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1. 发明申请

US20110236400A1 TETRAHYDROPYRANOCHROMENE GAMMA SECRETASE INHIBITORS 有权
标题翻译：四氢吡喃葡萄糖消炎酶抑制剂
公开(公告)号：US20110236400A1
公开(公告)日：2011-09-29
申请号：US12665580
申请日：2008-07-01
申请人： Wen-Lian Wu , Thomas A. Bara , Duane A. Burnett , John W. Clader , Martin S. Domalski , Yan Jin , Hubert B. Josien , Hongmei Li , Xian Liang , Dmitri A. Pissarnitski , Thavalakulamgara K. Sasikumar , Jesse K. Wong , Ruo Xu , Zhiqiang Zhao , Paul E. McNamara
发明人： Wen-Lian Wu , Thomas A. Bara , Duane A. Burnett , John W. Clader , Martin S. Domalski , Yan Jin , Hubert B. Josien , Hongmei Li , Xian Liang , Dmitri A. Pissarnitski , Thavalakulamgara K. Sasikumar , Jesse K. Wong , Ruo Xu , Zhiqiang Zhao , Paul E. McNamara
IPC分类号： A61K39/395 , C07D493/04 , C07D311/80 , C07D407/12 , A61K31/35 , A61K31/352 , A61K31/381 , A61P25/28 , A61P29/00 , A61P31/00 , C07C201/12 , C07C67/343
CPC分类号： C07D493/04 , C07D311/78 , C07D407/12
摘要： Disclosed are novel gamma secretase inhibitors of the formula. Also disclosed are methods of inhibiting gamma-secretase, methods of treating neurodegenerative diseases, and methods of treating Alzheimer's Disease. Also disclosed are processes for preparing alkenes in one reaction step using a mixture of an aldehyde (or ketone) and an alkyl substituted with two electron withdrawing groups, and reacting the mixture with: (a) a sulfonyl halide (e.g., a sulfonyl chloride) and a basic tertiary amine, or, (b) a sulfonyl anhydride and a basic amine, or (c) an aryl-C(O)-halide and a basic tertiary amine, or (d) an aryl-C(O)—O—C(O)-aryl and a basic tertiary amine, or (e) an heteroaryl-C(O)-halide and a basic tertiary amine, or (f) a heteroaryl-C(O)—O—C(O)-heteroaryl and a basic tertiary amine.
摘要翻译：公开了下式的新型γ-分泌酶抑制剂。还公开了抑制γ-分泌酶，治疗神经变性疾病的方法和治疗阿尔茨海默氏病的方法。还公开了在一个反应步骤中使用醛（或酮）和被两个吸电子基团取代的烷基的混合物制备烯烃的方法，并使该混合物与：（a）磺酰卤（例如磺酰氯）和（b）磺酰基酐和碱性胺，或（c）芳基-C（O） - 卤化物和碱式叔胺，或（d）芳基-C（O） - （O） - 芳基和碱式叔胺，或（e）杂芳基-C（O） - 卤化物和碱式叔胺，或（f）杂芳基-C（O）-O-C（O ） - 杂芳基和碱性叔胺。

2. 发明授权

US07396929B2 Synthesis of 3-amino-4-substituted pyrazole derivatives 失效
标题翻译： 3-氨基-4-取代的吡唑衍生物的合成
公开(公告)号：US07396929B2
公开(公告)日：2008-07-08
申请号：US11448191
申请日：2006-06-07
申请人： Jianshe Kong , Tao Meng , Paul E. McNamara , Xian Liang , Jesse K. Wong
发明人： Jianshe Kong , Tao Meng , Paul E. McNamara , Xian Liang , Jesse K. Wong
IPC分类号： C07D417/02
CPC分类号： C07D231/38
摘要： This application discloses a novel process to synthesize 3-amino-4-substituted pyrazole derivatives, which may be used, for example, as intermediates to prepare compounds having, for example, pharmaceutical utility.
摘要翻译：本申请公开了一种合成3-氨基-4-取代的吡唑衍生物的新方法，其可用于例如制备具有例如药物效用的化合物的中间体。

3. 发明申请

US20110286969A1 DEUTERATED COMPOUNDS AS HEPATITIS C VIRUS (HCV) INHIBITORS 审中-公开
标题翻译：作为HEPATITIS C病毒（HCV）抑制剂的去除化合物
公开(公告)号：US20110286969A1
公开(公告)日：2011-11-24
申请号：US13139131
申请日：2009-12-10
申请人： Malcolm MacCoss , F. George Njoroge , Frank Bennett , Srikanth Venkatraman , Joseph A. Kozlowski , Wensheng Yu , Paul E. McNamara , Pernilla R. Royster
发明人： Malcolm MacCoss , F. George Njoroge , Frank Bennett , Srikanth Venkatraman , Joseph A. Kozlowski , Wensheng Yu , Paul E. McNamara , Pernilla R. Royster
IPC分类号： A61K38/21 , A61P31/14 , C12N9/99 , C07K5/103 , A61K38/07
CPC分类号： A61K31/403 , A61K31/7056 , A61K38/21 , A61K38/212 , A61K45/06 , A61K47/64 , C07K5/06052 , A61K2300/00
摘要： The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as wet! as methods of using them to treat disorders associated with the HCV protease An illustrative inventsve compound is shown below: Formula (I).
摘要翻译：本发明公开了具有HCV蛋白酶抑制活性的新化合物以及制备这些化合物的方法。在另一个实施方案中，本发明公开了包含湿润的化合物的药物组合物。作为使用它们来治疗与HCV蛋白相关的病症的方法本发明的说明性化合物如下所示：式（I）。

