公开(公告)号：US06878704B2

公开(公告)日：2005-04-12

申请号：US10343596

申请日：2001-08-02

Applicant: Steven Aitken ,  Gerald Brooks ,  Steven Dabbs ,  Colin Henry Frydrych ,  Steven Howard ,  Eric Hunt

Inventor： Steven Aitken ,  Gerald Brooks ,  Steven Dabbs ,  Colin Henry Frydrych ,  Steven Howard ,  Eric Hunt

IPC: C07D237/24 ,  A61K31/352 ,  A61K31/366 ,  A61K31/4152 ,  A61K31/4375 ,  A61K31/44 ,  A61K31/4412 ,  A61K31/4427 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/47 ,  A61K31/4965 ,  A61K31/498 ,  A61K31/50 ,  A61K31/501 ,  A61K31/502 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/513 ,  A61K31/519 ,  A61K31/52 ,  A61K31/5377 ,  A61K31/541 ,  A61P17/00 ,  A61P27/16 ,  A61P31/04 ,  C07D213/80 ,  C07D213/89 ,  C07D215/48 ,  C07D215/56 ,  C07D231/22 ,  C07D237/28 ,  C07D239/36 ,  C07D239/46 ,  C07D239/47 ,  C07D239/54 ,  C07D239/557 ,  C07D239/56 ,  C07D241/24 ,  C07D241/26 ,  C07D241/28 ,  C07D309/38 ,  C07D311/22 ,  C07D311/24 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D409/12 ,  C07D417/06 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04 ,  C07D213/02

CPC classification number: C07D213/80 ,  C07D215/48 ,  C07D215/56 ,  C07D231/22 ,  C07D237/28 ,  C07D239/36 ,  C07D239/47 ,  C07D239/557 ,  C07D241/24 ,  C07D241/26 ,  C07D309/38 ,  C07D311/24 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04

Abstract: Pleuromutilin compounds of the formula: are of use in anti-bacterial therapy.

Abstract translation: 具有下列公式的Pleuromutilin化合物：用于抗菌治疗。

公开(公告)号：US20040157849A1

公开(公告)日：2004-08-12

申请号：US10634678

申请日：2003-08-05

Inventor： Chih-Hung Lee ,  Erol K. Bayburt ,  Stanley DiDomenico JR. ,  Irene Drizin ,  Arthur R. Gomtsyan ,  John R. Koenig ,  Richard J. Perner ,  Robert G. Schmidt JR. ,  Sean C. Turner ,  Tammie K. White ,  Guo Zhu Zheng

IPC: A61K031/517 ,  A61K031/496 ,  C07D43/02

CPC classification number: C07D249/08 ,  C07D209/08 ,  C07D217/02 ,  C07D217/22 ,  C07D217/24 ,  C07D217/26 ,  C07D231/12 ,  C07D231/56 ,  C07D233/56 ,  C07D237/28 ,  C07D401/12 ,  C07D405/12

Abstract: Compounds of formula (I) 1 are novel VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence and bladder overactivity.

Abstract translation: 式（I）化合物是可用于治疗疼痛，炎性热痛觉过敏，尿失禁和膀胱过度活动的新型VR1拮抗剂。

公开(公告)号：US20040092521A1

公开(公告)日：2004-05-13

申请号：US10292422

申请日：2002-11-12

Inventor： Robert J. Altenbach ,  Lawrence A. Black ,  Sou-Jen Chang ,  Marlon D. Cowart ,  Ramin Faghih ,  Gregory A. Gfesser ,  Yi-yin Ku ,  Huaqing Liu ,  Kirill A. Lukin ,  Diana L. Nersesian ,  Yu-ming Pu ,  Padam N. Sharma ,  Youssef L. Bennani

IPC: A61K031/53 ,  A61K031/525 ,  A61K031/519 ,  C07D487/02

CPC classification number: C07C255/58 ,  C07D207/08 ,  C07D207/12 ,  C07D207/14 ,  C07D207/20 ,  C07D213/30 ,  C07D213/38 ,  C07D213/61 ,  C07D213/64 ,  C07D213/85 ,  C07D215/12 ,  C07D215/14 ,  C07D215/20 ,  C07D217/14 ,  C07D237/12 ,  C07D237/14 ,  C07D237/28 ,  C07D239/26 ,  C07D239/28 ,  C07D239/42 ,  C07D239/52 ,  C07D241/12 ,  C07D241/42 ,  C07D261/08 ,  C07D263/32 ,  C07D277/28 ,  C07D295/073 ,  C07D295/088 ,  C07D295/096 ,  C07D295/112 ,  C07D295/135 ,  C07D295/155 ,  C07D401/04 ,  C07D401/10 ,  C07D403/04 ,  C07D403/10 ,  C07D405/04 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04 ,  C07D471/04

Abstract: Compounds of formula (I) 1 are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands and methods for using such compounds and compositions.

