公开(公告)号：US20090137623A1

公开(公告)日：2009-05-28

申请号：US12158435

申请日：2007-01-02

申请人： Naresh Kumar ,  Ian Anthony Cliffe ,  Mohammad Salman ,  Venkata P. Palle ,  Kirandeep Kaur ,  Yogesh D. Shejul ,  Anita Chugh ,  Suman Gupta ,  Abhijit Ray ,  Shivani Malhotra ,  Raj Kumar Shirumalla

发明人： Naresh Kumar ,  Ian Anthony Cliffe ,  Mohammad Salman ,  Venkata P. Palle ,  Kirandeep Kaur ,  Yogesh D. Shejul ,  Anita Chugh ,  Suman Gupta ,  Abhijit Ray ,  Shivani Malhotra ,  Raj Kumar Shirumalla

IPC分类号： A61K31/439 ,  C07D487/08 ,  A61P1/00 ,  A61P3/10 ,  A61P3/04 ,  A61P11/06

CPC分类号： C07D209/52

摘要： The present invention relates to muscarinic receptor modulators, specifically, 7-oxo-2-azabicyclo[2.2.1]heptanes of formula (I) which are useful for the treatment of various diseases and conditions, for example, Alzheimer's disease, glaucoma, psychosis, particularly schizophrenia or schizophreniform conditions, mania, pain, bipolar disorder, depression, sleeping disorders, epilepsy, gastrointestinal motility disorders, urinary incontinence, and cognition enhancement.

摘要翻译： 本发明涉及可用于治疗各种疾病和病症（例如阿尔茨海默病，青光眼，精神病）的式（I）的毒蕈碱受体调节剂，具体地，7-氧代-2-氮杂双环[2.2.1]庚烷 特别是精神分裂症或精神分裂症状，躁狂症，疼痛，双相情感障碍，抑郁症，睡眠障碍，癫痫，胃肠动力障碍，尿失禁和认知增强。

公开(公告)号：US20090131410A1

公开(公告)日：2009-05-21

申请号：US12089150

申请日：2006-10-05

申请人： Naresh Kumar ,  Kirandeep Kaur ,  Suman Gupta ,  Anita Chugh ,  Mohammad Salman ,  Raj Kumar Shirumalla ,  Shivani Malhotra

发明人： Naresh Kumar ,  Kirandeep Kaur ,  Suman Gupta ,  Anita Chugh ,  Mohammad Salman ,  Raj Kumar Shirumalla ,  Shivani Malhotra

IPC分类号： A61K31/55 ,  C07D223/14 ,  A61P3/10

CPC分类号： C07D221/24 ,  C07D405/12 ,  C07D409/12

摘要： Provided are muscarinic receptor antagonists, which can be useful in treating various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. Also provided are processes for preparing compounds described herein, pharmaceutical compositions thereof, and methods for treating diseases mediated through muscarinic receptors.

摘要翻译： 提供毒蕈碱受体拮抗剂，其可用于治疗通过毒蕈碱受体介导的呼吸，尿和胃肠道系统的各种疾病。 还提供了用于制备本文所述的化合物的方法，其药物组合物，以及用于治疗通过毒蕈碱受体介导的疾病的方法。

公开(公告)号：US20100222393A1

公开(公告)日：2010-09-02

申请号：US12159505

申请日：2006-12-21

申请人： Naresh Kumar ,  Jaskiran Kaur ,  Venkata P. Palle ,  Beenu Bhatt ,  Shelly Jindal ,  Anita Chugh ,  Suman Gupta ,  Abhijit Ray ,  Shivani Malhotra ,  Raj Kumar Shirumalla

发明人： Naresh Kumar ,  Jaskiran Kaur ,  Venkata P. Palle ,  Beenu Bhatt ,  Shelly Jindal ,  Anita Chugh ,  Suman Gupta ,  Abhijit Ray ,  Shivani Malhotra ,  Raj Kumar Shirumalla

