专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US09458136B2 Crystalline forms and processes for the preparation of cannabinoid receptor modulators 有权
标题翻译：用于制备大麻素受体调节剂的结晶形式和方法
公开(公告)号：US09458136B2
公开(公告)日：2016-10-04
申请号：US14001133
申请日：2012-02-24
申请人： Anthony C. Blackburn , Sangdon Han , Robert M. Jones , Antonio Garrido Montalban , Biman B. Pal , Jaimie Karyn Rueter
发明人： Anthony C. Blackburn , Sangdon Han , Robert M. Jones , Antonio Garrido Montalban , Biman B. Pal , Jaimie Karyn Rueter
IPC分类号： A61K31/4965 , C07D403/04 , A61K31/497
CPC分类号： C07D403/04 , A61K31/497 , A61P29/00 , C07B2200/13
摘要： The present invention relates to crystalline forms of (1aS,5aS)-2-(4-oxy-pyrazin-2-yl)-1a,2,5,5a-tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalene-4-carboxylic acid ((S)-1-hydroxymethyl-2,2-dimethyl-propyl)-amide (Compound 1) and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor and are therefore useful in the treatment of CB2 receptor-mediated disorders, for example, osteoarthritis; pain; hyperalgesia; allodynia; inflammatory hyperalgesia; neuropathic hyperalgesia; acute nociception; osteoporosis; multiple sclerosis-associated spasticity; autoimmune disorders; allergic reactions; CNS inflammation for example; atherosclerosis; undesired immune cell activity, and inflammation associated with a disorder selected from: osteoarthritis, anaphylaxis, Behcet's disease, graft rejection, vasculitis, gout, spondylitis, viral disease, bacterial disease, lupus, inflammatory bowel disease, autoimmune hepatitis, and type 1 diabetes mellitus; age-related macular degeneration; cough; leukemia; lymphoma; CNS tumors; prostate cancer; Alzheimer's disease; stroke-induced damage; dementia; amyotrophic lateral sclerosis; and Parkinson's disease.
摘要翻译：本发明涉及（1aS，5aS）-2-（4-氧 - 吡嗪-2-基）-1a，2,5,5a-四氢-1H-2,3-二氮杂 - 环丙烷[a] 顺式-4-羧酸（（S）-1-羟甲基-2,2-二甲基 - 丙基） - 酰胺（化合物1）及其药物组合物，其调节大麻素CB2受体的活性，因此可用于治疗 CB2受体介导的疾病，例如骨关节炎; 疼痛; 痛觉过敏异常性疼痛炎性痛觉过敏; 神经性痛觉过敏; 急性伤害感受骨质疏松症多发性硬化相关性痉挛状态; 自身免疫性疾病过敏反应; CNS炎症例如; 动脉粥样硬化不良免疫细胞活性和与选自以下的疾病相关的炎症：骨关节炎，过敏反应，贝切特氏病，移植排斥反应，血管炎，痛风，脊椎炎，病毒性疾病，细菌性疾病，狼疮，炎性肠病，自身免疫性肝炎和1型糖尿病 ; 年龄相关性黄斑变性; 咳嗽; 白血病; 淋巴瘤 CNS肿瘤; 前列腺癌; 阿尔茨海默氏病; 中风引起的损伤; 痴呆; 肌萎缩性侧索硬化; 和帕金森病。

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. 发明申请

US20140018371A1 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：US20140018371A1
公开(公告)日：2014-01-16
申请号：US14007759
申请日：2012-03-30
申请人： Robert M. Jones , Sangdon Han , Juerg Lehmann , Lars Thoresen
发明人： Robert M. Jones , Sangdon Han , Juerg Lehmann , Lars Thoresen
IPC分类号： A61K31/506 , C07D413/04 , A61K31/454 , C07D401/12 , A61K45/06 , A61K31/497 , C07D401/14 , C07D211/24 , C07D401/06 , A61K31/445 , A61K31/4545
CPC分类号： A61K31/506 , A61K31/445 , A61K31/454 , A61K31/4545 , A61K31/497 , A61K45/06 , C07D211/22 , C07D211/24 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D413/04 , C07D413/06
摘要： The present invention relates to compounds of Formula (Ia) and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as a single agent or in combination with one or more pharmaceutical agents, such as, an inhibitor of DPP-IV, a biguanide, or an alpha-glucosidase inhibitor, in the treatment of, for example, a disorder selected from: a GPR119-receptor-related disorder; a condition ameliorated by increasing a blood incretin level; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto.
摘要翻译：本发明涉及式（Ia）化合物及其药学上可接受的盐，溶剂合物和水合物，其可用作单一试剂或与一种或多种药剂组合使用，例如DPP-IV抑制剂，双胍或α-葡糖苷酶抑制剂，用于治疗例如选自以下的病症：GPR119-受体相关病症; 通过增加血液肠降血糖水平来改善病情; 代谢相关疾病; 2型糖尿病; 肥胖; 和相关的并发症。

