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11. 发明专利

JP2010254719A Substituted azetidinone compound, formulation and use thereof for treatment of hypercholesterolemia 审中-公开
标题翻译：替代AZETIDINONE化合物，用于治疗高脂血症的制剂及其用途
公开(公告)号：JP2010254719A
公开(公告)日：2010-11-11
申请号：JP2010181957
申请日：2010-08-16
申请人： Schering Corp , シェーリングコーポレイションSchering Corporation
发明人： BURNETT DUANE A , CLADER JOHN W
IPC分类号： C07D405/12 , A61K31/397 , A61K31/4025 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/00 , A61P25/00 , A61P25/28 , C07D405/14
CPC分类号： C07D405/12 , C07D405/14 , Y10S930/28
摘要： PROBLEM TO BE SOLVED: To provide a compound for treatment of hypercholesterolemia. SOLUTION: The invention provides the azetidinone compound of formula (I), a formulation and a method for preparing the same which can be useful for treating vascular conditions (for example, atherosclerosis or hypercholesterolemia), diabetes, obesity, stroke, demyelination, and for lowering plasma levels of sterols and/or stanols in a subject. The compound of formula (I) can form a sterol absorption inhibitor compound and/or a stanol absorption inhibitor compound, and a sterol biosynthesis inhibitor compound by being metabolized in vivo. COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：待解决的问题：提供治疗高胆固醇血症的化合物。解决方案：本发明提供式（I）的氮杂环丁酮化合物，其可用于治疗血管疾病（例如动脉粥样硬化或高胆固醇血症），糖尿病，肥胖症，中风，脱髓鞘的制剂及其制备方法，并用于降低受试者中甾醇和/或甾烷醇的血浆水平。式（I）化合物可以通过体内代谢形成甾醇吸收抑制剂化合物和/或甾烷醇吸收抑制剂化合物和甾醇生物合成抑制剂化合物。版权所有（C）2011，JPO＆INPIT

12. 发明专利

JP2009256390A Piperidine-based mch antagonist for treatment of obesity and cns disorders 审中-公开
标题翻译：基于哌啶的MCH拮抗剂治疗肥胖和CNS病症
公开(公告)号：JP2009256390A
公开(公告)日：2009-11-05
申请号：JP2009187565
申请日：2009-08-12
申请人： Schering Corp , シェーリングコーポレイションSchering Corporation
发明人： BURNETT DUANE A , WU WEN-LIAN
IPC分类号： C07D211/58 , A61K31/445 , A61K31/4523 , A61K31/4525 , A61K31/453 , A61K31/4535 , A61K31/454 , A61P1/14 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P5/50 , A61P9/12 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P43/00 , C07D211/34 , C07D211/52 , C07D211/96 , C07D401/04 , C07D401/06 , C07D401/08 , C07D401/10 , C07D405/04 , C07D405/06 , C07D405/08 , C07D409/04 , C07D409/06 , C07D409/14 , C07D417/06
CPC分类号： C07D401/04 , C07D211/34 , C07D211/52 , C07D211/58 , C07D211/96 , C07D401/06 , C07D401/10 , C07D405/04 , C07D405/06 , C07D409/04 , C07D409/06 , C07D409/14 , C07D417/06
摘要： PROBLEM TO BE SOLVED: To provide antagonists for melanin-concentrating hormone (MCH), use of them in treatment of obesity, eating disorders, diabetes, pharmacological compositions comprising such compounds, as well as methods of treatment using the compounds. SOLUTION: There are provided new antagonists for melanin-concentrating hormone (MCH) represented by a specific formula disclosed in the specification, use of them in treatment of obesity, eating disorders, and diabetes, the pharmacological compositions comprising such compounds, and the treating methods of using them. COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：要解决的问题：为了提供黑色素浓缩激素（MCH）的拮抗剂，使用它们来治疗肥胖症，进食障碍，糖尿病，包含这些化合物的药物组合物，以及使用该化合物的治疗方法。解决方案：提供了由说明书中公开的具体公式表示的黑色素浓缩激素（MCH）的新拮抗剂，其用于治疗肥胖症，进食障碍和糖尿病，包含这些化合物的药物组合物，以及使用它们的治疗方法。版权所有（C）2010，JPO＆INPIT

