公开(公告)号：WO03045918A8

公开(公告)日：2005-03-17

申请号：PCT/US0237956

申请日：2002-11-25

Applicant: SCHERING CORP

Inventor： BURNETT DUANE A ,  WU WEN-LIAN

IPC: 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 ,  C07D211/58 ,  C07D211/96 ,  C07D401/04 ,  C07D401/06 ,  C07D401/08 ,  C07D401/10 ,  C07D405/04 ,  C07D405/06 ,  C07D405/08 ,  C07D409/04 ,  C07D409/06 ,  C07D409/14 ,  C07D417/06 ,  A61K31/451

CPC classification number: 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

Abstract: The present invention discloses compounds of formula I, 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.

Abstract translation: 本发明公开了作为黑色素浓缩激素（MCH）的新型拮抗剂的式I化合物，以及这些化合物的制备方法。 在另一个实施方案中，本发明公开了包含这样的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。

公开(公告)号：WO2007038209A3

公开(公告)日：2007-07-12

申请号：PCT/US2006036858

申请日：2006-09-21

Applicant: SCHERING CORP ,  BURNETT DUANE A ,  WU WEN-LIAN

Inventor： BURNETT DUANE A ,  WU WEN-LIAN

IPC: C07D513/22 ,  A61K31/519 ,  A61P29/00 ,  C07D495/14 ,  C07D495/22 ,  C07D498/22

CPC classification number: C07D495/14

Abstract: In its many embodiments, the present invention provides tetracyclic compounds of formula (I) or formula (II) (wherein the various moieties 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.

Abstract translation: 在其许多实施方案中，本发明提供了可用作代谢型谷氨酸受体（mGluR）拮抗剂的式（I）或式（II）（其中各种部分如本文所定义）的四环化合物，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，尿失禁和神经变性疾病如阿尔茨海默病的治疗方法。

公开(公告)号：WO2005035504A3

公开(公告)日：2005-06-30

申请号：PCT/US2004015760

申请日：2004-05-20

Applicant: SCHERING CORP ,  BURNETT DUANE A ,  GREENLEE WILLIAM J ,  MCKITTRICK BRIAN ,  SU JING ,  ZHU ZHAONING ,  SASIKUMAR THAVALAKULAMGARA K ,  MAZZOLA ROBERT ,  QIANG LI ,  YE YUANZAN

Inventor： BURNETT DUANE A ,  GREENLEE WILLIAM J ,  MCKITTRICK BRIAN ,  SU JING ,  ZHU ZHAONING ,  SASIKUMAR THAVALAKULAMGARA K ,  MAZZOLA ROBERT ,  QIANG LI ,  YE YUANZAN

IPC: C07D223/14 ,  C07D401/12 ,  C07D403/10 ,  C07D407/12

CPC classification number: C07D223/14

Abstract: The present invention provides compounds of formula (I), which, are novel antagonists for D1/D5 receptors as well as methods for preparing such compounds. In another embodiment, the invention provides pharmaceutical compositions comprising such D1/D5 receptor antagonists as well as methods of using them to treat CNS disorders, obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.

Abstract translation: 本发明提供式（I）化合物，其为D1 / D5受体的新型拮抗剂以及制备这些化合物的方法。 在另一个实施方案中，本发明提供了包含这种D1 / D5受体拮抗剂的药物组合物以及使用它们治疗CNS障碍，肥胖，代谢紊乱，进食障碍如食欲过盛和糖尿病的方法。

公开(公告)号：WO2008033468A3

公开(公告)日：2008-08-14

申请号：PCT/US2007019934

申请日：2007-09-13

Applicant: SCHERING CORP ,  BURNETT DUANE A ,  MCKITTRICK BRIAN

Inventor： BURNETT DUANE A ,  MCKITTRICK BRIAN

IPC: C07D487/10 ,  A61K31/4747 ,  A61P3/06 ,  A61P25/02

CPC classification number: C07D487/10

Abstract: Disclosed are compounds of the formula (I), wherein Z 1 is -CH 2 - or -C(O)-, R 4 and R 5 are carbon chains (and optionally, together can form a C 2 bridge), u and v are independently an integer of 0-3 such that there sum is from 3 to 5, and R2 is heteroaryl, and R 1 and R 3 are as defined herein. Also disclosed are methods of treating pain, and methods of inhibiting the absorption of cholesterol using a compound of formula (I).

