-
公开(公告)号:US20190202785A1
公开(公告)日:2019-07-04
申请号:US16325880
申请日:2017-08-16
申请人: Novartis AG
发明人: Florian Karl KLEINBECK-RINIKER , Ives MAFLI , Benjamin MARTIN , Gerhard PENN , Gottfried SEDELMEIER , Joerg SEDELMEIER , Francesco VENTURONI
IPC分类号: C07D213/16 , C07C45/49 , C07C249/02 , C07C229/06 , C07C201/12 , C07D207/267
CPC分类号: C07D213/16 , C07B2200/07 , C07C45/49 , C07C67/347 , C07C201/06 , C07C201/12 , C07C201/16 , C07C205/51 , C07C205/53 , C07C227/18 , C07C229/06 , C07C231/02 , C07C249/02 , C07C249/08 , C07C251/38 , C07C269/00 , C07C271/22 , C07D207/12 , C07D207/267 , C07D213/36 , C07C229/34 , C07C233/51 , C07C69/738
摘要: The present invention relates to a new chemical synthesis, intermediates and catalysts useful for the preparation of the neprilysin (NEP) inhibitor sacubitril, inter alia via nitro 5 compounds. It further relates to new intermediate compounds and their use for said new chemical synthesis route, as well as a new catalyst ligand.
-
公开(公告)号:US20180179156A1
公开(公告)日:2018-06-28
申请号:US15736662
申请日:2016-06-06
发明人: Steven A. Rich , Emerich Eisenreich , Xuejun Karl Liu , Bingidimi Itute Mobele , Satish Goud Puppali
IPC分类号: C07D207/12 , C07C53/126 , C07C57/12 , C07C57/03
CPC分类号: C07D207/12 , C07C53/126 , C07C57/03 , C07C57/12
摘要: Novel glycopyrronium fatty acid salts have been developed. Bi-phasic reaction conditions enable the desired counterion exchange reactions between glycopyrronium bromide and fatty acid salts of alkali metals and alkaline earth metals in methods to form glycopyrronium fatty acid salts. In preferred embodiments, an excess of the free fatty acid in the reaction mixture stabilizes the glycopyrronium fatty acid salt and reduces the formation of the impurity, Acid A. In some preferred embodiments, between 0.2 and 1.2 molar equivalent of excess free fatty acid is added to the reaction mixture. In another embodiment, approximately 1.2 molar equivalent of excess free fatty acid is added to the reaction mixture.
-
公开(公告)号:US10004717B2
公开(公告)日:2018-06-26
申请号:US15438636
申请日:2017-02-21
申请人: Dermira, Inc.
发明人: John Allan Statler , Anthony Adrian Shaw , Delphine Caroline Imbert , Jennifer Leigh Nelson , Patricia Andres , Lisa Lynn McQueen , Stephan Xander Mattheus Boerrigter , Jon Gordon Selbo , Mark Christopher Andres
IPC分类号: A61K31/40 , C07D207/12 , A61K9/00 , A61K9/08 , A61K47/10 , A61K47/12 , A61K47/32 , A61K47/34
CPC分类号: A61K31/40 , A61K9/0014 , A61K9/08 , A61K47/10 , A61K47/12 , A61K47/32 , A61K47/34 , C07D207/12
摘要: Salts of glycopyrrolate, including solid forms and formulations such as topicals thereof, are disclosed. Methods of making glycopyrrolate salts, including formulations such as topicals thereof, and methods of treating hyperhidrosis with salts of glycopyrrolate, and formulations such as topicals thereof, are disclosed.
-
公开(公告)号:US09999673B2
公开(公告)日:2018-06-19
申请号:US13979336
申请日:2012-01-11
申请人: Kallanthottathil G. Rajeev , Muthiah Manoharan , Muthusamy Jayaraman , Martin Maier , Jayaprakash K. Nair , David Butler
发明人: Kallanthottathil G. Rajeev , Muthiah Manoharan , Muthusamy Jayaraman , Martin Maier , Jayaprakash K. Nair , David Butler
IPC分类号: A61K47/18 , C07C235/06 , C07C271/16 , C07D207/12 , C07D307/20 , C07D207/14 , C07D307/12 , C08G65/329 , A61K47/48
CPC分类号: A61K47/18 , A61K47/6911 , C07C235/06 , C07C271/16 , C07D207/12 , C07D207/14 , C07D307/12 , C07D307/20 , C08G65/329 , C08L2203/02
摘要: The invention provides poly(ethylene glycol)-lipid conjugates for use in drug delivery.
