公开(公告)号：US20240208916A1

公开(公告)日：2024-06-27

申请号：US18214841

申请日：2023-06-27

Applicant: The Regents of the University of California ,  Amydis, Inc.

Inventor： Jerry Yang ,  Emmanuel A. Theodorakis ,  Stella Sarraf

IPC: C07D295/155 ,  A61B5/00 ,  A61P25/28 ,  C07C255/42 ,  C07C255/58 ,  C07C255/59 ,  C07C311/35 ,  C07D211/06 ,  C07D213/57 ,  C07D213/85 ,  C07D241/04 ,  C07D265/30 ,  C07D295/04 ,  C07D307/52 ,  C07D333/22 ,  C07D401/04 ,  C07D401/14 ,  C07D405/04 ,  C07D405/10 ,  C07D407/10 ,  C07D409/04 ,  C07D409/10 ,  C07D409/14 ,  C07D413/10 ,  C07D413/12 ,  C07H13/04 ,  C07H19/056

CPC classification number: C07D295/155 ,  A61B5/0075 ,  A61P25/28 ,  C07C255/42 ,  C07C255/58 ,  C07C255/59 ,  C07C311/35 ,  C07D211/06 ,  C07D213/57 ,  C07D213/85 ,  C07D241/04 ,  C07D265/30 ,  C07D295/04 ,  C07D307/52 ,  C07D333/22 ,  C07D401/04 ,  C07D401/14 ,  C07D405/04 ,  C07D405/10 ,  C07D407/10 ,  C07D409/04 ,  C07D409/10 ,  C07D409/14 ,  C07D413/10 ,  C07D413/12 ,  C07H13/04 ,  C07H19/056 ,  A61B5/4082 ,  A61B5/4088

Abstract: Provided herein is the design and synthesis of novel molecular rotor fluorophores useful for detection of amyloid or amyloid like proteins. The fluorophores are designed to exhibit enhanced fluorescence emission upon associating with amyloid or amyloid like proteins as compared to unbound compound. Also disclosed herein are methods for treating diseases associated with amyloid or amyloid like proteins.

公开(公告)号：US20220220073A1

公开(公告)日：2022-07-14

申请号：US17638743

申请日：2020-08-24

Applicant: METISA BIOTECHNOLOGY CO., LTD

Inventor： Lixin ZHANG ,  Jing ZHANG ,  Jie WANG ,  Hongyan PEI ,  Zhubo SHENG ,  Zhuo KANG

IPC: C07D213/26 ,  C07D213/82 ,  C07D213/84 ,  C07C255/42 ,  A01N43/40 ,  A01N37/22

Abstract: This disclosure provides a bisamide compound and an application thereof, where the compound has a structure as shown by general formula I: the definition of each substituent in the formula is shown in the specification. The specification also discloses use thereof as an insecticide and an animal parasite control agent.

公开(公告)号：US20210205258A1

公开(公告)日：2021-07-08

申请号：US17205726

申请日：2021-03-18

Applicant: Milestone Pharmaceuticals Inc.

Inventor： Martin P. MAGUIRE

IPC: A61K31/277 ,  A61K9/08 ,  C07C255/42 ,  A61K9/00 ,  A61K47/12 ,  A61K47/18 ,  A61K47/20 ,  A61P9/10 ,  A61P9/06 ,  A61P25/06 ,  A61K47/02 ,  A61K47/10 ,  A61K47/26

Abstract: The present invention includes surprisingly water-soluble salts of a phenylalkylamine compound that are potent antagonists of L-type calcium channels. Aqueous solutions including salts of the instant invention are formulated for nasal administration and provide a novel therapeutic platform for the treatment of stable angina, migraine, and cardiac arrhythmia, such as paroxysmal supraventricular tachycardia.

公开(公告)号：US20190380993A1

公开(公告)日：2019-12-19

申请号：US16555766

申请日：2019-08-29

Applicant: Milestone Pharmaceuticals Inc.

