衍生物
公开(公告)号：WO2009106471A2
公开(公告)日：2009-09-03
申请号：PCT/EP2009051943
申请日：2009-02-19
申请人： NICOX SA , MERCK & CO INC , ALMIRANTE NICOLETTA , NICOTRA ALESSIA , MANDELLI VALENTINO , BIONDI STEFANO , STEFANINI SILVIA , SEBHAT IYASSU K , LO MICHAEL MAN-CHU
发明人： ALMIRANTE NICOLETTA , NICOTRA ALESSIA , MANDELLI VALENTINO , BIONDI STEFANO , STEFANINI SILVIA , SEBHAT IYASSU K , LO MICHAEL MAN-CHU
IPC分类号： C07D403/10 , A61P9/00 , C07D403/14 , C07D405/14
CPC分类号： C07D403/10 , C07D403/14 , C07D405/14
摘要： New angiotensin II receptor blocker nitroderivatives of general formula (I) and pharmaceutically acceptable salts or stereoisomers thereof: and their use for treating cardiovascular, renal and chronic liver diseases, inflammatory processes and metabolic syndromes.
摘要翻译：通式（I）的新型血管紧张素II受体阻断剂硝基衍生物及其药学上可接受的盐或立体异构体及其用于治疗心血管，肾和慢性肝脏疾病，炎症过程和代谢综合征的用途。

2. 发明申请

WO2008076246A3 NITRODERIVATIVES AS ANGIOTENSIN II RECEPTOR ANTAGONISTS 审中-公开
公开(公告)号：WO2008076246A3
公开(公告)日：2009-01-15
申请号：PCT/US2007025232
申请日：2007-12-11
申请人： MERCK & CO INC , NICOX SA , SEBHAT IYASSU K , LO MICHAEL MAN-CHU , NARGUND RAVI P , ALI AMJAD , FRANKLIN CHRIS , ALMIRANTE NICOLETTA , STORONI LAURA , STEFANINI SILVIA
发明人： SEBHAT IYASSU K , LO MICHAEL MAN-CHU , NARGUND RAVI P , ALI AMJAD , FRANKLIN CHRIS , ALMIRANTE NICOLETTA , STORONI LAURA , STEFANINI SILVIA
IPC分类号： C07D403/10 , A61K31/41 , A61P9/12
CPC分类号： C07D403/10
摘要： A compound having the structure (Formula I), wherein R is an angiotensin receptor antagonist active group, Y is -Y1-Y2-Y3-Y4-Y5.; Y1 is C(R1R2); R1 is selected from the group consisting of hydrogen and C1-4 alkyl; R2 is selected from the group consisting of hydrogen, C1-4 alkyl, and -0C(0)C1-4 alkyl; Y2 is O or CH2; Y3 is C(O) or CH2; Y4 is O or CH2; Y5 is -(CH2) 1-2-(X)0-1-(CH2)0-1- or is absent; X is -O- or -CR3R4-; and R3 and R4 are independently selected from the group consisting of hydrogen and C1-C4 alkyl; or a pharmaceutically acceptable salt or hydrate thereof, which is useful for treating hypertension.
摘要翻译：具有结构（式I）的化合物，其中R是血管紧张素受体拮抗剂活性基团，Y是-Y1-Y2-Y3-Y4-Y5。 Y1是C（R1R2）; R 1选自氢和C 1-4烷基; R 2选自氢，C 1-4烷基和-C（O）C 1-4烷基; Y2是O或CH2; Y 3是C（O）或CH 2; Y4是O或CH2; Y 5是 - （CH 2）1-2 - （X）0-1 - （CH 2）0-1-或不存在; X是-O-或-CR 3 R 4 - ; 并且R 3和R 4独立地选自氢和C 1 -C 4烷基; 或其药学上可接受的盐或水合物，其可用于治疗高血压。

