公开(公告)号：US06436960B1

公开(公告)日：2002-08-20

申请号：US09601426

申请日：2000-08-01

申请人： You Seung Shin ,  Jong Sung Koh ,  Hyun Il Lee ,  Jin Ho Lee ,  Jong Hyun Kim ,  Hyun Ho Chung ,  Kwi Hwa Kim ,  Tae Hwan Kwak ,  Seong Gu Ro ,  In Ae Ahn ,  Tae Saeng Choi ,  Young Hoon Oh ,  Chung Mi Kim ,  Sun Hwa Lee ,  Hyun Sung Kim

发明人： You Seung Shin ,  Jong Sung Koh ,  Hyun Il Lee ,  Jin Ho Lee ,  Jong Hyun Kim ,  Hyun Ho Chung ,  Kwi Hwa Kim ,  Tae Hwan Kwak ,  Seong Gu Ro ,  In Ae Ahn ,  Tae Saeng Choi ,  Young Hoon Oh ,  Chung Mi Kim ,  Sun Hwa Lee ,  Hyun Sung Kim

IPC分类号： A61K31454

CPC分类号： C07D401/14 ,  C07D417/14

摘要： The present invention relates to a novel piperidine derivative represented by formula (1) which shows an inhibitory activity against farnesyl transferase or pharmaceutically acceptable salts thereof, in which A, E and G are defined in the specification; to a process for preparation of the compound of formula (1); to an intermediate which is used in the preparation of the compound of formula (1); and to a pharmaceutical composition comprising the compound of formula (1) as an active ingredient.

摘要翻译： 本发明涉及式（1）所示的新型哌啶衍生物，其表现出对法呢基转移酶的抑制活性或其药学上可接受的盐，其中A，E和G在本说明书中定义; 涉及制备式（1）化合物的方法; 涉及用于制备式（1）化合物的中间体; 以及包含式（1）化合物作为活性成分的药物组合物。

公开(公告)号：US06268363B1

公开(公告)日：2001-07-31

申请号：US09554646

申请日：2000-05-17

申请人： Hyun Il Lee ,  Jong Sung Koh ,  Jin Ho Lee ,  Won Hee Jung ,  You Seung Shin ,  Hyun Ho Chung ,  Jong Hyun Kim ,  Seong Gu Ro ,  Tae Saeng Choi ,  Shin Wu Jeong ,  Tae Hwan Kwak ,  In Ae Ahn ,  Hyun Sung Kim ,  Sun Hwa Lee ,  Kwi Hwa Kim ,  Jung Kwon Yoo

发明人： Hyun Il Lee ,  Jong Sung Koh ,  Jin Ho Lee ,  Won Hee Jung ,  You Seung Shin ,  Hyun Ho Chung ,  Jong Hyun Kim ,  Seong Gu Ro ,  Tae Saeng Choi ,  Shin Wu Jeong ,  Tae Hwan Kwak ,  In Ae Ahn ,  Hyun Sung Kim ,  Sun Hwa Lee ,  Kwi Hwa Kim ,  Jung Kwon Yoo

IPC分类号： A61K314178

CPC分类号： C07D401/14 ,  C07D403/06 ,  C07D405/14 ,  C07D413/06 ,  C07D417/06 ,  C07D417/14

摘要： The present invention relates to a novel imidazole derivative represented by formula (1) which shows an inhibitory activity against farnesyl transferase or pharmaceutically acceptable salts or isomers thereof, in which A, n1 and Y are defined in the specification; to a process for preparation of the compound of formula (1); to intermediates which are used in the preparation of the compound of formula (1); and to a pharmaceutical composition comprising the compound of formula (1) as an active ingredient.

摘要翻译： 本发明涉及式（1）所示的新型咪唑衍生物，其表现出对法呢基转移酶的抑制活性或其药学上可接受的盐或异构体，其中A，n1和Y在本说明书中定义; 涉及制备式（1）化合物的方法; 用于制备式（1）化合物的中间体; 以及包含式（1）化合物作为活性成分的药物组合物。

公开(公告)号：US06518429B2

公开(公告)日：2003-02-11

申请号：US09813437

申请日：2001-03-20

申请人： Hyun Il Lee ,  Jong Sung Koh ,  Jin Ho Lee ,  Won Hee Jung ,  You Seung Shin ,  Hyun Ho Chung ,  Jong Hyun Kim ,  Seong Gu Ro ,  Tae Saeng Choi ,  Shin Wu Jeong ,  Tae Hwan Kwak ,  In Ae Ahn ,  Hyun Sung Kim ,  Sun Hwa Lee ,  Kwi Hwa Kim ,  Jung Kwon Yoo