13. 发明专利

JP2010047618A 2-substituted benzimidazole derivative as selective melanin concentrating hormone receptor antagonist for treatment of obesity and related disorder 审中-公开
标题翻译： 2-取代的苯并咪唑衍生物作为选择性的麦芽宁浓缩激素受体拮抗剂治疗肥胖和相关疾病
公开(公告)号：JP2010047618A
公开(公告)日：2010-03-04
申请号：JP2009275958
申请日：2009-12-03
申请人： Schering Corp , シェーリングコーポレイションSchering Corporation
发明人： WU WEN-LIAN , BURNETT DUANE A , CAPLEN MARY ANN
IPC分类号： C07D401/06 , A61K31/454 , A61K45/00 , A61P1/16 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/10 , A61P9/12 , A61P35/00 , A61P43/00 , C07D401/08 , C07D401/14 , C07D417/14
CPC分类号： C07D401/06 , C07D401/14 , C07D417/14
摘要： PROBLEM TO BE SOLVED: To provide new biaryl-piperidin-4-ylidene-methylbenzimidazole derivatives with antagonists activity for MCH (melanin-concentrating hormone). SOLUTION: There are disclosed the compounds represented by formula (I) wherein Ar, X, R 1 and R 11 are specifically defined, the compounds being new antagonists for MCH, as well as methods for preparing such compounds. In another embodiment, there are disclosed pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes. COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：要解决的问题：提供具有MCH（黑色素浓缩激素）拮抗剂活性的新的联芳基 - 哌啶-4-亚基 - 甲基苯并咪唑衍生物。解决方案：公开了由式（I）表示的化合物，其中Ar，X，R 11，R 11和R 11是特异性定义的，该化合物是新的拮抗剂 MCH，以及制备这些化合物的方法。在另一个实施方案中，公开了包含这样的MCH拮抗剂的药物组合物以及使用它们治疗肥胖，代谢紊乱，进食障碍如食欲过盛和糖尿病的方法。版权所有（C）2010，JPO＆INPIT

14. 发明专利

CA2490531C SPIROSUBSTITUTED PIPERIDINES AS SELECTIVE MELANIN CONCENTRATING HORMONE RECEPTOR ANTAGONISTS FOR THE TREATMENT OF OBESITY 未知
公开(公告)号：CA2490531C
公开(公告)日：2011-03-22
申请号：CA2490531
申请日：2003-06-26
申请人： SCHERING CORP
发明人： BURNETT DUANE A , WU WEN-LIAN , SASIKUMAR THAVALAKULAM K , DOMALSKI MARTIN S
IPC分类号： C07D471/10 , A61K31/438 , A61K45/00 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/12 , A61P25/00
摘要： The present invention discloses compounds according to formula which are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.

