公开(公告)号：US20110034500A1

公开(公告)日：2011-02-10

申请号：US12855514

申请日：2010-08-12

Applicant: Mikhail Chafeev ,  Sultan Chowdhury ,  Robert Fraser ,  Jianmin Fu ,  Rajender Kamboj ,  Shifeng Liu ,  Mehran Seid Bagherzadeh ,  Jianyu Sun ,  Serguei Sviridov

Inventor： Mikhail Chafeev ,  Sultan Chowdhury ,  Robert Fraser ,  Jianmin Fu ,  Rajender Kamboj ,  Shifeng Liu ,  Mehran Seid Bagherzadeh ,  Jianyu Sun ,  Serguei Sviridov

IPC: A61K31/438 ,  C07D491/22 ,  C07D495/22 ,  A61K31/407 ,  A61P29/00 ,  A61P25/24 ,  A61P9/00 ,  A61P11/00 ,  A61P25/00 ,  A61P25/06 ,  A61P25/04

CPC classification number: C07D491/22 ,  C07D495/22

Abstract: This invention is directed to spiroheterocyclic compounds of formula (I): wherein k, j, p, Q, R1, R3a, R3b, R3e, and R3d are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, that are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain. Pharmaceutical compositions comprising the compounds and methods of using the compounds are also disclosed.

Abstract translation: 本发明涉及式（I）的螺杂环化合物：其中k，j，p，Q，R1，R3a，R3b，R3e和R3d如本文所定义，作为其立体异构体，对映异构体，互变异构体或其混合物; 或其药学上可接受的盐，溶剂化物或前药，其可用于治疗和/或预防钠通道介导的疾病或病症，例如疼痛。 还公开了包含该化合物的药物组合物和使用该化合物的方法。

公开(公告)号：US20100240713A1

公开(公告)日：2010-09-23

申请号：US12663104

申请日：2008-06-05

Applicant: Jean-Jacques Cadieux ,  Mikhail Chafeev ,  Julia Fonarev ,  Jianmin Fu ,  Rajender Kamboj ,  Vishnumurthy Kodumuru ,  Serguei Sviridov ,  Zaihui Zhang

Inventor： Jean-Jacques Cadieux ,  Mikhail Chafeev ,  Julia Fonarev ,  Jianmin Fu ,  Rajender Kamboj ,  Vishnumurthy Kodumuru ,  Serguei Sviridov ,  Zaihui Zhang

IPC: A61K31/44 ,  C07C211/50 ,  C07C261/04 ,  C07C22/04 ,  C07C33/26 ,  C07D333/12 ,  C07D333/16 ,  C07D495/02 ,  C07D249/14 ,  C07D213/53 ,  A61K31/135 ,  A61K31/165 ,  A61K31/03 ,  A61K31/047 ,  A61K31/381 ,  A61K31/4196 ,  A61P43/00

CPC classification number: A61K31/155 ,  A61K31/275 ,  A61K31/381 ,  A61K31/4196 ,  A61K31/44 ,  Y02A50/411

Abstract: This invention is directed to compounds of formula (I), wherein m, formula (II), R1, R2 and R3 are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, for the treatment of iron disorders. This invention is also directed to pharmaceutical compositions comprising the compounds and methods of using the compounds to treat iron disorders.

Abstract translation: 本发明涉及式（I）化合物，其中m，式（II），R 1，R 2和R 3如本文所定义，为其立体异构体，对映异构体，互变异构体或其混合物; 或其药学上可接受的盐，溶剂合物或前药，用于治疗铁疾病。 本发明还涉及包含该化合物的药物组合物和使用该化合物治疗铁疾病的方法。

公开(公告)号：US07777036B2

公开(公告)日：2010-08-17

申请号：US11575638

申请日：2005-09-20

Applicant: Rajender Kamboj ,  Zaihui Zhang ,  Jianmin Fu ,  Mehran Seid Bagherzadeh ,  Serguei Sviridov ,  Sultan Chowdhury ,  Shifeng Liu ,  Vishnumurthy Kodumuru

Inventor： Rajender Kamboj ,  Zaihui Zhang ,  Jianmin Fu ,  Mehran Seid Bagherzadeh ,  Serguei Sviridov ,  Sultan Chowdhury ,  Shifeng Liu ,  Vishnumurthy Kodumuru

IPC: C07D419/00 ,  C07D413/00 ,  C07D405/00 ,  C07D277/00

CPC classification number: C07D213/82

Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I) where y, G, K, L, M, W, V, R2, R3, R4a, R6, R6a, R7, R7a, R8 and R8a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.

