公开(公告)号：US06936608B2

公开(公告)日：2005-08-30

申请号：US10416318

申请日：2001-11-08

Applicant: Michela Bettati ,  Peter Blurton ,  William Robert Carling ,  Mark Stuart Chambers ,  David James Hallett ,  Andrew Jennings ,  Richard Thomas Lewis ,  Michael Geoffrey Neil Russell ,  Leslie Joseph Street ,  Helen Jane Szekeres ,  Monique Bodil Van Neil

Inventor： Michela Bettati ,  Peter Blurton ,  William Robert Carling ,  Mark Stuart Chambers ,  David James Hallett ,  Andrew Jennings ,  Richard Thomas Lewis ,  Michael Geoffrey Neil Russell ,  Leslie Joseph Street ,  Helen Jane Szekeres ,  Monique Bodil Van Neil

IPC: A61K31/53 ,  A61P25/00 ,  A61P25/22 ,  C07D487/04 ,  A61P25/08 ,  A61P25/28

CPC classification number: C07D487/04

Abstract: A class of 7-phenylimidazo[1,2-b][1,2,4]triazine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group which is directly attached or bridged by an oxygen atom or a —NH— linkage, being selective ligands for GABAA receptors, in particular having good affinity for the α2 and/or α3 and/or α5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.

Abstract translation: 一类7-苯基咪唑并[1,2-b] [1,2,4]三嗪衍生物，其在苯环的间位被任选取代的被氧原子连接或桥连的芳基或杂芳基取代 或-NH-连接，作为GABA A受体的选择性配体，特别是对α2和/或α3和/或α5亚基具有良好的亲和力，因此在治疗和/ 或预防中枢神经系统的不良状况，包括焦虑，抽搐和认知障碍。

公开(公告)号：US5854268A

公开(公告)日：1998-12-29

申请号：US776024

申请日：1997-01-22

Applicant: Raymond Baker ,  Sylvie Bourrain ,  Jose Luis Castro Pineiro ,  Mark Stuart Chambers ,  Alexander Richard Guiblin ,  Sarah Christine Hobbs ,  Richard Alexander Jelley ,  Andrew Madin ,  Victor Giulio Matassa ,  Austin John Reeve ,  Michael Geoffrey Russell ,  Graham Andrew Showell ,  Francine Sternfeld ,  Leslie Joseph Street ,  Monique Bodil Van Niel

Inventor： Raymond Baker ,  Sylvie Bourrain ,  Jose Luis Castro Pineiro ,  Mark Stuart Chambers ,  Alexander Richard Guiblin ,  Sarah Christine Hobbs ,  Richard Alexander Jelley ,  Andrew Madin ,  Victor Giulio Matassa ,  Austin John Reeve ,  Michael Geoffrey Russell ,  Graham Andrew Showell ,  Francine Sternfeld ,  Leslie Joseph Street ,  Monique Bodil Van Niel

IPC: C07D401/14 ,  A61K31/41 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/445 ,  A61K31/475 ,  A61P9/00 ,  A61P25/04 ,  A61P43/00 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D471/04 ,  C07D521/00

CPC classification number: C07D249/08 ,  C07D231/12 ,  C07D233/56

Abstract: A class of substituted azetidine, pyrrolidine and piperidine derivatives are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.

Abstract translation: PCT No.PCT / GB95 / 01819 Sec。 371日期1997年1月22日 102（e）1997年1月22日PCT PCT 1995年8月1日PCT公布。 公开号WO96 / 04274 日期1996年2月15日一类取代的氮杂环丁烷，吡咯烷和哌啶衍生物是5-HT1样受体的选择性激动剂，它是人类5-HT1Dα受体亚型的有效激动剂，同时具有至少10倍的选择性亲和力 5-HT1Dα受体亚型相对于5-HT1Dβ亚型; 因此，它们可用于治疗和/或预防临床状况，特别是偏头痛和相关疾病，其中指出5-HT1D受体的亚型选择性激动剂，同时引起较少的副作用，特别是不利的心血管事件，比 与非亚型选择性5-HT1D受体激动剂相关的那些。

