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1.
公开(公告)号:US20250066359A1
公开(公告)日:2025-02-27
申请号:US18724366
申请日:2022-12-27
Inventor: Jianhua SHEN , Xin XIE , Yanglong ZHANG , Tingting ZHAO , Fanghui HAN , Ying YUN
IPC: C07D471/10 , A61K31/397 , A61K31/407 , A61K31/437 , A61K31/438 , A61K31/444 , A61K31/4523 , A61K31/495 , A61K31/496 , A61K31/5386 , A61K45/06 , A61P1/16 , A61P3/10 , C07D205/12 , C07D211/96 , C07D211/98 , C07D221/20 , C07D295/26 , C07D401/04 , C07D471/04 , C07D487/10 , C07D498/10
Abstract: Provided are a class of compounds which have a structure as shown in the following general formula (I) and are used as somatostatin receptor subtype 5 (SSTR5) antagonists, and a pharmaceutical composition and the use thereof. The compounds have good SSTR5 antagonistic activities, and can be used for preparing drugs for treating related diseases mediated by SSTR5.
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公开(公告)号:US20230159441A1
公开(公告)日:2023-05-25
申请号:US17955270
申请日:2022-09-28
Applicant: Ensysce Biosciences Inc.
Inventor: Lynn Kirkpatrick
IPC: C07C279/12 , C07D207/50 , C07D211/98 , C07D265/30 , C07D207/09 , A61K45/06
CPC classification number: C07C279/12 , C07D207/50 , C07D211/98 , C07D265/30 , C07D207/09 , A61K45/06
Abstract: The present disclosure provides methadone prodrugs, pharmaceutical compositions, and their methods of use, where the pharmaceutical compositions comprise a methadone prodrug that provides enzymatically-controlled release of methadone, and an optional enzyme inhibitor that interacts with the enzyme(s) that mediates the enzymatically-controlled release of methadone from the prodrug so as to attenuate enzymatic cleavage of the prodrug.
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公开(公告)号:US20230080054A1
公开(公告)日:2023-03-16
申请号:US17580652
申请日:2022-01-21
Applicant: ILDONG PHARMACEUTICAL CO., LTD.
Inventor: Jinah JEONG , Hyunjung KWAK , Gunhee KIM , Jeongeun KIM , Sanghwan LEE , Seolhee LEE , Jinhee LEE , Jihye CHOI , Hongchul YOON , Joontae PARK , Kyungmi AN , Jungwoo LEE , Eunjung LEE
IPC: C07D405/12 , C07D307/52 , C07D405/14 , C07D237/20 , C07D401/12 , C07D403/12 , C07D409/12 , C07C237/30 , C07D241/20 , C07D239/42 , C07D413/14 , C07D409/14 , C07D471/08 , C07D213/74 , C07D417/12 , C07D271/07 , C07D213/38 , C07D239/26 , C07D241/12 , C07D211/98
Abstract: The present invention relates to a new compound that can inhibit an anoctamin 6 protein, a composition comprising the compound, a method for preparing the compound, and a method for using the compound or composition.
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公开(公告)号:US20220024871A1
公开(公告)日:2022-01-27
申请号:US17203266
申请日:2021-03-16
Applicant: ACADIA Pharmaceuticals Inc.
Inventor: Marlon Carlos , Sagun Tandel , Roger Olsson , Mikael Hillgren , Matthew J. Fleming , Andreas Philipp Boudier , Beat T. Weber
IPC: C07D211/98
Abstract: Disclosed herein are methods for obtaining N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N-(4-(2-methylpropyloxy)phenylmethyl) carbamide (pimavanserin) comprising the step of contacting an intermediate according to Formula (A) or a salt thereof, with an intermediate Formula B, or a salt thereof, to produce pimavanserin or a salt thereof wherein Y is —ORi or —NR2aR2b; R3 is hydrogen or substituted or unsubstituted heteroalicyclyl, R4 is substituted or unsubstituted aralkyl; X is —OR22 or —NR23R24; (wherein R22 is hydrogen or substituted or unsubstituted C1-6alkyl and one of R23 and R24 is hydrogen and the other is hydrogen or N-methylpiperidin-4-yl); and R21 is —OCH2CH(CH3)2 or F; Also disclosed herein is the tartrate salt of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)phenylmethyl) carbamide and methods for obtaining the salt.
