公开(公告)号：US20240190930A1

公开(公告)日：2024-06-13

申请号：US18541907

申请日：2023-12-15

申请人： NEW YORK UNIVERSITY

发明人： Paramjit S. ARORA ,  Michael G. WUO

IPC分类号： C07K14/47 ,  A61K38/00 ,  A61K45/06 ,  A61K47/65 ,  A61P35/00 ,  C07C49/04 ,  C07D227/02 ,  C07D255/02 ,  C07D333/02 ,  C07K7/02 ,  C07K7/08

CPC分类号： C07K14/4702 ,  A61K47/65 ,  A61P35/00 ,  C07C49/04 ,  C07D227/02 ,  C07D255/02 ,  C07D333/02 ,  C07K7/02 ,  C07K7/08 ,  A61K38/00 ,  A61K45/06

摘要： This invention relates to macrostructures (and pharmaceutical formulations containing them) that include a parallel coiled-coil structure, wherein the parallel coiled-coil comprises a first coil of Formula I and a second coil of Formula II:


T1-f0-g0-a1-b1-c1-d1-e1-f1-g1-a2-b2-C2-d2-e2-f2-g2-a3-b3-c3-d3-e3-T2  (I)



T3-g′0-a′1-b′1-c′1-d′1-e′1-f′1-g′1-a′2-b′2-c′2-d′2-f′2-g′2-a′3-b′3-c′3-d′3-f′3-T4  (II),

as described in the present application. Methods of using these macrostructures are also disclosed.

公开(公告)号：US20190300961A1

公开(公告)日：2019-10-03

申请号：US15944725

申请日：2018-04-03

申请人： GUIZHOU MEDICAL UNIVERSITY ,  MATERNAL AND CHILD HEALTH HOSPITAL OF GUIYANG CITY ,  GUIZHOU ENTRY-EXIT INSPECTION AND QUARANTINE BUREAU

发明人： WENFENG YU ,  SHI ZHOU ,  ZHI HUANG ,  BI WANG ,  RUI GAO ,  DAI WEI ZHAO ,  HAI ZHUANG ,  YA LING LIANG

IPC分类号： C12Q1/6886 ,  C12Q1/6869 ,  C12Q1/686 ,  C07D227/02

摘要： A kit for determining ctDNA concentration and a method for determining ctDNA concentration is disclosed, wherein the method comprising dissolving extracted ctDNA in Tris-HCl buffer with pH>7.0 and adding into the buffer 2,7-bis(1-methyl-4-vinylpyridine)-9-ethylcarbazole iodised salt as a molecular probe, calculating the concentration of ctDNA in the solution by measuring the Fluorescence intensity of the solution. It has extremely high sensitivity in the determination of 0 μg/ml˜50 μg/ml ctDNA solution.

公开(公告)号：US08003792B2

公开(公告)日：2011-08-23

申请号：US11662703

申请日：2005-09-09

申请人： Ian M. Bell ,  Cory R. Theberge ,  Craig A. Stump ,  Xufang Zhang ,  Steven N. Gallicchio ,  C. Blair Zartman

发明人： Ian M. Bell ,  Cory R. Theberge ,  Craig A. Stump ,  Xufang Zhang ,  Steven N. Gallicchio ,  C. Blair Zartman

IPC分类号： A61K31/40 ,  A61K31/438 ,  C07D401/04 ,  C07D227/02

CPC分类号： C07D401/14 ,  C07D403/12 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D519/00 ,  Y02P20/582

摘要： The present invention is directed to compounds of Formula I: (where variables A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

摘要翻译： 本发明涉及式I化合物（其中变量A1，A2，B，J，K，m，n，R4，R5a，R5b和R5c如本文所定义）可用作CGRP受体的拮抗剂，并且可用于 治疗或预防CGRP涉及的疾病，如头痛，偏头痛和丛集性头痛。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及CGRP的疾病中的用途。