Inventor： Martin P. MAGUIRE ,  Elise RIOUX ,  Harry J. LEIGHTON

IPC: A61K31/277 ,  A61K31/275 ,  C07C255/42 ,  C07C255/43 ,  C07C229/34 ,  C07C229/38 ,  A61K31/216 ,  A61K31/26

Abstract: The present invention relates to the use of a pharmaceutically effective amount of an short-acting calcium channel blocking compound to treat ischemic heart conditions, cardiac arrhythmias, hypertensive crisis in an emergency room setting, hypertension before, during, or after surgery, no-reflow phenomenon following reperfusion, and diseases associated with decreased skeletal muscle blood flow. The invention also relates to pharmaceutical compositions formulated for use in such methods and to kits for such methods.

公开(公告)号：US20190142781A1

公开(公告)日：2019-05-16

申请号：US16246980

申请日：2019-01-14

Applicant: Milestone Pharmaceuticals Inc.

Inventor： Martin P. MAGUIRE ,  Elise RIOUX ,  Harry J. LEIGHTON

IPC: A61K31/277 ,  A61K31/26 ,  A61K31/216 ,  C07C229/38 ,  A61K31/275 ,  C07C255/42 ,  C07C229/34 ,  C07C255/43

Abstract: The present invention relates to the use of a pharmaceutically effective amount of an short-acting calcium channel blocking compound to treat ischemic heart conditions, cardiac arrhythmias, hypertensive crisis in an emergency room setting, hypertension before, during, or after surgery, no-reflow phenomenon following reperfusion, and diseases associated with decreased skeletal muscle blood flow. The invention also relates to pharmaceutical compositions formulated for use in such methods and to kits for such methods.

公开(公告)号：US10196345B2

公开(公告)日：2019-02-05

申请号：US14915474

申请日：2014-08-29

Applicant: The University of British Columbia ,  Centre for Drug Research and Development

Inventor： Edward Ewald Putnins ,  David Scott Grierson ,  Ronan F.B. Gealageas ,  Alice Andree Valentine Devineau ,  Edith Mary Dullaghan

IPC: C07C229/36 ,  C07C255/54 ,  C07D311/16 ,  C07C217/60 ,  C07C229/14 ,  C07C255/42 ,  C07C255/43 ,  C07D213/30 ,  C07C235/74 ,  C07D213/74 ,  C07D231/12 ,  C07D231/14 ,  C07D233/64 ,  C07D233/90 ,  C07D311/12 ,  C07F9/38

Abstract: Described herein are a series of compounds having the structure of Formula I: for use in the inhibition of MAO and uses thereof for the treatment of a barrier disease, obesity, solid epithelial cell tumor metastasis, diabetes, an auto-immune and inflammatory disease or a cardiometabolic disorder.

公开(公告)号：US10117848B2

公开(公告)日：2018-11-06

申请号：US15566122

申请日：2016-04-13

Applicant: Milestone Pharmaceuticals Inc.

Inventor： Martin P. Maguire

IPC: A61K31/277 ,  A61P9/06 ,  A61K47/10 ,  A61K47/26 ,  A61P9/10 ,  A61K47/02 ,  A61P25/06 ,  A61K47/20 ,  A61K47/18 ,  A61K9/00 ,  A61K47/12 ,  C07C255/42 ,  A61K9/08

Abstract: The present invention includes surprisingly water-soluble salts of a phenylalkylamine compound that are potent antagonists of L-type calcium channels. Aqueous solutions including salts of the instant invention are formulated for nasal administration and provide a novel therapeutic platform for the treatment of stable angina, migraine, and cardiac arrhythmia, such as paroxysmal supraventricular tachycardia.

公开(公告)号：US20170320835A1

公开(公告)日：2017-11-09

申请号：US15655570

申请日：2017-07-20

Applicant: Janssen Pharmaceutica NV

Inventor： Jérôme Emile Georges Guillemont ,  Patrice Palandjian ,  Marc René de Jonge ,  Lucien Maria Henricus Koymans ,  Hendrik Maarten Vinkers ,  Frederik Frans Desiré Daeyaert ,  Jan Heeres ,  Koen Jeanne Alfons Van Aken ,  Paulus Joannes Lewi ,  Paul Adriaan Jan Janssen

IPC: C07D239/48 ,  A61K31/505 ,  C07D409/12 ,  C07D405/12 ,  C07D403/12 ,  C07D401/14 ,  C07D401/12 ,  C07D239/47 ,  C07C257/12 ,  C07C255/42 ,  A61K45/06 ,  A61K31/551 ,  A61K31/541 ,  A61K31/5377 ,  A61K31/506 ,  C07D413/12 ,  C07D417/12

