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1. 发明申请

WO2012012339A4 GLYCOSYLATED ACETAMINOPHEN PRO-DRUG ANALOGS 审中-公开
标题翻译：甘氨酸乙酰胺类药物类似物
公开(公告)号：WO2012012339A4
公开(公告)日：2013-07-11
申请号：PCT/US2011044383
申请日：2011-07-18
申请人： NUTEK PHARMA LTD , SHULL BRIAN , BALDWIN JOHN , GOPALASWAMY RAMESH , HAROON ZISHAN
发明人： SHULL BRIAN , BALDWIN JOHN , GOPALASWAMY RAMESH , HAROON ZISHAN
IPC分类号： A01N43/04 , A61K31/70 , C07G3/00
CPC分类号： C07H15/203
摘要： The present invention relates to methods and compositions for the synthesis, production, and use of pro-drug analogs of the analgesic acetaminophen. This invention relates to a method for the production of a broad group of glycosides of acetaminophen derivatives.
摘要翻译：本发明涉及用于合成，制备和使用止痛对乙酰氨基酚的前药类似物的方法和组合物。本发明涉及一种生产广泛的对乙酰氨基酚衍生物糖苷的方法。

2. 发明申请

WO2006047302A1 BISSULFONAMIDE COMPOUNDS AS AGONISTS OF GALR1, COMPOSITIONS, AND METHODS OF USE 审中-公开
标题翻译：作为GALR1，组合物和使用方法的双酚A化合物
公开(公告)号：WO2006047302A1
公开(公告)日：2006-05-04
申请号：PCT/US2005/037932
申请日：2005-10-20
申请人： TRANSTECH PHARMA, INC. , MJALLI, Adnan, M.M. , GADDAM, Bapu , RAO, Mohan , BONDLELA, Muralidhar , GOPALASWAMY, Ramesh , ANDREWS, Robert, C. , DAVIS, Stephen , SIMILA, Suvi , REN, Tan
发明人： MJALLI, Adnan, M.M. , GADDAM, Bapu , RAO, Mohan , BONDLELA, Muralidhar , GOPALASWAMY, Ramesh , ANDREWS, Robert, C. , DAVIS, Stephen , SIMILA, Suvi , REN, Tan
IPC分类号： C07D333/62 , C07D233/54 , C07D333/34 , C07D413/04 , C07D307/82 , C07D409/12 , C07D413/12 , C07D495/04 , C07D213/42 , C07C311/29 , A61K31/381 , A61K31/343 , A61K31/4436 , A61K31/18
CPC分类号： C07D213/42 , C07C311/29 , C07D233/54 , C07D307/82 , C07D333/34 , C07D333/62 , C07D409/12 , C07D413/04 , C07D413/12 , C07D495/04
摘要： Embodiments of the present invention provide bissulfonamide compounds that are agonists of GalR1. The present invention further provides compositions comprising bissulfonamide compounds that are agonists of GalR1, and methods of use of such compounds and compositions.
摘要翻译：本发明的实施方案提供作为GalR1的激动剂的双磺酰胺化合物。本发明还提供了包含作为GalR1的激动剂的双磺酰胺化合物的组合物，以及这些化合物和组合物的使用方法。

3. 发明申请

WO2002069965A1 BENZIMIDAZOLE DERIVATIVES AS THERAPEUTIC AGENTS 审中-公开
标题翻译：苯扎咪唑衍生物作为治疗剂
公开(公告)号：WO2002069965A1
公开(公告)日：2002-09-12
申请号：PCT/US2002/006706
申请日：2002-03-05
申请人： TRANSTECH PHARMA, INC. , MJALLI, Adnan, M., M. , GOPALASWAMY, Ramesh
发明人： MJALLI, Adnan, M., M. , GOPALASWAMY, Ramesh
IPC分类号： A61K31/4184
CPC分类号： A61K31/4188 , C07D235/14 , C07D235/16
摘要： This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, ß-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.
摘要翻译：本发明提供某些化合物，其制备方法，包含该化合物的药物组合物及其在治疗人或动物疾病中的用途。本发明的化合物可用作晚期糖基化终产物（RAGE）的受体与其配体如晚期糖基化终产物（AGE），S100 /钙粒蛋白/ EN-RAGE，β-淀粉样蛋白和两性蛋白之间相互作用的调节剂，以及由RAGE引起的人类疾病的管理，治疗，控制或辅助治疗。这些疾病或疾病状态包括急性和慢性炎症，糖尿病晚期并发症的发展，例如血管通透性增加，肾病，动脉粥样硬化和视网膜病变，阿尔茨海默病的发展，勃起功能障碍和肿瘤侵袭和转移。

