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1. 发明授权

US06294530B1 1-azatricyclic-4-benzylpiperazines 失效
标题翻译： 1-氮杂环己基-4-苄基哌嗪
公开(公告)号：US06294530B1
公开(公告)日：2001-09-25
申请号：US09596020
申请日：2000-06-14
申请人： Xiaoyan Zhang , Kevin Hodgetts , Stanislaw Rachwal , Daniel Rosewater , Andrew Thurkauf
发明人： Xiaoyan Zhang , Kevin Hodgetts , Stanislaw Rachwal , Daniel Rosewater , Andrew Thurkauf
IPC分类号： C07D48704
CPC分类号： C07D471/06 , C07D487/06 , G01N33/6896 , G01N33/9413 , G01N2333/70571 , G01N2800/2835
摘要： Disclosed are 1-Azatricyclic-4-benzylpiperazine compounds which are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania, dementia, depression, anxiety, compulsive behavior, substance abuse, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.
摘要翻译：公开了可用于治疗和/或预防神经心理障碍的1-叠氮基-4-苄基哌嗪化合物，包括但不限于精神分裂症，躁狂症，痴呆，抑郁症，焦虑症，强迫行为，药物滥用，帕金森氏样运动与使用神经安定药相关的疾病和运动障碍。还提供药物组合物，包括包装的药物组合物。本发明的化合物也可用作组织样品中GABA A受体定位的探针。

2. 发明授权

US06403591B1 1-azatricyclic-4-benzylpiperazines 失效
标题翻译： 1-氮杂环己基-4-苄基哌嗪
公开(公告)号：US06403591B1
公开(公告)日：2002-06-11
申请号：US09894092
申请日：2001-06-28
申请人： Kevin Hodgetts , Stanislaw Rachwal , Daniel Rosewater , Andrew Thurkauf , Xiaoyan Zhang
发明人： Kevin Hodgetts , Stanislaw Rachwal , Daniel Rosewater , Andrew Thurkauf , Xiaoyan Zhang
IPC分类号： A61K31497
CPC分类号： C07D471/06 , C07D487/06 , G01N33/6896 , G01N33/9413 , G01N2333/70571 , G01N2800/2835
摘要： Disclosed are 1-Azatricyclic-4-benzylpiperazine compounds which are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania, dementia, depression, anxiety, compulsive behavior, substance abuse, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.
摘要翻译：公开了可用于治疗和/或预防神经心理障碍的1-叠氮基-4-苄基哌嗪化合物，包括但不限于精神分裂症，躁狂症，痴呆，抑郁，焦虑，强迫行为，药物滥用，帕金森氏样运动与使用神经安定药相关的疾病和运动障碍。还提供药物组合物，包括包装的药物组合物。本发明的化合物也可用作组织样品中GABA A受体定位的探针。

3. 发明授权

US06509366B2 Substituted imidazoles as selective modulators of Bradykinin B2 receptors 失效
标题翻译：取代的咪唑作为缓激肽B2受体的选择性调节剂
公开(公告)号：US06509366B2
公开(公告)日：2003-01-21
申请号：US09764805
申请日：2001-01-17
申请人： Stanislaw Rachwal , Alan Hutchison , Kenneth Shaw , George D. Maynard , Xiao-shu He , Robert DeSimone , Kevin Hodgetts
发明人： Stanislaw Rachwal , Alan Hutchison , Kenneth Shaw , George D. Maynard , Xiao-shu He , Robert DeSimone , Kevin Hodgetts
IPC分类号： A61K314174
CPC分类号： C07D233/64 , C07D233/68 , C07D401/06
摘要： Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein Y, R1, R2, R3, R4, R5, R6, R7 R7′ are variables defined herein, which compounds are modulators of Bradykinin B2 receptors. These compounds are therefore useful in the diagnosis and treatment of renal diseases, heart failure, hypertension, Meniere's disease, vaginal inflammation and pain, peripheral circulatory disorders, climacteric disturbance, retinochoroidal circulatory disorders, myocardial ischemia, myocardial infarction, postmyocardial infarction syndrome, angina pectoris, restenosis after percutaneous transluminal coronary angioplasty, hepatitis, liver cirrhosis, pancreatitis, ileus, diabetes, diabetic complications, male infertility, glaucoma, pain, asthma, and rhinitis, and for the increase of permeability of the blood-brain barrier or the blood-brain-tumor barrier.
摘要翻译：公开了下式的化合物或其药学上可接受的无毒盐，其中Y，R 1，R 2，R 3，R 4，R 5，R 6，R 7 R 7'是本文定义的变量，该化合物是缓激肽B2受体的调节剂。因此，这些化合物可用于诊断和治疗肾脏疾病，心力衰竭，高血压，梅尼埃病，阴道炎症和疼痛，外周循环障碍，更年期障碍，视网膜循环障碍，心肌缺血，心肌梗死，心肌梗死后综合征，心绞痛经皮腔内冠状动脉血管成形术，肝炎，肝硬化，胰腺炎，肠梗阻，糖尿病，糖尿病并发症，男性不育症，青光眼，疼痛，哮喘和鼻炎的再狭窄，以及增加血脑屏障或血液 - 脑肿瘤屏障。

