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公开(公告)号:US20190241508A1
公开(公告)日:2019-08-08
申请号:US16344092
申请日:2017-10-19
发明人: Jin-Quan Yu
IPC分类号: C07C269/04 , C07D319/18 , C07D213/61 , C07D213/64 , C07D213/40 , C07D215/12 , C07D241/42 , C07D333/22 , C07C209/68 , C07D471/04 , B01J31/22
CPC分类号: C07C269/04 , B01J31/2239 , B01J2231/44 , B01J2531/824 , C07B37/04 , C07C209/68 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07D213/40 , C07D213/61 , C07D213/64 , C07D215/12 , C07D241/42 , C07D319/18 , C07D333/22 , C07D471/04 , C07C211/40 , C07C271/22
摘要: Pd(II)-catalyzed g-G(sp3)-H arylation or heteroarylation of primary amines is realized by using 2-hydroxynicotinaldehyde as a catalytic transient directing group. Importantly, the catalyst and the directing group loading can be lowered to 2% and 4% respectively, thus demonstrating high efficiency of this newly designed transient directing group. Heterocyclic aryl iodides are also compatible with this reaction. Furthermore, swift synthesis of 1,2,3,4-tetrahydronaphthyridine derivatives is accomplished using this reaction.
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公开(公告)号:US20190194135A1
公开(公告)日:2019-06-27
申请号:US16098946
申请日:2017-05-05
发明人: Carmela Sidrauski , Marina Pliushchev , Jennifer M. Frost , Lawrence A. Black , Xiangdong Xu , Ramzi Farah Sweis , Lei Shi , Qingwei I. Zhang , Yunsong Tong , Charles W. Hutchins , Seungwon Chung , Michael J. Dart
IPC分类号: C07D213/42 , C07D261/08 , C07D231/12 , C07D241/12 , C07D213/89 , C07D271/10 , C07D307/36 , C07D277/28 , C07D471/04 , C07D333/20 , C07D209/14 , A61K31/44 , A61K31/42 , A61K31/415 , A61K31/4965 , A61K31/4245 , A61K31/341 , A61K31/426 , A61K31/4439 , A61K31/381 , A61K31/4045 , C07D263/32 , A61K31/421 , C07D235/00 , A61K31/417 , C07D239/34 , A61K31/505 , C07D237/08 , A61K31/50 , C07C235/22 , A61K31/197 , C07C311/16 , A61K31/18 , C07C323/09
CPC分类号: C07D213/42 , A61K31/18 , A61K31/197 , A61K31/341 , A61K31/381 , A61K31/4045 , A61K31/415 , A61K31/417 , A61K31/42 , A61K31/421 , A61K31/4245 , A61K31/426 , A61K31/44 , A61K31/4439 , A61K31/4965 , A61K31/50 , A61K31/505 , C07C235/22 , C07C311/16 , C07C323/09 , C07C2602/38 , C07C2602/40 , C07C2602/42 , C07C2602/44 , C07C2603/90 , C07D209/14 , C07D213/40 , C07D213/64 , C07D213/89 , C07D231/12 , C07D235/00 , C07D237/08 , C07D239/34 , C07D241/12 , C07D261/08 , C07D263/32 , C07D271/07 , C07D271/10 , C07D277/28 , C07D307/36 , C07D307/52 , C07D333/20 , C07D471/04
摘要: Provided herein are compounds, compositions, and methods useful for modulating the integrated stress response (ISR) and for treating related diseases; disorders and conditions.
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公开(公告)号:US20180273477A1
公开(公告)日:2018-09-27
申请号:US15935558
申请日:2018-03-26
发明人: Christian Manfred FRECH , Pasquale Gabriele GRIECO , Christine AEBERSOLD , Patrick MÜLLER , Jan-Erik INGENHOFF , Miriam OBERHOLZER , Viktorya RSTAKYAN , Roman Gerber AESCHBACHER
IPC分类号: C07D213/40
CPC分类号: C07D213/40 , C07D213/56
摘要: The present invention relates to a new route of synthesis to obtain pharmaceutically acceptable Vismodegib. In addition, besides the synthesis also suitable pharmaceutical compositions and the use of the compound for the treatment of basal-cell carcinomas are disclosed.
