公开(公告)号：US11905230B2

公开(公告)日：2024-02-20

申请号：US16617409

申请日：2018-05-24

申请人： CHINA PHARMACEUTICAL UNIVERSITY

发明人： Hai Qian ,  Wenlong Huang ,  Chunxia Liu ,  Jianyong Yang

IPC分类号： C07C229/42 ,  C07C255/49 ,  C07C317/28 ,  C07D261/08 ,  C07C255/59

CPC分类号： C07C229/42 ,  C07C255/59 ,  C07C317/28 ,  C07D261/08

摘要： The present invention relates to a novel phenoxyacetic acid derivative represented by the general formula (I), preparation method thereof and use of a pharmaceutical composition containing the derivative in preparing a medicament for treating diabetes and metabolic syndrome. The phenoxyacetic acid derivatives have excellent in vivo hypoglycemic activity, which can be used for preventing or treating diabetes.

公开(公告)号：US20190185413A1

公开(公告)日：2019-06-20

申请号：US16280996

申请日：2019-02-20

申请人： Quadriga Biosciences, Inc.

发明人： Bernd Jandeleit ,  Wolf-Nicolas Fischer ,  Kerry J. Koller ,  Gordon Ringold

IPC分类号： C07C229/42 ,  C07C233/54 ,  C07C271/22 ,  C07C237/30 ,  C07C239/20 ,  C07C271/14 ,  C07C271/46 ,  C07C229/22 ,  C07C309/69 ,  C07F9/48 ,  A61K45/06 ,  C07D303/32 ,  A61K31/137 ,  A61K31/336 ,  A61K31/245 ,  A61K31/27 ,  A61K31/197 ,  A61K31/255 ,  A61K31/662 ,  A61K31/196 ,  A61K31/42 ,  A61K31/365 ,  A61K31/519 ,  C07C229/60 ,  C07D303/36 ,  C07C237/04 ,  C07C229/34 ,  C07C215/68 ,  C07C291/04

CPC分类号： C07C229/42 ,  A61K31/137 ,  A61K31/196 ,  A61K31/197 ,  A61K31/245 ,  A61K31/255 ,  A61K31/27 ,  A61K31/336 ,  A61K31/365 ,  A61K31/42 ,  A61K31/519 ,  A61K31/662 ,  A61K45/06 ,  C07B2200/07 ,  C07C215/68 ,  C07C229/22 ,  C07C229/34 ,  C07C229/60 ,  C07C233/54 ,  C07C237/04 ,  C07C237/30 ,  C07C239/20 ,  C07C271/14 ,  C07C271/22 ,  C07C271/46 ,  C07C291/04 ,  C07C309/69 ,  C07D303/32 ,  C07D303/36 ,  C07F9/4808

摘要： β-Substituted β-amino acids, β-substituted β-amino acid derivatives, and β-substituted β-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs exhibit selective uptake in tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types.

公开(公告)号：US20180215707A1

公开(公告)日：2018-08-02

申请号：US15128932

申请日：2015-03-25

申请人： Piramal Enterprises Limited

发明人： Rajiv SHARMA ,  Bichismita SAHU ,  Sunil Vasantrao MALI ,  Deepak SINGH

IPC分类号： C07C317/32 ,  C07D335/06 ,  C07D295/088 ,  C07D295/192 ,  C07D207/27 ,  C07C237/52 ,  C07D295/26 ,  C07D311/22 ,  C07D265/36 ,  C07C311/21 ,  C07C381/10 ,  C07D213/30 ,  C07D231/12 ,  C07D233/58 ,  C07D257/04 ,  C07D305/08 ,  C07D211/14 ,  C07D295/135

CPC分类号： C07C317/32 ,  A61K31/165 ,  A61K31/18 ,  A61K31/277 ,  A61K31/351 ,  A61K31/382 ,  A61K31/402 ,  A61K31/5375 ,  C07C205/36 ,  C07C211/45 ,  C07C215/70 ,  C07C217/48 ,  C07C217/76 ,  C07C217/88 ,  C07C225/22 ,  C07C229/42 ,  C07C233/29 ,  C07C233/54 ,  C07C237/22 ,  C07C237/52 ,  C07C255/46 ,  C07C255/50 ,  C07C309/89 ,  C07C311/08 ,  C07C311/21 ,  C07C311/37 ,  C07C317/24 ,  C07C317/44 ,  C07C323/09 ,  C07C381/10 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/10 ,  C07D207/27 ,  C07D211/14 ,  C07D213/30 ,  C07D231/12 ,  C07D233/58 ,  C07D257/04 ,  C07D265/36 ,  C07D295/088 ,  C07D295/135 ,  C07D295/192 ,  C07D295/26 ,  C07D305/08 ,  C07D311/22 ,  C07D317/72 ,  C07D335/06 ,  C07F5/025 ,  C07F7/1804

摘要： The present invention relates to a compound of formula I, or an isotopic form, stereoisomer, a tautomer, a pharmaceutically acceptable salt, a solvate, a polymorph, a prodrug, N-oxide or S-oxide thereof; and processes for their preparation. The invention further relates to pharmaceutical compositions containing the compounds and their use in the treatment of diseases or disorders mediated by RORγ.

