公开(公告)号：US08202873B2

公开(公告)日：2012-06-19

申请号：US12597255

申请日：2008-05-07

申请人： Valentina O. Badescu ,  Anne Marie Camp ,  Barry Peter Clark ,  Michael Philip Cohen ,  Sandra Ann Filla ,  Peter Thaddeus Gallagher ,  Sarah Lynne Hellman ,  Michael Philip Mazanetz ,  Marta Maria Pineiro-Nunez ,  John Mehnert Schaus ,  Patrick Gianpietro Spinazze ,  Maria Ann Whatton

发明人： Valentina O. Badescu ,  Anne Marie Camp ,  Barry Peter Clark ,  Michael Philip Cohen ,  Sandra Ann Filla ,  Peter Thaddeus Gallagher ,  Sarah Lynne Hellman ,  Michael Philip Mazanetz ,  Marta Maria Pineiro-Nunez ,  John Mehnert Schaus ,  Patrick Gianpietro Spinazze ,  Maria Ann Whatton

IPC分类号： A61K31/4965

CPC分类号： C07D403/12 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

摘要： The present invention provides selective 5-HT7 receptor antagonist compounds of Formula I and their use in the treatment of migraine, persistent pain, and anxiety: where A and B are each independently —C(H)═ or —N═, provided that at least one of A and B is —N═, n is 1-3, m is 0-3, and R1-4 are as defined herein.

摘要翻译： 本发明提供式I的选择性5-HT7受体拮抗剂化合物及其在治疗偏头痛，持续性疼痛和焦虑中的用途：其中A和B各自独立地为-C（H）=或-N =，条件是在 A和B中的至少一个为-N =，n为1-3，m为0-3，R1-4如本文所定义。

公开(公告)号：US20100197700A1

公开(公告)日：2010-08-05

申请号：US12678345

申请日：2008-09-30

申请人： Valentina O Badescu ,  Sandra Ann Filla ,  Peter Thaddeus Gallagher ,  Maria Ann Whatton

发明人： Valentina O Badescu ,  Sandra Ann Filla ,  Peter Thaddeus Gallagher ,  Maria Ann Whatton

IPC分类号： A61K31/496 ,  C07D403/14 ,  A61P25/06

CPC分类号： C07D401/14 ,  C07D403/12 ,  C07D403/14

摘要： The present invention provides selective 5-HT7 receptor antagonist compounds of Formula I and their use in the treatment of migraine: where A is —C(H)═ or —N═ and R1-7 are as defined herein.

摘要翻译： 本发明提供式I的选择性5-HT7受体拮抗剂化合物及其在治疗偏头痛中的用途：其中A为-C（H）=或-N =且R1-7如本文所定义。

公开(公告)号：US07432280B2

公开(公告)日：2008-10-07

申请号：US10558588

申请日：2004-05-25

申请人： Christopher David Beadle ,  Manuel Javier Cases-Thomas ,  Barry Peter Clark ,  Peter Thaddeus Gallagher ,  John Joseph Masters ,  Graham Henry Timms ,  Magnus Wilhelm Walter ,  Maria Ann Whatton ,  Virginia Ann Wood ,  Jeremy Gilmore

发明人： Christopher David Beadle ,  Manuel Javier Cases-Thomas ,  Barry Peter Clark ,  Peter Thaddeus Gallagher ,  John Joseph Masters ,  Graham Henry Timms ,  Magnus Wilhelm Walter ,  Maria Ann Whatton ,  Virginia Ann Wood ,  Jeremy Gilmore

IPC分类号： A01N43/90 ,  A01N43/40 ,  A61K31/44 ,  A61K31/445 ,  C07D453/02 ,  C07D211/56 ,  C07D211/98

CPC分类号： C07D405/12 ,  C07D211/56 ,  C07D453/02

摘要： The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, which are useful for the inhibition of the uptake of one or more physiologically active monoamines (serotonin, norepinephrine, and dopamine).

