公开(公告)号：US20120238587A1

公开(公告)日：2012-09-20

申请号：US13423950

申请日：2012-03-19

Applicant: Gilnam Lee ,  Chul Soo Lim ,  Han Won Cho ,  Jeongbeob Seo ,  Albert Charles Gyorkos ,  Suk Young Cho ,  Eun Kyung Choi ,  Choung Soo Kim ,  Jung Jin Hwang

Inventor： Gilnam Lee ,  Chul Soo Lim ,  Han Won Cho ,  Jeongbeob Seo ,  Albert Charles Gyorkos ,  Suk Young Cho ,  Eun Kyung Choi ,  Choung Soo Kim ,  Jung Jin Hwang

IPC: A61K31/519 ,  A61P29/00 ,  A61P37/06 ,  A61P9/00 ,  A61P37/08 ,  A61P11/06 ,  C07D471/04 ,  A61P35/00

CPC classification number: C07D471/04 ,  A61K31/519

Abstract: The invention provides novel substituted pyridopyrimidines represented by Formula I or a pharmaceutically acceptable salt, solvate, polymorph, ester, tautomer or prodrug thereof, and a composition comprising these compounds. The compounds provided can be used as inhibitors of the phosphoinositide 3′ OH kinase family (PI3K) for the treatment of inflammatory diseases, cancer, cardiovascular diseases, allergy, asthma and autoimmune disorders.

Abstract translation: 本发明提供由式I表示的新型取代吡啶并嘧啶以及其药学上可接受的盐，溶剂合物，多晶型物，酯，互变异构体或前药，以及包含这些化合物的组合物。 所提供的化合物可用作磷酸肌醇3'OH激酶家族（PI3K）的抑制剂，用于治疗炎性疾病，癌症，心血管疾病，变态反应，哮喘和自身免疫性疾病。

公开(公告)号：US08664230B2

公开(公告)日：2014-03-04

申请号：US13423950

申请日：2012-03-19

Applicant: Gilnam Lee ,  Chul Soo Lim ,  Han Won Cho ,  Jeongbeob Seo ,  Albert Charles Gyorkos ,  Suk Young Cho ,  Eun Kyung Choi ,  Choung Soo Kim ,  Jung Jin Hwang

Inventor： Gilnam Lee ,  Chul Soo Lim ,  Han Won Cho ,  Jeongbeob Seo ,  Albert Charles Gyorkos ,  Suk Young Cho ,  Eun Kyung Choi ,  Choung Soo Kim ,  Jung Jin Hwang

IPC: A61K31/519 ,  C07D471/02

CPC classification number: C07D471/04 ,  A61K31/519

Abstract: The invention provides novel substituted pyridopyrimidines represented by Formula I or a pharmaceutically acceptable salt, solvate, polymorph, ester, tautomer or prodrug thereof, and a composition comprising these compounds. The compounds provided can be used as inhibitors of the phosphoinositide 3′ OH kinase family (PI3K) for the treatment of inflammatory diseases, cancer, cardiovascular diseases, allergy, asthma and autoimmune disorders.

Abstract translation: 本发明提供由式I表示的新型取代吡啶并嘧啶以及其药学上可接受的盐，溶剂合物，多晶型物，酯，互变异构体或前药，以及包含这些化合物的组合物。 所提供的化合物可用作磷酸肌醇3'OH激酶家族（PI3K）的抑制剂，用于治疗炎性疾病，癌症，心血管疾病，变态反应，哮喘和自身免疫性疾病。

公开(公告)号：US20100056515A1

公开(公告)日：2010-03-04

申请号：US12312087

申请日：2007-10-24

Applicant: Kazuyoshi Aso ,  Michiyo Mochizuki ,  Takuto Kojima ,  Katsumi Kobayashi ,  Scott Alan Pratt ,  Albert Charles Gyorkos ,  Christopher Peter Corrette ,  Suk Young Cho

Inventor： Kazuyoshi Aso ,  Michiyo Mochizuki ,  Takuto Kojima ,  Katsumi Kobayashi ,  Scott Alan Pratt ,  Albert Charles Gyorkos ,  Christopher Peter Corrette ,  Suk Young Cho

