公开(公告)号：WO2005007658A3

公开(公告)日：2005-06-16

申请号：PCT/US2004022417

申请日：2004-07-13

Applicant: ARENA PHARM INC ,  JONES ROBERT M ,  SEMPLE GRAEME ,  XIONG YIFENG ,  SHIN YOUNG-JUN ,  REN ALBERT S ,  CALDERON IMELDA ,  FIORAVANTI BEATRIZ ,  CHOI JIN SUN KAROLINE ,  SAGE CARLTON R

Inventor： JONES ROBERT M ,  SEMPLE GRAEME ,  XIONG YIFENG ,  SHIN YOUNG-JUN ,  REN ALBERT S ,  CALDERON IMELDA ,  FIORAVANTI BEATRIZ ,  CHOI JIN SUN KAROLINE ,  SAGE CARLTON R

IPC: A61P3/00 ,  A61P3/10 ,  C07D215/22 ,  C07D215/233 ,  C07D471/04 ,  C07D473/00 ,  C07D487/04 ,  C07D498/04 ,  A61K31/4375 ,  A61K31/47 ,  A61K31/519 ,  A61K31/52

CPC classification number: C07D215/233 ,  C07D471/04 ,  C07D473/00 ,  C07D487/04

Abstract: The present invention relates to certain fused aryl and heteroaryl derivatives of Formula (I) that are modulators of metabolism. Accordingly, compounds of the present invention are useful in the prophylaxis or treatment of metabolic disorders and complications thereof, such as, diabetes and obesity.

Abstract translation: 本发明涉及作为代谢调节剂的式（I）的某些稠合芳基和杂芳基衍生物。 因此，本发明化合物可用于预防或治疗代谢紊乱及其并发症，例如糖尿病和肥胖症。

公开(公告)号：WO2005051937A2

公开(公告)日：2005-06-09

申请号：PCT/US2004/038920

申请日：2004-11-18

Applicant: ARENA PHARMACEUTICALS, INC. ,  JUNG, Jae-Kyu ,  SEMPLE, Graeme ,  JOHNSON, Benjamin R.

Inventor： JUNG, Jae-Kyu ,  SEMPLE, Graeme ,  JOHNSON, Benjamin R.

IPC: C07D307/68

CPC classification number: C07D307/68 ,  C07D405/04 ,  C07D409/04 ,  C07D409/10

Abstract: System for selecting a colour shade comprising a very small number of colour dis­play cards with mixed shades of two or more colours. The system comprises means for selecting one shade among mixed shades, means for presenting the selected mixed shade as well as means for specifying the selected mixed shade for making paint in the desired colour tone.

Abstract translation: 用于选择颜色的系统，其包括具有两种或更多种颜色的混合色调的非常少量的彩色显示卡。 该系统包括用于选择混合色调中的一个色调的装置，用于呈现所选择的混合色调的装置以及用于指定所选择的混合色调以用于制作所需色调的油漆的装置。

公开(公告)号：WO2005044816A1

公开(公告)日：2005-05-19

申请号：PCT/US2004/035927

申请日：2004-10-29

Applicant: ARENA PHARMACEUTICALS, INC. ,  MERCK & CO., INC. ,  SEMPLE, Graeme ,  SCHRADER, Thomas ,  SKINNER, Philip, J. ,  COLLETTI, Steven, L. ,  GHARBAOUI, Tawfik ,  IMBRIGLIO, Jason, E. ,  JUNG, Jae-Kyi ,  LIANG, Rui ,  RAGHAVAN, Subharekha ,  SCHMIDT, Darby ,  TATA, James, R.

Inventor： SEMPLE, Graeme ,  SCHRADER, Thomas ,  SKINNER, Philip, J. ,  COLLETTI, Steven, L. ,  GHARBAOUI, Tawfik ,  IMBRIGLIO, Jason, E. ,  JUNG, Jae-Kyi ,  LIANG, Rui ,  RAGHAVAN, Subharekha ,  SCHMIDT, Darby ,  TATA, James, R.

IPC: C07D403/04

CPC classification number: C07D491/04 ,  C07D403/04 ,  C07D495/04

Abstract: The present invention relates to certain tetrazole derivatives of Formula (I), and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists for the RUP25 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of α-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers and the like.

