公开(公告)号：US06262030B1

公开(公告)日：2001-07-17

申请号：US09432500

申请日：1999-11-02

Applicant: Yong-Jin Wu ,  Wei-Guo Su

Inventor： Yong-Jin Wu ,  Wei-Guo Su

IPC: C07H1708

CPC classification number: C07H17/08

Abstract: The invention relates to the compounds of the formula 1 and to pharmaceutically acceptable salts thereof, wherein R1, R2, R3, X and Y are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formula 1, methods of using said compounds of formula 1 in the treatment of infections, and methods of preparing said the compounds of formula 1.

Abstract translation: 本发明涉及式1的化合物及其药学上可接受的盐，其中R 1，R 2，R 3，X和Y如本文所定义。 本发明还涉及含有式1化合物的药物组合物，使用式1化合物治疗感染的方法，以及制备所述式1化合物的方法。

公开(公告)号：US06777543B2

公开(公告)日：2004-08-17

申请号：US10441347

申请日：2003-05-19

Applicant: Yong-Jin Wu ,  Wei-Guo Su ,  Takushi Kaneko ,  Hamish McArthur

Inventor： Yong-Jin Wu ,  Wei-Guo Su ,  Takushi Kaneko ,  Hamish McArthur

IPC: C07H1708

CPC classification number: C07H17/08

Abstract: The invention relates to compounds of the formula and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1, R2, R3, R4, R5, R17, Rf, A, X, and Y are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formulas 1, methods of using the compounds of formula 1 in the treatment of infections and methods of preparing the compounds of formula 1.

Abstract translation: 本发明涉及下式的化合物及其药学上可接受的盐，前药和溶剂化物，其中R 1，R 2，R 3，R 4，R 5，R 17，R A，X和Y如本文所定义。 本发明还涉及含有式1化合物，使用式1化合物治疗感染的方法和制备式1化合物的方法的药物组合物。

公开(公告)号：US06420343B1

公开(公告)日：2002-07-16

申请号：US09399497

申请日：1999-09-20

Applicant: Wei-Guo Su ,  Takushi Kaneko ,  Yong-Jin Wu

Inventor： Wei-Guo Su ,  Takushi Kaneko ,  Yong-Jin Wu

IPC: A61K3170

CPC classification number: C07H17/08

Abstract: This invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, prodrugs and solvates thereof wherein X1, X2, R2 and R6 are as defined herein. The compounds of formula 1 are antibacterial and antiprotozoal agents that may be used to treat various bacterial and protozoal infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of treating bacterial and protozoal infections by administering the compounds of formula 1.

Abstract translation: 本发明涉及式1的化合物及其药学上可接受的盐，前药和溶剂合物，其中X 1，X 2，R 2和R 6如本文所定义。 式1的化合物是可用于治疗各种细菌和原生动物感染的抗细菌剂和抗原虫药，以及与这种感染有关的疾病。 本发明还涉及含有式1化合物的药物组合物和通过施用式1化合物来治疗细菌和原生动物感染的方法。

公开(公告)号：US06300316B1

公开(公告)日：2001-10-09

申请号：US09378886

申请日：1999-08-23

Applicant: Katherine E. Brighty ,  Takushi Kaneko ,  Robert G. Linde, II ,  Hiroko Masamune ,  Paul R. McGuirk ,  Wei-Guo Su ,  Yong-Jin Wu ,  Bingwei V. Yang

Inventor： Katherine E. Brighty ,  Takushi Kaneko ,  Robert G. Linde, II ,  Hiroko Masamune ,  Paul R. McGuirk ,  Wei-Guo Su ,  Yong-Jin Wu ,  Bingwei V. Yang

IPC: A61K3170

CPC classification number: C07D405/14 ,  C07D407/14 ,  C07D417/14 ,  C07D491/04 ,  C07D493/04 ,  C07H17/08

Abstract: This invention relates to compounds of the formula and to pharmaceutically acceptable salts thereof. The compounds of formula 1 are potent antibacterial and antiprotozoal agents that may be used to treat various bacterial and protozoal infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of treating bacterial and protozoal infections by administering the compounds of formula 1.

Abstract translation: 本发明涉及式的化合物及其药学上可接受的盐。 式1的化合物是可用于治疗与这种感染相关的各种细菌和原生动物感染和疾病的有效的抗细菌和抗原虫药。 本发明还涉及含有式1化合物的药物组合物和通过施用式1化合物来治疗细菌和原生动物感染的方法。

公开(公告)号：US06664238B1

公开(公告)日：2003-12-16

申请号：US09459116

申请日：1999-12-10

Applicant: Wei-Guo Su ,  Takushi Kaneko ,  Yong-Jin Wu

Inventor： Wei-Guo Su ,  Takushi Kaneko ,  Yong-Jin Wu

IPC: A61K3170

CPC classification number: C07H17/08

Abstract: This invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts and solvates thereof wherein X1, X2, R2, R15, R16 and R6 are as defined herein. The compounds of formula 1 are antibacterial and antiprotozoal agents that may be used to treat various bacterial and protozoal infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of treating bacterial and protozoal infections by administering the compounds of formula 1.

