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1. 发明申请

WO2018118827A1 HETEROCYCLIC COMPOUNDS AS HIV PROTEASE INHIBITORS 审中-公开
公开(公告)号：WO2018118827A1
公开(公告)日：2018-06-28
申请号：PCT/US2017/067160
申请日：2017-12-19
申请人： MERCK SHARP & DOHME CORP. , MCKITTRICK, Brian , CALDWELL, John, P. , MCCAULEY, John, A. , VACCARO, Henry , CHAN, Tin-Yau , KIM, Hyunjin , SMITH, Elizabeth , HONG, Liwu , KHAN, Tanweer , YING, Shihong , WANG, Hongwu
发明人： MCKITTRICK, Brian , CALDWELL, John, P. , MCCAULEY, John, A. , VACCARO, Henry , CHAN, Tin-Yau , KIM, Hyunjin , SMITH, Elizabeth , HONG, Liwu , KHAN, Tanweer , YING, Shihong , WANG, Hongwu
IPC分类号： A61K31/18 , C07C311/21 , C07D417/04 , A61K31/4439 , C07D317/68 , A61K31/36
摘要： The present invention is directed to compounds of Formula I, pharmaceutical compositions comprising the same, and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS.

2. 发明申请

WO2008033464A3 AZETIDINONE DERIVATIVES FOR THE TREATMENT OF DISORDERS OF THE LIPID METABOLISM 审中-公开
标题翻译：用于治疗脂肪代谢紊乱的AZETIDINONE衍生物
公开(公告)号：WO2008033464A3
公开(公告)日：2008-05-15
申请号：PCT/US2007019930
申请日：2007-09-13
申请人： SCHERING CORP , ASLANIAN ROBERT G , BENNETT CHAD E , BURNETT DUANE A , CHAN TIN-YAU , KISELGOF EUGENIA Y , KNUTSON CHAD E , HARRIS JOEL M , MC KITTRICK BRIAN A , PALANI ANANDAN , SMITH ELIZABETH M , VACCARO HENRY M , XIAO DONG , KIM HYUNJIN M
发明人： ASLANIAN ROBERT G , BENNETT CHAD E , BURNETT DUANE A , CHAN TIN-YAU , KISELGOF EUGENIA Y , KNUTSON CHAD E , HARRIS JOEL M , MC KITTRICK BRIAN A , PALANI ANANDAN , SMITH ELIZABETH M , VACCARO HENRY M , XIAO DONG , KIM HYUNJIN M
IPC分类号： C07D471/10 , A61K31/438 , A61P3/00
CPC分类号： C07D471/10
摘要： The present invention relates to Azetidinone Derivatives, compositions comprising an Azetidinone Derivative and methods for treating or preventing a disorder of lipid metabolism, pain, diabetes, a vascular condition, demyelination or nonalcoholic fatty liver disease, comprising administering to a patient an effective amount of an Azetidinone Derivative.
摘要翻译：本发明涉及氮杂环丁酮衍生物，包含氮杂环丁酮衍生物的组合物和用于治疗或预防脂质代谢紊乱，疼痛，糖尿病，血管病症，脱髓鞘或非酒精性脂肪性肝病的方法，包括向患者施用有效量的氮杂环丁酮衍生物。

