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公开(公告)号：US20220395501A1
公开(公告)日：2022-12-15
申请号：US17692753
申请日：2022-03-11
IPC分类号： A61K31/506 , C07D401/12 , C07D239/42 , C07D491/052 , C07D413/14 , C07D403/14 , C07D498/04 , C07D495/04 , C07D239/30 , C07D403/12 , C07D401/14 , C07D417/14 , C07D491/048 , C07D471/04 , C07D519/00 , C07D513/04 , C07D487/04 , C07D409/14 , C07D239/48 , C07D239/47 , A61K31/519 , A61K31/517 , A61K31/53 , A61K31/5377 , A61K31/541 , A61K31/551
摘要： The invention relates to treatment of graft versus host disease (GVHD) using compounds that inhibit ROCK2. In preferred aspects, the present invention provides methods for the treatment of GVHD, including chronic GVHD (cGVHD) using compounds having the formulae I-XXV, as set forth herein.
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公开(公告)号：US11440918B2
公开(公告)日：2022-09-13
申请号：US17667898
申请日：2022-02-09
发明人： Adam Galan , Wendy Luo , Ritu Lal
IPC分类号： C07D491/107 , A61P31/14 , C07D207/12 , C07D211/42 , C07D211/46 , C07D239/30 , C07D241/08 , C07D265/30 , C07D267/10 , C07D491/048 , C07D498/18
摘要： Disclosed herein are p38α mitogen-activated protein kinase inhibitors, pharmaceutical compositions thereof, and therapeutic methods of using the p38α mitogen-activated protein kinase inhibitors.
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公开(公告)号：US20220177495A1
公开(公告)日：2022-06-09
申请号：US17530119
申请日：2021-11-18
申请人： Sprint Bioscience AB
IPC分类号： C07F5/04 , C07D213/64 , C07D213/68 , C07D213/69 , C07D239/30 , C07D239/47 , C07D241/04 , C07D401/04 , C07D401/14 , C07D413/04 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The invention provides novel pyridinamine-pyridone and pyrimidinamine-pyridone compounds of formula (I), pharmaceutical compositions containing such compounds, and methods for using such compounds in treatment of diseases including cancer, type II diabetes, inflammatory disease, neurodegenerative disorders, cardiovascular disorders, autoimmune diseases and viral infections; wherein R1, R2, R3 and Z are as defined in the specification.
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公开(公告)号：US11337941B2
公开(公告)日：2022-05-24
申请号：US16804353
申请日：2020-02-28
发明人： Anne Bertolotti , Indrajit Das , Agnieszka Krzyzosiak , Adrien Rousseau , Kim Schneider , Anna Gudny Sigurdardottir
IPC分类号： A61K31/155 , C07C281/18 , A61P25/28 , A61P25/14 , A61P21/00 , C12Q1/42 , C07D239/30 , C07D213/61 , G01N33/573 , C12N11/14 , G01N21/31 , G01N33/53
摘要： The present invention relates to inhibitors of PPP1 R15A and PPP1 R15B and their use in therapy, particularly in the treatment of a disease state alleviated by the inhibition of PPP1 R15A and PPP1 R15B, for example a disorder associated with accumulation of misfolded proteins or proteostatsis disorder. Compounds of the invention include compounds having the formula IA or a pharmaceutically acceptable salt thereof, wherein R1a, R3a, R5a, Xa and Ya are as defined herein.
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公开(公告)号：US10662186B2
公开(公告)日：2020-05-26
申请号：US16067158
申请日：2016-12-30
发明人： Guangxin Xia , Qian Wang , Chen Shi , Xiong Zhai , Hui Ge , Xuemei Liao , Yu Mao , Zhixiong Xiang , Yanan Han , Guoyong Huo , Yanjun Liu
IPC分类号： A61K31/506 , C07D239/30 , C07D471/04 , A61P35/00 , C07F5/02 , C07F7/08 , C07F9/6561 , C07F9/6584
摘要： The present invention discloses a nitrogen-containing fused heterocyclic compound, as well as a preparation method, intermediate, composition and application thereof. The nitrogen-containing fused heterocyclic compound of the present invention as represented by formula (I), as well as the pharmaceutically acceptable salt, enantiomer, diastereomer, tautomer, solvate, metabolite or drug precursor thereof, exhibit a high selectivity and a high inhibitory activity with respect to CDK4 and CDK6 at a molecular level, an excellent inhibitory activity with respect to breast cancer cells at a cellular level, and significant inhibition of tumor cell proliferation associated with cyclin-dependent kinase activity at an animal level. The invention also exhibits a good stability with respect to human or mouse liver microsomes without significant inhibition of metabolic enzymes, good in vivo absorption in mice and rats, a high bioavailability and good druggability.