摘要翻译： 本发明提供式（I）化合物及其药学上可接受的盐，其可用于抑制一种或多种生理活性单胺（5-羟色胺，去甲肾上腺素和多巴胺）摄取。

公开(公告)号：US06329366B1

公开(公告)日：2001-12-11

申请号：US09442904

申请日：1999-11-18

申请人： John Fairhurst ,  Peter Thaddeus Gallagher ,  Martin Victor Miles

发明人： John Fairhurst ,  Peter Thaddeus Gallagher ,  Martin Victor Miles

IPC分类号： C07D41714

CPC分类号： C07D215/227 ,  C07D209/34 ,  C07D215/36 ,  C07D285/10 ,  C07D285/16 ,  C07D401/14 ,  C07D417/14

摘要： A pharmaceutical compound of the formula in which R1 and R2 are each hydrogen, halo, cyano or methyl, the dotted line represents an optional double bond, where R4 and R5 are each hydrogen, C1-6 alkyl, cyclopropyl or cyclopropyl-C1-6 alkyl, n is 0 or 1, and R3 is —SR6, —SOR6, —SO2R6, —COR6, —CH2OH or —CONHR7, where R6 is C1-6 alkyl and R7 is hydrogen or C1-6 alkyl; provided that when one of R1 and R2 is hydrogen and the other is fluoro, R4 and R5 are each hydrogen or C1-6 alkyl, and n is 0, then R3 is not —COR6 or —CONHR7; and salts thereof.

摘要翻译： R1和R2各自为氢，卤素，氰基或甲基的化学式为化合物，虚线表示任选的双键，其中R 4和R 5各自为氢，C 1-6烷基，环丙基或环丙基-C 1-6烷基 ，n为0或1，R 3为-SR 6，-SOR 6，-SO 2 R 6，-COR 6，-CH 2 OH或-CONHR 7，其中R 6为C 1-6烷基，且R 7为氢或C 1-6烷基; 并且R 2是氢，另一个是氟，R 4和R 5各自是氢或C 1-6烷基，n是0，则R 3不是-COR 6或-CONHR 7;及其盐。

公开(公告)号：US06166040A

公开(公告)日：2000-12-26

申请号：US309420

申请日：1999-05-11

申请人： John Fairhurst ,  Peter Thaddeus Gallagher ,  Martin Victor Miles ,  William Martin Owton ,  Colin William Smith

发明人： John Fairhurst ,  Peter Thaddeus Gallagher ,  Martin Victor Miles ,  William Martin Owton ,  Colin William Smith

IPC分类号： A61K31/4427 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4545 ,  A61P1/00 ,  A61P1/08 ,  A61P3/04 ,  A61P9/00 ,  A61P9/12 ,  A61P15/10 ,  A61P25/04 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P25/32 ,  A61P25/34 ,  A61P43/00 ,  C07D401/14 ,  A61K31/40 ,  A61K31/435 ,  C07D209/36 ,  C07D401/00

CPC分类号： C07D401/14

摘要： Pharmaceutical compounds of the formula: ##STR1## in which n is 1 to 6, m is 1 or 2 and p is 1 or 2, R.sup.1 and R.sup.2 are each hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, HO--C.sub.1-4 alkyl, C.sub.1-4 alkoxy-C.sub.1-4 alkyl, C.sub.1-4 alkylthio, halo, optionally substituted phenyl, optionally substituted phenyl-C.sub.1-4 alkyl, or R.sup.1 and R.sup.2 together with the carbon atom to which they are attached form a C.sub.3-6 cycloalkyl group, >C.dbd.O, C.dbd.NOR' where R' is hydrogen or C.sub.1-4 alkyl,R.sup.3, R.sup.4 and R.sup.5 are each hydrogen, halo, nitro, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkyl-CO--, where m is 0, 1 or 2, R'R"N--SO.sub.2 --, --COOR', --CONR'R", --NR'R", --N(OR')COOR", --COR', --NHSO.sub.2 R', where R' and R' are each hydrogen or C.sub.1-4 alkyl,R.sup.6 and R.sup.7 are each hydrogen or C.sub.1-4 alkyl,X is oxygen or sulphur,the dotted line represents an optional double bond, and the fluorine atom is attached at the 6- or 7-position; and salts thereof.

