公开(公告)号：US20140051676A1

公开(公告)日：2014-02-20

申请号：US14054221

申请日：2013-10-15

Applicant: Oliver BARKER ,  Jonathan Mark BENTLY ,  Mark Gary BOCK ,  Thomas CAIN ,  Praful CHOVATIA ,  Jennifer Ruth DOD ,  Florence EUSTACHE ,  Laura GLEAVE ,  Jonathan HARGRAVE ,  Alexander HEIFETZ ,  Richard LAW ,  Ali RAOOF ,  David WILLOWS

Inventor： Oliver BARKER ,  Jonathan Mark BENTLY ,  Mark Gary BOCK ,  Thomas CAIN ,  Praful CHOVATIA ,  Jennifer Ruth DOD ,  Florence EUSTACHE ,  Laura GLEAVE ,  Jonathan HARGRAVE ,  Alexander HEIFETZ ,  Richard LAW ,  Ali RAOOF ,  David WILLOWS

IPC: C07D413/04 ,  A61K31/53 ,  A61K45/06 ,  C07D451/02 ,  C07D491/107 ,  C07D487/04 ,  C07D498/08 ,  C07D413/14 ,  C07D417/14

CPC classification number: C07D413/14 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/5386 ,  A61K45/06 ,  C07D413/04 ,  C07D417/14 ,  C07D451/02 ,  C07D487/04 ,  C07D491/10 ,  C07D491/107 ,  C07D498/08

Abstract: The invention relates to new derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of chronic pain.

公开(公告)号：US09346816B2

公开(公告)日：2016-05-24

申请号：US14072324

申请日：2013-11-05

Applicant: Stephan-Georg Mueller ,  Christopher John Brown ,  Alexander Heifetz ,  Bernd Nosse ,  Juergen Prestle ,  Natacha Prevost ,  Klaus Rudolf ,  Stefan Scheuerer ,  Marcus Schindler ,  Dirk Stenkamp ,  Leo Thomas ,  Heather Tye

Inventor： Stephan-Georg Mueller ,  Christopher John Brown ,  Alexander Heifetz ,  Bernd Nosse ,  Juergen Prestle ,  Natacha Prevost ,  Klaus Rudolf ,  Stefan Scheuerer ,  Marcus Schindler ,  Dirk Stenkamp ,  Leo Thomas ,  Heather Tye

IPC: A61K31/55 ,  C07D487/14

CPC classification number: C07D487/14

Abstract: The present invention relates to compounds defined by formula I wherein the groups X, Y, W and R1 to R4 are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are agonists of the 5-HT2C receptor, and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this receptor, such as metabolic and CNS-related disorders.

Abstract translation: 本发明涉及由式I定义的化合物，其中基团X，Y，W和R 1至R 4如权利要求1所定义，具有有价值的药理学活性。 特别地，这些化合物是5-HT 2C受体的激动剂，因此适用于治疗和预防可被受体抑制影响的疾病，如代谢和CNS相关疾病。

公开(公告)号：US20120242544A1

公开(公告)日：2012-09-27

申请号：US13422832

申请日：2012-03-16

Applicant: Nachappa Gopalsami ,  Alexander Heifetz ,  Hual-Te Chien ,  Shaolin Liao ,  Eugene R. Koehl ,  Apostolos C. Raptis

Inventor： Nachappa Gopalsami ,  Alexander Heifetz ,  Hual-Te Chien ,  Shaolin Liao ,  Eugene R. Koehl ,  Apostolos C. Raptis

IPC: G01S13/95

CPC classification number: G01S13/95 ,  G01N21/3581 ,  G01N21/3586 ,  G01N21/359 ,  G01S13/58 ,  G01S13/958 ,  G01T7/00 ,  Y02A90/18

Abstract: A millimeter wave measurement system has been developed for remote detection of airborne nuclear radiation, based on electromagnetic scattering from radiation-induced ionization in air. Specifically, methods of monitoring radiation-induced ionization of air have been investigated, and the ionized air has been identified as a source of millimeter wave radar reflection, which can be utilized to determine the size and strength of a radiation source.

