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11. 发明授权

US08426414B2 Modulators of G protein-coupled receptor 88 有权
公开(公告)号：US08426414B2
公开(公告)日：2013-04-23
申请号：US12897004
申请日：2010-10-04
申请人： Yingzhi Bi , Carolyn Diane Dzierba , Joanne J. Bronson , Cynthia Fink , Michael Green , David Kimball , John E. Macor , Soojin Kwon , Yulian Zhang , Greg Zipp
发明人： Yingzhi Bi , Carolyn Diane Dzierba , Joanne J. Bronson , Cynthia Fink , Michael Green , David Kimball , John E. Macor , Soojin Kwon , Yulian Zhang , Greg Zipp
IPC分类号： C07D213/56 , C07D241/12 , A61K31/4418 , A61K31/4965 , A61P25/00
CPC分类号： C07D213/56 , C07D241/12
摘要： The present disclosure is generally directed to compounds which can modulate G-protein coupled receptor 88, compositions comprising such compounds, and methods for modulating G-protein coupled receptor 88.

12. 发明授权

US08217156B2 Solid forms of (2S,3R,4R,5S,6R)-2-(4-chloro-3-(4-ethoxybenzyl)phenyl)-6-(methylthio)tetrahydro-2H-pyran-3,4,5-triol and methods of their use 有权
标题翻译：（2S，3R，4R，5S，6R）-2-（4-氯-3-（4-乙氧基苄基）苯基）-6-（甲硫基）四氢-2H-吡喃-3,4,5-三醇及其使用方法
公开(公告)号：US08217156B2
公开(公告)日：2012-07-10
申请号：US12503225
申请日：2009-07-15
申请人： Susan Margaret De Paul , Anett Perlberg , Matthew Mangzhu Zhao
发明人： Susan Margaret De Paul , Anett Perlberg , Matthew Mangzhu Zhao
IPC分类号： C07H15/203 , C07H5/10
CPC分类号： C07H15/14 , A61K31/7028 , A61K31/7034 , C07H7/04
摘要： Solid forms of anhydrous (2S,3R,4R,5S,6R)-2-(4-chloro-3-(4-ethoxybenzyl)phenyl)-6-(methylthio)tetrahydro-2H-pyran-3,4,5-triol are disclosed, in addition to methods of their use in the treatment of various diseases and disorders.
摘要翻译：固体形式的无水（2S，3R，4R，5S，6R）-2-（4-氯-3-（4-乙氧基苄基）苯基）-6-（甲硫基）四氢-2H-吡喃-3,4,5- 除了它们用于治疗各种疾病和病症的方法之外，还公开了三醇。

13. 发明申请

US20110082178A1 METHODS OF TREATING AUTOIMMUNE AND INFLAMMATORY DISEASES AND DISORDERS 审中-公开
标题翻译：治疗自身免疫和炎症疾病和疾病的方法
公开(公告)号：US20110082178A1
公开(公告)日：2011-04-07
申请号：US12903657
申请日：2010-10-13
申请人： David J. Augeri , Jeffrey Bagdanoff , Simon D.P. Baugh , Kenneth G. Carson , Theodore C. Jessop , James E. Tarver
发明人： David J. Augeri , Jeffrey Bagdanoff , Simon D.P. Baugh , Kenneth G. Carson , Theodore C. Jessop , James E. Tarver
IPC分类号： A61K31/422 , A61K31/427 , A61K31/4196 , A61K31/4178 , A61P29/00 , A61P37/00 , A61P37/06 , A61P11/06 , A61P25/00 , A61P21/04 , A61P17/06 , A61P19/02 , A61P3/10
CPC分类号： C07D403/04 , C07D413/04 , C07D417/04
摘要： Heterocyclic compounds, compositions comprising them, and methods of their use for the treatment, prevention and management of inflammatory and autoimmune diseases and disorders are disclosed. Particular compounds are of formula I:
摘要翻译：公开了杂环化合物，包含它们的组合物及其用于治疗，预防和治疗炎性和自身免疫疾病和病症的方法。特定的化合物具有式I：

