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1. 发明授权

EP3099294B1 PHARMACEUTICAL COMPOSITION INCLUDING 5-{4-(AMINOSULFONYL)PHENYL}-2,2-DIMETHYL-4-(3-FLUOROPHENYL)-3(2H)-FURANONE AND CAPSULE FORMULATION INCLUDING THE PHARMACEUTICAL COMPOSITION 有权
公开(公告)号：EP3099294B1
公开(公告)日：2018-08-01
申请号：EP15742755.0
申请日：2015-01-29
申请人： Crystalgenomics Inc.
发明人： KIM, Byung-Ha , AHN, Sik Il , PARK, Jae-Yeon , KIM, Tae Ryong , CHO, Joong Myung , RO, Seonggu
IPC分类号： A61K9/48 , A61K31/34
CPC分类号： A61K31/34 , A61K9/485 , A61K9/4858 , A61K9/4866 , A61K31/397 , A61K31/42
摘要： The present invention relates to a pharmaceutical composition including (i) the compound of Formula 1 described in the specification or a pharmaceutically acceptable salt thereof, (ii) a pharmaceutically acceptable diluent, and (iii) a pharmaceutically acceptable lubricant. The compound of Formula 1 or pharmaceutically acceptable salt thereof has a 50% volume particle diameter (d(0.5)) of 3 μm to 9 μm. The pharmaceutical composition of the present invention has the advantages of good stability, high dissolution rate, improved content uniformity, and excellent pharmacokinetic properties. Due to these advantages, the pharmaceutical composition of the present invention is effective in treating inflammation or pain.

2. 发明公开

EP3099294A1 PHARMACEUTICAL COMPOSITION INCLUDING 5-{4-(AMINOSULFONYL)PHENYL}-2,2-DIMETHYL-4-(3-FLUOROPHENYL)-3(2H)-FURANONE AND CAPSULE FORMULATION INCLUDING THE PHARMACEUTICAL COMPOSITION 审中-公开
标题翻译：包括一种药物组合物5- {4-（氨基磺酰基）}苯基} -2,2-二甲基-4-（3-氟苯基）的药物组合物-3（2H） - 呋喃酮与胶囊制剂
公开(公告)号：EP3099294A1
公开(公告)日：2016-12-07
申请号：EP15742755.0
申请日：2015-01-29
申请人： Crystalgenomics Inc.
发明人： KIM, Byung-Ha , AHN, Sik Il , PARK, Jae-Yeon , KIM, Tae Ryong , CHO, Joong Myung , RO, Seonggu
IPC分类号： A61K31/34 , A61K31/255 , A61K9/48 , A61K47/38
CPC分类号： A61K31/34 , A61K9/485 , A61K9/4858 , A61K9/4866 , A61K31/397 , A61K31/42
摘要： The present invention relates to a pharmaceutical composition including (i) the compound of Formula 1 described in the specification or a pharmaceutically acceptable salt thereof, (ii) a pharmaceutically acceptable diluent, and (iii) a pharmaceutically acceptable lubricant. The compound of Formula 1 or pharmaceutically acceptable salt thereof has a 50% volume particle diameter (d
(0.5) ) of 3 μm to 9 μm. The pharmaceutical composition of the present invention has the advantages of good stability, high dissolution rate, improved content uniformity, and excellent pharmacokinetic properties. Due to these advantages, the pharmaceutical composition of the present invention is effective in treating inflammation or pain.
摘要翻译：本发明涉及包括式（I）1的在说明书或其药学上可接受的盐中所述的化合物，（ii）药学上可接受的稀释剂，和（iii）药学上可接受的润滑剂的药物组合物。式1或其药学上可接受的盐的化合物或其具有3微米的50％体积粒径（D（0.5））到9微米。本发明的药物组合物具有良好的稳定性，高的溶解速率，提高了含量均匀度，和优异的药代动力学性质的优点。由于优势论文，本发明的药物组合物可有效治疗炎症或疼痛。