IPC: A61K31/5377 ,  A61K31/4412 ,  A61K31/4166 ,  C07D413/10 ,  C07D401/12 ,  C07D235/26 ,  A61P25/24 ,  A61P25/22

CPC classification number: C07D235/26 ,  C07D235/30 ,  C07D401/12 ,  C07D403/12

Abstract: There is provided a compound of the formula (I): wherein R1 is an optionally substituted C1-10 alkyl; R2 is H, or a C1-6 alkyl which may be substituted with 1 to 3 substituents; R3 is a 5- or 6-membered aromatic group which may be substituted with 1 to 5 substituents, wherein the 5- or 6-membered aromatic group may be fused with a 5- or 6-membered ring which may be substituted with 1 to 3 C1-6 alkyls; R4 is a hydrogen, a halogen, a hydroxy, a cyano, a C1-6 alkyl or a C1-6 alkoxy; Z is —O—, —S—, —SO—, —SO2—, or —NR5— wherein R5 is a hydrogen or a C1-6 alkyl; or a salt thereof or a prodrug thereof, which have CRF receptor antagonist activity and use thereof.

Abstract translation: 提供式（I）的化合物：其中R 1是任选取代的C 1-10烷基; R2是H或可被1至3个取代基取代的C 1-6烷基; R3是可被1至5个取代基取代的5或6元芳族基团，其中5或6元芳族基团可以与可被1至5个取代基取代的5或6元环稠合 3 C 1-6烷基; R4是氢，卤素，羟基，氰基，C1-6烷基或C1-6烷氧基; Z是-O - ， - S - ， - SO - ， - SO 2 - 或-NR 5 - ，其中R 5是氢或C 1-6烷基; 或其盐或其前药，其具有CRF受体拮抗剂活性及其用途。

公开(公告)号：US08163935B2

公开(公告)日：2012-04-24

申请号：US11919435

申请日：2006-04-26

Applicant: Kazuyoshi Aso ,  Michiyo Mochizuki ,  Albert Charles Gyorkos ,  Christopher Peter Corrette ,  Suk Young Cho ,  Scott Alan Pratt ,  Christopher Stephen Siedem

Inventor： Kazuyoshi Aso ,  Michiyo Mochizuki ,  Albert Charles Gyorkos ,  Christopher Peter Corrette ,  Suk Young Cho ,  Scott Alan Pratt ,  Christopher Stephen Siedem

IPC: C07D403/02 ,  C07D235/24 ,  C07D235/26 ,  C07D235/30 ,  A61K31/415

CPC classification number: C07D403/04 ,  C07D235/26 ,  C07D235/30 ,  C07D335/02 ,  C07D401/04 ,  C07D401/12 ,  C07D405/04 ,  C07D409/04 ,  C07D409/10 ,  C07D409/12 ,  C07D413/04 ,  C07D417/10 ,  C07D471/04 ,  C07D471/06 ,  C07D495/04

Abstract: There is provided a CRF receptor antagonist comprising a compound of the formula (I): wherein R1 is an optionally substituted hydrocarbyl, an optionally substituted C-linked heterocyclic group, an optionally substituted N-linked heteroaryl group, a cyano or an acyl; R2 is an optionally substituted cyclic hydrocarbyl or an optionally substituted heterocyclic group; X is oxygen, sulfur or —NR3— (wherein R3 is a hydrogen, an optionally substituted hydrocarbyl or an acyl); Y1, Y2 and Y3 are each an optionally substituted carbon or a nitrogen, provided that one or less of Y1, Y2 and Y3 is nitrogen; and Z is a bond, —CO—, oxygen, sulfur, —SO—, —SO2—, —NR4—, —NR4-alk-, —CONR4— or —NR4CO— (wherein alk is an optionally substituted C1-4 alkylene and R4 is a hydrogen, an optionally substituted hydrocarbyl or an acyl); or a salt thereof or a prodrug thereof.

Abstract translation: 提供了包含式（I）化合物的CRF受体拮抗剂：其中R1是任选取代的烃基，任选取代的C连接的杂环基，任选取代的N-连接的杂芳基，氰基或酰基; R2是任选取代的环状烃基或任选取代的杂环基; X是氧，硫或-NR 3 - （其中R 3是氢，任选取代的烃基或酰基）; Y1，Y2和Y3各自为任选取代的碳或氮，条件是Y 1，Y 2和Y 3中的一个或多个为氮; 并且Z是键，-CO-，氧，硫，-SO - ， - SO 2 - ， - NR 4 - ， - NR 4 - 烷 - ， - CONR 4 - 或-NR 4 CO-（其中，alk是任选取代的C 1-4亚烷基 和R4是氢，任选取代的烃基或酰基）; 或其盐或其前药。