4. 发明授权

US08410119B2 Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto 失效
公开(公告)号：US08410119B2
公开(公告)日：2013-04-02
申请号：US12567221
申请日：2009-09-25
申请人： Robert M. Jones , Graeme Semple , Yifeng Xiong , Young-Jun Shin , Albert S. Ren , Imelda Calderon , Beatriz Fioravanti , Jin Sun Choi , Carleton R. Sage
发明人： Robert M. Jones , Graeme Semple , Yifeng Xiong , Young-Jun Shin , Albert S. Ren , Imelda Calderon , Beatriz Fioravanti , Jin Sun Choi , Carleton R. Sage
IPC分类号： A61K31/519 , C07D487/00
CPC分类号： C07D215/233 , C07D471/04 , C07D473/00 , C07D487/04
摘要： The present invention relates to certain fused aryl and heteroaryl derivatives of Formula (I) that are modulators of metabolism. Accordingly, compounds of the present invention are useful in the prophylaxis or treatment of metabolic disorders and complications thereof, such as, diabetes and obesity.

5. 发明申请

US20130023527A1 1,2,3-Trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto such as diabetes and hyperglycemia 有权
标题翻译： 1,2,3-三取代的芳基和杂芳基衍生物作为代谢调节剂以及与之相关疾病的预防和治疗，如糖尿病和高血糖
公开(公告)号：US20130023527A1
公开(公告)日：2013-01-24
申请号：US13618592
申请日：2012-09-14
申请人： Robert M. Jones , Graeme Semple , Beatriz Fioravanti , Guilherme Pereira , Imelda Calderon , Jane Laguerta Uy , Kameshwari Duvvuri , Jin Sun Karoline Choi , Yifeng Xiong , Vibha Dave , Mihai D. Azimioara
发明人： Robert M. Jones , Graeme Semple , Beatriz Fioravanti , Guilherme Pereira , Imelda Calderon , Jane Laguerta Uy , Kameshwari Duvvuri , Jin Sun Karoline Choi , Yifeng Xiong , Vibha Dave , Mihai D. Azimioara
IPC分类号： A61K31/506 , A61K31/451 , A61K31/541 , A61P3/10 , A61P3/04 , A61P3/06 , A61K31/4545 , A61P3/00
CPC分类号： C07D213/68 , C07D213/79 , C07D239/34 , C07D239/50 , C07D295/096 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/14 , C07D411/14 , C07D413/14 , C07D417/14 , C07D419/14
摘要： The present invention relates to certain 1,2,3-trisubstituted aryl and heteroaryl derivatives of Formula (Ia) that are modulators of metabolism. Accordingly, compounds of the present invention are useful in the prophylaxis or treatment of metabolic disorders and complications thereof, such as, diabetes and obesity.
摘要翻译：本发明涉及作为代谢调节剂的式（Ia）的某些1,2,3-三取代的芳基和杂芳基衍生物。因此，本发明的化合物可用于预防或治疗代谢紊乱及其并发症，例如糖尿病和肥胖症。

6. 发明申请

US20130023494A1 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：US20130023494A1
公开(公告)日：2013-01-24
申请号：US13639652
申请日：2011-04-05
申请人： Robert M. Jones , Sangdon Han , Daniel J. Buzard , Juerg Lehmann , Sanju Narayanan , Dawei Yue
发明人： Robert M. Jones , Sangdon Han , Daniel J. Buzard , Juerg Lehmann , Sanju Narayanan , Dawei Yue
IPC分类号： A61K31/445 , C07D413/04 , A61K31/454 , C07D401/04 , A61K31/506 , C07D401/14 , C07D401/12 , A61K31/497 , A61K31/501 , C07D417/14 , A61K31/541 , A61K31/4523 , A61P19/00 , A61P25/00 , A61P3/00 , A61P3/10 , A61P3/04 , A61K31/4985 , A61K31/69 , A61K31/4745 , A61K31/522 , A61K31/53 , A61K31/519 , C07D211/46
CPC分类号： C07D211/46 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D413/04 , C07D413/06 , C07D413/14 , C07D417/14
摘要： The present invention relates to compounds of Formula (Ia) and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as a single agent or in combination with one or more additional pharmaceutical agents, such as, an inhibitor of DPP-IV, a biguanide, an SGLT2 inhibitor, or an alpha-glucosidase inhibitor, in the treatment of, for example, a disorder selected from: a GPR119-receptor-related disorder; a condition ameliorated by increasing a blood incretin level; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto.
摘要翻译：本发明涉及式（Ia）化合物及其药学上可接受的盐，溶剂合物和水合物，其可用作单一试剂或与一种或多种另外的药剂如DPP-IV抑制剂组合使用，双胍类，SGLT2抑制剂或α-葡糖苷酶抑制剂，用于治疗例如选自以下的病症：GPR119-受体相关病症; 通过增加血液肠降血糖水平来改善病情; 代谢相关疾病; 2型糖尿病; 肥胖; 和相关的并发症。

