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51. 发明专利

PE20211701A1 COMPUESTOS BICICLICOS SUSTITUIDOS COMO MODULADORES DEL RECEPTOR FARNESOIDE X 未知
公开(公告)号：PE20211701A1
公开(公告)日：2021-09-01
申请号：PE2021001326
申请日：2020-02-14
申请人： SQUIBB BRISTOL MYERS CO
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： A61K31/427 , C07D217/06 , A61P3/06 , A61P13/00 , A61P35/00 , C07D403/12 , C07D413/12 , C07D413/14 , C07D417/12
摘要： SE REFIERE A COMPUESTOS BICICLICOS SUSTITUIDOS DE FORMULA (I) DONDE A, Q, X1, X2, X3, X4, R2, R3a, R3b, Z1, Z2, a, b Y d SON COMO SE DEFINEN EN LA DESCRIPCION. SON COMPUESTOS PREFERIDOS: N-((4-(4-CICLOPROPILFENIL)BICICLO[2.2.2]OCTAN-1-IL)METIL)-N-(3-(3-METIL-1,2,4-OXADIAZOL-5-IL)FENIL)ISOBUTIRAMIDA; N-(3-(3-ETIL-1,2,4-OXADIAZOL-5-IL)FENIL)-3-FLUORO-N-((4-(3-METIL-1,2,4-OXADIAZOL-5-IL)BICICLO[2.2.2]OCTAN-1-IL)METIL)BICICLO[1.1.1]PENTANO-1-CARBOXAMIDA; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON MODULADORES DEL RECEPTOR FARNESOIDE X (FXR) SIENDO UTILES EN EL TRATAMIENTO DE FIBROSIS PATOLOGICA, RECHAZO DE TRASPLANTES, CANCER, OSTEOPOROSIS, TRASTORNOS INFLAMATORIOS.

52. 发明专利

ES2822956T3 Compuestos de aminopiridina sustituidos con heteroarilo 未知
公开(公告)号：ES2822956T3
公开(公告)日：2021-05-05
申请号：ES16734832
申请日：2016-06-23
申请人： SQUIBB BRISTOL MYERS CO
发明人： DUNCIA JOHN V , GARDNER DANIEL S , HYNES JOHN , MACOR JOHN E , SANTELLA JOSEPH B , WU HONG , NAIR SATHEESH KESAVAN , PAIDI VENKATRAM REDDY , SARKUNAM KANDHASAMY , SISTLA RAMESH KUMAR , POLIMERA SUBBA RAO
IPC分类号： C07D487/04 , A61K31/5025 , A61K31/519 , A61P37/00
摘要： Un compuesto de Formula (I) **(Ver fórmula)** o una sal del mismo, en donde: HET es un heteroarilo seleccionado de imidazo[1,2-b]piridazinilo y pirazolo[1,5-a]pirimidinilo, en donde dicho heteroarilo esta unido al grupo piridinilo en el compuesto de Formula (I) mediante un atomo del anillo de carbono en dicho heteroarilo y en donde dicho heteroarilo esta sustituido con de cero a 2 Rb; A es pirazolilo, imidazolilo o triazolilo, cada uno sustituido con cero o 1 Ra; R3 es: (i) -CH2CH3, -CH(CH3)2, -CH2CHF2, -CH(CH3)CH2OH, oxetanilo, tetrahidropiranilo o cicloalquilo C3-5 sustituido con de cero a 2 F; (ii) pirazolilo sustituido con de cero a 2 sustituyentes seleccionados independientemente de alquilo C1-3, hidroxialquilo C1-3, fluoroalquilo C1-3, oxetanilo, tetrahidrofuranilo y tetrahidropiranilo; Ra es: (i) F, Cl, -OH, -CN, alquilo C1-6, fluoroalquilo C1-4, cianoalquilo C1-4 o hidroxialquilo C1-6; o (ii) cicloalquilo C3-6, azetidinilo, oxetanilo, tetrahidrofuranilo, tetrahidropiranilo, piperidinilo, piperazinilo, pirrolilo, pirrolidinonilo, morfolinilo, pirrolidinilo, fenilo, pirazolilo, imidazolilo, piridinilo o pirimidinilo, cada uno sustituido con de cero a 4 sustituyentes seleccionados independientemente de F, -CN, -OH, -NRyRy, alquilo C1-3, fluoroalquilo C1-3, -CH(fenilo)2, -O(alquilo C1-4), -C(O)(alquilo C1-4), -C(O)(deuteroalquilo C1-4), -C(O)(cicloalquilo C3-6), -C(O)O(alquilo C1-4), -C(O)NRyRy, -C(O)(fenilo), -C(O)(piridinilo), -C(O)CH2(cicloalquilo C3-6), - NHC(O)CH3, - NHC(O)OCH3, -NHC(O)OC(CH3)3, -S(O)2(alquilo C1-3) y -OS(O)2(alquilo C1-3); cada Rb se selecciona independientemente de F, Cl, -CN, -NH2, -CH3, -OCH3 y ciclopropilo; y cada Ry es independientemente H o alquilo C1-3.

