-
公开(公告)号：US20240199525A1
公开(公告)日：2024-06-20
申请号：US18511496
申请日：2023-11-16
Inventor： Yehenew Agazie
Abstract: The present invention provides a compound of the formula:
wherein R1 is a hydrogen or a COOH, R2 is a hydrogen or a COOH, R3 is a hydrogen or a COOH, R4 is one selected from the group consisting of H, COOH, and CH2COOH, and R5 is one selected from the group consisting of H, COOH, and CH2COOH. The present invention provides a compound having the formula:
wherein R is COOH or CH2COOH. Pharmaceutical compositions comprising one of these compounds and at least one of an acceptable pharmaceutical carrier, are provided. Methods of treating a patient having cancer are provided.-
公开(公告)号：US20180319737A1
公开(公告)日：2018-11-08
申请号：US16033645
申请日：2018-07-12
Applicant: Bristol-Myers Squibb Company
Inventor： PETER T. W. CHENG , David S. Yoon
IPC: C07C229/42 , C07D223/08 , A61K31/451 , A61K31/397 , A61K31/402 , A61K31/44 , A61K31/55 , C07C59/72 , A61K31/192 , A61K31/196 , C07C62/34 , C07C59/68 , C07C59/64 , C07D213/65 , C07D211/46 , C07D211/42 , C07D211/14 , C07D207/12 , C07D205/04
CPC classification number: C07C229/42 , A61K31/192 , A61K31/196 , A61K31/397 , A61K31/402 , A61K31/44 , A61K31/451 , A61K31/55 , C07C59/64 , C07C59/68 , C07C59/72 , C07C62/34 , C07C2601/02 , C07C2601/08 , C07C2601/18 , C07D205/04 , C07D207/12 , C07D211/14 , C07D211/42 , C07D211/46 , C07D213/65 , C07D223/08
Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR120 G protein-coupled receptor modulators which may be used as medicaments.
-
公开(公告)号：US09938222B2
公开(公告)日：2018-04-10
申请号：US15509214
申请日：2015-09-08
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Yan Shi , Peter T. W. Cheng , Ying Wang , Sutjano Jusuf , Shiwei Tao , Hao Zhang , Shung C. Wu , Jeffrey A. Robl
IPC: C07C62/34 , C07C59/64 , C07D307/79 , C07D277/30 , C07D213/55 , C07D231/12 , C07D213/65
CPC classification number: C07C62/34 , A61K31/192 , A61K31/343 , A61K31/415 , A61K31/426 , A61K31/44 , A61K31/4418 , C07C59/64 , C07C2601/02 , C07D207/323 , C07D213/55 , C07D213/65 , C07D231/12 , C07D277/30 , C07D277/593 , C07D307/79 , C07D307/82
Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR120 G protein-coupled receptor modulators which may be used as medicaments.
-
公开(公告)号：US20170260119A1
公开(公告)日：2017-09-14
申请号：US15508933
申请日：2015-04-28
Inventor： Pucha YAN , Yuanqiang LI , Daqing CHE , Xiangdong ZHANG , Kang CHEN , Yongliang YAN
IPC: C07C51/367 , B01J31/24 , B01J31/18 , C07B53/00
CPC classification number: C07C51/367 , B01J31/1815 , B01J31/189 , B01J31/2447 , B01J2231/643 , B01J2531/0241 , B01J2531/827 , C07B53/00 , C07B2200/07 , C07C59/01 , C07C59/11 , C07C59/48 , C07C59/50 , C07C59/56 , C07C59/64 , C07C2601/14 , C07F9/58
Abstract: The present invention relates to the technical field of organic chemistry, specifically an asymmetrical hydrogenation of an ∂-ketonic acid compound, the technical proposal being as shown by the following formula: Wherein R1 is a phenyl, a substituted phenyl, a naphthyl a substituted naphthyl, a C1-C6 alkyl or aralkyl, the substitute is a C1-C6 alkyl, a C1-C6 alkoxy, a halogen, the number of the substituents is 1-3.M is a chiral spiro-pyridyl amido phosphine ligand iridium complex having the following structure, Wherein, R is hydrogen, 3-methyl, 4-tBu or 6-methyl
-
公开(公告)号：US09556107B2
公开(公告)日：2017-01-31
申请号：US14467996
申请日：2014-08-25
Inventor： Ziao Xu , Yuanhai Zhao , Degang Li , Xiaoxiang Li
IPC: C07D295/192 , C07D295/096 , C07C213/02 , C07C59/64 , C07C235/34 , C07C253/00 , C07C255/36 , C07C255/37 , C07C327/22 , C07C233/11 , C07C327/44 , C07C237/20
CPC classification number: C07C213/02 , C07C59/64 , C07C233/11 , C07C235/34 , C07C237/20 , C07C253/00 , C07C255/36 , C07C255/37 , C07C327/22 , C07C327/44 , C07D295/096 , C07D295/192
Abstract: The invention discloses a novel intermediate for preparing tapentadol and analogs thereof, wherein the structural formula is shown as formula I or II, and the groups are defined as the specification. The invention further discloses a method for preparing the novel intermediate and use of the intermediate for preparing tapentadol and analogs thereof. The invention can remarkably improve the product yield and quality of tapentadol, reduce the production cost, and simplify the production procedure. The preparation process is environment friendly, thus more suitable for the requirements of industrial production.
