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1. 发明申请

WO2007103187A3 8-AZABICYCLO[3.2.1]OCTANE COMPOUNDS AS MU OPIOID RECEPTOR ANTAGONISTS 审中-公开
标题翻译： 8-AZABICYCLO [3.2.1] OCTANE化合物作为阿片受体拮抗剂
公开(公告)号：WO2007103187A3
公开(公告)日：2007-11-01
申请号：PCT/US2007005388
申请日：2007-02-28
申请人： THERAVANCE INC , LONG DANIEL , CHURCH TIMOTHY J , JACOBSEN JOHN R , JIANG LAN , SAITO DAISUKE ROLAND , STERGIADES IOANNA , VAN DYKE PRISCILLA , DALZIEL SEAN , PREZA LETICIA
发明人： LONG DANIEL , CHURCH TIMOTHY J , JACOBSEN JOHN R , JIANG LAN , SAITO DAISUKE ROLAND , STERGIADES IOANNA , VAN DYKE PRISCILLA , DALZIEL SEAN , PREZA LETICIA
IPC分类号： C07D451/02 , A61K31/46 , A61P1/10
CPC分类号： C07D451/02 , A61K31/439 , A61K31/46 , A61K31/485 , A61K45/06
摘要： The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula (I) wherein R 1 , R 2 , R 3 , A, and G are defined in the specification, or a pharmaceutically-acceptable salt or solvate thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
摘要翻译：本发明提供式（I）的新的8-氮杂双环[3.2.1]辛烷化合物，其中R 1，R 2，R 3， A和G在本说明书中定义，或其药学上可接受的盐或溶剂合物，其作为μ阿片受体的拮抗剂。本发明还提供包含这些化合物的药物组合物，使用这些化合物治疗与阿片样物质受体活性相关的病症的方法，以及可用于制备这些化合物的方法和中间体。

2. 发明申请

WO2009014610A2 PROCESS FOR PREPARING AN INTERMEDIATE TO MU OPIOID RECEPTOR ANTAGONISTS 审中-公开
标题翻译：制备阿片类阿片受体拮抗剂中间体的方法
公开(公告)号：WO2009014610A2
公开(公告)日：2009-01-29
申请号：PCT/US2008008607
申请日：2008-07-15
申请人： THERAVANCE INC , COLSON PIERRE-JEAN , YU YING , LONG DANIEL D , STERGIADES IOANNA
发明人： COLSON PIERRE-JEAN , YU YING , LONG DANIEL D , STERGIADES IOANNA
CPC分类号： C07D451/06 , C07D451/02 , Y02P20/55
摘要： The invention provides an efficient method for preparing 3-endo-(S- azabicyclo[3.2.1]oct-3-yl)benzamide by hydrogenation, under controlled conditions, of an amino-protected 3-(8-azabicyclo[3.2.1]oct-2-en-3-yl)benzamide intermediate in which the amino-protecting group is removable by catalytic hydrogenation.
摘要翻译：本发明提供了一种有效的制备3-内 - （S-氮杂双环[3.2.1]辛-3-基）苯甲酰胺的方法，该方法是在受控条件下氢化氨基保护的3-（8-氮杂二环[3.2.1 ]辛-2-烯-3-基）苯甲酰胺中间体，其中氨基保护基可通过催化氢化除去。

3. 发明申请

WO2004041806A3 SUBSTITUTED 4-AMINO-1-(PYRIDYLMETHYL) PIPERIDINE AS MUSCARINIC RECEPTOR ANTAGONISTS 审中-公开
标题翻译：取代的4-氨基-1-（吡咯烷基）哌嗪作为药物受体拮抗剂
公开(公告)号：WO2004041806A3
公开(公告)日：2004-08-05
申请号：PCT/US0334444
申请日：2003-10-29
申请人： THERAVANCE INC , MAMMEN MATHAI , WILSON RICHARD , CHEN YAN , DUNHAM SARAH , HUGHES ADAM , HUSFELD CRAIG , JI YU-HUA , LI LI , MISCHKI TREVOR , STERGIADES IOANNA
发明人： MAMMEN MATHAI , WILSON RICHARD , CHEN YAN , DUNHAM SARAH , HUGHES ADAM , HUSFELD CRAIG , JI YU-HUA , LI LI , MISCHKI TREVOR , STERGIADES IOANNA
IPC分类号： A61P13/10 , C07D401/00 , C07D401/14 , A61K31/4545
CPC分类号： C07D401/14
摘要： This invention provides 4-amino-1-(pyridylmethyl) piperidine of formula (I) and related compounds and pharmaceutically acceptable salts thereof which are useful as muscarinic receptor antagonists. This invention also provides pharmaceutical compositions containing such compounds; processes and intermediates useful for preparing such compounds; and methods for treating disease conditions mediated by muscarinic receptors, such as overactive bladder, irritable bowel syndrome and chronic obstructive pulmonary disease, using such compounds.
摘要翻译：本发明提供式（I）的4-氨基-1-（吡啶基甲基）哌啶及其可用作毒蕈碱受体拮抗剂的相关化合物及其药学上可接受的盐。本发明还提供含有这些化合物的药物组合物; 用于制备这些化合物的方法和中间体; 以及使用这些化合物治疗由毒蕈碱受体介导的疾病状况的方法，例如膀胱过度活动，肠易激综合征和慢性阻塞性肺疾病。