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公开(公告)号:US10047066B2
公开(公告)日:2018-08-14
申请号:US12744860
申请日:2008-12-01
IPC分类号: A61K31/5375 , A61K31/135 , A61K31/404 , A61K31/381 , A61K31/505 , C07D209/14 , C07D405/12 , C07D333/56 , A61K31/138 , A61K31/506 , C07C259/06 , C07C311/48 , C07C327/44 , C07C327/48 , C07C333/20 , C07D209/18 , C07D213/40 , C07D215/26 , C07D253/07 , C07D261/20 , C07D263/22 , C07D277/36 , C07D279/06 , C07D307/81 , C07D333/58 , C07D333/60 , C07D335/06 , C07D401/06 , C07D409/12 , C07D417/06 , C07D417/12 , C07D277/64 , C07D307/80 , A61P37/00 , A61K31/4045 , C07D403/12 , C07D401/12 , A61K31/4709 , C07D413/12 , A61K31/423 , C07C333/04 , A61K31/27 , C07D213/53 , A61K31/4406 , A61K31/4402 , A61K31/36 , A61K31/47 , A61K31/357 , A61K31/428
CPC分类号: C07D333/56 , A61K31/138 , A61K31/506 , C07C259/06 , C07C311/48 , C07C327/44 , C07C327/48 , C07C333/20 , C07D209/14 , C07D209/18 , C07D213/40 , C07D215/26 , C07D253/07 , C07D261/20 , C07D263/22 , C07D277/36 , C07D277/64 , C07D279/06 , C07D307/80 , C07D307/81 , C07D333/58 , C07D333/60 , C07D335/06 , C07D401/06 , C07D405/12 , C07D409/12 , C07D417/06 , C07D417/12 , Y02A50/409 , Y02A50/465
摘要: Presently provided are methods for (a) modulating an activity of indoleamine 2,3-dioxygenase comprising contacting an indoleamine 2,3-dioxygenase with a modulation effective amount of a compound as described in one of the aspects described herein; (b) treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression in a subject in need thereof, comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; (c) treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; (d) enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent and a compound as described in one of the aspects described herein; (e) treating tumor-specific immunosuppression associated with cancer comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; and (f) treating immunosuppression associated with an infectious disease, e.g., HIV-I infection, comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount a compound as described in one of the aspects described herein.
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公开(公告)号:US20180208568A1
公开(公告)日:2018-07-26
申请号:US15925517
申请日:2018-03-19
发明人: Justin S. CISAR , Cheryl A. GRICE , Todd K. JONES , Micah J. NIPHAKIS , Jae Won CHANG , Kenneth M. LUM , Benjamin F. CRAVATT
IPC分类号: C07D295/205 , C07D491/107 , C07C271/10 , C07D471/10 , C07D471/04 , C07D413/10 , C07D413/06 , C07D407/06 , C07D405/14 , C07D403/10 , C07D401/10 , C07D401/04 , C07D317/58 , C07D317/46 , C07D307/79 , C07D295/26 , C07D271/06 , C07D263/32 , C07D261/08 , C07D241/04 , C07D231/56 , C07D231/16 , C07D231/12 , C07D215/46 , C07D215/42 , C07D213/55 , C07D213/40 , C07D213/38 , C07D207/14 , C07D207/09 , C07D205/04 , C07C271/12 , C07D487/04
CPC分类号: C07D295/205 , C07C271/10 , C07C271/12 , C07D205/04 , C07D207/09 , C07D207/14 , C07D213/38 , C07D213/40 , C07D213/55 , C07D215/42 , C07D215/46 , C07D231/12 , C07D231/16 , C07D231/56 , C07D241/04 , C07D261/08 , C07D263/32 , C07D271/06 , C07D295/26 , C07D307/79 , C07D317/46 , C07D317/58 , C07D401/04 , C07D401/10 , C07D403/10 , C07D405/14 , C07D407/06 , C07D413/06 , C07D413/10 , C07D471/04 , C07D471/10 , C07D487/04 , C07D491/107
摘要: This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compounds as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from indications such as pain, solid tumor cancer and/or obesity comprising administering a disclosed compound or composition.
