公开(公告)号：US12173009B2

公开(公告)日：2024-12-24

申请号：US17944782

申请日：2022-09-14

Applicant: CELLTAXIS, LLC

Inventor： Damian O. Arnaiz ,  Greg Brown ,  Emmanuel Claret ,  Arwed Cleve ,  David Davey ,  William Guilford ,  Seock-Kyu Khim ,  Thomas Kirkland ,  Monica J. Kochanny ,  Amy Liang ,  David Light ,  John Parkinson ,  Guo Ping Wei ,  Bin Ye

IPC: C07D487/08 ,  C07C217/58 ,  C07C229/08 ,  C07C229/38 ,  C07C233/78 ,  C07C255/57 ,  C07C271/20 ,  C07D207/04 ,  C07D207/09 ,  C07D207/16 ,  C07D211/26 ,  C07D211/34 ,  C07D211/58 ,  C07D243/08 ,  C07D263/14 ,  C07D263/32 ,  C07D277/22 ,  C07D277/68 ,  C07D295/04 ,  C07D295/096 ,  C07D295/16 ,  C07D401/10 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D451/02 ,  C07D451/04

Abstract: This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.

公开(公告)号：US20230174562A1

公开(公告)日：2023-06-08

申请号：US17923831

申请日：2021-05-07

Applicant: TONIX PHARMACEUTICALS, INC. ,  TONIX PHARMACEUTICALS HOLDING CORP.

Inventor： Philip S. Schein ,  Darryl C. Rideout

IPC: C07F9/165 ,  A61K45/06 ,  A61P39/00 ,  A61K31/661 ,  C07D243/08 ,  A61K31/551 ,  C07D241/04 ,  A61K31/495 ,  C07D243/10 ,  C07D245/02 ,  A61K31/395 ,  C07D245/04 ,  C07D487/04 ,  A61K31/4985 ,  C07C53/18 ,  C07D241/38 ,  A61K31/498 ,  C07F9/6571 ,  A61K31/675 ,  C07C323/25 ,  A61K31/145

CPC classification number: C07F9/1651 ,  A61K45/06 ,  A61P39/00 ,  A61K31/661 ,  C07D243/08 ,  A61K31/551 ,  C07D241/04 ,  A61K31/495 ,  C07D243/10 ,  C07D245/02 ,  A61K31/5545 ,  C07D245/04 ,  C07D487/04 ,  A61K31/4985 ,  C07C53/18 ,  C07D241/38 ,  A61K31/498 ,  C07F9/657118 ,  A61K31/675 ,  C07C323/25 ,  A61K31/145 ,  C07B2200/13

Abstract: The present disclosure relates to prodrugs, double prodrugs, derivatives and analogues of 3-(methylamino)-2-((methy-lamino)methyl)propane-1-thiol. Their use as radio- and chemo-protectors is also described.

公开(公告)号：US11566025B2

公开(公告)日：2023-01-31

申请号：US16798859

申请日：2020-02-24

Applicant: Katholieke Universiteit Leuven

Inventor： Dorothée Bardiot ,  Gunter Carlens ,  Kai Dallmeier ,  Suzanne Kaptein ,  Mohamed Koukni ,  Arnaud Marchand ,  Johan Neyts ,  Wim Smets

IPC: C07D471/04 ,  A61K31/34 ,  C07D207/06 ,  A61K31/381 ,  A61K31/40 ,  A61K31/415 ,  A61K31/437 ,  A61K31/4439 ,  A61K45/06 ,  C07D207/323 ,  C07D207/335 ,  C07D211/06 ,  C07D211/16 ,  C07D223/04 ,  C07D241/04 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D231/12 ,  C07D333/22 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D405/04 ,  C07D405/06 ,  C07D409/04 ,  C07D409/06 ,  C07D409/14 ,  C07D413/04 ,  C07D413/06 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D261/08 ,  C07D265/30 ,  C07D267/10 ,  C07D275/02 ,  C07D498/04 ,  C07D279/12 ,  C07D409/12 ,  C07D403/06 ,  C07D405/12 ,  C07D407/06 ,  C07D271/04 ,  C07D285/06 ,  C07D403/12 ,  C07D243/06 ,  C07D513/04 ,  C07D407/04 ,  C07D307/46 ,  C07D243/08 ,  C07D263/32 ,  C07D271/08 ,  C07D277/28 ,  C07D285/10 ,  C07D307/52 ,  C07D413/12 ,  C07D487/04

Abstract: The present invention relates to a series of novel compounds, methods to prevent or treat viral infections in animals by using the novel compounds and to said novel compounds for use as a medicine, more preferably for use as a medicine to treat or prevent viral infections, particularly infections with RNA viruses, more particularly infections with viruses belonging to the family of the Flaviviridae, and yet more particularly infections with the Dengue virus. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the novel compounds, to the compositions or preparations for use as a medicine, more preferably for the prevention or treatment of viral infections. The invention also relates to processes for preparation of the compounds.

