公开(公告)号：US20100240653A1

公开(公告)日：2010-09-23

申请号：US12445795

申请日：2007-10-16

申请人： Vincent J. Santora ,  Ryan M. Hart ,  Jason B. Ibarra ,  Douglas M. Park ,  Albert S. Ren ,  Graeme Semple ,  Jeffrey A. Schultz ,  Brian M. Smith ,  Jeffrey Smith

发明人： Vincent J. Santora ,  Ryan M. Hart ,  Jason B. Ibarra ,  Douglas M. Park ,  Albert S. Ren ,  Graeme Semple ,  Jeffrey A. Schultz ,  Brian M. Smith ,  Jeffrey Smith

IPC分类号： A61K31/4025 ,  A61K31/5377 ,  A61K31/506 ,  A61K31/454 ,  A61K31/4439 ,  A61K31/40 ,  C07D413/12 ,  C07D403/10 ,  C07D401/12 ,  C07D401/10 ,  C07D409/10 ,  C07D207/06 ,  A61P25/28 ,  C07D405/10 ,  A61P25/00 ,  A61P25/24 ,  A61P3/04 ,  A61P25/18 ,  A61P37/08 ,  A61P11/00

CPC分类号： C07D207/06 ,  C07D401/12 ,  C07D403/10 ,  C07D405/12 ,  C07D409/10 ,  C07D417/10

摘要： The present invention relates to certain biphenyl sulfonamide derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the histamine H3-receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of histamine H3-associated disorders, such as, cognitive disorders, epilepsy, brain trauma, depression, obesity, disorders of sleep and wakefulness such as narcolepsy, shift-work syndrome, drowsiness as a side effect from a medication, maintenance of vigilance to aid in completion of tasks and the like, cataplexy, hypersomnia, somnolence syndrome, jet lag, sleep apnea and the like, attention deficit hyperactivity disorder (ADHD), schizophrenia, allergies, allergic responses in the upper airway, allergic rhinitis, nasal congestion, dementia, Alzheimer's disease and the like.

摘要翻译： 本发明涉及式（Ia）的某些联苯磺酰胺衍生物及其药物组合物，其调节组胺H3受体的活性。 本发明的化合物及其药物组合物涉及可用于治疗组胺H3相关疾病例如认知障碍，癫痫，脑外伤，抑郁症，肥胖症，睡眠障碍和觉醒症如发作性睡眠， 工作综合征，作为药物副作用的睡意，维持警惕以完成任务等，猝倒，睡眠过多，嗜睡症，时差，睡眠呼吸暂停等，注意力缺陷多动障碍（ADHD），精神分裂症 过敏，上呼吸道过敏反应，过敏性鼻炎，鼻塞，痴呆，阿尔茨海默氏病等。

公开(公告)号：US20080255137A1

公开(公告)日：2008-10-16

申请号：US11792742

申请日：2005-12-09

申请人： Brian M Smith ,  Vincent J. Santora ,  Rena Hayashi ,  Jason B. Ibarra ,  Jeffrey A. Schultz ,  Scott A. Estrada

发明人： Brian M Smith ,  Vincent J. Santora ,  Rena Hayashi ,  Jason B. Ibarra ,  Jeffrey A. Schultz ,  Scott A. Estrada

IPC分类号： A61K31/496 ,  C07D409/10 ,  C07D401/10 ,  C07D405/10 ,  C07D241/04 ,  A61P3/00 ,  A61P25/00

CPC分类号： C07D213/38 ,  C07D213/74 ,  C07D295/033 ,  C07D295/073 ,  C07D307/52 ,  C07D333/20

摘要： The present invention relates to certain N-biaryl and N-arylheteroaryl 2-substituted piperazine derivatives of Formula (Ia) that are modulators of the 5HT2C receptor. Accordingly, compounds of the present invention are useful for the treatment of 5HT2C receptor associated diseases or disorders, such as, obesity, Alzheimer Disease, erectile dysfunction and related disorders.