发明人： Hyun Il Lee ,  Jong Sung Koh ,  Jin Ho Lee ,  Won Hee Jung ,  You Seung Shin ,  Hyun Ho Chung ,  Jong Hyun Kim ,  Seong Gu Ro ,  Tae Saeng Choi ,  Shin Wu Jeong ,  Tae Hwan Kwak ,  In Ae Ahn ,  Hyun Sung Kim ,  Sun Hwa Lee ,  Kwi Hwa Kim ,  Jung Kwon Yoo

IPC分类号： C07D45302

CPC分类号： C07D401/14 ,  C07D403/06 ,  C07D405/14 ,  C07D413/06 ,  C07D417/06 ,  C07D417/14

摘要： The present invention relates to novel imidazole derivatives which show an inhibitory activity against farnesyl transferase, pharmaceutically acceptable salts or isomers thereof and pharmaceutical compositions comprising such imidazole derivatives. More particularly, the present invention relates to intermediate compounds which are used in the preparation of the imidazole derivatives of the invention. Related processes also are disclosed.

公开(公告)号：US06472526B1

公开(公告)日：2002-10-29

申请号：US10005262

申请日：2001-12-03

申请人： Hyun Il Lee ,  Jong Sung Koh ,  Jin Ho Lee ,  Won Hee Jung ,  You Seung Shin ,  Hyun Ho Chung ,  Jong Hyun Kim ,  Seong Gu Ro ,  Tae Saeng Choi ,  Shin Wu Jeong ,  Tae Hwan Kwak ,  In Ae Ahn ,  Hyun Sung Kim ,  Sun Hwa Lee ,  Kwi Hwa Kim ,  Jung Kwon Yoo

发明人： Hyun Il Lee ,  Jong Sung Koh ,  Jin Ho Lee ,  Won Hee Jung ,  You Seung Shin ,  Hyun Ho Chung ,  Jong Hyun Kim ,  Seong Gu Ro ,  Tae Saeng Choi ,  Shin Wu Jeong ,  Tae Hwan Kwak ,  In Ae Ahn ,  Hyun Sung Kim ,  Sun Hwa Lee ,  Kwi Hwa Kim ,  Jung Kwon Yoo

IPC分类号： C07D40306

CPC分类号： C07D401/14 ,  C07D403/06 ,  C07D405/14 ,  C07D413/06 ,  C07D417/06 ,  C07D417/14

摘要： The present invention relates to a novel imidazole derivative represented by formula (1) which shows an inhibitory activity against farnesyl transferase or pharmaceutically acceptable salts or isomers thereof, in which A, n1 and Y are defined in the specification; to a process for preparation of the compound of formula (1); to intermediates which are used in the preparation of the compound of formula (1): and to a pharmaceutical composition comprising the compound of formula (1) as an active ingredient.

摘要翻译： 本发明涉及式（1）所示的新型咪唑衍生物，其表现出对法呢基转移酶的抑制活性或其药学上可接受的盐或异构体，其中A，n1和Y在本说明书中定义; 涉及制备式（1）化合物的方法; 用于制备式（1）化合物的中间体：和包含式（1）化合物作为活性成分的药物组合物。

公开(公告)号：US06384061B1

公开(公告)日：2002-05-07

申请号：US09463551

申请日：2000-03-30

申请人： Jin Ho Lee ,  Jong Sung Koh ,  Jong Hyun Kim ,  Hyun Il Lee ,  Won Hee Jung ,  Seong Gu Ro ,  You Seong Shin ,  Sang Woong Kim ,  Ki Won Park ,  Tae Hwan Kwak ,  Kyung Duk Moon ,  Hyun Ho Chung

发明人： Jin Ho Lee ,  Jong Sung Koh ,  Jong Hyun Kim ,  Hyun Il Lee ,  Won Hee Jung ,  Seong Gu Ro ,  You Seong Shin ,  Sang Woong Kim ,  Ki Won Park ,  Tae Hwan Kwak ,  Kyung Duk Moon ,  Hyun Ho Chung

IPC分类号： A61K3144

CPC分类号： C07D401/14 ,  C07D233/76 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14

摘要： The present invention relates to novel hydantoin compounds represented by formula (I) which shows an inhibitory activity against farnesyl transferase, and thus can be used as an anti-cancer agent, or pharmaceutically acceptable salts thereof, in which R1, R2, R3 and R4 are as defined in the present application. The present invention also relates to a process for preparation of the compound of formula (I), and to an anti-cancer composition comprising the compound of formula (I) as an active ingredient.

