公开(公告)号：US06890921B1

公开(公告)日：2005-05-10

申请号：US09526224

申请日：2000-03-15

申请人： Linda Jolliffe ,  William Murray ,  Virginia Pulito ,  Allen Reitz ,  Xiaobing Li ,  Linda Mulcahy ,  Cynthia Maryanoff ,  Frank Villani

发明人： Linda Jolliffe ,  William Murray ,  Virginia Pulito ,  Allen Reitz ,  Xiaobing Li ,  Linda Mulcahy ,  Cynthia Maryanoff ,  Frank Villani

IPC分类号： C07D295/12 ,  A61K31/397 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/402 ,  A61K31/4025 ,  A61K31/445 ,  A61K31/496 ,  A61K31/55 ,  A61P13/08 ,  C07D205/08 ,  C07D207/12 ,  C07D207/26 ,  C07D207/27 ,  C07D207/28 ,  C07D209/44 ,  C07D209/48 ,  C07D211/40 ,  C07D211/76 ,  C07D221/20 ,  C07D223/10 ,  C07D225/02 ,  C07D225/08 ,  C07D241/04 ,  C07D295/08 ,  C07D295/13 ,  C07D401/12 ,  C07D403/12

CPC分类号： C07D207/27 ,  C07D207/28 ,  C07D209/48 ,  C07D211/76 ,  C07D223/10 ,  C07D295/13

摘要： This invention relates to a series of arylsubstituted piperazines, of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention selectively inhibit binding to the α-1a adrenergic receptor, a receptor which has been implicated in benign prostatic hyperplasia. As such the compounds are potentially useful in the treatment of this and other disease.

摘要翻译： 本发明涉及一系列含有它们的式I药物组合物和其制备中使用的中间体的芳基取代哌嗪。 本发明的化合物选择性地抑制与α-1a肾上腺素能受体的结合，α受体是与良性前列腺增生有关的受体。 因此，这些化合物在治疗这种疾病和其他疾病中潜在有用。

公开(公告)号：US5441942A

公开(公告)日：1995-08-15

申请号：US250483

申请日：1994-05-27

申请人： Michael G. Goodman ,  Robert Chen ,  Allen Reitz

发明人： Michael G. Goodman ,  Robert Chen ,  Allen Reitz

IPC分类号： C07H19/16 ,  A61K31/70 ,  C07H19/173

CPC分类号： C07H19/16

摘要： Immunostimulating 7,8-disubstituted guanine derivatives that also contain a .beta.-9,1'-linked-2',3'-dideoxy-2',3'-didehydroribosyl substituent are disclosed whose structures are represented by Formula I ##STR1## wherein X is O or S; R.sup.1 is a hydrocarbyl or substituted hydrocarbyl moiety having a length of about one to about seven carbon atoms; R.sup.2 is hydrogen or C.sub.1 -C.sub.8 acyl; and the pharmaceutically acceptable base addition salts thereof. Also disclosed are compositions containing an immunostimulating guanine derivative and processes for using the same.

摘要翻译： 公开了免疫刺激还含有β-9,1'-连接-2'，3'-二脱氧-2'，3'-二脱氧山梨糖基取代基的7,8-二取代鸟嘌呤衍生物，其结构由式I表示 其中X是O或S; R1是具有约1至约7个碳原子长度的烃基或取代的烃基部分; R2是氢或C1-C8酰基; 及其药学上可接受的碱加成盐。 还公开了含有免疫刺激性鸟嘌呤衍生物的组合物及其使用方法。

公开(公告)号：US20070232630A1

公开(公告)日：2007-10-04

申请号：US11671732

申请日：2007-02-06

申请人： Ellen Baxter ,  Allen Reitz ,  Michael Parker ,  Yifang Huang ,  Chih Ho ,  Eric Strobel ,  Charles Reynolds

发明人： Ellen Baxter ,  Allen Reitz ,  Michael Parker ,  Yifang Huang ,  Chih Ho ,  Eric Strobel ,  Charles Reynolds

IPC分类号： A61K31/519 ,  C07D491/14 ,  C07D487/14

CPC分类号： C07D498/08 ,  C07D487/08

摘要： The present invention is directed to macrocycle derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease (AD) and related disorders. The compounds of the invention are inhibitors of β-secretase, also known as β-site cleaving enzyme and BACE, BACE1, Asp2 and memapsin2.