Abstract translation: 式（I）化合物可用于治疗由组胺-3受体配体预防或改善的病症或病症。 还公开了包含组胺-3受体配体的药物组合物和使用这些化合物和组合物的方法。

公开(公告)号：US06624160B2

公开(公告)日：2003-09-23

申请号：US09808836

申请日：2001-03-15

Applicant: Valerie A. Vaillancourt ,  Scott D. Larsen ,  Sajiv K. Nair

Inventor： Valerie A. Vaillancourt ,  Scott D. Larsen ,  Sajiv K. Nair

IPC: A61K3154

CPC classification number: C07D403/04 ,  C07D237/28 ,  C07D403/06 ,  C07D405/06 ,  C07D405/12 ,  C07D413/06 ,  C07D413/14

Abstract: This invention provides compounds of formula I; which are useful as antiviral agents.

Abstract translation: 本发明提供式I化合物，其可用作抗病毒剂。

公开(公告)号：US20030158198A1

公开(公告)日：2003-08-21

申请号：US10364210

申请日：2003-02-11

Inventor： Chih-Hung Lee ,  Erol K. Bayburt ,  Stanley DiDomenico JR. ,  Irene Drizin ,  Arthur R. Gomtsyan ,  John R. Koenig ,  Richard J. Perner ,  Robert G. Schmidt JR. ,  Sean C. Turner ,  Tammie K. White ,  Guo Zhu Zheng

IPC: C07D455/02 ,  A61K031/53 ,  A61K031/517 ,  A61K031/498 ,  A61K031/496 ,  A61K031/4709

CPC classification number: C07D249/08 ,  C07D209/08 ,  C07D217/02 ,  C07D217/22 ,  C07D217/24 ,  C07D217/26 ,  C07D231/12 ,  C07D231/56 ,  C07D233/56 ,  C07D237/28 ,  C07D401/12 ,  C07D405/12

Abstract: Compound of formula (I) 1 are novel VR1 antagonist that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence and bladder overactivity.

Abstract translation: 式（I）化合物是可用于治疗疼痛，炎性热痛觉过敏，尿失禁和膀胱过度活动的新型VR1拮抗剂。

公开(公告)号：US20030105074A1

公开(公告)日：2003-06-05

申请号：US10281194

申请日：2002-10-28

Applicant: Eisai Co., Ltd.

Inventor： Nobuhisa Watanabe ,  Norio Karibe ,  Kazuki Miyazaki ,  Fumihiro Ozaki ,  Atsushi Kamada ,  Shuhei Miyazawa ,  Yoshimitsu Naoe ,  Toshihiko Kaneko ,  Itaru Tsukada ,  Tadashi Nagakura ,  Hiroki Ishihara ,  Kohtarou Kodama ,  Hideyuki Adachi

IPC: A61K031/55 ,  A61K031/502 ,  C07D43/02

CPC classification number: C07D231/12 ,  C07D233/56 ,  C07D237/28 ,  C07D237/34 ,  C07D249/08 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D409/14 ,  C07D411/14 ,  C07D417/04 ,  C07D417/14 ,  C07D451/06 ,  C07D471/08 ,  C07D491/04 ,  C07D491/08 ,  C07D491/10

Abstract: The present invention provides a phthalazine compound as a therapeutic agent for erectile dysfunction represented by the following formula, a pharmacologically acceptable salt thereof or a hydrate thereof: 1 wherein R1 and R2 are the same as or different from each other and represent a halogen atom, a C1 to C4 alkyl group which may be substituted with a halogen atom, a C1 to C4 alkoxy group which may be substituted with a halogen atom or a cyano group; X represents a cyano group, a nitro group, a halogen atom, a hydroxyimino group which may be substituted or a heteroaryl group which may be substituted; Y represents a heteroaryl group, an aryl group which may be substituted, an alkynyl group which may substituted, an alkenyl group, an alkyl group, an optionally substituted saturated or unsaturated 4- to 8-membered amine ring, and the cyclic amine compound is a monocyclic compound, bicyclic compound or a spiro compound; l is an integer of 1 to 3; provided that the case where l is 1 or 2, X is a cyano group, a nitro group or a chlorine atom, R1 is a chlorine atom, R2 is a methoxy group and Y is a 5- or 6-memberred amine ring substituted with a hydroxyl group is excluded.