Abstract translation: 本发明涉及式（I）的某些四唑衍生物及其药学上可接受的盐，其表现出有用的药理学性质，例如作为RUP25受体的激动剂。 本发明还提供含有本发明化合物的药物组合物，以及使用本发明化合物和组合物治疗代谢相关疾病包括血脂异常，动脉粥样硬化，冠心病，胰岛素抵抗，2型糖尿病 ，综合征-X等。 此外，本发明还提供本发明化合物与其它活性剂如属于α-葡糖苷酶抑制剂类，醛糖还原酶抑制剂，双胍类，HMG-CoA还原酶抑制剂，角鲨烯合成 抑制剂，贝特类，LDL分解代谢增强剂，血管紧张素转换酶（ACE）抑制剂，胰岛素分泌增强剂等。

公开(公告)号：WO2005011677A1

公开(公告)日：2005-02-10

申请号：PCT/US2004/018389

申请日：2004-06-10

Applicant: ARENA PHARMACEUTICALS, INC. ,  SEMPLE, Graeme ,  GHARBAOUI, Tawfik ,  SHIN, Young-Jun ,  DECAIRE, Marc ,  AVERBUJ, Claudia ,  SKINNER, Philip, J.

Inventor： SEMPLE, Graeme ,  GHARBAOUI, Tawfik ,  SHIN, Young-Jun ,  DECAIRE, Marc ,  AVERBUJ, Claudia ,  SKINNER, Philip, J.

IPC: A61K31/415

CPC classification number: C07D231/14 ,  A61K31/415 ,  A61K45/06 ,  A61K2300/00

Abstract: The present invention relates to certain pyrazole carboxylic acid and ester derivatives, and pharmaceutically acceptable salts thereof, which exhibit useful pharmaceutical properties, for example as agonists for the RUP25 receptor. (I) Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the prophylaxis or treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of α -glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers and the like.the substituents are defined in claim 1.

Abstract translation: 本发明涉及表现出有用的药物性质的某些吡唑羧酸和酯衍生物及其药学上可接受的盐，例如作为RUP25受体的激动剂。 （I）本发明还提供含有本发明化合物的药物组合物，以及使用本发明化合物和组合物预防或治疗代谢相关疾病包括血脂异常，动脉粥样硬化，冠心病，胰岛素 抗性，2型糖尿病，综合征等。 此外，本发明还提供本发明化合物与其它活性剂如属于α-葡糖苷酶抑制剂类，醛糖还原酶抑制剂，双胍类，HMG-CoA还原酶抑制剂，角鲨烯合成 抑制剂，贝特类，LDL分解代谢增强剂，血管紧张素转换酶（ACE）抑制剂，胰岛素分泌增强剂等。取代基如权利要求1中所定义。

公开(公告)号：WO2005007647A1

公开(公告)日：2005-01-27

申请号：PCT/US2004/022327

申请日：2004-07-09

Applicant: ARENA PHARMACEUTICALS, INC. ,  JONES, Robert, M. ,  SEMPLE, Graeme ,  XIONG, Yifeng ,  SHIN, Young-Jun ,  REN, Albert, S. ,  CALDERON, Imelda ,  CHOI, Jin, Sun, Karoline ,  FIORAVANTI, Beatriz ,  LEHMANN, Juerg ,  BRUCE, Marc, A.

Inventor： JONES, Robert, M. ,  SEMPLE, Graeme ,  XIONG, Yifeng ,  SHIN, Young-Jun ,  REN, Albert, S. ,  CALDERON, Imelda ,  CHOI, Jin, Sun, Karoline ,  FIORAVANTI, Beatriz ,  LEHMANN, Juerg ,  BRUCE, Marc, A.

IPC: C07D401/12

CPC classification number: C07D239/52 ,  C07D239/54 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention relates to certain trisubstituted aryl and heteroaryl derivatives of Formula (I) that are modulators of metabolism. Accordingly, compounds of the present invention are useful in the prophylaxis or treatment of metabolic disorders and complications thereof, such as, diabetes and obesity.

Abstract translation: 本发明涉及作为代谢调节剂的式（I）的某些三取代芳基和杂芳基衍生物。 因此，本发明的化合物可用于预防或治疗代谢紊乱及其并发症，例如糖尿病和肥胖症。

公开(公告)号：WO2004065380A1

公开(公告)日：2004-08-05

申请号：PCT/US2004/001267

申请日：2004-01-14

Applicant: ARENA PHARMACEUTICALS INC. ,  JONES, Robert, M. ,  SEMPLE, Graeme ,  FIORAVANTI, Beatriz ,  PEREIRA, Guilherme ,  CALDERON, Imelda ,  UY, Jane ,  DUVVURI, Kameshwari ,  CHOI, Jin Sun Karoline ,  XIONG, Yifeng ,  DAVE, Vibha

Inventor： JONES, Robert, M. ,  SEMPLE, Graeme ,  FIORAVANTI, Beatriz ,  PEREIRA, Guilherme ,  CALDERON, Imelda ,  UY, Jane ,  DUVVURI, Kameshwari ,  CHOI, Jin Sun Karoline ,  XIONG, Yifeng ,  DAVE, Vibha

IPC: C07D401/14

CPC classification number: C07D213/68 ,  C07D213/79 ,  C07D239/34 ,  C07D239/50 ,  C07D295/096 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D409/14 ,  C07D411/14 ,  C07D413/14 ,  C07D417/14 ,  C07D419/14

Abstract: The present invention relates to certain 1,2,3-trisubstituted aryl and heteroaryl derivatives of Fomula (Ia) that are modulators of metabolism. Accordingly, compounds of the present invention are useful in the prophylaxis or treatment of metabolic disorders and complications thereof, such as, diabetes and obesity.