3. 发明申请

WO2008004899A2 METHOD AND APPARATUS FOR FORMULATING INDIVIDUALISED DOSES OF NUTRITION 审中-公开
标题翻译：用于制定个体营养剂量的方法和装置
公开(公告)号：WO2008004899A2
公开(公告)日：2008-01-10
申请号：PCT/NZ2007000171
申请日：2007-07-06
申请人： ALEXANDER DAVID LIONEL JAMES , ARCHER RICHARD , XIAO HUANG , SMITH ELIZABETH ANNE
发明人： ALEXANDER DAVID LIONEL JAMES , ARCHER RICHARD , XIAO HUANG , SMITH ELIZABETH ANNE
CPC分类号： A23L33/15 , A23L33/10
摘要： The invention in one form provides a nutrient dosage formulation system. The system comprises a nutrition table maintained in computer memory; a customer profile table maintained in computer memory; an overall dose calculator configured to retrieve selected codified dose values from at least one row of the nutrition table based on the health condition values of a row of the customer profile table and to calculate an overall codified dose value from the retrieved codified dose values; and an individualised dose calculator configured to calculate a dosage formulation of one of the nutrition components for a customer based at least partly on the overall codified dose rate. The invention in another form comprises a method of formulating one or more nutrient doses for a customer.
摘要翻译：本发明以一种形式提供营养剂量制剂系统。该系统包括维持在计算机存储器中的营养台; 维护在计算机存储器中的客户简档表; 配置为基于所述客户简档表的行的健康状况值从所述营养表的至少一排中检索所选择的编码剂量值并根据所检索的编码剂量值计算总体编码剂量值的总体剂量计算器; 以及个体化剂量计算器，其被配置为至少部分地基于总编码剂量率来计算顾客的营养成分之一的剂量制剂。另一种形式的本发明包括为顾客制定一种或多种营养剂量的方法。

4. 发明申请

WO1994003481A1 DIAMINO ACID DERIVATIVES AS ANTIHYPERTENSIVES 审中-公开
标题翻译： DIAMINO酸衍生物作为抗生素
公开(公告)号：WO1994003481A1
公开(公告)日：1994-02-17
申请号：PCT/US1993007137
申请日：1993-08-03
申请人： SCHERING CORPORATION , NEUSTADT, Bernard, R. , SMITH, Elizabeth, M. , TULSHIAN, Deen
发明人： SCHERING CORPORATION
IPC分类号： C07K05/02
CPC分类号： C07K5/022 , A61K38/00 , C07D209/20
摘要： Novel diamino acid derivative dual inhibitors of neutral endopeptidase and angiotensin converting enzyme of formula (I), wherein: Z is amino, lower alkylamino, di-(lower alkyl)amino R9C(O)NH- or an optionally substituted guanidino group; R1 is hydrogen or R7R8N-; R2 is hydrogen, lower alkyl, cyclolower alkyl, aryllower alkyl or heteroaryl lower alkyl; and R3 is hydrogen, lower alkyl or cyclo lower alkyl; or R2 and R3, together with the carbon to which they are attached, comprise a 3-7 membered carbocyclic ring; R4 is hydrogen, lower alkyl, aryl lower alkyl or heteroaryl lower alkyl; R5 and R6 are independently hydroxy, lower alkoxy, amino, aryl lower alkoxy, lower alkylamino and di-(lower alkyl)amino; R7 is R9C(O)- or R10SO2-; and R8 is hydrogen, lower alkyl, aryl lower alkyl or aryl; or R7 and R8, together with the nitrogen to which they are attached, comprise a 5-7 membered ring; R9 is lower alkyl, aryllower alkyl, aryl, heteroaryl lower alkyl, heteroaryl, lower alkoxy, aryl lower alkoxy, amino, alkylamino or dialkylamino; R10 is lower alkyl, aryl lower alkyl, aryl, heteroaryl lower alkyl, amino, lower alkylamino, di-(lower alkyl)amino or heteroaryl; n is 1, 2, 3, 4 or 5; and m is 1, 2, 3, 4 or 5; or a pharmaceutically acceptable addition salt thereof, useful in the treatment of cardiovascular disorders, are disclosed.
摘要翻译：式（I）的中性内肽酶和血管紧张素转换酶的新型二氨基酸衍生物双重抑制剂，其中：Z是氨基，低级烷基氨基，二（低级烷基）氨基R9C（O）NH-或任选取代的胍基; R1是氢或R7R8N-; R2是氢，低级烷基，环己烷烷基，芳基低级烷基或杂芳基低级烷基; 并且R 3是氢，低级烷基或环低级烷基; 或R 2和R 3与它们所连接的碳一起包含3-7元碳环; R4是氢，低级烷基，芳基低级烷基或杂芳基低级烷基; R5和R6独立地是羟基，低级烷氧基，氨基，芳基低级烷氧基，低级烷基氨基和二（低级烷基）氨基; R7是R9C（O） - 或R10SO2-; R8是氢，低级烷基，芳基低级烷基或芳基; 或R 7和R 8与它们所连接的氮一起包含5-7元环; R 9为低级烷基，芳基低级烷基，芳基，杂芳基低级烷基，杂芳基，低级烷氧基，芳基低级烷氧基，氨基，烷基氨基或二烷基氨基。 R 10为低级烷基，芳基低级烷基，芳基，杂芳基低级烷基，氨基，低级烷基氨基，二 - （低级烷基）氨基或杂芳基; n为1,2,3,4或5; m为1,2,3,4或5; 或其药学上可接受的加成盐，其可用于治疗心血管疾病。

