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1. 发明专利

IL285510D0 Substituted amide compounds useful as farnesoid x receptor modulators 未知
公开(公告)号：IL285510D0
公开(公告)日：2021-09-30
申请号：IL28551021
申请日：2021-08-10
申请人： SQUIBB BRISTOL MYERS CO , WACKER DEAN A , NARA SUSHEEL JETHANAND , CHERUKU SRINIVAS , SARKUNAM KANDHASAMY , JAIPURI FIROZ ALI , THANGAVEL SOODAMANI , NARAYAN RISHIKESH , JOGI SRINIVAS , KATHI PAVAN KALYAN
发明人： WACKER DEAN A , NARA SUSHEEL JETHANAND , CHERUKU SRINIVAS , SARKUNAM KANDHASAMY , JAIPURI FIROZ ALI , THANGAVEL SOODAMANI , NARAYAN RISHIKESH , JOGI SRINIVAS , KATHI PAVAN KALYAN
摘要： Disclosed are compounds of Formula (I): or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt or solvate thereof, when Q is: (i) halo, cyano, hydroxyl, NRxRx, C(O)OH, C(O)NH2, C1-6 alkyl substiuted with zero to 6 R1a, or P(O)R1cR1c, or (ii) L R1; and A, X1, X2, X3, X4, Z1, Z2, R1, R1a, R1c, R2, R3a, R3b, Rx, L, a, b, and d are defined herein. Also disclosed are methods of using these compounds to modulate the activity of farnesoid X receptor (FXR); pharmaceutical compositions comprising these compounds; and methods of treating a disease, disorder, or condition associated with FXR dysregulation, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.

2. 发明专利

IL285557D0 Substituted amide compounds useful as farnesoid x receptor modulators 未知
公开(公告)号：IL285557D0
公开(公告)日：2021-09-30
申请号：IL28555721
申请日：2021-08-11
申请人： SQUIBB BRISTOL MYERS CO , WACKER DEAN A , NARA SUSHEEL JETHANAND , CHERUKU SRINIVAS , SARKUNAM KANDHASAMY , JAIPURI FIROZ ALI , THANGAVEL SOODAMANI , NARAYAN RISHIKESH , BANDREDDY SUBBA REDDY , JOGI SRINIVAS , KATHI PAVAN KALYAN
发明人： WACKER DEAN A , NARA SUSHEEL JETHANAND , CHERUKU SRINIVAS , SARKUNAM KANDHASAMY , JAIPURI FIROZ ALI , THANGAVEL SOODAMANI , NARAYAN RISHIKESH , BANDREDDY SUBBA REDDY , JOGI SRINIVAS , KATHI PAVAN KALYAN
IPC分类号： A61P1/16 , A61P1/18 , A61P11/00 , A61P35/00
摘要： Disclosed are compounds of Formula (I) or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt or solvate thereof, wherein Q is a 5-membered heterocyclyl or 5-membered heteroaryl having 1 to 4 heteroatoms independently selected from N, O, and S, substituted with zero to 4 R1; and A, X1, X2, X3, X4, Z1, Z2, R1, R2, R3a, R3b, a, b, and d are defined herein. Also disclosed are methods of using these compounds to modulate the activity of farnesoid X receptor (FXR); pharmaceutical compositions comprising these compounds; and methods of treating a disease, disorder, or condition associated with FXR dysregulation, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.

3. 发明专利

IL285246D0 Substituted bicyclic compounds as farnesoid x receptor modulators 未知
公开(公告)号：IL285246D0
公开(公告)日：2021-09-30
申请号：IL28524621
申请日：2021-07-29
申请人： SQUIBB BRISTOL MYERS CO , WACKER DEAN A , NARA SUSHEEL JETHANAND , CHERUKU SRINIVAS , SARKUNAM KANDHASAMY , JAIPURI FIROZ ALI , THANGAVEL SOODAMANI , NARAYAN RISHIKESH , BANDREDDY SUBBA REDDY , JOGI SRINIVAS , KATHI PAVAN KALYAN
发明人： WACKER DEAN A , NARA SUSHEEL JETHANAND , CHERUKU SRINIVAS , SARKUNAM KANDHASAMY , JAIPURI FIROZ ALI , THANGAVEL SOODAMANI , NARAYAN RISHIKESH , BANDREDDY SUBBA REDDY , JOGI SRINIVAS , KATHI PAVAN KALYAN
摘要： Disclosed are compounds of Formula (I):or a stereoisomer, a tautomer, or a salt or solvate thereof, wherein all the variables are as defined herein. These compounds modulate the activity of farnesoid X receptor (FXR), for example, as agonists. Also disclosed are pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with FXR dysregulation, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.