摘要翻译： 下式的药物化合物：其中n为1至6，m为1或2，p为1或2，R 1和R 2各自为氢，C 1-4烷基，C 1-4烷氧基，HO-C 1-4烷基， C 1-4烷氧基-C 1-4烷基，C 1-4烷硫基，卤素，任选取代的苯基，任选取代的苯基-C 1-4烷基，或R 1和R 2与它们所连接的碳原子一起形成C 3-6环烷基 基团，C = O，C = NOR，其中R'是氢或C 1-4烷基，R 3，R 4和R 5各自是氢，卤素，硝基，C 1-4烷基，C 1-4烷氧基，C 1-4烷基 - CO-，其中m是0,1或2，R'R''N-SO2-，-COOR'，-CONR'R“，-NR'R”，-N（OR'）COOR“ -COR'，-NHSO 2 R'，其中R'和R'各自为氢或C 1-4烷基，R 6和R 7各自为氢或C 1-4烷基，X为氧或硫，虚线为任选的双键， 并且氟原子连接在6-或7-位; 及其盐。

公开(公告)号：US5668172A

公开(公告)日：1997-09-16

申请号：US518447

申请日：1995-08-23

申请人： Peter Thaddeus Gallagher ,  William Martin Owton ,  Andrew Caerwyn Williams

发明人： Peter Thaddeus Gallagher ,  William Martin Owton ,  Andrew Caerwyn Williams

IPC分类号： A61K31/165 ,  A61K31/19 ,  A61K31/192 ,  A61K31/235 ,  A61P29/00 ,  A61P43/00 ,  C07C65/40 ,  C07C66/02 ,  C07C69/94 ,  C07C235/84 ,  C07C50/18

CPC分类号： A61K31/192 ,  C07C66/02

摘要： A pharmaceutical compound of the formula ##STR1## in which R is hydrogen, halo or F.sub.2 HCO--; or a salt, amide or ester thereof, useful in the treatment of skeletal diseases.

摘要翻译： 用于治疗骨骼疾病的式IMAMA的酰胺或其酯的药物化合物。

公开(公告)号：US20120202797A1

公开(公告)日：2012-08-09

申请号：US13357627

申请日：2012-01-25

申请人： Anne Marie CAMP ,  Peter Thaddeus GALLAGHER ,  Andrew James LEDGARD ,  Adam Jan SANDERSON ,  David Andrew COATES

发明人： Anne Marie CAMP ,  Peter Thaddeus GALLAGHER ,  Andrew James LEDGARD ,  Adam Jan SANDERSON ,  David Andrew COATES

IPC分类号： A61K31/5517 ,  A61P25/20 ,  C07D487/04

CPC分类号： C07D487/04

摘要： A dual H1/5-HT2A receptor antagonist of the formula: its uses, and methods for its preparation are described.

摘要翻译： 描述了下式的双重H1 / 5-HT2A受体拮抗剂：其用途及其制备方法。

公开(公告)号：US20100120785A1

公开(公告)日：2010-05-13

申请号：US12597255

申请日：2008-05-07

申请人： Valentina O. Badescu ,  Anne Marie Camp ,  Barry Peter Clark ,  Michael Philip Cohen ,  Sandra Ann Filla ,  Peter Thaddeus Gallagher ,  Sarah Lynne Hellman ,  Michael Philip Mazanetz ,  Marta Maria Pineiro-Nunez ,  John Mehnert Schaus ,  Patrick Gianpietro Spinazze ,  Maria Ann Whatton

发明人： Valentina O. Badescu ,  Anne Marie Camp ,  Barry Peter Clark ,  Michael Philip Cohen ,  Sandra Ann Filla ,  Peter Thaddeus Gallagher ,  Sarah Lynne Hellman ,  Michael Philip Mazanetz ,  Marta Maria Pineiro-Nunez ,  John Mehnert Schaus ,  Patrick Gianpietro Spinazze ,  Maria Ann Whatton

IPC分类号： A61K31/497 ,  C07D241/02 ,  A61P25/06

CPC分类号： C07D403/12 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

摘要： The present invention provides selective 5-HT7 receptor antagonist compounds of Formula I and their use in the treatment of migraine, persistent pain, and anxiety: where A and B are each independently C(H)═ or N═, provided that at least one of A and B is —N═, n is 1-3, m is 0-3, and R14 are as defined herein.