CPC classification number: C07D239/48 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  A61K45/06 ,  C07C255/42 ,  C07C257/12 ,  C07D239/47 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

Abstract: This invention concerns HIV replication inhibitors of formula the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein the ring containing -a1=a2-a3=a4- and -b1=b2-b3=b4- represents phenyl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl; n is 0 to 5; m is 1 to 4; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; substituted C1-6alkyl, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonyloxy; substituted C1-6alkyloxyC1-6alkylcarbonyl; R2 is hydroxy, halo, optionally substituted C1-6alkyl, C3-7cycloalkyl, optionally substituted C2-6alkenyl, optionally substituted C2-6alkynyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(═O)pR6, —NH—S(═O)pR6, —C(═O)R6, —NHC(═O)H, —C(═O)NHNH2, —NHC(═O)R6, —C(═NH)R6 or a 5-membered heterocycle; X1 is —NR5—, —NH—NH—, —N═N—, —O—, —C(═O)—, C1-4alkanediyl, —CHOH—, —S—, —S(═O)p—, —X2—C1-4alkanediyl- or —C1-4alkanediyl-X2—; R3 is NHR13; NR13R14; —C(═O)—NHR13; —C(═O)—NR13R14; —C(═O)—R15; —CH═N—NH—C(═O)—R16; substituted C1-6alkyl; optionally substituted C1-6alkyloxyC1-6alkyl; substituted C2-6alkenyl; substituted C2-6alkynyl; C1-6alkyl substituted with hydroxy and a second substituent; —C(═N—O—R8)—C1-4alkyl; R7; or —X3—R7; R4 is halo, hydroxy, C1-6alkyl, C3-7cycloalkyl, C1-6alkyloxy, cyano, nitro, polyhaloC1-6alkyl, polyhaloC1-6alkyloxy, aminocarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonyl, formyl, amino, mono- or di(C1-4alkyl)amino; their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.

公开(公告)号：US20170312242A1

公开(公告)日：2017-11-02

申请号：US15653367

申请日：2017-07-18

Applicant: Milestone Pharmaceuticals Inc.

Inventor： Martin P. MAGUIRE ,  Elise RIOUX ,  Harry J. LEIGHTON

IPC: A61K31/277 ,  C07C255/42 ,  C07C229/34 ,  A61K31/216 ,  A61K31/275 ,  A61K31/26 ,  C07C255/43 ,  C07C229/38

CPC classification number: A61K31/277 ,  A61K31/216 ,  A61K31/26 ,  A61K31/275 ,  C07C229/34 ,  C07C229/38 ,  C07C255/42 ,  C07C255/43

Abstract: The present invention relates to the use of a pharmaceutically effective amount of an short-acting calcium channel blocking compound to treat ischemic heart conditions, cardiac arrhythmias, hypertensive crisis in an emergency room setting, hypertension before, during, or after surgery, no-reflow phenomenon following reperfusion, and diseases associated with decreased skeletal muscle blood flow. The invention also relates to pharmaceutical compositions formulated for use in such methods and to kits for such methods.

公开(公告)号：US09737503B2

公开(公告)日：2017-08-22

申请号：US15262567

申请日：2016-09-12

Applicant: Milestone Pharmaceuticals Inc.

Inventor： Martin P. Maguire ,  Elise Rioux ,  Harry J. Leighton

IPC: A61K31/275 ,  C07C229/00 ,  C07C255/43 ,  A61K31/277 ,  C07C229/34 ,  C07C255/42 ,  C07C229/38 ,  A61K31/216 ,  A61K31/26

CPC classification number: A61K31/277 ,  A61K31/216 ,  A61K31/26 ,  A61K31/275 ,  C07C229/34 ,  C07C229/38 ,  C07C255/42 ,  C07C255/43

Abstract: The present invention relates to the use of a pharmaceutically effective amount of an short-acting calcium channel blocking compound to treat ischemic heart conditions, cardiac arrhythmias, hypertensive crisis in an emergency room setting, hypertension before, during, or after surgery, no-reflow phenomenon following reperfusion, and diseases associated with decreased skeletal muscle blood flow. The invention also relates to pharmaceutical compositions formulated for use in such methods and to kits for such methods.