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公开(公告)号:US10000464B2
公开(公告)日:2018-06-19
申请号:US15336143
申请日:2016-10-27
申请人: PAION UK LIMITED
IPC分类号: C07D213/55 , C07D401/04 , C07D213/40 , C07D487/04 , C07F9/6558 , C07D213/50
CPC分类号: C07D401/04 , C07D213/40 , C07D213/50 , C07D487/04 , C07F9/65586
摘要: The invention concerns a new process for preparing 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4H-imidazo[1,2-a][1,4]benzodiazepine-4-yl]-propionic acid methyl ester or 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4H-imidazo[1,2-a][1,4]benzodiazepine-4-yl]propionic acid methyl ester benzene sulfonate (P) which comprises reacting 3-[(S)-7-bromo-2-((R and/or S)-2-hydroxy-propylamino)-5-pyridin-2-yl-3H-benzo[e][1,4]diazepin-3-yl]-propionic acid methyl ester of formula (EM) with an oxidizing agent and optionally treating the reaction product under acidic conditions, such as to produce the compound of formula (F) or the compound (P), and new compounds useful as starting materials or as intermediates for performing that process.
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公开(公告)号:US20180127368A1
公开(公告)日:2018-05-10
申请号:US15806554
申请日:2017-11-08
发明人: David Marcoux , Myra Beaudoin Bertrand , T.G. Murali Dhar , Michael G. Yang , Zili Xiao , Hai-Yun Xiao , Yeheng Zhu , Carolyn A. Weigelt , Douglas G Batt
IPC分类号: C07D211/48 , C07D213/40 , C07D295/195 , C07D213/75 , C07D333/48 , C07C317/44 , C07D335/02 , C07D471/04 , C07D307/22 , C07D241/08 , C07D207/10 , C07D207/16 , C07D231/08 , C07D309/10 , C07D211/96 , C07D471/10 , C07D205/04 , C07D207/277 , C07D257/04 , C07D205/08 , A61P37/00
CPC分类号: C07D211/48 , A61P37/00 , C07B2200/05 , C07B2200/07 , C07C317/20 , C07C317/24 , C07C317/30 , C07C317/44 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/38 , C07C2602/44 , C07C2602/50 , C07C2603/08 , C07C2603/12 , C07C2603/16 , C07C2603/90 , C07D205/04 , C07D205/08 , C07D207/09 , C07D207/10 , C07D207/16 , C07D207/277 , C07D207/28 , C07D211/62 , C07D211/78 , C07D211/96 , C07D213/40 , C07D213/56 , C07D213/75 , C07D213/81 , C07D215/36 , C07D231/06 , C07D231/08 , C07D231/18 , C07D233/64 , C07D233/76 , C07D233/78 , C07D233/90 , C07D241/08 , C07D249/12 , C07D257/04 , C07D261/18 , C07D263/20 , C07D285/06 , C07D295/16 , C07D295/195 , C07D305/08 , C07D307/22 , C07D309/10 , C07D333/48 , C07D335/02 , C07D401/04 , C07D401/12 , C07D405/04 , C07D405/12 , C07D471/04 , C07D471/10 , C07F9/091
摘要: There are described RORγ modulators of the formula (I), or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders.