Abstract translation: 公开了在哺乳动物，优选人中治疗SCD介导的疾病或病症的方法，其中所述方法包括向有需要的哺乳动物施用式（I）化合物，其中y，G，K，L，M， W，V，R2，R3，R4a，R6，R6a，R7，R7a，R8和R8a在本文中定义。 还公开了包含式（I）化合物的药物组合物。

公开(公告)号：US07754711B2

公开(公告)日：2010-07-13

申请号：US11055034

申请日：2005-02-09

Applicant: Nagasree Chakka ,  Mikhail Chafeev ,  Sultan Chowdhury ,  Jian-Min Fu ,  Duanjie Hou ,  Rajender Kamboj ,  Vishnumurthy Kodumuru ,  Shifeng Liu ,  Vandna Raina ,  Shaoyi Sun ,  Serguei Sviridov ,  Michael D. Winther ,  Zaihui Zhang ,  Melwyn Abreo ,  Mark W. Holladay ,  Wenbao Li ,  Sengen Sun ,  Chi Tu ,  Heinz W. Gschwend

Inventor： Nagasree Chakka ,  Mikhail Chafeev ,  Sultan Chowdhury ,  Jian-Min Fu ,  Duanjie Hou ,  Rajender Kamboj ,  Vishnumurthy Kodumuru ,  Shifeng Liu ,  Vandna Raina ,  Shaoyi Sun ,  Serguei Sviridov ,  Michael D. Winther ,  Zaihui Zhang ,  Melwyn Abreo ,  Mark W. Holladay ,  Wenbao Li ,  Sengen Sun ,  Chi Tu ,  Heinz W. Gschwend

IPC: A61K31/551 ,  A61K31/5513 ,  A61K31/50 ,  A61K31/502 ,  A61K31/501 ,  C07D245/02 ,  C07D243/04 ,  C07D243/08 ,  C07D403/04 ,  C07D401/14 ,  C07D403/14 ,  A61P7/12

CPC classification number: C07D237/20 ,  A61K31/00 ,  A61K31/501 ,  A61K31/551 ,  C07D237/22 ,  C07D237/24

Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (Ia): where x, y, W, V, R2, R3, R4, R5, R6, R6a, R7, R7a, R8, R8a, R9 and R9a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.

Abstract translation: 公开了治疗哺乳动物，优选人类的SCD介导的疾病或病症的方法，其中所述方法包括向有需要的哺乳动物施用式（Ia）化合物：其中x，y，W，V，R 2 ，R3，R4，R5，R6，R6a，R7，R7a，R8，R8a，R9和R9a如本文所定义。 还公开了包含式（I）化合物的药物组合物。

公开(公告)号：US20100173967A1

公开(公告)日：2010-07-08

申请号：US12445264

申请日：2007-10-12

Applicant: Mikhail Chafeev ,  Sultan Chowdhury ,  Robert Fraser ,  Jianmin Fu ,  Rajender Kamboj ,  Duanjie Hou ,  Shifeng Liu ,  Mehran Seid Bagherzadeh ,  Serguei Sviridov ,  Shaoyi Sun ,  Jianyu Sun ,  Nagasree Chakka ,  Tom Hsieh ,  Vandna Raina

Inventor： Mikhail Chafeev ,  Sultan Chowdhury ,  Robert Fraser ,  Jianmin Fu ,  Rajender Kamboj ,  Duanjie Hou ,  Shifeng Liu ,  Mehran Seid Bagherzadeh ,  Serguei Sviridov ,  Shaoyi Sun ,  Jianyu Sun ,  Nagasree Chakka ,  Tom Hsieh ,  Vandna Raina

IPC: A61K31/404 ,  A61P9/10 ,  A61P17/04 ,  A61P35/00

CPC classification number: A61K31/407 ,  A61K31/437

Abstract: This invention is directed to methods of using spiro-oxindole compounds of formula (I): wherein k, j, Q, R1, R2a, R2b, R2c, R2d, R3a, R3b, R3c, and R3d are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, for the treatment and/or prevention of hypercholesterolemia, benign prostatic hyperplasia, pruritis and cancer.

