公开(公告)号：US20080161309A1

公开(公告)日：2008-07-03

申请号：US12034945

申请日：2008-02-21

Applicant: Paul Vincent Fish ,  Malcolm Christian MacKenny ,  Alan Stobie ,  Florian Wakenhut ,  Gavin Alistair Whitlock

Inventor： Paul Vincent Fish ,  Malcolm Christian MacKenny ,  Alan Stobie ,  Florian Wakenhut ,  Gavin Alistair Whitlock

IPC: A61K31/5375 ,  C07D295/00 ,  A61P13/02 ,  A61P15/00 ,  A61P25/22 ,  A61P25/00

CPC classification number: C07D413/06 ,  A61K31/535 ,  C07D265/30 ,  C07D413/12

Abstract: The present invention provides compounds of Formula I wherein R1, R2, R3, and n have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of conditions including urinary disorders, pain, premature ejaculation, ADHD and fibromyalgia. Also provided are pharmaceutical compositions comprising one or more compounds of Formula I.

Abstract translation: 本发明提供式I化合物，其中R 1，R 2，R 3，和n具有在本说明书中定义的任何值 和其药学上可接受的盐，其可用作治疗包括尿失禁，疼痛，早泄，ADHD和纤维肌痛等症状的药剂。 还提供了包含一种或多种式I化合物的药物组合物。

公开(公告)号：US20070105870A1

公开(公告)日：2007-05-10

申请号：US10586029

申请日：2005-01-03

Applicant: Gerwyn Bish ,  Alan Brown ,  Paul Fish ,  Michael Fray ,  Alan Stobie ,  Florian Wakenhut ,  Gavin Whitlock

Inventor： Gerwyn Bish ,  Alan Brown ,  Paul Fish ,  Michael Fray ,  Alan Stobie ,  Florian Wakenhut ,  Gavin Whitlock

IPC: A61K31/495 ,  C07D241/04

CPC classification number: C07D295/205 ,  C07D249/18 ,  C07D295/073 ,  C07D295/096

Abstract: A compound of formula (I), wherein R1 is H; R2 is aryl, het, C3-8cycloalkyl, C1-6alkyl, (CH2)2aryl or R4, wherein each of the cycloalkyl, aryl, het and R4 groups is optionally substituted by at least one substituent independently selected from C1-6alkyl, C1-6alkoxy, OH, halo, CF3, OCF3, OCHF2, O(CH2)yCF3, CN, CONH2, CON(H)C1-6alkyl, CON(C1-6alkyl)2, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl, C1-4alkoxy-C1-4alkoxy, SCF3, C1-6alkyISO2, C1-4alkyl-S-C1-4alkyl, C1-4alkyl-S—, C1-4alkyINR10R11 and NR10R11; or R1 and R2, together with the carbon atom to which they are bound, form a 5- or 6-membered carbocycle or a 5- or 6-membered heterocycle containing at least one N, O or S heteroatom; R3 is aryl, het or R4, each optionally substituted by at least one substituent independently selected from C1-6-alkyl, C1-6-alkoxy, het, OH, halo, CF3, OCF3, OCHF2, O(CH2)yCF3, CN, CONH2, CON(H)C1-6alkyl, CON(C1-6alkyl)2, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl, C1-4alkoxy-C1-4alkoxy, SCF3, C1-6alkyISO2, C1-4alkyl-S-C1-4alkyl, C1-4alkyl-S—, C1-4alkylNR10R11and NR10R11; R4 is a phenyl group fused to a 5- or 6 membered carbocycle, or a phenyl group fused to a 5- or 6-membered heterocycle containing at least one N, O or S heteroatom; R5 is H or C1-6alkyl; R10 and R11 are the same or different and are independently H or C1-4alkyl; A is a C1-3alkylene chain which is optionally substituted by OH, C1-4alkyl or C1-4alkoxy; x is an integer from 1 to 3; y is 1 or 2; z is an integer from 1 to 3; aryl is phenyl, naphthyl, anthracyl or phenanthryl; and het is an aromatic or non-aromatic 4, 5- or 6-membered heterocycle which contains at least one N, O or S heteroatom, optionally fused to a 5- or 6-membered carbocycle or a second 4, 5- or 6-membered heterocycle which contains at least one N, O or S heteroatom.