公开(公告)号：US5719147A

公开(公告)日：1998-02-17

申请号：US525259

申请日：1995-09-08

Applicant: Conrad P. Dorn ,  Paul E. Finke ,  Jeffrey J. Hale ,  Malcolm MacCoss ,  Sander G. Mills ,  Shrenik K. Shah ,  Mark Stuart Chambers ,  Timothy Harrison ,  Tamara Ladduwahetty ,  Brian John Williams

Inventor： Conrad P. Dorn ,  Paul E. Finke ,  Jeffrey J. Hale ,  Malcolm MacCoss ,  Sander G. Mills ,  Shrenik K. Shah ,  Mark Stuart Chambers ,  Timothy Harrison ,  Tamara Ladduwahetty ,  Brian John Williams

IPC: C07D265/30 ,  C07D265/32 ,  C07D279/12 ,  C07D413/04 ,  C07D413/06 ,  C07D413/14 ,  A61K31/54 ,  A61K31/535 ,  C07D417/04

CPC classification number: C07D265/30 ,  C07D265/32 ,  C07D279/12 ,  C07D413/04 ,  C07D413/06 ,  C07D413/14 ,  Y10S514/825

Abstract: Substituted heterocycles of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.

公开(公告)号：US5681833A

公开(公告)日：1997-10-28

申请号：US302936

申请日：1994-09-20

Applicant: Jose Luis Castro Pineiro ,  Mark Stuart Chambers ,  Sarah Christine Hobbs ,  Victor Giulio Matassa

Inventor： Jose Luis Castro Pineiro ,  Mark Stuart Chambers ,  Sarah Christine Hobbs ,  Victor Giulio Matassa

IPC: A61K31/55 ,  A61K31/551 ,  A61P1/04 ,  A61P25/04 ,  A61P25/20 ,  C07D243/14 ,  C07D243/24 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14

CPC classification number: C07D403/12 ,  C07D243/14 ,  C07D243/24 ,  C07D403/14

Abstract: Compounds of Formula (I), and salts and prodrugs thereof, wherein said formula, R.sup.1 represents certain optionally substituted alkyl or C.sub.3-7 cycloalkyl; R.sup.2 represents (II) or (III), where m is 0, 1, 2 or 3; R.sup.9 is H or C.sub.1-6 alkyl; R.sup.10 is imidazolyl, triazolyl or tetrazolyl, and R.sup.11 is H, C.sub.1-6 alkyl or halo; R.sup.3 is C.sub.1-6 alkyl, halo or NR.sup.6 R.sup.7 ; R.sup.4 is C.sub.1-7 alkyl, C.sub.3-10 cycloalkyl, C.sub.3-10 cycloalkylC.sub.1-4 alkyl, C.sub.6-10 bicycloalkyl, optionally substituted aryl, or NR.sub.12 R.sub.13 ; R.sup.5 is H or C.sub.1-4 alkyl; n is 0, 1, 2 or 3; which are CCK and/or gastrin antagonists useful in therapy.

Abstract translation: PCT No.PCT / GB93 / 00599 Sec。 371日期1994年9月20日 102（e）1994年9月20日PCT 1993年3月23日PCT公布。 出版物WO93 / 19052 （III）式（I）化合物及其盐和前药，其中所述式R1表示某些任选取代的烷基或C 3 -C 10烷基， 7环烷基; R2表示（II）或（III），其中m为0,1,2或3; R9是H或C1-6烷基; R10是咪唑基，三唑基或四唑基，R11是H，C1-6烷基或卤素; R3是C1-6烷基，卤素或NR6R7; R 4是C 1-7烷基，C 3-10环烷基，C 3-10环烷基C 1-4烷基，C 6-10二环烷基，任选取代的芳基或NR 12 R 13; R5是H或C1-4烷基; n为0,1,2或3; 其是可用于治疗的CCK和/或胃泌素拮抗剂。