摘要翻译： 本发明涉及作为5HT 2C受体的调节剂的式（Ia）的某些N-联芳基和N-芳基杂芳基2-取代的哌嗪衍生物。 因此，本发明的化合物可用于治疗5HT 2C受体相关疾病或障碍，如肥胖，阿尔茨海默病，勃起功能障碍和相关疾病。

公开(公告)号：US20080119477A1

公开(公告)日：2008-05-22

申请号：US11792894

申请日：2005-12-09

申请人： Brian M. Smith ,  Vincent J. Santora ,  Rena Hayashi ,  Jason B. Ibarra ,  Jeffrey A. Schultz ,  Scott A. Estrada

发明人： Brian M. Smith ,  Vincent J. Santora ,  Rena Hayashi ,  Jason B. Ibarra ,  Jeffrey A. Schultz ,  Scott A. Estrada

IPC分类号： A61K31/496 ,  A61K31/495 ,  C07D409/02 ,  C07D403/02 ,  C07D405/02

CPC分类号： C07D295/073 ,  C07D213/38 ,  C07D295/096 ,  C07D307/52 ,  C07D333/20

摘要： The present invention relates to certain biarylz and arylheteroaryl piperazine derivatives of Formula (Ia) that are modulators of the 5HT2c receptor. Accordingly, compounds of the present invention are useful for the treatment of 5HT2c receptor associated diseases or disorders, such as, obesity, Alzheimer Disease, erectile dysfunction and related disorders.

摘要翻译： 本发明涉及作为5HT 2C受体的调节剂的式（Ia）的某些双芳基和芳基杂芳基哌嗪衍生物。 因此，本发明的化合物可用于治疗5HT 2C受体相关疾病或病症，例如肥胖症，阿尔茨海默病，勃起功能障碍和相关疾病。

公开(公告)号：US20150191454A1

公开(公告)日：2015-07-09

申请号：US14566019

申请日：2014-12-10

申请人： Thuy-Anh Tran ,  Rena Hayashi ,  Jason B. Ibarra ,  Brett Ullman ,  Ning Zou

发明人： Thuy-Anh Tran ,  Rena Hayashi ,  Jason B. Ibarra ,  Brett Ullman ,  Ning Zou

IPC分类号： C07D409/04 ,  C07D403/04 ,  C07D253/07 ,  C07D237/14 ,  C07D401/04

CPC分类号： C07D237/14 ,  C07D253/07 ,  C07D401/04 ,  C07D403/04 ,  C07D409/04

摘要： Cyclohexane derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pulmonary arterial hypertension (PAH) and related disorders; platelet aggregation; coronary artery disease; myocardial infarction; transient ischemic attack; angina; stroke; ischemia-reperfusion injury; restenosis; atrial fibrillation; blood clot formation in an angioplasty or coronary bypass surgery individual or in an individual suffering from atrial fibrillation; atherosclerosis; atherothrombosis; asthma or a symptom thereof; a diabetic-related disorder such as diabetic peripheral neuropathy, diabetic nephropathy or diabetic retinopathy; glaucoma or other disease of the eye with abnormal intraocular pressure; hypertension; inflammation; psoriasis; psoriatic arthritis; rheumatoid arthritis; Crohn's disease; transplant rejection; multiple sclerosis; systemic lupus erythematosus (SLE); ulcerative colitis; ischemia-reperfusion injury; restenosis; atherosclerosis; acne; type 1 diabetes; type 2 diabetes; sepsis; and chronic obstructive pulmonary disorder (COPD).

摘要翻译： 式Ia的环己烷衍生物及其药物组合物，其调节PGI 2受体的活性。 本发明的化合物及其药物组合物涉及可用于治疗肺动脉高压（PAH）和相关疾病的方法; 血小板聚集; 冠状动脉疾病; 心肌梗死; 短暂性脑缺血发作; 心绞痛 行程; 缺血再灌注损伤; 再狭窄; 房颤; 在血管成形术或冠状动脉旁路手术个体或患有心房颤动的个体中血凝块形成; 动脉粥样硬化 动脉粥样硬化血栓形成 哮喘或其症状; 糖尿病性相关疾病如糖尿病性周围神经病变，糖尿病性肾病或糖尿病性视网膜病变; 青光眼或其他眼睛异常眼内疾病; 高血压; 炎; 银屑病; 牛皮癣关节炎 类风湿关节炎; 克罗恩病; 移植排斥反应 多发性硬化症 系统性红斑狼疮（SLE）; 溃疡性结肠炎 缺血再灌注损伤; 再狭窄; 动脉粥样硬化 粉刺; 1型糖尿病; 2型糖尿病; 败血症 和慢性阻塞性肺疾病（COPD）。