4. 发明申请

WO2012012339A2 GLYCOSYLATED ACETAMINOPHEN PRO-DRUG ANALOGS 审中-公开
标题翻译：甘氨酸乙酰胺类药物类似物
公开(公告)号：WO2012012339A2
公开(公告)日：2012-01-26
申请号：PCT/US2011/044383
申请日：2011-07-18
申请人： NUTEK PHARMA LTD. , SHULL, Brian , BALDWIN, John , GOPALASWAMY, Ramesh , HAROON, Zishan
发明人： SHULL, Brian , BALDWIN, John , GOPALASWAMY, Ramesh , HAROON, Zishan
IPC分类号： A61K31/7036 , C07H15/22 , A61P25/04
CPC分类号： C07H15/203
摘要： The present invention relates to methods and compositions for the synthesis, production, and use of pro-drug analogs of the analgesic acetaminophen. This invention relates to a method for the production of a broad group of glycosides of acetaminophen derivatives.
摘要翻译：本发明涉及用于合成，制备和使用止痛对乙酰氨基酚的前药类似物的方法和组合物。本发明涉及一种生产广泛的对乙酰氨基酚衍生物糖苷的方法。

5. 发明申请

WO2003075921A2 MONO- AND BICYCLIC AZOLE DERIVATIVES THAT INHIBIT THE INTERACTION OF LIGANDS WITH RAGE 审中-公开
标题翻译：抑制配偶与RAGE相互作用的单体和双相性氨基酸衍生物
公开(公告)号：WO2003075921A2
公开(公告)日：2003-09-18
申请号：PCT/US2003/006749
申请日：2003-03-05
申请人： TRANSTECH PHARMA, INC. , MJALLI, Adnan, M., M. , ANDREWS, Robert, C. , GOPALASWAMY, Ramesh , HARI, Anitha , AVOR, Kwasi , QABAJA, Ghassan , GUO, Xiao-Chuan , GUPTA, Suparna , JONES, David, R. , CHEN, Xin
发明人： MJALLI, Adnan, M., M. , ANDREWS, Robert, C. , GOPALASWAMY, Ramesh , HARI, Anitha , AVOR, Kwasi , QABAJA, Ghassan , GUO, Xiao-Chuan , GUPTA, Suparna , JONES, David, R. , CHEN, Xin
IPC分类号： A61K31/4184
CPC分类号： C07D233/64 , C07D235/08 , C07D235/12 , C07D235/14 , C07D235/18 , C07D235/30 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/12 , C07D413/12 , C07D453/02
摘要： This invention provides certain compounds of formula I wherein A 1 is O, S or -N(R 2 )-, and methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, β-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer’s disease, erectile dysfunction, and tumor invasion and metastasis.
摘要翻译：本发明提供某些其中A1是O，S或-N（R2） - 的式I化合物及其制备方法，包含该化合物的药物组合物及其在治疗人或动物病症中的用途。本发明的化合物可用作晚期糖基化终产物（RAGE）的受体与其配体如晚期糖基化终产物（AGE），S100 /钙粒蛋白/ EN-RAGE，β-淀粉样蛋白和两性蛋白之间的相互作用的调节剂，以及由RAGE引起的人类疾病的管理，治疗，控制或辅助治疗。这些疾病或疾病状态包括急性和慢性炎症，糖尿病晚期并发症的发展，例如血管通透性增加，肾病，动脉粥样硬化和视网膜病变，阿尔茨海默病的发展，勃起功能障碍和肿瘤侵袭和转移。

6. 发明申请

WO2012012339A3 GLYCOSYLATED ACETAMINOPHEN PRO-DRUG ANALOGS 审中-公开
标题翻译：糖基化ACETAMINOPHEN PRO-DRUG类似物
公开(公告)号：WO2012012339A3
公开(公告)日：2012-04-12
申请号：PCT/US2011044383
申请日：2011-07-18
申请人： NUTEK PHARMA LTD , SHULL BRIAN , BALDWIN JOHN , GOPALASWAMY RAMESH , HAROON ZISHAN
发明人： SHULL BRIAN , BALDWIN JOHN , GOPALASWAMY RAMESH , HAROON ZISHAN
IPC分类号： A01N43/04 , A61K31/70 , C07G3/00
CPC分类号： C07H15/203
摘要： The present invention relates to methods and compositions for the synthesis, production, and use of pro-drug analogs of the analgesic acetaminophen. This invention relates to a method for the production of a broad group of glycosides of acetaminophen derivatives.
摘要翻译：本发明涉及用于合成，生产和使用镇痛药对乙酰氨基酚的前药类似物的方法和组合物。本发明涉及生产对乙酰氨基酚衍生物的一大组糖苷的方法。

