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1. 发明授权

US10894787B2 Modulators of the GPR119 receptor and the treatment of disorders related thereto 有权
公开(公告)号：US10894787B2
公开(公告)日：2021-01-19
申请号：US13825601
申请日：2011-09-21
申请人： Robert M. Jones , Juerg Lehmann , Weichao Chen , Jeffrey Edwards , Glen Marquez , Michael E. Morgan , Abu J. M. Sadeque , Sun Hee Kim
发明人： Robert M. Jones , Juerg Lehmann , Weichao Chen , Jeffrey Edwards , Glen Marquez , Michael E. Morgan , Abu J. M. Sadeque , Sun Hee Kim
IPC分类号： A61K38/00 , C07D413/14 , A61K31/506 , A61K45/06
摘要： The present invention relates to the GPR119 receptor agonists: 3-fluoro-4-(5-fluoro-6-(4-3-(2-fluoropropan-2-yl)-1,2,4-oxadiazol-5-yl)piperidin-1-yl)pyrimidin-4-ylamino)-N,N-imethylbenzamide; 3-fluoro-4-(5-fluoro-6-(4-(3-(2-fluoropropan-2-yl)-1,2,4-oxadiazol-5-yl)piperidin-1-yl)pyrimidin-4-ylamino)-N-methylbenzamide; and 3-fluoro-4-(5-fluoro-6-(4-(3-(2-fluoropropan-2-yl)-1,2,4-oxadiazol-5-yl)piperidin-1-yl)pyrimidin-4-ylamino)benzamide, and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as a single pharmaceutical agent or in combination with one or more additional pharmaceutical agents, such as, a DPP-IV inhibitor, a biguanide, an alpha-glucosidase inhibitor, an insulin analogue, a sulfonylurea, an SGLT2 inhibitor, a meglitinide, a thiazolidinedione, or an anti-diabetic peptide analogue, in the treatment of, for example, a disorder selected from: a GPRI19-receptor-related disorder; a condition ameliorated by increasing secretion of an incretin; a condition ameliorated by increasing a blood incretin level; a condition characterized by low bone mass; a neurological disorder; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto.

2. 发明申请

US20140051629A1 MODULATORS OF THE GPR119 RECEPTOR AND THE TREATMENT OF DISORDERS RELATED THERETO 审中-公开
标题翻译： GPR119受体的调节剂和与之相关的疾病的治疗
公开(公告)号：US20140051629A1
公开(公告)日：2014-02-20
申请号：US13825601
申请日：2011-09-21
申请人： Robert M. Jones , Juerg Lehmann , Weichao Chen , Jeffrey Edwards , Glen Marquez , Michael E. Morgan , Abu J.M. Sadeque , Sun Hee Kim
发明人： Robert M. Jones , Juerg Lehmann , Weichao Chen , Jeffrey Edwards , Glen Marquez , Michael E. Morgan , Abu J.M. Sadeque , Sun Hee Kim
IPC分类号： C07D413/14 , A61K45/06 , A61K31/506
CPC分类号： C07D413/14 , A61K31/506 , A61K45/06
摘要： The present invention relates to the GPR119 receptor agonists: 3-fluoro-4-(5-fluoro-6-(4-(3-(2-fluoropropan-2-yl)-1,2,4-oxadiazol-5-yl)piperidin-1-yl)pyrimidin-4-ylamino)-N,N-dimethylbenzamide; -fluoro-4-(5-fluoro-6-(4-(3-(2-fluoro-propan-2-yl)-1,2,4-oxadiazol-5-yl)piperidin-1-yl)pyrimidin-4-ylamino)-N-methylbenzamide; and 3-fluoro-4-(5-fluoro-6-(4-(3-(2-fluoropropan-2-yl)-1,2,4-oxadiazol-5-yl)piperidin-1-yl)pyrimidin-4-ylamino)benzamide, and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as a single pharmaceutical agent or in combination with one or more additional pharmaceutical agents, such as, a DPP-IV inhibitor, a biguanide, an alpha-glucosidase inhibitor, an insulin analogue, a sulfonylurea, an SGLT2 inhibitor, a meglitinide, a thiazolidinedione, or an anti-diabetic peptide analogue, in the treatment of for example, a disorder selected from: a GPR119-receptor-related disorder; a condition ameliorated by increasing secretion of an incretin; a condition ameliorated by increasing a blood incretin level; a condition characterized by low bone mass; a neurological disorder; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto.
摘要翻译：本发明涉及GPR119受体激动剂：3-氟-4-（5-氟-6-（4-（3-（2-氟丙-2-基）-1,2,4-恶二唑-5-基）哌啶-1-基）嘧啶-4-基氨基）-N，N-二甲基苯甲酰胺; - 氟-4-（5-氟-6-（4-（3-（2-氟 - 丙-2-基）-1,2,4-恶二唑-5-基）哌啶-1-基）吡啶-4-基氨基）-N-甲基苯甲酰胺; 和3-氟-4-（5-氟-6-（4-（3-（2-氟丙-2-基）-1,2,4-恶二唑-5-基）哌啶-1-基） 4-氨基）苯甲酰胺及其药学上可接受的盐，溶剂合物和水合物，其可用作单一药剂或与一种或多种另外的药剂如DPP-IV抑制剂，双胍类，α 葡萄糖苷酶抑制剂，胰岛素类似物，磺酰脲类，SGLT2抑制剂，氯噻嗪，噻唑烷二酮或抗糖尿病肽类似物，用于治疗例如选自以下的病症：GPR119-受体相关病症; 通过增加肠降血糖素的分泌而改善的状况; 通过增加血液肠降血糖水平来改善病情; 以低骨量为特征的病症; 神经障碍代谢相关疾病; 2型糖尿病; 肥胖; 和相关的并发症。