3. 发明授权

EP1948601B1 FAB I INHIBITOR AND PROCESS FOR PREPARING SAME 有权
标题翻译： FAB I抑制剂和方法及其
公开(公告)号：EP1948601B1
公开(公告)日：2016-04-13
申请号：EP06799211.5
申请日：2006-10-13
申请人： Crystalgenomics, Inc.
发明人： KIM, Cheol Min , HYUN, Young Lan , SHIN,Dong Kyu , RO, Seonggu , CHO, Joong Myung
IPC分类号： A61K31/4412 , A61P31/04 , C07D209/18 , C07D495/04 , C07D487/04 , C07D471/04
CPC分类号： C07D213/64 , C07D213/69 , C07D213/70 , C07D213/74 , C07D237/16 , C07D239/47 , C07D239/52 , C07D401/06 , C07D401/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/14

4. 发明公开

EP2226315A1 2-AMINOQUINAZOLINE DERIVATIVE 审中-公开
标题翻译： 2- AMINOCHINAZOLIN-衍生金融
公开(公告)号：EP2226315A1
公开(公告)日：2010-09-08
申请号：EP08869161.3
申请日：2008-12-26
申请人： Carna Biosciences Inc. , Crystalgenomics, Inc.
发明人： SAWA, Masaaki , YOKOTA, Koichi , MORIYAMA, Hideki , SHIN, Myoungyoup , RO, Seonggu , CHO, Joong Myung
IPC分类号： C07D239/84 , A61K31/517 , A61K31/5377 , A61P3/00 , A61P5/00 , A61P9/00 , A61P11/06 , A61P19/08 , A61P25/00 , A61P25/28 , A61P29/00 , A61P35/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12
CPC分类号： C07D239/84 , C07D401/14 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： An object of the present invention is to provide compounds which are useful as protein kinase inhibitors.
Disclosed is a 2-aminoquinazoline derivative represented by the following formula (I):

wherein R 1 represents a lower alkyl group which may be substituted with a halogen atom, or a halogen atom; R 2 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a halogen atom, a hydroxyl group, a substituted or unsubstituted lower alkoxy group, a substituted or unsubstituted amino group, a substituted or unsubstituted acylamino group, a carboxyl group, a lower alkoxycarbonyl group, a carbamoyl group, or a substituted or unsubstituted lower alkylureido group; and X, Y and Z each independently represents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a halogen atom, a hydroxyl group, a carboxyl group, a lower alkoxycarbonyl group, a cyano group, a carbamoyl group, a substituted or unsubstituted lower alkoxy group, a substituted or unsubstituted amino group, a substituted or unsubstituted lower alkoxycarbonylamino group, a substituted or unsubstituted lower alkylaminocarbonyl group, a lower alkylsulfonylamino group, a substituted or unsubstituted lower alkylureido group, or a substituted or unsubstituted acylamino group, or X and Y may be combined to form a 5- to 6-membered ring forming a bicyclic fused ring, wherein the 5- to 6-membered ring may optionally have a substituent, provided that when X and Y are not combined to form a fused ring, R 2 represents a hydrogen atom and, when X and Y are combined to form a fused ring, a saturated or unsaturated, bicyclic alicyclic or heterocyclic fused ring can be formed.
摘要翻译：本发明的目的是提供可用作蛋白激酶抑制剂的化合物。公开了由下式（I）表示的2-氨基喹唑啉衍生物：其中R 1表示可以被卤素原子或卤素原子取代的低级烷基; R 2表示氢原子，取代或未取代的低级烷基，卤素原子，羟基，取代或未取代的低级烷氧基，取代或未取代的氨基，取代或未取代的酰氨基，羧基，低级烷氧基羰基，氨基甲酰基或取代或未取代的低级烷基脲基; X，Y和Z各自独立地表示氢原子，取代或未取代的低级烷基，卤素原子，羟基，羧基，低级烷氧基羰基，氰基，氨基甲酰基，取代或未取代的取代或未取代的低级烷氧基羰基氨基，取代或未取代的低级烷基氨基羰基，低级烷基磺酰基氨基，取代或未取代的低级烷基脲基，或取代或未取代的酰基氨基，或X 并且Y可以组合形成一个形成双环稠合环的5至6元环，其中5至6元环可以任选地具有取代基，条件是当X和Y不组合形成稠环时 R 2表示氢原子，当X和Y组合形成稠环时，可以形成饱和或不饱和的双环脂环或杂环稠合环。

