公开(公告)号：US20070161648A1

公开(公告)日：2007-07-12

申请号：US11549176

申请日：2006-10-13

申请人： Terry Hughes ,  Stuart Emanuel ,  Catherine Rugg ,  Peter Connolly

发明人： Terry Hughes ,  Stuart Emanuel ,  Catherine Rugg ,  Peter Connolly

IPC分类号： A61K31/496 ,  A61K31/454 ,  A61K31/404 ,  C07D403/02

CPC分类号： C07D209/46 ,  C07D209/48 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14

摘要： The present invention is directed to novel substituted dihydro-isoindolone compounds of formula (I): and forms thereof, wherein Ring A, X3, R1, R2, R3, R4 and R6 are as herein defined, and their synthesis and use as protein kinase inhibitors and interactions thereof.

摘要翻译： 本发明涉及式（I）的新型取代的二氢 - 异吲哚酮化合物及其形式，其中环A，X 3，R 1，R 2， 2，R 3，R 4和R 6如本文所定义，并且它们的合成和用作蛋白激酶抑制剂和 其相互作用。

公开(公告)号：US20070123542A1

公开(公告)日：2007-05-31

申请号：US11453128

申请日：2006-06-14

申请人： George Chiu ,  Peter Connolly ,  Jessica Liu ,  Steven Middleton ,  Virginia Pulito ,  Shengjian Li

发明人： George Chiu ,  Peter Connolly ,  Jessica Liu ,  Steven Middleton ,  Virginia Pulito ,  Shengjian Li

IPC分类号： A61K31/495 ,  C07D241/04

CPC分类号： C07D295/155 ,  C07D295/135

摘要： The present invention relates to substituted [4-(4-phenyl-piperazin-1-yl)-cyclohexyl]-urea compounds of Formula (I) and pharmaceutically acceptable forms thereof, as α1a/α1d adrenoreceptor modulators for the treatment of benign prostatic hypertrophy and lower urinary tract symptoms. The present invention also relates to pharmaceutical compositions comprising said new compounds, new processes to prepare these new compounds and new uses as a medicine as well as methods of treatment.

摘要翻译： 本发明涉及式（I）的取代的[4-（4-苯基 - 哌嗪-1-基） - 环己基] - 脲化合物及其药学上可接受的形式，作为α1a / 用于治疗良性前列腺肥大和下尿路症状的肾上腺素受体调节剂。 本发明还涉及包含所述新化合物的药物组合物，制备这些新化合物的新方法和作为药物的新用途以及治疗方法。

公开(公告)号：US20070112016A1

公开(公告)日：2007-05-17

申请号：US11440731

申请日：2006-05-25

申请人： Kathleen Battista ,  Gilles Bignan ,  Peter Connolly ,  Jessica Liu ,  Steven Middleton ,  Michael Orsini

发明人： Kathleen Battista ,  Gilles Bignan ,  Peter Connolly ,  Jessica Liu ,  Steven Middleton ,  Michael Orsini

IPC分类号： A61K31/4747 ,  C07D471/10

CPC分类号： C07D471/10

摘要： The present invention is directed to novel 3-spirocyclic indolyl derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the ORL-1 receptor.

摘要翻译： 本发明涉及新颖的3-螺环吲哚衍生物，含有它们的药物组合物及其用于治疗由ORL-1受体调节的病症和状况的用途。

公开(公告)号：US20070093500A1

公开(公告)日：2007-04-26

申请号：US11451196

申请日：2006-06-12

申请人： George Chiu ,  Peter Connolly ,  Jessica Liu ,  Steven Middleton ,  Virginia Pulito ,  Shengjian Li

发明人： George Chiu ,  Peter Connolly ,  Jessica Liu ,  Steven Middleton ,  Virginia Pulito ,  Shengjian Li

IPC分类号： A61K31/496 ,  C07D403/02 ,  C07D471/02

CPC分类号： C07D209/48 ,  C07D209/66 ,  C07D471/04

摘要： The present invention relates to substituted isoindole-1,3-dione compounds of Formula (I) and pharmaceutically acceptable forms thereof, as α1a/α1d adrenoreceptor modulators for the treatment of benign prostatic hypertrophy and lower urinary tract symptoms. The present invention also relates to pharmaceutical compositions comprising said new compounds, new processes to prepare these new compounds and new uses as a medicine as well as methods of treatment.