4. 发明申请

US20050059826A1 Substituted fused pyrroleoximes and fused pyrazoleoximes 失效
标题翻译：取代的稠合吡咯肟和稠合吡唑肟
公开(公告)号：US20050059826A1
公开(公告)日：2005-03-17
申请号：US10858496
申请日：2004-06-01
申请人： George Maynard , LingHong Xie , Stanislaw Rachwal
发明人： George Maynard , LingHong Xie , Stanislaw Rachwal
IPC分类号： A61K31/4045 , A61P25/20 , A61P25/22 , A61P25/24 , C07D209/42 , C07D231/56 , C07D401/12 , C07D275/04 , C07D261/20
CPC分类号： C07D231/56 , C07D209/42 , C07D401/12
摘要： Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R1 and R2 are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are also disclosed.
摘要翻译：公开了下式的化合物及其药学上可接受的盐，其中R，Ar，A，n，R 1和R 2在本文中定义。这些化合物是GABAA脑受体的高度选择性激动剂，拮抗剂或反向激动剂或GABAA脑受体的激动剂，拮抗剂或反向激动剂的前药，因此可用于诊断和治疗焦虑症，抑郁症，唐氏综合症，睡眠和癫痫发作障碍，过量与苯二氮卓类药物和增强记忆。还公开了药物组合物，包括包装的药物组合物。

5. 发明授权

US06852730B2 Substituted fused pyrazolecarboxylic acid arylamides and related compounds 失效
标题翻译：取代的稠合吡唑甲酰芳基酰胺和相关化合物
公开(公告)号：US06852730B2
公开(公告)日：2005-02-08
申请号：US10360963
申请日：2003-02-07
申请人： George Maynard , Jun Yuan , Stanislaw Rachwal
发明人： George Maynard , Jun Yuan , Stanislaw Rachwal
IPC分类号： G01N33/53 , A61K31/435 , A61K31/4439 , A61K31/519 , A61P25/00 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P43/00 , C07D401/12 , C07D471/04 , C07D487/04 , G01N33/60 , A61K31/437 , A61K31/55 , C07D487/14
CPC分类号： C07D471/04 , C07B2200/05 , C07D487/04
摘要： Heterocyclic compounds such as 3,4,5,6-tetrahydro-2,3,10-triaza-benzo[e]azulene-1-carboxylic acid arylamides, 5,7-Dihydro-6H-pyrazolo[3,4-h]quinoline-9-carboxylic acid arylamides, 5,7-Dihydro-6H-pyrazolo[3,4-h]quinazoline-9-carboxylic acid arylamides, 2,4,5,6-Tetrahydro-1,2,6,7-tetraaza-as-indacene-8-carboxylic acid arylamides and related compounds are disclosed. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the treatment of anxiety, depression, sleep and seizure disorders, overdose with benzodiazepine drugs, Alzheimer's dementia, and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Intermediates useful for the synthesis of pyrazolecarboxylic acid arylamides are also provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.
摘要翻译：杂环化合物如3,4,5,6-四氢-2,3,10-三氮杂 - 苯并[e]薁-1-羧酸芳基酰胺，5,7-二氢-6H-吡唑并[3,4-h] 喹啉-9-羧酸芳基酰胺，5,7-二氢-6H-吡唑并[3,4-h]喹唑啉-9-羧酸芳基酰胺，2,4,5,6-四氢-1,2,6,7- 四氮杂 - 引嗪并] -8-羧酸芳基酰胺和相关化合物。这些化合物是用于GABAA脑受体的G选择性激动剂，拮抗剂或反向激动剂或GABAA脑受体的激动剂，拮抗剂或反向激动剂的前药，因此可用于治疗焦虑，抑郁，睡眠和癫痫发作，用苯二氮卓类药物过量服用，阿尔茨海默病的痴呆，并增强记忆力。还提供药物组合物，包括包装的药物组合物。还提供了可用于合成吡唑甲酰芳基酰胺的中间体。本发明的化合物也可用作组织样品中GABA A受体定位的探针。