5. 发明申请

WO2010062559A1 SUBSTITUTED PYRAZOLOQUINOLINES AND DERIVATIVES THEREOF 审中-公开
标题翻译：取代的吡唑啉醇及其衍生物
公开(公告)号：WO2010062559A1
公开(公告)日：2010-06-03
申请号：PCT/US2009/062071
申请日：2009-10-26
申请人： SCHERING CORPORATION , HO, Ginny D , YANG, Shu-Wei , SMITH, Elizabeth M , MCELROY, William Thomas , BASU, Kallol , SMOTRYSKI, Jennifer , TAN, Zheng , MCKITTRICK, Brian A. , TULSHIAN, Deen B.
发明人： HO, Ginny D , YANG, Shu-Wei , SMITH, Elizabeth M , MCELROY, William Thomas , BASU, Kallol , SMOTRYSKI, Jennifer , TAN, Zheng , MCKITTRICK, Brian A. , TULSHIAN, Deen B.
IPC分类号： C07D471/04 , C07D491/113 , A61K31/4439 , A61P25/18
CPC分类号： C07D471/04 , C07D491/113
摘要： The present invention relates to substituted pyrazoloquinolines of formula I and derivatives thereof, the use of the compounds as phosphodiesterase 10 (PDElO) inhibitors for the treatment of PDElO -modulated disorders, to pharmaceutical compositions comprising the compounds, and to the use of additional substituted pyrazoloquinolines and derivatives thereof for the treatment of PDElO -modulated disorders.
摘要翻译：本发明涉及式I的取代吡唑并喹啉及其衍生物，该化合物作为磷酸二酯酶10（PDE10）抑制剂用于治疗PDE10-调节性疾病的用途，包含该化合物的药物组合物的用途，以及使用其它取代的吡唑并喹啉及其衍生物用于治疗PDE10-调节性疾病。

6. 发明申请

WO2008033464A2 AZETIDINONE DERIVATIVES AND METHODS OF USE THEREOF 审中-公开
标题翻译： AZETIDINONE衍生物及其使用方法
公开(公告)号：WO2008033464A2
公开(公告)日：2008-03-20
申请号：PCT/US2007/019930
申请日：2007-09-13
申请人： SCHERING CORPORATION , ASLANIAN, Robert, G. , BENNETT, Chad, E. , BURNETT, Duane, A. , CHAN, Tin-Yau , KISELGOF, Eugenia, Y. , KNUTSON, Chad, E. , HARRIS, Joel, M. , MC KITTRICK, Brian, A. , PALANI, Anandan , SMITH, Elizabeth, M. , VACCARO, Henry, M. , XIAO, Dong , KIM, Hyunjin, M.
发明人： ASLANIAN, Robert, G. , BENNETT, Chad, E. , BURNETT, Duane, A. , CHAN, Tin-Yau , KISELGOF, Eugenia, Y. , KNUTSON, Chad, E. , HARRIS, Joel, M. , MC KITTRICK, Brian, A. , PALANI, Anandan , SMITH, Elizabeth, M. , VACCARO, Henry, M. , XIAO, Dong , KIM, Hyunjin, M.
CPC分类号： C07D471/10
摘要： The present invention relates to Azetidinone Derivatives, compositions comprising an Azetidinone Derivative and methods for treating or preventing a disorder of lipid metabolism, pain, diabetes, a vascular condition, demyelination or nonalcoholic fatty liver disease, comprising administering to a patient an effective amount of an Azetidinone Derivative.
摘要翻译：本发明涉及氮杂环丁酮衍生物，包含氮杂环丁酮衍生物的组合物和用于治疗或预防脂质代谢紊乱，疼痛，糖尿病，血管病症，脱髓鞘或非酒精性脂肪性肝病的方法，包括向患者施用有效量的氮杂环丁酮衍生物。

