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1. 发明授权

US4871739A Substituted 6H-7,8-dihydrothiapyrano(3,2-D)-pyrimidines as hyopglycemic agents 失效
标题翻译：取代的6H-7,8-二氢硫杂（3,2-D） - 嘧啶作为血糖水平
公开(公告)号：US4871739A
公开(公告)日：1989-10-03
申请号：US5720
申请日：1987-01-21
申请人： John J. Baldwin , Richard L. Tolman , Mu T. Wu
发明人： John J. Baldwin , Richard L. Tolman , Mu T. Wu
IPC分类号： A61K31/495 , A61P27/02 , A61P27/06 , C07D495/04
CPC分类号： C07D495/04
摘要： There are disclosed certain 2-substituted-4-substituted 6H-7,8-dihydrothiapyrano[3,2-d]pyrimidines which have oral hypoglycemic activity and with such ability to lower blood sugar are useful in the treatment of type II diabetes and/or obesity with associated insulin resistance. Processes for the preparation of such compounds and compositions containing such compounds as the active ingredient thereof are also disclosed. The compounds are also .beta.-adrenergic blocking agonists or .alpha.-adrenergic blocking agents and act as ocular antihypertensives and are useful for the treatment of glaucoma and other eye disorders.
摘要翻译：公开了具有口服降血糖活性并具有降低血糖的能力的某些2-取代-4-取代的6H-7,8-二氢硫吡喃并[3,2-d]嘧啶可用于治疗II型糖尿病和/ 或具有相关胰岛素抵抗的肥胖。还公开了制备这些化合物和含有这些化合物作为其活性成分的组合物的方法。该化合物也是β-肾上腺素能阻断激动剂或α-肾上腺素能阻断剂，并且作为眼部抗高血压药物，并且可用于治疗青光眼和其它眼睛疾病。

2. 发明授权

US4994464A Piperazinylpyrimidines as .beta.-adrenergic receptor blockers 失效
标题翻译：哌嗪基嘧啶作为β-肾上腺素能受体阻断剂
公开(公告)号：US4994464A
公开(公告)日：1991-02-19
申请号：US417535
申请日：1989-10-05
申请人： Richard L. Tolman , John J. Baldwin , Arthur F. Wagner , Adolph Pietruszkiewicz
发明人： Richard L. Tolman , John J. Baldwin , Arthur F. Wagner , Adolph Pietruszkiewicz
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： Certain piperazinylpyrimidines have pronounced .beta.-adrenergic blocking properties and some of the compounds are particularly useful in the treatment of elevated intraocular pressure and glaucoma.
摘要翻译：某些哌嗪基嘧啶具有显着的β-肾上腺素能阻断性质，并且一些化合物特别可用于治疗眼内压升高和青光眼。

3. 发明授权

US4889856A 7,8-dihydro-4-(1-pierazinyl)-6H-thiopyrano-[3,2-d] pyrimidines as .beta.-blockers 失效
标题翻译： 7,8-二氢-4-（1-吡嗪基）-6H-噻喃并[3,2-d]嘧啶作为β-阻断剂
公开(公告)号：US4889856A
公开(公告)日：1989-12-26
申请号：US91471
申请日：1987-08-31
申请人： Richard L. Tolman , Arthur F. Wagner , John J. Baldwin , Adolph Pietruszkiewicz
发明人： Richard L. Tolman , Arthur F. Wagner , John J. Baldwin , Adolph Pietruszkiewicz
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： 7,8-Dihydro-4-(1-piperazinyl)-6H-thiopyranopyrimidines have .beta.-adrenergic blocking properties and are thus useful in the treatment of cardiovascular ailments known to be amenable to .beta.-blocker therapy. Certain of the compounds are useful in the treatment of elevated intraocular pressure by topical ocular administration.
摘要翻译： 7,8-二氢-4-（1-哌嗪基）-6H-噻喃并嘧啶具有β-肾上腺素能阻断性质，因此可用于治疗已知适用于β-阻断剂治疗的心血管疾病。某些化合物可用于通过局部眼部给药治疗眼内压升高。