4. 发明申请

WO2004106279A3 CRYSTALLINE FORM OF beta2 ADRENERGIC RECEPTOR AGONIST 审中-公开
标题翻译： β2ADRENERGIC受体激动剂的晶体形式
公开(公告)号：WO2004106279A3
公开(公告)日：2005-02-03
申请号：PCT/US2004016602
申请日：2004-05-26
申请人： THERAVANCE INC , STERGIADES IOANNA , YOST EDWARD , HUBBARD CRISTIN , ZHANG WEIJIANG
发明人： STERGIADES IOANNA , YOST EDWARD , HUBBARD CRISTIN , ZHANG WEIJIANG
IPC分类号： A61K31/16 , A61P11/08 , C07C215/00 , C07C233/07 , C07C233/43 , A61K31/167
CPC分类号： C07C233/43 , C07B2200/13
摘要： The invention provides a novel beta2 adrenergic receptor agonist in crystalline salt form. The invention also provides pharmaceutical compositions comprising the novel beta2 adrenergic receptor agonist in crystalline salt form, formulations containing the pharmaceutical compositions, methods of using the crystalline salt to treat diseases associated with beta2 adrenergic receptor activity, and processes useful for preparing such crystalline compounds.
摘要翻译：本发明提供了一种结晶盐形式的新型β2肾上腺素能受体激动剂。本发明还提供了包含结晶盐形式的新型β2肾上腺素能受体激动剂，含有药物组合物的制剂，使用该结晶盐治疗与β2肾上腺素能受体活性相关的疾病的方法，以及可用于制备该结晶化合物的方法的药物组合物。

5. 发明专利

JP2012211193A 8-AZABICYCLO[3.2.1]OCTANE COMPOUND AS μ OPIOID RECEPTOR ANTAGONIST 审中-公开
标题翻译： 8-AZABICYCLO [3.2.1] OCTAE化合物作为μ阿片受体拮抗剂
公开(公告)号：JP2012211193A
公开(公告)日：2012-11-01
申请号：JP2012171119
申请日：2012-08-01
申请人： Theravance Inc , セラヴァンス, インコーポレーテッド
发明人： LONG DANIEL , CHURCH TIMOTHY J , JACOBSEN JOHN R , JIANG LAN , SAITO DAISUKE ROLAND , STERGIADES IOANNA , VAN DYKE PRISCILLA , DALZIEL SEAN , PREZA LETICIA
IPC分类号： C07D451/02 , A61K31/46 , A61P1/00 , A61P3/04 , A61P25/30
CPC分类号： C07D451/02 , A61K31/439 , A61K31/46 , A61K31/485 , A61K45/06
摘要： PROBLEM TO BE SOLVED: To provide 8-azabicyclo[3.2.1]octane compounds as μ opioid receptor antagonist.SOLUTION: The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula (I): wherein R, R, R, A, and G are defined in the specification, or a pharmaceutically-acceptable salt or solvate thereof, which are antagonists at the μ opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with μ opioid receptor activity, and processes and intermediates useful for preparing such compounds.
摘要翻译：待解决的问题：提供8-氮杂双环[3.2.1]辛烷化合物作为μ阿片受体拮抗剂。解决方案：本发明提供式（I）的新型8-氮杂双环[3.2.1]辛烷化合物：其中R 1 ，R

6. 发明专利

JP2010059214A Substituted 4-amino-1-(pyridylmethyl)piperidine as muscarinic receptor antagonist 审中-公开
标题翻译：取代的4-氨基-1-（吡咯烷基）哌嗪作为药物受体拮抗剂
公开(公告)号：JP2010059214A
公开(公告)日：2010-03-18
申请号：JP2009285737
申请日：2009-12-16
申请人： Theravance Inc , セラヴァンス, インコーポレーテッド
发明人： MAMMEN MATHAI , WILLSON RICHARD , CHEN YAN , DUNHAM SARAH , HUGHES ADAM , HUSFELD CRAIG , JI YU-HUA , LI LI , MISCHKI TREVOR , STERGIADES IOANNA
IPC分类号： C07D401/14 , A61K31/4545 , A61K31/5377 , A61P1/00 , A61P11/00 , A61P13/10 , A61P43/00 , C07D401/00
CPC分类号： C07D401/14
摘要： PROBLEM TO BE SOLVED: To provide new muscarinic receptor antagonists. SOLUTION: There are provided a substituted 4-amino-1-(pyridylmethyl)piperidine and related compounds and pharmaceutically acceptable salts thereof which are useful as muscarinic receptor antagonists. There are also provided: pharmaceutical compositions containing such compounds; and intermediates useful for preparing such compounds; and methods for treating disease conditions mediated by muscarinic receptors, (such as overactive bladder, irritable bowel syndrome and chronic obstructive pulmonary disease) using such compounds. COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：要解决的问题：提供新的毒蕈碱受体拮抗剂。提供了可用作毒蕈碱受体拮抗剂的取代的4-氨基-1-（吡啶基甲基）哌啶及其相关化合物及其药学上可接受的盐。还提供：含有这些化合物的药物组合物; 和可用于制备这些化合物的中间体; 以及使用这些化合物治疗由毒蕈碱受体介导的疾病状态（例如膀胱过度活动，肠易激综合征和慢性阻塞性肺病）的方法。版权所有（C）2010，JPO＆INPIT