公开(公告)号：US20120053180A1

公开(公告)日：2012-03-01

申请号：US13050801

申请日：2011-03-17

Applicant: Sang Uk Kang ,  Min Jeong Kim ,  Byung Nam Kang ,  Wei Tan ,  Albert Charles Gyorkos ,  Suk Young Cho

Inventor： Sang Uk Kang ,  Min Jeong Kim ,  Byung Nam Kang ,  Wei Tan ,  Albert Charles Gyorkos ,  Suk Young Cho

IPC: A61K31/501 ,  A61K31/496 ,  C07D239/34 ,  A61K31/505 ,  C07D241/04 ,  A61K31/495 ,  C07D403/04 ,  C07D211/96 ,  A61K31/445 ,  C07D213/68 ,  A61K31/4412 ,  C07C69/22 ,  A61K31/222 ,  C07C317/22 ,  A61K31/085 ,  C07C43/235 ,  A61P3/00 ,  A61P3/10 ,  A61P9/00 ,  C07D403/12

CPC classification number: C07D403/12 ,  C07C43/247 ,  C07C317/22 ,  C07C317/44 ,  C07C2601/14 ,  C07D211/96 ,  C07D237/22 ,  C07D239/34 ,  C07D295/096 ,  C07D417/12 ,  C07D417/14 ,  C07D451/06 ,  C07D451/10 ,  C07D471/04

Abstract: This invention relates to a series of substituted cyclohexane containing analogues which are agonists of GPR119 intended to treat metabolic diseases mediated by GPR119 including Type I & II diabetes mellitus. Diabetes mellitus is an ever-increasing threat to human health causing various complications (blindness, kidney failure, neuropathy, heart attack, stroke, etc.). Recently it was found that activation of GPR119 which is highly expressed in pancreatic beta cells causes glucose dependent insulin secretion and GLP-1 release. Many pharmaceuticals are currently developing GPR119 agonists and herein we disclose alternative GPR119 agonists. Our invention describes GPR119 agonists having structural Formula (I), pharmaceutically acceptable salt or solvate of Formula (I), isomer or prodrug of Formula (I), and combination therapy of Formula (I) with other anti-diabetic drugs like DPP-IV inhibitors and/or insulin sensitizers.

Abstract translation: 本发明涉及一系列取代的含环己烷的类似物，其是旨在治疗包括I型和II型糖尿病的GPR119介导的代谢疾病的GPR119的激动剂。 糖尿病是导致各种并发症（失明，肾衰竭，神经病，心脏病发作，中风等）的人类健康日益严重的威胁。 最近发现，在胰腺β细胞中高度表达的GPR119的激活导致葡萄糖依赖性胰岛素分泌和GLP-1释放。 许多药物目前正在开发GPR119激动剂，在此我们公开了另外的GPR119激动剂。 我们的发明描述了具有结构式（I），式（I）的药学上可接受的盐或溶剂化物，式（I）的异构体或前药，以及式（I）与其它抗糖尿病药物如DPP-IV的组合治疗的GPR119激动剂 抑制剂和/或胰岛素敏化剂。

公开(公告)号：US07714009B2

公开(公告)日：2010-05-11

申请号：US10577334

申请日：2004-10-27

Applicant: Albert Charles Gyorkos ,  Christopher Peter Corrette ,  Suk Young Cho ,  Timothy Mark Turner ,  Scott Alan Pratt ,  Kazuyoshi Aso ,  Masakuni Kori ,  Michiyo Gyoten

Inventor： Albert Charles Gyorkos ,  Christopher Peter Corrette ,  Suk Young Cho ,  Timothy Mark Turner ,  Scott Alan Pratt ,  Kazuyoshi Aso ,  Masakuni Kori ,  Michiyo Gyoten

IPC: A61K31/4168 ,  C07D403/12 ,  C07D403/14 ,  C07D235/30

CPC classification number: C07D235/30 ,  C07D471/04

Abstract: There is provided a CRF receptor antagonist comprising a compound of the formula (I): wherein, ring A is a 5-membered ring represented by the formula (A′): wherein X is a carbon and X1 is an oxygen, a sulfur or —NR5—, or formula (A″): wherein X is a nitrogen and R6 is an optionally substituted hydrocarbyl, R1 is an amino substituted by two optionally substituted hydrocarbyl groups, R2 is an phenyl, Y1 is CR3a or a nitrogen, Y2 is CR3b or a nitrogen and Y3 is CR3c or a nitrogen, provided that one or less of Y1, Y2, and Y3 is nitrogen, W is a bond, —(CH2)n-, and Z is a bond, —NR4—, etc.; or a salt thereof or a prodrug thereof.