4. 发明申请

US20120225906A1 PIPERIDINE RENIN INHIBITORS 失效
标题翻译：哌啶仁宁抑制剂
公开(公告)号：US20120225906A1
公开(公告)日：2012-09-06
申请号：US13469562
申请日：2012-05-11
申请人： John J. Baldwin , David A. Claremon , Colin M. Tice , Salvacion Cacatian , Lawrence W. Dillard , Alexey V. Ishchenko , Jing Yuan , Zhenrong Xu , Gerard McGeehan , Wei Zhao , Robert D. Simpson , Suresh B. Singh , Lanqi Jia , Patrick T. Flaherty
发明人： John J. Baldwin , David A. Claremon , Colin M. Tice , Salvacion Cacatian , Lawrence W. Dillard , Alexey V. Ishchenko , Jing Yuan , Zhenrong Xu , Gerard McGeehan , Wei Zhao , Robert D. Simpson , Suresh B. Singh , Lanqi Jia , Patrick T. Flaherty
IPC分类号： A61K31/453 , A61P3/04 , A61P9/12 , A61P9/04 , A61P9/00 , A61P25/28 , A61P25/00 , A61P27/02 , A61P27/06 , A61P5/42 , A61P25/22 , A61P13/12 , A61P9/10
CPC分类号： C07D309/04 , C07D405/12
摘要： The present invention is directed to aspartic protease inhibitors represented by the following structural formula: or a pharmaceutically acceptable salt thereof.The present invention is also directed to pharmaceutical compositions comprising the aspartic protease inhibitors of Structural Formula (I).Methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using these aspartic protease inhibitors are also disclosed.
摘要翻译：本发明涉及由以下结构式表示的天冬氨酸蛋白酶抑制剂：或其药学上可接受的盐。本发明还涉及包含结构式（I）的天冬氨酸蛋白酶抑制剂的药物组合物。还公开了在有需要的受试者中拮抗一种或多种天冬氨酸蛋白酶的方法，以及使用这些天冬氨酸蛋白酶抑制剂治疗受试者天冬氨酸蛋白酶介导的病症的方法。

5. 发明申请

US20110213029A1 3,4-Di-Substituted Cyclobutene-1,2-Diones as CXC-Chemokine Receptor Ligands 审中-公开
标题翻译： 3,4-二取代的环丁烯-1,2-二酮作为CXC趋化因子受体配体
公开(公告)号：US20110213029A1
公开(公告)日：2011-09-01
申请号：US13102554
申请日：2011-05-06
申请人： Arthur G. Taveras , Cynthia J. Aki , Richard W. Bond , Jianping Chao , Michael Dwyer , Johan A. Ferreira , Jianhua Chao , Younong Yu , John J. Baldwin , Bernd Kaiser , Ge Li , J. Robert Merritt , Purakkattle J. Biju , Kingsley H. Nelson, JR. , Laura L. Rokosz , Gaifa Lai , James P. Jakway , Minglang Wu , Evan A. Hecker , Daniel Lundell , Jay S. Fine
发明人： Arthur G. Taveras , Cynthia J. Aki , Richard W. Bond , Jianping Chao , Michael Dwyer , Johan A. Ferreira , Jianhua Chao , Younong Yu , John J. Baldwin , Bernd Kaiser , Ge Li , J. Robert Merritt , Purakkattle J. Biju , Kingsley H. Nelson, JR. , Laura L. Rokosz , Gaifa Lai , James P. Jakway , Minglang Wu , Evan A. Hecker , Daniel Lundell , Jay S. Fine
IPC分类号： A61K31/341 , A61P11/00
CPC分类号： C07C237/30 , C07C225/20 , C07C237/36 , C07C237/44 , C07C255/59 , C07C311/39 , C07C2601/04 , C07C2601/14 , C07C2602/08 , C07D207/335 , C07D213/74 , C07D217/24 , C07D295/26 , C07D307/38 , C07D307/52 , C07D307/68 , C07D307/81 , C07D307/82 , C07D307/83 , C07D317/46 , C07D319/18 , C07D333/20 , C07D333/36 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14
摘要： There are disclosed compounds of the formula or a pharmaceutically acceptable salt or solvate thereof which are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and cancer.
摘要翻译：公开了可用于治疗趋化因子介导的疾病如急性和慢性炎症性疾病和癌症的下式的化合物或其药学上可接受的盐或溶剂合物。