4. 发明专利

IL254720D0 Inhibitors of indoleamine 2,3-dioxygenase for the treatment of cancer 未知
公开(公告)号：IL254720D0
公开(公告)日：2017-11-30
申请号：IL25472017
申请日：2017-09-26
申请人： SQUIBB BRISTOL MYERS CO , HUANG AUDRIS , SHAN WEIFANG , ROY SAUMYA , BALOG JAMES AARON , CHERNEY EMILY CHARLOTTE , MARKWALDER JAY A , SEITZ STEVEN P , WILLIAMS DAVID K , NARA SUSHEEL JETHANAND , THANGAVEL SOODAMANI , SISTLA RAMESH KUMAR , CHERUKU SRINIVAS , THANGATHIRUPATHY SRINIVASAN , KANYABOINA YADAGIRI , PULICHARLA NAGALAKSHMI
发明人： HUANG AUDRIS , SHAN WEIFANG , ROY SAUMYA , BALOG JAMES AARON , CHERNEY EMILY CHARLOTTE , MARKWALDER JAY A , SEITZ STEVEN P , WILLIAMS DAVID K , NARA SUSHEEL JETHANAND , THANGAVEL SOODAMANI , SISTLA RAMESH KUMAR , CHERUKU SRINIVAS , THANGATHIRUPATHY SRINIVASAN , KANYABOINA YADAGIRI , PULICHARLA NAGALAKSHMI
IPC分类号： C07C20060101
摘要： There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.

5. 发明专利

IL254722D0 Inhibitors of indoleamine 2,3-dioxygenase for the treatment of cancer 未知
公开(公告)号：IL254722D0
公开(公告)日：2017-11-30
申请号：IL25472217
申请日：2017-09-26
申请人： SQUIBB BRISTOL MYERS CO , GUO WEIWEI , HUANG AUDRIS , SHAN WEIFANG , ROY SAUMYA , BALOG JAMES AARON , CHERNEY EMILY CHARLOTTE , MARKWALDER JAY A , SEITZ STEVEN P , WILLIAMS DAVID K , NARA SUSHEEL JETHANAND , THANGAVEL SOODAMANI , SISTLA RAMESH KUMAR , CHERUKU SRINIVAS , THANGATHIRUPATHY SRINIVASAN , KANYABOINA YADAGIRI , PULICHARLA NAGALAKSHMI , MURUGESAN NATESAN
发明人： GUO WEIWEI , HUANG AUDRIS , SHAN WEIFANG , ROY SAUMYA , BALOG JAMES AARON , CHERNEY EMILY CHARLOTTE , MARKWALDER JAY A , SEITZ STEVEN P , WILLIAMS DAVID K , NARA SUSHEEL JETHANAND , THANGAVEL SOODAMANI , SISTLA RAMESH KUMAR , CHERUKU SRINIVAS , THANGATHIRUPATHY SRINIVASAN , KANYABOINA YADAGIRI , PULICHARLA NAGALAKSHMI , MURUGESAN NATESAN
IPC分类号： C07C20060101
摘要： There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.

6. 发明公开

KR20180056764A 비아릴 키나제 억제제 审中-公开
公开(公告)号：KR20180056764A
公开(公告)日：2018-05-29
申请号：KR20187011873
申请日：2016-09-29
申请人： SQUIBB BRISTOL MYERS CO
发明人： BRONSON JOANNE J , CHEN LING , DITTA JONATHAN L , DZIERBA CAROLYN DIANE , JALAGAM PRASADA RAO , LUO GUANGLIN , MACOR JOHN E , MAISHAL TARUN KUMAR , NARA SUSHEEL JETHANAND , RAJAMANI RAMKUMAR , SISTLA RAMESH KUMAR , THANGAVEL SOODAMANI
IPC分类号： C07D401/04 , A61K31/437 , A61K31/4418 , A61K31/444 , A61P25/00 , A61P25/16 , A61P25/28 , C07D471/04
CPC分类号： C07D231/12 , C07D213/65 , C07D213/74 , C07D213/75 , C07D239/36 , C07D239/42 , C07D239/72 , C07D401/04 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07D471/04 , C07D487/04 , C07D495/04 , C07D513/04
摘要： 본개시내용은일반적으로 AAK1 (어댑터연관키나제 1)을억제할수 있는화합물, 이러한화합물을포함하는조성물, 및 AAK1을억제하는방법에관한것이다.