Abstract translation: 本发明涉及式1的化合物及其药学上可接受的盐和溶剂化物，其中X 1，X 2，R 2，R 15，R 16和R 6如本文所定义 。 式1的化合物是可用于治疗各种细菌和原生动物感染的抗细菌剂和抗原虫药，以及与这种感染有关的疾病。 本发明还涉及含有式1化合物的药物组合物和通过施用式1化合物来治疗细菌和原生动物感染的方法。

公开(公告)号：US06258785B1

公开(公告)日：2001-07-10

申请号：US09449136

申请日：1999-11-24

Applicant: Wei-Guo Su ,  Takushi Kaneko ,  Yong-Jin Wu ,  Daniel J. Durkin ,  Kathleen T. Smyth

Inventor： Wei-Guo Su ,  Takushi Kaneko ,  Yong-Jin Wu ,  Daniel J. Durkin ,  Kathleen T. Smyth

IPC: A61K3170

CPC classification number: C07H17/08

Abstract: The invention relates to crystalline 9-E-(O-methyl)oxime of 11,12-dideoxy-3-de(2,6-dideoxy-3-C-methyl-3-O-methyl-&agr;-L-ribohexopyranosyloxy)-6-O-methyl-12,11-(iminocarbonyl-(2-(3-(4-(3-pyridinyl)-1H-imidazol-1-yl)propyl)hydrazono))-3-oxoerythromycin wherein said crystalline compound is as the free base of said compound, the hemihydrate of said compound or the mesylate (methanesufonic acid) salt of said compound. The invention also relates to pharmaceutical compositions containing the foregoing crystalline compound and to methods of treating bacterial and protozoa infections by administering said crystalline compound.

Abstract translation: 本发明涉及11,12-二脱氧-3-脱（2,6-二脱氧-3-C-甲基-3-O-甲基-α-L-核糖六吡喃糖基氧基）的结晶9-E-（O-甲基）肟， -6-O-甲基-12,11-（亚氨基羰基 - （2-（3-（4-（3-吡啶基）-1H-咪唑-1-基）丙基）亚肼基））-3-氧代红霉素，其中所述结晶化合物 是所述化合物的游离碱，所述化合物的半水合物或所述化合物的甲磺酸盐（甲磺酸）盐。 本发明还涉及含有上述结晶化合物的药物组合物和通过施用所述结晶化合物治疗细菌和原生动物感染的方法。

公开(公告)号：US08604024B2

公开(公告)日：2013-12-10

申请号：US13477143

申请日：2012-05-22

Applicant: Lorin A. Thompson, III ,  Jianliang Shi ,  Yong-Jin Wu ,  Lawrence R. Marcin ,  Ramkumar Rajamani ,  Mendi A. Higgins

Inventor： Lorin A. Thompson, III ,  Jianliang Shi ,  Yong-Jin Wu ,  Lawrence R. Marcin ,  Ramkumar Rajamani ,  Mendi A. Higgins

IPC: C07D279/08 ,  C07D513/04 ,  C07D417/10

CPC classification number: C07D279/08 ,  C07D417/04 ,  C07D417/10 ,  C07D417/12 ,  C07D513/04

Abstract: Compounds of formula (I), including pharmaceutically acceptable salts thereof, are set forth herein: wherein X is selected from the group of CH2, O, and NR2; m=0 or 1; R1 at each instance is selected from the group of halogen, hydroxy, amino, C1-4alkylamino, C1-4dialkylamino, haloC1-4 alkyl, CN, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, and C2-C4 alkynyl; L is a bond, —NHCO—, —NH—, or L and Z together can be absent; Z is a C6-C10-aryl group or a 5-10 membered heterocyclic group which can be further substituted with from 0-3 substituents selected from the group of halogen, haloC1-4 alkoxy, 4-methoxyphenyl, hydroxy, amino, C1-4alkylamino, C1-4dialkylamino, haloC1-4 alkyl, CN, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, and C2-C4 alkynyl; R2 is selected from the group of hydrogen, benzyl, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, acetyl, and methanesulfonyl; and R3, R4 and R5 are independently selected from hydrogen or C1-4alkyl.