14. 发明授权

US07875622B2 Methods and compositions for treating pulmonary hypertension and related diseases and disorders 有权
标题翻译：用于治疗肺动脉高压及相关疾病和病症的方法和组合物
公开(公告)号：US07875622B2
公开(公告)日：2011-01-25
申请号：US12169815
申请日：2008-07-09
申请人： Arthur T. Sands
发明人： Arthur T. Sands
IPC分类号： A61K31/505
CPC分类号： A61K31/5585 , A61K31/198 , A61K31/405 , A61K31/4192 , A61K31/4418 , A61K31/4965 , A61K31/497 , A61K31/505 , A61K31/53 , A61K31/5377 , A61K31/5578 , A61K45/06
摘要： Methods of treating pulmonary hypertension are disclosed. Particular methods comprise the administration of a tryptophan hydroxylase inhibitor and at least one other active pharmaceutical ingredient to patient in need thereof. Pharmaceutical formulations are also disclosed.
摘要翻译：公开了治疗肺动脉高压的方法。具体的方法包括向有需要的患者施用色氨酸羟化酶抑制剂和至少一种其它活性药物成分。还公开了药物制剂。

15. 发明授权

US07723345B2 Multicyclic amino acid derivatives and methods of their use 有权
标题翻译：多环氨基酸衍生物及其使用方法
公开(公告)号：US07723345B2
公开(公告)日：2010-05-25
申请号：US11638677
申请日：2006-12-12
申请人： Arokiasamy Devasagayaraj , Haihong Jin , Brett Marinelli , Lakshama Samala , Zhi-Cai Shi , Ashok Tunoori , Ying Wang , Chengmin Zhang
发明人： Arokiasamy Devasagayaraj , Haihong Jin , Brett Marinelli , Lakshama Samala , Zhi-Cai Shi , Ashok Tunoori , Ying Wang , Chengmin Zhang
IPC分类号： A61K31/505 , C07D239/02
CPC分类号： C07D251/18 , C07B2200/07 , C07C229/36 , C07C229/42 , C07C229/44 , C07C275/42 , C07C311/29 , C07C2601/08 , C07D213/74 , C07D239/34 , C07D239/42 , C07D239/47 , C07D239/48 , C07D241/20 , C07D241/24 , C07D249/06 , C07D251/16 , C07D251/22 , C07D251/52 , C07D401/04 , C07D403/04 , C07D403/12 , C07D409/04 , C07D409/12 , C07D413/12
摘要： Compounds of formulae I and II are disclosed, as well as compositions comprising them and methods of their use to treat, prevent and manage serotonin-mediated diseases and disorders:
摘要翻译：公开了式I和II的化合物，以及包含它们的组合物及其用于治疗，预防和控制5-羟色胺介导的疾病和障碍的方法：

16. 发明授权

US07332338B2 Vectors for making genomic modifications 有权
标题翻译：用于进行基因组修饰的载体
公开(公告)号：US07332338B2
公开(公告)日：2008-02-19
申请号：US10917273
申请日：2004-08-11
申请人： Brian Zambrowicz , Glenn A. Friedrich , Arthur T. Sands
发明人： Brian Zambrowicz , Glenn A. Friedrich , Arthur T. Sands
IPC分类号： C12N15/00 , C12N15/86 , C07H21/04
CPC分类号： C12N15/86 , A01K2217/075 , C12N15/102 , C12N15/1051 , C12N15/1065 , C12N15/1086 , C12N15/85 , C12N2740/13043 , C12N2800/60 , C12N2840/203 , C12N2840/44
摘要： Methods and vectors (both DNA and retroviral) are provided for the construction of a Library of mutated cells. The Library will preferably contain mutations in essentially all genes present in the genome of the cells. The nature of the Library and the vectors allow for methods of screening for mutations in specific genes, and for gathering nucleotide sequence data from each mutated gene to provide a database of tagged gene sequences. Such a database provides a means to access the individual mutant cell clones contained in the Library. The invention includes the described Library, methods of making the same, and vectors used to construct the Library. Methods are also provided for accessing individual parts of the Library either by sequence or by pooling and screening. The invention also provides for the generation of non-human transgenic animals which are mutant for specific genes as isolated and generated from the cells of the Library.
摘要翻译：提供方法和载体（DNA和逆转录病毒）用于构建突变细胞库。该文库优选地在基因组中存在基因组中所有基因的突变。图书馆和载体的性质允许筛选特定基因突变的方法，并收集每个突变基因的核苷酸序列数据，以提供标记基因序列的数据库。这样的数据库提供了访问图书馆中包含的各个突变细胞克隆的方法。本发明包括描述的库，制作方法和用于构建库的向量。还提供了通过序列或汇总和筛选来访问图书馆的各个部分的方法。本发明还提供了从文库细胞分离和产生的特异性基因突变的非人转基因动物的产生。

