公开(公告)号：US20220017467A1

公开(公告)日：2022-01-20

申请号：US17487836

申请日：2021-09-28

申请人： Mayo Foundation for Medical Education and Research

发明人： Eugenia Trushina ,  Robert Greenhouse ,  Kevin Greenman ,  William Thomas

IPC分类号： C07D213/36 ,  C07D213/74 ,  C07D213/81 ,  C07D235/06 ,  C07D239/26 ,  C07C217/52 ,  C07D213/38 ,  C07D213/40 ,  A61K31/44 ,  A61K31/137 ,  C07D213/82

摘要： Compounds and compositions that can modulate mitochondrial function in neuronal cells are provided herein, as are methods for using the compounds and compositions to treat or prevent conditions such as Alzheimer's disease. For example, compounds of Formula I, compositions containing the compounds, and methods for using the compounds and compositions are provided herein: wherein X is absent, CH2, or C(O); R1 is H, OH, CN, NO2, halo, C1-3 alkyl, C1-3 haloalkyl, C1-3 alkoxy, C1-3 haloalkoxy, C3-7 cycloalkyl, amino, C1-3 alkylamino, or di(C1-3 alkyl)amino; R2 is H or C1-6 alkyl; R3 is H, C1-6 alkyl, —C(O)(C1-3 alkyl), or —C(O)O(C1-3 alkyl); R4 is C3-10 cycloalkyl, C6-10 aryl, 5-10 membered heteroaryl, or 5-10 membered heterocycloalkyl, each optionally substituted by 1, 2, 3, or 4 independently selected R5 groups; and R5 is OH, CN, NO2, halo, C1-3 alkyl, C1-3 haloalkyl, C1-3 alkoxy, C1-3 haloalkoxy, C3-7 cycloalkyl, amino, C1-3 alkylamino, or di(C1-3 alkyl)amino.

公开(公告)号：US10562878B2

公开(公告)日：2020-02-18

申请号：US15836261

申请日：2017-12-08

申请人： Sunovion Pharmaceuticals Inc.

发明人： Liming Shao ,  Fengjiang Wang ,  Scott Christopher Malcolm ,  Michael Charles Hewitt ,  Larry R. Bush ,  Jianguo Ma ,  Mark A. Varney ,  Una Campbell ,  Sharon Rae Engel ,  Larry Wendell Hardy ,  Patrick Koch ,  John E. Campell

IPC分类号： C07D333/20 ,  C07C211/17 ,  C07C211/40 ,  C07C215/42 ,  C07C215/44 ,  C07C217/52 ,  C07C217/74 ,  C07C323/32 ,  C07D207/06 ,  C07D207/08 ,  C07D211/14 ,  C07D265/14 ,  C07D277/28 ,  C07D295/06 ,  C07D307/52 ,  C07D317/58 ,  C07D317/72 ,  C07D319/06 ,  C07D491/056 ,  C07C211/29 ,  C07D211/16

摘要： The invention relates to novel cyclohexylamine derivatives and their use in the treatment and/or prevention of central nervous system (CNS) disorders, such as depression, anxiety, schizophrenia and sleep disorder as well as methods for their synthesis. The invention also relates to pharmaceutical compositions containing the compounds of the invention, as well as methods of inhibiting reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine from the synaptic cleft and methods of modulating one or more monoamine transporter.

公开(公告)号：US20190352263A1

公开(公告)日：2019-11-21

申请号：US16433254

申请日：2019-06-06

申请人： Mayo Foundation for Medical Education and Research

发明人： Eugenia Trushina ,  Robert Greenhouse ,  Kevin Greenman ,  William Thomas

IPC分类号： C07D213/36 ,  C07D213/82 ,  C07D213/38 ,  C07D213/81 ,  C07D213/40 ,  C07D213/74 ,  C07C217/52 ,  C07D239/26 ,  C07D235/06