6. 发明申请

US20080032975A1 Substituted Fused Pyrroleoximes and Fused Pyrazoleoximes 审中-公开
标题翻译：取代的熔融吡咯肟和稠合吡唑油肟
公开(公告)号：US20080032975A1
公开(公告)日：2008-02-07
申请号：US11872332
申请日：2007-10-15
申请人： George Maynard , LingHong Xie , Stanislaw Rachwal
发明人： George Maynard , LingHong Xie , Stanislaw Rachwal
IPC分类号： A61K31/416 , A61K31/404 , A61K31/4439 , A61K31/50 , A61K31/5377 , A61P25/00 , C07D209/42 , C07D231/54 , C07D401/12 , C07D403/12 , C07D413/12 , G01N33/53
CPC分类号： C07D231/56 , C07D209/42 , C07D401/12
摘要： Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R1 and R2 are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are also disclosed.
摘要翻译：公开了下式的化合物及其药学上可接受的盐，其中R，Ar，A，n，R 1和R 2是本文定义的。这些化合物是高度选择性的激动剂，拮抗剂或反义激动剂，用于GABA A A受体或GABA A A受体的激动剂，拮抗剂或反向激动剂的前药，因此可用于诊断和治疗焦虑症，抑郁症，唐氏综合征，睡眠和癫痫发作障碍，用苯二氮卓类药物服用过量，并增加记忆力。还公开了药物组合物，包括包装的药物组合物。

7. 发明申请

US20050148601A1 Neurokinin-3 receptor modulators: diaryl imidazole derivatives 审中-公开
标题翻译：神经激肽-3受体调节剂：二芳基咪唑衍生物
公开(公告)号：US20050148601A1
公开(公告)日：2005-07-07
申请号：US11007652
申请日：2004-12-07
申请人： George Maynard , Stanislaw Rachwal , Wallace Pringle , Jun Yuan , Linghong Xie , Yuelian Xu , Bingsong Han
发明人： George Maynard , Stanislaw Rachwal , Wallace Pringle , Jun Yuan , Linghong Xie , Yuelian Xu , Bingsong Han
IPC分类号： A61K31/4178 , A61K31/427 , A61K31/4439 , A61K31/498 , A61K31/506 , A61K31/538 , C07D233/54 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/12 , C07D413/02 , C07D413/04 , C07D417/02 , C07D417/04 , C07D43/02
CPC分类号： C07D233/90 , C07D233/64 , C07D405/04
摘要： The invention relates to compounds of general Formula I: wherein the variables are as defined herein. Also provided are pharmaceutical compositions comprising such compounds, and methods for treating patients suffering from a disorder responsive to neurokinin-3 receptor modulation. NK-3 receptor modulators provided herein are also useful as probes for the localization of NK-3 receptors.
摘要翻译：本发明涉及通式I的化合物：其中变量如本文所定义。还提供了包含这些化合物的药物组合物，以及用于治疗患有对神经激肽-3受体调节有响应的病症的患者的方法。本文提供的NK-3受体调节剂也可用作NK-3受体定位的探针。

8. 发明授权

US06656941B2 Aryl substituted tetrahydroindazoles 失效
标题翻译：芳基取代的四氢茚满
公开(公告)号：US06656941B2
公开(公告)日：2003-12-02
申请号：US09947702
申请日：2001-09-06
申请人： George Maynard , Pamela Albaugh , Stanislaw Rachwal , Linda Gustavson
发明人： George Maynard , Pamela Albaugh , Stanislaw Rachwal , Linda Gustavson
IPC分类号： A61K3150
CPC分类号： C07D231/56 , C07D401/12 , G01N2333/70571
摘要： Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein the variables R1, R2, R3, n, and Ar are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.
摘要翻译：公开了下式的化合物及其药学上可接受的盐，其中变量R1，R2，R3，n和Ar如本文所定义。这些化合物是GABAA脑受体的高度选择性激动剂，拮抗剂或反向激动剂或GABAA脑受体的激动剂，拮抗剂或反向激动剂的前药，因此可用于诊断和治疗焦虑症，抑郁症，唐氏综合症，睡眠和癫痫发作障碍，过量与苯二氮卓类药物和增强记忆。

