公开(公告)号：US20070287713A1

公开(公告)日：2007-12-13

申请号：US11779319

申请日：2007-07-18

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

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

IPC: A61K31/41 ,  A61K31/42 ,  A61K31/44 ,  A61K31/445 ,  A61K31/4965 ,  A61K31/497 ,  A61K31/505 ,  A61P3/10 ,  C07D239/02 ,  C07D257/00 ,  C07D263/30 ,  C07D271/06 ,  C07D401/02 ,  C07D403/02 ,  C07D413/02

CPC classification number: C07D413/12 ,  C07D413/14

Abstract: 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; A is (CH2)x where x is 1 to 5, or A is (CH2)x1, where x1 is 1 to 5 with an alkenyl bond or an alkynyl bond embedded anywhere in the chain, or A is —(CH2)x2—O—(CH2)x3— where x2 is 0 to 5 and x3 is 0 to 5, provided that at least one of x2 and x3 is other than 0; B is a bond or is (CH2)x4 where x4 is 1 to 5; 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. R1 is H or alkyl; R2 is H, alkyl, alkoxy, halogen, amino, substituted amino or cyano; R2a, R2b and R2c may be the same or different and are selected from H, alkyl, alkoxy, halogen, amino, substituted amino or cyano; and R3, E, Z and Y are as defined herein.

公开(公告)号：US07241780B2

公开(公告)日：2007-07-10

申请号：US10964395

申请日：2004-10-13

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 ,  C07D213/02

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：US20050119311A1

公开(公告)日：2005-06-02

申请号：US10964395

申请日：2004-10-13

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

Inventor： Peter 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 ,  C07D417/14 ,  A61K31/4439 ,  A61K31/444

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：US20050004184A1

公开(公告)日：2005-01-06

申请号：US10826100

申请日：2004-04-15

Applicant: Denis Ryono ,  Jon Hangeland ,  Todd Friends ,  Tamara Dejneka ,  Pratik Devasthale ,  Yolanda Caringal ,  Minsheng Zhang ,  Arthur Doweyko ,  Johan Malm ,  Andrei Sanin

Inventor： Denis Ryono ,  Jon Hangeland ,  Todd Friends ,  Tamara Dejneka ,  Pratik Devasthale ,  Yolanda Caringal ,  Minsheng Zhang ,  Arthur Doweyko ,  Johan Malm ,  Andrei Sanin

IPC: A61K20060101 ,  A61K31/16 ,  A61K31/165 ,  A61K31/19 ,  A61K31/277 ,  A61K31/421 ,  A61K31/44 ,  A61K47/00 ,  C07C205/00 ,  C07C235/20 ,  C07C255/49 ,  C07C381/00

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.

Abstract translation: 提供具有通式I的甲状腺受体配体，其中：R 1是R 2和R 3相同或不同，是氢，卤素，1至4个碳的烷基或3至5个碳原子的环烷基，条件是R2中的至少一个 并且R 3不是氢; R 4是R 5和R 6相同或不同，并且选自氢，芳基，杂芳基，烷基，环烷基，芳烷基或杂芳烷基。 R7是芳基，杂芳基，烷基，芳烷基或杂芳烷基; R8是芳基，杂芳基或环烷基; R9为R7或氢; R 10是氢，卤素，氰基或烷基; R 11和R 12各自独立地选自氢，卤素，烷氧基，羟基（-OH）氰基和烷基; R13是羧酸（COOH）或其酯，膦酸和次膦酸或其酯，磺酸，四唑，异羟肟酸，噻唑烷二酮，酰基磺酰胺或本领域已知的其它羧酸替代物; R 14和R 15可以相同或不同，并且选自氢和烷基，或者R 14和R 15可以连接在一起形成2至5个亚甲基 - [ - （CH 2）m - ，m = 2,3,4或 5]，从而形成3-至6-元环烷基环; R16是氢或1至4个碳的烷基; R 17和R 18相同或不同，选自氢，卤素和烷基; n为0或1至4的整数; X是氧（-O-），硫（-S-），磺酰基（-SO 2 - ），亚磺酰基（-SO-）硒（-Se-），羰基（-CO-），氨基（-NH-）或 亚甲基（-CH 2 - ） 其中取代基如本文所述。 此外，提供了一种用于预防，抑制或治疗与代谢功能障碍相关或依赖于T3调节基因的表达的疾病或病症的方法，其中如上所述的化合物以治疗有效量施用。

公开(公告)号：US06727271B2

公开(公告)日：2004-04-27

申请号：US10081075

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: A61K3142

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: 提供具有结构的化合物，其中Q是C或N，A是O或S，Z是O或键，X是CH或N和R 1，R 2，R 2a，R 2b R 2，R 3，R 3，Y，x，m和n如本文所定义，该化合物可用作抗糖尿病，降血脂药和抗肥胖剂。

公开(公告)号：US06653314B2

公开(公告)日：2003-11-25

申请号：US10080981

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: A61K31505

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: 提供具有结构的化合物，其中Q是C或N，A是O或S，Z是O或键，X是CH或N和R 1，R 2，R 2a，R 2b >，R 2c，R 3，Y，x，m和n如本文所定义，该化合物可用作抗糖尿病，降血脂药和抗肥胖剂。