摘要翻译： 本发明涉及式（I）的取代的异吲哚-1,3-二酮化合物及其药学上可接受的形式，作为用于治疗的α1a1/α1D1肾上腺素受体调节剂 良性前列腺肥大和下尿路症状。 本发明还涉及包含所述新化合物的药物组合物，制备这些新化合物的新方法和作为药物的新用途以及治疗方法。

公开(公告)号：US20080015214A1

公开(公告)日：2008-01-17

申请号：US11550421

申请日：2006-10-18

申请人： Gilles Bignan ,  Kathleen Battista ,  Peter Connolly ,  Jessica Liu ,  Steven Middleton ,  Michael Orsini ,  Allen Reitz

发明人： Gilles Bignan ,  Kathleen Battista ,  Peter Connolly ,  Jessica Liu ,  Steven Middleton ,  Michael Orsini ,  Allen Reitz

IPC分类号： A61K31/454 ,  A61K31/437 ,  A61K31/4545 ,  A61P1/00 ,  A61P25/00 ,  A61P9/00 ,  C07D401/02 ,  C07D401/14 ,  C07D471/02

CPC分类号： C07D401/04 ,  C07D405/14 ,  C07D471/04

摘要： The present invention is directed to novel 3-piperidin-4-yl-indole derivatives of formula (I) and forms thereof, wherein X, R1, R2, R3, R4 and R5 are as herein defined, pharmaceutical compositions thereof and use as ORL-1 receptor modulators for treating, preventing or ameliorating ORL-1 receptor mediated disorders and conditions.

摘要翻译： 本发明涉及新的式（I）的3-哌啶-4-基 - 吲哚衍生物及其形式，其中X，R 1，R 2，R R 4，R 4和R 5如本文所定义，其药物组合物用作ORL-1受体调节剂，用于治疗，预防或改善 ORL-1受体介导的病症和病症。

公开(公告)号：US20060223825A1

公开(公告)日：2006-10-05

申请号：US11376432

申请日：2006-03-15

申请人： George Chiu ,  Shengjian Li ,  Peter Connolly ,  Virginia Pulito ,  Jingchun Liu ,  Steven Middleton

发明人： George Chiu ,  Shengjian Li ,  Peter Connolly ,  Virginia Pulito ,  Jingchun Liu ,  Steven Middleton

IPC分类号： A61K31/496 ,  C07D403/04

CPC分类号： C07D213/74

摘要： The present invention relates to piperazine substituted cyclohexane- 1,4-diamine compounds of Formula (I) and pharmaceutically acceptable forms thereof, as α1a/α1d adrenoreceptor modulators for the treatment of benign prostatic hypertrophy and lower urinary tract symptoms. The present invention also relates to pharmaceutical compositions comprising said new compounds, new processes to prepare these new compounds and new uses as a medicine as well as methods of treatment.

摘要翻译： 本发明涉及式（I）的哌嗪取代的环己烷-1,4-二胺化合物及其药学上可接受的形式，作为α1a1/α1D1肾上腺素受体调节剂 治疗良性前列腺肥大和下尿路症状。 本发明还涉及包含所述新化合物的药物组合物，制备这些新化合物的新方法和作为药物的新用途以及治疗方法。

公开(公告)号：US20060217419A1

公开(公告)日：2006-09-28

申请号：US11376348

申请日：2006-03-15

申请人： George Chiu ,  Shengjian Li ,  Peter Connolly ,  Virginia Pulito ,  Jingchun Liu ,  Steven Middleton

发明人： George Chiu ,  Shengjian Li ,  Peter Connolly ,  Virginia Pulito ,  Jingchun Liu ,  Steven Middleton

IPC分类号： A61K31/454 ,  A61K31/445 ,  C07D401/02 ,  C07D211/26

CPC分类号： C07D211/14 ,  C07D211/22 ,  C07D405/12

摘要： The present invention relates to piperidine substituted cyclohexane-1,4-diamine compounds of Formula (I) and pharmaceutically acceptable forms thereof, as α1a/α1d adrenoreceptor modulators for the treatment of benign prostatic hypertrophy and lower urinary tract symptoms. The present invention also relates to pharmaceutical compositions comprising said new compounds, new processes to prepare these new compounds and new uses as a medicine as well as method of treatments.