公开(公告)号：US5688945A

公开(公告)日：1997-11-18

申请号：US770488

申请日：1996-12-20

申请人： Susanna Karin Maria Bjork ,  Birgitta Kristina Gotthammar ,  Mats Torbjorn Linderberg ,  Johan Per Luthman ,  Kerstin Margareta Irma Persson ,  Robert Schwarcz

发明人： Susanna Karin Maria Bjork ,  Birgitta Kristina Gotthammar ,  Mats Torbjorn Linderberg ,  Johan Per Luthman ,  Kerstin Margareta Irma Persson ,  Robert Schwarcz

IPC分类号： C07D333/04 ,  A61K31/195 ,  A61K31/196 ,  A61K31/275 ,  A61K31/34 ,  A61K31/341 ,  A61K31/38 ,  A61K31/381 ,  A61P9/10 ,  A61P25/00 ,  A61P43/00 ,  C07C205/26 ,  C07C205/37 ,  C07C205/59 ,  C07C227/04 ,  C07C227/16 ,  C07C227/18 ,  C07C229/64 ,  C07C229/70 ,  C07C253/30 ,  C07C255/57 ,  C07C255/59 ,  C07C315/04 ,  C07C317/46 ,  C07C317/48 ,  C07C319/20 ,  C07C323/62 ,  C07C323/63 ,  C07D307/34 ,  C07F7/12 ,  C07D227/02 ,  C07C315/00 ,  C07C317/00

CPC分类号： C07C205/59 ,  C07C205/26 ,  C07C205/37 ,  C07C229/64 ,  C07C229/70 ,  C07C255/59 ,  C07C2102/10

摘要： The present invention relates to novel derivatives of 3-hydroxyanthranilic acid, 3-HANA, of the general formula I ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and selected from H and alkyl; X is selected from alkylthio, arylthio, aryloxy, halogen and cyano; R.sup.3, R.sup.4 are the same or different and selected from halogen, methyl, fluoroalkyl, cyano and Z--R.sup.5 wherein Z is selected from CH.sub.n, NH.sub.m, O, S, SO.sub.2 and CO wherein n=1 or 2; m=0 or 1 and R.sup.5 is selected from alkyl, aryl and fluoroalkyl; or R.sup.3 and R.sup.4 together form a saturated or unsaturated ring system Y--V--Z wherein Y and Z, independently of each other, are as defined for Z above and V is selected from C.sub.1 -C.sub.3 alkylene or alkenylene, --N.dbd., --N.dbd.N-- and ##STR2## wherein R.sub.7 =H or alkyl; or a pharmaceutically acceptable salt thereof, methods and intermediates for their preparation, novel pharmaceutical compositions and the use thereof for inhibiting the enzyme 3-hydroxy-anthranilate oxygenase, 3-HAO, responsible for the production of the endogenous neurotoxin quinolinic acid, QUIN.

摘要翻译： 本发明涉及通式Ⅰ的3-羟基邻氨基苯甲酸的新型衍生物，3-HANA，其中R 1和R 2相同或不同并且选自H和烷基; X选自烷硫基，芳硫基，芳氧基，卤素和氰基; R 3，R 4相同或不同，选自卤素，甲基，氟烷基，氰基和Z-R 5，其中Z选自CH n，NH m，O，S，SO 2和CO，其中n = 1或2; m = 0或1，R 5选自烷基，芳基和氟烷基; 或R3和R4一起形成饱和或不饱和的环系YVZ，其中Y和Z彼此独立地如上述Z所定义，V选自C 1 -C 3亚烷基或亚烯基-N =，-N = N- 和＆lt; IMAGE＆gt;其中R7 = H或烷基; 或其药学上可接受的盐，其制备方法和中间体，新型药物组合物及其用于抑制负责产生内源性神经毒素喹啉酸QUIN的3-羟基 - 邻氨基苯甲酸加氧酶3-HAO的用途。