Abstract translation: 本发明涉及作为代谢调节剂的式（Ia）的某些1,2,3-三取代的芳基和杂芳基衍生物。 因此，本发明化合物可用于预防或治疗代谢紊乱及其并发症，例如糖尿病和肥胖症。

公开(公告)号：WO2004032928A1

公开(公告)日：2004-04-22

申请号：PCT/US2003/032174

申请日：2003-10-09

Applicant: ARENA PHARMACEUTICALS, INC. ,  SEMPLE, Graeme ,  AVERBUJ, Claudia ,  SKINNER, Philip ,  GHARBAOUI, Tawfik ,  SHIN, Young-Jun

Inventor： SEMPLE, Graeme ,  AVERBUJ, Claudia ,  SKINNER, Philip ,  GHARBAOUI, Tawfik ,  SHIN, Young-Jun

IPC: A61K31/45

CPC classification number: C07D231/16 ,  C07D231/14

Abstract: The present invention relates to certain pyrazole carboxylic acid derivatives of Formula (Ia), and pharmaceutically acceptable salts thereof, as antilipolytic agents and against for the receptor RUP25, wherein: R 2 is H, halogen, C 1-12 alkyl or C 1-12 haloalkyl; and R 3 is C 3-6 cycloalkyl, C 1-12 alkyl, C 1-12 haloalkyl, C 3-6 cycloalkyl-C 1-4 -alkylene, aryl-C 1-4 -alkylene or heteroaryl-C 1-4 -alkylene, wherein said aryl-C 1-4 -alkylene and heteroaryl-C 1-4 -alkylene can be optionally substituted 1 to 5 substituents selected from the substituents listed in the claims. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for pharmaceutical compositions in combination with other active agents, for example, those agents belonging to the class of α-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers, thiazolidinedione and the like.

Abstract translation: 本发明涉及某些式（Ia）的吡唑羧酸衍生物及其药学上可接受的盐，作为抗脂解剂和抗受体RUP25，其中：R2是H，卤素，C1-12烷基或C1-12卤代烷基; 且R 3为C 3-6环烷基，C 1-12烷基，C 1-12卤代烷基，C 3-6环烷基-C 1-4亚烷基，芳基-C 1-4亚烷基或杂芳基-C 1-4 - 亚烷基，其中所述芳基-C1 -4-亚烷基和杂芳基-C 1-4 - 亚烷基可以是任选取代的1至5个选自权利要求中所列取代基的取代基。 本发明还提供含有本发明化合物的药物组合物，以及使用本发明化合物和组合物治疗代谢相关疾病包括血脂异常，动脉粥样硬化，冠心病，胰岛素抵抗，2型糖尿病 ，综合征-X等。 此外，本发明还提供了与其它活性剂（例如属于α-葡糖苷酶抑制剂，醛糖还原酶抑制剂，双胍类，HMG-CoA还原酶抑制剂，角鲨烯合成抑制剂，贝特类）的那些试剂组合的药物组合物 ，LDL分解代谢增强剂，血管紧张素转换酶（ACE）抑制剂，胰岛素分泌增强剂，噻唑烷二酮等。

公开(公告)号：WO1995006041A1

公开(公告)日：1995-03-02

申请号：PCT/GB1994001858

申请日：1994-08-25

Applicant: YAMANOUCHI PHARMACEUTICAL CO. LTD. ,  FERRING RESEARCH LTD. ,  SEMPLE, Graeme ,  RYDER, Hamish ,  SZELKE, Michael ,  SATOH, Masato ,  OHTA, Mitsuaki ,  MIYATA, Keiji ,  NISHIDA, Akito

Inventor： YAMANOUCHI PHARMACEUTICAL CO. LTD. ,  FERRING RESEARCH LTD.

IPC: C07D243/24

CPC classification number: C07D401/04 ,  C07D243/24

Abstract: A benzodiazepine derivative of formula (I), or a pharmaceutically acceptable salt thereof, wherein (a) R is selected from alkyl or cycloalkyl groups, (b) R is a tertiary cyclic amino substituent of structure (II), (III) or (IV), in which a is 1-6; (c) X is either CH or N. These compounds are gastrin and/or CCK-B receptor antagonists.