公开(公告)号：US07119088B2

公开(公告)日：2006-10-10

申请号：US10782285

申请日：2004-02-18

Applicant: Justin Stephen Bryans ,  Patrick Stephen Johnson ,  Thomas Ryckmans ,  Alan Stobie

Inventor： Justin Stephen Bryans ,  Patrick Stephen Johnson ,  Thomas Ryckmans ,  Alan Stobie

IPC: A61K31/5517 ,  C07D487/14 ,  C07D498/14 ,  C07D513/14

CPC classification number: C07D401/04 ,  C07D413/14 ,  C07D487/04 ,  C07D513/04

Abstract: A compound of formula (I), or a pharmaceutically acceptable derivative thereof, wherein A, B, V, W, X, Y, and Z are as defined herein; pharmaceutical compositions thereof; and uses thereof.

Abstract translation: 式（I）化合物或其药学上可接受的衍生物，其中A，B，V，W，X，Y和Z如本文所定义; 其药物组合物; 及其用途。

公开(公告)号：US20060111429A1

公开(公告)日：2006-05-25

申请号：US11280128

申请日：2005-11-15

Applicant: Paul Fish ,  Thomas Ryckmans ,  Alan Stobie ,  Florian Wakenhut ,  Gavin Whitlock

Inventor： Paul Fish ,  Thomas Ryckmans ,  Alan Stobie ,  Florian Wakenhut ,  Gavin Whitlock

IPC: A61K31/40 ,  C07D207/10

CPC classification number: C07D207/14 ,  C07D405/12

Abstract: A compound of Formula (I) and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein: R1, R2, R3 and R20 are each independently H, Cl, Br, F, I, CF3, OCF3, Me or Et; R4 is het or C3-7 cycloalkyl optionally substituted by C1-4 alkyl, C1-4 alkoxy, alkoxyalkyl containing 2 to 4 carbon atoms or —S—(C1-4 alkyl); a is 0 or 1; and het is a non-aromatic 4-, 5- or 6-membered heterocycle which contains at least one N, O or S heteroatom, optionally fused to a 5- or 6-membered carbocyclic group or a second 4-, 5- or 6-membered heterocycle which contains at least one N, O or S heteroatom, wherein the het group is optionally substituted by at least one substituent independently selected from C1-8alkyl, C1-8alkoxy, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl and C1-4alkyl-S—C1-4alkyl; provided that at least one of R1, R2 and R3 are other than H. The compounds of the invention exhibit activity as both serotonin and noradrenaline re-uptake inhibitors and therefore have utility in a variety of therapeutic areas, for example urinary incontinence.

Abstract translation: 式（I）的化合物及其药学和/或兽医学上可接受的衍生物，其中：R 1，R 2，R 3和R 3 各自独立地为H，Cl，Br，F，I，CF 3，OCF 3，Me或Et; R 4是H或任选被C 1-4烷基取代的C 3-7环烷基，C 1-4 - 烷氧基，含有2至4个碳原子的烷氧基烷基或-S-（C 1-4烷基）; a是0或1; 并且它是非芳族的4-，5-或6-元杂环，其含有至少一个N，O或S杂原子，任选地与5或6元碳环基团或第二个4-，5-或 其含有至少一个N，O或S杂原子的6元杂环，其中所述基团任选地被至少一个独立地选自C 1-8烷基，C 1- 8个烷氧基，OH，卤素，CF 3，OCF 3，SCF 3，羟基-C 1-6 C 1-4烷基，C 1-4烷氧基-C 1-6烷基和C 1-4烷基-S SC 1 -4 烷基; 条件是R 1，R 2和R 3中的至少一个不是H.本发明的化合物表现出作为血清素的活性 和去甲肾上腺素再摄取抑制剂，因此可用于各种治疗领域，例如尿失禁。

公开(公告)号：US06979690B2

公开(公告)日：2005-12-27

申请号：US10337497

申请日：2003-01-07

Applicant: Geoffrey Gymer ,  Kiyoshi Kawamura ,  Sachiko Mihara ,  Mikio Morita ,  Alan Stobie ,  Chikara Uchida ,  Seiji Nukui

Inventor： Geoffrey Gymer ,  Kiyoshi Kawamura ,  Sachiko Mihara ,  Mikio Morita ,  Alan Stobie ,  Chikara Uchida ,  Seiji Nukui

IPC: A61K31/4545 ,  A61P1/00 ,  A61P1/04 ,  A61P1/08 ,  A61P1/10 ,  A61P1/14 ,  A61P9/00 ,  A61P9/10 ,  A61P25/00 ,  A61P25/04 ,  A61P25/06 ,  A61P25/22 ,  A61P25/28 ,  A61P43/00 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  A61K31/445