公开(公告)号：US20110224262A1

公开(公告)日：2011-09-15

申请号：US13131203

申请日：2009-11-24

申请人： Thuy-Anh Tran ,  Jason B. Ibarra ,  Young-Jun Shin ,  Brett Ullman ,  Ning Zou ,  Xi Zeng

发明人： Thuy-Anh Tran ,  Jason B. Ibarra ,  Young-Jun Shin ,  Brett Ullman ,  Ning Zou ,  Xi Zeng

IPC分类号： A61K31/4439 ,  C07D231/54 ,  A61K31/416 ,  C07D231/10 ,  A61K31/415 ,  C07D401/04 ,  C07D405/04 ,  C07D409/04 ,  A61K31/4155 ,  A61P9/00 ,  A61P7/02 ,  A61P11/06 ,  A61P3/10 ,  A61P27/06 ,  A61P27/02 ,  A61P29/00 ,  A61P17/06 ,  A61P9/12 ,  A61P19/02 ,  A61P41/00 ,  A61P21/00 ,  A61P1/00

CPC分类号： C07D409/04 ,  A61P9/00 ,  A61P11/00 ,  C07D231/12 ,  C07D231/18 ,  C07D231/54 ,  C07D231/56 ,  C07D401/04 ,  C07D405/04

摘要： Pyrazole derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pulmonary arterial hypertension (PAH) and related disorders; platelet aggregation; coronary artery disease; myocardial infarction; transient ischemic attack; angina; stroke; ischemia-reperfusion injury; restenosis; atrial fibrillation; blood clot formation in an angioplasty or coronary bypass surgery individual or in an individual suffering from atrial fibrillation; atherosclerosis; atherothrombosis; asthma or a symptom thereof; a diabetic-related disorder such as diabetic peripheral neuropathy, diabetic nephropathy or diabetic retinopathy; glaucoma or other disease of the eye with abnormal intraocular pressure; hypertension; inflammation; psoriasis; psoriatic arthritis; rheumatoid arthritis; Crohn's disease; transplant rejection; multiple sclerosis; systemic lupus erythematosus (SLE); ulcerative colitis; ischemia-reperfusion injury; restenosis; atherosclerosis; acne; type 1 diabetes; type 2 diabetes; sepsis; and chronic obstructive pulmonary disorder (COPD).

摘要翻译： 式Ia的吡唑衍生物及其药物组合物，其调节PGI 2受体的活性。 本发明的化合物及其药物组合物涉及可用于治疗肺动脉高压（PAH）和相关疾病的方法; 血小板聚集; 冠状动脉疾病; 心肌梗死; 短暂性脑缺血发作; 心绞痛 行程; 缺血再灌注损伤; 再狭窄; 房颤; 在血管成形术或冠状动脉旁路手术个体或患有心房颤动的个体中血凝块形成; 动脉粥样硬化 动脉粥样硬化血栓形成 哮喘或其症状; 糖尿病性相关疾病如糖尿病性周围神经病变，糖尿病性肾病或糖尿病性视网膜病变; 青光眼或其他眼睛异常眼内疾病; 高血压; 炎; 银屑病; 牛皮癣关节炎 类风湿关节炎; 克罗恩病; 移植排斥反应 多发性硬化症 系统性红斑狼疮（SLE）; 溃疡性结肠炎 缺血再灌注损伤; 再狭窄; 动脉粥样硬化 粉刺; 1型糖尿病; 2型糖尿病; 败血症 和慢性阻塞性肺疾病（COPD）。

公开(公告)号：US07153875B2

公开(公告)日：2006-12-26

申请号：US10094142

申请日：2002-03-07

申请人： Magnus Pfahl ,  Catherine Tachdjian ,  Hussien A. Al-Shamma ,  Andrea Fanjul ,  David P.M. Pleynet ,  Lyle W. Spruce ,  Torsten R. Wiemann ,  Jason B. Ibarra

发明人： Magnus Pfahl ,  Catherine Tachdjian ,  Hussien A. Al-Shamma ,  Andrea Fanjul ,  David P.M. Pleynet ,  Lyle W. Spruce ,  Torsten R. Wiemann ,  Jason B. Ibarra