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公开(公告)号:US09964531B2
公开(公告)日:2018-05-08
申请号:US14760696
申请日:2014-01-21
申请人: University of Oregon
IPC分类号: C07D213/61 , C07D213/73 , C07D213/74 , G01N33/18 , C07D213/36 , C07D213/56 , C07D207/335 , C07D213/40 , C07D213/68 , G01N31/22
CPC分类号: G01N33/182 , C07D207/335 , C07D213/36 , C07D213/40 , C07D213/56 , C07D213/68 , C07D213/74 , G01N31/22 , Y10T436/193333
摘要: Disclosed herein are host or receptor compounds that bind targets of interest. In one embodiment the compounds bind ions, such as metal ions.A compound, or a protonate or salt thereof, having the formula of: Formula IIa wherein R6 is an aminoalkoxy, alkylamino, nitro or —NH2; n is 1 or 2; each R2 is independently selected from an optionally substituted alkyl, halogen, optionally substituted alkoxy, optionally substituted carboxyl, or amide; a is 0 to 4.
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公开(公告)号:US09957261B2
公开(公告)日:2018-05-01
申请号:US15416472
申请日:2017-01-26
发明人: Giuseppe Cecere , Guido Galley , Annick Goergler , Roger Norcross , Philippe Pflieger , Alina Tirla , Philipp Schmid
IPC分类号: C07D417/12 , C07D231/14 , C07D239/28 , C07D405/12 , C07C233/80 , C07C231/12 , C07C275/40 , C07C273/18 , C07D239/42 , C07D213/40 , C07C209/78 , C07C311/21 , C07D409/14 , C07D213/81 , C07D213/73 , C07D213/82 , C07D311/58 , C07D231/20 , C07D405/04 , C07D241/20 , C07D261/18 , C07D213/61 , C07C255/58 , C07C211/60 , C07C255/60 , C07C275/42 , C07C217/92 , C07C237/48 , C07C255/42 , C07C303/40 , C07D213/74 , C07D213/75
CPC分类号: C07D417/12 , C07C209/78 , C07C211/60 , C07C217/92 , C07C231/12 , C07C233/80 , C07C237/48 , C07C255/42 , C07C255/58 , C07C255/60 , C07C273/1854 , C07C275/40 , C07C275/42 , C07C303/40 , C07C311/21 , C07C2601/02 , C07C2602/10 , C07D213/40 , C07D213/61 , C07D213/73 , C07D213/74 , C07D213/75 , C07D213/81 , C07D213/82 , C07D231/14 , C07D231/20 , C07D239/28 , C07D239/42 , C07D241/20 , C07D261/18 , C07D311/58 , C07D405/04 , C07D405/12 , C07D409/14
摘要: The present invention relates to compounds TAAR receptor antagonists of formula I wherein X, R, L, Ar and R1 are as described herein, compositions containing compounds of formula I, methods of manufacture of compounds of formula I and methods of treating psychiatric disorders with compounds of formula I.
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公开(公告)号:US20180057447A1
公开(公告)日:2018-03-01
申请号:US15559762
申请日:2016-03-24
发明人: Hisanori ITOH , Yoji HORI , Masashi OTSUKA , Takaji MATSUMOTO , Tomoharu SATO
IPC分类号: C07C233/58 , A23L2/52 , A23L27/00 , A61K8/42 , C07C69/75 , A61K8/37 , C07C255/44 , C07C233/63 , C07C233/60 , C07D213/40 , A61K8/49 , C07C69/68 , C07D317/72 , A61Q19/10 , A61Q11/00
CPC分类号: C07C233/58 , A23L2/00 , A23L2/52 , A23L27/00 , A23V2002/00 , A61K8/37 , A61K8/42 , A61K8/4926 , A61K8/4973 , A61Q11/00 , A61Q19/10 , C07C69/68 , C07C69/75 , C07C233/60 , C07C233/63 , C07C255/44 , C07C2601/14 , C07D213/40 , C07D317/72 , C09K3/00
摘要: The purpose of the present invention is to provide a cooling agent composition containing a novel methyl menthol derivative having no undesirable feeling of stimulation, malodor, bitterness, or the like, it being possible to use the cooling agent composition as a cooling agent or sensory stimulation agent having exceptional persistence of a sense of coolness and refreshing feeling. The present invention pertains to a cooling agent composition containing a methyl menthol derivative represented by general formula (1A) or general formula (1B).
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