公开(公告)号：US07893058B2

公开(公告)日：2011-02-22

申请号：US11803015

申请日：2007-05-11

Applicant: Martin James Inglis Andrews ,  Paul Edwards ,  Philip Huxley ,  Wolfgang Schmidt ,  Veronique Birault ,  Mark Stuart Chambers ,  Clifford John Harris ,  Angus MacLeod ,  Kim Louise Hirst ,  Juha Andrew Clase ,  Gregory Bar

Inventor： Martin James Inglis Andrews ,  Paul Edwards ,  Philip Huxley ,  Wolfgang Schmidt ,  Veronique Birault ,  Mark Stuart Chambers ,  Clifford John Harris ,  Angus MacLeod ,  Kim Louise Hirst ,  Juha Andrew Clase ,  Gregory Bar

IPC: C07D487/04 ,  A61K31/4985

CPC classification number: C07D487/04

Abstract: Novel imidazo[1,2-a]pyrazine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, arthritis, inflammation, and others.

Abstract translation: 公开了具有下列表示的式的新型咪唑并[1,2-a]吡嗪化合物：该化合物可以制备为药物组合物，并且可用于预防和治疗包括人在内的哺乳动物中的多种病症， 包括作为非限制性实例的关节炎，炎症等。

公开(公告)号：US20090286798A1

公开(公告)日：2009-11-19

申请号：US12436219

申请日：2009-05-06

Applicant: Martin James Inglis Andrews ,  Mark Stuart Chambers ,  Hervé Van De Poël ,  Grégory Louis Joseph Bar

Inventor： Martin James Inglis Andrews ,  Mark Stuart Chambers ,  Hervé Van De Poël ,  Grégory Louis Joseph Bar

IPC: A61K31/4985 ,  C07D487/04 ,  A61P29/00

CPC classification number: C07D519/00

Abstract: Novel[1.2.4]triazolo[1,5-a]pyrazine and imidazo[1,2-a]pyrazine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, and others.

Abstract translation: 公开了具有下列化学式的新型[1.2.4]三唑并[1,5-a]吡嗪和咪唑并[1,2-a]吡嗪化合物：该化合物可以制备为药物组合物，并且可以使用 用于预防和治疗包括人在内的哺乳动物中的各种病症，包括作为非限制性实例，疼痛，炎症等。

公开(公告)号：US20090137549A1

公开(公告)日：2009-05-28

申请号：US11983402

申请日：2007-11-08

Applicant: Paul John Edward ,  Mark Stuart Chambers ,  Christel Jeanne Marie Menet ,  Stephen Robert Fletcher ,  Rebecca Elizabeth Jarvis ,  Herve Van De Poel ,  Alexander Sudau ,  Alastair Rae ,  Peter Stanley Thomas

Inventor： Paul John Edward ,  Mark Stuart Chambers ,  Christel Jeanne Marie Menet ,  Stephen Robert Fletcher ,  Rebecca Elizabeth Jarvis ,  Herve Van De Poel ,  Alexander Sudau ,  Alastair Rae ,  Peter Stanley Thomas

IPC: A61K31/397 ,  C07D487/04 ,  A61P19/02 ,  C07D413/14

CPC classification number: C07D487/04

Abstract: The present invention relates to compounds that are inhibitors of PDE1A, a phosphodiesterase that is involved in the modulation of the degradation of cartilage, joint degeneration and diseases involving such degradation and/or inflammation.

Abstract translation: 本发明涉及作为PDE1A抑制剂的化合物，其是参与软骨降解调节，关节变性和涉及这种降解和/或炎症的疾病的磷酸二酯酶。

公开(公告)号：US20090131446A1

公开(公告)日：2009-05-21

申请号：US12151586

申请日：2008-05-07

Applicant: Martin James Inglis Andrews ,  Mark Stuart Chambers ,  Wolfgang Schmidt ,  Gregory Louis Joseph Bar

Inventor： Martin James Inglis Andrews ,  Mark Stuart Chambers ,  Wolfgang Schmidt ,  Gregory Louis Joseph Bar

IPC: A61K31/4985 ,  C07D487/04

CPC classification number: C07D487/04

Abstract: Novel fused pyrazine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, inflammation, rheumatoid arthritis and others.