7. 发明公开

KR20180056765A 비아릴 키나제 억제제 审中-公开
公开(公告)号：KR20180056765A
公开(公告)日：2018-05-29
申请号：KR20187011874
申请日：2016-09-29
申请人： SQUIBB BRISTOL MYERS CO
发明人： BRONSON JOANNE J , CHEN LING , DITTA JONATHAN L , DZIERBA CAROLYN DIANE , JALAGAM PRASADA RAO , LUO GUANGLIN , MACOR JOHN E , MAISHAL TARUN KUMAR , NARA SUSHEEL JETHANAND , RAJAMANI RAMKUMAR , SISTLA RAMESH KUMAR , THANGAVEL SOODAMANI
IPC分类号： C07D401/04 , A61K31/167 , A61K31/506 , A61P25/00 , A61P25/28 , C07D213/75 , C07D401/14 , C07D413/14
CPC分类号： C07D401/04 , C07D213/26 , C07D213/61 , C07D213/63 , C07D213/73 , C07D213/75 , C07D213/85 , C07D237/20 , C07D239/26 , C07D239/30 , C07D239/34 , C07D239/42 , C07D401/14 , C07D413/14 , C07D471/04
摘要： 본개시내용은일반적으로 AAK1 (어댑터연관키나제 1)을억제할수 있는화합물, 이러한화합물을포함하는조성물, 및 AAK1을억제하는방법에관한것이다.

8. 发明专利

CO2021010611A2 Compuestos bicíclicos sustituidos como moduladores del receptor farnesoide x 未知
公开(公告)号：CO2021010611A2
公开(公告)日：2021-08-30
申请号：CO2021010611
申请日：2021-08-12
申请人： SQUIBB BRISTOL MYERS CO
发明人： NARA SUSHEEL JETHANAND , THANGAVEL SOODAMANI , CHERUKU SRINIVAS , WACKER DEAN A , SARKUNAM KANDHASAMY , JAIPURI FIROZ ALI , NARAYAN RISHIKESH , BANDREDDY SUBBA REDDY , JOGI SRINIVAS , KATHI PAVAN KALYAN
IPC分类号： C07D217/06 , A61K31/427 , A61P3/06 , A61P13/00 , A61P35/00 , C07D403/12 , C07D413/12 , C07D413/14 , C07D417/12
摘要： Se describen los compuestos de la Fórmula (I): (I) o un estereoisómero, un tautómero o una sal o solvato del mismo, en donde todas las variables son como se definen en el presente documento. Estos compuestos modulan la actividad del receptor Farnesoide X (FXR), por ejemplo, como agonistas. También se describen composiciones farmacéuticas que comprenden estos compuestos y métodos para tratar una enfermedad, trastorno o condición asociada con la desregulación del FXR, tal como fibrosis patológica, rechazo de trasplantes, cáncer, osteoporosis y trastornos inflamatorios, mediante el uso de los compuestos y composiciones farmacéuticas.