7. 发明授权

US07994675B2 Generic crimped rotor for an electric brushless direct current motor 有权
标题翻译：用于电动无刷直流电动机的通用卷曲转子
公开(公告)号：US07994675B2
公开(公告)日：2011-08-09
申请号：US12569890
申请日：2009-09-29
申请人： Robert M. Jones , Joseph M. Lisiecki
发明人： Robert M. Jones , Joseph M. Lisiecki
IPC分类号： H02K1/30
CPC分类号： H02K1/278 , H02K3/38 , H02K5/04 , H02K5/18 , H02K5/225 , H02K11/33 , H02K16/00 , H02K21/16 , H02K29/08 , H02K2213/12
摘要： A rotor having a substantially cylindrical configuration for use in a brushless direct current electric motor having a high torque to size ratio. The rotor has an outer peripheral surface. The rotor also has a central rotor shaft and a first and second retaining ends mounted on the central rotor shaft and spaced from one another. The rotor also has a plurality of magnets configured to provide a magnetic flux with a stator disposed around the central rotor shaft. The magnets are radially disposed on the shaft and the rotor also has a sheath. The sheath is crimped around the radially disposed permanent magnets, and holds the magnets around the shaft. The sheath is lightweight and minimizes a gap between the permanent magnets and the stator to provide for an electromagnetic flux between the magnets and the stator windings, and for rotation of the central rotor shaft.
摘要翻译：具有大体圆柱形构造的转子，用于具有高扭矩与大尺寸比的无刷直流电动机。转子具有外周面。转子还具有中心转子轴和安装在中心转子轴上并彼此间隔开的第一和第二保持端。转子还具有多个磁体，其被配置为提供磁通量，该定子设置在中心转子轴周围。磁体径向设置在轴上，转子也具有护套。鞘被卷绕在径向设置的永磁体周围，并将磁体保持在轴周围。护套是轻质的，并且使永磁体和定子之间的间隙最小化，以提供磁体和定子绕组之间的电磁通量，并且用于中心转子轴的旋转。

8. 发明申请

US20110130409A1 SUBSTITUTED 1,2,3,4-TETRAHYDROCYCLOPENTA[B]INDOL-3-YL)ACETIC ACID DERIVATIVES USEFUL IN THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISORDERS 有权
标题翻译：取代的1,2,3,4-四氢环戊二烯并[B]吲哚-3-基）乙酸衍生物用于治疗自身免疫和炎症性疾病
公开(公告)号：US20110130409A1
公开(公告)日：2011-06-02
申请号：US13055333
申请日：2009-07-22
申请人： Robert M. Jones , Daniel J. Buzard , Sangdon Han , Sun Hee Kim , Juerg Lehmann , Brett Ullman , Jeanne V. Moody , Xiuwen Zhu , Scott Stirn
发明人： Robert M. Jones , Daniel J. Buzard , Sangdon Han , Sun Hee Kim , Juerg Lehmann , Brett Ullman , Jeanne V. Moody , Xiuwen Zhu , Scott Stirn
IPC分类号： A61K31/497 , C07D209/94 , C07D403/12 , C07D401/12 , C07D417/12 , A61K31/403 , A61K31/4439 , A61K31/433 , A61P37/06 , A61P29/00 , A61P35/00 , A61P17/06 , A61P25/28 , A61P3/10 , A61P1/00 , A61P17/10 , A61P31/00 , A61P31/12
CPC分类号： C07D209/94 , A61K31/137 , A61K31/198 , A61K31/404 , A61K31/433 , A61K31/4439 , A61K31/497 , C07C211/27 , C07C229/26 , C07C255/03 , C07C279/14 , C07D209/70 , C07D209/88 , C07D401/12 , C07D401/14 , C07D403/12 , C07D417/12 , Y02A50/475
摘要： The present invention relates to certain substituted 1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid derivatives of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1 receptor-associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, microbial infections or diseases and viral infections or diseases.
摘要翻译：本发明涉及式（Ia）的某些取代的1,2,3,4-四氢环戊并[b]吲哚-3-基）乙酸衍生物及其药学上可接受的盐，其表现出有用的药理学性质，例如作为激动剂的S1P1受体。本发明还提供含有本发明化合物的药物组合物，以及使用本发明化合物和组合物治疗S1P1受体相关疾病例如牛皮癣，类风湿性关节炎，克罗恩病，移植排斥反应的方法，多发性硬化症，系统性红斑狼疮，溃疡性结肠炎，I型糖尿病，痤疮，微生物感染或疾病以及病毒感染或疾病。