公开(公告)号：US20180125986A1

公开(公告)日：2018-05-10

申请号：US15808182

申请日：2017-11-09

申请人： Apparao Satyam

发明人： Apparao Satyam

IPC分类号： A61K47/54 ,  C07C201/04 ,  C07C203/04 ,  C07C227/18 ,  A61K31/621 ,  C07C229/42 ,  A61K31/21 ,  A61K31/216 ,  A61K31/60

CPC分类号： A61K47/542 ,  A61K31/21 ,  A61K31/216 ,  A61K31/60 ,  A61K47/55 ,  C07C201/04 ,  C07C203/04 ,  C07C227/18 ,  C07C229/42

摘要： The present invention relates to nitric oxide releasing prodrugs of known drugs or therapeutic agents wherein the drug or therapeutic agents contain at least one carboxylic acid group. The invention also relates to processes for the preparation of these nitric oxide releasing prodrugs, to pharmaceutical compositions containing them and to methods of using these prodrugs.

公开(公告)号：US09937139B2

公开(公告)日：2018-04-10

申请号：US15594904

申请日：2017-05-15

申请人： QUADRIGA BIOSCIENCES, INC.

发明人： Bernd Jandeleit ,  Wolf-Nicolas Fischer ,  Kerry J. Koller

IPC分类号： C07C229/08 ,  A61K31/197 ,  C07C271/46 ,  C07C309/69 ,  C07D257/04 ,  A61K31/41 ,  A61K31/662 ,  C07C229/42 ,  C07C237/30 ,  C07C239/20 ,  C07F9/48 ,  C07C239/18 ,  C07F9/32 ,  A61K47/54 ,  A61K47/48

CPC分类号： A61K31/197 ,  A61K31/41 ,  A61K31/662 ,  A61K47/542 ,  C07C229/08 ,  C07C229/42 ,  C07C237/30 ,  C07C239/18 ,  C07C239/20 ,  C07C271/46 ,  C07C309/69 ,  C07D257/04 ,  C07F9/3264 ,  C07F9/48 ,  C07F9/4816

摘要： β-Substituted γ-amino acids, β-substituted γ-amino acid derivatives, and β-substituted γ-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates, capable of passing through the blood-brain barrier, and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres and methods of using the compounds for treating tumors are also disclosed. The β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres exhibit an improved selectivity toward tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres exhibit an increased efficacy on a variety of tumor types.

公开(公告)号：US20180078517A1

公开(公告)日：2018-03-22

申请号：US15826042

申请日：2017-11-29

申请人： QUADRIGA BIOSCIENCES, INC.

发明人： BERND JANDELEIT ,  WOLF-NICOLAS FISCHER ,  KERRY J. KOLLER

IPC分类号： A61K31/197 ,  C07F9/30 ,  C07C233/35 ,  C07C237/20 ,  C07C229/42 ,  A61K31/27 ,  A61K31/255 ,  C07C229/08 ,  C07F9/32 ,  C07C239/20 ,  C07C237/30 ,  C07C229/34 ,  C07C229/22 ,  C07F9/48 ,  A61K31/662 ,  C07C309/69 ,  C07C271/46 ,  C07C237/04 ,  C07C309/66

CPC分类号： A61K31/197 ,  A61K31/255 ,  A61K31/27 ,  A61K31/662 ,  C07C229/08 ,  C07C229/22 ,  C07C229/34 ,  C07C229/42 ,  C07C233/35 ,  C07C237/04 ,  C07C237/20 ,  C07C237/30 ,  C07C239/20 ,  C07C271/46 ,  C07C309/66 ,  C07C309/69 ,  C07F9/306 ,  C07F9/3264 ,  C07F9/48 ,  C07F9/4816

摘要： β-Substituted β-amino acids, β-substituted β-amino acid derivatives, and β-substituted β-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs exhibit selective uptake in tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types.

公开(公告)号：US09914697B2

公开(公告)日：2018-03-13

申请号：US14738004

申请日：2015-06-12

申请人： Johnson Matthey Public Limited Company

发明人： Saroop Singh Matharu ,  Gurijala Venu Reddy ,  James J. Mencel ,  Xiaoyong Sun

IPC分类号： C07C227/42 ,  C07C211/00 ,  A61K31/196 ,  C07C229/42 ,  C07C225/22 ,  C07C221/00 ,  C07C227/22

CPC分类号： C07C227/42 ,  A61K31/196 ,  C07B2200/13 ,  C07C221/00 ,  C07C225/22 ,  C07C227/22 ,  C07C229/42

摘要： Different polymorphs of bromfenac sodium may be prepared and interconverted using crystallization/recrystallization, drying and/or hydration techniques.