Abstract translation: 本发明涉及使用式（I）的螺 - 羟吲哚化合物的方法：其中k，j，Q，R1，R2a，R2b，R2c，R2d，R3a，R3b，R3c和R3d如本文所定义， 立体异构体，对映异构体，互变异构体或其混合物; 或其药学上可接受的盐，溶剂合物或前药，用于治疗和/或预防高胆固醇血症，良性前列腺增生，瘙痒症和癌症。

公开(公告)号：US20100160362A1

公开(公告)日：2010-06-24

申请号：US12445270

申请日：2007-10-12

Applicant: Jean-Jacques Cadieux ,  Sultan Chowdhury ,  Jianmin Fu ,  Rajender Kamboj ,  Tom Hsieh ,  Qi Jia ,  Shifeng Liu ,  Jianyu Sun

Inventor： Jean-Jacques Cadieux ,  Sultan Chowdhury ,  Jianmin Fu ,  Rajender Kamboj ,  Tom Hsieh ,  Qi Jia ,  Shifeng Liu ,  Jianyu Sun

IPC: A61K31/438 ,  C07D491/20

CPC classification number: C07D471/22 ,  C07D471/20

Abstract: This invention is directed to methods of using spiro-oxindole compounds of formula (I): wherein j, k, m, Q, X, R1, R2a, R2b, R2c, R2d and R3 are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, N-oxide, solvate or prodrug thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.

Abstract translation: 本发明涉及使用式（I）的螺 - 羟吲哚化合物的方法：其中j，k，m，Q，X，R1，R2a，R2b，R2c，R2d和R3如本文所定义，作为立体异构体， 其互变异构体或其混合物; 或其药学上可接受的盐，N-氧化物，溶剂合物或前药，用于治疗和/或预防钠通道介导的疾病或病症，例如疼痛。

公开(公告)号：US20100152187A1

公开(公告)日：2010-06-17

申请号：US11916243

申请日：2006-06-05

Applicant: Jianmin Fu ,  Duanjie Hou ,  Rajender Kamboj ,  Vishnumurthy Kodumuru ,  Natalia Pokrovskaia ,  Vandna Raina ,  Shaoyi Sun ,  Serguei Sviridov ,  Zaihui Zhang

Inventor： Jianmin Fu ,  Duanjie Hou ,  Rajender Kamboj ,  Vishnumurthy Kodumuru ,  Natalia Pokrovskaia ,  Vandna Raina ,  Shaoyi Sun ,  Serguei Sviridov ,  Zaihui Zhang

IPC: A61K31/5377 ,  C12N9/99 ,  A61K31/4439 ,  A61K31/426 ,  A61P3/10 ,  A61P3/04 ,  A61P9/10

CPC classification number: C07D277/587 ,  A61K31/426 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/5377 ,  A61K31/616 ,  A61K38/26 ,  A61K38/28 ,  A61K45/06 ,  C07D277/56 ,  C07D417/06 ,  C07D417/12

Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I), where V, W, R1, R2, R3 and R4 are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.

Abstract translation: 公开了治疗哺乳动物，优选人类的SCD介导的疾病或病症的方法，其中所述方法包括向有需要的哺乳动物施用式（I）化合物，其中V，W，R 1，R 2，R 3 和R4在本文中定义。 还公开了包含式（I）化合物的药物组合物。

公开(公告)号：US20100048584A1

公开(公告)日：2010-02-25

申请号：US12552868

申请日：2009-09-02

Applicant: Melwyn Abreo ,  Daniel F. Harvey ,  Heinz W. Gschwend ,  Wenbao Li ,  Chi Tu ,  Rajender Kamboj ,  Michael D. Winther ,  Vishnumurthy Kodumuru ,  Cindy J. Hudson ,  Mikhail A. Kondratenko ,  Shifeng Liu ,  Vandna Raina ,  Serguei Sviridov ,  Zaihui Zhang ,  Mehran Seid Bagherzadeh ,  Shaoyi Sun

Inventor： Melwyn Abreo ,  Daniel F. Harvey ,  Heinz W. Gschwend ,  Wenbao Li ,  Chi Tu ,  Rajender Kamboj ,  Michael D. Winther ,  Vishnumurthy Kodumuru ,  Cindy J. Hudson ,  Mikhail A. Kondratenko ,  Shifeng Liu ,  Vandna Raina ,  Serguei Sviridov ,  Zaihui Zhang ,  Mehran Seid Bagherzadeh ,  Shaoyi Sun

IPC: A61K31/496 ,  C12N9/99 ,  A61P3/04 ,  A61P3/00 ,  C07D401/04 ,  C07D401/14

CPC classification number: C07D213/71 ,  A61K31/00 ,  A61K31/501 ,  C07D213/75 ,  C07D213/76

Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): wherein x, y, W, V, R1, R2, R3, R4, R5, R6, R7, R7a, R8, R8a, R9, R9a, R10 and R10a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.