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公开(公告)号：US20200039903A1
公开(公告)日：2020-02-06
申请号：US16499478
申请日：2018-03-26
申请人： Merck Patent GmbH
IPC分类号： C07C25/18 , C07D213/06 , C07D213/127 , C07D401/14 , C07D405/14 , C07D471/04 , C07C17/35 , C07C43/225 , C07C41/18 , C07F7/08 , C07C25/22 , C07D239/30
摘要： The present invention relates to aromatic compounds suitable for preparation of asymmetric polydentate ligands. The present invention further describes a process for preparing asymmetric polydentate ligands and metal complexes comprising these ligands which are suitable for use as emitters in organic electroluminescent devices.
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公开(公告)号：US10435385B2
公开(公告)日：2019-10-08
申请号：US15871552
申请日：2018-01-15
发明人： Kei Yoshida , Takeo Wakita , Hiroyuki Katsuta , Akiyoshi Kai , Yutaka Chiba , Kiyoshi Takahashi , Hiroko Kato , Nobuyuki Kawahara , Michikazu Nomura , Hidenori Daido , Junji Maki , Shinichi Banba
IPC分类号： C07C237/42 , C07D333/38 , A01N37/44 , A01N43/08 , A01N43/10 , A01N43/12 , A01N43/16 , A01N43/30 , A01N43/40 , A01N43/42 , A01N43/54 , A01N43/56 , A01N43/58 , A01N43/78 , A01N43/80 , C07C317/40 , C07C323/42 , C07C327/48 , C07D207/416 , C07D213/64 , C07D213/73 , C07D213/81 , C07D213/82 , C07D213/89 , C07D215/52 , C07D231/14 , C07D231/16 , C07D239/30 , C07D241/24 , C07D263/34 , C07D275/03 , C07D277/56 , C07D307/24 , C07D307/68 , C07D307/84 , C07D309/08 , C07D309/28 , C07D317/62 , C07D333/68 , A01N37/22 , A01N43/60 , C07C237/48 , C07D207/34 , C07D239/28 , C07D261/18 , C07D307/85 , C07D317/46
摘要： A compound represented by Formula (1): The compound can be used as insecticides.
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公开(公告)号：US10369149B2
公开(公告)日：2019-08-06
申请号：US15567224
申请日：2015-12-30
发明人： Jong Yeon Hwang , Hyoung Rae Kim , Jae Du Ha , Sung Yun Cho , Hee Jung Jung , Pilho Kim , Chang Soo Yun , Chong Ock Lee , Chi Hoon Park , Chong Hak Chae , Sunjoo Ahn
IPC分类号： A61K31/506 , C07D239/30 , C07D239/48 , A23L33/10 , A61P35/00 , C07B43/04 , C07C13/48
摘要： The present invention relates to a 4-(2-amino-tetrahydronaphthaleneyl)pyrimidine derivative, a preparation method thereof, and a pharmaceutical composition for the prevention or treatment of cancer comprising the same as an active ingredient. The 4-(2-amino-tetrahydronaphthaleneyl)pyrimidine derivative, the optical isomer thereof, or the pharmaceutically acceptable salt thereof of the present invention is very effective in suppressing anaplastic lymphoma kinase (ALK) activity and as a result it can improve the effectiveness of treatment on cancer cells having anaplastic lymphoma kinase (ALK) fusion proteins such as EML4-ALK and NPM-ALK, so that it can be effectively used as a pharmaceutical composition for preventing or treating cancer.