53. 发明专利

CA3129619A1 SUBSTITUTED AMIDE COMPOUNDS USEFUL AS FARNESOID X RECEPTOR MODULATORS 未知
公开(公告)号：CA3129619A1
公开(公告)日：2020-08-20
申请号：CA3129619
申请日：2020-02-14
申请人： SQUIBB BRISTOL MYERS CO
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： C07C233/56 , A61K31/165 , A61K31/35 , A61K31/4196 , C07D271/06 , C07D277/64 , C07D295/04 , C07D405/04 , C07D405/14 , C07D413/04
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.

54. 发明专利

TN2016000271A1 HETEROARYL SUBSTITUTED NICOTINAMIDE COMPOUNDS. 未知
公开(公告)号：TN2016000271A1
公开(公告)日：2017-10-06
申请号：TN2016000271
申请日：2015-01-02
申请人： SQUIBB BRISTOL MYERS CO
发明人： ARUNACHALAM PIRAMANAYAGAM , DUNCIA JOHN V , GARDNER DANIEL S , HYNES JOHN , KUMAR SREEKANTHA RATNA , MURUGESAN NATESAN , NAIR SATHEESH KESAVAN , PAIDI VENKATRAM REDDY , SANTELLA JOSEPH B , SARKUNAM KANDHASAMY , WU HONG
IPC分类号： A61K31/437 , A61K31/455 , A61K31/519 , A61K31/52 , A61P29/00 , A61P37/00 , C07D401/04 , C07D401/14 , C07D471/04 , C07D473/00 , C07D487/04
摘要： Disclosed are compounds of Formula (1) or salts thereof, wherein: HET is a heteroaryl selected from pyrazolyl, indolyl, pyrrolo[2,3-b]pyridinyl, pyrrolo[2,3-d]pyrimidinyl, pyrazolo[3,4-b]pyridinyl, pyrazolo[3,4-d]pyrimidinyl, 2,3-dihydro-1H-pyrrolo[2,3-b]pyridinyl, imidazo[4,5-b] pyridinyl, and purinyl, wherein said heteroaryl is substituted with R a and R b ; and R 1 and R 2 are define herein. Also disclosed are methods of using such compounds as modulators of IRAK4, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing inflammatory and autoimmune diseases.

55. 发明专利

PE09292015A1 INHIBIDORES DEL VIRUS DE LA HEPATITIS C 未知
公开(公告)号：PE09292015A1
公开(公告)日：2015-06-13
申请号：PE0005052015
申请日：2012-10-19
申请人： SQUIBB BRISTOL MYERS CO
发明人： SUN LI-QIANG , MULL ERIC , GILLIS ERIC P , BOWSHER MICHAEL S , ZHAO QIAN , RENDUCHINTALA KISHORE V , SARKUNAM KANDHASAMY , NAGALAKSHMI PULICHARLA , BABU SURESH P V K , SCOLA PAUL MICHAEL
IPC分类号： C07D487/04 , A61K38/12 , A61K38/55
摘要： La invencion describe inhibidores del virus de la Hepatitis C que presentan la formula general (I): Tambien se describen composiciones que comprenden los compuestos y metodos para el uso de los compuestos para inhibir el VHC. Los compuestos preferidos son: ((2R, 6S, 7R. 9R, 13aS, 14aR, 16aS, Z)-14a-(((1-(fluorometil) ciclopropil) sulfonil) carbamoil)-2-((3-(4-isopropoxifenil)-6-metoxiisoquinolin-1-il) oxi)-7, 9-dimetil-5,16-dioxo-1,2,3,5,6,7,8,9,10, 11, 13ª, 14, 14a, 15, 16, 16a-hexadecahidrociclopropa[e] pirrolo[1, 2- a][1, 4] diazaciclopentadecin-6-il) carbamato de (R)-3-(trifluorometil) tetrahidro-2H-piran-3-ilo; ((2R, 6S, 7R, 9R, 13aS, 14aR, 16aS, Z)-2-((7-fluoro-6-metoxiisoquinolin-1-il) oxi)-14a-(((1-(fluorometil) ciclopropil) sulfonil) carbamoil)-7, 9-dimetil-5 , 16-dioxo-1, 2, 3, 5, 6, 7, 8, 9, 10, 11, 13a, 14, 14a, 15, 16, 16a-hexadecahidrociclopropa[e] pirrolo[1, 2-a] [1, 4]diazaciclopentadecin-6-il) carbamato de 1, 1, 1,-trifluoro-2-metilpropan-2-ilo, entre otros