Abstract translation: 公开了式（I）的化合物，其中Z 1是-CH 2 - 或-C（O） - ，R 4和 R 5是碳链（并且可选地，一起可以形成C 2 H 2桥），u和v独立地是0-3的整数，使得总和为3 至5，且R 2为杂芳基，R 1和R 3如本文所定义。 还公开了治疗疼痛的方法，以及使用式（I）化合物抑制胆固醇吸收的方法。

公开(公告)号：WO2009008980A2

公开(公告)日：2009-01-15

申请号：PCT/US2008008192

申请日：2008-07-01

Applicant: SCHERING CORP ,  WU WEN-LIAN ,  BARA THOMAS A ,  BURNETT DUANE A ,  CLADER JOHN W ,  DOMALSKI MARTIN S ,  JIN YAN ,  JOSIEN HUBERT B ,  LI HONGMEI ,  LIANG XIAN ,  PISSARNITSKI DMITRI A ,  SASIKUMAR THAVALAKULAMGARA K ,  WONG JESSE K ,  XU RUO ,  ZHAO ZHIQIANG ,  MCNAMARA PAUL

Inventor： WU WEN-LIAN ,  BARA THOMAS A ,  BURNETT DUANE A ,  CLADER JOHN W ,  DOMALSKI MARTIN S ,  JIN YAN ,  JOSIEN HUBERT B ,  LI HONGMEI ,  LIANG XIAN ,  PISSARNITSKI DMITRI A ,  SASIKUMAR THAVALAKULAMGARA K ,  WONG JESSE K ,  XU RUO ,  ZHAO ZHIQIANG ,  MCNAMARA PAUL

IPC: C07D311/78 ,  A61K31/35 ,  A61K31/352 ,  A61P25/28 ,  C07D407/12 ,  C07D493/04

CPC classification number: C07D493/04 ,  C07D311/78 ,  C07D407/12

Abstract: Disclosed are novel gamma secretase inhibitors of the formula. Also disclosed are methods of inhibiting gamma-secretase, methods of treating neurodegenerative diseases, and methods of treating Alzheimer's Disease. Also disclosed are processes for preparing alkenes in one reaction step using a mixture of an aldehyde (or ketone) and an alkyl substituted with two electron withdrawing groups, and reacting the mixture with: (a) a sulfonyl halide (e.g., a sulfonyl chloride) and a basic tertiary amine, or, (b) a sulfonyl anhydride and a basic amine, or (c) an aryl-C(O)-halide and a basic tertiary amine, or (d) an aryl-C(O)-O-C(O)-aryl and a basic tertiary amine, or (e) an heteroaryl-C(O)-halide and a basic tertiary amine, or (f) a heteroaryl-C(O)-O-C(O)-heteroaryl and a basic tertiary amine.

Abstract translation: 公开了下式的新型γ分泌酶抑制剂。 还公开了抑制γ-分泌酶的方法，治疗神经退行性疾病的方法以及治疗阿尔茨海默氏病的方法。 还公开了使用醛（或酮）和被两个吸电子基团取代的烷基的混合物在一个反应​​步骤中制备烯烃的方法，并使该混合物与以下物质反应：（a）磺酰卤（例如磺酰氯） （b）磺酰基酸酐和碱性胺，或（c）芳基-C（O） - 卤化物和碱性叔胺，或（d）芳基-C（O） - OC（O） - 芳基和碱性叔胺，或（e）杂芳基-C（O） - 卤化物和碱性叔胺，或（f）杂芳基-C（O）-OC（O） - 杂芳基和 一种碱性叔胺。

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

Applicant: 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

Inventor： 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 classification number: C07D495/14

Abstract: 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.