IPC分类号： A61K31/4439 ,  C07D233/54 ,  A61K31/4164 ,  C07D401/02 ,  A61P11/00 ,  A61P13/00 ,  A61P1/00 ,  A61P3/04 ,  A61P3/10

CPC分类号： C07D233/54 ,  C07D233/14 ,  C07D233/56 ,  C07D233/64 ,  C07D401/12

摘要： Compounds of Formula (I), wherein represents a single bond when G is —OH and double bond when G is —O; R1 and R2 are independently selected from hydrogen, alkyl, alkenyl, alkynyl, aralkyl, cycloalkyl, aryl, heteroaryl, heterocyclyl, heterocyclylalkyl or heteroarylalkyl; R3 is selected from the group selected from hydrogen, hydroxy, alkoxy, alkenyloxy or alkynyloxy; X is selected from oxygen, —NH, —NR (wherein R is alkyl, alkenyl, alkenyl, alkynyl or aryl), sulphur or no atom; Het is heterocyclyl or heteroaryl; n is an integer from 1 to 6; are muscarinic receptor antagonists, which are useful, among other uses, for the treatment of various diseases of the respiratory, urinary and 4 i gastrointestinal systems mediated through muscarinic receptors.

摘要翻译： 式（I）的化合物，当G为-OH时，当G为-O时，表示单键; R 1和R 2独立地选自氢，烷基，烯基，炔基，芳烷基，环烷基，芳基，杂芳基，杂环基，杂环基烷基或杂芳基烷基; R3选自氢，羟基，烷氧基，烯氧基或炔氧基; X选自氧，-NH，-NR（其中R是烷基，烯基，烯基，炔基或芳基），硫或无原子; Het是杂环基或杂芳基; n是1至6的整数; 是毒蕈碱受体拮抗剂，其可用于治疗通过毒蕈碱受体介导的呼吸，尿和4I胃肠系统的各种疾病，以及其它用途。

公开(公告)号：US20100056496A1

公开(公告)日：2010-03-04

申请号：US12439771

申请日：2007-09-04

申请人： Naresh Kumar ,  Kirandeep Kaur ,  Yogesh D. Shejul ,  Abhijit Ray ,  Suman Gupta ,  Shivani Malhotra ,  Rajkumar Shirumalla

发明人： Naresh Kumar ,  Kirandeep Kaur ,  Yogesh D. Shejul ,  Abhijit Ray ,  Suman Gupta ,  Shivani Malhotra ,  Rajkumar Shirumalla

IPC分类号： A61K31/55 ,  C07D223/14 ,  A61P1/00 ,  A61P11/00 ,  A61P3/00

CPC分类号： C07D221/24 ,  C07D209/12 ,  C07D209/14

摘要： The present invention generally relates to muscarinic receptor antagonists, which are useful, among other uses, for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The present invention also relates to processes for preparing compounds described herein, pharmaceutical compositions thereof, and methods for treating diseases mediated through muscarinic receptors. Formula (I) or a pharmaceutically accepted salt, pharmaceutically acceptable solvate, enantiomers, diastereomer, polymorph or N-oxide thereof, wherein X is.

摘要翻译： 本发明一般涉及毒蕈碱受体拮抗剂，其可用于治疗通过毒蕈碱受体介导的呼吸，泌尿和胃肠系统的各种疾病，以及其它用途。 本发明还涉及制备本文所述化合物的方法，其药物组合物，以及用于治疗通过毒蕈碱受体介导的疾病的方法。 式（I）或其药学上可接受的盐，药学上可接受的溶剂合物，对映异构体，非对映体，多晶型物或N-氧化物，其中X为。

公开(公告)号：US20090105221A1

公开(公告)日：2009-04-23

申请号：US11576096

申请日：2005-09-28

申请人： Mohammad Salman ,  Pakala Kumara Savithru Sarma ,  Arani Pal ,  Anita Chugh ,  Suman Gupta ,  Venkata P. Palle ,  Naresh Kumar ,  Kirandeep Kaur

发明人： Mohammad Salman ,  Pakala Kumara Savithru Sarma ,  Arani Pal ,  Anita Chugh ,  Suman Gupta ,  Venkata P. Palle ,  Naresh Kumar ,  Kirandeep Kaur