摘要： Compounds and compositions that can modulate mitochondrial function in neuronal cells are provided herein, as are methods for using the compounds and compositions to treat or prevent conditions such as Alzheimer's disease. For example, compounds of Formula I, compositions containing the compounds, and methods for using the compounds and compositions are provided herein: wherein X is absent, CH2, or C(O); R1 is H, OH, CN, NO2, halo, C1-3 alkyl, C1-3 haloalkyl, C1-3 alkoxy, C1-3 haloalkoxy, C3-7 cycloalkyl, amino, C1-3 alkylamino, or di(C1-3 alkyl)amino; R2 is H or C1-6 alkyl; R3 is H, C1-6 alkyl, —C(O)(C1-3 alkyl), or —C(O)O(C1-3 alkyl); R4 is C3-10 cycloalkyl, C6-10 aryl, 5-10 membered heteroaryl, or 5-10 membered heterocycloalkyl, each optionally substituted by 1, 2, 3, or 4 independently selected R5 groups; and R5 is OH, CN, NO2, halo, C1-3 alkyl, C1-3 haloalkyl, C1-3 alkoxy, C1-3 haloalkoxy, C3-7 cycloalkyl, amino, C1-3 alkylamino, or di(C1-3 alkyl)amino.

公开(公告)号：US20190076450A1

公开(公告)日：2019-03-14

申请号：US16188444

申请日：2018-11-13

申请人： Bristol-Myers Squibb Company

发明人： Alaric J. Dyckman ,  T.G. Murali Dhar ,  Hai-Yun Xiao ,  John L. Gilmore ,  Michael G. Yang ,  Zili Xiao ,  David Marcoux

IPC分类号： A61K31/695 ,  C07F7/08 ,  A61K31/505 ,  A61K31/137 ,  A61K31/15 ,  A61K31/165 ,  A61K31/166 ,  A61K31/17 ,  A61K31/222 ,  A61K31/24 ,  A61K31/27 ,  A61K31/337 ,  A61K31/351 ,  A61K31/352 ,  A61K31/381 ,  A61K31/415 ,  A61K31/4174 ,  A61K31/426 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/47 ,  A61K31/4965 ,  A61K31/661 ,  C07F9/09 ,  C07F9/572 ,  C07F9/54 ,  C07C235/46 ,  C07C323/25 ,  C07C217/74 ,  C07C275/26 ,  C07D213/38 ,  C07D209/46 ,  C07C251/44 ,  C07C251/42 ,  C07C251/38 ,  C07C323/29 ,  C07D241/04 ,  C07D215/14 ,  A61K31/135 ,  C07D213/69 ,  C07D213/32 ,  C07C251/54 ,  C07C219/24 ,  C07C217/52 ,  C07D333/16 ,  C07D319/20 ,  C07D311/76 ,  C07D311/58 ,  C07D309/12 ,  C07D309/06 ,  C07D277/24 ,  C07D239/26 ,  C07D231/12 ,  C07D217/24 ,  C07C317/28 ,  C07C271/34 ,  C07C251/52 ,  C07C233/41 ,  C07C217/58 ,  C07C215/42 ,  C07F9/655 ,  C07F9/62 ,  C07D305/08 ,  C07D241/12 ,  C07D231/20 ,  C07D215/12 ,  C07D213/70

摘要： Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V): and/or a salt thereof, wherein R1 is —OH or —OP(O)(OH)2, and X1, X2, X3, R2, R2a, Ra, Rb, and Rc are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.