公开(公告)号：US3936467A

公开(公告)日：1976-02-03

申请号：US454643

申请日：1974-03-25

申请人： Richard William James Carney ,  George DE Stevens

发明人： Richard William James Carney ,  George DE Stevens

IPC分类号： C07D207/20 ,  C07D207/26 ,  C07D207/27 ,  C07D207/40 ,  C07D207/404 ,  C07D207/44 ,  C07D207/448 ,  C07D209/44 ,  C07D209/46 ,  C07D209/48 ,  C07D211/40 ,  C07D217/24 ,  C07D227/02 ,  C07D295/18

CPC分类号： C07D207/27 ,  C07C255/00 ,  C07D207/20 ,  C07D207/404 ,  C07D207/448 ,  C07D209/44 ,  C07D209/46 ,  C07D209/48 ,  C07D217/24 ,  C07D295/18 ,  Y10S514/825

摘要： New .alpha.-(cyclic tert. aminophenyl)-aliphatic acids, e.g. those of the formula ##SPC1##R.sub.1 = h or alkylR.sub.2 = h, alk(en)yl, cycloalk(en)- yl or cycloalk(en)yl-alkylA = hydroxylated lower alkyleneAnd functional derivatives thereof, are anti-inflammatory agents.

摘要翻译： 新的α-（环状叔氨基苯基） - 脂族酸，例如 式R1 = H或烷基R2 = H，烷（烯）基，环烯（en） - 基或环烷基（烯）基 - 烷基A =羟基化低级亚烷基及其功能衍生物，为抗炎剂。

公开(公告)号：US11891422B2

公开(公告)日：2024-02-06

申请号：US16684082

申请日：2019-11-14

申请人： NEW YORK UNIVERSITY

发明人： Paramjit S. Arora ,  Michael G. Wuo

IPC分类号： A61P35/00 ,  C07K7/02 ,  C07K7/08 ,  C07D255/02 ,  C07D227/02 ,  C07D333/02 ,  A61K45/06 ,  A61K38/00 ,  C07C49/04 ,  C07K14/47 ,  A61K47/65 ,  C07K14/01

CPC分类号： C07K14/4702 ,  A61K47/65 ,  A61P35/00 ,  C07C49/04 ,  C07D227/02 ,  C07D255/02 ,  C07D333/02 ,  C07K7/02 ,  C07K7/08 ,  A61K38/00 ,  A61K45/06

摘要： This invention relates to macrostructures (and pharmaceutical formulations containing them) that include a parallel coiled-coil structure, wherein the parallel coiled-coil comprises a first coil of Formula I and a second coil of Formula II:

T1-f0-g0-a1-b1-c1-d1-e1-f1-g1-a2-b2-c2-d2-e2-f2-g2-a3-b3-c3-d3-e3-T2  (I)

T3-g′0-a′1-b′1-c′1-d′1-e′1-f′1-g′1-a′2-b′2-c′2-d′2-e′2-f′2-g′2-a′3-b′3-c′3-d′3-e′3-f′3-T4  (II),

as described in the present application. Methods of using these macrostructures are also disclosed.

公开(公告)号：US20220289802A1

公开(公告)日：2022-09-15

申请号：US17723921

申请日：2022-04-19

申请人： NEW YORK UNIVERSITY ,  CORNELL UNIVERSITY

发明人： Paramjit S. ARORA ,  Ethel CESARMAN ,  Michael G. WUO ,  Jouliana SADEK

IPC分类号： C07K14/47 ,  A61K47/65 ,  A61P35/00 ,  C07K7/02 ,  C07K7/08 ,  C07D255/02 ,  C07D227/02 ,  C07D333/02 ,  C07C49/04

摘要： This invention relates to macrostructures (and pharmaceutical formulations containing them) that include a parallel coiled-coil structure, wherein the parallel coiled-coil comprises a first coil of Formula I and a second coil of Formula II: T1-f0-g0-a1-b1-c1-d1-e1-f1-g1-a2-b2-c2-d2-e2-f2-g2-a3-b3-c3-d3-e3-T2  (I) T3-g′0-a′1-b′1-c′1-d′1-e′1-f′1-g′1-a′2-b′2-c′2-d′2-e′2-f′2-g′2-a′3-b′3-c′3-d′3-e′3-f′3-T4  (II), as described in the present application. Methods of using these macrostructures are also disclosed.