Abstract translation: 本发明公开了一种制备他喷他多及其类似物的新型中间体，其结构式如式I或II所示，其定义为说明书。 本发明进一步公开了一种制备新型中间体的方法以及用于制备他喷他多和其类似物的中间体。 本发明可显着提高他喷他多的产品产量和质量，降低生产成本，简化生产工艺。 制备工艺环保，更适合工业生产要求。
-
Patent Agency Ranking
6.发明授权Chiral phosphines for palladium-catalyzed asymmetric α-arylation of ester enolates to produce tertiary stereocenters in high enantioselectivity 有权用于钯催化的酯烯醇化物的不对称α-芳基化的手性膦以产生高对映体选择性的三元立体中心公开(公告)号：US09512155B2
公开(公告)日：2016-12-06
申请号：US14239541
申请日：2012-08-17
Applicant: Steve Jianrong Zhou , Zhiyan Huang
Inventor： Steve Jianrong Zhou , Zhiyan Huang
IPC: C07C69/95 , C07F9/50 , C07D215/14 , C07D333/38 , C07F9/53 , C07C253/30 , C07C67/00 , C07C51/09 , C07C51/00 , C07C69/612 , C07C69/616
CPC classification number: C07F9/5022 , C07B2200/07 , C07C51/00 , C07C51/09 , C07C67/00 , C07C69/612 , C07C69/616 , C07C253/30 , C07C2601/14 , C07D215/14 , C07D333/38 , C07F9/509 , C07F9/5325 , C07C255/57 , C07C69/738 , C07C69/608 , C07C69/76 , C07C69/734 , C07C59/64
Abstract: The disclosure provides new and improved methods for the Pd-catalyzed asymmetric α-arylation of ester compounds, which produce the corresponding α-aryl moiety in high enantioselectivity (generally >90% ee). The present methods utilize a palladium catalyst supported by new (R)—H8-BINOL-derived monophosphine ligands. The method is applicable to a wide variety of aryl triflate substrates having variations in both electronic and steric properties. These aryl triflate substrates react with various α-alkyl (Z)- and/or (E)-0-trimethylsilyl ketene acetals in the presence of a Pd catalyst, (R)—H8-BINOL-derived monophosphine ligand, and a mild activator, for example, LiOAC, to provide the asymmetric α-arylation of ester compounds in high ee.
Abstract translation: 本公开提供了用于酯化合物的Pd催化的不对称α-芳基化的新的和改进的方法，其产生具有高对映体选择性（通常> 90％ee）的相应的α-芳基部分。 本发明的方法利用由新的（R）-H8-BINOL衍生的单膦配体支持的钯催化剂。 该方法适用于各种具有电子和空间特性变化的三氟甲磺酸芳基酯基材。 这些芳基三氟甲磺酸酯底物在Pd催化剂，（R）-H8-BINOL衍生的单膦配体和温和活化剂的存在下，与各种α-烷基（Z） - 和/或（E）-O-三甲基甲硅烷基乙烯酮缩醛反应 ，例如LiOAC，以提供酯化合物在高ee中的不对称α-芳基化。
-
公开(公告)号：US20160083327A1
公开(公告)日：2016-03-24
申请号：US14944721
申请日：2015-11-18
Applicant: FIBROSTATIN, S.L.
Inventor： Juan Saus , Santos Fustero , Juan F. Sanz-Cervera , Enrique Pérez-Payá , Raül Blasco , Francisco Revert-Ros , Fernando Revert
IPC: C07C59/52 , C07D213/55 , C07C69/732 , C07C69/734 , C07C67/313
CPC classification number: C07C59/52 , C07C45/68 , C07C47/565 , C07C59/56 , C07C59/64 , C07C59/70 , C07C67/313 , C07C69/732 , C07C69/734 , C07C69/738 , C07C309/65 , C07D213/26 , C07D213/34 , C07D213/48 , C07D213/55 , C07D213/58
Abstract: Disclosed are compounds of formula: that inhibiting GPBP activity, making them useful as therapeutics in antibody-mediated disorders, drug-resistant cancer, inflammation, protein misfolding and ER stress-mediated disorders, and aberrant apoptosis.
-
8.发明申请公开(公告)号：US20160052866A1
公开(公告)日：2016-02-25
申请号：US14467996
申请日：2014-08-25
Inventor： ZIAO XU , YUANHAI ZHAO , DEGANG LI , XIAOXIANG LI
IPC: C07C213/02 , C07D295/096 , C07D295/192 , C07C59/64 , C07C235/34
CPC classification number: C07C213/02 , C07C59/64 , C07C233/11 , C07C235/34 , C07C237/20 , C07C253/00 , C07C255/36 , C07C255/37 , C07C327/22 , C07C327/44 , C07D295/096 , C07D295/192
Abstract: The invention discloses a novel intermediate for preparing tapentadol and analogues thereof, wherein the structural formula is shown as formula I or II, and the groups are defined as the specification. The invention further discloses a method for preparing the novel intermediate and use of the intermediate for preparing tapentadol and analogues thereof. The invention can remarkably improve the product yield and quality of tapentadol, reduce the production cost, and simplify the production procedure. The preparation process is environment friendly, thus more suitable for the requirements of industrial production.