9. 发明申请

US20170044373A1 CHROMOPHORES FOR PHOTOCHROMIC COMPOSITIONS USEFUL FOR THREE DIMENSIONAL DISPLAY APPLICATIONS 审中-公开
标题翻译：用于三维显示应用的光致变色组合物的色素
公开(公告)号：US20170044373A1
公开(公告)日：2017-02-16
申请号：US15306428
申请日：2015-04-21
申请人： Tao Gu , Bogumila Rachwal , Ozair Siddiqui , Stanislaw Rachwal , Isamu Kitahara , Sergey Simavoryan , Peng Wang , Michiharu Yamamoto , NITTO DENKO CORPORATION
发明人： Tao Gu , Bogumila Rachwal , Ozair Siddiqui , Stanislaw Rachwal , Isamu Kitahara , Sergey Simavoryan , Peng Wang , Michiharu Yamamoto
IPC分类号： C09B62/008 , G02B1/04 , G02B5/23
CPC分类号： C09B62/0081 , C07C255/65 , C07D213/42 , C07D231/12 , C07D239/26 , C07D249/06 , C07D261/08 , C08K5/23 , C08L33/12 , C09B29/0003 , C09B29/0011 , C09B29/0807 , C09B62/0083 , C09B62/0086 , C09B62/0088 , C09D133/12 , C09K19/601 , G02B1/04 , G02B5/23 , G11B7/24044 , G11B7/244 , G11B7/245
摘要： Described herein are novel azo-benzene type chromophores. The chromophores are useful in photochromic compositions comprising a polymer matrix and a chromophore, wherein the chromophore is a novel azo-benzene type structure. The photochromic composition is photoresponsive upon irradiation by at least one wavelength of laser light across the visible light spectrum. Photochromic devices which comprise the novel azo-benzene type chromophore compound show significantly higher photoinduced birefringence, higher diffraction efficiency, and brighter images than devices that comprise well known azo-benzene chromophores. The photochromic composition may include a liquid crystal.
摘要翻译：本文描述的是新型偶氮苯型发色团。发色团可用于包含聚合物基质和发色团的光致变色组合物，其中发色团是新颖的偶氮 - 苯型结构。光致变色组合物在通过可见光光谱的至少一个激光波长照射时是光响应的。包含新型偶氮 - 苯型发色团化合物的光致变色装置显示比包含公知的偶氮苯发色团的装置显着更高的光诱导双折射，更高的衍射效率和更亮的图像。光致变色组合物可以包括液晶。

10. 发明授权

US07799913B2 Carbonylbenzoxazine compounds for enhancing glutamatergic synaptic responses 失效
标题翻译：羰基苯并恶嗪化合物用于增强谷氨酸能突触应答
公开(公告)号：US07799913B2
公开(公告)日：2010-09-21
申请号：US10495049
申请日：2002-11-25
申请人： Gary A. Rogers , Matthew Allan , Clayton Harris , Jianjie Huang , Christopher M. Marrs , Rudolf Mueller , Stanislaw Rachwal
发明人： Gary A. Rogers , Matthew Allan , Clayton Harris , Jianjie Huang , Christopher M. Marrs , Rudolf Mueller , Stanislaw Rachwal
IPC分类号： C07D265/12 , C07D265/14 , C07D491/04 , C07D498/04 , C07D513/04 , C07D515/04 , A61K31/536 , A61K31/5365 , A61P25/18
CPC分类号： C07D265/22 , C07D413/06
摘要： This invention related to the prevention and treatment of cerebral insufficiency, including enhancement of receptor functioning in synapses in brain networks responsible for higher order behaviors. These brain networks are involved in cognitive abilities related to memory impairment, such as is observed In a variety of dementias, and in imbalances in neuronal activity between different brain regions, as is suggested in disorders such as Parkinson′s disease, schizophrenia and affective disorders. In a particular aspect, the present invention relates to compounds useful for treatment of such conditions and methods of using these compounds for such treatment.
摘要翻译：本发明涉及预防和治疗脑功能不全，包括增强负责高阶行为的脑网络突触中的受体功能。这些脑网络涉及与记忆障碍相关的认知能力，例如在各种痴呆中观察到的，以及在不同脑区域之间的神经元活动的不平衡，如帕金森病，精神分裂症和情感障碍。在一个具体方面，本发明涉及可用于治疗这些病症的化合物和使用这些化合物进行这种治疗的方法。

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