4. 发明授权

US4906635A Carboxyalkyl dipeptides as antiglaucoma agents 失效
标题翻译：羧甲基二肽作为抗青光眼剂
公开(公告)号：US4906635A
公开(公告)日：1990-03-06
申请号：US220183
申请日：1988-07-18
申请人： Bernard R. Neustadt , David R. Andrews , Paul E. McNamara , Robert W. Watkins
发明人： Bernard R. Neustadt , David R. Andrews , Paul E. McNamara , Robert W. Watkins
IPC分类号： A61K38/00 , C07D285/32 , C07K5/02
CPC分类号： C07K5/0222 , C07D285/32 , A61K38/00
摘要： Methods and pharmaceutical compositions are disclosed for reducing intraocular pressure. The methods and compositions employ an active ingredient which comprises certain benzothiadiazinyl and quinazolinyl substituted carboxyalkyl dipeptides wherein the benzothiadiazinyl or quinazolinyl portions are joined to the dipeptide portions by an aminocarbonyl group.
摘要翻译：公开了用于降低眼内压的方法和药物组合物。所述方法和组合物使用包含某些苯并噻二嗪基和喹唑啉基取代的羧基烷基二肽的活性成分，其中苯并噻二嗪基或喹唑啉基部分通过氨基羰基连接到二肽部分。

5. 发明授权

US4778795A Carboxyalkyl dipeptides as antiglaucoma agents 失效
公开(公告)号：US4778795A
公开(公告)日：1988-10-18
申请号：US903545
申请日：1986-09-03
申请人： Bernard R. Neustadt , David R. Andrews , Paul E. McNamara , Robert W. Watkins
发明人： Bernard R. Neustadt , David R. Andrews , Paul E. McNamara , Robert W. Watkins
IPC分类号： A61K38/00 , C07D285/32 , C07K5/02 , A61K31/505 , A61K31/44
CPC分类号： C07K5/0222 , C07D285/32 , A61K38/00 , Y10S514/913
摘要： Methods and pharmaceutical compositions are disclosed for reducing intraocular pressure. The methods and compositions employ an active ingredient which comprises certain benzothiadiazinyl and quinazolinyl substituted carboxyalkyl dipeptides wherein the benzothiadiazinyl or quinazolinyl portions are joined to the dipeptide portions by an aminocarbonyl group.

6. 发明授权

US4634556A Crystalline sodium (5R, 6S, 8R)-6-(1-hydroxyethyl)-2-(2-carbamoyloxyethylthio)-penem-3-carboxylate and process for making same 失效
标题翻译：结晶钠（5R，6S，8R）-6-（1-羟乙基）-2-（2-氨基甲酰氧基乙硫基） - 庚-3-烯酸甲酯及其制备方法
公开(公告)号：US4634556A
公开(公告)日：1987-01-06
申请号：US732533
申请日：1985-05-10
申请人： John K. Jenkins , John S. Chiu , Charles G. Eckhart , Paul E. McNamara , Stanley Rosenhouse , Richard E. Youngstrom
发明人： John K. Jenkins , John S. Chiu , Charles G. Eckhart , Paul E. McNamara , Stanley Rosenhouse , Richard E. Youngstrom
IPC分类号： C07D499/88 , C07D499/00 , A61K31/425
CPC分类号： C07D499/88
摘要： A novel, stable, crystalline sodium (5R,6S,8R)-6-(1-hydroxyethyl)-2-(2-carbamoyloxyethylthio)-penem-3-carboxylate (designated as Form II) is prepared by forming a homogenous solution of sodium (5R,6S,8R)-6-(1-hydroxyethyl)-2-(2-carbamoyloxyethylthio)-penem-3-carboxylate combined with stirring the homogenous solution for a time and at a temperature sufficient to produce Form II and recovering Form II. Form II may also be prepared by contacting a first solution obtained by dissolving (5R,6S,8R)-6-(1-hydroxyethyl)-2-(2-carbamoyloxyethylthio)-penem-3-carboxylic acid in dimethylacetamide with a second solution obtained by dissolving a sodium salt of an organic acid having a pKa of up to about 5, e.g., sodium 2-ethylhexanoate in acetone, in the presence of at least 5 volume percent water while stirring the reaction mixture so formed at a temperature and for a time sufficient to produce Form II followed by recovering Form II.Form II exhibits a greater physical stability and increased solid state chemical stability and reduced hygroscopicity over that of the amorphous form (e.g., Form I) which renders Form II greatly superior to Form I as a clinically suitable antibacterial agent.
摘要翻译：通过形成均匀的溶液来制备新的稳定的结晶的（5R，6S，8R）-6-（1-羟乙基）-2-（2-氨基甲酰氧基乙硫基） - 庚-3-烯氧基化钠（命名为II型）的（5R，6S，8R）-6-（1-羟乙基）-2-（2-氨基甲酰氧基乙硫基） - 庚-3-烯酰氧基化合物与搅拌均匀溶液一段时间并在足以产生II型并恢复II型。形式II也可以通过将通过将（5R，6S，8R）-6-（1-羟乙基）-2-（2-氨基甲酰氧基乙硫基） - 亚氨基-3-碳氧基酸溶解在二甲基乙酰胺中获得的第一溶液与第二溶液通过在至少5体积％的水的存在下，将具有高达约5的pKa的有机酸的钠盐例如2-乙基己酸酯溶解在丙酮中而获得的溶液，同时搅拌在温度下形成的反应混合物，一段时间足以生产II型，然后恢复II型。 II型具有更大的物理稳定性和增加的固态化学稳定性，并且比非晶形式（例如，形式I）的吸湿性降低，其使得II型作为临床合适的抗菌剂大大优于I型。