Abstract translation: 公开了在哺乳动物，优选人中治疗SCD介导的疾病或病症的方法，其中所述方法包括向有需要的哺乳动物施用式（I）化合物：其中x，y，W，V，R 1 ，R2，R3，R4，R5，R6，R7，R7a，R8，R8a，R9，R9a，R10和R10a在本文中定义。 还公开了包含式（I）化合物的药物组合物。

公开(公告)号：US20100029718A1

公开(公告)日：2010-02-04

申请号：US12442279

申请日：2007-09-19

Applicant: Natalie Dales ,  Zaihui Zhang ,  Rajender Kamboj ,  Jianmin Fu ,  Shaoyi Sun ,  Natalia Pokrovskaia ,  Serguei Sviridov

Inventor： Natalie Dales ,  Zaihui Zhang ,  Rajender Kamboj ,  Jianmin Fu ,  Shaoyi Sun ,  Natalia Pokrovskaia ,  Serguei Sviridov

IPC: A61K31/427 ,  C07D417/04 ,  C07D417/14 ,  A61K31/454 ,  A61K31/4545 ,  A61P3/00

CPC classification number: C07D417/04 ,  C07D417/14

Abstract: The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.

公开(公告)号：US07605161B2

公开(公告)日：2009-10-20

申请号：US10566193

申请日：2004-07-29

Applicant: Melwyn Abreo ,  Daniel F. Harvey ,  Heinz W. Gschwend ,  Wenbao Li ,  Chi Tu ,  Rajender Kamboj ,  Michael D. Winther ,  Vishnumurthy Kodumuru ,  Cindy J. Hudson ,  Mikhail A. Kondratenko ,  Shifeng Liu ,  Vandna Raina ,  Serguei Sviridov ,  Zaihui Zhang ,  Mehran Seid Bagherzadeh ,  Shaoyi Sun

Inventor： Melwyn Abreo ,  Daniel F. Harvey ,  Heinz W. Gschwend ,  Wenbao Li ,  Chi Tu ,  Rajender Kamboj ,  Michael D. Winther ,  Vishnumurthy Kodumuru ,  Cindy J. Hudson ,  Mikhail A. Kondratenko ,  Shifeng Liu ,  Vandna Raina ,  Serguei Sviridov ,  Zaihui Zhang ,  Mehran Seid Bagherzadeh ,  Shaoyi Sun

IPC: A61K31/497 ,  C07D241/04 ,  C07D295/00

CPC classification number: C07D213/71 ,  A61K31/00 ,  A61K31/501 ,  C07D213/75 ,  C07D213/76

Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): wherein: W is —O—, —N(R1)—, C(O), S(O)t; (where t is 0, 1 or 2), N(R1)S(O)2, S(O)2N(R1), C(O)N(R1) or N(R1)C(O)N(R1); and V is C(O), C(S), C(O)N(R1)—, C(O)O—, S(O)2—, S(O)2N(R1)— or C(R11)H; and x, y, R1, R2, R3, R4, R5, R6, R7, R7a, R8, R8a, R9, R9a, R10 and R10a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.

Abstract translation: 公开了在哺乳动物，优选人中治疗SCD介导的疾病或病症的方法，其中所述方法包括向有需要的哺乳动物施用式（I）化合物：其中：W是-O - ， - N （R 1） - ，C（O），S（O）t; （其中t为0,1或2），N（R1）S（O）2，S（O）2N（R1），C（O）N（R1）或N（R1）C（O） ）; 并且V是C（O），C（S），C（O）N（R 1） - ，C（O）O-，S（O）2 - ，S（O）2 N（R 1） - 或C ）H; 并且x，y，R1，R2，R3，R4，R5，R6，R7，R7a，R8，R8a，R9，R9a，R10和R10a在本文中定义。 还公开了包含式（I）化合物的药物组合物。