Abstract translation: 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。

公开(公告)号：WO2008033464A3

公开(公告)日：2008-05-15

申请号：PCT/US2007019930

申请日：2007-09-13

Applicant: SCHERING CORP ,  ASLANIAN ROBERT G ,  BENNETT CHAD E ,  BURNETT DUANE A ,  CHAN TIN-YAU ,  KISELGOF EUGENIA Y ,  KNUTSON CHAD E ,  HARRIS JOEL M ,  MC KITTRICK BRIAN A ,  PALANI ANANDAN ,  SMITH ELIZABETH M ,  VACCARO HENRY M ,  XIAO DONG ,  KIM HYUNJIN M

Inventor： ASLANIAN ROBERT G ,  BENNETT CHAD E ,  BURNETT DUANE A ,  CHAN TIN-YAU ,  KISELGOF EUGENIA Y ,  KNUTSON CHAD E ,  HARRIS JOEL M ,  MC KITTRICK BRIAN A ,  PALANI ANANDAN ,  SMITH ELIZABETH M ,  VACCARO HENRY M ,  XIAO DONG ,  KIM HYUNJIN M

IPC: C07D471/10 ,  A61K31/438 ,  A61P3/00

CPC classification number: C07D471/10

Abstract: The present invention relates to Azetidinone Derivatives, compositions comprising an Azetidinone Derivative and methods for treating or preventing a disorder of lipid metabolism, pain, diabetes, a vascular condition, demyelination or nonalcoholic fatty liver disease, comprising administering to a patient an effective amount of an Azetidinone Derivative.

Abstract translation: 本发明涉及氮杂环丁酮衍生物，包含氮杂环丁酮衍生物的组合物和用于治疗或预防脂质代谢紊乱，疼痛，糖尿病，血管病症，脱髓鞘或非酒精性脂肪性肝病的方法，包括向患者施用有效量的 氮杂环丁酮衍生物。

公开(公告)号：WO2007084595A3

公开(公告)日：2007-09-07

申请号：PCT/US2007001302

申请日：2007-01-18

Applicant: SCHERING CORP ,  ASBEROM THEODROS ,  BARA THOMAS ,  BENNETT CHAD E ,  BURNETT DUANE A ,  CAPLEN MARY ANN ,  CLADER JOHN W ,  COLE DAVID J ,  DOMALSKI MARTIN S ,  JOSIEN HUBERT B ,  KNUTSON CHAD E ,  LI HONGMEI ,  MCBRIAR MARK D ,  PISSARNITSKI DMITRI A ,  QIANG LI ,  RAJAGOPALAN MURALI ,  SASIKUMAR THAVALAKULAMGAR K ,  SU JING ,  TANG HAIQUN ,  WU WEN-LIAN ,  XU RUO ,  ZHAO ZHIQIANG

Inventor： ASBEROM THEODROS ,  BARA THOMAS ,  BENNETT CHAD E ,  BURNETT DUANE A ,  CAPLEN MARY ANN ,  CLADER JOHN W ,  COLE DAVID J ,  DOMALSKI MARTIN S ,  JOSIEN HUBERT B ,  KNUTSON CHAD E ,  LI HONGMEI ,  MCBRIAR MARK D ,  PISSARNITSKI DMITRI A ,  QIANG LI ,  RAJAGOPALAN MURALI ,  SASIKUMAR THAVALAKULAMGAR K ,  SU JING ,  TANG HAIQUN ,  WU WEN-LIAN ,  XU RUO ,  ZHAO ZHIQIANG