5. 发明公开

EP1945606A1 ALKYLCARBAMOYL NAPHTHALENYLOXY- OCTENOYLHYDROXYAMIDE DERIVATIVES HAVING INHIBITORY ACTIVITY AGAINST HISTONE DEACETYLASE AND PREPARATION THEREOF 审中-公开
标题翻译：具有抑制作用的生产和组蛋白去乙酰ALKYLCARBAMOYLNAPHTHALINYLOXYOCTENOYLHYDROXYAMIDDERIVATE
公开(公告)号：EP1945606A1
公开(公告)日：2008-07-23
申请号：EP06812321.5
申请日：2006-10-31
申请人： KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY , Crystalgenomics, Inc.
发明人： LEE, Cheol Hae , JUNG, Hee Jung , KIM, Jae Hak , JEONG, Won Jang , CHO, Joong Myung , RO, Seonggu , HYUN, Young Lan , SHIN, Dongkyu , LEE, Cheol Soon 6f, 2nd Building Of Asan Institute
IPC分类号： C07C237/32
CPC分类号： C07C259/06 , C07C2601/14 , C07C2601/16 , C07D207/12 , C07D207/14 , C07D211/58 , C07D213/75 , C07D233/54 , C07D233/61 , C07D295/185 , C07D307/66 , C07D333/20
摘要： This invention discloses a novel alkylcarbamoyl naphthalenyloxy octenoylhydroxyamide derivative of formula (1) useful for inhibiting the enzyme activity of histone deacetylase, which leads to effective suppression of the cancer cell proliferation, a method for preparing same and a pharmaceutical composition comprising same.
摘要翻译：本发明盘松式的新颖的烷基氨基甲酰基萘氧基octenoylhydroxyamide衍生物（1）为组蛋白脱乙酰酶抑制活性，这导致有效地抑制癌症细胞的增殖，其制备方法和包含其的药物组合物是有用的。

6. 发明公开

EP2188295A2 PYRIDINE DERIVATIVES AND METHODS OF USE THEREOF 审中-公开
标题翻译：吡啶及其使用方法
公开(公告)号：EP2188295A2
公开(公告)日：2010-05-26
申请号：EP08831492.7
申请日：2008-08-08
申请人： Crystalgenomics, Inc.
发明人： KIM, Sun, Nam , HONG, Yong, Rae , SHIN, Dongkyu , RO, Seonggu , CHO, Joong, Myung , LEE, Mi Jung , CHANG, Ho, Jin
IPC分类号： C07D495/04 , C07D491/048 , C07D471/04
CPC分类号： C07D495/04 , C07D471/04 , C07D491/048
摘要： Disclosed herein are pyridine derivatives, or a pharmaceutically acceptable salt, ester, amide, or prodrug thereof, pharmaceutical compositions comprising the same, and methods of modulating the level or activity of HIF in a subject, inhibiting hydroxylation of HIF α in a subject, modulating expression of HIF -regulated genes in a subject, treating an HIF-related disorder in a subject, increasing levels of endogenous EPO in a subject, or treating a disorder in a subject, using the disclosed compounds.

7. 发明公开

EP1984370A1 IMIDAZOPYRIDINE DERIVATIVES INHIBITING PROTEIN KINASE ACTIVITY, METHOD FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITION CONTAINING SAME 审中-公开
标题翻译：蛋白激酶抑制活性咪唑，其制备方法和药物组合物包含此
公开(公告)号：EP1984370A1
公开(公告)日：2008-10-29
申请号：EP07701041.1
申请日：2007-01-23
申请人： Crystalgenomics, Inc. , YUYU Pharma, Inc.
发明人： LEE, Seung Chul , CHOI, Jin Seok , OH, Jung Hoon , PARK, Boonsaeng , KIM, Yong Eun , LEE, Jun Hee , SHIN, Dongkyu , KIM, Cheol Min , HYUN, Young-Lan , LEE, Cheol Soon , CHO, Joong-Myung , RO, Seonggu
IPC分类号： C07D487/04
CPC分类号： C07D471/04
摘要： The inventive imidazopyridine derivative can be used in a pharmaceutical composition for preventing or treating diseases such as diabetes, obesity, dementia, cancer, and inflammation, since it can efficiently inhibit the activities of several protein kinases including glycogen synthase kinase-3 (GSK-3), aurora kinase, extracellular signal-regulated kinase (ERK), protein kinase B (AKT), and the likes, to control signal transductions thereof.

