公开(公告)号：US10017458B2

公开(公告)日：2018-07-10

申请号：US14665928

申请日：2015-03-23

申请人： University of Florida Research Foundation, Inc.

发明人： Raymond G. Booth

IPC分类号： C07C211/42 ,  A61K31/13 ,  C07C217/74

CPC分类号： C07C211/42 ,  A61K31/13 ,  C07C217/74 ,  C07C2601/14 ,  C07C2602/10

摘要： The invention relates to protein binding interacting/binding compounds and methods of identifying and using them. The invention further relates to pharmaceutical compositions and methods for treating 5-HT2C and/or RSK disorders, including diseases and disorders mediated by CPCRs and/or RSKs.

公开(公告)号：US09944589B2

公开(公告)日：2018-04-17

申请号：US14650292

申请日：2013-12-03

申请人： Istituto Europeo de Oncologia S.r.L.

发明人： Mario Varasi ,  Paola Vianello ,  Florian Thaler ,  Paolo Trifiro′ ,  Ciro Mercurio ,  Giuseppe Meroni

IPC分类号： C07C211/40 ,  A61K31/4025 ,  A61K31/404 ,  A61K31/4164 ,  A61K31/496 ,  C07D215/12 ,  C07D295/195 ,  C07D207/50 ,  C07D213/61 ,  C07D311/70 ,  C07D211/58 ,  C07D263/04 ,  C07D233/02 ,  C07D271/113 ,  C07C209/00 ,  C07C231/12 ,  C07C269/06 ,  C07C303/36 ,  C07D319/16 ,  C07D233/32 ,  C07D239/42 ,  C07D249/06 ,  C07D263/22 ,  C07D271/10 ,  C07D295/155 ,  C07D213/64 ,  C07D307/54 ,  C07C271/28 ,  C07C211/49 ,  C07C215/42 ,  C07C217/58 ,  C07C217/74 ,  C07C233/44 ,  C07C233/80 ,  C07C237/06 ,  C07C247/16 ,  C07C311/21

CPC分类号： C07C211/40 ,  A61K31/4025 ,  A61K31/404 ,  A61K31/4164 ,  A61K31/496 ,  C07C209/00 ,  C07C211/49 ,  C07C215/42 ,  C07C217/58 ,  C07C217/74 ,  C07C231/12 ,  C07C233/44 ,  C07C233/80 ,  C07C237/06 ,  C07C247/16 ,  C07C269/06 ,  C07C271/28 ,  C07C303/36 ,  C07C311/21 ,  C07C2601/02 ,  C07D207/50 ,  C07D211/58 ,  C07D213/61 ,  C07D213/64 ,  C07D215/12 ,  C07D233/02 ,  C07D233/32 ,  C07D239/42 ,  C07D249/06 ,  C07D263/04 ,  C07D263/22 ,  C07D271/10 ,  C07D271/113 ,  C07D295/155 ,  C07D295/195 ,  C07D307/54 ,  C07D311/70 ,  C07D319/16 ,  A61K2300/00

摘要： The present invention relates to cyclopropyl derivatives of general formula (I), wherein A, R1, and R2 are as defined in the specification. The present application also relates to pharmaceutical compositions containing such compounds and to their use in therapy.

公开(公告)号：US20180085327A1

公开(公告)日：2018-03-29

申请号：US15597516

申请日：2017-05-17

申请人： Auspex Pharmaceuticals, Inc.