摘要翻译： 本发明涉及大环衍生物，含有它们的药物组合物及其在治疗阿尔茨海默病（AD）和相关疾病中的用途。 本发明的化合物是β-分泌酶的抑制剂，也称为β-位点切割酶和BACE，BACE1，Asp2和memapsin2。

公开(公告)号：US20060276528A1

公开(公告)日：2006-12-07

申请号：US11359626

申请日：2006-02-22

申请人： Ahmed Abdel-Magid ,  Bruce Maryanoff ,  Steven Mehrman ,  Michael Parker ,  Allen Reitz

发明人： Ahmed Abdel-Magid ,  Bruce Maryanoff ,  Steven Mehrman ,  Michael Parker ,  Allen Reitz

IPC分类号： A61K31/404 ,  A61K31/381 ,  A61K31/4025 ,  A61K31/343 ,  C07D333/02

CPC分类号： C07D307/81 ,  C07D209/14 ,  C07D333/58 ,  C07D409/12

摘要： The present invention is directed to novel benzo-fused heteroaryl sulfamide derivatives, pharmaceutical compositions containing them and their use in the treatment of epilepsy and related disorders. The present invention is further directed to a crystalline form of N-(benzo[b]thien-3-ylmethyl)-sulfamide and a process for its preparation.

摘要翻译： 本发明涉及新颖的苯并稠合杂芳基磺酰胺衍生物，含有它们的药物组合物及其在治疗癫痫和相关疾病中的用途。 本发明还涉及N-（苯并[b]噻吩-3-基甲基） - 磺酰胺的结晶形式及其制备方法。

公开(公告)号：US20060183902A1

公开(公告)日：2006-08-17

申请号：US11353581

申请日：2006-02-14

申请人： Ellen Baxter ,  Samuel Nortey ,  Allen Reitz ,  Virginia Pulito ,  Steven Middleton

发明人： Ellen Baxter ,  Samuel Nortey ,  Allen Reitz ,  Virginia Pulito ,  Steven Middleton

IPC分类号： C07D401/00 ,  A61K31/497 ,  C07D403/00

CPC分类号： C07D209/08 ,  C07D401/10

摘要： The present invention relates to new compounds of Formula (I): and pharmaceutically acceptable forms thereof, use of the compounds as α1a and/or α1d adrenoreceptor modulators, including use of a pharmaceutical composition, medicine or medicament comprising said compounds, a process to prepare said compounds and a method for treating an α1a and/or α1d adrenoreceptor mediated disorder.

摘要翻译： 本发明涉及式（I）的新化合物及其药学上可接受的形式：化合物作为α1a1和/或α1d1肾上腺素受体调节剂的用途，包括使用 包含所述化合物的药物组合物，药物或药物，制备所述化合物的方法以及治疗α1a1和/或α1d1肾上腺素受体介导的病症的方法。

公开(公告)号：US20060178390A1

公开(公告)日：2006-08-10

申请号：US11398239

申请日：2006-04-05

申请人： Alfonzo Jordan ,  Allen Reitz ,  Kevin Pan

发明人： Alfonzo Jordan ,  Allen Reitz ,  Kevin Pan

IPC分类号： A61K31/4747 ,  C07D471/10

CPC分类号： C07D471/10

摘要： The present invention is directed to novel 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, substance abuse, neuropathic pain, acute pain, migraine, asthma, cough and for improved cognition.

摘要翻译： 本发明涉及通式的新的1,3,8-三氮杂螺[4.5]癸-4-酮衍生物，其中所有变量如本文所定义，可用于治疗ORL-1 G介导的病症和病症 蛋白偶联受体。 更具体地，本发明的化合物可用于治疗诸如焦虑，抑郁，药物滥用，神经性疼痛，急性疼痛，偏头痛，哮喘，咳嗽和改善认知的病症和病症。

公开(公告)号：US20060058373A1

公开(公告)日：2006-03-16

申请号：US11265670

申请日：2005-11-02

申请人： Ahmed Abdel-Magid ,  Cynthia Maryanoff ,  Steven Mehrman ,  Allen Reitz ,  Bruce Maryanoff

发明人： Ahmed Abdel-Magid ,  Cynthia Maryanoff ,  Steven Mehrman ,  Allen Reitz ,  Bruce Maryanoff

IPC分类号： A61K31/255 ,  C07C311/45 ,  A61K31/695

CPC分类号： C07H5/06 ,  C07H9/04

摘要： The present invention is directed to novel compounds of the formula (I) wherein X, R1, R2, R3, R4, R5 and R6 are as described in the specification, processes for the preparation of and pharmaceutical compositions comprising said derivatives. The compounds of the present invention are useful for the treatment of epilepsy. The invention is further directed to a process for the preparation of compounds of formula (XX), wherein X, R3, R4, R5 and R6 are as described in the specification.

