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1. 发明申请

WO2009002423A3 POLYCYCLIC GUANINE DERIVATIVES AND USE THEREOF 审中-公开
标题翻译：多环类衍生物及其用途
公开(公告)号：WO2009002423A3
公开(公告)日：2009-04-23
申请号：PCT/US2008007592
申请日：2008-06-18
申请人： SCHERING CORP , ALBANY MOLECULAR RES INC , TULSHIAN DEEN , GEISS WILLIAM B , MARTIN GREGORY S , LE VAN-DUC , HABER JAMES C JR , MATASI JULIUS J , CZARNIECKI MICHAEL F , COOKE STEPHANIE NICOLE
发明人： TULSHIAN DEEN , GEISS WILLIAM B , MARTIN GREGORY S , LE VAN-DUC , HABER JAMES C JR , MATASI JULIUS J , CZARNIECKI MICHAEL F , COOKE STEPHANIE NICOLE
IPC分类号： C07D487/14 , A61K31/519 , A61P25/00
CPC分类号： C07D487/14
摘要： The present invention relates to Polycyclic Guanine Derivatives, compositions comprising the Polycyclic Guanine Derivatives and methods of using the Polycyclic Guanine Derivatives to treat pain or an inflammatory disease.
摘要翻译：本发明涉及多环鸟嘌呤衍生物，包含多环鸟嘌呤衍生物的组合物和使用多环鸟嘌呤衍生物治疗疼痛或炎性疾病的方法。

2. 发明申请

WO03048164A3 ADENOSINE A2A RECEPTOR ANTAGONISTS 审中-公开
标题翻译：腺苷A2A受体拮抗剂
公开(公告)号：WO03048164A3
公开(公告)日：2003-10-16
申请号：PCT/US0238134
申请日：2002-11-26
申请人： SCHERING CORP
发明人： MATASI JULIUS J , CALDWELL JOHN P , TULSHIAN DEEN , SILVERMAN LISA S , NEUSTADT BERNARD R
IPC分类号： A61K31/519 , A61K31/5377 , A61K45/00 , A61P25/00 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/28 , A61P43/00 , C07D487/04 , A61K31/505
CPC分类号： C07D487/04
摘要： This invention relates to compounds having the structural formula (I) or pharmaceutically acceptable salts or solvates thereof, wherein R, R and R are as defined in the specification, pharmaceutical compositions thereof, and methods of treating stroke or central nervous system diseases by administering the compound of the present invention to a patient in need of such treatment.
摘要翻译：本发明涉及具有结构式（I）的化合物或其药学上可接受的盐或溶剂化物，其中R，R 2和R 3如说明书中所定义，其药物组合物，以及治疗中风或中枢的方法通过将本发明的化合物给予需要这种治疗的患者的神经系统疾病。

3. 发明申请

WO2007070393A2 MGLUR1 ANATGONISTS AS THERAPEUTIC AGENTS 审中-公开
标题翻译： MGLUR1 ANATGONISTS作为治疗剂
公开(公告)号：WO2007070393A2
公开(公告)日：2007-06-21
申请号：PCT/US2006046943
申请日：2006-12-11
申请人： SCHERING CORP , MATASI JULIUS J , TULSHIAN DEEN , BURNETT DUANE A , WU WEN-LIAN , KORAKAS PETER , SILVERMAN LISA S , THAVALAKULAMGARA SASIKUMAR K , QIANG LI , DOMALSKI MARTIN S
发明人： MATASI JULIUS J , TULSHIAN DEEN , BURNETT DUANE A , WU WEN-LIAN , KORAKAS PETER , SILVERMAN LISA S , THAVALAKULAMGARA SASIKUMAR K , QIANG LI , DOMALSKI MARTIN S
CPC分类号： C07D495/14
摘要： In its many embodiments, the present invention provides tricyclic compounds of formula (I) (wherein J 1 - J 4 , X, and R 1 - R 5 are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimer's disease.
摘要翻译：在其许多实施方案中，本发明提供了式（I）的三环化合物（其中J 1，X 4，X和R 1，（mGluR）拮抗剂（特别是作为选择性代谢型谷氨酸受体1拮抗剂），含有该化合物的药物组合物以及使用该化合物和组合物治疗治疗与代谢型谷氨酸受体（例如mGluR1）相关的疾病，例如疼痛，偏头痛，焦虑症，尿失禁和神经退行性疾病，例如阿尔茨海默氏病。

