公开(公告)号：US20110040105A1

公开(公告)日：2011-02-17

申请号：US12988109

申请日：2009-04-15

申请人： Christian H. Huber ,  Young Mi Khulman ,  Sagun K. Tandel ,  Stephen R. Johannsen ,  Tingmin Wang ,  Paul Angell

发明人： Christian H. Huber ,  Young Mi Khulman ,  Sagun K. Tandel ,  Stephen R. Johannsen ,  Tingmin Wang ,  Paul Angell

IPC分类号： C07D295/023 ,  C07C315/04

CPC分类号： C07D207/06 ,  C07C309/89 ,  C07C313/04 ,  C07C317/18 ,  C07C317/22 ,  C07C317/44

摘要： Processes useful for making a pharmaceutically useful compound according to Formula (I), forms of such a compound, and intermediates useful in such processes are described.

摘要翻译： 描述了可用于制备根据式（I）的药用有用化合物，这种化合物的形式和用于此类方法的中间体的方法。

公开(公告)号：US08853419B2

公开(公告)日：2014-10-07

申请号：US13575458

申请日：2011-01-27

申请人： Antonio Garrido Montalban ,  Daniel J. Buzard ,  John A. DeMattei ,  Tawfik Gharbaoui ,  Stephen R. Johannsen ,  Ashwin M. Krishnan ,  Young Mi Khulman ,  You-An Ma ,  Michael John Martinelli ,  Suzanne Michiko Sato ,  Dipanjan Sengupta

发明人： Antonio Garrido Montalban ,  Daniel J. Buzard ,  John A. DeMattei ,  Tawfik Gharbaoui ,  Stephen R. Johannsen ,  Ashwin M. Krishnan ,  Young Mi Khulman ,  You-An Ma ,  Michael John Martinelli ,  Suzanne Michiko Sato ,  Dipanjan Sengupta

IPC分类号： C07D209/80 ,  A61K31/403 ,  C07D209/94

CPC分类号： C12P17/10 ,  C07B2200/13 ,  C07C17/278 ,  C07D209/80 ,  C07D209/88 ,  C07D209/94 ,  C07D295/155

摘要： The present invention relates to processes and intermediates useful in the preparation of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid of Formula (Ia) and salts thereof, an S1P1 receptor modulator that is useful in the treatment of S1P1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions characterized by an underlying defect in vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development and atherosclerosis).

摘要翻译： 本发明涉及可用于制备（R）-2-（7-（4-环戊基-3-（三氟甲基）苄氧基）-1,2,3,4-四氢环戊二烯并[b]吲哚-3 - 基）乙酸及其盐，可用于治疗S1P1受体相关疾病的S1P1受体调节剂，例如由淋巴细胞介导的疾病和病症，移植排斥反应，自身免疫性疾病和病症，炎性 疾病和病症（例如急性和慢性炎性病症），癌症和特征在于血管完整性的潜在缺陷或与血管发生相关的病症，例如可能是病理性的（例如，可能发生在炎症，肿瘤发展和动脉粥样硬化） 。

公开(公告)号：US20120295947A1

公开(公告)日：2012-11-22

申请号：US13575458

申请日：2011-01-27

申请人： Antonio Garrido Montalban ,  Daniel J. Buzard ,  John A. DeMattei ,  Tawfik Gharbaoui ,  Stephen R. Johannsen ,  Ashwin M. Krishnan ,  Young Mi Khulman ,  You-An Ma ,  Michael John Martinelli ,  Suzanne Michiko Sato ,  Dipanjan Sengupta

发明人： Antonio Garrido Montalban ,  Daniel J. Buzard ,  John A. DeMattei ,  Tawfik Gharbaoui ,  Stephen R. Johannsen ,  Ashwin M. Krishnan ,  Young Mi Khulman ,  You-An Ma ,  Michael John Martinelli ,  Suzanne Michiko Sato ,  Dipanjan Sengupta

IPC分类号： C12P17/10 ,  A61K31/403 ,  A61P25/00 ,  A61P37/06 ,  A61P9/12 ,  A61P17/10 ,  A61P29/00 ,  A61P17/06 ,  C07D209/70 ,  A61P3/10

CPC分类号： C12P17/10 ,  C07B2200/13 ,  C07C17/278 ,  C07D209/80 ,  C07D209/88 ,  C07D209/94 ,  C07D295/155

摘要： The present invention relates to processes and intermediates useful in the preparation of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid of Formula (Ia) and salts thereof, an S1P1 receptor modulator that is useful in the treatment of S1P1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions characterized by an underlying defect in vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development and atherosclerosis).

摘要翻译： 本发明涉及可用于制备（R）-2-（7-（4-环戊基-3-（三氟甲基）苄氧基）-1,2,3,4-四氢环戊二烯并[b]吲哚-3 - 基）乙酸及其盐，可用于治疗S1P1受体相关疾病的S1P1受体调节剂，例如由淋巴细胞介导的疾病和病症，移植排斥反应，自身免疫性疾病和病症，炎性 疾病和病症（例如急性和慢性炎性病症），癌症和特征在于血管完整性的潜在缺陷或与血管发生相关的病症，例如可能是病理性的（例如，可能发生在炎症，肿瘤发展和动脉粥样硬化） 。

公开(公告)号：US20100292288A1

公开(公告)日：2010-11-18

申请号：US12663415

申请日：2008-06-06

申请人： Anthony C. Blackburn ,  John A. DeMattei ,  Ryan M. Hart ,  Young Mi Khulman ,  Michael Mesleh ,  Jeffrey Smith

发明人： Anthony C. Blackburn ,  John A. DeMattei ,  Ryan M. Hart ,  Young Mi Khulman ,  Michael Mesleh ,  Jeffrey Smith

IPC分类号： A61K31/40 ,  C07D207/04 ,  A61P25/28 ,  A61P25/08 ,  A61P25/00 ,  A61P25/24 ,  A61P3/04 ,  A61P25/20 ,  A61P25/18 ,  A61P11/00 ,  A61P29/00

CPC分类号： C07D207/06

摘要： The present invention is directed to novel salts of (R)-1-{2-[4′-(3-methoxy-propane-1-sulfonyl)-biphenyl-4-yl]-ethyl}-2-methyl-pyrrolidine, and crystalline forms, and compositions thereof that modulate the activity of the histamine H3-receptor and are useful in the treatment of histamine H3-receptor 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, pain, dementia, Alzheimer's disease and the like.

摘要翻译： 本发明涉及（R）-1- {2- [4' - （3-甲氧基 - 丙磺酰基） - 联苯-4-基] - 乙基} -2-甲基 - 吡咯烷的新型盐， 调节组胺H3受体活性的结晶形式及其组合物，可用于治疗组胺H3受体相关疾病，例如认知障碍，癫痫，脑创伤，抑郁症，肥胖症，睡眠障碍和 觉醒，如发作性睡病，转移综合征，嗜睡作为药物的副作用，维持警惕以帮助完成任务等，猝死，睡眠过多，嗜睡综合征，时差，睡眠呼吸暂停等，注意力缺陷 过敏性疾病（ADHD），精神分裂症，过敏反应，上呼吸道过敏反应，过敏性鼻炎，鼻充血，疼痛，痴呆，阿尔茨海默氏病等。