7. 发明专利

ES2366058T3 COMPUESTOS DE 8-AZABICICLO[3.2.1]OCTANO COMO ANTAGONISTAS DE LOS RECEPTORES OPIOIDES MU. 未知
公开(公告)号：ES2366058T3
公开(公告)日：2011-10-14
申请号：ES07752111
申请日：2007-02-28
申请人： THERAVANCE INC
发明人： LONG DANIEL , CHURCH TIMOTHY J , JACOBSEN JOHN R , JIANG LAN , SAITO DAISUKE ROLAND , STERGIADES IOANNA , VAN DYKE PRISCILLA
IPC分类号： C07D451/02
摘要： Un compuesto de fórmula (I): **Fórmula** donde: R1 se elige entre-ORa, -C(O)NRaRb, -NHS(O)2Rc, -NRaRb, -C(O)ORa y -CH2OH; A es alquilenilo C1-4; R2 es cicloalquilo C3-12 o arilo C6-10, de modo que cicloalquilo C3-12 y arilo C6-10 están cada uno opcionalmente sustituidos con un -ORa, con uno o dos halógenos, con uno o dos alquilos C1-3 sustituidos con dos o tres halógenos, o con uno, dos, tres o cuatro alquilos C1-3; G es alquilenilo C1-4; R3 se elige entre hidrógeno, -C(O)R4, -C(O)NHR5, -S(O)2Rc y -S(O)2NRaRb; R4 es cicloalquilo C3-6 o alquilo C1-6, donde el cicloalquilo C3-6 está opcionalmente sustituido con un -ORa y el alquilo C1-6 está opcionalmente sustituido con uno o dos sustituyentes escogidos entre -ORa, -C(O)ORa, -S(O)2R6, -C(O)NRaRb, -NRaRb, -NHC(O)NRaRb, -CN, cicloalquilo C3-6 y fenilo, o con un D-(CH2)JR7, donde D es donde j es 1, 2, o 3, n es 1 o 2 y p es 1 o 2, R6 es alquilo C1-6 opcionalmente sustituido con R7, R7 es -C(O)ORa, -C(O)NRaRb, -NRaRb o -NHC(O)NRaRb, R5 es alquilo C1-6, benzo[1.3]dioxol o -(CH2)q-fenilo, donde el fenilo está opcionalmente sustituido con uno o dos sustituyentes escogidos entre halógeno, -ORa, alquilo C1-3 y alcoxi C1-3, donde el alquilo C1-3 y el alcoxi C1-3 están opcionalmente sustituidos con 2 o 3 halógenos, y q es 0, 1 o 2, Ra y Rb son, independientemente, hidrógeno o alquilo C1-4, y Rc es alquilo C1-3, con la condición de que, cuando R2 sea fenilo sustituido en la posición 4 R3 no sea -C(O)R4, donde R4 es alquilo C1-4 sustituido con -C(O)ORa; o una sal o solvato farmacéuticamente aceptable del mismo.

8. 发明专利

DE602004024383D1 未知
公开(公告)号：DE602004024383D1
公开(公告)日：2010-01-14
申请号：DE602004024383
申请日：2004-05-07
申请人： THERAVANCE INC
发明人： AXT SABINE , STERGIADES IOANNA
IPC分类号： C07D215/26 , A61K31/4704 , A61P11/06

9. 发明专利

AT450511T 未知
公开(公告)号：AT450511T
公开(公告)日：2009-12-15
申请号：AT04751604
申请日：2004-05-07
申请人： THERAVANCE INC
发明人： AXT SABINE , STERGIADES IOANNA
IPC分类号： C07D215/26 , A61K31/4704 , A61P11/06

10. 发明专利

AU2008279749A1 Process for preparing an intermediate to MU opioid receptor antagonists 未知
公开(公告)号：AU2008279749A1
公开(公告)日：2009-01-29
申请号：AU2008279749
申请日：2008-07-15
申请人： THERAVANCE INC
发明人： STERGIADES IOANNA , LONG DANIEL D , YU YING , COLSON PIERRE-JEAN
IPC分类号： C07D451/02
摘要： A process for preparing a compound of formula 1 , having the chemical name 3- endo -(8-azabicyclo[3.2.1]oct-3-yl)benzamide, or a salt thereof: the process comprising hydrogenating a compound of formula 2, having the chemical name 3-(8-azabicyclo[3.2.]oct-2-en-3-yl)benzamide: or an acid salt thereof, in the presence of a palladium metal catalyst, and, when the compound of formula 2 is in the form of a free base, in the presence of an acid, to provide a compound of formula 1 or a salt thereof.

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