IPC分类号： A61K31/55 ,  C07D223/14 ,  C07D405/12 ,  A61P11/00 ,  A61P1/00

CPC分类号： C07D401/12 ,  C07D221/24 ,  C07D405/06 ,  C07D405/12 ,  C07D409/12

摘要： This present invention generally relates to muscarinic receptor antagonists of Formula (I), which are useful, among other uses, for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to the process for the prepration of disclosed compounds, pharmaceutical compositions containing the disclosed compounds, and the methods for treating diseases mediated through muscarinic receptors.

摘要翻译： 本发明一般涉及式（I）的毒蕈碱受体拮抗剂，其可用于治疗通过毒蕈碱受体介导的呼吸，泌尿和胃肠系统的各种疾病。 本发明还涉及所述化合物的制备方法，包含所公开的化合物的药物组合物，以及通过毒蕈碱受体介导的疾病的治疗方法。

公开(公告)号：US20090012116A1

公开(公告)日：2009-01-08

申请号：US11995376

申请日：2006-07-11

申请人： Naresh Kumar ,  Kirandeep Kaur ,  Sandeep Sinha ,  Suman Gupta ,  Venkata P. Palle ,  Anita Chugh

发明人： Naresh Kumar ,  Kirandeep Kaur ,  Sandeep Sinha ,  Suman Gupta ,  Venkata P. Palle ,  Anita Chugh

IPC分类号： A61K31/44 ,  C07D453/02 ,  A61K31/40 ,  C07D487/08

CPC分类号： C07D209/52 ,  C07D405/12 ,  C07D409/12 ,  C07D471/08

摘要： Provided are muscarinic receptor antagonists, which can be useful in treating various diseases of the respiratory, urinary or gastrointestinal system mediated through muscarinic receptors. Also provided are processes for preparing compounds described herein, pharmaceutical compositions comprising compounds described herein, and methods for treating diseases mediated through muscarinic receptors.

摘要翻译： 提供毒蕈碱受体拮抗剂，其可用于治疗通过毒蕈碱受体介导的呼吸，泌尿或胃肠系统的各种疾病。 还提供了用于制备本文所述化合物的方法，包含本文所述化合物的药物组合物，以及用于治疗通过毒蕈碱受体介导的疾病的方法。

公开(公告)号：US20100168197A1

公开(公告)日：2010-07-01

申请号：US12528987

申请日：2008-02-27

申请人： Naresh Kumar ,  Jaskiran Kaur ,  Shelly Aeron ,  Abhijit Ray ,  Suman Gupta ,  Shivani Malhotra ,  Raj Kumar Shirumalla

发明人： Naresh Kumar ,  Jaskiran Kaur ,  Shelly Aeron ,  Abhijit Ray ,  Suman Gupta ,  Shivani Malhotra ,  Raj Kumar Shirumalla

IPC分类号： A61K31/4164 ,  C07D233/54

CPC分类号： C07D235/08 ,  C07D233/54 ,  C07D409/06

摘要： This present invention generally relates to muscarinic receptor antagonists, which are useful, among other uses, for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to the process for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds, and the methods for treating diseases mediated through muscarinic receptors.

摘要翻译： 本发明一般涉及毒蕈碱受体拮抗剂，其可用于治疗通过毒蕈碱受体介导的呼吸，泌尿和胃肠系统的各种疾病，以及其它用途。 本发明还涉及制备所公开的化合物的方法，含有所公开的化合物的药物组合物，以及用于治疗通过毒蕈碱受体介导的疾病的方法。

公开(公告)号：US20100144801A1

公开(公告)日：2010-06-10

申请号：US12443838

申请日：2007-10-02

申请人： Naresh Kumar ,  Jaskiran Kaur ,  Abhijit Ray ,  Suman Gupta ,  Shivani Malhotra ,  Rajkumar Shirumalla

发明人： Naresh Kumar ,  Jaskiran Kaur ,  Abhijit Ray ,  Suman Gupta ,  Shivani Malhotra ,  Rajkumar Shirumalla