Abstract translation: 本发明提供作为下述式表示的勃起功能障碍治疗剂的酞嗪化合物，其药理学上可接受的盐或其水合物：其中R1和R2彼此相同或不同，表示卤素原子， 可以被卤素原子取代的C1〜C4烷基，可被卤素原子或氰基取代的C1〜C4烷氧基; X表示氰基，硝基，卤素原子，可被取代的羟基亚氨基或可被取代的杂芳基; Y表示可以被取代的杂芳基，可以被取代的芳基，可以被取代的炔基，烯基，烷基，任选取代的饱和或不饱和的4-至8-元胺环，环胺化合物是 单环化合物，双环化合物或螺环化合物; l为1〜3的整数， 条件是其中l为1或2的情况，X为氰基，硝基或氯原子，R1为氯原子，R2为甲氧基，Y为被5或6成员取代的胺环 不包括羟基。

公开(公告)号：US06498159B1

公开(公告)日：2002-12-24

申请号：US09508197

申请日：2000-03-08

Applicant: Nobuhisa Watanabe ,  Norio Karibe ,  Kazuki Miyazaki ,  Fumihiro Ozaki ,  Atsushi Kamada ,  Shuhei Miyazawa ,  Yoshimitsu Naoe ,  Toshihiko Kaneko ,  Itaru Tsukada ,  Tadashi Nagakura ,  Hiroki Ishihara ,  Kohtarou Kodama ,  Hideyuki Adachi

Inventor： Nobuhisa Watanabe ,  Norio Karibe ,  Kazuki Miyazaki ,  Fumihiro Ozaki ,  Atsushi Kamada ,  Shuhei Miyazawa ,  Yoshimitsu Naoe ,  Toshihiko Kaneko ,  Itaru Tsukada ,  Tadashi Nagakura ,  Hiroki Ishihara ,  Kohtarou Kodama ,  Hideyuki Adachi

IPC: A61K31502

CPC classification number: C07D231/12 ,  C07D233/56 ,  C07D237/28 ,  C07D237/34 ,  C07D249/08 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D409/14 ,  C07D411/14 ,  C07D417/04 ,  C07D417/14 ,  C07D451/06 ,  C07D471/08 ,  C07D491/04 ,  C07D491/08 ,  C07D491/10

Abstract: The present invention provides a phthalazine compound as a therapeutic agent for erectile dysfunction represented by the following formula, a pharmacologically acceptable salt thereof or a hydrate thereof: wherein R1 and R2 are the same as or different from each other and represent a halogen atom, a C1 to C4 alkyl group which may be substituted with a halogen atom, a C1 to C4 alkoxy group which may be substituted with a halogen atom or a cyano group; X represents a cyano group, a nitro group, a halogen atom, a hydroxyimino group which may be substituted or a heteroaryl group which may be substituted; Y represents a heteroaryl group, an aryl group which may be substituted, an alkynyl group which may substituted, an alkenyl group, an alkyl group, an optionally substituted saturated or unsaturated 4- to 8-membered amine ring, and the cyclic amine compound is a monocyclic compound, bicyclic compound or a spiro compound; l is an integer of 1 to 3; provided that the case where l is 1 or 2, X is a cyano group, a nitro group or a chlorine atom, R1 is a chlorine atom, R2 is a methoxy group and Y is a 5- or 6-membered amine ring substituted with a hydroxyl group is excluded.

Abstract translation: 本发明提供作为下述式表示的勃起功能障碍治疗剂的酞嗪化合物，其药理学上可接受的盐或其水合物：其中R1和R2彼此相同或不同，表示卤素原子， 可以被卤素原子取代的C1〜C4烷基，可被卤素原子或氰基取代的C1〜C4烷氧基; X表示氰基，硝基，卤素原子，可被取代的羟基亚氨基或可被取代的杂芳基; Y表示可以被取代的杂芳基，可以被取代的芳基，可以被取代的炔基，烯基，烷基，任选取代的饱和或不饱和的4-至8-元胺环，环胺化合物是 单环化合物，双环化合物或螺环化合物; l为1〜3的整数， 条件是其中l为1或2的情况，X为氰基，硝基或氯原子，R 1为氯原子，R 2为甲氧基，Y为被5或6元环取代的5-或6-元胺环 不包括羟基。

公开(公告)号：US20020161237A1

公开(公告)日：2002-10-31

申请号：US09754888

申请日：2001-01-05

Inventor： Nader Fotouhi ,  Paul Gillespie ,  Robert William Guthrie ,  Sherrie Lynn Pietranico-Cole ,  Weiya Yun

IPC: C07C235/84 ,  C07C255/50 ,  C07D257/04

CPC classification number: C07D249/08 ,  C07B2200/07 ,  C07C233/85 ,  C07C233/87 ,  C07C311/46 ,  C07D209/08 ,  C07D211/34 ,  C07D213/55 ,  C07D215/14 ,  C07D233/26 ,  C07D235/16 ,  C07D237/28 ,  C07D239/52 ,  C07D249/18 ,  C07D261/08 ,  C07D271/12 ,  C07D277/30 ,  C07D277/38 ,  C07D277/62 ,  C07D277/64 ,  C07D285/14 ,  C07D307/16 ,  C07D317/60 ,  C07D333/24 ,  C07D333/60 ,  C07D401/12 ,  C07D403/12 ,  C07D409/04 ,  C07D417/04 ,  C07F9/4006 ,  C07F9/5728 ,  C07F9/6524 ,  C07F9/65583

