公开(公告)号：US20050153951A1

公开(公告)日：2005-07-14

申请号：US10940443

申请日：2004-09-14

申请人： Ramesh Kanojia ,  Alfonzo Jordan ,  Allen Reitz ,  Mark Macielag ,  Boyu Zhao

发明人： Ramesh Kanojia ,  Alfonzo Jordan ,  Allen Reitz ,  Mark Macielag ,  Boyu Zhao

IPC分类号： C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  A61K31/541 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/454 ,  A61K31/5377

CPC分类号： C07D413/04 ,  C07D413/14 ,  C07D417/14

摘要： This invention provides compounds having the following general structures: This invention also provides pharmaceutical compositions comprising same and methods of using these compositions to treat and prevent disorders characterized by neuronal damage.

摘要翻译： 本发明提供具有以下一般结构的化合物：本发明还提供包含其的药物组合物和使用这些组合物治疗和预防以神经元损伤为特征的疾病的方法。

公开(公告)号：US20060079687A1

公开(公告)日：2006-04-13

申请号：US11197669

申请日：2005-08-04

申请人： Ellen Baxter ,  Francois Bischoff ,  Robert Boyd ,  Mirielle Braeken ,  Steve Coats ,  Yifang Huang ,  Alfonzo Jordan ,  Chi Luo ,  Marc Mercken ,  Serge Maria Pieters ,  Allen Reitz ,  Charles Reynolds ,  Tina Ross ,  Brett Tounge ,  Mark Schulz ,  Hans De Winter

发明人： Ellen Baxter ,  Francois Bischoff ,  Robert Boyd ,  Mirielle Braeken ,  Steve Coats ,  Yifang Huang ,  Alfonzo Jordan ,  Chi Luo ,  Marc Mercken ,  Serge Maria Pieters ,  Allen Reitz ,  Charles Reynolds ,  Tina Ross ,  Brett Tounge ,  Mark Schulz ,  Hans De Winter

IPC分类号： C07D239/84 ,  C07D403/02

CPC分类号： C07D413/06 ,  C07D239/84 ,  C07D401/06 ,  C07D403/06 ,  C07D403/12 ,  C07D405/06

摘要： The present invention is directed to novel 2-amino-3,4-dihydro-quinazoline 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.

摘要翻译： 本发明涉及新的2-氨基-3,4-二氢 - 喹唑啉衍生物，含有它们的药物组合物及其在治疗阿尔茨海默病（AD）和相关病症中的用途。 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。

公开(公告)号：US20050004154A1

公开(公告)日：2005-01-06

申请号：US10909858

申请日：2004-08-02

申请人： Alfonzo Jordan ,  Allen Reitz ,  Kevin Pan

发明人： Alfonzo Jordan ,  Allen Reitz ,  Kevin Pan

IPC分类号： A61K31/438 ,  A61P11/06 ,  A61P11/14 ,  A61P25/00 ,  A61P25/06 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P43/00 ,  C07D471/10 ,  A61K31/4747

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：US20060079686A1

公开(公告)日：2006-04-13

申请号：US11197608

申请日：2005-08-04

申请人： Ellen Baxter ,  Robert Boyd ,  Steven Coats ,  Alfonzo Jordan ,  Allen Reitz ,  Charles Reynolds ,  Malcolm Scott

发明人： Ellen Baxter ,  Robert Boyd ,  Steven Coats ,  Alfonzo Jordan ,  Allen Reitz ,  Charles Reynolds ,  Malcolm Scott

IPC分类号： C07D403/02 ,  C07D239/84

CPC分类号： C07D215/227 ,  C07D401/06 ,  C07D403/06 ,  C07D403/12 ,  C07D405/06 ,  C07D413/06

摘要： The present invention is directed to novel 2-amino-3,4-dihydro-quinazoline 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.

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：US20060030604A1

公开(公告)日：2006-02-09

申请号：US11236097

申请日：2005-09-27

申请人： Magdalena Elsinger ,  Louis Fitzpatrick ,  Daniel Lee ,  Kevin Pan ,  Carlos Plata-Salaman ,  Allen Reitz ,  Virginia Smith-Swintosky ,  Boyu Zhao

发明人： Magdalena Elsinger ,  Louis Fitzpatrick ,  Daniel Lee ,  Kevin Pan ,  Carlos Plata-Salaman ,  Allen Reitz ,  Virginia Smith-Swintosky ,  Boyu Zhao

IPC分类号： C07D285/08 ,  A61K31/433

CPC分类号： C07D285/08 ,  A61K8/49 ,  A61Q5/006 ,  A61Q19/00 ,  A61Q19/007 ,  C07D333/16 ,  C07D417/12 ,  C07F9/4018

摘要： The present invention is directed to novel 1,2,4-thiadiazol-2-ium derivatives useful as agonists or antagonists of the melanocortin receptor. More particularly, the compounds of the present invention are useful for the treatment of metabolic, CNS and dermatological disorders such as obesity, impaired oral glucose tolerance, elevated blood glucose levels, type II diabetes, Syndrome X, diabetic retinopathy, spinal cord injury, nerve injury, acute neurodegenerative disorders, chronic neurodegenerative disorders, plexopathies, male erectile dysfunction, dry eyes, acne, dry skin, aged skin, seborrheic dermatitis, rosacea, excessive ear wax, meibomian gland disorder, pseudofolliculitis, yeast infections, dandruff, hidradenitis suppurativa, ocular rosacea and eccrine gland disorder.