3. 发明授权

US5256651A Hydrophilic-hydrophobic derivatives of polygalactomannans containing tertiary amine functionality 失效
标题翻译：含有叔胺官能团的聚半乳甘露聚糖的亲水疏水衍生物
公开(公告)号：US5256651A
公开(公告)日：1993-10-26
申请号：US890293
申请日：1992-05-27
申请人： Martha A. Phelps , Michael E. Morgan
发明人： Martha A. Phelps , Michael E. Morgan
IPC分类号： A61K38/00 , C07K14/435 , A61K31/715 , C07H15/04 , C08B37/00
CPC分类号： C07K14/43572 , A61K38/00 , Y10S507/922 , Y10S8/929
摘要： Triple derivatives of polygalactomannan i.e., dialkylaminoalkyl ether-hydroxyalkyl ether - long aliphatic chain ether of polygalactomannan, are useful as thickening agents for aqueous fluids.
摘要翻译：聚半乳甘露聚糖的三元衍生物，即聚半乳甘露聚糖的二烷基氨基烷基醚 - 羟烷基醚 - 长脂族链醚可用作含水流体的增稠剂。

4. 发明授权

US4677201A Titanium-glycol useful as crosslinking agents for polygalactomannans 失效
标题翻译：可用作聚半乳甘露聚糖的交联剂的钛 - 二醇
公开(公告)号：US4677201A
公开(公告)日：1987-06-30
申请号：US830823
申请日：1986-02-19
申请人： Michael E. Morgan
发明人： Michael E. Morgan
IPC分类号： C06B23/00 , C06B45/10 , C08B37/14 , C09K8/68 , C07H1/00
CPC分类号： C06B23/001 , C06B45/10 , C08B37/0087 , C08B37/0096 , C09K8/685 , Y10S507/903 , Y10S507/922
摘要： Aqueous solutions of polygalactomannans are cross-linked with the reaction product of titanium tetrachloride and a water-soluble alcohol or diol further reacted with ammonia or a water-soluble amine. Such crosslinked products are useful in fracturing solutions for secondary oil recovery or in gel explosives.
摘要翻译：聚半乳甘露聚糖的水溶液与四氯化钛和水溶性醇或二醇的反应产物与氨或水溶性胺进一步反应。这种交联产物可用于二次油回收或凝胶炸药的压裂溶液中。

5. 发明授权

US4605736A Titanium-glycol useful, as crosslinking agents, for polygalactomannans 失效
标题翻译：用于聚半乳甘露聚糖的二醇作为交联剂
公开(公告)号：US4605736A
公开(公告)日：1986-08-12
申请号：US743246
申请日：1985-06-11
申请人： Michael E. Morgan
发明人： Michael E. Morgan
IPC分类号： C07F7/00 , C08B37/14 , C09K8/68 , C07H1/00
CPC分类号： C07F7/006 , C08B37/0087 , C08B37/0096 , C09K8/685
摘要： Aqueous solutions of polygalactomannans are crosslinked with the reaction product of titanium tetrachloride and a water-soluble alcohol or diol. Such crosslinked products are useful in fracturing solutions for secondary oil recovery or in gel explosives.
摘要翻译：聚半乳甘露聚糖的水溶液与四氯化钛与水溶性醇或二醇的反应产物交联。这种交联产物可用于二次油回收或凝胶炸药的压裂溶液中。

6. 发明授权

US5233032A Hydrophobically modified hydroxybutyl ethers of polygalactomannan 失效
标题翻译：聚半乳甘露聚糖的疏水改性羟丁基醚
公开(公告)号：US5233032A
公开(公告)日：1993-08-03
申请号：US546560
申请日：1990-06-29
申请人： George M. Zody , Michael E. Morgan
发明人： George M. Zody , Michael E. Morgan
IPC分类号： C08B37/00 , C09K8/62
CPC分类号： C09K8/62 , C08B37/0093 , C08B37/0096 , Y10S507/922
摘要： Polygalactomannans containing a hydroxybutyl ether substituent and a hydrophobic substituent can be used in the fracturing of subterranean formations.
摘要翻译：含有羟丁基醚取代基和疏水性取代基的聚半乳甘露聚糖可以用于地层的压裂。