IPC分类号： A61K31/44 ,  C07D213/55 ,  C07D233/54 ,  A61K31/4164 ,  A61P11/00 ,  A61P13/00 ,  A61P1/00 ,  A61P3/00

CPC分类号： C07D233/64 ,  C07D211/70 ,  C07D213/30

摘要： The present invention generally relates to muscarinic receptor antagonists of formula I, which are useful, among other uses, for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to the process for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds, and the methods for treating diseases mediated through muscarinic receptors. Formula (I) wherein Het: is heterocyclyl or heteroaryl X: O, S or NR1 and the other substituents are defined as in the claims.

摘要翻译： 本发明一般涉及式I的毒蕈碱受体拮抗剂，其可用于治疗通过毒蕈碱受体介导的呼吸，泌尿和胃肠系统的各种疾病，以及其它用途。 本发明还涉及制备所公开的化合物的方法，含有所公开的化合物的药物组合物，以及用于治疗通过毒蕈碱受体介导的疾病的方法。 式（I）其中Het：是杂环基或杂芳基X：O，S或NR1，其它取代基如权利要求中所定义。

公开(公告)号：US20080319002A1

公开(公告)日：2008-12-25

申请号：US11570749

申请日：2004-06-16

申请人： Anita Mehta ,  Mohammad Salman ,  Pakala Kumara Savithru Sarma ,  Anita Chugh ,  Suman Gupta

发明人： Anita Mehta ,  Mohammad Salman ,  Pakala Kumara Savithru Sarma ,  Anita Chugh ,  Suman Gupta

IPC分类号： A61K31/4353 ,  C07D221/04 ,  A61P1/00 ,  A61P13/02 ,  A61P3/04 ,  A61P3/10 ,  A61P9/00

CPC分类号： C07D405/12 ,  C07D405/14

摘要： This present invention generally relates to xanthine derivatives as muscarinic receptor antagonists which are useful, among other uses, for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to the process for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds, and the methods for treating diseases mediated through muscarinic receptors.

摘要翻译： 本发明一般涉及作为毒蕈碱受体拮抗剂的黄嘌呤衍生物，其可用于治疗通过毒蕈碱受体介导的呼吸，泌尿和胃肠系统的各种疾病。 本发明还涉及制备所公开的化合物的方法，含有所公开的化合物的药物组合物，以及用于治疗通过毒蕈碱受体介导的疾病的方法。

公开(公告)号：US20080280883A1

公开(公告)日：2008-11-13

申请号：US11575825

申请日：2005-09-23

申请人： Mohammad Salman ,  Pakala Kumara Savithru Sarma ,  Sankaranarayanan Dharmarajan ,  Anita Chugh ,  Suman Gupta

发明人： Mohammad Salman ,  Pakala Kumara Savithru Sarma ,  Sankaranarayanan Dharmarajan ,  Anita Chugh ,  Suman Gupta

IPC分类号： A61K31/551 ,  A61K31/439 ,  C07D221/22 ,  C07D265/30 ,  A61P11/00 ,  A61K31/5375 ,  C07D405/08

CPC分类号： C07D295/088 ,  C07D207/14 ,  C07D211/14 ,  C07D211/42 ,  C07D211/44 ,  C07D211/58 ,  C07D223/04 ,  C07D243/08 ,  C07D295/108 ,  C07D307/81 ,  C07D317/58 ,  C07D401/04 ,  C07D471/08 ,  C07D487/08

摘要： This present invention generally relates to muscarinic receptor antagonists which are useful, among other uses, for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to the process for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds, and the methods for treating diseases mediated through muscarinic receptors.

摘要翻译： 本发明一般涉及毒蕈碱受体拮抗剂，其可用于治疗通过毒蕈碱受体介导的呼吸，泌尿和胃肠系统的各种疾病，以及其它用途。 本发明还涉及制备所公开的化合物的方法，含有所公开的化合物的药物组合物，以及用于治疗通过毒蕈碱受体介导的疾病的方法。