摘要翻译： 本发明提供式I的选择性5-HT7受体拮抗剂化合物及其在治疗偏头痛，持续性疼痛和焦虑中的用途：其中A和B各自独立地为C（H）=或N =，条件是至少一种 A和B为-N =，n为1-3，m为0-3，R 14如本文所定义。

公开(公告)号：US07488728B2

公开(公告)日：2009-02-10

申请号：US10567639

申请日：2004-08-09

申请人： Barry Peter Clark ,  Peter Thaddeus Gallagher

发明人： Barry Peter Clark ,  Peter Thaddeus Gallagher

IPC分类号： A61K31/5377 ,  C07D413/12

CPC分类号： C07D413/12

摘要： The invention relates to compounds of formula (I): wherein R, R1, R2 and X are defined herein, their preparation, and their use as pharmaceuticals.

摘要翻译： 本发明涉及式（I）化合物：其中R，R 1，R 2和X如本文所定义，其制备及其作为药物的用途。

公开(公告)号：US07410996B2

公开(公告)日：2008-08-12

申请号：US10533328

申请日：2003-10-24

申请人： Serge Louis Boulet ,  Sandra Ann Filla ,  Peter Thaddeus Gallagher ,  Kevin John Hudziak ,  Anette Margareta Johansson ,  Rushad E. Karanjawala ,  John Joseph Masters ,  Victor Giulio Matassa ,  Brian Michael Mathes ,  Richard Edmund Rathmell ,  Maria Ann Whatton ,  Chad Nolan Wolfe

发明人： Serge Louis Boulet ,  Sandra Ann Filla ,  Peter Thaddeus Gallagher ,  Kevin John Hudziak ,  Anette Margareta Johansson ,  Rushad E. Karanjawala ,  John Joseph Masters ,  Victor Giulio Matassa ,  Brian Michael Mathes ,  Richard Edmund Rathmell ,  Maria Ann Whatton ,  Chad Nolan Wolfe

IPC分类号： A61K31/381 ,  C07D333/64

CPC分类号： C07D275/04 ,  C07C217/16 ,  C07C217/30 ,  C07C217/48 ,  C07C323/32 ,  C07D307/86 ,  C07D333/54 ,  C07D333/62 ,  C07D475/04

摘要： There is provided a compound of formula (I) wherein A is selected from —O— and —S—; X is selected from phenyl optionally substituted with up to 5 substituents each independently selected from halo, C1-C4 alkyl and C1-C4 alkoxy, thienyl optionally substituted with up to 3 substituents each independently selected from halo and C1-C4 alkyl, and C2-C8 alkyl, C2-C8 alkenyl, C3-C8 cycloalkyl and C4-C8 cycloalkylalkyl, each of which may be optionally substituted with up to 3 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, —CF3, —CN and —CONH2; Y is selected from phenyl, naphthyl, dihydrobenzothienyl, benzothiazolyl, benzoisothiazolyl, quinolyl, isoquinolyl, naphthyridyl, thienopyridyl, indanyl, 1,3-benzodioxolyl, benzothienyl, indolyl and benzofuranyl, each of which may be optionally substituted with up to 4 or, where possible, up to 5 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, nitro, acetyl, —CF3, —SCF3 and cyano; and when Y is indolyl it may be substituted or further substituted by an N-substituent selected from C1-C4 alkyl; Z is selected from OR3 or F, wherein R3 is selected from H, C1-C6 alkyl and phenyl C1-C6 alkyl; R1 and R2 are each independently H or C1-C4 alkyl; and pharmaceutically acceptable salts thereof with the proviso that when Y is optionally substituted phenyl or optionally substituted 1,3-benzodioxolyl and Z is OR3 and X is optionally substituted phenyl then A is —S—.