Abstract translation: 提供了包含式（I）化合物的CRF受体拮抗剂：其中环A是由式（A'）表示的5元环：其中X是碳，X 1是氧，硫或 -NR5-或式（A“）：其中X是氮，R6是任选取代的烃基，R 1是被两个任选取代的烃基取代的氨基，R 2是苯基，Y 1是CR 3 a或氮，Y 2是 CR3b或氮，Y3为CR3c或氮，条件是Y1，Y2和Y3中的一个或多个为氮，W为键， - （CH2）n-，Z为键，-NR4-等 。 或其盐或其前药。

公开(公告)号：US20120238599A1

公开(公告)日：2012-09-20

申请号：US13423898

申请日：2012-03-19

Applicant: Gilnam Lee ,  Han Won Cho ,  Eun Jin Song ,  Hye Sun Jeon ,  Min Jeong Kim ,  Jeongbeob Seo ,  Albert Charles Gyorkos ,  Suk Young Cho

Inventor： Gilnam Lee ,  Han Won Cho ,  Eun Jin Song ,  Hye Sun Jeon ,  Min Jeong Kim ,  Jeongbeob Seo ,  Albert Charles Gyorkos ,  Suk Young Cho

IPC: A61K31/4365 ,  A61K31/4355 ,  C07D213/82 ,  A61K31/4412 ,  A61P35/00 ,  C07D498/04 ,  A61K31/437 ,  C07D513/04 ,  C12N9/99 ,  A61P29/00 ,  C07D491/048 ,  C07D495/04

CPC classification number: C07D213/82 ,  C07D491/048 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04 ,  C12N9/12 ,  C12Y207/12002

Abstract: The invention provides novel substituted heterocyclic compounds represented by Formula I and Formula II, or a pharmaceutically acceptable salt, solvate, polymorph, ester, tautomer or prodrug thereof, and a composition comprising these compounds. The compounds provided can be used as inhibitors of MEK and are useful in the treatment of inflammatory diseases, cancer and other hyperproliferative diseases. The invention further provides a method of treatment for inflammatory diseases, cancer and other hyperproliferative diseases in mammals, especially humans.

Abstract translation: 本发明提供由式I和式II表示的新型取代的杂环化合物或其药学上可接受的盐，溶剂合物，多晶型物，酯，互变异构体或前药，以及包含这些化合物的组合物。 所提供的化合物可用作MEK的抑制剂，并且可用于治疗炎性疾病，癌症和其它过度增生性疾病。 本发明还提供了一种治疗哺乳动物，特别是人类的炎性疾病，癌症和其它过度增生性疾病的方法。

公开(公告)号：US07897607B2

公开(公告)日：2011-03-01

申请号：US10593891

申请日：2005-04-06

Applicant: Albert Charles Gyorkos ,  Christopher Peter Corrette ,  Suk Young Cho ,  Timothy Mark Turner ,  Kazuyoshi Aso ,  Masakuni Kori ,  Michiyo Mochizuki ,  Kevin Ronald Condroski ,  Christopher Stephen Siedem ,  Steven Armen Boyd

Inventor： Albert Charles Gyorkos ,  Christopher Peter Corrette ,  Suk Young Cho ,  Timothy Mark Turner ,  Kazuyoshi Aso ,  Masakuni Kori ,  Michiyo Mochizuki ,  Kevin Ronald Condroski ,  Christopher Stephen Siedem ,  Steven Armen Boyd

IPC: C07D487/04 ,  A61K31/519

CPC classification number: C07D213/74 ,  C07C225/20 ,  C07C2602/08 ,  C07D215/233 ,  C07D215/56 ,  C07D231/56 ,  C07D237/28 ,  C07D239/46 ,  C07D239/47 ,  C07D239/56 ,  C07D239/94 ,  C07D239/95 ,  C07D239/96 ,  C07D265/36 ,  C07D455/02 ,  C07D471/04 ,  C07D487/04