Abstract translation: 公开了具有下列表示的式的新型稠合吡嗪化合物：该化合物可以制备成药物组合物，并且可用于预防和治疗包括人在内的哺乳动物中的各种病症，包括以非限制性方式 例如炎症，类风湿关节炎等。

公开(公告)号：US07030128B2

公开(公告)日：2006-04-18

申请号：US10472680

申请日：2002-03-19

Applicant: Wesley Peter Blackaby ,  Jose Luis Castro Pineiro ,  Mark Stuart Chambers ,  Simon Charles Goodacre ,  David James Hallett ,  Philip Jones ,  Richard Thomas Lewis ,  Angus Murray MacLeod ,  Robert James Maxey ,  Kevin William Moore ,  Leslie Joseph Street

Inventor： Wesley Peter Blackaby ,  Jose Luis Castro Pineiro ,  Mark Stuart Chambers ,  Simon Charles Goodacre ,  David James Hallett ,  Philip Jones ,  Richard Thomas Lewis ,  Angus Murray MacLeod ,  Robert James Maxey ,  Kevin William Moore ,  Leslie Joseph Street

IPC: A61K31/519 ,  C07D487/04 ,  A61P25/22

CPC classification number: C07D487/04 ,  A61K31/519

Abstract: A class of imidazo[1,2-α]pyrimidine derivatives, substituted at the 3-position by an optionally substituted five-membered or six-membered heteroaromatic ring, are selective ligands for GABAA receptors, in particular having good affinity for the α2 and/or α3 and/or α5 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.

Abstract translation: 一类由任选取代的五元或六元杂芳环在3-位上被取代的咪唑并[1,2-α]嘧啶衍生物，是GABA A A受体的选择性配体， 特别是对α2和/或α3和/或α5亚基具有良好的亲和力，因此有益于治疗和/或预防中枢神经系统的不利条件，包括焦虑，抽搐和认知障碍。

公开(公告)号：US06900209B2

公开(公告)日：2005-05-31

申请号：US10432391

申请日：2001-11-22

Applicant: Mark Stuart Chambers ,  Philip Jones ,  Angus Murray MacLeod ,  Robert James Maxey ,  Helen Jane Szekeres

Inventor： Mark Stuart Chambers ,  Philip Jones ,  Angus Murray MacLeod ,  Robert James Maxey ,  Helen Jane Szekeres

IPC: C07D487/04 ,  A61K31/5025 ,  A61P25/28

CPC classification number: C07D487/04

Abstract: The present invention provides a compound of formula (I) wherein A is an optionally substituted C1-4alkylidene group or a bond, R20 and R21 are hydrogen, alkyl groups or heterocyclic groups, R1 and R2 are small substituents or hydrogen, L is O, S or substituted N, X is a 5- or 6-membered heteroaromatic ring, Y is C1-4alkylidene and Z is a 5- or 6-membered heteroaromatic ring; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising it; its use in therapy; its use in making medicaments for treating neurodegenerative disease and methods of using it to enhance cognition.

Abstract translation: 本发明提供式（I）的化合物，其中A是任选取代的C 1-4烷基或键，R 20和R 21， / SO 2是氢，烷基或杂环基，R 1和R 2是小取代基或氢，L是O，S或取代的N，X是5 - 或6-元杂芳环，Y是C 1-4 - 亚烷基，Z是5-或6-元杂芳环; 或其药学上可接受的盐; 包含它的药物组合物; 其用于治疗; 其用于制备用于治疗神经退行性疾病的药物和使用其增强认知的方法。