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公开(公告)号:US10934257B2
公开(公告)日:2021-03-02
申请号:US16764315
申请日:2019-07-19
Inventor: Biao Wang , Qiao Jiang , Bingbing Li , Murong Peng , Weijian Xie
IPC: C07D211/98
Abstract: The present disclosure discloses a method for safely preparing pimavanserin and tartrate thereof by using triphosgene. The synthesis route includes: Raw materials used in the method of the present disclosure are safe and inexpensive, thereby effectively reducing the production costs. The method of the present disclosure has mild reaction conditions, and avoids using phosgene, which is highly toxic and difficult to handle is avoided. Thus, the method is readily implemented industrially.
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公开(公告)号:US10034886B2
公开(公告)日:2018-07-31
申请号:US15711858
申请日:2017-09-21
Applicant: Celgene International II SÀRL
Inventor: Marcus F. Boehm , Esther Martinborough , Manisha Moorjani , Junko Tamiya , Liming Huang , Adam R. Yeager , Enugurthi Brahmachary , Thomas Fowler , Andrew Novak , Premji Meghani , Michael Knaggs , Daniel Glynn , Mark Mills
IPC: A61K31/506 , C07D403/10 , A61K31/551 , A61K31/4725 , A61K31/495 , A61K31/4545 , A61K31/454 , A61K31/4468 , A61K31/4439 , A61K31/445 , A61K31/44 , A61K31/433 , A61K31/4245 , A61K31/426 , A61K31/421 , A61K31/4178 , C07D495/04 , C07D471/04 , A61K31/402 , C07D417/12 , C07D413/12 , C07D413/04 , C07D409/14 , C07D409/12 , C07D407/12 , C07D405/12 , C07D403/12 , C07D403/04 , C07D401/12 , C07D401/06 , C07D401/04 , C07D295/135 , C07D295/084 , C07D285/12 , C07D285/08 , C07D277/30 , C07D271/107 , C07D271/06 , C07D263/32 , C07D253/065 , C07D253/06 , C07D243/08 , C07D241/12 , C07D241/08 , C07D239/74 , C07D239/34 , C07D239/26 , C07D237/08 , C07D231/12 , C07D215/14 , C07D213/55 , C07D211/98 , C07D211/22 , C07D207/08 , A61K38/26 , A61K31/53 , A61K31/505 , A61K31/501 , A61K31/50 , A61K31/4965 , A61K31/497 , A61K31/4709
CPC classification number: A61K31/551 , A61K31/402 , A61K31/4178 , A61K31/421 , A61K31/4245 , A61K31/426 , A61K31/433 , A61K31/44 , A61K31/4439 , A61K31/445 , A61K31/4468 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/495 , A61K31/4965 , A61K31/497 , A61K31/50 , A61K31/501 , A61K31/505 , A61K31/506 , A61K31/53 , A61K38/26 , C07D207/08 , C07D211/22 , C07D211/98 , C07D213/55 , C07D215/14 , C07D231/12 , C07D237/08 , C07D239/26 , C07D239/34 , C07D239/74 , C07D241/08 , C07D241/12 , C07D243/08 , C07D253/06 , C07D253/065 , C07D263/32 , C07D271/06 , C07D271/107 , C07D277/30 , C07D285/08 , C07D285/12 , C07D295/084 , C07D295/135 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/10 , C07D403/12 , C07D405/12 , C07D407/12 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/12 , C07D417/12 , C07D471/04 , C07D495/04
Abstract: Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “” represents either or both the R and S form of the compound): where A, B, C, Y1, Y2, Z, R1, R2, R3, R4, R5, W1, n, p and q are as defined herein.