发明人： Thomas G. Gant ,  Sepshr Sarshar

IPC分类号： A61K31/137 ,  C07C255/37 ,  C07C235/34 ,  C07C217/74 ,  A61K45/06 ,  C07C65/21 ,  C07B59/00

CPC分类号： A61K31/137 ,  A61K45/06 ,  C07B59/001 ,  C07B2200/05 ,  C07C65/21 ,  C07C217/74 ,  C07C235/34 ,  C07C255/37 ,  C07C2601/14

摘要： Chemical syntheses and medical uses of novel inhibitors of the uptake of monoamine neurotransmitters and pharmaceutically acceptable salts and prodrugs thereof, for the treatment and/or management of psychotropic disorders, anxiety disorder, generalized anxiety disorder, depression, post-traumatic stress disorder, obsessive-compulsive disorder, panic disorder, hot flashes, senile dementia, migraine, hepatopulmonary syndrome, chronic pain, nociceptive pain, neuropathic pain, painful diabetic retinopathy, bipolar depression, obstructive sleep apnea, psychiatric disorders, premenstrual dysphoric disorder, social phobia, social anxiety disorder, urinary incontinence, anorexia, bulimia nervosa, obesity, ischemia, head injury, calcium overload in brain cells, drug dependence, and/or premature ejaculation are described.

公开(公告)号：US09868718B2

公开(公告)日：2018-01-16

申请号：US14502532

申请日：2014-09-30

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. Campbell

IPC分类号： C07C13/28 ,  C07D333/20 ,  C07C211/17 ,  C07C211/29 ,  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 ,  C07D211/16

CPC分类号： C07D333/20 ,  C07C211/17 ,  C07C211/29 ,  C07C211/40 ,  C07C215/42 ,  C07C215/44 ,  C07C217/52 ,  C07C217/74 ,  C07C323/32 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/10 ,  C07C2601/14 ,  C07C2601/16 ,  C07C2602/08 ,  C07D207/06 ,  C07D207/08 ,  C07D211/14 ,  C07D211/16 ,  C07D265/14 ,  C07D277/28 ,  C07D295/06 ,  C07D307/52 ,  C07D317/58 ,  C07D317/72 ,  C07D319/06 ,  C07D491/056

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：US20180009735A1

公开(公告)日：2018-01-11

申请号：US15658219

申请日：2017-07-24

申请人： GENENTECH, INC. ,  CONSTELLATION PHARMACEUTICALS, INC.

发明人： Brian K. Albrecht ,  James Edmund Audia ,  Alexandre Cote ,  Martin Duplessis ,  Victor S. Gehling ,  Andrew Charles Good ,  Jean-Christophe Harmange ,  Yves LeBlanc ,  Christopher G. Nasveschuk ,  Alexander M. Taylor ,  Rishi G. Vaswani

IPC分类号： C07C211/42 ,  C07D401/12 ,  A61K31/135 ,  A61K31/166 ,  C07D309/04 ,  C07D305/08 ,  C07D295/185 ,  C07D231/12 ,  C07D215/08 ,  C07D213/38 ,  C07D211/46 ,  C07D211/26 ,  C07D207/06 ,  C07D205/12 ,  C07D205/04 ,  C07C317/36 ,  C07C255/58 ,  C07C237/48 ,  C07C229/50 ,  C07C217/74 ,  A61K45/06 ,  A61K31/517 ,  A61K31/495 ,  A61K31/4747 ,  A61K31/4545 ,  A61K31/445 ,  A61K31/4406 ,  A61K31/437 ,  A61K31/4155 ,  A61K31/415 ,  A61K31/40 ,  A61K31/397 ,  A61K31/351 ,  A61K31/337 ,  A61K31/277 ,  A61K31/196 ,  C07D405/12

CPC分类号： C07C211/42 ,  A61K31/135 ,  A61K31/166 ,  A61K31/196 ,  A61K31/277 ,  A61K31/337 ,  A61K31/351 ,  A61K31/397 ,  A61K31/40 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/437 ,  A61K31/4406 ,  A61K31/445 ,  A61K31/4545 ,  A61K31/4747 ,  A61K31/495 ,  A61K31/517 ,  A61K45/06 ,  C07C217/74 ,  C07C229/50 ,  C07C237/48 ,  C07C255/58 ,  C07C317/36 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2603/94 ,  C07D205/04 ,  C07D205/12 ,  C07D207/06 ,  C07D211/26 ,  C07D211/46 ,  C07D211/78 ,  C07D213/38 ,  C07D215/08 ,  C07D231/12 ,  C07D295/185 ,  C07D305/08 ,  C07D309/04 ,  C07D401/12 ,  C07D405/12

摘要： Provided herein are compounds of formula I: and salts thereof and compositions and uses thereof. The compounds are useful as inhibitors of LSD1. Also included are pharmaceutical compositions comprising a compound of formula I or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various LSD1-mediated disorders.