Abstract: There is provided a CRF receptor antagonist comprising a compound of the formula (I): A-W—Ar  (I) wherein, A is a group represented by the formula (A1) or (A2): (wherein, ring Aa is a 5- or 6-membered ring which may be further substituted; ring Ab is a 5- or 6-membered ring which may be further substituted; ring Ac is a 5- or 6-membered ring which may be substituted; R1 is optionally substituted alkyl, substituted amino, substituted hydroxy, etc.; X is carbonyl, —O—, —S—, etc.; Y1, Y2 and Q are independently optionally substituted carbon or nitrogen;  is a single or double bond); W is a bond, optionally substituted methylene, optionally substituted imino, —O—, —S—, etc.; Ar is optionally substituted aryl or optionally substituted heteroaryl; or a salt thereof or a prodrug thereof.

Abstract translation: 提供了包含式（I）的化合物的CRF受体拮抗剂：AW-Ar（I）其中A是由式（A1）或（A2）表示的基团：（其中环Aa是5- 或6元环，其可以被进一步取代;环Ab是可进一步取代的5-或6-元环;环Ac是可被取代的5-或6-元环; R 1是任选取代的烷基， 取代的氨基，取代的羟基等; X是羰基，-O-，-S-等; Y1，Y2和Q独立地是任选取代的碳或氮;是单键或双键）; W是一个键，任意取代的亚甲基，任选取代的亚氨基，-O - ， - S-等; Ar是任选取代的芳基或任选取代的杂芳基; 或其盐或其前药。

公开(公告)号：US20090312383A1

公开(公告)日：2009-12-17

申请号：US11919435

申请日：2006-04-26

Applicant: Kazuyoshi Aso ,  Michiyo Mochizuki ,  Albert Charles Gyorkos ,  Christopher Peter Corrette ,  Suk Young Cho ,  Scott Alan Pratt ,  Christopher Stephen Siedem

Inventor： Kazuyoshi Aso ,  Michiyo Mochizuki ,  Albert Charles Gyorkos ,  Christopher Peter Corrette ,  Suk Young Cho ,  Scott Alan Pratt ,  Christopher Stephen Siedem

IPC: A61K31/4184 ,  C07D235/14 ,  C07D403/06 ,  A61P25/00 ,  A61P25/24 ,  A61P25/22

CPC classification number: C07D403/04 ,  C07D235/26 ,  C07D235/30 ,  C07D335/02 ,  C07D401/04 ,  C07D401/12 ,  C07D405/04 ,  C07D409/04 ,  C07D409/10 ,  C07D409/12 ,  C07D413/04 ,  C07D417/10 ,  C07D471/04 ,  C07D471/06 ,  C07D495/04

Abstract: There is provided a CRF receptor antagonist comprising a compound of the formula (I): wherein R1 is an optionally substituted hydrocarbyl, an optionally substituted C-linked heterocyclic group, an optionally substituted N-linked heteroaryl group, a cyano or an acyl; R2 is an optionally substituted cyclic hydrocarbyl or an optionally substituted heterocyclic group; X is oxygen, sulfur or —NR3— (wherein R3 is a hydrogen, an optionally substituted hydrocarbyl or an acyl); Y1, Y2 and Y3 are each an optionally substituted carbon or a nitrogen, provided that one or less of Y1, Y2 and Y3 is nitrogen; and Z is a bond, —CO—, oxygen, sulfur, —SO—, —SO2—, —NR4—, —NR4-alk-, —CONR4— or —NR4CO— (wherein alk is an optionally substituted C1-4 alkylene and R4 is a hydrogen, an optionally substituted hydrocarbyl or an acyl); or a salt thereof or a prodrug thereof.

Abstract translation: 提供了包含式（I）化合物的CRF受体拮抗剂：其中R1是任选取代的烃基，任选取代的C连接的杂环基，任选取代的N-连接的杂芳基，氰基或酰基; R2是任选取代的环状烃基或任选取代的杂环基; X是氧，硫或-NR 3 - （其中R 3是氢，任选取代的烃基或酰基）; Y1，Y2和Y3各自为任选取代的碳或氮，条件是Y1，Y2和Y3中的一个或多个为氮; 并且Z是键，-CO-，氧，硫，-SO - ， - SO 2 - ， - NR 4 - ， - NR 4 - 烷 - ， - CONR 4 - 或-NR 4 CO-（其中，alk是任选取代的C 1-4亚烷基 和R4是氢，任选取代的烃基或酰基）; 或其盐或其前药。