公开(公告)号：US20120232075A1

公开(公告)日：2012-09-13

申请号：US13411450

申请日：2012-03-02

Applicant: Martin James Inglis Andrews ,  Mark Stuart Chambers ,  Wolfgang Schmidt ,  Giovanni Alessandro Tricarico ,  Grégory Louis Joseph Bar ,  Kim Louise Hirst ,  Olga Raquel Pinto Santos Oliveira Roussel ,  Juha Andrew Clase

Inventor： Martin James Inglis Andrews ,  Mark Stuart Chambers ,  Wolfgang Schmidt ,  Giovanni Alessandro Tricarico ,  Grégory Louis Joseph Bar ,  Kim Louise Hirst ,  Olga Raquel Pinto Santos Oliveira Roussel ,  Juha Andrew Clase

IPC: A61K31/4985 ,  A61K31/5377 ,  A61P29/00 ,  A61P19/02 ,  A61P19/10 ,  A61P19/04 ,  A61P1/02 ,  A61P35/04 ,  A61P11/00 ,  A61P11/06 ,  A61P13/12 ,  A61P1/16 ,  A61P9/10 ,  A61P9/04 ,  A61P25/00 ,  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：US08138193B2

公开(公告)日：2012-03-20

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: A61K31/4965

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：US08133895B2

公开(公告)日：2012-03-13

申请号：US12151586

申请日：2008-05-07

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: A61K31/4965

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：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：US6143773A

公开(公告)日：2000-11-07

申请号：US296848

申请日：1999-04-22

Applicant: Howard Barff Broughton ,  Mark Stuart Chambers

Inventor： Howard Barff Broughton ,  Mark Stuart Chambers

IPC: C07D498/04 ,  C07D495/04 ,  A61K31/42

CPC classification number: C07D498/04

Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein A is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, arylC.sub.1-6 alkyl, aryl, S(O).sub.p R.sup.1, OR.sup.1 or NR.sup.1 R.sup.12 ;B is optionally substituted 5- or 6-membered heteroaromatic ring or C(O)NR.sup.10 R.sup.11 ;R.sup.1 is hydrogen, optionally substituted C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl or C.sub.3-6 cycloalkenyl, optionally substituted aryl, arylC.sub.1-6 alkyl, arylC.sub.2-6 alkenyl or arylC.sub.2-6 alkynyl or an optionally substituted 5- or 6-membered heteroaromatic ring;R.sup.2 and R.sup.3 are hydrogen or C.sub.1-6 alkyl;R.sup.4 is hydrogen, C.sub.1-8 alkyl, C.sub.2-8 alkenyl, C.sub.2-8 alkynyl, aryl or CH.sub.2 (CO).sub.m NR.sup.8 R.sup.9 ;R.sup.5 is NR.sup.6 R.sup.7, C.sub.1-6 alkyl or C.sub.1-6 alkoxy;R.sup.6 is independently as defined for R.sup.4 ;R.sup.7 is aryl optionally substituted by halogen, nitro or cyano;R.sup.8 is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.3-6 cycloalkenyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl; arylC.sub.1-6 alkyl, arylC.sub.2-6 alkenyl or arylC.sub.2-6 alkynyl optionally substituted on the aryl ring by halogen, nitro or cyano; thiophene or pyridine;R.sup.9 is C.sub.1-6 alkyl; C.sub.2- alkenyl; C.sub.2-6 alkynyl; or phenyl optionally substituted by one, two or three substituents independently chosen from halogen, CF.sub.3, OCH.sub.3, nitro and cyano;R.sup.10 and R.sup.11 are individually hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl or C.sub.3-8 cycloalkyl or R.sup.10 and R.sup.11, together with the nitrogen atom to which they are attached, form a saturated 4 to 8 membered ring optionally containing an oxygen atom or a further nitrogen atom as a ring member, the further nitrogen atom being unsubstituted or substituted by C.sub.1-4 alkyl, C.sub.2-4 alkenyl or C.sub.2-4 alkynyl;R.sup.12 is hydrogen or C.sub.1-6 alkyl;m is zero or 1;p is zero, 1 or 2;q is 0, 1 or 2; andr is 0, 1 or 2;the preparation of these compounds, their use in enhancing cognition in disease states, particularly Alzheimer's disease, and methods of treatment using them.