Abstract translation: 包括其药学上可接受的盐的式（I）化合物在本文中阐述：其中X选自CH 2，O和NR 2; m = 0或1; 每个实例的R 1选自卤素，羟基，氨基，C 1-4烷基氨基，C 1-4二烷基氨基，卤代C 1-4烷基，CN，C 1 -C 6烷基或环烷基，C 1 -C 6烷氧基和C 2 -C 4炔基; L是键，-NHCO-，-NH-或L和Z可以不存在; Z是可以被0-3个选自卤素，卤代C 1-4烷氧基，4-甲氧基苯基，羟基，氨基，C 1 -C 10 - 芳基的取代基取代的C 6 -C 10 - 芳基或5-10元杂环基， C 1-4烷基氨基，卤代C 1-4烷基，CN，C 1 -C 6烷基或环烷基，C 1 -C 6烷氧基和C 2 -C 4炔基; R 2选自氢，苄基，C 1 -C 6烷基或环烷基，C 1 -C 6烷氧基，乙酰基和甲磺酰基; 并且R 3，R 4和R 5独立地选自氢或C 1-4烷基。

公开(公告)号：US07144881B2

公开(公告)日：2006-12-05

申请号：US10719184

申请日：2003-11-21

Applicant: Yong-Jin Wu ,  Alexandre L'Heureux ,  Li-Qiang Sun

Inventor： Yong-Jin Wu ,  Alexandre L'Heureux ,  Li-Qiang Sun

IPC: A61K31/535 ,  C07D265/30 ,  C07D211/72 ,  C07D307/78 ,  C07C239/00

CPC classification number: C07C233/60 ,  A61K31/192 ,  A61K31/343 ,  A61K31/40 ,  A61K31/44 ,  A61K31/4406 ,  A61K31/5375 ,  C07C233/58 ,  C07C233/59 ,  C07C2601/02 ,  C07D207/14 ,  C07D213/40 ,  C07D213/61 ,  C07D295/135 ,  C07D307/81

Abstract: The present invention provides novel arylcyclopropylcarboxylic amides and related derivatives having the general Formula I wherein R, R1, R2, R3, R4, R5, R6 and R7 are as defined in the specification, or a nontoxic pharmaceutically acceptable salt, solvate or hydrate thereof which are openers or activators of KCNQ potassium channels. The present invention also provides pharmaceutical compositions comprising said arylcyclopropylcarboxylic amides and to the method of treatment of disorders sensitive to KCNQ potassium channel opening activity such as migraine or a migraine attack, bipolar disorders, epilepsy, acute and chronic pain and anxiety.

Abstract translation: 本发明提供新的芳基环丙基羧酰胺和具有通式I的相关衍生物，其中R 1，R 2，R 2，R 3，R 3， R 4，R 5，R 6和R 7如说明书中所定义，或无毒的药学上可接受的盐 ，其为KCNQ钾通道的开放剂或活化剂的溶剂化物或水合物。 本发明还提供包含所述芳基环丙基羧酰胺的药物组合物和治疗对KCNQ钾通道开放活性敏感的疾病如偏头痛或偏头痛发作，双相情感障碍，癫痫，急性和慢性疼痛和焦虑症的方法。

公开(公告)号：US06933308B2

公开(公告)日：2005-08-23

申请号：US10730781

申请日：2003-12-09

Applicant: Kenneth M. Boy ,  Yong-Jin Wu

Inventor： Kenneth M. Boy ,  Yong-Jin Wu

IPC: A61P25/06 ,  A61P25/08 ,  A61P25/18 ,  A61P25/22 ,  C07D277/56 ,  C07D417/12 ,  C07D417/14 ,  C07D277/20 ,  A61K31/427 ,  C07D213/02 ,  C07D295/02

CPC classification number: C07D417/12 ,  C07D277/56 ,  C07D417/14

Abstract: Novel aminoalkylthiazole derivatives of Formula I are described which are openers of KCNQ potassium channels and are useful in the treatment of disorders responsive to the opening of the KCNQ potassium channels, including pain and migraine.

Abstract translation: 描述了式I的新型氨基烷基噻唑衍生物，其是KCNQ钾通道的开放剂，并且可用于治疗响应于KCNQ钾通道开放的病症，包括疼痛和偏头痛。

公开(公告)号：US06159945A

公开(公告)日：2000-12-12

申请号：US402338

申请日：1999-10-06

Applicant: Yong-Jin Wu

Inventor： Yong-Jin Wu

IPC: C07H17/08 ,  A61K31/70

CPC classification number: C07H17/08

Abstract: The invention relates to compounds of the formula I ##STR1## and to pharmaceutically acceptable salts thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and X are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formula I, methods of using said compounds of formula I in the treatment of infections, and methods of preparing said compounds of formula I.

Abstract translation: PCT No.PCT / IB98 / 01578第 371 1999年10月6日第 102（e）日期1999年10月6日PCT提交1998年10月9日PCT公布。 WO99 /​​ 21866 PCT出版物 日期1999年5月6日本发明涉及式I化合物及其药学上可接受的盐，其中R1，R2，R3，R4和X如本文所定义。 本发明还涉及含有式I化合物的药物组合物，使用式I化合物治疗感染的方法，以及制备所述式I化合物的方法。