Abstract translation: 已经开发了一种基于空气中辐射诱导电离的电磁散射的空中核辐射的远程检测的毫米波测量系统。 具体来说，已经研究了辐射诱导的空气电离的监测方法，电离空气已被确定为毫米波雷达反射源，可用于确定辐射源的尺寸和强度。

公开(公告)号：US20100113485A1

公开(公告)日：2010-05-06

申请号：US12609470

申请日：2009-10-30

Applicant: Dale S. Dhanoa ,  Oren Becker ,  Silvia Noiman ,  Sekar Reddy Alla ,  Srinivasa Rao Cheruku ,  Rosa E. Mele'ndez ,  Anurag Sharadendu ,  Dongli Chen ,  Yael Marantz ,  Sharon Shacham ,  Alexander Heifetz ,  Boaz Inbal ,  Venkitasamy Kesavan ,  Shay Bar-Haim

Inventor： Dale S. Dhanoa ,  Oren Becker ,  Silvia Noiman ,  Sekar Reddy Alla ,  Srinivasa Rao Cheruku ,  Rosa E. Mele'ndez ,  Anurag Sharadendu ,  Dongli Chen ,  Yael Marantz ,  Sharon Shacham ,  Alexander Heifetz ,  Boaz Inbal ,  Venkitasamy Kesavan ,  Shay Bar-Haim

IPC: A61K31/519 ,  C07D495/04 ,  A61P35/00 ,  A61P9/12 ,  A61P15/10 ,  A61P9/00 ,  A61P25/06 ,  A61P1/00 ,  A61P11/06 ,  A61P11/00 ,  A61P29/00 ,  A61P25/00 ,  A61P25/28 ,  A61P25/24 ,  A61P25/22 ,  A61P15/00 ,  A61P19/00 ,  A61P5/00 ,  A61P5/08

CPC classification number: C07D495/04

Abstract: The invention relates to 5-HT receptor modulators, particularly 5-HT2B antagonists. Novel piperidinylamino-thieno[2,3-d]pyrimidine compounds represented by Formula I, II and III, and uses thereof for treating conditions including pulmonary arterial hypertension, congestive heart failure, and hypertension.

Abstract translation: 本发明涉及5-HT受体调节剂，特别是5-HT 2B拮抗剂。 由式I，II和III表示的新型哌啶基氨基 - 噻吩并[2,3-d]嘧啶化合物及其用于治疗包括肺动脉高压，充血性心力衰竭和高血压的病症的用途。

公开(公告)号：US07576211B2

公开(公告)日：2009-08-18

申请号：US11269042

申请日：2005-11-08

Applicant: Dale S. Dhanoa ,  Oren Becker ,  Silvia Noiman ,  Dongli Chen ,  Yael Marantz ,  Sharon Shacham ,  Alexander Heifetz ,  Boaz Inbal ,  Shay Bar-Haim ,  Pradyumna Mohanty ,  Mercedes Lobera ,  Laurence Wu

Inventor： Dale S. Dhanoa ,  Oren Becker ,  Silvia Noiman ,  Dongli Chen ,  Yael Marantz ,  Sharon Shacham ,  Alexander Heifetz ,  Boaz Inbal ,  Shay Bar-Haim ,  Pradyumna Mohanty ,  Mercedes Lobera ,  Laurence Wu

IPC: C07D495/04

CPC classification number: C07D495/04

Abstract: The invention relates to 5-HT receptor agonists and partial agonists. Novel thienopyridinone compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include Alzheimer's disease, cognition disorders, irritable bowel syndrome, nausea, emesis, vomiting, prokinesia, gastroesophageal reflux disease, nonulcer dyspepsia, depression, anxiety, urinary incontinence, migraine, arrhythmia, atrial fibrillation, ischemic stroke, gastritis, gastric emptying disorders, feeding disorders, gastrointestinal disorders, constipation, erectile dysfunction, and respiratory depression. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.