IPC分类号： C07D401/06 ,  A61K31/44

CPC分类号： C07D277/20 ,  C07D277/34 ,  C07D417/06 ,  C07D417/10 ,  C07D417/14

摘要： The invention relates to certain heterocyclic compounds useful for the treatment of cancer and other diseases, having the Formula (I): wherein: (a) m is an integer 0 or 1; (b) R12 is an alkyl, a substituted alkyl, a cycloalkyl, a substituted cycloalkyl, a heterocyclic, a substituted heterocyclic, a heteroaryl, a substituted heteroaryl, an aryl or a substituted aryl residue; (c) Ar3 is an aryl, a substituted aryl, a heteroaryl or a substituted heteroaryl residue; (d) Ar4 is an aryl, a substituted aryl, a heteroaryl or a substituted heteroaryl residue; (e) R5 is hydrogen, hydroxy, alkyl or substituted alkyl; (f) ----- represents a bond present or absent; and (g) W, X, Y and Z are independently or together —C(O)—, C(S), S, O, or NH; or a pharmaceutically acceptable salt thereof.

摘要翻译： 本发明涉及可用于治疗癌症和其它疾病的某些杂环化合物，其具有式（I）：其中：（a）m为整数0或1; （b）R 12是烷基，取代的烷基，环烷基，取代的环烷基，杂环，取代的杂环，杂芳基，取代的杂芳基，芳基或取代的芳基; （c）Ar 3是芳基，取代的芳基，杂芳基或取代的杂芳基残基; （d）Ar 4是芳基，取代的芳基，杂芳基或取代的杂芳基残基; （e）R 5是氢，羟基，烷基或取代的烷基; （f）-----代表存在或不存在的债券; 和（g）W，X，Y和Z独立地或一起为-C（O） - ，C（S），S，O或NH; 或其药学上可接受的盐。

公开(公告)号：US08940891B2

公开(公告)日：2015-01-27

申请号：US13133036

申请日：2009-12-07

申请人： Thuy-Anh Tran ,  Rena Hayashi ,  Jason B. Ibarra ,  Brett Ullman ,  Ning Zou

发明人： Thuy-Anh Tran ,  Rena Hayashi ,  Jason B. Ibarra ,  Brett Ullman ,  Ning Zou

IPC分类号： C07D253/07 ,  C07D401/04 ,  C07D403/04 ,  A61K31/53 ,  A61K31/4427 ,  A61P9/12 ,  A61P11/08 ,  C07D409/04 ,  C07D237/14 ,  A61K31/50 ,  A61K31/501

CPC分类号： C07D237/14 ,  C07D253/07 ,  C07D401/04 ,  C07D403/04 ,  C07D409/04

摘要： Cyclohexane derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pulmonary arterial hypertension (PAH) and related disorders; platelet aggregation; coronary artery disease; myocardial infarction; transient ischemic attack; angina; stroke; ischemia-reperfusion injury; restenosis; atrial fibrillation; blood clot formation in an angioplasty or coronary bypass surgery individual or in an individual suffering from atrial fibrillation; atherosclerosis; atherothrombosis; asthma or a symptom thereof; a diabetic-related disorder such as diabetic peripheral neuropathy, diabetic nephropathy or diabetic retinopathy; glaucoma or other disease of the eye with abnormal intraocular pressure; hypertension; inflammation; psoriasis; psoriatic arthritis; rheumatoid arthritis; Crohn's disease; transplant rejection; multiple sclerosis; systemic lupus erythematosus (SLE); ulcerative colitis; ischemia-reperfusion injury; restenosis; atherosclerosis; acne; type 1 diabetes; type 2 diabetes; sepsis; and chronic obstructive pulmonary disorder (COPD).