摘要翻译： 本发明涉及式（I）所示的新型乙内酰脲化合物，其表现出对法呢基转移酶的抑制活性，因此可用作抗癌剂或其药学上可接受的盐，其中R1，R2，R3和R4 如本申请中所定义。 本发明还涉及制备式（I）化合物的方法，以及包含式（I）化合物作为活性成分的抗癌组合物。

公开(公告)号：US07879848B2

公开(公告)日：2011-02-01

申请号：US11910370

申请日：2006-03-30

申请人： Chang-Seok Lee ,  Jong Sung Koh ,  Ki Dong Koo ,  Geun Tae Kim ,  Kyoung-Hee Kim ,  Sang Yong Hong ,  Sungsub Kim ,  Min-Jung Kim ,  Hyeon Joo Yim ,  Dongchul Lim ,  Hye Jin Kim ,  Hee Oon Han ,  Seong Cheol Bu ,  Oh Hwan Kwon ,  Sung Ho Kim ,  Gwong-Cheung Hur ,  Ji Young Kim ,  Zi-Ho Yeom ,  Dong-Jun Yeo

发明人： Chang-Seok Lee ,  Jong Sung Koh ,  Ki Dong Koo ,  Geun Tae Kim ,  Kyoung-Hee Kim ,  Sang Yong Hong ,  Sungsub Kim ,  Min-Jung Kim ,  Hyeon Joo Yim ,  Dongchul Lim ,  Hye Jin Kim ,  Hee Oon Han ,  Seong Cheol Bu ,  Oh Hwan Kwon ,  Sung Ho Kim ,  Gwong-Cheung Hur ,  Ji Young Kim ,  Zi-Ho Yeom ,  Dong-Jun Yeo

IPC分类号： C07D471/04 ,  C07D413/14 ,  A61K31/519 ,  A61K31/5355 ,  A61K31/4355 ,  A61P3/10 ,  A61K31/437 ,  A61K31/5025 ,  C07D487/04 ,  C07D217/14 ,  C07D498/04

CPC分类号： C07D487/04 ,  C07D401/06 ,  C07D413/06 ,  C07D471/04 ,  C07D498/04 ,  C07D513/04

摘要： Novel compounds exhibiting good inhibitory activity versus Dipeptidyl Peptidase-IV(DPP-IV) include those of the following formula (1) or pharmaceutically acceptable salt thereof: wherein A is a substituted or unsubstituted 1,4,5,7-tetrahydro-pyrazolo[3,4-c]pyridine, 5,6 -dihydro-8H-[1,2,4]triazolo[4,3-a]pyrazine, 4,5-dihydro-7H-isooxazolo[3,4-c]pyridine, 3,4 -dihydroisoquinoline, 5,8-dihydropyrido[3,4-d]pyrimidine, or 6,7 -dihydro[1,3]thiazolo[4,5,c]pyridine, and B is a substituted or unsubstituted piperidin-2-one, morpholin-3-one, oxazolidin-2-one, pyrrolidin-2-one, or 1,5-dihydro-pyrrol-2-one. Methods of preparing the novel inhibitory compounds of formula (1) and pharmaceutical compositions containing the same as an active agent are disclosed.

摘要翻译： 对二肽基肽酶-IV（DPP-IV）显示出良好抑制活性的新型化合物包括下式（1）或其药学上可接受的盐：其中A是取代或未取代的1,4,5,7-四氢 - 吡唑并[ 3,4-c]吡啶，5,6-二氢-8H- [1,2,4]三唑并[4,3-a]吡嗪，4,5-二氢-7H-异恶唑并[3,4-c]吡啶 ，3,4-二氢异喹啉，5,8-二氢吡啶并[3,4-d]嘧啶或6,7-二氢[1,3]噻唑并[4,5，c]吡啶，B是取代或未取代的哌啶 -2-酮，吗啉-3-酮，恶唑烷-2-酮，吡咯烷-2-酮或1,5-二氢 - 吡咯-2-酮。 公开了制备式（1）的新型抑制性化合物和含有它们作为活性剂的药物组合物的方法。