Abstract translation: 本发明涉及5-HT受体激动剂和部分激动剂。 公开了由式I表示的新型噻吩并吡啶酮化合物及其用于治疗由5-HT受体直接或间接介导的疾病的合成和用途。 这些病症包括阿尔茨海默病，认知障碍，肠易激综合征，恶心，呕吐，呕吐，运动失调，胃食管反流病，非溃疡性消化不良，抑郁症，焦虑症，尿失禁，偏头痛，心律失常，心房颤动，缺血性卒中，胃炎，胃排空障碍 ，喂食障碍，胃肠道疾病，便秘，勃起功能障碍和呼吸抑制。 还包括制备方法和新型中间体及其药物盐。

公开(公告)号：US07491727B2

公开(公告)日：2009-02-17

申请号：US11516345

申请日：2006-09-05

Applicant: Dale S. Dhanoa ,  Dongli Chen ,  Oren Becker ,  Silvia Noiman ,  Srinivasa R. Cheruku ,  Yael Marantz ,  Anurag Sharadendu ,  Sharon Shacham ,  Alexander Heifetz ,  Pradyumna Mohanty ,  Boaz Inbal ,  Merav Fichman ,  Raphael Nudelman ,  Shay Bar-Haim

Inventor： Dale S. Dhanoa ,  Dongli Chen ,  Oren Becker ,  Silvia Noiman ,  Srinivasa R. Cheruku ,  Yael Marantz ,  Anurag Sharadendu ,  Sharon Shacham ,  Alexander Heifetz ,  Pradyumna Mohanty ,  Boaz Inbal ,  Merav Fichman ,  Raphael Nudelman ,  Shay Bar-Haim

IPC: A61K31/495 ,  A61K31/496

CPC classification number: C07D213/74 ,  C07D211/96 ,  C07D239/42 ,  C07D295/13 ,  C07D401/12

Abstract: The invention relates to 5-HT receptor agonists or antagonists. Novel arylpiperazinyl sulfonamide compounds represented by Formula I, and synthesis and uses thereof for treating diseases including those mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include central nervous system disorders such as generalized anxiety disorder, ADD/ADHD, neural injury, stroke, and migraine. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.

Abstract translation: 本发明涉及5-HT受体激动剂或拮抗剂。 公开了由式I表示的新型芳基哌嗪基磺酰胺化合物及其用于治疗包括由5-HT受体直接或间接介导的疾病的疾病的合成和用途。 这些病症包括中枢神经系统疾病，如广泛性焦虑症，ADD / ADHD，神经损伤，中风和偏头痛。 还包括制备方法和新型中间体及其药物盐。

公开(公告)号：US07488736B2

公开(公告)日：2009-02-10

申请号：US10955434

申请日：2004-09-30

Applicant: Dale S. Dhanoa ,  Oren Becker ,  Silvia Noiman ,  Pradyumna Mohanty ,  Dongli Chen ,  Mercedes Lobera ,  Laurence Wu ,  Yael Marantz ,  Boaz Inbal ,  Alexander Heifetz ,  Shay Bar-Haim ,  Sharon Shacham

Inventor： Dale S. Dhanoa ,  Oren Becker ,  Silvia Noiman ,  Pradyumna Mohanty ,  Dongli Chen ,  Mercedes Lobera ,  Laurence Wu ,  Yael Marantz ,  Boaz Inbal ,  Alexander Heifetz ,  Shay Bar-Haim ,  Sharon Shacham

IPC: A01N43/42 ,  C07D471/02

CPC classification number: C07D495/04

Abstract: The invention relates to 5-HT receptor agonists and partial agonists. Thienopyridinone compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include Alzheimer's disease, cognition disorders, irritable bowel syndrome, nausea, emesis, vomiting, prokinesia, gastroesophageal reflux disease, nonulcer dyspepsia, depression, anxiety, urinary incontinence, migraine, arrhythmia, atrial fibrillation, ischemic stroke, gastritis, gastric emptying disorders, feeding disorders, gastrointestinal disorders, constipation, erectile dysfunction, and respiratory depression. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.

Abstract translation: 本发明涉及5-HT受体激动剂和部分激动剂。 公开了由式I表示的噻吩并吡啶酮化合物及其用于治疗由5-HT受体直接或间接介导的疾病的合成及其用途。 这些病症包括阿尔茨海默病，认知障碍，肠易激综合征，恶心，呕吐，呕吐，运动失调，胃食管反流病，非溃疡性消化不良，抑郁症，焦虑症，尿失禁，偏头痛，心律失常，心房颤动，缺血性卒中，胃炎，胃排空障碍 ，喂食障碍，胃肠道疾病，便秘，勃起功能障碍和呼吸抑制。 还包括制备方法和新型中间体及其药物盐。