CPC classification number: C07D401/06 ,  C07D401/12 ,  C07D401/14

Abstract: This invention provides compounds of the formula (I) and (II): or the pharmaceutically acceptable esters thereof, and the pharmaceutically acceptable salts thereof: wherein R1 is hydrogen or halo; R2 and R3 are independently hydrogen or C1-6 alkyl; R4 and R5 are independently hydrogen or C1-6 alkyl; R6 is hydrogen, C1-12 alkyl, C1-6 alkoxy (C1-6)alkyl or C1-12 alkyl substituted by up to 3 substituents selected from the groups consisting of C3-8 cycloalkyl, aryl, heteroaryl and heterocyclic; R7 and R8 are hydrogen or taken together may form alkylene chain having one or two carbon atoms; R9 is C1-6 alkyl or C3-8 cycloalkyl; R10 is C1-6 alkyl or NR11R12; L is (CR11R12)n or NR11; M is NR11 or (CR11R12)n; R11 and R12 are independently hydrogen or C1-6 alkyl; n is an integer from 0 to 5; and m is an integer from 0 to 2; said heterocyclic, aryl and heteroaryl are unsubstituted or are substituted by at least one substituent selected from the group consisting of halo and C1-6 alkyl; with the proviso that when R9 is C1-6 alkyl, L is not NR11. These compounds have 5-HT4 receptor binding activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans. This invention also provides a pharmaceutical composition comprising the above compound.

公开(公告)号：US06333326B1

公开(公告)日：2001-12-25

申请号：US09367303

申请日：1999-08-02

Applicant: Alan Stobie ,  Elisabeth Colette Louise Gautier ,  David Charles Waite ,  Robert James Crook

Inventor： Alan Stobie ,  Elisabeth Colette Louise Gautier ,  David Charles Waite ,  Robert James Crook

IPC: C07D40114

CPC classification number: C07D401/14

Abstract: This invention relates to 2,3(1H,4H)-quinoxalinedione derivatives which are selective antagonists of N-methyl-D-aspartate receptors. More particularly, this invention relates to 5-triazolyl-2,3(1H,4H)-quinoxalinedione derivatives and to the preparation of, compositions containing, and the uses of, such derivatives. It also relates to a method for treating acute neurodegeneration disorders and chronic neurological disorders.

Abstract translation: 本发明涉及作为N-甲基-D-天冬氨酸受体的选择性拮抗剂的2,3（1H，4H） - 喹喔啉二酮衍生物。 更具体地说，本发明涉及5-三唑基-2,3（1H，4H） - 喹喔啉二酮衍生物及其制备方法，含有这些衍生物的用途和用途。 它还涉及治疗急性神经变性疾病和慢性神经障碍的方法。

公开(公告)号：US5171744A

公开(公告)日：1992-12-15

申请号：US598288

申请日：1990-10-16

Applicant: Peter E. Cross ,  Alan Stobie

Inventor： Peter E. Cross ,  Alan Stobie

IPC: C07D403/12 ,  A61K31/435 ,  A61K31/439 ,  A61P11/00 ,  A61P11/08 ,  C07D231/10 ,  C07D233/54 ,  C07D249/04 ,  C07D409/14 ,  C07D453/02

CPC classification number: C07D453/02 ,  Y10S514/826

Abstract: Compounds having the formula: ##STR1## wherein X is either (a) a phenyl group optionally substituted by 1 or 2 substituents each independently selected from halo, CF.sub.3, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy and hydroxy, or (b) a thienyl group; and Y is an imidazolyl, pyrazolyl, triazolyl or tetrazolyl group optionally substituted by 1 or 2 substituents each independently selected from halo, CF.sub.3, C.sub.1 -C.sub.4 alkoxy, hydroxy and amino; and pharmaceutically acceptable salts thereof, are antimuscarinic bronchodilators useful in the treatment of chronic obstructive airways disease and asthma.

Abstract translation: 具有下式的化合物：其中X是（a）任选被1或2个独立地选自卤素，CF 3，C 1 -C 4烷基，C 1 -C 4烷氧基和羟基的取代基取代的苯基，或（ b）噻吩基; Y是任选被1或2个独立地选自卤素，CF 3，C 1 -C 4烷氧基，羟基和氨基的取代基取代的咪唑基，吡唑基，三唑基或四唑基; 和其药学上可接受的盐是可用于治疗慢性阻塞性气道疾病和哮喘的抗毒蕈碱性支气管扩张剂。