公开(公告)号：US20170349577A1

公开(公告)日：2017-12-07

申请号：US15537805

申请日：2015-12-17

Applicant: GlaxoSmithKline Intellectual Property Development Limited

Inventor： Anne Marie Jeanne BOUILLOT ,  Alexis DENIS ,  Ann Louise WALKER ,  John LIDDLE

IPC: C07D413/12

CPC classification number: C07D413/12

Abstract: Compound of formula (I) wherein: R1 is heteroaryl either unsubstituted or substituted by methyl, ethyl, halo or ═O; and R2 is H, methyl or ethyl; and salts thereof are KMO inhibitors and may be useful in the treatment of various disorders, for example acute pancreatitis, chronic kidney disease, acute kidney disease, acute kidney injury, other conditions associated with systemic inflammatory response syndrome (SIRS), Huntington's disease, Alzheimer's disease, spinocerebellar ataxias, Parkinson's disease, AIDS-dementia complex, HIV infection, amylotrophic lateral sclerosis (ALS), depression, schizophrenia, sepsis, cardiovascular shock, severe trauma, acute lung injury, acute respiratory distress syndrome, acute cholecystitis, severe burns, pneumonia, extensive surgical procedures, ischemic bowel, severe acute hepatic disease, severe acute hepatic encephalopathy or acute renal failure.

公开(公告)号：US20170291899A1

公开(公告)日：2017-10-12

申请号：US15514416

申请日：2015-09-22

Applicant: GlaxoSmithKline Intellectual Property Development Limited

Inventor： Niall Andrew ANDERSON ,  Ian Baxter CAMPBELL ,  Matthew Howard James CAMPBELL-CRAWFORD ,  Ashley Paul HANCOCK ,  Seble LEMMA ,  Simon John Fawcett MACDONALD ,  John Martin PRITCHARD ,  Panayiotis Alexandrou PROCOPIOU

IPC: C07D471/04 ,  C07B59/00

CPC classification number: C07D471/04 ,  C07B59/002 ,  C07B2200/05

Abstract: A compound of formula (I) or a salt thereof: wherein R1 represents a five-membered aromatic heterocycle selected from a N- or a C-linked mono- or di-substituted pyrazole, an N- or a C-linked optionally mono- or di-substituted triazole or an N- or a C-linked optionally mono- or di-substituted imidazole, which five-membered aromatic heterocycle may be substituted by one or two of the groups selected a methyl group, an ethyl group, a fluorine atom, a hydroxymethyl group, a 2-hydroxypropan-2-yl group, a trifluoromethyl group, a difluoromethyl group or a fluoromethyl group, except that when R1 represents an N-linked mono- or di-substituted pyrazole, Ri does not represent 3,5-Dimethyl-1H-pyrazol-1-yl, 5-Methyl-1H-pyrazol-1-yl, 5-Ethyl-3-methyl-1H-pyrazol-1-yl, 3,5-Diethyl-1H-pyrazol-1-yl, 4-Fluoro-3,5-dimethyl-1H-pyrazol-1-yl, 3-Methyl-1H-pyrazol-1-yl or 1H-pyrazol-1-yl.

公开(公告)号：US20170290818A1

公开(公告)日：2017-10-12

申请号：US15514414

申请日：2015-09-22

Applicant: GlaxoSmithKline Intellectual Property Development Limited

Inventor： Niall Andrew ANDERSON ,  Matthew Howard James CAMPBELL-CRAWFORD ,  Ashley Paul HANCOCK ,  Seble LEMMA ,  Simon John Fawcett MACDONALD ,  John Martin PRITCHARD ,  Panayiotis Alexandrou PROCOPIOU ,  Stephen SWANSON

IPC: A61K31/4375 ,  C07D207/04 ,  C07D471/04

CPC classification number: A61K31/4375 ,  C07D207/04 ,  C07D471/04

Abstract: A compound according to formula (I) wherein R1 is hydrogen, cyclopropyl, or pyrazolyl, wherein said pyrazolyl is optionally substituted by one or two methyl groups; or a pharmaceutically acceptable salt thereof.

