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：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：US20180230159A1

公开(公告)日：2018-08-16

申请号：US15891585

申请日：2018-02-08

Applicant: Celtaxsys, Inc.

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

CPC classification number: C07D487/08 ,  C07B2200/07 ,  C07C217/58 ,  C07C229/08 ,  C07C229/38 ,  C07C233/78 ,  C07C255/57 ,  C07C271/20 ,  C07C2601/14 ,  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：US20180127389A1

公开(公告)日：2018-05-10

申请号：US15624417

申请日：2017-06-15

Applicant: H. Lundbeck A/S

Inventor： Thomas Ruhland ,  Garrick Paul Smith ,  Benny Bang-Andersen ,  Ask Puschl ,  Ejner Knud Moltzen ,  Kim Andersen

IPC: C07D295/145 ,  C07D295/033 ,  C07D211/20 ,  C07D243/08 ,  C07D211/70 ,  C07D295/096

CPC classification number: C07D295/145 ,  C07D211/20 ,  C07D211/70 ,  C07D243/08 ,  C07D295/033 ,  C07D295/096

Abstract: The invention provides compounds represented by the general formula I wherein the substituents are defined in the application. The compounds are useful in the treatment of an affective disorder, including depression, anxiety disorders including general anxiety disorder and panic disorder and obsessive compulsive disorder.

公开(公告)号：US09949984B2

公开(公告)日：2018-04-24

申请号：US15301523

申请日：2015-04-01

Applicant: UNIVERSITÉ LAVAL

Inventor： Yvon Cormier ,  Evelyne Israel-Assayag

IPC: A61K31/435 ,  A61K31/44 ,  A61K31/551 ,  C07D243/08 ,  C07D401/04

CPC classification number: A61K31/551 ,  A61K31/435 ,  A61K31/44 ,  C07D243/08 ,  C07D401/04

Abstract: A method for treating cancer comprising administering to a patient in need thereof an effective amount of a compound having the formula: wherein R1 and R2 are independently alkyl of 1 to 6 carbon atoms or cycloalkyl of 3 to 6 carbon atoms, Xa is CH or N, Ya is hydrogen or a substituent, each of which is independently selected; n is an integer from 1 to 5, J is a counter ion.

公开(公告)号：US20180021346A1

公开(公告)日：2018-01-25

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: A61K31/551 ,  C07D417/12 ,  C07D413/12 ,  C07D413/04 ,  C07D409/14 ,  C07D409/12 ,  C07D407/12 ,  C07D405/12 ,  C07D403/12 ,  C07D403/10 ,  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 ,  C07D471/04 ,  C07D237/08 ,  C07D231/12 ,  C07D215/14 ,  C07D213/55 ,  C07D211/98 ,  C07D211/22 ,  C07D207/08 ,  A61K38/26 ,  A61K31/53 ,  A61K31/506 ,  A61K31/505 ,  A61K31/501 ,  A61K31/50 ,  A61K31/4965 ,  A61K31/497 ,  A61K31/495 ,  A61K31/4725 ,  A61K31/4709 ,  A61K31/4545 ,  A61K31/454 ,  A61K31/4468 ,  A61K31/4439 ,  A61K31/445 ,  A61K31/44 ,  A61K31/433 ,  A61K31/4245 ,  A61K31/426 ,  A61K31/421 ,  A61K31/4178 ,  C07D495/04 ,  A61K31/402 ,  C07D239/26

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.

公开(公告)号：US09795613B2

公开(公告)日：2017-10-24

申请号：US14965777

申请日：2015-12-10

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: C07D403/10 ,  A61K31/506 ,  A61K31/551 ,  C07D403/12 ,  C07D215/14 ,  C07D231/12 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D237/08 ,  C07D239/26 ,  C07D407/12 ,  C07D409/12 ,  C07D409/14 ,  C07D239/74 ,  C07D413/04 ,  C07D413/12 ,  C07D241/12 ,  C07D417/12 ,  C07D471/04 ,  C07D253/06 ,  C07D207/08 ,  C07D271/06 ,  C07D495/04 ,  C07D295/084 ,  C07D295/135 ,  C07D213/55 ,  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 ,  A61K31/53 ,  A61K38/26 ,  C07D211/22 ,  C07D211/98 ,  C07D239/34 ,  C07D241/08 ,  C07D243/08 ,  C07D253/065 ,  C07D263/32 ,  C07D271/107 ,  C07D277/30 ,  C07D285/08 ,  C07D285/12 ,  C07D405/12

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.