7. 发明授权

US4616012A Carboxyalkyl dipeptides as antiglaucoma agents 失效
公开(公告)号：US4616012A
公开(公告)日：1986-10-07
申请号：US797104
申请日：1985-11-12
申请人： Bernard R. Neustadt , David R. Andrews , Paul E. McNamara , Robert W. Watkins
发明人： Bernard R. Neustadt , David R. Andrews , Paul E. McNamara , Robert W. Watkins
IPC分类号： A61K38/00 , C07D285/32 , C07K5/062 , A61K31/54
CPC分类号： C07K5/06026 , C07D285/32 , C07K5/06034 , C07K5/06086 , C07K5/06191 , A61K38/00 , Y10S514/913
摘要： Methods and pharmaceutical compositions are disclosed for reducing intraocular pressure. The methods and compositions employ an active ingredient which comprises certain benzothiadiazinyl and quinazolinyl substituted carboxyalkyl dipeptides wherein the benzothiadiazinyl or quinazolinyl portions are joined to the dipeptide portions by an aminocarbonyl group.

8. 发明授权

US5017567A Carboxyalkyl dipeptides as antiglaucoma agents 失效
标题翻译：羧甲基二肽作为抗青光眼剂
公开(公告)号：US5017567A
公开(公告)日：1991-05-21
申请号：US460425
申请日：1990-01-03
申请人： Bernard R. Neustadt , David R. Andrews , Paul E. McNamara , Robert W. Watkins
发明人： Bernard R. Neustadt , David R. Andrews , Paul E. McNamara , Robert W. Watkins
IPC分类号： A61K38/00 , C07D285/32 , C07K5/02
CPC分类号： C07K5/0222 , C07D285/32 , A61K38/00 , Y10S514/913
摘要： Methods and pharmaceutical compositions are disclosed for reducing intraocular pressure. The methods and compositions employ an active ingredient which comprises certain benzothiadiazinyl and quinazolinyl substituted carboxyalkyl dipeptides wherein the benzothiadiazinyl or quinazolinyl portions are joined to the dipeptide portions by an aminocarbonyl group.
摘要翻译：公开了用于降低眼内压的方法和药物组合物。所述方法和组合物使用包含某些苯并噻二嗪基和喹唑啉基取代的羧基烷基二肽的活性成分，其中苯并噻二嗪基或喹唑啉基部分通过氨基羰基连接到二肽部分。

9. 发明授权

US4559340A Antihypertensive agents 失效
标题翻译：抗高血压药
公开(公告)号：US4559340A
公开(公告)日：1985-12-17
申请号：US555311
申请日：1983-11-25
申请人： Bernard R. Neustadt , David R. Andrews , Paul E. McNamara
发明人： Bernard R. Neustadt , David R. Andrews , Paul E. McNamara
IPC分类号： A61K38/00 , C07D285/32 , C07K5/02 , C07D417/12 , A61K31/54
CPC分类号： C07K5/0222 , C07D285/32 , A61K38/00 , Y10S530/80
摘要： There are disclosed benzothiadiazinyl and quinazolinyl substituted carboxylalkyl dipeptides, wherein the benzothiodiazinyl or quinazolinyl portions are joined to the dipeptide portions by an aminocarbonyl group. Compounds of this invention are useful as antihypertensive agents, in the treatment of congestive heart failure and in the treatment of glaucoma. In addition, compounds of this invention have diuretic activity.
摘要翻译：公开了苯并噻二嗪基和喹唑啉基取代的羧基烷基二肽，其中苯并二氮嗪基或喹唑啉基部分通过氨基羰基连接到二肽部分。本发明化合物可用作抗高血压药，用于治疗充血性心力衰竭和治疗青光眼。此外，本发明的化合物具有利尿活性。

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