公开(公告)号：US10166249B2

公开(公告)日：2019-01-01

申请号：US15648250

申请日：2017-07-12

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： Alaric J. Dyckman ,  T. G. Murali Dhar ,  Hai-Yun Xiao ,  John L. Gilmore ,  Michael G. Yang ,  Zili Xiao ,  David Marcoux

IPC分类号： A61K31/695 ,  C07C215/42 ,  C07C217/52 ,  C07C217/58 ,  C07C219/24 ,  C07C233/41 ,  C07C251/52 ,  C07C251/54 ,  C07C271/34 ,  C07C317/28 ,  C07D213/32 ,  C07D213/69 ,  C07D213/70 ,  C07D215/12 ,  C07D217/24 ,  C07D231/12 ,  C07D231/20 ,  C07D239/26 ,  C07D241/12 ,  C07D277/24 ,  C07D305/08 ,  C07D309/06 ,  C07D309/12 ,  C07D311/58 ,  C07D311/76 ,  C07D319/20 ,  C07D333/16 ,  C07F7/08 ,  C07F9/62 ,  C07F9/655 ,  A61K31/135 ,  C07D215/14 ,  C07D241/04 ,  C07C323/29 ,  C07C251/38 ,  C07C251/42 ,  C07C251/44 ,  C07D209/46 ,  C07D213/38 ,  C07C275/26 ,  C07C217/74 ,  C07C323/25 ,  C07C235/46 ,  C07F9/54 ,  C07F9/572 ,  C07F9/09 ,  A61K31/137 ,  A61K31/15 ,  A61K31/165 ,  A61K31/166 ,  A61K31/17 ,  A61K31/222 ,  A61K31/24 ,  A61K31/27 ,  A61K31/337 ,  A61K31/351 ,  A61K31/352 ,  A61K31/381 ,  A61K31/415 ,  A61K31/4174 ,  A61K31/426 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/47 ,  A61K31/4965 ,  A61K31/505 ,  A61K31/661

摘要： Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V): and/or a salt thereof, wherein R1 is —OH or —OP(O)(OH)2, and X1, X2, X3, R2, R2a, Ra, Rb, and Rc are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.

公开(公告)号：US09693975B2

公开(公告)日：2017-07-04

申请号：US15239446

申请日：2016-08-17

申请人： KALYRA PHARMACEUTICALS, INC.

发明人： Kevin Duane Bunker

IPC分类号： C07C217/52 ,  C07C235/74 ,  C07C233/06 ,  C07C233/23 ,  C07C211/62 ,  C07C233/41 ,  C07C233/52 ,  C07C233/63 ,  A61K31/16 ,  A61K45/06 ,  A61K31/13 ,  A61K31/14 ,  A61K31/215 ,  A61K31/216 ,  A61K31/235 ,  A61K9/00 ,  A61K31/133 ,  A61K31/22 ,  A61K31/221 ,  A61K31/24

CPC分类号： A61K31/16 ,  A61K9/0014 ,  A61K9/0019 ,  A61K31/13 ,  A61K31/133 ,  A61K31/14 ,  A61K31/215 ,  A61K31/216 ,  A61K31/22 ,  A61K31/221 ,  A61K31/235 ,  A61K31/24 ,  A61K45/06 ,  C07C211/62 ,  C07C217/52 ,  C07C233/06 ,  C07C233/23 ,  C07C233/41 ,  C07C233/52 ,  C07C233/63 ,  C07C235/74 ,  C07C2602/38

摘要： Analgesic compounds for treatment of pain or fever, comprising a bicyclopentane moiety linked to an amine, combinations of the compounds with opioid analgesic drugs, and methods for treating pain or fever by administering the compounds.

公开(公告)号：US09073819B2

公开(公告)日：2015-07-07

申请号：US14128310

申请日：2012-06-29

申请人： Jahanshah Amin ,  Kirpal S. Bisht ,  Meghanath Gali

发明人： Jahanshah Amin ,  Kirpal S. Bisht ,  Meghanath Gali

IPC分类号： A61K31/357 ,  C07C215/44 ,  C07D317/72 ,  C07C211/40 ,  C07C217/52 ,  C07C325/02 ,  C07C251/20 ,  C07C251/44 ,  C07C323/30

CPC分类号： C07C215/44 ,  C07C211/40 ,  C07C217/52 ,  C07C251/20 ,  C07C251/44 ,  C07C323/30 ,  C07C325/02 ,  C07C2601/14 ,  C07D317/72

摘要： Embodiments of the present disclosure provide compositions including ketamine analogs, salts, and disalts, pharmaceutical compositions including ketamine analogs, salts, or disalts, methods of treatment of a condition or disease, methods of treatment using compositions or pharmaceutical compositions, and the like.