公开(公告)号：US09758489B2

公开(公告)日：2017-09-12

申请号：US14801126

申请日：2015-07-16

Applicant: Novira Therapeutics, Inc.

Inventor： George D. Hartman

IPC: A61K31/55 ,  A61K31/435 ,  C07D223/00 ,  C07D213/00 ,  C07D243/08 ,  C07D401/04 ,  A61K31/551 ,  C07D471/08 ,  A61K31/439 ,  A61K31/5513 ,  A61K45/06 ,  C07D487/08 ,  A61K38/21 ,  A61K39/29 ,  C07D401/14

CPC classification number: C07D243/08 ,  A61K31/439 ,  A61K31/55 ,  A61K31/551 ,  A61K31/5513 ,  A61K38/21 ,  A61K39/292 ,  A61K45/06 ,  C07D401/04 ,  C07D401/14 ,  C07D471/08 ,  C07D487/08 ,  A61K2300/00

Abstract: Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.

公开(公告)号：US20170253568A1

公开(公告)日：2017-09-07

申请号：US15059232

申请日：2016-03-02

Applicant: Lawrence Livermore National Security, LLC

Inventor： Carlos Valdez ,  Edmond Y. Lau ,  Brian P. Mayer

IPC: C07D249/06 ,  A01N25/32 ,  B01J31/06 ,  B01J31/18 ,  B01J31/02

CPC classification number: C07D249/06 ,  A01N25/32 ,  B01J31/0237 ,  B01J31/06 ,  B01J31/182 ,  B01J2531/16 ,  B01J2531/26 ,  B01J2531/842 ,  B01J2531/845 ,  B01J2531/847 ,  C07D243/08 ,  C07D249/04 ,  A01N43/647 ,  A01N59/16

Abstract: Novel compositions of matter based on homopiperazine precursor materials and forming a homopiperazine-based ligand are disclosed, along with suitable techniques and materials for the synthesis and utilization thereof. In particular various synthetic schemes and techniques for applying the disclosed compositions of matter as a decontaminating agent. The decontaminating agents include homopiperazine-based ligand-metal complexes that are particularly effective at neutralizing toxicity of nerve agents, pesticides, and other toxic organophosphorus-based compounds. In preferred approaches, the homopiperazine-based ligand-metal complexes act as catalysts to facilitate substitution of a leaving group of the organophosphorus-based compound with a functional group that does not permit the organophosphorus-based compound to inactivate acetylcholinesterase upon introduction of the organophosphorus-based compound to a living organism such as insects and mammals. Advantageously, the catalytic homopiperazine-based ligand-metal complexes are formed using inexpensive, readily-available precursor materials, and may be utilized to neutralize toxins without relying on damaging caustic reactants or environmentally unfriendly organic solvents.

公开(公告)号：US20170217947A1

公开(公告)日：2017-08-03

申请号：US15501295

申请日：2015-08-04

Applicant: Sandoz AG

Inventor： Roland Barth ,  Kathrin Höferl-Prantz ,  Frank Richter ,  Gerhard Schwenter

IPC: C07D413/14 ,  C07D249/06 ,  C07D403/10 ,  C07D243/08

CPC classification number: C07D413/14 ,  C07C269/04 ,  C07C269/06 ,  C07D243/08 ,  C07D249/06 ,  C07D403/06 ,  C07D403/10 ,  C07C271/22 ,  C07C271/20

Abstract: The present invention relates to a process for the preparation of a compound of formula (A), Further, the present invention relates to the respective compound (A) as such and to its use in the preparation of antifungal agent.