Abstract translation: 本发明公开了一种制备他喷他多及其类似物的新型中间体，其结构式如式I或II所示，这些基团定义为说明书。 本发明进一步公开了一种制备新型中间体的方法以及用于制备他喷他多和其类似物的中间体。 本发明可显着提高他喷他多的产品产量和质量，降低生产成本，简化生产工艺。 制备工艺环保，更适合工业生产要求。
-
公开(公告)号：US09260375B2
公开(公告)日：2016-02-16
申请号：US13306372
申请日：2011-11-29
Applicant: Ken Chikauchi , Mizuyo Ida , Takao Abe , Yukiko Hiraiwa , Akihiro Morinaka , Toshiaki Kudo
Inventor： Ken Chikauchi , Mizuyo Ida , Takao Abe , Yukiko Hiraiwa , Akihiro Morinaka , Toshiaki Kudo
IPC: C07C57/02 , A61K31/43 , A61K31/397 , A61K31/00 , C07C69/593 , A61K31/194 , C07C57/145 , A61K31/445 , A61K31/495 , A61K31/5375 , A61K45/06 , C07C51/00 , C07C57/13 , C07C57/26 , C07C57/42 , C07C57/50 , C07C59/52 , C07C59/64 , C07C59/70 , C07C69/618 , C07C69/734 , C07C217/22 , C07C233/65 , C07C235/20 , C07C237/22 , C07C279/08 , C07C323/54 , C07D211/46 , C07D211/60 , C07D213/80 , C07D295/192 , C07D309/06 , A61K31/407 , A61K31/546
CPC classification number: A61K31/225 , A61K31/166 , A61K31/194 , A61K31/215 , A61K31/235 , A61K31/24 , A61K31/351 , A61K31/40 , A61K31/407 , A61K31/4164 , A61K31/4406 , A61K31/445 , A61K31/4453 , A61K31/495 , A61K31/5375 , A61K31/546 , A61K45/06 , C07C51/00 , C07C57/13 , C07C57/145 , C07C57/26 , C07C57/42 , C07C57/50 , C07C59/52 , C07C59/64 , C07C59/70 , C07C69/593 , C07C69/60 , C07C69/608 , C07C69/618 , C07C69/732 , C07C69/734 , C07C217/22 , C07C233/65 , C07C235/20 , C07C235/84 , C07C237/22 , C07C279/08 , C07C279/14 , C07C323/54 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07D207/12 , C07D211/46 , C07D211/60 , C07D213/55 , C07D213/80 , C07D233/60 , C07D295/15 , C07D295/16 , C07D295/192 , C07D309/06 , Y02A50/473 , Y02A50/475 , A61K2300/00
Abstract: A new metallo-β-lactamase inhibitor which acts as a medicament for inhibiting the inactivation of β-lactam antibiotics and recovering anti-bacterial activities is disclosed. The maleic acid derivatives having the general formula (I) have metallo-β-lactamase inhibiting activities. It is possible to recover the anti-bacterial activities of β-lactam antibiotics against metallo-β-lactamase producing bacteria by combining the compound of the general formula (I) with β-lactam antibiotics.
Abstract translation: 公开了一种新的金属 - β-内酰胺酶抑制剂，其用作抑制β-内酰胺抗生素灭活和回收抗细菌活性的药物。 具有通式（I）的马来酸衍生物具有金属 - β-内酰胺酶抑制活性。 通过将通式（I）的化合物与β-内酰胺抗生素结合，可以回收抗β-生物反相抗生素对产生金属 - β-内酰胺酶的细菌的抗菌活性。
-
10.发明授权Compounds and uses thereof for treating inflammation and modulating immune responses 有权用于治疗炎症和调节免疫应答的化合物及其用途公开(公告)号：US09174916B2
公开(公告)日：2015-11-03
申请号：US13769644
申请日：2013-02-18
Applicant: PURAPHARM COMPANY LIMITED , VERSITECH LIMITED
Inventor： Allan Sy Lau , Lai Hung Cindy Yang , Chi Chung Stanley Chik , Chun Bong James Li
IPC: C07C59/64 , A61K31/235 , C07C69/734
CPC classification number: C07C59/64 , A61K31/235 , C07C69/734
Abstract: The present invention provides compounds, and compositions comprising these compounds, which have immunomodulatory activity and/or anti-inflammatory activity.
Abstract translation: 本发明提供了具有免疫调节活性和/或抗炎活性的化合物和包含这些化合物的组合物。
-
-
-
-
-
-
-
-
-
Search Results
834
records
(took 0.034 seconds)