摘要翻译： 本公开的实施方案提供了包含氯胺酮类似物，盐和糖的组合物，包括氯胺酮类似物，盐或糖的药物组合物，治疗病症或疾病的方法，使用组合物或药物组合物的治疗方法等。

公开(公告)号：US20140121380A1

公开(公告)日：2014-05-01

申请号：US14128131

申请日：2012-06-21

申请人： Qingguo Meng ,  Mina Yang ,  Tao Wang ,  Qilin Wang ,  Jun Li ,  Zheng Ruan

发明人： Qingguo Meng ,  Mina Yang ,  Tao Wang ,  Qilin Wang ,  Jun Li ,  Zheng Ruan

IPC分类号： C07D333/20 ,  C07C217/52 ,  C07D213/36 ,  C07C215/46

CPC分类号： C07D333/20 ,  C07C213/00 ,  C07C213/08 ,  C07C215/46 ,  C07C217/52 ,  C07C2602/10 ,  C07D213/36 ,  C07C215/64 ,  C07C217/12 ,  C07C217/08

摘要： A method for industrially preparing a nitrogen substituted 6-amino-5,6,7,8-tetrahydronaphthol is disclosed. The method comprises includes reacting a nitrogen substituted amino-5,6,7,8-tetrahydronaphthol compound of formula (II) with a 2-substituted ethyl sulfonate compound of formula (III) under an alkaline condition and in the presence of a sulfite.

摘要翻译： 公开了一种工业上制备氮取代的6-氨基-5,6,7,8-四氢萘酚的方法。 该方法包括在碱性条件下和在亚硫酸盐存在下使式（II）的氮取代的氨基-5,6,7,8-四氢萘酚化合物与式（III）的2-取代的乙基磺酸酯化合物反应。

公开(公告)号：US20130317114A1

公开(公告)日：2013-11-28

申请号：US13992587

申请日：2011-12-09

申请人： Jennifer Riggs-Sauthier ,  Bo-Liang Deng ,  Hema Gursahani

发明人： Jennifer Riggs-Sauthier ,  Bo-Liang Deng ,  Hema Gursahani

IPC分类号： C07C217/52

CPC分类号： C07C217/52

摘要： The invention provides small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the characteristics of the small molecule drug not attached to the water-soluble oligomer.

摘要翻译： 本发明提供通过共价连接水溶性低聚物进行化学修饰的小分子药物。 本发明化合物当通过多种施用途径中的任一种施用时，显示出与未附着于水溶性低聚物的小分子药物的特性不同的特征。

公开(公告)号：US06909017B2

公开(公告)日：2005-06-21

申请号：US10638703

申请日：2003-08-11

申请人： Wolfgang Hell

发明人： Wolfgang Hell

IPC分类号： C07D275/06 ,  C07B55/00 ,  C07C213/10 ,  C07C217/52 ,  C07C217/74

CPC分类号： C07C213/10 ,  C07B2200/07 ,  C07C217/74

摘要： The invention relates to a method for isolating and purifying (1RS,2RS)-2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)-cyclohexanol as a saccharinate from a mixture of the diastereomers (1SR,2)RS-2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)-cyclohexanol and (1SR-2RS)-2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)-cyclohexanol and optionally impurities.

摘要翻译： 本发明涉及从非对映异构体（1SR，2）的混合物中分离纯化（1RS，2RS）-2 - [（二甲基氨基）甲基] -1-（3-甲氧基苯基） - 环己醇作为糖精的方法， 2 - [（二甲基氨基）甲基] -1-（3-甲氧基苯基） - 环己醇和（1SR-2RS）-2 - [（二甲基氨基）甲基] -1-（3-甲氧基苯基） - 环己醇和任选的杂质。