4. 发明专利

JP2008303217A Adenosine A2a receptor antagonist 审中-公开
标题翻译：腺苷A2a受体拮抗剂
公开(公告)号：JP2008303217A
公开(公告)日：2008-12-18
申请号：JP2008147394
申请日：2008-06-04
申请人： Schering Corp , シェーリングコーポレイションSchering Corporation
发明人： MATASI JULIUS J , CALDWELL JOHN P , TULSHIAN DEEN , SILVERMAN LISA S , NEUSTADT BERNARD R
IPC分类号： C07D487/04 , A61K31/519 , A61K31/5377 , A61K45/00 , A61P25/00 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/28 , A61P43/00 , C07D519/00
CPC分类号： C07D487/04
摘要： PROBLEM TO BE SOLVED: To provide a medicine for the treatment of central nervous system diseases, especially Parkinson's disease. SOLUTION: The invention relates to a compound expressed by structural formula (I), its pharmaceutically acceptable salt or solvate, its pharmaceutical composition, and a method for the treatment of stroke or central nervous system diseases by the administration of the compound of the present invention to a patient necessitating the treatment of such diseases. More particularly, the invention relates to a substituted 1,2,4-triazolo[1,5-c]pyrimidine adenosine A 2a receptor antagonist, use of the compound for the treatment of central nervous system diseases, especially Parkinson's disease, and a pharmaceutical composition containing the compound. COPYRIGHT: (C)2009,JPO&INPIT
摘要翻译：要解决的问题：提供治疗中枢神经系统疾病，特别是帕金森病的药物。解决方案：本发明涉及由结构式（I）表示的化合物，其药学上可接受的盐或溶剂合物，其药物组合物，以及通过给予中和或中枢神经系统疾病的治疗方法本发明涉及需要治疗这些疾病的患者。更具体地说，本发明涉及取代的1,2,4-三唑并[1,5-c]嘧啶腺苷A 2a 受体拮抗剂，该化合物用于治疗中枢神经系统疾病，特别是帕金森病，以及含有该化合物的药物组合物。版权所有（C）2009，JPO＆INPIT

5. 发明专利

JP2008297312A Imidazo (4,3-e)-1,2,4-triazolo(1,5-c) pyrimidine as adenosine a2a receptor antagonist 审中-公开
标题翻译：咪唑（4,3-E）-1,2,4-三唑（1,5-C）嘧啶作为腺苷A2A受体拮抗剂
公开(公告)号：JP2008297312A
公开(公告)日：2008-12-11
申请号：JP2008192667
申请日：2008-07-25
申请人： Schering Corp , シェーリングコーポレイションSchering Corporation
发明人： TULSHIAN DEEN , SILVERMAN LISA S , MATASI JULIUS J , KISELGOF EUGENIA Y , CALDWELL JOHN P
IPC分类号： C07D487/14 , A61K31/198 , A61K31/505 , A61K31/519 , A61K45/00 , A61K45/06 , A61P9/00 , A61P9/10 , A61P25/00 , A61P25/16 , A61P25/24 , A61P25/28 , A61P43/00 , C07D519/00
CPC分类号： C07D487/14 , A61K31/198 , A61K31/505 , A61K45/06 , Y02P20/582 , A61K2300/00
摘要： PROBLEM TO BE SOLVED: To provide adenosine A 2a receptor antagonist. SOLUTION: Compounds having the structural formula (I) or a pharmaceutically acceptable salt thereof, their use in the treatment of Parkinson's disease, and pharmaceutical compositions containing them are disclosed. Wherein R is an optionally substituted phenyl or a heteroaryl, a cycloalkenyl, -C(=CH 2 )CH 3 , -C≡C-CH 3 , -CH=C(CH 3 ) 2 , X is an alkylene, -C(O)CH 2 - or -C(O)N(R 2 )CH 2 -; R 14 is H or a halogen or an optionally substituted alkyl; Y, Z, Q, Q 1 , m, n, R 2 , R 3 , R 4 , R 6 , R 7 and R 8 are each a specific group, number, etc. COPYRIGHT: (C)2009,JPO&INPIT
摘要翻译：待解决的问题：提供腺苷A 2a 受体拮抗剂。解决方案：公开了具有结构式（I）的化合物或其药学上可接受的盐，其用于治疗帕金森病的药物和含有它们的药物组合物。其中R是任选取代的苯基或杂芳基，环烯基，-C（= CH）2 CH 3，-S≡C-CH 3， SB>，-CH = C（CH 3 SB 3）SB 2，X是亚烷基，-C（O）CH 2 SB-或-C （O）N（R 2 ）CH 2 - ; R 14是H或卤素或任选取代的烷基; Y，Z，Q，Q 1 ，m，n，R 2 ，R 3， R 6 ，R 7 和R 8 分别是特定组，数字等。