7. 发明申请

WO2012142147A2 SYNTHESIS AND USE OF GLYCOSIDE DERIVATIVES OF PROPOFOL 审中-公开
标题翻译：丙泊酚糖苷衍生物的合成与应用
公开(公告)号：WO2012142147A2
公开(公告)日：2012-10-18
申请号：PCT/US2012033105
申请日：2012-04-11
申请人： NUTEK PHARMA LTD , SHULL BRIAN , BALDWIN JOHN , GOPALASWAMY RAMESH , HAROON ZISHAN
发明人： SHULL BRIAN , BALDWIN JOHN , GOPALASWAMY RAMESH , HAROON ZISHAN
IPC分类号： G01N21/59 , B05D3/00 , B05D7/00
CPC分类号： C07H15/18 , A61K31/7028 , C07H5/10 , C07H15/04 , C07H15/203 , C07H15/26
摘要： The present invention relates to methods and compositions for the synthesis, production, and use of pro-drug propofol analogs. This invention relates to a method for the production of a broad group of glycosylated propofol carbohydrate derivatives.
摘要翻译：本发明涉及用于前药丙泊酚类似物的合成，生产和使用的方法和组合物。本发明涉及生产广泛的糖基化丙泊酚碳水化合物衍生物的方法。

8. 发明申请

WO2012142147A3 SYNTHESIS AND USE OF GLYCOSIDE DERIVATIVES OF PROPOFOL 审中-公开
公开(公告)号：WO2012142147A3
公开(公告)日：2012-10-18
申请号：PCT/US2012/033105
申请日：2012-04-11
申请人： NUTEK PHARMA LTD. , SHULL, Brian , BALDWIN, John , GOPALASWAMY, Ramesh , HAROON, Zishan
发明人： SHULL, Brian , BALDWIN, John , GOPALASWAMY, Ramesh , HAROON, Zishan
IPC分类号： A61K9/14
摘要： The present invention relates to methods and compositions for the synthesis, production, and use of pro-drug propofol analogs. This invention relates to a method for the production of a broad group of glycosylated propofol carbohydrate derivatives.

9. 发明申请

WO2012142141A1 SYNTHESIS AND USE OF GLYCOSIDE PRO-DRUG ANALOGS 审中-公开
标题翻译：合成和使用糖苷类药物类似物
公开(公告)号：WO2012142141A1
公开(公告)日：2012-10-18
申请号：PCT/US2012/033098
申请日：2012-04-11
申请人： NUTEK PHARMA LTD. , SHULL, Brian , BALDWIN, John , GOPALASWAMY, Ramesh , HAROON, Zishan
发明人： SHULL, Brian , BALDWIN, John , GOPALASWAMY, Ramesh , HAROON, Zishan
IPC分类号： A61K31/70 , C07G3/00
CPC分类号： C07H15/18 , C07H15/26
摘要： The present invention relates to methods and compositions for the synthesis, production, and use of pro-drug analogs. This invention relates to a method for the production of a broad group of glycosylated drugs, including but not limited to propofol, acetaminophen, and camptothecin carbohydrate derivatives.
摘要翻译：本发明涉及用于合成，生产和使用前体药物类似物的方法和组合物。本发明涉及生产广泛的糖基化药物的方法，包括但不限于异丙酚，对乙酰氨基酚和喜树碱碳水化合物衍生物。

10. 发明申请

WO2007095124A3 BENZAZOLE DERIVATIVES, COMPOSITIONS, AND METHODS OF USE AS AURORA KINASE INHIBITORS 审中-公开
标题翻译：苯并噻唑衍生物，组合物和使用作为AURORA激酶抑制剂的方法
公开(公告)号：WO2007095124A3
公开(公告)日：2007-11-01
申请号：PCT/US2007003579
申请日：2007-02-09
申请人： TRANSTECH PHARMA INC , MJALLI ADNAN M M , GRELLA BRIAN S , SUBRAMANIAN GOVINDAN , ARIMILLI MURTY N , GOPALASWAMY RAMESH , ANDREWS ROBERT C , DAVIS STEPHEN , GUO XIAOCHUAN , ZHU JEFF
发明人： MJALLI ADNAN M M , GRELLA BRIAN S , SUBRAMANIAN GOVINDAN , ARIMILLI MURTY N , GOPALASWAMY RAMESH , ANDREWS ROBERT C , DAVIS STEPHEN , GUO XIAOCHUAN , ZHU JEFF
IPC分类号： C07D417/12 , A61K31/416 , A61K31/4184 , A61P35/00 , C07D403/12
CPC分类号： C07D417/14 , C07D401/14 , C07D403/12 , C07D403/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D487/04
摘要： The present invention relates to compounds and methods from the treatment of cancer. The invention provides compounds that inhibit Aurora kinase, pharmaceutical compositions comprising compounds that inhibit Aurora kinase, and methods for the treatment of cancer using the compounds of the presentation invention or pharmaceutical compositions comprising compounds of the present invention.
摘要翻译：本发明涉及治疗癌症的化合物和方法。本发明提供抑制极光激酶的化合物，包含抑制极光激酶的化合物的药物组合物，以及使用本发明化合物或包含本发明化合物的药物组合物治疗癌症的方法。

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