3. 发明申请

WO2009106470A3 ANGIOTENSIN II RECEPTOR ANTAGONISTS 审中-公开
标题翻译： ANGIOTENSIN II受体拮抗剂
公开(公告)号：WO2009106470A3
公开(公告)日：2010-06-24
申请号：PCT/EP2009051942
申请日：2009-02-19
申请人： NICOX SA , MERCK SHARP & DOHME , ALMIRANTE NICOLETTA , NICOTRA ALESSIA , STEFANINI SILVIA , BIONDI STEFANO , ONGINI ENNIO , ALI AMJAD , LO MICHAEL MAN-CHU
发明人： ALMIRANTE NICOLETTA , NICOTRA ALESSIA , STEFANINI SILVIA , BIONDI STEFANO , ONGINI ENNIO , ALI AMJAD , LO MICHAEL MAN-CHU
IPC分类号： C07D257/04 , A61P9/12 , C07D403/10 , C07D409/06
CPC分类号： C07D257/04 , C07D403/10 , C07D409/06
摘要： The present invention relates to nitrooxyderivatives of angiotensin Il receptor antagonists based on the formulae (IIa) to (IIk).
摘要翻译：本发明涉及基于式（IIa）至（IIk）的血管紧张素II受体拮抗剂的硝基氧基衍生物。

4. 发明申请

WO2008076247A3 NITRODERIVATIVES AS ANGIOTENSIN II RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为血管紧张素Ⅱ受体拮抗剂的氮转铁蛋白
公开(公告)号：WO2008076247A3
公开(公告)日：2009-01-15
申请号：PCT/US2007025233
申请日：2007-12-11
申请人： MERCK & CO INC , NICOX SA , SEBHAT IYASSU K , LO MICHAEL MAN-CHU , NARUGUND RAVI P , ALI AMJAD , FRANKLIN CHRIS , ALMIRANTE NICOLETTA , STORONI LAURA , STEFANINI SILVIA
发明人： SEBHAT IYASSU K , LO MICHAEL MAN-CHU , NARUGUND RAVI P , ALI AMJAD , FRANKLIN CHRIS , ALMIRANTE NICOLETTA , STORONI LAURA , STEFANINI SILVIA
IPC分类号： C07D403/10 , A61K31/41 , A61P9/12
CPC分类号： C07D403/10
摘要： A compound having the structure (Formula I), wherein R is an angiotensin receptor antagonist active group, Y is -Y1-Y2-Y3-Y4-Y5.; Y1 is C(R1R2); R1 is selected from the group consisting of hydrogen and C1-4 alkyl; R2 is selected from the group consisting of hydrogen, C1-4 alkyl, and -0C(0)C1-4 alkyl; Y2 is O or CH2; Y3 is C(O) or CH2; Y4 is O or CH2; Y5 is -(CH2) 1-2-(X)0-1-(CH2)0-1- or is absent; X is -O- or -CR3R4-; and R3 and R4 are independently selected from the group consisting of hydrogen and C1-C4 alkyl; or a pharmaceutically acceptable salt or hydrate thereof, which is useful for treating hypertension.
摘要翻译：具有结构（式I）的化合物，其中R是血管紧张素受体拮抗剂活性基团，Y是-Y 1 -Y 2 -Y 3 -Y 4 -Y 5。 Y1是C（R1R2）; R1选自氢和C1-4烷基; R2选自氢，C1-4烷基和-OC（O）C1-4烷基; Y2是O或CH2; Y3是C（O）或CH2; Y4是O或CH2; Y5是 - （CH2）1-2-（X）0-1-（CH2）0-1-或不存在; X是-O-或-CR 3 R 4 - ; 并且R 3和R 4独立地选自氢和C 1 -C 4烷基; 或其药学上可接受的盐或水合物，其可用于治疗高血压。