6. 发明专利

DE602006019911D1 MGLUR1-ANTAGONISTEN ALS THERAPEUTISCHE WIRKSTOFFE 未知
公开(公告)号：DE602006019911D1
公开(公告)日：2011-03-10
申请号：DE602006019911
申请日：2006-12-11
申请人： SCHERING CORP
发明人： MATASI JULIUS J , TULSHIAN DEEN , BURNETT DUANE A , WU WEN-LIAN , KORAKAS PETER , SILVERMAN LISA S , THAVALAKULAMGARA SASIKUMAR K , QIANG LI , DOMALSKI MARTIN S
IPC分类号： C07D495/14

7. 发明专利

CO6251257A2 DERIVADOS DE GUANINA POLICICLICOS Y SUS METODOS DE USO 未知
公开(公告)号：CO6251257A2
公开(公告)日：2011-02-21
申请号：CO09144826
申请日：2009-12-17
申请人： SCHERING CORP
发明人： TULSHIAN DEEN , GEISS WILLIAM B , MARTIN GREGORY S , LE VAN-DUC , HABER JR JAMES , MATASI JULIUS J , CZARNIECKI MICHAEL F
IPC分类号： A61K31/519 , A61P25/00 , C07D487/14
摘要： 1.- Un compuesto que tiene la fórmula:o una sal, solvato, éster o prodroga farmacéuticamenteaceptable de los mismos, en donde:R1 es alquilo-C1-C6 o alquilo-alquilen-O-C1-C6;R2 es alquilo, arilo, -alquilen-arilo, heterociclo alquilo oheteroarilo, cualquiera de las cuales puede estaropcionalmente sustituido por R5;R3 es alquilo, -alquilen-arilo, cicloalquilo, -alquilencicloalquiloo -alquileno-heterocicloalquilo, en donde ungrupo arilo, cicloalquilo o heterocicloalquilo puede estaropcionalmente sustituido con R7;cada aparición de R4 es independientemente H o alquilo-C1-C6, o ambos grupos R4 junto con el átomo de carbono alcual están unidos, se juntan para formar un grupocicloalquilo de 3 a 7 miembros, que se puedeopcionalmente fusionar con un anillo de benceno;R5 representa de 1 a 3 grupos, cada uno se seleccionóindependientemente de alquenilo, alquinilo, arilo,heterocicloalquilo, heteroarilo, halo, -CN, -C(O)OR6, -C(O)R6, -C(O)N(R6)2, -S(O)2NHR6, -OH, -Oalquilo,haloalquilo, -Ohaloalquilo y -NHC(O)N(R6)2, donde ungrupo arilo, heterocicloalquilo o heteroarilo puede estaropcionalmente sustituido con hasta 3 grupos, cada unoindependientemente seleccionado de alquilo-C1-C6, halo,-C(O)OR6 y -C(O)N(R6)2;cada aparición de R6 es independientemente H, alquilo-C1-C6, arilo o heterocicloalquilo, en donde un grupo arilo oheterocicloalquilo puede estar opcionalmente sustituido conhasta 3 grupos, cada uno independientementeseleccionado de alquilo, -Oalquilo, halo, -CN, haloalquilo,-alquilen-C(O)N(R8)2, -C(O)N(R8)2, -C(O)OR8,heterocicloalquil-C(O)-, alquil-C(O) o N(R8)2;R7 representa de 1 a 3 grupos, cada unoindependientemente seleccionado de alquilo -C1-C6, halo,arilo, -N(R8)2, -C(O)OR8, -C(O)N(R8)2 y haloalquilo; ycada aparición de R8 es independientemente H, alquilo -C1-C6 o arilo.2.- El compuesto de la Reivindicación 1, en dondeR1 es alquilo-C1-C6.3.- El compuesto de la Reivindicación 2, en dondeR1 es metilo o etilo.4.- El compuesto de la Reivindicación 2, en dondeR2 es fenilo, que puede estar opcionalmente sustituido conR5.