Abstract: Compounds of formula 1 and 1-1, 1 wherein R1 is hydrogen, hydroxy, amino or halogen, R2 is hydrogen, hydroxy, or halogen and R3 is hydrogen (Formula 1) or R1 is hydrogen and R2 and R3 taken together with the ethenylene group connecting them form phenyl, pyrrole, pyrroline, oxopyrroline, pyrazole, triazole, or imidazole (Formula 1-1), A is 2 R4 R5 are hydrogen, methyl, ethyl or halogen except that R4 r5 cannot both be hydrogen; and 1) B is hydrogen, or lower alkyl; or 2) B is 3 where R6 R7 R8 and R9 are independently hydrogen, hydroxy, aminosulfonyl, halogen, lower alkoxy, cyano, amino, lower alkyl, lower alkyl amino, or nitro; or 3) B is 4 where R10 is hydrogen, hydroxy, halogen, or lower alkyl and C is a five- or six- membered ring with 0 to 3 heteroatoms which heteroatoms are selected from nitrogen, oxygen, and sulfur, which ring may be unsubstituted or mono- or di- substituted with lower alkyl, cycloalkyl, amino, or substituted amino; 4) B is 5 where X and Y are independently methylene or nitrogen; or 5) B is 6 where at leat one of T, U, V, or W is nitrogen, and any of T, U, V or W which is carbon may be substituted with lower alkyl, lower alkyl amino, lower alkoxy, hydroxy, aminosulfonyl, halogen, cyano, amino, or nitro; or 6) B is 7 where Y is carbon or nitrogen; or 7) B is a five-membered aromatic ring with 1 to 3 heteratoms selected from nitrogen, oxygen, and sulfur which ring may be unsubstituted or mono- or di-substituted with lower alkyl, cycloalky, trifluoroloweralkyl, amino, halogen, substituted amino, or which ring may be fused with a 5 or 6 membered aromatic ring containing 0 to 3 heteroatoms which heteroatoms are selected from nitrogen, oxygen, and sulfur; and pharmaceutically acceptable salts thereof, and related prodrugs, pharmaceutical compositions and methods of treatment, which compounds are useful for treating psoriasis.

公开(公告)号：US06469003B1

公开(公告)日：2002-10-22

申请号：US09762877

申请日：2001-02-14

Applicant: Makoto Gotoh ,  Koji Umimoto ,  Masanobu Onishi ,  Akiyuki Satoh ,  Yoshitami Oshita ,  Masashi Nagamine

Inventor： Makoto Gotoh ,  Koji Umimoto ,  Masanobu Onishi ,  Akiyuki Satoh ,  Yoshitami Oshita ,  Masashi Nagamine

IPC: A61K3150

CPC classification number: C07D401/04 ,  C07D237/14 ,  C07D237/18 ,  C07D237/24 ,  C07D237/28 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D417/04 ,  C07D471/12

Abstract: A pyridazinone derivative represented by formula (I): a pharmaceutically acceptable salt thereof, or a derivative thereof, or a pharmaceutical composition comprising as an active ingredient the derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or diluent.

Abstract translation: 由式（I）表示的哒嗪酮衍生物：其药学上可接受的盐或其衍生物，或包含其衍生物或药学上可接受的盐和药学上可接受的载体或稀释剂作为活性成分的药物组合物。

公开(公告)号：US20020042397A1

公开(公告)日：2002-04-11

申请号：US09808902

申请日：2001-03-15

Inventor： Valerie A. Vaillancourt ,  Scott D. Larsen ,  Sajiv K. Nair

IPC: A61K031/675 ,  C07D413/02 ,  A61K031/5377 ,  A61K031/502

CPC classification number: C07D405/06 ,  C07D237/28 ,  C07D413/06

Abstract: Certain novel 4-hydroxycinnoline-3-carboxyamides. The compounds are particularly effective in the treatment or prevention of viral infections, particularly infections caused by herpes viruses including herpes simplex virus types 1 and 2, human herpes virus types 6, 7 and 8, varicello zoster virus, human cytomegalovirus or Epstein-Barr virus.

Abstract translation: 某些新型4-羟基噌啉-3-羧酰胺。 该化合物特别有效地治疗或预防病毒感染，特别是由疱疹病毒引起的感染，包括1型和2型单纯疱疹病毒，6,7和8型人疱疹病毒，水痘带状疱疹病毒，人巨细胞病毒或爱泼斯坦 - 巴尔病毒 。