公开(公告)号：US09725407B2

公开(公告)日：2017-08-08

申请号：US15004039

申请日：2016-01-22

Applicant: GlaxoSmithKline Intellectual Property Development Limited

Inventor： Alan Hornsby Davidson ,  David Festus Charles Moffat ,  Francesca Ann Day ,  Alastair David Graham Donald

IPC: C07C259/06 ,  C07D211/58 ,  C07D211/34 ,  C07C311/19 ,  C07D213/56 ,  C07D215/22 ,  C07D241/04 ,  C07D333/70 ,  C07D409/12 ,  C07D471/04

CPC classification number: C07C259/06 ,  C07C311/19 ,  C07C2601/08 ,  C07C2601/14 ,  C07D211/34 ,  C07D211/58 ,  C07D213/56 ,  C07D215/22 ,  C07D241/04 ,  C07D333/70 ,  C07D409/12 ,  C07D471/04

Abstract: Compounds of formula (I) inhibit HDAC activity: wherein A, B and D independently represent ═C— or ═N—; W is a divalent radical —CH═CH— or CH2CH2—; R1 is an ester group; R2 is the side chain of a natural or non-natural alpha-amino acid; z is 0 or 1; and Y, L1, and X1 are as defined in the claims.

公开(公告)号：US20170119779A1

公开(公告)日：2017-05-04

申请号：US15319575

申请日：2014-06-16

Applicant: GlaxoSmithKline Intellectual Property Development Limited ,  The Chancellor, Masters and Scholars of the University of Cambridge

Inventor： Gordon Campbell Sinclair SMITH

IPC: A61K31/5377 ,  A61K9/00

CPC classification number: A61K31/5377 ,  A61K9/0019 ,  A61K9/0053

Abstract: The present invention relates to a method of treating pre-term labour with retosiban in subjects with conditions resulting in uterine overdistension including polyhydroamnios and multiple gestation. In another aspect, the invention relates to a method of preventing pre-term labour in subjects by the prophylactic administration of retosiban.

公开(公告)号：US09624202B2

公开(公告)日：2017-04-18

申请号：US15271581

申请日：2016-09-21

Applicant: GlaxoSmithKline Intellectual Property Development Limited

Inventor： Jae U. Jeong

IPC: A61K31/55 ,  C07D223/08 ,  C07D403/12 ,  A61K31/553 ,  C07D413/14 ,  C07D403/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D487/04 ,  C07D267/14 ,  C07D498/04 ,  C07D281/10

CPC classification number: A61K31/553 ,  A61K31/55 ,  C07D223/08 ,  C07D267/14 ,  C07D281/10 ,  C07D403/12 ,  C07D403/14 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D487/04 ,  C07D498/04

Abstract: Disclosed are compounds having the formula: wherein X, Y, Z1, Z2, Z3, Z4, R5, RA, m, A. L, and B are as defined herein, and methods of making and using the same.

公开(公告)号：US09586953B2

公开(公告)日：2017-03-07

申请号：US14397218

申请日：2013-09-13

Applicant: GlaxoSmithKline Intellectual Property Development Limited

Inventor： Linda N. Casillas ,  Pamela A. Haile ,  Robert W. Marquis, Jr.

IPC: C07D417/12 ,  A61K31/428 ,  A61K31/517 ,  C07F9/6561

CPC classification number: C07D417/12 ,  A61K31/09 ,  A61K31/198 ,  A61K31/381 ,  A61K31/428 ,  A61K31/433 ,  A61K31/517 ,  C07F9/6561

Abstract: Disclosed are compounds having the formula: wherein X is as defined herein, and methods of making and using the same.

Abstract translation: 公开了具有下式的化合物：其中X如本文所定义，及其制备和使用方法。

公开(公告)号：US20170008878A1

公开(公告)日：2017-01-12

申请号：US15271581

申请日：2016-09-21

Applicant: GlaxoSmithKline Intellectual Property Development Limited

Inventor： Deepak BANDYOPADHYAY ,  Patrick M. EIDAM ,  Peter J. GOUGH ,  Philip Anthony HARRIS ,  Jae U. JEONG ,  Jianxing KANG ,  Bryan Wayne KING ,  Ami LAKDAWALA SHAH ,  Lara Kathryn LEISTER ,  Robert W. MARQUIS, JR. ,  Attiq RAHMAN ,  Joshi M. RAMANJULU ,  Clark A. SEHON ,  Robert SINGHAUS, JR. ,  Daohua ZHANG

IPC: C07D403/12

CPC classification number: A61K31/553 ,  A61K31/55 ,  C07D223/08 ,  C07D267/14 ,  C07D281/10 ,  C07D403/12 ,  C07D403/14 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D487/04 ,  C07D498/04

Abstract: Disclosed are compounds having the formula: wherein X, Y, Z1, Z2, Z3, Z4, R5, RA, m, A. L, and B are as defined herein, and methods of making and using the same.