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公开(公告)号:US09688633B2
公开(公告)日:2017-06-27
申请号:US14774508
申请日:2014-03-14
Applicant: INSTITUT DE RECHERCHE POUR LE DEVELOPPEMENT
Inventor: Ignacio Aldana Moraza , Silvia Victoria Blair Trujillo , Eric Deharo , Giovanny Garavito , Adela Mendoza Lizaldez , Silvia Perez-Silanes
IPC: A61K31/445 , C07D211/04 , C07D211/70 , C07D409/06 , C07D211/98 , A61K31/4418 , A61K31/451 , A61K45/06 , C07D211/58
CPC classification number: C07D211/70 , A61K31/4418 , A61K31/451 , A61K45/06 , C07D211/58 , C07D211/98 , C07D409/06 , Y02A50/411
Abstract: The present invention relates to new arylaminoalcohol derivatives of formula (I), and to a method for the preparation of such compounds: I The invention also relates to the use of these compounds as medicaments, and in particular for the prevention and/or the treatment of parasitic diseases caused by apicomplexan parasites such as malaria and toxoplasmosis. Finally, the invention relates to pharmaceutical compositions containing such compounds of formula (I) as active principles.
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8.
公开(公告)号:US20170057914A1
公开(公告)日:2017-03-02
申请号:US15349297
申请日:2016-11-11
Applicant: BAYER CROPSCIENCE AG , BAYER INTELLECTUAL PROPERTY GMBH
Inventor: Adeline KOEHLER , Bernd ALIG , Angela BECKER , Arnd VOERSTE , Ulrich GOERGENS , Reiner FISCHER , Wahed Ahmed MORADI , Silvia CEREZO-GALVEZ , Julia Johanna HAHN , Kerstin ILG , Hans-Georg SCHWARZ , Takuya GOMIBUCHI , Masahito ITO , Daiei YAMAZAKI , Katsuhiko SHIBUYA , Eiichi SHIMOJO
IPC: C07C323/41 , C07C323/45 , C07C317/40 , C07C315/02 , C07C323/36 , C07D333/38 , C07D207/34 , C07D307/68 , C07C319/14 , C07D213/78 , C07D295/13 , C07D241/24 , C07D207/22 , C07D279/06 , C07D263/28 , C07D277/16 , C07D277/54 , C07C335/16 , C07D239/28 , C07D305/08 , C07D211/98 , C07D307/24 , C07D277/38 , C07D331/04 , C07D333/48 , C07D211/38 , C07D401/06 , C07D285/08 , C07C319/20
CPC classification number: A01N41/10 , A01N41/12 , A01N43/08 , A01N43/10 , A01N43/36 , A01N43/40 , A01N43/60 , A01N43/84 , A01N43/86 , C07C315/02 , C07C317/34 , C07C317/40 , C07C319/14 , C07C319/20 , C07C323/36 , C07C323/41 , C07C323/44 , C07C323/45 , C07C335/16 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D207/22 , C07D207/34 , C07D211/38 , C07D211/72 , C07D211/98 , C07D213/61 , C07D213/78 , C07D239/28 , C07D241/24 , C07D263/28 , C07D277/16 , C07D277/18 , C07D277/38 , C07D277/54 , C07D279/06 , C07D285/08 , C07D295/125 , C07D295/13 , C07D305/08 , C07D307/24 , C07D307/68 , C07D331/04 , C07D333/38 , C07D333/48 , C07D401/06
Abstract: The present invention relates to novel N-arylamide-substituted trifluoroethyl sulfide derivatives of the formula (I) in which X1, X2, X3, X4, R1, R2, R3, n have the meanings given in the description—to their use as acaricides and insecticides for controlling animal pests and to processes and intermediates for their preparation
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9.