6. 发明申请

US20100048636A1 Aspartic Protease Inhibitors 失效
标题翻译：天冬氨酸蛋白酶抑制剂
公开(公告)号：US20100048636A1
公开(公告)日：2010-02-25
申请号：US12084928
申请日：2006-11-13
申请人： John J. Baldwin , David A. Claremon , Colin Tice , Salvacion Cacatian , Lawrence W. Dillard , Alexey V. Ishchenko , Jing Yuan , Zhenrong Xu , Gerard McGeehan , Robert D. Simpson , Suresh B. Singh , Wei Zhao , Patrick T. Flaherty
发明人： John J. Baldwin , David A. Claremon , Colin Tice , Salvacion Cacatian , Lawrence W. Dillard , Alexey V. Ishchenko , Jing Yuan , Zhenrong Xu , Gerard McGeehan , Robert D. Simpson , Suresh B. Singh , Wei Zhao , Patrick T. Flaherty
IPC分类号： A61K31/4523 , C07D211/78 , A61K31/445 , C07D405/02 , A61P9/00 , A61P9/12 , A61P9/10
CPC分类号： C07D211/26 , C07D211/22 , C07D401/12 , C07D407/12 , C07D409/06 , C07D417/06 , Y02P20/55
摘要： The present invention is directed to aspartic protease inhibitors. Certain aspartic protease inhibitors of the invention can be represented by the following structural formula or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.
摘要翻译：本发明涉及天冬氨酸蛋白酶抑制剂。本发明的某些天冬氨酸蛋白酶抑制剂可以由以下结构式表示或其药学上可接受的盐。本发明还涉及包含所公开的天冬氨酸蛋白酶抑制剂的药物组合物。本发明还涉及在有需要的受试者中拮抗一种或多种天冬氨酸蛋白酶的方法，以及使用所公开的天冬氨酸蛋白酶抑制剂治疗受试者中天冬氨酸蛋白酶介导的病症的方法。

7. 发明申请

US20090312369A1 Renin Inhibitors 失效
标题翻译：肾素抑制剂
公开(公告)号：US20090312369A1
公开(公告)日：2009-12-17
申请号：US12311012
申请日：2007-09-18
申请人： John J. Baldwin , David A. Claremon , Colin M. Tice , Salvacion Cacatian , Lawrence W. Dillard , Alexey V. Ishchenko , Jing Yuan , Zhenrong Xu , Gerard McGeehan , Wei Zhao , Robert D. Simpson , Suresh B. Singh , Lanqi Jia , Patrick T. Flaherty
发明人： John J. Baldwin , David A. Claremon , Colin M. Tice , Salvacion Cacatian , Lawrence W. Dillard , Alexey V. Ishchenko , Jing Yuan , Zhenrong Xu , Gerard McGeehan , Wei Zhao , Robert D. Simpson , Suresh B. Singh , Lanqi Jia , Patrick T. Flaherty
IPC分类号： A61K31/453 , C07D405/12 , A61P9/10 , A61P9/12 , A61P9/04 , C07D315/00
CPC分类号： C07D309/04 , C07D405/12
摘要： The present invention is directed to aspartic protease inhibitors represented by the following structural formula (I), or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the aspartic protease inhibitors of Structural Formula (I). Methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using these aspartic protease inhibitors are also disclosed.
摘要翻译：本发明涉及由以下结构式（I）表示的天冬氨酸蛋白酶抑制剂或其药学上可接受的盐。本发明还涉及包含结构式（I）的天冬氨酸蛋白酶抑制剂的药物组合物。还公开了在有需要的受试者中拮抗一种或多种天冬氨酸蛋白酶的方法，以及使用这些天冬氨酸蛋白酶抑制剂治疗受试者天冬氨酸蛋白酶介导的病症的方法。