8. 发明授权

EP2940014B1 2,3-DIHYDRO-ISOINDOLE-1-ON DERIVATIVE AS BTK KINASE SUPPRESSANT, AND PHARMACEUTICAL COMPOSITION INCLUDING SAME 有权
公开(公告)号：EP2940014B1
公开(公告)日：2018-09-26
申请号：EP13867650.7
申请日：2013-12-26
申请人： Crystalgenomics, Inc.
发明人： HONG, Yong Rae , NA, Jeong Eun , MIN, Im Sook , CHA, Hyun Ju , KWON, Sool Ki , RO, Seonggu , CHO, Joong Myung
IPC分类号： C07D403/04 , A61K31/4178 , A61P35/00 , A61P25/00
CPC分类号： C07D403/10 , A61K31/4178 , A61K45/06 , A61P35/00 , C07D403/04
摘要： The present invention provides a compound selected from the group consisting of a compound of formula (I), pharmaceutically acceptable salts, esters, prodrugs, hydrates, solvates and isomers thereof; a use of the compound for the treatment, relief or prevention of diseases caused by absormal or uncontrolled activation of protein kinase, and a use of the compound for the manufacture of a medicament for the treatment, relief or prevention of the diseases; a pharmaceutical composition comprising the compound as an active ingredient; and a method for the treatment, relief or prevention of the diseases using the compound. The inventive compound is useful for the treatment, relief or prevention of diseases caused by abnormal or uncontrolled activation of protein kinase.

9. 发明公开

EP1590333A1 GLYCOGEN SYNTHASE KINASE 3BETA INHIBITOR, COMPOSITION AND PROCESS FOR THE PREPARATION THEREOF 审中-公开
标题翻译：糖原合酶激酶3β的抑制剂，组合物和方法及其
公开(公告)号：EP1590333A1
公开(公告)日：2005-11-02
申请号：EP04703520.9
申请日：2004-01-20
申请人： Crystalgenomics, Inc. , Yuyu Inc.
发明人： CHO, Joong Myung , RO, Seonggu , LEE, Tae Gyu , LEE, Kyung Joo , SHIN, Dongkyu , HYUN, Young-Lan , LEE, Seung Chul , KIM, Jin Hwan , JEON, Young Ho
IPC分类号： C07D235/18
CPC分类号： C07D235/18 , C07D401/12 , C07D403/12 , C07D409/12
摘要： Novel compounds having hydroxybenzoimidazole carboxylic amide are useful for inhibiting glycogen synthase kinase 3β (GSK-3β).

10. 发明公开

EP3428161A1 2,3-DIHYDRO-ISOINDOLE-1-ON DERIVATIVE AS BTK KINASE SUPPRESSANT, AND PHARMACEUTICAL COMPOSITION INCLUDING SAME 有权
公开(公告)号：EP3428161A1
公开(公告)日：2019-01-16
申请号：EP18190153.9
申请日：2013-12-26
申请人： Crystalgenomics, Inc.
发明人： HONG, Yong Rae , NA, Jeong Eun , MIN, Im Sook , CHA, Hyun Ju , KWON, Sool Ki , RO, Seonggu , CHO, Joong Myung
IPC分类号： C07D403/04 , C07D403/10 , A61P35/00 , A61K31/4178 , A61P25/00
摘要： The present invention provides a compound selected from the group consisting of a compound of formula (I), pharmaceutically acceptable salts, esters, prodrugs, hydrates, solvates and isomers thereof; a use of the compound for the treatment, relief or prevention of diseases caused by absormal or uncontrolled activation of protein kinase, and a use of the compound for the manufacture of a medicament for the treatment, relief or prevention of the diseases; a pharmaceutical composition comprising the compound as an active ingredient; and a method for the treatment, relief or prevention of the diseases using the compound. The inventive compound is useful for the treatment, relief or prevention of diseases caused by abnormal or uncontrolled activation of protein kinase.

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