公开(公告)号:US20150361037A1
公开(公告)日:2015-12-17
申请号:US14760765
申请日:2013-12-16
Applicant: MERCK PATENT GMBH
Inventor: Christos TSAKLAKIDIS , Markus KLEIN , Paul CZODROWSKI
IPC: C07C279/22 , A61K31/19 , A61K31/165 , C07D209/48 , A61K31/4035 , C07C311/46 , A61K31/18 , A61K31/277 , C07D213/58 , A61K31/4409 , A61K31/4402 , C07D257/04 , A61K31/41 , C07D323/02 , A61K31/36 , C07D307/68 , A61K31/341 , C07D333/24 , A61K31/381 , A61K31/44 , C07D309/14 , A61K31/351 , C07D211/98 , A61K31/4468 , C07D309/06 , C07D335/02 , A61K31/382 , C07D333/28 , C07D213/61 , C07D207/12 , A61K31/4015 , A61K31/401 , C07D295/15 , A61K31/5375 , A61K31/216 , C07D271/10 , A61K31/4245 , C07D285/06 , A61K31/433 , C07D233/58 , A61K31/4164 , C07D249/08 , A61K31/4196 , C07D231/12 , C07C277/08 , C07C53/18
CPC classification number: C07C279/22 , A61K31/165 , A61K31/18 , A61K31/19 , A61K31/216 , A61K31/277 , A61K31/341 , A61K31/351 , A61K31/36 , A61K31/381 , A61K31/382 , A61K31/401 , A61K31/4015 , A61K31/4035 , A61K31/41 , A61K31/4164 , A61K31/4196 , A61K31/4245 , A61K31/433 , A61K31/44 , A61K31/4402 , A61K31/4409 , A61K31/4468 , A61K31/5375 , C07C53/18 , C07C277/08 , C07C311/46 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2602/42 , C07C2603/74 , C07D207/12 , C07D207/16 , C07D207/267 , C07D207/273 , C07D209/48 , C07D211/58 , C07D211/98 , C07D213/40 , C07D213/56 , C07D213/58 , C07D213/61 , C07D231/12 , C07D233/58 , C07D233/61 , C07D249/08 , C07D257/04 , C07D271/06 , C07D271/10 , C07D271/113 , C07D277/28 , C07D285/06 , C07D295/15 , C07D307/68 , C07D309/06 , C07D309/14 , C07D317/58 , C07D317/60 , C07D323/02 , C07D333/20 , C07D333/24 , C07D333/28 , C07D335/02
Abstract: The present invention relates to compounds of the formula (I) and in particular to medicaments comprising at least one compound of the formula I for use in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions in the triggering of which cathepsin D is involved, in particular for use in the treatment and/or prophylaxis of osteoarthritis, traumatic cartilage injuries, arthritis, pain, allodynia or hyperalgesia.
Abstract translation: 本发明涉及式(I)化合物,特别涉及包含至少一种式I化合物的药物,其用于治疗和/或预防触发组织蛋白酶D的生理和/或病理生理条件 涉及,特别是用于治疗和/或预防骨关节炎,创伤性软骨损伤,关节炎,疼痛,异常性疼痛或痛觉过敏。
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公开(公告)号:US08957214B2
公开(公告)日:2015-02-17
申请号:US13814753
申请日:2011-08-26
Applicant: Shinzo Kagabu , Masaaki Mitomi , Shigeki Kitsuda , Ryo Horikoshi , Masahiro Nomura , Yasumichi Onozaki
Inventor: Shinzo Kagabu , Masaaki Mitomi , Shigeki Kitsuda , Ryo Horikoshi , Masahiro Nomura , Yasumichi Onozaki
IPC: C07D213/00 , A01N43/40 , C07D211/98 , A01N43/50 , A01N43/78 , A01N47/40 , C07C233/05 , C07C233/12 , C07C261/04 , C07C271/12 , C07C311/09 , C07F9/58 , C07D401/06
CPC classification number: A01N43/40 , A01N37/18 , A01N43/50 , A01N43/54 , A01N43/58 , A01N43/78 , A01N47/02 , A01N47/12 , A01N47/40 , A01N57/32 , C07C233/05 , C07C233/12 , C07C261/04 , C07C271/12 , C07C311/09 , C07D211/98 , C07D213/36 , C07D213/40 , C07D213/42 , C07D213/61 , C07D213/75 , C07D237/08 , C07D277/32 , C07D333/20 , C07D401/06 , C07D401/12 , C07D405/12 , C07D417/12 , C07F9/58
Abstract: A compound of formula (Ie′): wherein Ar′, R1, R4e and Y are as defined herein and a method of controlling pests using the compound.
Abstract translation: 式(Ie')的化合物:其中Ar',R 1,R 4e和Y如本文所定义,以及使用该化合物控制害虫的方法。
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