Abstract translation: 式（I）的苯并二氮杂衍生物或其药学上可接受的盐，其中（a）R 1选自烷基或环烷基，（b）R 2是结构（II）的叔环氨基取代基， ，（III）或（IV），其中a为1-6; （c）X是CH或N.这些化合物是胃泌素和/或CCK-B受体拮抗剂。

公开(公告)号：WO9320099A3

公开(公告)日：1993-11-25

申请号：PCT/GB9300614

申请日：1993-03-25

Applicant: FERRING BV ,  YAMANOUCHI PHARMA CO LTD ,  RYDER HAMISH ,  KENDRICK DAVID ALAN ,  SEMPLE GRAEME ,  MIYATA KEIJI ,  BATT ANDRZEJ ROMAN ,  MATHEWS ELIZABETH ALICE ,  ROOKER DAVID PHILIP ,  NISHIDA AKITO

Inventor： RYDER HAMISH ,  KENDRICK DAVID ALAN ,  SEMPLE GRAEME ,  MIYATA KEIJI ,  BATT ANDRZEJ ROMAN ,  MATHEWS ELIZABETH ALICE ,  ROOKER DAVID PHILIP ,  NISHIDA AKITO

IPC: A61K38/00 ,  C07D207/08 ,  C07D209/18 ,  C07D217/14 ,  C07D401/12 ,  C07K5/02 ,  C07K5/06 ,  C07K5/078 ,  C07K5/097 ,  C07K5/117 ,  A61K37/43 ,  C07D217/12 ,  C07D403/12 ,  C07K5/08

CPC classification number: C07D207/08 ,  A61K38/00 ,  C07D209/18 ,  C07D217/14 ,  C07D401/12 ,  C07K5/0202 ,  C07K5/0205 ,  C07K5/06078 ,  C07K5/06139 ,  C07K5/06156 ,  C07K5/0821 ,  C07K5/1024

Abstract: This invention relates to novel compounds with the general structure A-B-C and their pharmaceutically acceptable salts, to medicinal compositions containing them, and to the use of such medicinal compositions in the treatment of certain disease states. The compounds of the invention are represented schematically as A-B-C wherein S1-S4 are in general lypophilic residues, S5 is a polar or hydrophilic residue, and L1-L5 are optional linking units. The compounds of this invention bind to CCK and/or gastrin receptors with high affinity and are therefore useful in the treatment of diseases which involve the dysfunction of a physiological process regulated by either of these hormones.

公开(公告)号：WO1993020099A2

公开(公告)日：1993-10-14

申请号：PCT/GB1993000614

申请日：1993-03-25

Applicant: FERRING B.V. ,  YAMANOUCHI PHARMACEUTICAL CO. LTD. ,  RYDER, Hamish ,  KENDRICK, David, Alan ,  SEMPLE, Graeme ,  MIYATA, Keiji ,  BATT, Andrzej, Roman ,  MATHEWS, Elizabeth, Alice ,  ROOKER, David, Philip ,  NISHIDA, Akito ,  AZUZAWA, Shinobu ,  SZELKE, Michael

Inventor： FERRING B.V. ,  YAMANOUCHI PHARMACEUTICAL CO. LTD.

IPC: C07K05/02

CPC classification number: C07D207/08 ,  A61K38/00 ,  C07D209/18 ,  C07D217/14 ,  C07D401/12 ,  C07K5/0202 ,  C07K5/0205 ,  C07K5/06078 ,  C07K5/06139 ,  C07K5/06156 ,  C07K5/0821 ,  C07K5/1024

Abstract: This invention relates to novel compounds with the general structure A-B-C and their pharmaceutically acceptable salts, to medicinal compositions containing them, and to the use of such medicinal compositions in the treatment of certain disease states. The compounds of the invention are represented schematically as A-B-C wherein S -S are in general lypophilic residues, S is a polar or hydrophilic residue, and L -L are optional linking units. The compounds of this invention bind to CCK and/or gastrin receptors with high affinity and are therefore useful in the treatment of diseases which involve the dysfunction of a physiological process regulated by either of these hormones.

Abstract translation: 本发明涉及具有一般结构A-B-C及其药学上可接受的盐的新化合物与含有它们的药物组合物，以及这些药物组合物在治疗某些疾病状态中的用途。 本发明的化合物示意性地表示为ABC，其中S 1 -S 4通常为亲水性残基，S 5为极性或亲水性残基，L 1 -L 5为任选连接 单位。 本发明的化合物以高亲和力结合CCK和/或胃泌素受体，因此可用于治疗涉及由这些激素调节的生理过程的功能障碍的疾病。