公开(公告)号：US20060128772A1

公开(公告)日：2006-06-15

申请号：US11344772

申请日：2006-02-01

申请人： Magdalena Eisinger ,  Louis Fitzpatrick ,  Daniel Lee ,  Kevin Pan ,  Carlos Plata-Salaman ,  Allen Reitz ,  Virginia Smith-Swintosky ,  Boyu Zhao

发明人： Magdalena Eisinger ,  Louis Fitzpatrick ,  Daniel Lee ,  Kevin Pan ,  Carlos Plata-Salaman ,  Allen Reitz ,  Virginia Smith-Swintosky ,  Boyu Zhao

IPC分类号： A61K31/433 ,  C07D285/08

CPC分类号： C07D285/08 ,  A61K8/49 ,  A61Q5/006 ,  A61Q19/00 ,  A61Q19/007 ,  C07D417/12

摘要： The present invention is directed to novel 1,2,4-thiadiazole derivatives useful as agonists or antagonists of the melanocortin receptor. More particularly, the compounds of the present invention are useful for the treatment of metabolic, CNS and dermatological disorders such as obesity, impaired oral glucose tolerance, elevated blood glucose levels, type II diabetes, Syndrome X, diabetic retinopathy, spinal cord injury, nerve injury, acute neurodegenerative disorders, chronic neurodegenerative disorders, plexopathies, male erectile dysfunction, dry eyes, acne, dry skin, aged skin, seborrheic dermatitis, rosacea, excessive ear wax, meibomian gland disorder, pseudofolliculitis, yeast infections, dandruff, hidradenitis suppurativa, ocular rosacea and eccrine gland disorder.

公开(公告)号：US20070293476A1

公开(公告)日：2007-12-20

申请号：US11750579

申请日：2007-05-18

申请人： Virginia Smith-Swintosky ,  Michael Parker ,  Allen Reitz ,  Bruce Maryanoff

发明人： Virginia Smith-Swintosky ,  Michael Parker ,  Allen Reitz ,  Bruce Maryanoff

IPC分类号： A61K31/55 ,  A61K31/454 ,  A61K31/405 ,  A61K31/4025 ,  A61K31/381 ,  A61K31/343

CPC分类号： A61K45/06 ,  A61K31/381

摘要： The present invention is directed to a method for the treatment of epilepsy and related disorders comprising administering to a subject in need thereof, co-therapy with a therapeutically effective amount of a benzo-heteroaryl sulfamide derivative as described herein and a therapeutically effective amount of one or more anticonvulsant and/or anti-epileptic agents.

摘要翻译： 本发明涉及治疗癫痫和相关病症的方法，其包括向有需要的受试者施用治疗有效量的如本文所述的苯并杂芳基磺酰胺衍生物和治疗有效量的一种 或更多抗惊厥药和/或抗癫痫剂。

公开(公告)号：US20070155827A1

公开(公告)日：2007-07-05

申请号：US11612249

申请日：2006-12-18

申请人： Virginia Smith-Swintosky ,  Allen Reitz

发明人： Virginia Smith-Swintosky ,  Allen Reitz

IPC分类号： A61K31/36 ,  A61K31/353

CPC分类号： A61K31/353 ,  A61K31/352 ,  A61K31/357

摘要： The present invention is a method for the treatment of depression comprising administering to a subject in need thereof a therapeutically effective amount of one or more novel benzo-fused heterocycle sulfamide derivatives of formula (I) and formula (II) as herein defined. The present invention is directed to a method for the treatment of depression, which includes mono-therapy and alternatively, co-therapy with at least one antidepressant.

摘要翻译： 本发明是一种治疗抑郁症的方法，包括向有需要的受试者施用治疗有效量的如本文所定义的一种或多种式（I）和式（II）的新型苯并稠合的杂环磺酰胺衍生物。 本发明涉及一种治疗抑郁症的方法，其包括单一治疗，或者与至少一种抗抑郁药共同治疗。

公开(公告)号：US5382580A

公开(公告)日：1995-01-17

申请号：US250484

申请日：1994-05-27

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

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

IPC分类号： C07D473/18 ,  A61K31/535

CPC分类号： C07D473/18

摘要： Immunostimulating 7,8-disubstituted guanine derivatives that also contain a morpholinyl group as a position-9 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 group having a length of about one to about seven carbon atoms; R.sup.2 is a hydrogen or C.sub.1 -C.sub.8 acyl; R.sup.3 is hydrogen, a C.sub.1 -C.sub.5 aliphatic hydrocarbyl, aralkyl or substituted aralkyl group; and the pharmaceutically acceptable base addition salts thereof. Also disclosed are compositions containing an immunostimulating substituted guanine derivative and processes for using the same.

摘要翻译： 公开了其还含有吗啉基作为位置-9取代基的7,8-二取代的鸟嘌呤衍生物，其结构由式I其中X是O或S表示; R1是长度为约1至约7个碳原子的烃基或取代的烃基; R2是氢或C1-C8酰基; R3是氢，C1-C5脂族烃基，芳烷基或取代的芳烷基; 及其药学上可接受的碱加成盐。 还公开了含有免疫刺激性取代的鸟嘌呤衍生物的组合物及其使用方法。