7. 发明申请

WO2008004899A3 METHOD AND APPARATUS FOR FORMULATING INDIVIDUALISED DOSES OF NUTRITION 审中-公开
公开(公告)号：WO2008004899A3
公开(公告)日：2008-01-10
申请号：PCT/NZ2007/000171
申请日：2007-07-06
申请人： FONTERRA CO-OPERATIVE GROUP LIMITED , ALEXANDER, David, Lionel, James , ARCHER, Richard , XIAO, Huang , SMITH, Elizabeth, Anne
发明人： ALEXANDER, David, Lionel, James , ARCHER, Richard , XIAO, Huang , SMITH, Elizabeth, Anne
IPC分类号： G06Q50/00
摘要： The invention in one form provides a nutrient dosage formulation system. The system comprises a nutrition table maintained in computer memory; a customer profile table maintained in computer memory; an overall dose calculator configured to retrieve selected codified dose values from at least one row of the nutrition table based on the health condition values of a row of the customer profile table and to calculate an overall codified dose value from the retrieved codified dose values; and an individualised dose calculator configured to calculate a dosage formulation of one of the nutrition components for a customer based at least partly on the overall codified dose rate. The invention in another form comprises a method of formulating one or more nutrient doses for a customer.

8. 发明申请

WO1991005796A1 CARBOXYALKYL DIPEPTIDE INHIBITORS OF ENDOPEPTIDASES 审中-公开
标题翻译：羧酰胆碱抑制剂内皮抑素
公开(公告)号：WO1991005796A1
公开(公告)日：1991-05-02
申请号：PCT/US1990005640
申请日：1990-10-10
申请人： SCHERING CORPORATION , HASLANGER, Martin, F. , NEUSTADT, Bernard, R. , SMITH, Elizabeth, M.
发明人： SCHERING CORPORATION
IPC分类号： C07K05/02
CPC分类号： A61K38/04 , A61K31/40 , C07K5/06078 , A61K31/195 , A61K31/22 , A61K2300/00
摘要： Carboxyalkyl dipeptide inhibitors of endopeptidases of formula (I) or pharmaceutically acceptable salt thereof, wherein R is H, alkyl, arylalkyl or aryl; R is H, alkyl, alkenyl or alkynyl, wherein the alkyl portion is substituted with 0-3 substituents independently selected from the group consisting of hydroxy, alkoxy, alkoxyalkoxy, alkylthio, aryl, alkoxyalkylthio, arylalkoxy and arylalkylthio; R and R are independently alkyl or arylalkyl; or R and R together with the carbon to which they are attached form an optionally substituted 5-, 6- or 7-membered ring wherein said ring comprises 0 to 1 heteroatoms selected from the group consisting of sulfur and oxygen; R is H, alkyl, alkoxyalkyl, alkylthioalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, arylalkoxyalkyl or arylalkylthioalkyl; R is hydroxy, alkoxy, or R ; R is hydroxy, alkoxy, aryloxy, arylalkoxy, amino, alkylamino or dialkylamino; m is 0 or 1; and n is 0, 1, 2, or 3, use of the compounds, alone or in combination with an ACE inhibitor or an ANF, in the treatment of cardiovascular disorders such as hypertension, congestive heart failure, edema and renal insufficiency, use of the compounds in the treatment of pain conditions, and pharmaceutical compositions containing said compounds are disclosed.
摘要翻译：式（I）的内肽酶的羧甲基二肽抑制剂或其药学上可接受的盐，其中R 1是H，烷基，芳烷基或芳基; R 2是H，烷基，烯基或炔基，其中烷基部分被独立地选自羟基，烷氧基，烷氧基烷氧基，烷硫基，芳基，烷氧基烷硫基，芳基烷氧基和芳基烷硫基的0-3个取代基取代。 R 3和R 4独立地是烷基或芳基烷基; 或R 3和R 4与它们所连接的碳一起形成任选取代的5-，6-或7-元环，其中所述环包含0至1个选自硫和氧的杂原子 ; R 5是H，烷基，烷氧基烷基，烷硫基烷基，芳基，芳基烷基，杂芳基，杂芳基烷基，芳基烷氧基烷基或芳基烷硫基烷基; R 6是羟基，烷氧基或R 5; R 7是羟基，烷氧基，芳氧基，芳基烷氧基，氨基，烷基氨基或二烷基氨基; m为0或1; 和n为0,1,2或3，单独使用或与ACE抑制剂或ANF组合用于治疗心血管疾病如高血压，充血性心力衰竭，水肿和肾功能不全的使用，公开了治疗疼痛病症的化合物和含有所述化合物的药物组合物。