-
公开(公告)号:US09994574B2
公开(公告)日:2018-06-12
申请号:US14441690
申请日:2013-11-12
IPC分类号: C07D487/04 , A61K31/519 , C07C269/04 , C07D207/12 , C07D207/34 , C07C53/06 , C07C55/07 , C07D207/44 , A61P35/00
CPC分类号: C07D487/04 , C07B2200/13 , C07C53/06 , C07C55/07 , C07C269/04 , C07D207/12 , C07D207/34 , C07D207/44 , C07C271/22
摘要: The invention relates to salt forms of (3R,4S)-1-((4-amino-5H-pyrrolo[3,2-d]pyrimidin-7-yl)methyl)-4-(methyl-thiomethyl)pyrrolidin-3-ol, as well as polymorphic forms of the salts. The invention further relates to processes for preparing the salt forms and to the use of the salt forms in the treatment of diseases and disorders where it is desirable to inhibit 5′-methylthioadenosine phosphorylase (MTAP).
-
公开(公告)号:US09963444B2
公开(公告)日:2018-05-08
申请号:US15311817
申请日:2015-05-13
发明人: Michael Malamas , Alexandros Makriyannis , Kumara Vadivel Subramanian , Kyle M. Whitten , Nikolai M. Zvonok , Jay Matthew West , Michael Mccormack , Spiro Pavlopoulos
IPC分类号: C07C255/46 , C07D405/12 , C07D403/12 , C07D317/54 , C07D319/18 , C07D231/12 , C07D401/12 , C07D413/12 , C07D261/08 , C07D205/04 , C07D207/12 , C07D211/10 , C07D211/26 , C07D211/46 , C07D213/46 , C07D213/64 , C07C331/20 , C07C331/24 , C07C331/26 , C07D213/30 , C07D213/36 , C07D239/26 , C07D239/28 , C07D241/18 , C07D295/13 , C07D295/135 , C07D317/58
CPC分类号: C07D405/12 , C07B2200/07 , C07C255/46 , C07C331/20 , C07C331/24 , C07C331/26 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07D205/04 , C07D207/12 , C07D211/10 , C07D211/26 , C07D211/46 , C07D213/30 , C07D213/36 , C07D213/46 , C07D213/64 , C07D231/12 , C07D239/26 , C07D239/28 , C07D241/18 , C07D261/08 , C07D295/13 , C07D295/135 , C07D317/54 , C07D317/58 , C07D319/18 , C07D401/12 , C07D403/12 , C07D413/12
摘要: A compound is represented as Formula I, a tautomer thereof, a stereoisomer thereof, or a pharmaceutically acceptable salt thereof. Compounds of Formula I are inhibitors of N-acylethanolamine hydrolyzing acid amidase (NAAA). The present technology is directed to compounds, compositions, and methods to inhibit N-acylethanolamine hydrolyzing acid amidase and to treat N-acylethanolamine hydrolyzing acid amidase mediated conditions in a subject.
-
公开(公告)号:US20180118722A1
公开(公告)日:2018-05-03
申请号:US15566971
申请日:2016-04-14
发明人: Timo STELLFELD , Carlo STRESEMANN , Roman HILLIG , Silke KÖHR , Detlef STÖCKIGT , Jörg WEISKE , Naomi BARAK , Clara CHRIST , Antonius TER LAAK , Volker BADOCK
IPC分类号: C07D403/04 , C07D231/06 , C07D207/12 , C07C267/00 , A61P35/00
CPC分类号: C07D403/04 , A61P35/00 , C07C267/00 , C07D207/12 , C07D231/06
摘要: The present invention relates to protein-lysine N-methyltransferase SMYD2 (SET and MYND domain-containing protein 2) inhibitors, in particular SMYD2-inhibitory substituted cyanoguanidine-pyrazolines of general formula (I), wherein R1, R3, R4, R5 and n have the meaning as described and defined herein, as well as to pharmaceutical compositions comprising compounds according to the invention and to their prophylactic and therapeutic use for hyperproliferative disorders, in particular for cancer, respectively tumour disorders. The present invention furthermore relates to the use of SMYD2 inhibitors for benign hyperplasias, atherosclerotic disorders, sepsis, autoimmune disorders, vascular disorders, viral infections, neurodegenerative disorders, inflammatory disorders, atherosclerotic disorders and the control of male fertility.