摘要翻译： 本发明涉及新的式（I）化合物，

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：US20050203092A1

公开(公告)日：2005-09-15

申请号：US10987562

申请日：2004-11-12

申请人： Elfrida Benjamin ,  Frank Brown ,  Robert Zivin ,  Michael McMillan ,  Zhong Zhong ,  Allen Reitz ,  Tina Ross

发明人： Elfrida Benjamin ,  Frank Brown ,  Robert Zivin ,  Michael McMillan ,  Zhong Zhong ,  Allen Reitz ,  Tina Ross

IPC分类号： C07D239/12 ,  C07D239/42 ,  C07D239/52 ,  C07D401/12 ,  C07D405/04 ,  C07D409/04 ,  C07D495/04 ,  C07D413/02 ,  A61K31/506 ,  A61K31/5377 ,  C07D43/02

CPC分类号： C07D239/42 ,  C07D239/12 ,  C07D239/52 ,  C07D401/12 ,  C07D405/04 ,  C07D409/04 ,  C07D495/04

摘要： This invention provides novel neuroprotective 4-pyrimidineamine derivatives and neuroprotective pharmaceutical compositions comprising 4-pyrimidinamines. This invention also provides methods of using these compositions to prevent ischemic cell death, particularly neuronal cell death, and reduce the likelihood of neuronal cell death in a subject due to a traumatic event. Finally, this invention provides an apparatus for administering to a subject the instant pharmaceutical compositions.

摘要翻译： 本发明提供新颖的神经保护性4-嘧啶胺衍生物和包含4-嘧啶胺的神经保护药物组合物。 本发明还提供了使用这些组合物来预防缺血性细胞死亡，特别是神经元细胞死亡并降低由于创伤性事件导致受试者神经元细胞死亡的可能性的方法。 最后，本发明提供了一种向受试者施用本发明的药物组合物的装置。

公开(公告)号：US20050004136A1

公开(公告)日：2005-01-06

申请号：US10898130

申请日：2004-07-23

申请人： Kevin Pan ,  Michael Parker ,  Allen Reitz ,  Steven Coats ,  Cheryl Kordik ,  Chi Luo

发明人： Kevin Pan ,  Michael Parker ,  Allen Reitz ,  Steven Coats ,  Cheryl Kordik ,  Chi Luo

IPC分类号： C07D295/18 ,  A61K31/445 ,  A61K31/4525 ,  A61K31/4535 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/495 ,  A61K31/496 ,  A61K31/5377 ,  A61P1/08 ,  A61P17/04 ,  A61P25/00 ,  A61P25/06 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P29/00 ,  C07D211/16 ,  C07D211/34 ,  C07D213/44 ,  C07D213/56 ,  C07D213/75 ,  C07D295/192 ,  C07D307/46 ,  C07D307/68 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D405/10 ,  C07D405/12 ,  C07D409/10 ,  C07D409/12 ,  C07D413/06 ,  C07D413/14 ,  A61K31/497 ,  C07

CPC分类号： C07D213/75 ,  C07D211/16 ,  C07D213/44 ,  C07D295/192 ,  C07D307/46 ,  C07D401/10 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/06 ,  C07D413/14

摘要： Novel amidoalkyl-piperidine and amidoalkyl-piperazine derivatives of the general formula wherein all variables are as described herein, useful in the treatment of disorders, such as depression, dementia, schizophrenia, bipolar disorders, anxiety, emesis, acute or neuropathic pain, itching, migraine and movement disorders.

摘要翻译： 新颖的通式的酰氨基烷基 - 哌啶和酰氨基烷基 - 哌嗪衍生物，其中所有变量如本文所述，可用于治疗疾病如抑郁症，痴呆，精神分裂症，双相情感障碍，焦虑，呕吐，急性或神经性疼痛，瘙痒， 偏头痛和运动障碍。