7. 发明授权

US5179083A Coating composition containing as thickeners polygalactomannans modified with hydrophilic and hydrophobic groups 失效
标题翻译：包含用亲水和疏水基团改性的增稠剂聚半乳甘露聚糖的涂料组合物
公开(公告)号：US5179083A
公开(公告)日：1993-01-12
申请号：US548120
申请日：1990-07-05
申请人： George M. Zody , Michael E. Morgan
发明人： George M. Zody , Michael E. Morgan
IPC分类号： C08B37/00 , C09D7/00
CPC分类号： C09D7/002 , C08B37/0087 , C08L5/00
摘要： Water-borne coating compositions are made, using as a thickening agent, a polygalactomannan having both hydrophilic and hydrophobic substituents.
摘要翻译：使用具有亲水性和疏水性取代基的聚半乳甘露聚糖作为增稠剂制备水性涂料组合物。

8. 发明授权

US4973637A Polymers made from quaternary ammonium acrylic monomers 失效
标题翻译：由季铵丙烯酸单体制成的聚合物
公开(公告)号：US4973637A
公开(公告)日：1990-11-27
申请号：US483374
申请日：1990-02-22
申请人： Michael E. Morgan , Martha A. Phelps
发明人： Michael E. Morgan , Martha A. Phelps
IPC分类号： A61K8/81 , A61Q5/06 , C07C233/36 , C08F20/60
CPC分类号： C08F20/60 , A61K8/8158 , A61Q5/06 , C07C233/36
摘要： Quaternary ammonium containing monomers, represented by the formula: ##STR1## wherein R.sub.1 is H or methyl, R.sub.2 is an alkyl group containing 6 to 22 carbon atoms, D is an alkylene group containing 1 to 4 carbon atoms, or a hydroxylalkylene group containing 2 to 4 carbon atoms and X is an anion, are polymerized to form polymers useful in hair care preparations.
摘要翻译：其中R1为H或甲基，R2为含有6-22个碳原子的烷基，D为含有1至4个碳原子的亚烷基，或含有2个羟基亚烷基的季铵含单体至4个碳原子，X为阴离子，聚合形成可用于护发制剂的聚合物。

9. 发明授权

US4941537A Method for reducing the viscosity of aqueous fluid 失效
标题翻译：降低含水流体粘度的方法
公开(公告)号：US4941537A
公开(公告)日：1990-07-17
申请号：US371651
申请日：1989-06-22
申请人： Paul W. Langemeier , Martha A. Phelps , Michael E. Morgan
发明人： Paul W. Langemeier , Martha A. Phelps , Michael E. Morgan
IPC分类号： C08K3/16 , C08K5/3477 , C09K8/62
CPC分类号： C09K8/62 , C08K3/16 , C08K5/3477 , Y10S507/921 , Y10S507/922
摘要： The viscosity of aqueous fluids thickened with a tertiary amino polygalactomannan is reduced by the addition of an alkali metal or alkaline earth metal salt of hypochlorous acid, or a chlorinated isocyanurate.
摘要翻译：用叔氨基聚半乳甘露聚糖增稠的含水流体的粘度通过加入次氯酸的碱金属或碱土金属盐或氯化异氰脲酸酯而降低。

10. 发明授权

US4918228A Quaternary ammonium acrylic monomers and alcohol soluble polymers made therefrom 失效
标题翻译：季铵盐丙烯酸单体和由其制备的醇溶性聚合物
公开(公告)号：US4918228A
公开(公告)日：1990-04-17
申请号：US313908
申请日：1989-02-23
申请人： Michael E. Morgan , Martha A. Phelps
发明人： Michael E. Morgan , Martha A. Phelps
IPC分类号： A61K8/81 , A61Q5/06 , C07C233/36 , C08F20/60
CPC分类号： A61K8/8158 , A61Q5/06 , C07C233/36 , C08F20/60
摘要： Quaternary ammonium containing monomers, represented by the formula: ##STR1## wherein R.sub.1 is H or methyl, R.sub.2 is an alkyl group containing 6 to 22 carbon atoms, D is an alkylene group containing 1 to 4 carbon atoms, or a hydroxyalkylene group containing 2 to 4 carbon atoms and X is an anion, are polymerized to form polymers useful in hair care preparations.
摘要翻译：由下式表示的含季铵的单体：其中R 1为H或甲基，R 2为含有6至22个碳原子的烷基，D为含有1至4个碳原子的亚烷基或含有2个的羟基亚烷基至4个碳原子，X为阴离子，聚合形成可用于护发制剂的聚合物。

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