公开(公告)号：US08012983B2

公开(公告)日：2011-09-06

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: A61K31/4965

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：US07915256B2

公开(公告)日：2011-03-29

申请号：US12399979

申请日：2009-03-08

Applicant: Martin James Inglis Andrews ,  Paul Edwards ,  Mark Stuart Chambers ,  Wolfgang Schmidt ,  Juha Andrew Clase ,  Gregory Bar ,  Kim Louise Hirst ,  Angus MacLeod

Inventor： Martin James Inglis Andrews ,  Paul Edwards ,  Mark Stuart Chambers ,  Wolfgang Schmidt ,  Juha Andrew Clase ,  Gregory Bar ,  Kim Louise Hirst ,  Angus MacLeod

IPC: C07D403/12 ,  A61K31/506

CPC classification number: C07D487/04

Abstract: Novel [1.2.4]triazolo[1,5-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]吡嗪化合物：该化合物可以制备成药物组合物，并可用于预防和治疗各种病症 在包括人的哺乳动物中，包括作为非限制性实例的疼痛，炎症等。

公开(公告)号：US20100240666A1

公开(公告)日：2010-09-23

申请号：US12753383

申请日：2010-04-02

Applicant: Martin James Inglis ANDREWS ,  Mark Stuart Chambers ,  Wolfgang Schmidt ,  Grégory Louis Joseph Bar

Inventor： Martin James Inglis ANDREWS ,  Mark Stuart Chambers ,  Wolfgang Schmidt ,  Grégory Louis Joseph Bar

IPC: A61K31/4985 ,  C07D471/04 ,  A61P19/02

CPC classification number: C07D487/04

Abstract: Novel fused pyrazine compounds are disclosed that have a formula represented by the following: with Z, R1, R2, R8 and R9 as defined in the written description. 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: 公开了具有由以下表示的式的新型稠合吡嗪化合物：如书面描述中所定义的Z，R 1，R 2，R 8和R 9。 化合物可以制备成药物组合物，并且可以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，炎症，类风湿性关节炎等。

公开(公告)号：US07592456B2

公开(公告)日：2009-09-22

申请号：US11791195

申请日：2005-11-28

Applicant: Mark Stuart Chambers ,  Neil Roy Curtis ,  Emanuela Gancia ,  Myra Gilligan ,  Alexander Charles Humphries ,  Tamara Ladduwahetty ,  Robert James Maxey ,  Kevin John Merchant

Inventor： Mark Stuart Chambers ,  Neil Roy Curtis ,  Emanuela Gancia ,  Myra Gilligan ,  Alexander Charles Humphries ,  Tamara Ladduwahetty ,  Robert James Maxey ,  Kevin John Merchant

IPC: C07D215/00 ,  C07D401/02 ,  C07D401/00 ,  C07D401/10 ,  C07C305/00

CPC classification number: C07D401/12 ,  C07C311/08 ,  C07C317/14 ,  C07C317/22 ,  C07C317/24 ,  C07C317/32 ,  C07C317/42 ,  C07C317/44 ,  C07C323/65 ,  C07C2601/04 ,  C07D213/61 ,  C07D213/64 ,  C07D213/70 ,  C07D215/36 ,  C07D215/60 ,  C07D233/64 ,  C07D241/12 ,  C07D249/06 ,  C07D249/08 ,  C07D249/18 ,  C07D261/08 ,  C07D271/10 ,  C07D277/26 ,  C07D333/34 ,  C07D471/04 ,  C07D473/38

Abstract: Compounds of formula (I) are potent and selective 5-HT2A antagonists, useful in treatment of a variety of adverse conditions of the CNS.

Abstract translation: 式（I）化合物是有效和选择性的5-HT2A拮抗剂，可用于治疗各种不良的CNS病症。

公开(公告)号：US07501411B2

公开(公告)日：2009-03-10

申请号：US11809294

申请日：2007-05-30

Applicant: Martin James Inglis Andrews ,  Paul Edwards ,  Mark Stuart Chambers ,  Wolfgang Schmidt ,  Juha Andrew Clase ,  Gregory Bar ,  Kim Louise Hirst ,  Angus MacLeod

Inventor： Martin James Inglis Andrews ,  Paul Edwards ,  Mark Stuart Chambers ,  Wolfgang Schmidt ,  Juha Andrew Clase ,  Gregory Bar ,  Kim Louise Hirst ,  Angus MacLeod

IPC: C07D487/04 ,  A61K31/4985

CPC classification number: C07D487/04

Abstract: Novel [1.2.4]triazolo[1,5-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]吡嗪化合物：该化合物可以制备成药物组合物，并可用于预防和治疗各种病症 在包括人的哺乳动物中，包括作为非限制性实例的疼痛，炎症等。

公开(公告)号：US06900215B2

公开(公告)日：2005-05-31

申请号：US10100797

申请日：2002-03-19

Applicant: Mark Stuart Chambers ,  Simon Charles Goodacre ,  David James Hallett ,  Andrew Jennings ,  Philip Jones ,  Richard Thomas Lewis ,  Kevin William Moore ,  Michael Geoffrey Neil Russell ,  Leslie Joseph Street ,  Helen Jane Szekeres