摘要翻译： 本发明涉及式（I）的哌啶取代的环己烷-1,4-二胺化合物及其药学上可接受的形式，作为α1a1/α1d1肾上腺素受体调节剂 治疗良性前列腺肥大和下尿路症状。 本发明还涉及包含所述新化合物的药物组合物，制备这些新化合物的新方法和作为药物的新用途以及治疗方法。

公开(公告)号：US20060173015A1

公开(公告)日：2006-08-03

申请号：US11262551

申请日：2005-10-28

申请人： George Chiu ,  Shengjian Li ,  Peter Connolly ,  Virginia Pulito ,  Jessica Liu ,  Steven Middleton

发明人： George Chiu ,  Shengjian Li ,  Peter Connolly ,  Virginia Pulito ,  Jessica Liu ,  Steven Middleton

IPC分类号： A61K31/495 ,  A61K31/496 ,  C07D403/02 ,  C07D241/04

CPC分类号： C07D213/71 ,  C07D295/116

摘要： The present invention relates to compounds of Formula (I) or a pharmaceutically acceptable form thereof, as dual selective α1a/α1d adrenoreceptor antagonists for the treatment of benign prostatic hypertrophy and lower urinary tract symptoms. The present invention also relates to pharmaceutical compositions comprising said new compounds, new processes to prepare these new compounds and new uses as a medicine as well as method of treatments.

摘要翻译： 本发明涉及用于治疗良性前列腺肥大的双重选择性α1A/α1D1肾上腺素受体拮抗剂的式（I）化合物或其药学上可接受的形式， 下尿路症状。 本发明还涉及包含所述新化合物的药物组合物，制备这些新化合物的新方法和作为药物的新用途以及治疗方法。

公开(公告)号：US20060030577A1

公开(公告)日：2006-02-09

申请号：US11242654

申请日：2005-10-04

申请人： Kathleen Battista ,  Gilles Bignan ,  Peter Connolly ,  Allen Reitz ,  Tina Ross ,  Malcolm Scott ,  Steven Middleton ,  Michael Orsini

发明人： Kathleen Battista ,  Gilles Bignan ,  Peter Connolly ,  Allen Reitz ,  Tina Ross ,  Malcolm Scott ,  Steven Middleton ,  Michael Orsini

IPC分类号： A61K31/4747 ,  C07D471/10

CPC分类号： C07D471/10

摘要： The present invention is directed to novel hydroxy alkyl substituted 1,3,8-triazaspiro[4.5]decan-4-one derivatives of the general formula wherein all variables are as defined herein, useful in the treatment of disorders and conditions mediated by the ORL-1 G-protein coupled receptor. More particularly, the compounds of the present invention are useful in the treatment of disorders and conditions such as anxiety, depression, panic, dementia, mania, bipolar disorder, substance abuse, neuropathic pain, acute pain, chronic pain, migraine, asthma, cough, psychosis, schizophrenia, epilepsy, hypertension, obesity, eating disorders, cravings, diabetes, cardiac arrhythmia, irritable bowel syndrome, Crohn's disease, urinary incontinence, adrenal disorders, attention deficit disorder (ADD), attention deficit hyperactivity disorder (ADHD), Alzheimer's disease, for improved cognition or memory and for mood stabilization.

公开(公告)号：US20050266575A1

公开(公告)日：2005-12-01

申请号：US10854904

申请日：2004-05-27

申请人： Kevin Mayo ,  Mary Beavers ,  Michael Orsini ,  Steven Middleton ,  Peter Connolly

发明人： Kevin Mayo ,  Mary Beavers ,  Michael Orsini ,  Steven Middleton ,  Peter Connolly

IPC分类号： C07K7/08 ,  G01N24/00 ,  G01N24/08 ,  G01N33/00 ,  G06F19/00

CPC分类号： C07K7/08 ,  G01N24/08 ,  G16B15/00 ,  G16B20/00 ,  G16C20/50 ,  Y10T436/24

摘要： Nociepeptin pharmacophores, methods of determining a nociceptin pharmocophore, nociceptin solution structures, and methods of identifying compounds as potential nociceptin mimics are provided.

摘要翻译： 提供了诺美胃蛋白药代动力学，确定伤害感受肽药代动力学的方法，伤害感受肽溶液结构以及将化合物鉴定为潜在的伤害感受肽模拟物的方法。