公开(公告)号：US09856232B1

公开(公告)日：2018-01-02

申请号：US15628476

申请日：2017-06-20

申请人： KING SAUD UNIVERSITY

发明人： Mashooq Ahmad Bhat ,  Mohamed Abdulrahman Al-Omar

IPC分类号： C07D401/02 ,  C07D239/10 ,  C07D273/02 ,  C07D227/02 ,  C07D221/00 ,  A61K31/505

CPC分类号： C07D401/02 ,  A61K31/505 ,  C07D221/00 ,  C07D227/02 ,  C07D239/10 ,  C07D273/02

摘要： A dihydropyrimidinone derivative includes a compound having a chemical structure according to Formula 1: wherein Z is selected from CH2O, O, and N; X is selected from O and S; and R represents aryl, substituted aryl, heteroaryl, or substituted heteroaryl, wherein the substituted aryl or substituted heteroaryl have one or more substituents selected from the group consisting of halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, nitro, hydroxyl, alkylthio, alkylamino, heteroaryl, aryloxy, haloaryloxy, arylthio, arylamino, and pharmaceutically acceptable salts thereof. The present subject matter also relates to a method of making a dihydropyrimidinone derivative, a method of treating a gastrointestinal disease, a method of treating an ulcer, a pharmaceutical composition, and a method of making a pharmaceutical composition.

公开(公告)号：US20070225331A1

公开(公告)日：2007-09-27

申请号：US11803670

申请日：2007-05-14

申请人： Michael Hoemann

发明人： Michael Hoemann

IPC分类号： A61K31/445 ,  C07D227/02

CPC分类号： C07D211/26 ,  C07D211/22

摘要： One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, analgesia, schizophrenia, Parkinson's disease, restless leg syndrome, sleeping disorders, attention deficit hyperactivity disorder, irritable bowel syndrome, premature ejaculation, menstrual dysphoria syndrome, urinary incontinence, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.

公开(公告)号：US5849755A

公开(公告)日：1998-12-15

申请号：US969794

申请日：1997-11-13

申请人： Heinrich Christian Englert ,  Uwe Gerlach ,  Dieter Mania ,  Wolfgang Linz ,  Heinz Gogelein ,  Erik Klaus

发明人： Heinrich Christian Englert ,  Uwe Gerlach ,  Dieter Mania ,  Wolfgang Linz ,  Heinz Gogelein ,  Erik Klaus

IPC分类号： C07D311/04 ,  A61K31/35 ,  A61K31/352 ,  A61K31/353 ,  A61K31/355 ,  A61K31/40 ,  A61K31/4025 ,  A61P9/00 ,  A61P9/06 ,  C07D207/26 ,  C07D209/34 ,  C07D211/76 ,  C07D217/24 ,  C07D227/02 ,  C07D311/16 ,  C07D311/18 ,  C07D311/42 ,  C07D311/58 ,  C07D311/70 ,  C07D405/12

CPC分类号： C07D405/12 ,  C07D311/58 ,  C07D311/70

摘要： 3-amidochromanylsulfonyl(thio)ureas of the formula (I): ##STR1## which are valuable pharmaceutically active compounds for the treatment of disturbances of the cardiovascular system, in particular for the treatment of arrhythmias, for preventing sudden cardiac death or for influencing a reduced contractility of the heart, and processes for their preparation, their use and pharmaceutical preparations comprising them.

摘要翻译： 式（I）的3-酰氨基苯并二氢吡喃基磺酰基（硫代）脲：作为治疗心血管系统紊乱的有价值的药物活性化合物，特别是用于治疗心律不齐的有用的药物活性化合物，用于预防心源性猝死或 用于影响心脏收缩力的降低，及其制备方法及其用途以及包含它们的药物制剂。