5. 发明申请

WO2009070241A3 ANGIOTENSIN II RECEPTOR ANTAGONISTS 审中-公开
标题翻译： ANGIOTENSIN II受体拮抗剂
公开(公告)号：WO2009070241A3
公开(公告)日：2009-11-12
申请号：PCT/US2008012984
申请日：2008-11-21
申请人： MERCK & CO INC , NICOX SA , ALI AMJAD , LO MICHAEL MAN-CHU , FRANKLIN CHRIS , ALMIRANTE NICOLETTA , STEFANINI SILVIA , STORONI LAURA , BIONDI STEFANO , ONGINI ENNIO
发明人： ALI AMJAD , LO MICHAEL MAN-CHU , FRANKLIN CHRIS , ALMIRANTE NICOLETTA , STEFANINI SILVIA , STORONI LAURA , BIONDI STEFANO , ONGINI ENNIO
IPC分类号： C07D403/10 , A61K31/41 , A61P9/12
CPC分类号： C07D403/10
摘要： A compound having the structure (A) wherein R is an angiotensin receptor antagonist active group, and Y is 1) -(CH2)3R5, 2) -C(O)(CH2)2R5, 3) -C(R1R2)OC(O)O(CH2)nR5, wherein n is 1 or 2, 4) -C(R1R2)OC(O)CH2CH2R5, 5) -C(R1R2)OC(O)OCH2CH2C(R3R4)R5, Formula (B), and Formula (C) provided that when Y is -C(O)(CH2)2R5, then R is Formula (D) R1, R2, R3 and R4 are independently selected from the group consisting of hydrogen and C1-4 alkyl; R5 is CH(ONO2)CH(ONO2)R6; R6 is selected from CH3, CH2CH3 and CH(CH3)2; or a pharmaceutically acceptable salt or hydrate thereof, which is useful for treating hypertension.
摘要翻译：具有结构（A）的化合物，其中R是血管紧张素受体拮抗剂活性基团，Y是1） - （CH 2）3 R 5，2）-C（O）（CH 2）2 R 5，3）-C（R 1 R 2）OC（ O（CH 2）n R 5，其中n为1或2，4）-C（R 1 R 2）OC（O）CH 2 CH 2 R 5，5）-C（R 1 R 2）OC（O）OCH 2 CH 2 C（R 3 R 4）和式（C），条件是当Y为-C（O）（CH 2）2 R 5时，则R为式（D）R 1，R 2，R 3和R 4独立地选自氢和C 1-4烷基; R5是CH（ONO2）CH（ONO2）R6; R 6选自CH 3，CH 2 CH 3和CH（CH 3）2; 或其药学上可接受的盐或水合物，其可用于治疗高血压。

6. 发明申请

WO2008095841A3 NITRIC OXIDE DONOR COMPOUNDS 审中-公开
标题翻译：硝酸氧化物化合物
公开(公告)号：WO2008095841A3
公开(公告)日：2008-10-30
申请号：PCT/EP2008051092
申请日：2008-01-30
申请人： NICOX SA , ALMIRANTE NICOLETTA , BIONDI STEFANO , ONGINI ENNIO , STORONI LAURA , NICOTRA ALESSIA
发明人： ALMIRANTE NICOLETTA , BIONDI STEFANO , ONGINI ENNIO , STORONI LAURA , NICOTRA ALESSIA
IPC分类号： C07C203/04 , A61K31/223 , A61K31/27 , A61P9/10 , C07C271/22
CPC分类号： C07C229/20 , A61K31/223 , A61K31/225 , A61K31/265 , A61K31/27 , A61K31/40 , A61K31/403 , A61K45/06 , C07C203/02 , C07C229/08 , C07C229/22 , C07C229/24 , C07C229/26 , C07C229/36 , C07C237/08 , C07C271/22 , C07C279/14 , C07C291/02 , C07C323/58 , C07D207/16 , C07D209/52
摘要： The invention relates to nitric oxide donor compounds and their use for treating cardiovascular diseases, inflammation, pain, fever, gastrointestinal disorders, ophthalmic diseases, hepatic disorders, renal diseases, respiratory disorders, immunological diseases, bone metabolism dysfunctions, central and peripheral nervous system diseases, sexual dysfunctions, infectious diseases, for the inhibition of platelet aggregation and platelet adhesion, for treating pathological conditions resulting from abnormal cell proliferation, vascular diseases. The invention also relates to compositions comprising at least one nitric oxide releasing compounds of the invention and composition comprising at least one nitric oxide releasing compounds according to the invention and at least one therapeutic agent.
摘要翻译：本发明涉及一氧化氮供体化合物及其用于治疗心血管疾病，炎症，疼痛，发热，胃肠道疾病，眼科疾病，肝脏疾病，肾脏疾病，呼吸系统疾病，免疫疾病，骨代谢功能障碍，中枢和周围神经系统疾病，性功能障碍，感染性疾病，用于抑制血小板聚集和血小板粘附，用于治疗由异常细胞增殖，血管疾病引起的病理状况。本发明还涉及包含至少一种本发明的释放氧化氮的化合物和包含至少一种根据本发明的一氧化氮释放化合物和至少一种治疗剂的组合物的组合物。