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公开(公告)号：US20180134681A1
公开(公告)日：2018-05-17
申请号：US15871552
申请日：2018-01-15
发明人： Kei Yoshida , Takeo Wakita , Hiroyuki Katsuta , Akiyoshi Kai , Yutaka Chiba , Kiyoshi Takahashi , Hiroko Kato , Nobuyuki Kawahara , Michikazu Nomura , Hidenori Daido , Junji Maki , Shinichi Banba
IPC分类号： C07D333/38 , C07D317/46 , C07D213/64 , C07D239/28 , C07D261/18 , C07D307/85 , C07C237/48 , A01N43/60 , A01N37/22 , C07D207/416 , C07C327/48 , C07C323/42 , C07C317/40 , C07C237/42 , A01N43/80 , A01N43/78 , A01N43/58 , A01N43/56 , A01N43/54 , A01N43/42 , A01N43/40 , A01N43/30 , A01N43/16 , A01N43/12 , A01N43/10 , A01N43/08 , A01N37/44 , C07D333/68 , C07D317/62 , C07D309/28 , C07D309/08 , C07D307/84 , C07D307/68 , C07D307/24 , C07D277/56 , C07D275/03 , C07D263/34 , C07D241/24 , C07D239/30 , C07D231/16 , C07D231/14 , C07D215/52 , C07D213/89 , C07D213/82 , C07D213/81 , C07D213/73 , C07D207/34
CPC分类号： C07D333/38 , A01N37/22 , A01N37/44 , A01N43/08 , A01N43/10 , A01N43/12 , A01N43/16 , A01N43/30 , A01N43/40 , A01N43/42 , A01N43/54 , A01N43/56 , A01N43/58 , A01N43/60 , A01N43/78 , A01N43/80 , C07C237/42 , C07C237/48 , C07C317/40 , C07C323/42 , C07C327/48 , C07D207/34 , C07D207/416 , C07D213/64 , C07D213/73 , C07D213/81 , C07D213/82 , C07D213/89 , C07D215/52 , C07D231/14 , C07D231/16 , C07D239/28 , C07D239/30 , C07D241/24 , C07D261/18 , C07D263/34 , C07D275/03 , C07D277/56 , C07D307/24 , C07D307/68 , C07D307/84 , C07D307/85 , C07D309/08 , C07D309/28 , C07D317/46 , C07D317/62 , C07D333/68
摘要： An object of the present invention is to provide a compound represented by Formula (1): wherein A1, A2, A3 and A4 each represent a carbon atom, a nitrogen atom or an oxidized nitrogen atom; R1 and R2 each represent a hydrogen atom, an optionally substituted alkyl group or an optionally substituted C1-C4 alkylcarbonyl group; G1 and G2 each represent an oxygen atom or a sulfur atom; X, which may be identical or different each other, represents a hydrogen atom, a halogen atom, a C1-C3 alkyl group or a trifluoromethyl group; n is an integer of 0 to 4; and Q1 represents an optionally substituted phenyl group, an optionally substituted naphthyl group or an optionally substituted heterocyclic group; Q2 represents a phenyl group or heterocyclic group having one or more substituents, at least one of the substituent being any of a C1-C4 haloalkoxy group, a C2-C6 perfluoroalkyl group, a C1-C6 perfluoroalkylthio group, a C1-C6 perfluoroalkylsulfinyl group and a C1-C6 perfluoroalkylsulfonyl group, an insecticide comprising the compound as the active ingredient, and a process for preparation thereof.
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公开(公告)号：US20180086723A1
公开(公告)日：2018-03-29
申请号：US15828163
申请日：2017-11-30
申请人： University of Pittsburgh - Of the Commonwealth System of Higher Education , The United States Government as Represented by the Department of Veterans Affairs
发明人： Raju Reddy
IPC分类号： C07D241/20 , C07D241/18 , C07D241/16 , C07D241/12 , C07D239/52 , C07D239/26 , C07D239/42 , C07D239/38 , C07D239/34 , C07D239/30 , C07D239/47
CPC分类号： C07D241/20 , C07D239/26 , C07D239/30 , C07D239/34 , C07D239/38 , C07D239/42 , C07D239/47 , C07D239/52 , C07D241/12 , C07D241/16 , C07D241/18
摘要： Disclosed is a compound, or a pharmaceutically acceptable salt or ester thereof, having a structure of: X1-L-X2 wherein L is a linking moiety comprising an enone; and X1 and X2 are each independently an optionally-substituted N-heterocycle. Also disclosed are method for treating pulmonary conditions and other organ or system conditions with the compounds.
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