15. 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

16. 发明专利

ES2326980T3 AMINOBENZIMIDAZOLES UTILES COMO ANTAGONISTAS SELECTIVOS DEL RECEPTOR DE LA HORMONA CONCENTRADA DE MELAMINA (MCH) PARA EL TRATAMIENTO DE LA OBESIDAD Y DESORDENES ASOCIADOS. 未知
公开(公告)号：ES2326980T3
公开(公告)日：2009-10-22
申请号：ES04789487
申请日：2004-09-30
申请人： SCHERING CORP
发明人： SASIKUMAR THAVALAKULAMGARA K , BURNETT DUANE A
IPC分类号： A61K31/4184 , A61P3/04 , C07D235/30 , C07D401/12 , C07D403/12
摘要： Un compuesto representado por la fórmula estructural ** ver fórmula** o una de sus sales o solvatos farmacéuticamente aceptables, donde la línea discontinua en ** ver fórmula** representa (i) un enlace opcional que puede estar presente o ausente, y si está presente, forma un enlace doble con el enlace sencillo adyacente, o (ii) -C(R 5 R 8 )-, -C(R 5 R 8 )-C(R 5 R 8 )- o -C(R 11 R 12 ); m es 1, 2, 3 o 4; n es 0, 1 o 2; p es 0, 1 o 2; Ar es arilo, heteroarilo, arilo sustituido con R 4 o heteroarilo sustituido con R 4 ; Z es -NR 5 R 6 , -NR 5 C(O)R 3 , -C(O)NR 5 R 6 , -NR 5 C(O)NR 5 R 6 , -NR 5 C(O)OR 3 , -NR 5 S(O2)R 3 , -S(O2)NR 5 R 6 , -S(O2)R 3 , -C(O)R 3 , -C(O)OR 6 , -OH, alcoxi, **ver fórmula** o ** ver fórmula** R 1 es 1 a cuatro radicales, cada R 1 se selecciona independientemente del grupo que consiste en hidrógeno, -OH, halógeno, alquilo, alcoxi, -OCF3, -CF3 o -CN, o dos radicales R1 en carbonos adyacentes del anillo se pueden unir entre sí para formar un grupo metilendioxi o etilendioxi; R 2 es hidrógeno, alquilo, alquilo sustituido con R 10 , cicloalquilo, cicloalquilo sustituido con R 10 , aralquilo, heterociclilo, -C(O)R 3 , -S(O2)R 3 o -C(O)NR 5 R 6 ; R 3 es alquilo, arilo, aralquilo, heteroarilo, aralquilo sustituido con R 4 , arilo sustituido con R 4 o heteroarilo sustituido con R 4 ; R 4 es de 1 a 5 radicales, cada R 4 se selecciona independientemente del grupo que consiste en hidrógeno, heterociclilo, heterociclilo sustituido con R 9 , heterociclilalquil-, heterociclilalquilo sustituido con R 9 , -OH, -alcoxi, -OCF 3, -CN, alquilo, halógeno, -NR 5 R 6 , -NR 5 C(O)R 7 , -C(O)NR 5 R 8 , -NR 5 S(O 2)R 7 , -S(O 2) NR 5 R 6 , -S(O2)R 7 , -COR 7 , -C(O)OR 5 , CF3, -(alquilen)NR 5 R 6 , -(alquilen)NR 6 C(O)R 7 , -(alquilen)NR 6 S(O2) R 7 , -(alquilen)-NR 5 C(O)NR 5 R 6 , -(alquilen)NR 5 C(O)OR 7 , CHO, -C=(NOR 5 ) y ** ver fórmula** R 5 es hidrógeno o alquilo; R 6 es hidrógeno, alquilo, arilo, aralquilo o heteroarilo; R 7 es alquilo; arilo, aralquilo o heteroarilo; R 8 es hidrógeno o alquilo; R 9 es alquilo, -OH o hidroxialquilo; R 10 es alcoxi, halógeno, -C(O)NR 5 R 6 , -C(O)OR 6 , -NR 5 R 6 o -OH; R 11 es hidrógeno o halógeno; y R 12 es hidrógeno o halógeno.