7. 发明申请

WO2007104652A3 NON-PEPTIDIC RENIN INHIBITORS NITRODERIVATIVES 审中-公开
标题翻译：非特异性RENIN抑制剂NITRODERIVATIVES
公开(公告)号：WO2007104652A3
公开(公告)日：2008-01-10
申请号：PCT/EP2007051933
申请日：2007-03-01
申请人： NICOX SA , ALMIRANTE NICOLETTA , BIONDI STEFANO , ONGINI ENNIO
发明人： ALMIRANTE NICOLETTA , BIONDI STEFANO , ONGINI ENNIO
IPC分类号： C07D211/78 , A61K31/439 , A61P9/12 , C07D401/12 , C07D405/12 , C07D451/02 , C07D451/14 , C07D487/08 , C07D498/08 , C07D513/08
CPC分类号： C07D487/08 , C07D211/78 , C07D401/12 , C07D405/12 , C07D451/02 , C07D451/14 , C07D513/08
摘要： Non-peptidic renin inhibitors nitroderivatives of general formula (I): A 1 -(X a -ONO 2 ) j 5 (I) having wider pharmacological activity and enhanced tolerability. They can be employed for treating or preventing cardiovascular, renal and chronic liver diseases, inflammatory processes and metabolic syndrome.
摘要翻译：非肽肽肾素抑制剂通式（I）的硝基衍生物：其中，R 1，R 2，R 3， SUB（5）（I）具有较强的药理活性和增强的耐受性。它们可用于治疗或预防心血管，肾脏和慢性肝脏疾病，炎症过程和代谢综合征。

8. 发明申请

WO2008074450A3 NON-PEPTIDIC RENIN INHIBITORS NITRODERIVATIVES 审中-公开
标题翻译：非特异性RENIN抑制剂NITRODERIVATIVES
公开(公告)号：WO2008074450A3
公开(公告)日：2009-01-08
申请号：PCT/EP2007011078
申请日：2007-12-13
申请人： NICOX SA , ALMIRANTE NICOLETTA , BIONDI STEFANO , ONGINI ENNIO
发明人： ALMIRANTE NICOLETTA , BIONDI STEFANO , ONGINI ENNIO
IPC分类号： C07D211/42 , A61K31/451 , A61K31/4709 , A61K31/495 , A61K31/538 , A61K45/06 , A61P1/16 , A61P3/00 , A61P9/00 , A61P13/00 , A61P29/00 , C07D241/24 , C07D295/185 , C07D295/205 , C07D401/12 , C07D401/14 , C07D413/12
CPC分类号： C07D413/14 , C07D211/42 , C07D241/04 , C07D401/12 , C07D413/12
摘要： Non-peptidic renin inhibitors nitroderivatives of general formula (I) : A1-(Xa-ONO2)j having wider pharmacological activity and enhanced tolerability. They can be employed for treating or preventing cardiovascular, renal and chronic liver diseases, inflammatory processes and metabolic syndrome.
摘要翻译：非肽肽肾素抑制剂通式（I）的硝基衍生物：A1-（Xa-ONO2）j具有更广泛的药理活性和增强的耐受性。它们可用于治疗或预防心血管，肾脏和慢性肝脏疾病，炎症过程和代谢综合征。