公开(公告)号：US20220213081A1

公开(公告)日：2022-07-07

申请号：US17566915

申请日：2021-12-31

Applicant: California Institute of Technology

Inventor： Brian M. Stoltz ,  Alexander W. Sun ,  Stephan N. Hess ,  Carina I. Jette ,  Irina Geibel ,  Shoshana Bachman ,  Masaki Hayashi ,  Hideki Shimizu ,  Jeremy B. Morgan ,  Shunya Sakurai ,  Zachary P. Sercel

IPC: C07D413/14 ,  C07D207/26 ,  C07D243/08 ,  C07D239/06 ,  C07D507/00 ,  C07D241/08

Abstract: Described here are transition metal-catalyzed enantioselective arylation and vinylation reactions of α-substituted lactams, such as γ-lactams. The use of various electrophiles and ligands are described, and result in the construction of α-quaternary centers in good yields (up to 91% yield) and high enantioselectivities (up to 97% ee).

公开(公告)号：US11267819B2

公开(公告)日：2022-03-08

申请号：US16738190

申请日：2020-01-09

Applicant: CELLTAXIS, LLC

Inventor： Damian O. Arnaiz ,  Greg Brown ,  Emmanuel Claret ,  Arwed Cleve ,  David Davey ,  William Guilford ,  Seock-Kyu Khim ,  Thomas Kirkland ,  Monica J. Kochanny ,  Amy Liang ,  David Light ,  John Parkinson ,  Guo Ping Wei ,  Bin Ye

IPC: C07D487/08 ,  C07C217/58 ,  C07C229/38 ,  C07C233/78 ,  C07C255/57 ,  C07C271/20 ,  C07D207/04 ,  C07D211/58 ,  C07D243/08 ,  C07D295/04 ,  C07D295/16 ,  C07D451/04 ,  C07D207/09 ,  C07D211/26 ,  C07D263/32 ,  C07D295/096 ,  C07D401/10 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07C229/08 ,  C07D263/14 ,  C07D401/12 ,  C07D207/16 ,  C07D211/34 ,  C07D277/22 ,  C07D277/68 ,  C07D451/02

Abstract: This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.

公开(公告)号：US20210388011A1

公开(公告)日：2021-12-16

申请号：US17315258

申请日：2021-05-07

Applicant: TONIX PHARMACEUTICALS, INC. ,  TONIX PHARMACEUTICALS HOLDING CORP.

Inventor： Philip S. Schein ,  Darryl C. Rideout

IPC: C07F9/24 ,  C07F9/6574 ,  C07D241/04 ,  C07D243/08 ,  C07D243/10 ,  C07D401/04 ,  C07D487/04 ,  A61K45/06 ,  A61P39/00

Abstract: The present disclosure relates to prodrugs, double prodrugs, derivatives and analogues of 3-(methylamino)-2-((methylamino)methyl)propane-1-thiol. Their use as radio- and chemo-protectors is also described.

公开(公告)号：US11059807B2

公开(公告)日：2021-07-13

申请号：US16204053

申请日：2018-11-29

Applicant: Dicerna Pharmaceuticals, Inc.

Inventor： Bob Dale Brown

IPC: C07D403/06 ,  C07D233/61 ,  C07D233/64 ,  C07D239/42 ,  C07D241/04 ,  C07C237/06 ,  C07D295/03 ,  C07D211/36 ,  C07D295/13 ,  C07D295/15 ,  C07C211/21 ,  C12N15/11 ,  C12N15/113 ,  C12N15/88 ,  A61K9/127 ,  A61K31/713 ,  A61K47/18 ,  A61K47/22 ,  A61K9/107 ,  A61K9/14 ,  C07D243/08 ,  C07D401/04 ,  C07D403/04 ,  A61K38/00

Abstract: The present invention relates to lipid compounds and uses thereof. In particular, the compounds include a class of cationic lipids having an amine moiety, such as an amino-amine or an amino-amide moiety. The lipid compounds are useful for in vivo or in vitro delivery of one or more agents (e.g., a polyanionic payload or an antisense payload, such as an RNAi agent).