9. 发明专利

ES2765730T3 Inhibidores de biaril cinasa 未知
公开(公告)号：ES2765730T3
公开(公告)日：2020-06-10
申请号：ES16785279
申请日：2016-09-29
申请人： SQUIBB BRISTOL MYERS CO
发明人： BRONSON JOANNE J , CHEN LING , DITTA JONATHAN L , DZIERBA CAROLYN DIANE , JALAGAM PRASADA RAO , LUO GUANGLIN , MACOR JOHN E , MAISHAL TARUN KUMAR , NARA SUSHEEL JETHANAND , RAJAMANI RAMKUMAR , SISTLA RAMESH KUMAR , THANGAVEL SOODAMANI
IPC分类号： C07D401/04 , C07D213/26 , C07D213/61 , C07D213/63 , C07D213/73 , C07D213/75 , C07D213/85 , C07D237/20 , C07D239/26 , C07D239/30 , C07D239/34 , C07D239/42 , C07D401/14 , C07D413/14 , C07D471/04
摘要： Un compuesto seleccionado de (R)-2,4-dimetil-1-((3-metil-5-(2-metilpirimidin-4-il)piridin-2-il)oxi)pentan-2-amina; (S)-2,4-dimetil-1-((3-metil-5-(2-metilpirimidin-4-il)piridin-2-il)oxi)pentan-2-amina; 5-(2-amino-4-metil-2-(trifluorometil)pentiloxi)-6-metil-2,4'-bipiridin-2'-ilcarbamato de metilo; 1,1,1-trifluoro-4-metil-2-(((3-metil-5-(2-metilpirimidin-4-il)piridin-2-il)oxi)metil)pentan-2-amina; (S)-6-(4-((2-amino-2,4-dimetilpentil)oxi)-3-(trifluorometil)fenil)pirimidin-4-amina; (S)-1-((2-(fluorometil)-6-(2-metilpirimidin-4-il)piridin-3-il)oxi)-2,4-dimetilpentan-2-amina; (5-((2-amino-2,4-dimetilpentil)oxi)-6-(fluorometil)-[2,4'-bipiridin]-2'-il)carbamato de (S)-metilo; (S)-6-(4-((2-amino-2,4-dimetilpentil)oxi)-3-clorofenil)pirimidin-4-amina; (S)-2,4-dimetil-1-(4-(2-metilpirimidin-4-il)-2-(trifluorometil)fenoxi)pentan-2-amina; (S)-4-(4-((2-amino-2,4-dimetilpentil)oxi)-3-(trifluorometil)fenil)piridin-2-amina; (S)-2,4-dimetil-1-((5-(2-metilpirimidin-4-il)-3-(oxazol-5-il)piridin-2-il)oxi)pentan-2-amina; (S)-2,4-dimetil-1-((6-(2-metilpirimidin-4-il)-4-(oxazol-5-il)piridin-3-il)oxi)pentan-2-amina; (5-(4-((2-amino-2,4-dimetilpentil)oxi)-3-cianofenil)piridazin-3-il)carbamato de (S)-metilo; (5-(4-((2-amino-2,4-dimetilpentil)oxi)-3-clorofenil)piridazin-3-il)carbamato de (S)-metilo; (4-(6-((2-amino-2,4-dimetilpentil)oxi)-5-cloropiridin-3-il)pirimidin-2-il)carbamato de (R)-metilo; (4-(4-((2-amino-2,4-dimetilpentil)oxi)-3-cianofenil)pirimidin-2-il)carbamato de (S)-metilo; (4-(4-((2-amino-2,4-dimetilpentil)oxi)-3-(trifluorometil)fenil)pirimidin-2-il)carbamato de (S)-metilo; (4-(4-((2-amino-2,4-dimetilpentil)oxi)-3-clorofenil)pirimidin-2-il)carbamato de (S)-metilo; (S)-1-(2-cloro-4-(6-metilpirimidin-4-il)fenoxi)-2,4-dimetilpentan-2-amina; (S)-2,4-dimetil-1-(4-(6-metilpirimidin-4-il)-2-(trifluorometil)fenoxi)pentan-2-amina; (4-(4-((2-amino-2,4-dimetilpentil)oxi)-3-fluorofenil)pirimidin-2-il)carbamato de (S)-metilo; (4-(4-((2-amino-2,4-dimetilpentil)oxi)-3-(trifluorometil)fenil)pirimidin-2-il)carbamato de (S)-isopropilo; (4-(5-((2-amino-2,4 dimetilpentil)oxi)-6-metilpiridin-2-il)pirimidin-2-il)carbamato de (S)-metilo; (S)-4-(5-((2-amino-2,4-dimetilpentil)oxi)-6-metilpiridin-2-il)pirimidin-2-amina; (4-(4-((2-amino-2,4-dimetilpentil)oxi)-3-(trifluorometil)fenil)pirimidin-2-il)carbamato de (S)-etilo; (S)-2-((2-amino-2,4-dimetilpentil)oxi)-5-(2-(difluorometil)pirimidin-4-il)benzonitrilo; (S)-1-(4-(2-metoxipirimidin-4-il)-2-(trifluorometil)fenoxi)-2,4-dimetilpentan-2-amina; (S)-4-(4-((2-amino-2,4-dimetilpentil)oxi)-3 (trifluorometil)fenil)pirimidin-2-ol; (S)-1-((4-(difluorometil)-6-(6-metilpirimidin-4-il)piridin-3-il)oxi)-2,4-dimetilpentan-2-amina; (S)-1-((2-(difluorometil)-6-(2-(difluorometil)pirimidin-4-il)piridin-3-il)oxi)-2,4-dimetilpentan-2-amina; (S)-1-((6-(fluorometil)-2'-metil-[2,4'-bipiridin]-5-il)oxi)-2,4-dimetilpentan-2-amina; (4-(5-((2-amino-2,4-dimetilpentil)oxi)-6-(difluorometil)piridin-2-il)pirimidin-2-il)carbamato de (S)-metilo; (S)-1-((2',6-bis(fluorometil)-[2,4'-bipiridin]-5-il)oxi)-2,4-dimetilpentan-2-amina; (S)-1-((2'-(difluorometil)-6-(fluorometil)-[2,4'-bipiridin]-5-il)oxi)-2,4-dimetilpentan-2-amina; 2',6-bis(difluorometil)-5-((2-isobutilazetidin-2-il)metoxi)-2,4'-bipiridina; (S)-2,4-dimetil-1-(4-(2-metil-1H-pirrolo[2,3-b]piridin-4-il)-2-(trifluorometil) fenoxi) pentan-2-amina; (S)-2-((2-amino-2,4-dimetilpentil)oxi)-5-(2-metil-1H-pirrolo[2,3-b]piridin-4-il)benzonitrilo; (S)-2,4-dimetil-1-(2-metil-4-(2-metilpirimidin-4-il)fenoxi)pentan-2-amina; (S)-2,4-dimetil-1-(2-metil-4-(2-(trifluorometil)pirimidin-4-il)fenoxi)pentan-2-amina ; (S)-1-(2-fluoro-4-(2-(trifluorometil)pirimidin-4-il)fenoxi)-2,4-dimetilpentan-2-amina; (S)-1-(2-fluoro-4-(2-isopropilpirimidin-4-il)fenoxi)-2,4-dimetilpentan-2-amina; (S)-6-(5-((2-amino-2,4-dimetilpentil)oxi)-6-metilpiridin-2-il)pirimidin-4-amina; (S)-1-((2'-fluoro-4-metil-[2,4'-bipiridin]-5-il)oxi)-2,4-dimetilpentan-2-amina; (S)-2,4-dimetil-1-((6-metil-2'-(trifluorometil)-[2,4'-bipiridin]-5-il)oxi)pentan-2-amina; (S)-2,4-dimetil-1-((4-metil-2'-(trifluorometil)-[2,4'-bipiridin]-5-il)oxi)pentan-2-amina; (S)-1-(2-(difluorometil)-4-(6-metilpirimidin-4-il)fenoxi)-2,4-dimetilpentan-2-amina; (S)-1-(2-(fluorometil)-4-(2-metilpirimidin-4-il)fenoxi)-2,4-dimetilpentan-2-amina; (R)-2,4-dimetil-1-((2-metil-6-(2-metilpirimidin-4-il)piridin-3-il)oxi)pentan-2-amina; (S)-1-((6-(difluorometil)-2'-(fluorometil)-[2,4'-bipiridin]-5-il)oxi)-2,4-dimetilpentan-2-amina; (S)-1-((6-(difluorometil)-2'-(trifluorometil)-[2,4'-bipiridin]-5-il)oxi)-2,4-dimetilpentan-2-amina; (S)-2,4-dimetil-1-(5-metil-2-(piridin-4-il)tiazol-4-iloxi)pentan-2-amina; ...

10. 发明专利

AU2016243937A1 Inhibitors of indoleamine 2,3-dioxygenase for the treatment of cancer 未知
公开(公告)号：AU2016243937A1
公开(公告)日：2017-11-23
申请号：AU2016243937
申请日：2016-04-01
申请人： SQUIBB BRISTOL MYERS CO
发明人： BALOG JAMES AARON , CHERNEY EMILY CHARLOTTE , GUO WEIWEI , HUANG AUDRIS , MARKWALDER JAY A , SEITZ STEVEN P , SHAN WEIFANG , WILLIAMS DAVID K , MURUGESAN NATESAN , NARA SUSHEEL JETHANAND , ROY SAUMYA , THANGAVEL SOODAMANI , SISTLA RAMESH KUMAR , CHERUKU SRINIVAS , THANGATHIRUPATHY SRINIVASAN , KANYABOINA YADAGIRI , PULICHARLA NAGALAKSHMI
IPC分类号： C07D309/14 , A61K31/136 , A61K31/17 , A61P35/00 , C07C229/00 , C07D239/42 , C07D261/14 , C07D317/66 , C07D335/02 , C07D401/12 , C07D405/12 , C07D409/12 , C07D487/04
摘要： There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.

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