公开(公告)号：US09809557B2

公开(公告)日：2017-11-07

申请号：US14355010

申请日：2012-10-31

申请人： Claus Selch Larsen

发明人： Claus Selch Larsen ,  Susan Weng Larsen ,  Mette Agergaard Thing ,  Jesper Langgaard Kristensen ,  Henrik Jensen ,  Jesper Østergaard

IPC分类号： A61K31/44 ,  C07D235/06 ,  A61K47/48 ,  C07C219/10 ,  C07C219/32 ,  C07C229/42 ,  C07D487/04 ,  C07D233/61 ,  C07D235/16 ,  C07D235/18 ,  C07D213/55

CPC分类号： C07D235/06 ,  A61K47/54 ,  A61K47/545 ,  C07C219/10 ,  C07C219/32 ,  C07C229/42 ,  C07D213/55 ,  C07D233/61 ,  C07D235/16 ,  C07D235/18 ,  C07D487/04

摘要： The present invention relates to novel depot formulations (prodrugs) comprising an immobility promoting unit linked via an ester to an active pharmaceutical ingredient, i.a. common NSAIDs. The novel depot formulations are suitable for intra-articular injections and are soluble at slightly acidic pH to facilitate ease of injection, and sparingly soluble at physiological pH thereby precipitating at the site of administration. The precipitate will slowly dissolve and the active drug is released from dissolved depot formulation following esterase mediated cleavage of the ester link between the immobility promoting unit and the active pharmaceutical agent.

公开(公告)号：US20170143836A1

公开(公告)日：2017-05-25

申请号：US15365088

申请日：2016-11-30

申请人： Rutgers, The State University of New Jersey ,  Lehigh University

发明人： Jeffrey D. Laskin ,  Diane E. Heck ,  Mou-Tuan Huang ,  Karine Fabio ,  Jeffrey C. Lacey ,  Sherri C. Young ,  Pramod Mohanta ,  Christophe Gullion ,  Ned D. Heindel

IPC分类号： A61K31/695 ,  C07F7/08 ,  C07D209/28 ,  A61K31/192 ,  A61K31/405 ,  A61K9/00 ,  C07C69/96 ,  C07C229/42

CPC分类号： C07F7/0812 ,  A61K9/0014 ,  A61K31/19 ,  A61K31/192 ,  A61K31/196 ,  A61K31/405 ,  A61K47/54 ,  A61K47/55 ,  C07C69/96 ,  C07C229/42 ,  C07C2602/10 ,  C07D209/28 ,  C07F7/081

摘要： A new family of therapeutics which provides a controlled-release delivery platform for non-steroidal anti-inflammatory agents on an ester or an ester-carbonate backbone is disclosed herein. These agents are reversible inhibitors of acetylcholinesterase and are thus useful for clinical conditions benefiting from inflammation suppression and cholinergic intervention. These compounds are of the general formula wherein n=0, 1; X═C, Si, and N+ and NSAID=ibuprofen, naproxen, indomethacin and diclofenac. Other embodiments are also disclosed.

公开(公告)号：US20160296484A1

公开(公告)日：2016-10-13

申请号：US15181817

申请日：2016-06-14

申请人： QUADRIGA BIOSCIENCES, INC.

发明人： BERND JANDELEIT ,  WOLF-NICOLAS FISCHER ,  KERRY J. KOLLER

IPC分类号： A61K31/197 ,  A61K31/255 ,  A61K31/27 ,  A61K31/662

CPC分类号： A61K31/197 ,  A61K31/255 ,  A61K31/27 ,  A61K31/662 ,  C07C229/08 ,  C07C229/22 ,  C07C229/34 ,  C07C229/42 ,  C07C233/35 ,  C07C237/04 ,  C07C237/20 ,  C07C237/30 ,  C07C239/20 ,  C07C271/46 ,  C07C309/66 ,  C07C309/69 ,  C07F9/306 ,  C07F9/3264 ,  C07F9/48 ,  C07F9/4816

摘要： β-Substituted β-amino acids, β-substituted β-amino acid derivatives, and β-substituted β-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs exhibit selective uptake in tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types.

摘要翻译： β取代的β-氨基酸，β-取代的β-氨基酸衍生物和β-取代的β-氨基酸类似物和（生物）等电点及其作为化学治疗剂的用途。 β-取代的β-氨基酸衍生物和β-取代的β-氨基酸类似物和（生物）等分子体是选择性LAT1 / 4F2hc底物，并且在表达LAT1 / 4F2hc转运蛋白的肿瘤中表现出快速吸收和保留。 还公开了合成β-取代的β-氨基酸衍生物和β-取代的β-氨基酸类似物的方法和使用该化合物治疗癌症的方法。 β-取代的β-氨基酸衍生物和β-取代的β-氨基酸类似物在表达LAT1 / 4F2hc转运蛋白的肿瘤细胞中表现出选择性摄取，并且当在体内施用于受试者时，其积累在癌细胞中。 β取代的β-氨基酸衍生物和β-取代的β-氨基酸类似物和（生物）等体积体对几种肿瘤类型表现出细胞毒性。