公开(公告)号：US20080188471A1

公开(公告)日：2008-08-07

申请号：US11910370

申请日：2006-03-30

申请人： Chang-Seok Lee ,  Jong Sung Koh ,  Ki Dong Koo ,  Geun Tae Kim ,  Kyoung-Hee Kim ,  Sang Yong Hong ,  Sungsub Kim ,  Min-Jung Kim ,  Hyeon Joo Yim ,  Dongchul Lim ,  Hye Jin Kim ,  Hee Oon Han ,  Seong Cheol Bu ,  Oh Hwan Kwon ,  Sung Ho Kim ,  Gwong-Cheung Hur ,  Ji Young Kim ,  Zi-Ho Yeom ,  Dong-Jun Yeo

发明人： Chang-Seok Lee ,  Jong Sung Koh ,  Ki Dong Koo ,  Geun Tae Kim ,  Kyoung-Hee Kim ,  Sang Yong Hong ,  Sungsub Kim ,  Min-Jung Kim ,  Hyeon Joo Yim ,  Dongchul Lim ,  Hye Jin Kim ,  Hee Oon Han ,  Seong Cheol Bu ,  Oh Hwan Kwon ,  Sung Ho Kim ,  Gwong-Cheung Hur ,  Ji Young Kim ,  Zi-Ho Yeom ,  Dong-Jun Yeo

IPC分类号： A61K31/4985 ,  A61P3/04 ,  A61P3/10 ,  C07D471/04 ,  A61K31/5355 ,  C07D487/04 ,  C07D413/02 ,  A61K31/519

CPC分类号： C07D487/04 ,  C07D401/06 ,  C07D413/06 ,  C07D471/04 ,  C07D498/04 ,  C07D513/04

摘要： The present invention relates to novel compounds exhibiting good inhibitory activity versus Dipeptidyl Peptidase-IV (DPP-IV), methods of preparing the same and pharmaceutical compositions containing the same as an active agent.

摘要翻译： 本发明涉及相对于二肽基肽酶-IV（DPP-IV）显示出良好抑制活性的新化合物，其制备方法和含有该活性剂的药物组合物。

公开(公告)号：US5763631A

公开(公告)日：1998-06-09

申请号：US667133

申请日：1996-06-20

申请人： Sung Chun Kim ,  Nakyen Choy ,  Chang Sun Lee ,  Ho I. Choi ,  Jong Sung Koh ,  Heungsik Yoon ,  Chi Hyo Park ,  Sang Soo Kim ,  Young Chan Son

发明人： Sung Chun Kim ,  Nakyen Choy ,  Chang Sun Lee ,  Ho I. Choi ,  Jong Sung Koh ,  Heungsik Yoon ,  Chi Hyo Park ,  Sang Soo Kim ,  Young Chan Son

IPC分类号： A61K31/335 ,  A61K31/00 ,  A61K31/336 ,  A61K38/00 ,  A61P31/00 ,  A61P31/12 ,  A61P31/18 ,  C07C213/02 ,  C07C217/08 ,  C07C269/04 ,  C07C271/20 ,  C07C271/22 ,  C07D301/02 ,  C07D303/36 ,  C07D303/38 ,  C07D303/40 ,  C07D303/46 ,  C07D405/12 ,  C07D405/14 ,  C07D493/08 ,  C07K5/02 ,  C07K5/06 ,  C07K5/065 ,  C07K5/078 ,  C07K7/02 ,  C07D303/08 ,  C07D215/38 ,  C07D235/04 ,  C07D413/00

CPC分类号： C07D303/38 ,  C07C217/08 ,  C07C271/20 ,  C07C271/22 ,  C07D303/36 ,  C07D303/46 ,  C07D405/12 ,  C07D405/14 ,  C07D493/08 ,  C07K5/0207 ,  C07K5/06026 ,  C07K5/06078 ,  C07K5/06139 ,  C07K7/02 ,  A61K38/00 ,  C07C2101/14

摘要： Cis-epoxide compounds of formula (I-3) and pharmaceutically acceptable salts, hydrates and solvates thereof: ##STR1## wherein: R.sup.1 is a cycloalkyl, or arly-substituted lower alkyl group; K and J are independently a group having the formula of ##STR2## wherein R.sup.18 is a lower alkyl group optionally substituted with an aryl radical; X is O, NH, or N--CH.sub.3 ; and R.sup.19 is an aromatic hetercyclic sysstem containing a nitrogen atom in its ring, or a lower alkyl group optionally substituted with an aryl radical, or a hydrogen; G is an amino acid which is linked to K-- and ##STR3## by peptide bonds in formula (I-3); Q is an amino acid which is linked to by peptide bonds in formula (I-3), or a group having the formula of wherein R.sup.20 is a lower alkyl group optionally substituted with an aromatic radical; and Y is CH.sub.2, O or NH; and r is 0 or 1, except that Q is a group having the formula of r is 0.