-
公开(公告)号:US09920028B2
公开(公告)日:2018-03-20
申请号:US15200356
申请日:2016-07-01
发明人: Takeshi Kuboyama , Tomohiro Era , Tomoyuki Naoi
IPC分类号: C07D401/04 , C07C217/08 , C07D211/58 , C07C219/06 , C07C237/22 , C07D491/056 , A61K47/18 , C07C217/28 , C07C219/08 , C07D207/08 , C07D207/12 , A61K47/16 , A61K47/22 , A61K9/00 , A61K9/127 , C12N15/113 , C07C217/40 , C07C237/06 , C07C271/22
CPC分类号: C07D401/04 , A61K9/0019 , A61K9/1272 , A61K47/16 , A61K47/18 , A61K47/186 , A61K47/22 , C07C217/08 , C07C217/28 , C07C217/40 , C07C219/06 , C07C219/08 , C07C237/06 , C07C237/22 , C07C271/22 , C07D207/08 , C07D207/12 , C07D211/58 , C07D491/056 , C12N15/113 , C12N2310/14 , C12N2320/30 , C12N2310/321 , C12N2310/3521
摘要: The present invention provides a cationic lipid, which allow nucleic acids to be easily introduced into cells, represented by formula (I) (wherein: R1 and R2 are, the same or different, alkenyl, etc, and X1 and X2 are hydrogen atoms, or are combined together to form a single bond or alkylene, and X3 is absent or is alkyl, etc, Y is absent or anion, a and b are, the same or different, 0 to 3, and L3 is a single bond, etc, R3 is alkyl, etc, L1 and L2 are —O—, —CO—O— or —O—CO—), a composition comprising the cationic lipid and a nucleic acid, and a method for introducing a nucleic acid into a cell by using the composition comprising the cationic lipid and the nucleic acid, and the like.
-
公开(公告)号:US20180042908A1
公开(公告)日:2018-02-15
申请号:US15784376
申请日:2017-10-16
发明人: Atsushi NAGANAWA , Kensuke KUSUMI , Kazuhiro OTSUKI , Tetsuya SEKIGUCHI , Akito KAKUUCHI , Koji SHINOZAKI , Hiroshi YAMAMOTO , Shigeyuki NONAKA
IPC分类号: A61K31/445 , A61K31/454 , A61K31/453 , A61K31/4523 , A61K31/40 , A61K31/397 , C07D401/12 , C07D207/12 , C07D211/52 , C07D207/16 , C07D211/48 , C07D205/04 , A61K31/4545 , C07D405/12
CPC分类号: A61K31/445 , A61K31/397 , A61K31/40 , A61K31/4523 , A61K31/453 , A61K31/454 , A61K31/4545 , C07D205/04 , C07D207/12 , C07D207/16 , C07D211/48 , C07D211/52 , C07D401/12 , C07D405/12
摘要: The compound of the formula (I-1): wherein all the symbols have the same meanings as described in the specification, has two cyclic groups, particularly phenoxy groups at specific substitution positions and thus has high human S1P2 antagonistic activity. The compound may therefore be used as a therapeutic agent for S1P2-mediated diseases such as diseases resulting from vascular constriction, fibrosis, and respiratory diseases.
-
公开(公告)号:US20180030484A1
公开(公告)日:2018-02-01
申请号:US15488320
申请日:2017-04-14
申请人: Genomatica, Inc.
发明人: Anthony P. Burgard , Robin E. Osterhout , Stephen J. Van Dien , Cara Ann Tracewell , Priti Pharkya , Stefan Andrae
IPC分类号: C12P7/18 , C08G69/26 , C08G63/66 , C08G63/12 , C08G63/06 , C12N9/10 , C12P19/02 , C12P7/24 , C08G18/32 , C12N9/88 , C12N9/04 , C12N9/06 , C07D207/12
CPC分类号: C12P7/18 , C07D207/12 , C08G18/3206 , C08G63/06 , C08G63/12 , C08G63/66 , C08G69/26 , C12N9/0006 , C12N9/0028 , C12N9/1007 , C12N9/88 , C12P7/24 , C12P19/02 , C12Y101/01224 , C12Y101/01244 , C12Y101/02007 , C12Y105/0102 , C12Y201/01 , C12Y201/0109 , C12Y402/01 , Y02P20/52
摘要: Provided herein is a non-naturally occurring microbial organism having a methanol metabolic pathway that can enhance the availability of reducing equivalents in the presence of methanol. Such reducing equivalents can be used to increase the product yield of organic compounds produced by the microbial organism, such as 1,4-butanediol (BDO). Also provided herein are methods for using such an organism to produce BDO.
-
-
-
-
-
-
-
-
-