摘要翻译： 式Ia的环己烷衍生物及其药物组合物，其调节PGI 2受体的活性。 本发明的化合物及其药物组合物涉及可用于治疗肺动脉高压（PAH）和相关疾病的方法; 血小板聚集; 冠状动脉疾病; 心肌梗死; 短暂性脑缺血发作; 心绞痛 行程; 缺血再灌注损伤; 再狭窄; 房颤; 在血管成形术或冠状动脉旁路手术个体或患有心房颤动的个体中血凝块形成; 动脉粥样硬化 动脉粥样硬化血栓形成 哮喘或其症状; 糖尿病性相关疾病如糖尿病性周围神经病变，糖尿病性肾病或糖尿病性视网膜病变; 青光眼或其他眼睛异常眼内疾病; 高血压; 炎; 银屑病; 牛皮癣关节炎 类风湿关节炎; 克罗恩病; 移植排斥反应 多发性硬化症 系统性红斑狼疮（SLE）; 溃疡性结肠炎 缺血再灌注损伤; 再狭窄; 动脉粥样硬化; 粉刺; 1型糖尿病; 2型糖尿病; 败血症 和慢性阻塞性肺疾病（COPD）。

公开(公告)号：US20110245251A1

公开(公告)日：2011-10-06

申请号：US13133036

申请日：2009-12-07

申请人： Thuy-Anh Tran ,  Rena Hayashi ,  Jason B. Ibarra ,  Brett Ullman ,  Ning Zou

发明人： Thuy-Anh Tran ,  Rena Hayashi ,  Jason B. Ibarra ,  Brett Ullman ,  Ning Zou

IPC分类号： A61K31/53 ,  C07D237/14 ,  C07D401/04 ,  C07D409/04 ,  C07D403/04 ,  C07D253/07 ,  A61K31/50 ,  A61K31/501 ,  C12N5/071 ,  A61P9/12 ,  A61P7/02 ,  A61P9/00 ,  A61P9/10 ,  A61P11/06 ,  A61P3/10 ,  A61P13/12 ,  A61P27/02 ,  A61P25/02 ,  A61P27/06 ,  A61P29/00 ,  A61P17/06 ,  A61P19/02 ,  A61P37/06 ,  A61P25/28 ,  A61P17/10 ,  A61P11/00

CPC分类号： C07D237/14 ,  C07D253/07 ,  C07D401/04 ,  C07D403/04 ,  C07D409/04

摘要： Cyclohexane derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pulmonary arterial hypertension (PAH) and related disorders; platelet aggregation; coronary artery disease; myocardial infarction; transient ischemic attack; angina; stroke; ischemia-reperfusion injury; restenosis; atrial fibrillation; blood clot formation in an angioplasty or coronary bypass surgery individual or in an individual suffering from atrial fibrillation; atherosclerosis; atherothrombosis; asthma or a symptom thereof; a diabetic-related disorder such as diabetic peripheral neuropathy, diabetic nephropathy or diabetic retinopathy; glaucoma or other disease of the eye with abnormal intraocular pressure; hypertension; inflammation; psoriasis; psoriatic arthritis; rheumatoid arthritis; Crohn's disease; transplant rejection; multiple sclerosis; systemic lupus erythematosus (SLE); ulcerative colitis; ischemia-reperfusion injury; restenosis; atherosclerosis; acne; type 1 diabetes; type 2 diabetes; sepsis; and chronic obstructive pulmonary disorder (COPD).

摘要翻译： 式Ia的环己烷衍生物及其药物组合物，其调节PGI 2受体的活性。 本发明的化合物及其药物组合物涉及可用于治疗肺动脉高压（PAH）和相关疾病的方法; 血小板聚集; 冠状动脉疾病; 心肌梗死; 短暂性脑缺血发作; 心绞痛 行程; 缺血再灌注损伤; 再狭窄; 房颤; 在血管成形术或冠状动脉旁路手术个体或患有心房颤动的个体中血凝块形成; 动脉粥样硬化 动脉粥样硬化血栓形成 哮喘或其症状; 糖尿病性相关疾病如糖尿病性周围神经病变，糖尿病性肾病或糖尿病性视网膜病变; 青光眼或其他眼睛异常眼内疾病; 高血压; 炎; 银屑病; 牛皮癣关节炎 类风湿关节炎; 克罗恩病; 移植排斥反应 多发性硬化症 系统性红斑狼疮（SLE）; 溃疡性结肠炎 缺血再灌注损伤; 再狭窄; 动脉粥样硬化 粉刺; 1型糖尿病; 2型糖尿病; 败血症 和慢性阻塞性肺疾病（COPD）。