IPC: C07D311/22 ,  C07D311/80 ,  C07D311/92 ,  C07D311/94 ,  C07D313/08 ,  C07D335/06

CPC classification number: C07D311/22 ,  C07C317/14 ,  C07C317/20 ,  C07C317/44 ,  C07C2602/08 ,  C07C2602/10 ,  C07C2602/12 ,  C07D311/80 ,  C07D311/92 ,  C07D311/94 ,  C07D313/08 ,  C07D335/06 ,  C07D405/12 ,  C07D409/12 ,  C07D491/04 ,  C07D493/04

Abstract: This invention discloses novel gamma secretase inhibitors of the formula: R 2 and R 3 , or R 2 and R 4 , or R 3 and R 4 , together with the atoms to which they are bound, can form a fused cycloalkyl or fused heterocycloalkyl ring. The cycloalkyl ring or the heterocycloalkyl ring can be optionally substituted with one or more substituents. One or more compounds of formula (I), or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.

Abstract translation: 本发明公开了下式的新型γ分泌酶抑制剂：R 2和R 3，或R 2和R 4 O / >或R 3和R 4以及它们所结合的原子可以形成稠合的环烷基或稠合的杂环烷基环。 环烷基环或杂环烷基环可任选被一个或多个取代基取代。 一种或多种式（I）化合物或包含这些化合物的制剂可以是有用的，例如， 治疗阿尔茨海默病。

公开(公告)号：WO2005063697A3

公开(公告)日：2005-12-22

申请号：PCT/US2004042934

申请日：2004-12-21

Applicant: SCHERING CORP ,  BURNETT DUANE A ,  WU WEN-LIAN ,  DOMALSKI MARTIN S ,  CAPLEN MARY ANN ,  SPRING RICHARD ,  LACHOWICZ JEAN E

Inventor： BURNETT DUANE A ,  WU WEN-LIAN ,  DOMALSKI MARTIN S ,  CAPLEN MARY ANN ,  SPRING RICHARD ,  LACHOWICZ JEAN E

IPC: A61K31/277 ,  A61K31/405 ,  A61K31/44 ,  A61K31/445 ,  A61K31/495 ,  A61K45/06 ,  C07C255/57 ,  C07C257/14 ,  C07C257/18 ,  C07D211/28 ,  C07D295/155 ,  C07D295/205 ,  C07D295/14

CPC classification number: C07D295/205 ,  A61K45/06 ,  C07C255/57 ,  C07C257/14 ,  C07C257/18 ,  C07D209/08 ,  C07D209/86 ,  C07D211/14 ,  C07D213/53 ,  C07D215/26 ,  C07D215/48 ,  C07D233/64 ,  C07D295/073 ,  C07D295/112 ,  C07D295/155 ,  C07D317/58 ,  C07D319/18 ,  C07D333/20 ,  C07D405/12

Abstract: The present invention provides compounds, which, are novel antagonists for D1 receptors as well as methods for preparing such compounds. In another embodiment, the invention provides pharmaceutical compositions comprising such D1 receptor antagonists as well as methods of using them to treat CNS disorders, obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.

Abstract translation: 本发明提供了作为D1受体的新型拮抗剂的化合物以及这些化合物的制备方法。 在另一个实施方案中，本发明提供包含这种D1受体拮抗剂的药物组合物以及使用它们治疗CNS障碍，肥胖，代谢紊乱，进食障碍如食欲过盛和糖尿病的方法。

公开(公告)号：JP2010254719A

公开(公告)日：2010-11-11

申请号：JP2010181957

申请日：2010-08-16

Applicant: Schering Corp ,  シェーリング コーポレイションSchering Corporation

Inventor： BURNETT DUANE A ,  CLADER JOHN W

IPC: C07D405/12 ,  A61K31/397 ,  A61K31/4025 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P9/00 ,  A61P25/00 ,  A61P25/28 ,  C07D405/14

CPC classification number: C07D405/12 ,  C07D405/14 ,  Y10S930/28

Abstract: 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

Abstract translation: 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