9. 发明申请

WO2007045551A2 RENIN INHIBITORS NITRODERIVATIVES 审中-公开
标题翻译： RENIN抑制剂NITRODERIVATIVES
公开(公告)号：WO2007045551A2
公开(公告)日：2007-04-26
申请号：PCT/EP2006066952
申请日：2006-10-02
申请人： NICOX SA , ALMIRANTE NICOLETTA , MONOPOLI ANGELA , ONGINI ENNIO
发明人： ALMIRANTE NICOLETTA , MONOPOLI ANGELA , ONGINI ENNIO
IPC分类号： C07D233/54 , C07D211/58 , C07D215/08 , C07D215/38
CPC分类号： C07D233/54 , C07D211/58 , C07D215/08 , C07D215/38 , C07D277/20 , C07D401/14 , C07D417/12
摘要： Renin inhibitors nitroderivatives of formula (I): A-(X 0 -ONO 2 ) s (I) having wider pharmacological activity and enhanced tolerability. They can be employed for treating or preventing congestive heart failure, coronary diseases, cardiac insufficiency, left ventricular dysfunction and hypertrophy, cardiac fibrosis, myocardial ischemia, stroke, atherosclerosis, restenosis post angioplasty, renal insufficiency, renal ischemia, renal failure, renal fibrosis, glomerulonephritis, renal colic, ocular and pulmonary hypertension, glaucoma, hypertension, diabetic complications such as nephropathy, vasculopathy and neuropathy, peripheral vascular diseases, liver fibrosis, portal hypertension, metabolic syndrome, erectile dysfunction, complications after vascular or cardiac surgery, complications of treatment with immunosuppressive agents after organ transplantation, hyperaldosteronism, lung fibrosis, scleroderma, anxiety, cognitive disorders.
摘要翻译：式（I）的肾素抑制剂硝基衍生物：具有更宽的药理活性和增强的耐受性的A-（X-O -OR 2）（I）。它们可用于治疗或预防充血性心力衰竭，冠心病，心功能不全，左心室功能障碍和肥大，心脏纤维化，心肌缺血，中风，动脉粥样硬化，血管成形术后再狭窄，肾功能不全，肾缺血，肾衰竭，肾纤维化，肾小球性肾炎，肾绞痛，眼睛和肺动脉高压，青光眼，高血压，糖尿病并发症如肾病，血管病变和神经病变，外周血管疾病，肝纤维化，门静脉高压，代谢综合征，勃起功能障碍，血管或心脏手术后并发症，并发症器官移植后用免疫抑制剂，醛固酮增多症，肺纤维化，硬皮病，焦虑症，认知障碍。

10. 发明申请

WO2005011646A3 NITROOXY DERIVATIVES OF LOSARTAN, VALSATAN, CANDESARTAN, TELMISARTAN, EPROSARTAN AND OLMESARTAN AS ANGIOTENSIN-II RECEPTOR BLOCKERS FOR THE TREATMENT OF CARDIOVASCULAR DISEASES 审中-公开
标题翻译：洛沙坦，VALSATAN，CANDESARTAN，TELMISARTAN，EPROSARTAN和OLMESARTAN作为治疗心血管疾病的ANGIOTENSIN-II受体阻断剂的NITROOXY衍生物
公开(公告)号：WO2005011646A3
公开(公告)日：2005-04-21
申请号：PCT/EP2004051550
申请日：2004-07-20
申请人： NICOX SA , ALMIRANTE NICOLETTA , DEL SOLDATO PIERO , ONGINI ENNIO
发明人： ALMIRANTE NICOLETTA , DEL SOLDATO PIERO , ONGINI ENNIO
IPC分类号： C07D235/20 , C07D257/04 , C07D403/10 , C07D409/06 , A61K31/4178 , A61K31/41 , A61K31/4184 , C07D403/04
CPC分类号： C07D257/04 , C07D235/20 , C07D403/10 , C07D409/06
摘要： Nitrooxy derivatives of the angiotensin-II receptor blockers Iosartan vaalsartan, candesartan, telmisartan, eprosartan and olmesartan and related compounds of formula (I): R-(Y-ONO2)s wherein R is of formula (II) or (III): R0 is e.g: and R1 is: (IIa), (IIb), (IIc), (IId) or (IIe).
摘要翻译：血管紧张素II受体阻断剂的硝基氧基衍生物，依沙沙坦，坎地沙坦，替米沙坦，依普罗沙坦和奥美沙坦及其相关的式（I）化合物：R-（Y-ONO 2）s其中R为式（II）或（III）（IIa），（IIb），（IIc），（IId）或（IIe）。

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