9. 发明申请

WO2018118829A1 HETEROCYCLIC COMPOUNDS AS HIV PROTEASE INHIBITORS 审中-公开
公开(公告)号：WO2018118829A1
公开(公告)日：2018-06-28
申请号：PCT/US2017/067163
申请日：2017-12-19
申请人： MERCK SHARP & DOHME CORP. , MCKITTRICK, Brian , CALDWELL, John, P. , MCCAULEY, John, A. , VACCARO, Henry , CHAN, Tin-Yau , KIM, Hyunjin , SMITH, Elizabeth , HONG, Liwu , KHAN, Tanweer , YING, Shihong , WANG, Hongwu , WILLIAMS, Peter, D. , KIM, Jae-Hun , NOLT, M. Brad , CAPLEN, Mary Ann
发明人： MCKITTRICK, Brian , CALDWELL, John, P. , MCCAULEY, John, A. , VACCARO, Henry , CHAN, Tin-Yau , KIM, Hyunjin , SMITH, Elizabeth , HONG, Liwu , KHAN, Tanweer , YING, Shihong , WANG, Hongwu , WILLIAMS, Peter, D. , KIM, Jae-Hun , NOLT, M. Brad , CAPLEN, Mary Ann
IPC分类号： A61K31/4178 , C07D403/06 , C07D493/04
摘要： The present invention is directed to compounds of Formula I pharmaceutical compositions comprising the same, and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS.

10. 发明申请

WO2008033447A1 AZETIDINE AND AZETIDONE DERIVATIVES USEFUL IN TREATING PAIN AND DISORDERS OF LIPID METABOLISM 审中-公开
标题翻译： AZETIDINE和AZETIDONE衍生物有助于治疗脂肪代谢的疼痛和疾病
公开(公告)号：WO2008033447A1
公开(公告)日：2008-03-20
申请号：PCT/US2007/019901
申请日：2007-09-13
申请人： SCHERING CORPORATION , MCKITTRICK, Brian , SMITH, Elizabeth, M. , BENNETT, Chad, E. , BURNETT, Duane, A. , KNUTSON, Chad, E.
发明人： MCKITTRICK, Brian , SMITH, Elizabeth, M. , BENNETT, Chad, E. , BURNETT, Duane, A. , KNUTSON, Chad, E.
IPC分类号： A61K31/397 , C07D471/10 , C07D487/10 , A61K31/438 , A61P29/00
CPC分类号： C07D471/10 , C07D487/10
摘要： Disclosed are compounds of formula (I) wherein Z 1 is -CH 2 - or -C(O)-, R 4 and R 5 are carbon chains (and optionally, together can form a C 2 bridge), u and v are independently an integer of 0-3 such that there sum is from 3 to 5, and R 2 is heteroaryl, and R 1 and R 3 are as defined herein. Also disclosed are methods of treating pain using a compound of formula (I).
摘要翻译：公开了式（I）的化合物，其中Z 1是-CH 2 - 或-C（O） - ，R 4和R 4， SUP> 5是碳链（并且可选地，一起可以形成C 2 H 2桥），u和v独立地是0-3的整数，使得总和为3至5 R 2是杂芳基，R 1和R 3如本文所定义。还公开了使用式（I）化合物治疗疼痛的方法。

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