56. 发明专利

NZ618594A Hepatitis c virus inhibitors 未知
公开(公告)号：NZ618594A
公开(公告)日：2015-02-27
申请号：NZ61859412
申请日：2012-05-01
申请人： SQUIBB BRISTOL MYERS CO
发明人： MEANWELL NICHOLAS A , HIEBERT SHELDON , RAJAMANI RAMKUMAR , SUN LI-QIANG , MULL ERIC , GILLIS ERIC P , BOWSHER MICHAEL S , ZHAO QIAN , RENDUCHINTALA KISHORE V , SARKUNAM KANDHASAMY , NAGALAKSHMI PULICHARLA , BABU P V K SURESH , SCOLA PAUL MICHAEL
IPC分类号： C07K5/12 , A61K38/12 , C07D487/04
摘要： Disclosed are macrocyclic peptide-based inhibitors of hepatitis C virus (HCV) compounds of formula (I) where the substituents are as disclosed in the specification. Examples of compounds of formula (I) are: 1,1,1-trifluoro-2-methylpropan-2-yl (2R,6S,7R,9R,13aS,14aR,16aS,Z)- 14a-(cyclopropylsulfonylcarbamoyl)-7-ethyl-2-(4-methoxyisoquinolin-1-yloxy)-9-methyl-5,16-dioxo-1,2,3,5,6,7,8,9,10,11,13a,14,14a,15,16,16ahexadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecin-6-ylcarbamate; tert-butyl ((2R,6S,7R,9S,13aS,14aR,16aS,Z)-7-ethyl-14a-(((1-(fluoromethyl)cyclopropyl)sulfonyl)carbamoyl)-2-((3-methoxyisoquinolin-1-yl)oxy)-9-methyl-5,16-dioxo-1,2,3,5,6,7,8,9,10,11,13a,14,14a,15,16,16ahexadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecin-6-yl)carbamate and (2R,6S,7R,9R,13aR,14aR,16aS)-6-(3-(tert-butyl)ureido)-N-((1- (fluoromethyl)cyclopropyl)sulfonyl)-2-((4-methoxyisoquinolin-1-yl)oxy)-7,9-dimethyl-5,16-dioxooctadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a-carboxamide.

57. 发明专利

MA35160B1 Inhibiteur du virus de l'hépatite c 未知
公开(公告)号：MA35160B1
公开(公告)日：2014-06-02
申请号：MA36507
申请日：2013-11-29
申请人： SQUIBB BRISTOL MYERS CO
发明人： ZHAO QIAN , MEANWELL NICHOLAS A , HIEBERT SHELDON , RAJAMANI RAMKUMAR , SUN LI-QIANG , MULL ERIC , GILLIS ERIC P , BOWSHER MICHAEL S , RENDUCHINTALA KISHORE V , SARKUNAM KANDHASAMY , NAGALAKSHMI PULICHARLA , BABU P V K SURESH , SCOLA PAUL MICHAEL
IPC分类号： C07K5/12
摘要： L'invention concerne des inhibiteurs du virus de l'hépatite c ayant la formule générale (i) suivante. Elle concerne également des compositions comprenant les composés et les procédés d'utilisation de ces composés pour inhiber le vhc.

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