公开(公告)号：US08580959B2

公开(公告)日：2013-11-12

申请号：US13122617

申请日：2009-10-08

Applicant: Pratik Devasthale ,  William N. Washburn ,  Kishore V. Renduchintala ,  Radhakrishnan Sridhar

Inventor： Pratik Devasthale ,  William N. Washburn ,  Kishore V. Renduchintala ,  Radhakrishnan Sridhar

IPC: C07D487/04 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  A61K31/53 ,  A61K31/4427 ,  A61K31/4523 ,  A61K31/401 ,  A61P3/04 ,  A61P3/10

CPC classification number: C07D487/04 ,  A61K31/53 ,  A61K31/541

Abstract: The present application provides compounds that are useful as MCHR1 antagonists, especially for the treatment of obesity, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein the variables are defined herein.

Abstract translation: 本申请提供了可用作MCHR1拮抗剂的化合物，特别是用于治疗肥胖症，包括根据式I的所有立体异构体，溶剂合物，前药和药学上可接受的形式，其中变量在本文中定义。

公开(公告)号：US20060264457A1

公开(公告)日：2006-11-23

申请号：US11430657

申请日：2006-05-09

Applicant: Pratik Devasthale ,  Wei Wang ,  Lawrence Hamann ,  Stephen O'Connor ,  John Fevig

Inventor： Pratik Devasthale ,  Wei Wang ,  Lawrence Hamann ,  Stephen O'Connor ,  John Fevig

IPC: C07D471/02 ,  C07D487/02

CPC classification number: C07D471/04

Abstract: Compounds are provided having the formula (I) wherein R, X, Y, Z, A and n are as defined herein, which are inhibitors of dipeptidyl peptidase IV and thus are useful in treating diabetes and related diseases.

公开(公告)号：US20100298276A1

公开(公告)日：2010-11-25

申请号：US12469791

申请日：2009-05-21

Applicant: Denis E. Ryono ,  Jon J. Hangeland ,  Todd J. Friends ,  Tamara Dejneka ,  Pratik Devasthale ,  Yolanda V. Caringal ,  Minsheng Zhang ,  Arthur M.P. Doweyko ,  Johan Malm ,  Andrei Sanin

Inventor： Denis E. Ryono ,  Jon J. Hangeland ,  Todd J. Friends ,  Tamara Dejneka ,  Pratik Devasthale ,  Yolanda V. Caringal ,  Minsheng Zhang ,  Arthur M.P. Doweyko ,  Johan Malm ,  Andrei Sanin

IPC: A61K31/662 ,  C07F9/02 ,  A61P3/10

CPC classification number: C07C311/46 ,  A61K31/4439 ,  A61K31/662 ,  A61K45/06 ,  C07C43/29 ,  C07C43/295 ,  C07C59/68 ,  C07C59/72 ,  C07C65/24 ,  C07C65/26 ,  C07C69/16 ,  C07C69/736 ,  C07C69/94 ,  C07C205/38 ,  C07C217/58 ,  C07C233/29 ,  C07C235/34 ,  C07C235/42 ,  C07C235/46 ,  C07C235/52 ,  C07C235/60 ,  C07C235/62 ,  C07C235/64 ,  C07C311/37 ,  C07C2601/02 ,  C07C2601/14 ,  C07C2602/08 ,  C07C2603/18 ,  C07D213/30 ,  C07D239/26 ,  C07D257/04 ,  C07D263/14 ,  C07D263/32 ,  C07D277/24 ,  C07D285/06 ,  C07D307/42 ,  C07D307/52 ,  C07D307/87 ,  C07D317/58 ,  C07D317/60 ,  C07D333/32 ,  C07F9/306 ,  C07F9/3241 ,  C07F9/4056 ,  A61K2300/00