公开(公告)号：US09730875B2

公开(公告)日：2017-08-15

申请号：US15012227

申请日：2016-02-01

申请人： Henkel AG & Co. KGaA

发明人： Thomas Gerke ,  Christian Kropf ,  Ursula Huchel ,  Axel Griesbeck ,  Agnieszka Landes

IPC分类号： C07C217/74 ,  C07D207/06 ,  A61K8/49 ,  C07C217/22 ,  C11D3/50 ,  A61K8/41 ,  A61Q13/00 ,  A61L9/015

CPC分类号： A61K8/4913 ,  A61K8/416 ,  A61L9/015 ,  A61Q13/00 ,  C07C217/22 ,  C07C217/74 ,  C07D207/06 ,  C11D3/50 ,  C11D3/507

摘要： Fragrances that provide a scent of freshness tend to be volatile and are therefore not very economical when used in typical applications such as washing or cleaning processes, so they have to be used in relatively large quantities to be able to produce adequate effects. The disclosed photolabile pro-fragrances provide a much longer-lasting sense of fragrance, in particular with a scent of freshness, when used in typical applications, thus allowing said fragrances to be used economically.

公开(公告)号：US20160368857A1

公开(公告)日：2016-12-22

申请号：US15254020

申请日：2016-09-01

申请人： Oryzon Genomics S.A.

发明人： Alberto ORTEGA MUÑOZ ,  Matthew Colin Thor FYFE ,  Marc MARTINELL PEDEMONTE ,  Maria de los Àngeles ESTIARTE MARTINEZ ,  Nuria VALLS VIDAL ,  Guido KURZ ,  Julio Cesar CASTRO PALOMINO LARIA

IPC分类号： C07C211/36 ,  C07D277/28 ,  C07D213/38 ,  C07C217/74 ,  C07C213/00 ,  C07D207/14 ,  C07C211/38 ,  C07C271/24 ,  C07C269/00 ,  C07C275/26 ,  C07C273/00 ,  C07D295/135 ,  C07C215/64 ,  C07D231/56 ,  C07D231/12 ,  C07D333/20 ,  C07D213/57 ,  C07D213/73 ,  C07D295/26 ,  C07D295/096 ,  C07D213/30 ,  C07D213/74 ,  C07C209/28

CPC分类号： C07C211/36 ,  C07B2200/07 ,  C07C209/28 ,  C07C211/37 ,  C07C211/38 ,  C07C211/40 ,  C07C213/00 ,  C07C215/46 ,  C07C215/64 ,  C07C217/54 ,  C07C217/74 ,  C07C269/00 ,  C07C271/24 ,  C07C273/00 ,  C07C273/18 ,  C07C275/26 ,  C07C311/08 ,  C07C311/21 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/14 ,  C07C2602/08 ,  C07D207/14 ,  C07D213/30 ,  C07D213/38 ,  C07D213/57 ,  C07D213/73 ,  C07D213/74 ,  C07D231/12 ,  C07D231/56 ,  C07D277/28 ,  C07D295/096 ,  C07D295/135 ,  C07D295/26 ,  C07D307/52 ,  C07D333/20

摘要： The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.