8. 发明专利

CA2468681C ADENOSINE A2A RECEPTOR ANTAGONISTS 未知
公开(公告)号：CA2468681C
公开(公告)日：2011-01-25
申请号：CA2468681
申请日：2002-11-26
申请人： SCHERING CORP
发明人： MATASI JULIUS J , CALDWELL JOHN P , TULSHIAN DEEN , SILVERMAN LISA S , NEUSTADT BERNARD R
IPC分类号： C07D487/04 , A61K31/505 , A61K31/519 , A61K31/5377 , A61K45/00 , A61P25/00 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/28 , A61P43/00
摘要： This invention relates to compounds having the structural formula (I) or pharmaceutically acceptable salts or solvates thereof, wherein R, R2 and R3 are as defined in the specification, pharmaceutical compositions thereof, and methods of treating stroke or central nervous system diseases by administering the compound of the present invention to a patient in need of such treatment.

9. 发明专利

MX2010000098A DERIVADOS DE GUANINA POLICICLICOS Y SUS METODOS DE USO. 未知
公开(公告)号：MX2010000098A
公开(公告)日：2010-04-21
申请号：MX2010000098
申请日：2008-06-18
申请人： SCHERING CORP
发明人： TULSHIAN DEEN , LE VAN-DUC , GEISS WILLIAM B , MARTIN GREGORY S , HABER JAMES C JR , MATASI JULIUS J , CZARNIECKI MICHAEL F , COOKE STEPHANIE NICOLE
IPC分类号： C07D487/14 , A61K31/519 , A61P25/00
摘要： La presente invenci?n se refiere a derivados de guanina polic?clicos, composiciones que comprenden los derivados de guanina polic?clicos y los m?todos de uso de los derivados de guanina polic?clicos para tratar el dolor o una enfermedad inflamatoria.

10. 发明专利

ZA200404160B Adenosine A2A receptor antagonists. 未知
公开(公告)号：ZA200404160B
公开(公告)日：2005-04-08
申请号：ZA200404160
申请日：2004-05-27
申请人： SCHERING CORP
发明人： MATASI JULIUS J , TULSHIAN DEEN , NEUSTADT BERNARD R , CALDWELL JOHN P , SILVERMAN LISA S
IPC分类号： A61K31/519 , A61K31/5377 , A61K45/00 , A61P25/00 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/28 , A61P43/00 , C07D487/04 , C07D , A61K , A61P
摘要： Disclosed are compounds having the structural formula or pharmaceutically acceptable salts or solvates thereof, wherein R is optionally substituted heteroaryl, optionally substituted phenyl, cycloalkenyl, -C(-CH 2 )CH 3 , -C≡C-CH 3 , -CH-C(CH 3 ) 2 , or -CH-CH-CH 3 ; R 2 is -W-X, -NR 19 (CH 2 ) m -W-X, and -NR 19 CH(CH 3 )-W-X, or R 2 is alkyl, alkenyl and -NR 18 R 19 , each optionally substituted -W-X; R 3 is H, halo, alkyl, trifluoromethyl, alkoxy, alkoxyalkyl, hydroxyalkyl, alkylamino, alkylaminoalkyl, dialkylamino, dialkylaminoalkyl, aminoalkyl, aryl, heteroaryl, or CN; R 18 is a bond, -CH(OH)-, -CH(CH 3 )-, -C(CH 3 ) n -, -(CH 2 ) n -or -O(CH 2 ) n -; W is aryl or heteroaryl, each optionally substituted; X is H, NH 2 , or substituted amino, or X is -R 18 -Y-Z; and n, R 19 , Y and Z are as defined in the specification; pharmaceutical compositions thereof, and methods of treating stroke or central nervous system diseases by administering the compound of the present invention to a patient in need of such treatment.

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