Abstract: Thyroid receptor ligands are provided which have the general formula I wherein: R1 is R2 and R3 are the same or different and are hydrogen, halogen, alkyl of 1 to 4 carbons or cycloalkyl of 3 to 5 carbons, provided that at least one of R2 and R3 is other than hydrogen; R4 is R5 and R6 are the same or different and are selected from hydrogen, aryl, heteroaryl, alkyl, cycloalkyl, aralkyl or heteroaralkyl. R7 is aryl, heteroaryl, alkyl, aralkyl, or heteroaralkyl; R8 is aryl, heteroaryl, or cycloalkyl; R9 is R7 or hydrogen; R10 is hydrogen, halogen, cyano or alkyl; R11 and R12 are each independently selected from the group consisting of hydrogen, halogen, alkoxy, hydroxy (—OH) cyano, and alkyl; R13 is carboxylic acid (COOH) or esters thereof, phosphonic and phosphinic acid or esters thereof, sulfonic acid, tetrazole, hydroxamic acid, thiazolidinedione, acylsulfonamide, or other carboxylic acid surrogates known in the art; R14 and R15 may be the same or different and are selected from hydrogen and alkyl, or R14 and R15 may be joined together forming a chain of 2 to 5 methylene groups [—(CH2)m-, m=2, 3, 4 or 5], thus forming 3- to 6-membered cycloalkyl rings; R16 is hydrogen or alkyl of 1 to 4 carbons; R17 and R18 are the same or different and selected from hydrogen, halogen and alkyl; n is 0 or an integer from 1 to 4; X is oxygen (—O—), sulfur (—S—), sulfonyl (—SO2—), sulfenyl (—SO—) selenium (—Se—), carbonyl (—CO—), amino (—NH—) or methylene (—CH2-); wherein the substituents are as described herein. In addition, a method is provided for preventing, inhibiting or treating diseases or disorders associated with metabolism dysfunction or which are dependent upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount.

公开(公告)号：US20090298794A1

公开(公告)日：2009-12-03

申请号：US12473346

申请日：2009-05-28

Applicant: William N. Washburn ,  Saleem Ahmad ,  Pratik Devasthale ,  Jeffrey A. Robl ,  Animesh Goswami ,  Zhiwei Guo ,  Ramesh N. Patel

Inventor： William N. Washburn ,  Saleem Ahmad ,  Pratik Devasthale ,  Jeffrey A. Robl ,  Animesh Goswami ,  Zhiwei Guo ,  Ramesh N. Patel

IPC: A61K31/519 ,  C07D495/04 ,  C07F9/6512 ,  A61K31/675 ,  C12P17/16 ,  A61P3/00 ,  A61P25/00 ,  A61P29/00

CPC classification number: C07D495/04

Abstract: The present invention provides compounds having the following Formula IA and IB, which are useful as MCHR1 antagonists, and includes prodrugs and pharmaceutically acceptable salts thereof:

Abstract translation: 本发明提供具有以下式IA和IB的化合物，其可用作MCHR1拮抗剂，并且包括其前药和药学上可接受的盐：

公开(公告)号：US07084162B2

公开(公告)日：2006-08-01

申请号：US10655876

申请日：2003-09-05

Applicant: Peter T. Cheng ,  Pratik Devasthale ,  Yoon Jeon ,  Sean Chen ,  Hao Zhang

Inventor： Peter T. Cheng ,  Pratik Devasthale ,  Yoon Jeon ,  Sean Chen ,  Hao Zhang

IPC: A61K31/421 ,  C07D263/32

CPC classification number: C07D263/58 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D263/32 ,  C07D277/24 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D495/04

Abstract: Compounds are provided which have the structure wherein Q is C or N, A is O or S, Z is O or a bond, X is CH or N and R1, R2, R2a, R2b, R2c, R3, Y, x, m, and n are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.

Abstract translation: 提供具有其中Q为C或N，A为O或S，Z为O或键，X为CH或N，R 1，R 2， R 2，R 2b，R 2b，R 2c，R 3，Y，x，m和 n如本文所定义，这些化合物可用作抗糖尿病，降血脂症和抗肥胖剂。

公开(公告)号：US06919358B2

公开(公告)日：2005-07-19

申请号：US10080965

申请日：2002-02-22

Applicant: Peter T. Cheng ,  Pratik Devasthale ,  Yoon Jeon ,  Sean Chen ,  Hao Zhang

Inventor： Peter T. Cheng ,  Pratik Devasthale ,  Yoon Jeon ,  Sean Chen ,  Hao Zhang

IPC: C07D263/32 ,  C07D263/58 ,  C07D277/24 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D495/04 ,  C07D521/00 ,  A61K31/443

CPC classification number: C07D263/58 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D263/32 ,  C07D277/24 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D495/04

Abstract: Compounds are provided which have the structure wherein Q is C or N, A is O or S, Z is O or a bond, X is CH or N and R1, R2, R2a, R2b, R2c, R3, Y, x, m, and n are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.

公开(公告)号：US20110195934A1

公开(公告)日：2011-08-11

申请号：US13122995

申请日：2009-10-08

Applicant: Pratik Devasthale ,  Wliiam N. Washburn ,  Wei Wang ,  Andres Hernandez ,  Saleem Ahmad ,  Guohua Zhao

Inventor： Pratik Devasthale ,  Wliiam N. Washburn ,  Wei Wang ,  Andres Hernandez ,  Saleem Ahmad ,  Guohua Zhao

IPC: A61K31/4162 ,  C07D487/04 ,  A61K31/4439 ,  A61K31/444 ,  C07F9/6503 ,  A61K31/675 ,  A61K31/506 ,  A61K31/4545 ,  A61K31/4192 ,  A61P3/04 ,  A61P3/10

CPC classification number: C07D487/04

Abstract: The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable faints thereof according to wherein all of the variables are defined herein.