公开(公告)号：US09506095B2

公开(公告)日：2016-11-29

申请号：US13759382

申请日：2013-02-05

申请人： LES LABORATOIRES SERVIER

发明人： Sandrine Pedragosa-Moreau ,  François Lefoulon

IPC分类号： C12P41/00 ,  C12P17/10 ,  C12P7/40 ,  C12P7/62 ,  C12P13/00 ,  C07C67/08 ,  C07C51/08 ,  C07C213/02 ,  C07C231/02 ,  C07D223/16

CPC分类号： C12P17/10 ,  C07B2200/07 ,  C07C51/08 ,  C07C67/08 ,  C07C213/02 ,  C07C231/02 ,  C07C2602/06 ,  C07D223/16 ,  C12P7/40 ,  C12P7/62 ,  C12P13/001 ,  C12P41/005 ,  C12Y301/01 ,  Y02P20/52 ,  C07C62/34 ,  C07C69/757 ,  C07C217/74 ,  C07C235/40

摘要： Process for the enzymatic synthesis of the compound of formula (I): wherein R1 represents a hydrogen atom or an alkyl group. Application in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid.

摘要翻译： 在合成伊伐布拉德及其加成盐与药学上可接受的酸时的应用。

公开(公告)号：US20160297745A1

公开(公告)日：2016-10-13

申请号：US14895656

申请日：2015-09-23

申请人： APOTEX INC.

发明人： Ghassan YARED ,  Gustavo DE-DEUS

IPC分类号： C07C213/02 ,  C07C213/08 ,  C07C217/74

CPC分类号： C07D333/20 ,  C07C213/02 ,  C07C213/04 ,  C07C213/08 ,  C07C217/74

摘要： The present invention provides processes for the preparation of a compound of Formula 2 or a salt thereof, wherein R1 is selected from the group consisting of H, C1-C3 alkyl, and C(0)R3; R3 is selected from the group consisting of C1-C6 alkyl, C6-C10aryl and C7-C20 arylalkyl; the carbon atom marked with “*” is racemic, enantiomerically enriched in the (R)-configuration, or enantiomerically enriched in the (S)-configuration. Also provided are intermediate compounds of the processes.

公开(公告)号：US09422225B2

公开(公告)日：2016-08-23

申请号：US12234236

申请日：2008-09-19

申请人： Thomas G. Gant ,  Sepehr Sarshar

发明人： Thomas G. Gant ,  Sepehr Sarshar

IPC分类号： C07C211/00 ,  C07C65/21 ,  C07C217/74 ,  C07C235/34 ,  C07C255/37

CPC分类号： A61K31/137 ,  A61K45/06 ,  C07B59/001 ,  C07B2200/05 ,  C07C65/21 ,  C07C217/74 ,  C07C235/34 ,  C07C255/37 ,  C07C2601/14

摘要： Chemical syntheses and medical uses of novel inhibitors of the uptake of monoamine neurotransmitters and pharmaceutically acceptable salts and prodrugs thereof, for the treatment and/or management of psychotropic disorders, anxiety disorder, generalized anxiety disorder, depression, post-traumatic stress disorder, obsessive-compulsive disorder, panic disorder, hot flashes, senile dementia, migraine, hepatopulmonary syndrome, chronic pain, nociceptive pain, neuropathic pain, painful diabetic retinopathy, bipolar depression, obstructive sleep apnea, psychiatric disorders, premenstrual dysphoric disorder, social phobia, social anxiety disorder, urinary incontinence, anorexia, bulimia nervosa, obesity, ischemia, head injury, calcium overload in brain cells, drug dependence, and/or premature ejaculation are described.

摘要翻译： 用于治疗和/或治疗精神病症，焦虑障碍，广泛性焦虑症，抑郁症，创伤后应激障碍，强迫症的单胺神经递质及其药学上可接受的盐和前药的新型抑制剂的化学合成和医学用途， 强迫症，恐慌症，热潮红，老年痴呆，偏头痛，肝肺综合征，慢性疼痛，伤害性疼痛，神经性疼痛，疼痛性糖尿病性视网膜病变，双相抑郁症，阻塞性睡眠呼吸暂停，精神疾病，经前焦虑症，社交恐惧症，社交焦虑症 ，尿失禁，厌食症，神经性贪食症，肥胖症，局部缺血，头部损伤，脑细胞中的钙超载，药物依赖性和/或早泄。