8. 发明申请

US20090306079A1 3,4-DI-SUBSTITUTED CYCLOBUTENE-1,2-DIONES AS CXC-CHEMOKINE RECEPTOR LIGANDS 有权
标题翻译：作为CXC-CHEMOKINE受体配体的3,4-二取代的环己基-1,2-二酮
公开(公告)号：US20090306079A1
公开(公告)日：2009-12-10
申请号：US12352781
申请日：2009-01-13
申请人： Arthur G. Taveras , Cynthia J. Aki , Richard W. Bond , Jianping Chao , Michael Dwyer , Johan A. Ferreira , Jianhua Chao , Younong Yu , John J. Baldwin , Bernd Kaiser , Ge Li , J. Robert Merritt , Purakkattle J. Biju , Kingsley H. Nelson, JR. , Laura L. Rokosz , Gaifa Lai , James P. Jakway , Minglang Wu , Evan A. Hecker , Daniel Lundell , Jay S. Fine
发明人： Arthur G. Taveras , Cynthia J. Aki , Richard W. Bond , Jianping Chao , Michael Dwyer , Johan A. Ferreira , Jianhua Chao , Younong Yu , John J. Baldwin , Bernd Kaiser , Ge Li , J. Robert Merritt , Purakkattle J. Biju , Kingsley H. Nelson, JR. , Laura L. Rokosz , Gaifa Lai , James P. Jakway , Minglang Wu , Evan A. Hecker , Daniel Lundell , Jay S. Fine
IPC分类号： A61K31/535 , C07D401/04 , C07D295/14 , A61P37/02 , A61P9/12 , A61K31/497
CPC分类号： C07C237/30 , C07C225/20 , C07C237/36 , C07C237/44 , C07C255/59 , C07C311/39 , C07C2601/04 , C07C2601/14 , C07C2602/08 , C07D207/335 , C07D213/74 , C07D217/24 , C07D295/26 , C07D307/38 , C07D307/52 , C07D307/68 , C07D307/81 , C07D307/82 , C07D307/83 , C07D317/46 , C07D319/18 , C07D333/20 , C07D333/36 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14
摘要： There are disclosed compounds of the formula or a pharmaceutically acceptable salt or solvate thereof which are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and cancer.
摘要翻译：公开了可用于治疗趋化因子介导的疾病如急性和慢性炎症性疾病和癌症的下式的化合物或其药学上可接受的盐或溶剂合物。

9. 发明授权

US07338968B2 Thiadiazoles AS CXC- and CC- chemokine receptor ligands 失效
标题翻译：噻二唑AS CXC-和CC-趋化因子受体配体
公开(公告)号：US07338968B2
公开(公告)日：2008-03-04
申请号：US11013753
申请日：2004-12-16
申请人： Purakkattle J. Biju , Arthur G. Taveras , J. Robert Merritt , John J. Baldwin , Younong Yu , Junying Zheng , Jianhua Chao , Cynthia J. Aki
发明人： Purakkattle J. Biju , Arthur G. Taveras , J. Robert Merritt , John J. Baldwin , Younong Yu , Junying Zheng , Jianhua Chao , Cynthia J. Aki
IPC分类号： C07D285/10 , A61K31/433
CPC分类号： C07D285/10 , C07D285/06 , C07D417/12 , C07D417/14
摘要： Disclosed are novel compounds of the formula: and the pharmaceutically acceptable salts and solvates thereof. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and ischemia reperfusion injury, pain (e.g., acute pain, acute and chronic inflammatory pain, and neuropathic pain) using a compound of formula IA.
摘要翻译：公开了下式的新化合物及其药学上可接受的盐和溶剂合物。包含取代基A的基团的实例包括杂芳基，芳基，杂环烷基，环烷基，芳基，炔基，烯基，氨基烷基，烷基或氨基。包含取代基B的基团的实例包括芳基和杂芳基。还公开了治疗趋化因子介导的疾病，例如癌症，血管生成，血管生成性眼部疾病，肺部疾病，多发性硬化，类风湿性关节炎，骨关节炎，中风和缺血再灌注损伤，疼痛（例如急性疼痛，急性和慢性炎性疼痛和神经性疼痛），使用式IA化合物。

10. 发明申请

US20080016602A1 Hat With Storage Pockets 审中-公开
标题翻译：帽子与存储口袋
公开(公告)号：US20080016602A1
公开(公告)日：2008-01-24
申请号：US11780968
申请日：2007-07-20
申请人： John J. Baldwin
发明人： John J. Baldwin
IPC分类号： A42B1/24
CPC分类号： A42B1/241
摘要： A contoured hat including a basket portion, a first pocket having a first elastic opening arranged on an outer surface of the basket portion, a brim portion extending outwardly in a first direction away from the basket portion, and a second pocket having a second elastic opening arranged on a surface of the brim portion. The pockets may be contoured and may include a elastic cord for adjustability. The pockets may also be elastically deformable and may contour objects contained therein to inhibit movement of the objects. The hat may be made from a flexible and breathable material throughout.
摘要翻译：包括筐部分的轮廓帽，具有布置在筐部分的外表面上的第一弹性开口的第一袋，沿远离筐部分的第一方向向外延伸的边缘部分和具有第二弹性开口的第二袋布置在边缘部分的表面上。口袋可以是轮廓，并且可以包括用于可调节性的弹性绳。口袋还可以是可弹性变形的，并且可以轮廓包含在其中的物体以抑制物体的移动。帽子可以由柔性和透气材料制成。

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