Abstract translation: 本申请提供了化合物，包括所有的立体异构体，溶剂合物，前药和药学上可接受的害怕，根据其中所有变量都在本文中定义。

公开(公告)号：US07951793B2

公开(公告)日：2011-05-31

申请号：US11779319

申请日：2007-07-18

Applicant: Peter T. W. Cheng ,  Sean Chen ,  Pratik Devasthale ,  Charles Z. Ding ,  Timothy F. Herpin ,  Shung Wu ,  Hao Zhang ,  Wei Wang ,  Xiang-Yang Ye

Inventor： Peter T. W. Cheng ,  Sean Chen ,  Pratik Devasthale ,  Charles Z. Ding ,  Timothy F. Herpin ,  Shung Wu ,  Hao Zhang ,  Wei Wang ,  Xiang-Yang Ye

IPC: A61K31/397 ,  C07D205/08 ,  A01N43/00

CPC classification number: C07D413/12 ,  C07D413/14

Abstract: Compounds are provided which have the structure wherein Z1 is (CH2)q or C═O; Z2 is (CH2)p or C═O; D is —CH═ or C═O or (CH2)m where m is 0, 1, 2 or 3; n=0, 1 or 2; p=1 or 2; q=0, 1 or 2; Q is C or N; X is CH or N; X2 is C, N, O or S; X3 is C, N, O or S; X4 is C, N, O or S; X5 is C, N, O or S; X6 is C, N, O or S; provided that at least one of X2, X3, X4 X5 and X6 is N; and at least one of X2, X3, X4 X5 and X6 is C; and A, B, R1, R2, R2a, R4, R3, E, Z and Y are as defined herein, which compounds are useful in treating diabetes and related diseases.

Abstract translation: 提供具有其中Z 1是（CH 2）q或C = O的结构的化合物; Z2是（CH2）p或C = O; D是-CH =或C = O或（CH 2）m，其中m为0,1,2或3; n = 0,1或2; p = 1或2; q = 0,1或2; Q是C或N; X是CH或N; X2是C，N，O或S; X3为C，N，O或S; X4为C，N，O或S; X5为C，N，O或S; X6为C，N，O或S; 条件是X 2，X 3，X 4 X 5和X 6中的至少一个为N; X2，X3，X4，X5和X6中的至少一个为C; 并且A，B，R1，R2，R2a，R4，R3，E，Z和Y如本文所定义，该化合物可用于治疗糖尿病和相关疾病。

公开(公告)号：US07521557B2

公开(公告)日：2009-04-21

申请号：US11430657

申请日：2006-05-09

Applicant: Pratik Devasthale ,  Wei Wang ,  Lawrence G. Hamann ,  John M. Fevig

Inventor： Pratik Devasthale ,  Wei Wang ,  Lawrence G. Hamann ,  John M. Fevig

IPC: C07D471/02 ,  A01N43/42

CPC classification number: C07D471/04

Abstract: Compounds are provided having the formula (I) wherein R, X, Y, Z, A and n are as defined herein, which are inhibitors of dipeptidyl peptidase IV and thus are useful in treating diabetes and related diseases.

Abstract translation: 提供具有式（I）的化合物，其中R，X，Y，Z，A和n如本文所定义，其是二肽基肽酶IV的抑制剂，因此可用于治疗糖尿病和相关疾病。

公开(公告)号：US07053106B2

公开(公告)日：2006-05-30

申请号：US10737210

申请日：2003-12-16

Applicant: Peter T. Cheng ,  Pratik Devasthale ,  Yoon Jeon ,  Sean Chen ,  Hao Zhang

Inventor： Peter T. Cheng ,  Pratik Devasthale ,  Yoon Jeon ,  Sean Chen ,  Hao Zhang

IPC: A61K31/44 ,  A61K31/425 ,  A61K31/42

CPC classification number: C07D263/58 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D263/32 ,  C07D277/24 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D495/04

Abstract: Compounds are provided which have the structure wherein Q is C or N, A is O or S, Z is O or a bond, X is CH or N and R1, R2, R2a, R2b, R3, Y, x, m, and n are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.

Abstract translation: 提供具有其中Q为C或N，A为O或S，Z为O或键，X为CH或N，R 1，R 2， R 2，R 2b，R 2b，R 3，Y，x，m和n如本文所定义，该化合物是有用的 作为抗糖尿病，降血脂药和抗肥胖剂。