Abstract translation: 其中X，Y，Z 1，Z 2，Z 3，Z 4，R 5，RA，m，A L和B如本文所定义，以及制备和使用它们的方法。

公开(公告)号：US20160368911A1

公开(公告)日：2016-12-22

申请号：US14898782

申请日：2014-07-01

Applicant: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED

Inventor： Sebastien Andre CAMPOS ,  John David HARLING ,  Afjal Hussain MIAH ,  Ian Edward, David SMITH

IPC: C07D417/14 ,  C07D413/14 ,  A61K31/422 ,  A61K45/06 ,  C07D471/10 ,  A61K31/435 ,  C07K5/062 ,  A61K38/05 ,  A61K31/427 ,  A61K31/496

CPC classification number: C07D417/14 ,  A61K31/422 ,  A61K31/427 ,  A61K31/435 ,  A61K31/496 ,  A61K38/05 ,  A61K45/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D471/10 ,  C07K5/06052

Abstract: A compound of formula (I): or a pharmaceutically acceptable salt thereof, compositions, combinations and medicaments containing said compounds and processes for their preparation. The invention also relates to the use of said compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of the estrogen receptor, including degrading the estrogen receptor, the treatment of diseases and conditions mediated by the estrogen receptor,

Abstract translation: 或其药学上可接受的盐，含有所述化合物的组合物，组合和药物及其制备方法。 本发明还涉及所述化合物，组合，组合物和药物的用途，例如作为雌激素受体活性的抑制剂，包括降解雌激素受体，治疗由雌激素受体介导的疾病和病症，

公开(公告)号：US20160215059A1

公开(公告)日：2016-07-28

申请号：US15006560

申请日：2016-01-26

Applicant: GlaxoSmithKline Intellectual Property Development Limited

Inventor： Yao-Bin Liu ,  Patrick Mayes ,  Radha Shah Parmar

IPC: C07K16/28 ,  C07K16/30 ,  A61K45/06

CPC classification number: C07K16/2818 ,  A61K39/3955 ,  A61K39/39558 ,  A61K45/06 ,  A61K2039/505 ,  A61K2039/507 ,  C07K16/2803 ,  C07K16/2896 ,  C07K16/30 ,  C07K16/3015 ,  C07K16/3023 ,  C07K16/3038 ,  C07K16/3069 ,  C07K2317/21 ,  C07K2317/24 ,  C07K2317/33 ,  C07K2317/56 ,  C07K2317/565 ,  C07K2317/71 ,  C07K2317/75 ,  C07K2317/92

Abstract: The present invention relates to an ICOS binding protein, or antigen binding portion thereof that is an agonist human ICOS and does not induce complement, ADCC, or CDC when placed in contact with a T cell in vivo and methods of treating cancer, infectious disease and/or sepsis with said ICOS binding protein or antigen binding portion thereof. Further the ICOS binding proteins or antigen binding portions thereof of the present invention are capable of activating a T cell when placed in contact with said T cell; stimulating T cell proliferation when placed in contact with said T cell and/or inducing cytokine production when placed in contact with said T cell. The present invention relates to ICOS binding proteins or antigen binding portions thereof comprising one or more oft SEQ ID NO:1; SEQ ID NO:2; SEQ ID NO:3; SEQ ID NO:4; SEQ ID NO:5; and/or SEQ ID NO:6.

Abstract translation: 本发明涉及ICOS结合蛋白或其抗原结合部分，其是激动剂人ICOS，并且当其与体内的T细胞接触时不诱导补体，ADCC或CDC，以及治疗癌症，感染性疾病和 /或与所述ICOS结合蛋白或其抗原结合部分的败血症。 此外，本发明的ICOS结合蛋白或其抗原结合部分当与所述T细胞接触时能够激活T细胞; 当与所述T细胞接触时刺激T细胞增殖和/或当与所述T细胞接触时诱导细胞因子产生。 本发明涉及包含SEQ ID NO：1中的一个或多个的ICOS结合蛋白或其抗原结合部分; SEQ ID NO：2; SEQ ID NO：3; SEQ ID NO：4; SEQ ID NO：5; 和/或SEQ ID NO：6。