Inventor： Mark Stuart Chambers ,  Simon Charles Goodacre ,  David James Hallett ,  Andrew Jennings ,  Philip Jones ,  Richard Thomas Lewis ,  Kevin William Moore ,  Michael Geoffrey Neil Russell ,  Leslie Joseph Street ,  Helen Jane Szekeres

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

CPC classification number: C07D487/04

Abstract: A class of 3-phenylimidazo[1,2-α]pyrimidine 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, and further substituted on the phenyl ring by alkyl, trifluoromethyl, alkoxy or one or two halogen atoms, especially fluoro, 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3-苯基咪唑并[1,2-a]嘧啶衍生物，其在苯环的间位被被氧原子或-NH-键直接连接或桥连的任选取代的芳基或杂芳基取代， 并且在苯环上被烷基，三氟甲基，烷氧基或一个或两个卤原子，特别是氟取代，是GABA A A受体的选择性配体，特别是对α2和/或α3具有良好的亲和力 和/或其α5亚基，因此有益于治疗和/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：US5998415A

公开(公告)日：1999-12-07

申请号：US065020

申请日：1998-04-17

Applicant: Mark Stuart Chambers ,  Sarah Christine Hobbs ,  Leslie Joseph Street

Inventor： Mark Stuart Chambers ,  Sarah Christine Hobbs ,  Leslie Joseph Street

IPC: C07D403/06 ,  C07D521/00 ,  A61K31/495 ,  C07D403/14

CPC classification number: C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D403/06

Abstract: A class of piperazinones, homopiperazinones and thione analogues thereof, substituted at the 1-position by an optionally substituted alkenyl, alkynyl, aryl-alkyl or heteroaryl-alkyl moiety, and linked at the 4-position via an alkylene spacer to a fused bicyclic heteroaromatic moiety, typically indolyl, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype while 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, while 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 / GB96 / 02624。 371日期：1998年4月17日 102（e）1998年4月17日PCT PCT 1996年10月28日PCT公布。 公开号WO97 / 16446 日期1997年5月9日一类哌嗪酮，高哌嗪酮和其硫酮类似物在1位被任选取代的烯基，炔基，芳基 - 烷基或杂芳基 - 烷基部分取代，并通过亚烷基间隔基在4-位连接至 稠合双环杂芳族部分，通常为吲哚基，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，同时对5-HT1Dα受体亚型具有至少10倍的选择性亲和力 相对于5-HT1Dβ亚型; 因此，它们可用于治疗和/或预防临床症状，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，同时引起更少的副作用，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：US5919783A

公开(公告)日：1999-07-06

申请号：US776626

申请日：1997-01-21

Applicant: Mark Stuart Chambers ,  Victor Giulio Matassa ,  Leslie Joseph Street

Inventor： Mark Stuart Chambers ,  Victor Giulio Matassa ,  Leslie Joseph Street

IPC: C07D521/00 ,  A61K31/495 ,  C07D403/14 ,  C07D471/04

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

Abstract: Compounds of formula (I), or a salt or prodrug thereof, wherein Z represents an optionally substituted five-membered heteroaromatic ring selected from furan, thiophene, pyrrole, oxazole, thiazole, isoxazole, isothiazole, imidazole, pyrazole, oxadiazole, thiadiazole, triazole, and tetrazole; E represents a chemical bond or a straight or branched alkylene chain containing from 1-4 carbon atoms; Q represents a straight or branched alkylene chain containing from 1-6 carbon atoms; T represents nitrogen or CH; R.sup.1 represents aryl(C.sub.1-6)alkyl or heteroaryl(C.sub.1-6)alkyl, either of which groups may be optionally substituted; and R.sup.2 represents hydrogen or C.sub.1-6 alkyl 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. ##STR1##

Abstract translation: PCT No.PCT / GB95 / 01756 Sec。 371日期1997年1月21日 102（e）1997年1月21日PCT PCT 1995年7月24日PCT公布。 出版物WO96 / 04269 日期：2002年2月15日式（I）化合物或其盐或前体药物，其中Z表示选自呋喃，噻吩，吡咯，恶唑，噻唑，异恶唑，异噻唑，咪唑，吡唑等的任选取代的五元杂芳族环， 恶二唑，噻二唑，三唑和四唑; E表示化学键或含有1-4个碳原子的直链或支链亚烷基链; Q表示含有1-6个碳原子的直链或支链亚烷基链; T表示氮或CH; R1表示芳基（C1-6）烷基或杂芳基（C1-6）烷基，其中任一个可以任选被取代; 并且R 2表示氢或C 1-6烷基是5-HT1样受体的选择性激动剂，其是人5-HT1Dα受体亚型的有效激动剂，同时对5-HT1Dα受体亚型具有至少10倍的选择性亲和力 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：US08178530B2

公开(公告)日：2012-05-15

申请号：US12970632

申请日：2010-12-16

Applicant: Martin James Inglis Andrews ,  Paul Edwards ,  Reginald Christophe Xavier Brys ,  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 ,  Reginald Christophe Xavier Brys ,  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.

公开(公告)号：US08173656B2

公开(公告)日：2012-05-08

申请号：US12970659

申请日：2010-12-16

Applicant: Martin James Inglis Andrews ,  Paul Edwards ,  Reginald Christophe Xavier Brys ,  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 ,  Reginald Christophe Xavier Brys ,  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。