17. 发明公开

US20230357182A1 SOLID FORMS OF (S)-1-((2',6-BIS(DIFLUOROMETHYL)-[2,4'-BIPYRIDIN]-5-YL)OXY)-2,4-DIMETHYLPENTAN-2-AMINE AND SALTS THEREOF 审中-公开
公开(公告)号：US20230357182A1
公开(公告)日：2023-11-09
申请号：US18114104
申请日：2023-02-24
申请人： Lexicon Pharmaceuticals, Inc.
发明人： Qun LI , Wenxue WU , Matthew Mangzhu ZHAO
IPC分类号： C07D401/04 , A61K31/444 , A61K9/28 , A61P29/00
CPC分类号： C07D401/04 , A61K31/444 , A61K9/28 , A61P29/00 , C07B2200/13
摘要： Salts of the AAK1 inhibitor (S)-1-((2′,6-bis(difluoromethyl)-[2,4′-bipyridin]-5-yl)oxy)-2,4-dimethylpentan-2-amine and solid forms thereof are disclosed, as are pharmaceutical formulations comprising them and methods of their preparation.

18. 发明申请

US20220235085A1 PROCESS FOR PREPARING THE CRYSTALLINE FORM II OF SOTAGLIFLOZIN 有权
公开(公告)号：US20220235085A1
公开(公告)日：2022-07-28
申请号：US17631209
申请日：2020-07-31
申请人： Lexicon Pharmaceuticals, Inc.
发明人： Bruno BUREL , Jérome CEZERAC , Stéphane DUTHEIL , Martial ETIENNE , Richard FLACHER , Antonio NOBREGA
IPC分类号： C07H13/08 , C07H1/06
摘要： The present document relates to a process for the preparation of the crystalline form II of sotagliflozin, wherein said crystalline form II of sotagliflozin is directly obtained from the following compound of formula (A) and by using toluene or xylene or mixture thereof as solvent medium for the crystallization.

19. 发明申请

US20220054464A1 COMPOUNDS AND METHODS FOR TREATING VIRAL INFECTIONS 有权
公开(公告)号：US20220054464A1
公开(公告)日：2022-02-24
申请号：US17233830
申请日：2021-04-19
申请人： Lexicon Pharmaceuticals, Inc.
发明人： Suma GOPINATHAN , Praveen TYLE , Qi Melissa YANG
IPC分类号： A61K31/444 , A61P31/14
摘要： Provided herein are methods of treating, managing and/or preventing viral infections. A particular method comprises administering to a subject in need thereof an effective amount of an adaptor associated kinase 1 inhibitor of Formula (I):

20. 发明授权

US10968192B2 Crystalline solid forms of N-(1-((2-(dimethylamino)ethyl)amino)-2-methyl-1-oxopropan-2-yl)-4-(4-(2-methyl-5-((2S,3R,4R,5S,6R)-3,4,5-trihydroxy-6-(methylthio)tetrahydro-2H-pyran-2-yl)benzyl)phenyl)butanamide and methods of their synthesis 有权
公开(公告)号：US10968192B2
公开(公告)日：2021-04-06
申请号：US16579106
申请日：2019-09-23
申请人： Lexicon Pharmaceuticals, Inc.
发明人： Mark Stephen Bednarz , Kuangchu Dai , Jeffrey Manning Eckert , Ngiap-Kie Lim , Lauren Sirois , Wenxue Wu , Matthew Mangzhu Zhao
IPC分类号： C07D309/10 , C07D207/16
摘要： Methods of preparing, and solid forms of N-(1-((2-(dimethylamino)ethyl)amino)-2-methyl-1-oxopropan-2-yl)-4-(4-(2-methyl-5-((2S,3R,4R,5S,6R)-3,4,5-trihydroxy-6-(methylthio)tetrahydro-2H-pyran-2-yl)benzyl)phenyl)butanamide, and salts, solvates and cocrystals thereof, are disclosed.

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