公开(公告)号：US20190276414A1

公开(公告)日：2019-09-12

申请号：US16304634

申请日：2017-06-02

Applicant: ENANTIA, S.L.

Inventor： Alexander Christian COMELY ,  Nicolas TESSON

IPC: C07D243/08 ,  C07C39/16 ,  C07D413/14 ,  C07B57/00

Abstract: Relating to processes for preparing suvorexant or its pharmaceutically acceptable salts through the formation of a cocrystal of (R)-benzyl 5-methyl-1,4-diazepane-1-carboxylate hydrochloride with (R)-(+)-1,1,2-triphenyl-1,2-ethanediol ((R)-TED). This cocrystal provides the resolution of an intermediate of suvorexant, in particular, of (rac)-benzyl5-methyl-1,4-diazepane-1-carboxy-lateor a hydrochloride salt thereof. It also relates to a new cocrystal useful in such preparation processes.

公开(公告)号：US20190202783A1

公开(公告)日：2019-07-04

申请号：US16295364

申请日：2019-03-07

Applicant: Heptares Therapeutics Limited

Inventor： Giles Albert Brown ,  Miles Stuart Congreve ,  Mark Pickworth ,  Benjamin Gerald Tehan

IPC: C07D207/14 ,  C07D487/10 ,  C07D209/96 ,  C07D271/06 ,  C07D413/12 ,  C07D487/04 ,  C07D471/04 ,  C07D413/14 ,  C07D409/08 ,  C07D243/08 ,  C07D471/10 ,  C07D403/04 ,  C07D401/08 ,  C07D213/57 ,  C07D295/205 ,  C07D413/04

CPC classification number: C07D207/14 ,  C07D209/96 ,  C07D213/57 ,  C07D243/08 ,  C07D271/06 ,  C07D295/205 ,  C07D401/08 ,  C07D403/04 ,  C07D409/08 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10

Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor or M1 and M4 receptors and which are useful in the treatment of muscarinic M1 or M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula wherein Q4, Q5, R5, p, V, Q1, Q2, X1, X2 and W are defined herein.

公开(公告)号：US10308655B2

公开(公告)日：2019-06-04

申请号：US15578086

申请日：2015-12-23

Applicant: AJOU UNIVERSITY INDUSTRY-ACADEMIC COOPERATION FOUNDATION

Inventor： Sang Dun Choi ,  Prasannavenkatesh Durai ,  Asma Achek

IPC: C07D487/04 ,  A61P1/00 ,  A61P27/02 ,  A61P1/02 ,  A61P7/00 ,  A61P19/06 ,  A61P25/28 ,  A61P11/06 ,  A61P31/12 ,  A61P17/00 ,  A61P19/02 ,  A61P37/08 ,  A61P13/12 ,  A61P27/16 ,  A61P11/00 ,  A61P29/00 ,  A61P1/04 ,  A61P27/00 ,  C07C251/24 ,  C07D207/277 ,  C07D211/26 ,  C07D211/34 ,  C07D243/08 ,  C07D265/30 ,  C07D333/78 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D409/12 ,  C07D471/04 ,  C07D471/10 ,  A61K9/00 ,  A61K31/5377 ,  A61K31/551 ,  A61K31/4178 ,  A61K31/4453 ,  A61K31/496 ,  A61K31/506

Abstract: The present disclosure relates to a novel small molecule TLR2 antagonist, and particularly, to 19 novel TLR2 antagonists, a pharmaceutical composition, including the antagonists, for preventing or treating inflammatory diseases, and a TLR4 regulator.The novel TLR2 antagonists according to the present disclosure can be effectively used as a preparation for oral administration by having low molecular weight and high oral bioavailability, and can be useful in pharmaceutical compositions for preventing or treating inflammatory diseases since the secretion of IL-8 is effectively inhibited and in vivo cytotoxicity is not induced. In addition, the novel TLR2 antagonists according to the present disclosure can be used as a TLR4 regulator.