摘要翻译： 式（I-3）的顺式环氧化合物及其药学上可接受的盐，水合物和溶剂化物：其中：R1是环烷基或芳取代的低级烷基; K和J独立地是具有下式的基团：其中R18是任选被芳基取代的低级烷基; X是O，NH或N-CH 3; R19是在其环中含有氮原子的芳族杂环体系，或任选被芳基取代的低级烷基或氢; G是通过式（I-3）中的肽键与K-和连接的氨基酸; Q是通过式（I-3）中的肽键连接的氨基酸或具有下式的基团：其中R 20是任选被芳族基团取代的低级烷基; 并且Y是CH 2，O或NH; 并且r为0或1，除了Q是具有式r的基团为0。

公开(公告)号：US5773468A

公开(公告)日：1998-06-30

申请号：US572402

申请日：1995-12-14

申请人： Sung Chun Kim ,  Young Chan Son ,  Ho Il Choi ,  Heungsik Yoon ,  Chi Hyo Park ,  Nakyen Choy ,  Chang Sun Lee ,  Jong Sung Koh ,  Kwang Yul Moon ,  Won Hee Jung ,  Chung Ryeol Kim

发明人： Sung Chun Kim ,  Young Chan Son ,  Ho Il Choi ,  Heungsik Yoon ,  Chi Hyo Park ,  Nakyen Choy ,  Chang Sun Lee ,  Jong Sung Koh ,  Kwang Yul Moon ,  Won Hee Jung ,  Chung Ryeol Kim

IPC分类号： A61K38/00 ,  C07D303/46 ,  A01N43/20 ,  A01N31/34

CPC分类号： C07D303/46 ,  A61K38/00

摘要： The present invention relates to a novel compound of formula (I) and pharmaceutically acceptable salts, hydrates and solvates thereof which is an irreversible HIV protease inhibitor; a process for the preparation thereof; and a pharmaceutical composition containing the compound as an active ingredient which is useful for treating or preventing diseases caused by HIV infection. ##STR1##

摘要翻译： 本发明涉及新的式（I）化合物及其药学上可接受的盐，水合物和溶剂化物，其是不可逆的HIV蛋白酶抑制剂; 其制备方法; 以及含有该化合物作为活性成分的药物组合物，其可用于治疗或预防由HIV感染引起的疾病。 （一）

公开(公告)号：US08404677B2

公开(公告)日：2013-03-26

申请号：US12916368

申请日：2010-10-29

申请人： Hong Woo Kim ,  Jong Sung Koh ,  Jaekyoo Lee ,  Ho-Juhn Song ,  Youngsam Kim ,  Hee Kyu Lee ,  Jang-Sik Choi ,  Sun-Hee Lim ,  Sunhwa Chang

发明人： Hong Woo Kim ,  Jong Sung Koh ,  Jaekyoo Lee ,  Ho-Juhn Song ,  Youngsam Kim ,  Hee Kyu Lee ,  Jang-Sik Choi ,  Sun-Hee Lim ,  Sunhwa Chang

IPC分类号： C07D471/04 ,  C07D211/86 ,  A61K31/519 ,  A61K31/4375

CPC分类号： A61K31/519 ,  C07D471/04

摘要： The present invention provides a new group of protein kinase inhibitors, pyrido[4,3,-d]pyrimidin-5-one derivatives, and pharmaceutically acceptable salts thereof that are useful for intreating cell proliferative disease and disorder such as cancer, autoimmune diseases, infection, cardiovascular disease and neurodegenerative disease and disorder. The present invention provides methods for synthesizing and administering the protein kinase inhibitor compounds. The present invention also provides pharmaceutical formulations comprising at least one of the protein kinase inhibitor compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor. The invention also provides useful intermediates generated during the syntheses of the pyrido[4,3,-d]pyrimidin-5-one derivatives.

摘要翻译： 本发明提供了一组新的蛋白激酶抑制剂，吡啶并[4,3，-d]嘧啶-5-酮衍生物及其药学上可接受的盐，其可用于促进细胞增殖性疾病和病症如癌症，自身免疫性疾病， 感染，心血管疾病和神经退行性疾病和障碍。 本发明提供了合成和施用蛋白激酶抑制剂化合物的方法。 本发明还提供了包含至少一种蛋白激酶抑制剂化合物以及药学上可接受的载体，稀释剂或赋形剂的药物制剂。 本发明还提供了在吡啶并[4,3， - d]嘧啶-5-酮衍生物的合成过程中产生的有用的中间体。