公开(公告)号：US20050222175A1

公开(公告)日：2005-10-06

申请号：US10947995

申请日：2004-09-23

Applicant: Dale Dhanoa ,  Oren Becker ,  Silvia Noiman ,  Sekar Reddy ,  Srinivasa Cheruku ,  Rosa Mele'ndez ,  Anurag Sharadendu ,  Dongli Chen ,  Yael Marantz ,  Sharon Shacham ,  Alexander Heifetz ,  Boaz Inbal ,  Venkitasamy Kesavan ,  Shay Bar-Haim

Inventor： Dale Dhanoa ,  Oren Becker ,  Silvia Noiman ,  Sekar Reddy ,  Srinivasa Cheruku ,  Rosa Mele'ndez ,  Anurag Sharadendu ,  Dongli Chen ,  Yael Marantz ,  Sharon Shacham ,  Alexander Heifetz ,  Boaz Inbal ,  Venkitasamy Kesavan ,  Shay Bar-Haim

IPC: A61K31/519 ,  C07D495/04 ,  C07D498/02

CPC classification number: C07D495/04

Abstract: The invention relates to 5-HT receptor antagonists. Novel piperidinylamino-thieno [2,3-d]pyrimidine compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include central nervous system disorders such as pulmonary arterial hypertension, migraine, hypertension, disorders of the gastrointestinal tract, restenosis, asthma, obstructive airway disease, prostatic hyperplasia and priapism, anxiety, depression, schizophrenia, neural injury and stroke. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also provided.

Abstract translation: 本发明涉及5-HT受体拮抗剂。 公开了由式I表示的新型哌啶基氨基 - 噻吩并[2,3-d]嘧啶化合物及其用于治疗由5-HT受体直接或间接介导的疾病的合成和用途。 这些病症包括中枢神经系统疾病如肺动脉高压，偏头痛，高血压，胃肠道疾病，再狭窄，哮喘，阻塞性气道疾病，前列腺增生和阴茎异常勃起，焦虑，抑郁，精神分裂症，神经损伤和中风。 还提供了制备方法和新型中间体及其药用盐。

公开(公告)号：US08941061B2

公开(公告)日：2015-01-27

申请号：US13432743

申请日：2012-03-28

Applicant: Nachappa Gopalsami ,  Shaolin Liao ,  Thomas W. Elmer ,  Eugene R. Koehl ,  Alexander Heifetz ,  Apostolos C. Raptis

Inventor： Nachappa Gopalsami ,  Shaolin Liao ,  Thomas W. Elmer ,  Eugene R. Koehl ,  Alexander Heifetz ,  Apostolos C. Raptis

IPC: G01S13/00

CPC classification number: G01S13/89 ,  G01K11/006

Abstract: A compressive scanning approach for millimeter wave imaging and sensing. A Hadamard mask is positioned to receive millimeter waves from an object to be imaged. A subset of the full set of Hadamard acquisitions is sampled. The subset is used to reconstruct an image representing the object.

Abstract translation: 用于毫米波成像和感测的压缩扫描方法。 Hadamard面罩定位成从要成像的物体接收毫米波。 对全套Hadamard收购的一个子集进行抽样。 该子集用于重建表示对象的图像。

公开(公告)号：US20130257646A1

公开(公告)日：2013-10-03

申请号：US13432743

申请日：2012-03-28

Applicant: Nachappa GOPALSAMI ,  Shaolin Liao ,  Thomas W. Elmer ,  Eugene R. Koehl ,  Alexander Heifetz ,  Apostolos C. Raptis

Inventor： Nachappa GOPALSAMI ,  Shaolin Liao ,  Thomas W. Elmer ,  Eugene R. Koehl ,  Alexander Heifetz ,  Apostolos C. Raptis

IPC: G01S13/00

CPC classification number: G01S13/89 ,  G01K11/006

Abstract: A compressive scanning approach for millimeter wave imaging and sensing. A Hadamard mask is position to receive millimeter waves from an object to be imaged. A subset of the full set of Hadamard acquisitions is sampled. The subset is used to reconstruct an image representing the object.

Abstract translation: 用于毫米波成像和感测的压缩扫描方法。 Hadamard面具可以从要成像的物体接收毫米波。 对全套Hadamard收购的一个子集进行抽样。 该子集用于重建表示对象的图像。