9. 发明申请

US20100210666A1 METHODS OF USING A G PROTEIN-COUPLED RECEPTOR TO IDENTIFY PEPTIDE YY (PYY) SECRETAGOGUES AND COMPOUNDS USEFUL IN THE TREATMENT OF CONDITIONS MODULATED BY PYY 审中-公开
标题翻译：使用G蛋白偶联受体鉴定PYY（PYY）秘密肽和化合物的方法可用于治疗由PYY调节的病症
公开(公告)号：US20100210666A1
公开(公告)日：2010-08-19
申请号：US12765414
申请日：2010-04-22
申请人： Zhi-Liang Chu , James N. Leonard , Robert M. Jones
发明人： Zhi-Liang Chu , James N. Leonard , Robert M. Jones
IPC分类号： A61K31/506 , C12Q1/02 , A61P9/00 , A61P35/00 , A61P29/00 , A61P3/00
CPC分类号： G01N33/68 , G01N33/5044 , G01N2333/726 , G01N2800/042 , G01N2800/044 , G01N2800/065 , G01N2800/108 , G01N2800/323
摘要： The present invention relates to methods of using GPR119 receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditions modulated by PYY, such as conditions modulated by stimulation of NPY Y2 receptor (Y2R). Agonists of GPR119 receptor are useful as therapeutic agents for treating or preventing a condition modulated by PYY, such as a condition modulated by stimulation of Y2R. Conditions modulated by PYY such as may be a condition modulated by stimulation of Y2R include bone-related conditions, metabolic disorders, angiogenesis-related conditions, ischemia-related conditions, convulsive disorders, malabsorptive disorders, cancers, and inflammatory disorders.
摘要翻译：本发明涉及使用GPR119受体鉴定肽YY（PYY）促分泌素和可用于治疗由PYY调节的病症的化合物的方法，例如通过刺激NPY Y2受体（Y2R）调节的病症。 GPR119受体的激动剂可用作治疗或预防由PYY调节的病症的治疗剂，例如通过刺激Y2R调节的病症。由PYY调节的病症例如可能是通过Y2R刺激调节的病症包括骨相关病症，代谢紊乱，血管生成相关病症，缺血相关病症，惊厥症，吸收不良障碍，癌症和炎症性疾病。

10. 发明申请

US20100203556A1 METHODS OF USING A G PROTEIN-COUPLED RECEPTOR TO IDENTIFY PEPTIDE YY (PYY) SECRETAGOGUES AND COMPOUNDS USEFUL IN THE TREATMENT OF CONDITIONS MODULATED BY PYY 失效
公开(公告)号：US20100203556A1
公开(公告)日：2010-08-12
申请号：US12765406
申请日：2010-04-22
申请人： Zhi-Liang Chu , James N. Leonard , Robert M. Jones
发明人： Zhi-Liang Chu , James N. Leonard , Robert M. Jones
IPC分类号： G01N33/53 , C12Q1/02
CPC分类号： G01N33/68 , G01N33/5044 , G01N2333/726 , G01N2800/042 , G01N2800/044 , G01N2800/065 , G01N2800/108 , G01N2800/323
摘要： The present invention relates to methods of using GPR119 receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditions modulated by PYY, such as conditions modulated by stimulation of NPY Y2 receptor (Y2R). Agonists of GPR119 receptor are useful as therapeutic agents for treating or preventing a condition modulated by PYY, such as a condition modulated by stimulation of Y2R. Conditions modulated by PYY such as may be a condition modulated by stimulation of Y2R include bone-related conditions, metabolic disorders, angiogenesis-related conditions, ischemia-related conditions, convulsive disorders, malabsorptive disorders, cancers, and inflammatory disorders.

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式