18. 发明专利

PE20090435A1 INHIBIDORES DE TETRAHIDROPIRANOCROMENO DE GAMMA SECRETASA 未知
公开(公告)号：PE20090435A1
公开(公告)日：2009-04-18
申请号：PE2008001121
申请日：2008-07-02
申请人： SCHERING CORP
发明人： BARA THOMAS A , BURNETT DUANE A , CLADER JOHN W , DOMALSKI MARTIN S , JIN YAN , JOSIEN HUBERT B , LI HONGMEI , LIANG XIAN , PISSARNITSKI DMITRI , SASIKUMAR TRAVALAKULAMGARA K , WONG JESSE K , XU RUO , ZHAO ZHIQIANG , MCNAMARA PAUL E , WU WEN-LIAN
IPC分类号： A61K31/35 , A61K31/352 , A61P25/28 , C07D311/78 , C07D407/12 , C07D493/04
摘要： REFERIDA A UN COMPUESTO DE FORMULA (I), DONDE X ES N, CH2; R1 ES -ALQUILEN-SO2-ALQUILO(C1-C6), -ALQUILEN-SO2-HALOALQUILO(C1-C6), ALQUILEN-(1,1-DIOXIDO DE TETRAHIDROTIOFENO), ENTRE OTROS; R2 ES H, ALQUILO; Ar ES ARILO, HETEROARILO, ARILO SUSTITUIDO CON UNO O MAS L1A, ENTRE OTROS; L1A ES HALOGENO, ALQUILO, -CN, CF3, -O-(HALOALQUILO(C1-C6)), ENTRE OTROS; L1 ES HALOGENO, -CN, -CF3, -O-ALQUILO(C1-C6), -C(O)-O-ALQUILO(C1-C6), ALQUILEN-OH, ENTRE OTROS; n ES 0-3. SON COMPUESTOS PREFERIDOS: (a), (b), ENTRES OTROS. SE REFIERE TAMBIEN UN PROCEDIMIENTO DE PREPARACION Y A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDRORES DE GAMMA-SECRETASA, UTILES EN EL TRATAMIENTO DE ENFERMEDADES NEURODEGENERATIVAS, ENFERMEDAD DE ALZHEIMER E INHIBIENDO EL DEPOSITO DE PROTEINA AMIELOIDE EN, SOBRE O ALREDEDOR DEL TEJIDO NEUROLOGICO

19. 发明专利

PE04472009A1 BENCENSULFONIL-CROMANO, TIOCROMANO, TETRAHIDRONAFTALENO E INHIBIDORES RELACIONADOS DE LA GAMMA SECRETASA 未知
公开(公告)号：PE04472009A1
公开(公告)日：2009-04-18
申请号：PE0011842008
申请日：2008-07-15
申请人： SCHERING CORP
发明人： SASIKUMAR THAVALAKULAMGARA K , BURNETT DUANE A , ASBEROM THEODROS , WU WEN-LIAN , XU RUO , LI HONGMEI , JOSIEN HUBERT B
IPC分类号： A61K31/35 , A61K31/519 , A61K31/54 , A61K31/542 , C07D491/04
CPC分类号： C07D493/04 , C07D491/04 , C07D513/04 , C07D513/14
摘要： SE REFIERE A UN COMPUESTO DE FORMULA 1, DONDE X ES -O-, -S-, -S(O2)-, ENTRE OTROS; ----ES ENLACE OPCIONAL; Y, Z SON CADA UNO N, C; Q ES ANILLO DE 5-8 MIEMBROS FUSIONADOS CON A1 Y Q1; Q1 ES ANILLO DE 5-7 MIEMBROS CON UN HETEROATOMO SLEECIONADO DE N, O, S(O) Y S(O2) FUSIONADO CON Q; L1 ES HALOGENO, ALQUILO, -CN, -CF3, -O-(ALQUILO C1-C6), ENTRE OTROS; Ar ES ARILO SUSTITUIDO O NO, HETEROARILO SUSTITUIDO O NO. UN COMPUESTO PREFERIDO ES (5aR,13aS)-11bR-[(4-CLOROFENIL)SULFONIL]-8,11-DIFLUORO-2,3,5a,6,11b,12,13,13a-OCTAHIDRO[1]BENZOPIRANO[4',3':5,6]PIRIDO[1,2-c]PIRIMIDIN-4(1H)-ONA. DICHOS COMPUESTOS SON INHIBIDORES DE GAMMA SECRETASA UTILES EN EL TRATAMIENTO DE ALZHEIMER

20. 发明专利

CA2700964A1 GAMMA SECRETASE MODULATORS 未知
公开(公告)号：CA2700964A1
公开(公告)日：2009-04-09
申请号：CA2700964
申请日：2008-09-25
申请人： SCHERING CORP
发明人： ZHU ZHAONING , GREENLEE WILLIAM J , CALDWELL JOHN P , MAZZOLA ROBERT D JR , MCKITTRICK BRIAN , BENNETT CHAD E , BURNETT DUANE A
IPC分类号： C07D233/76 , A61K31/4178 , A61P25/28 , C07D233/86 , C07D233/88 , C07D403/04
摘要： In its many embodiments, the present invention provides a novel class of 5-membered, nitrogen-containing heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.

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