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1. 发明申请

WO2011060295A8 KINASE INHIBITORS 审中-公开
标题翻译：激酶抑制剂
公开(公告)号：WO2011060295A8
公开(公告)日：2011-10-27
申请号：PCT/US2010056583
申请日：2010-11-12
申请人： GENOSCO , OSCOTEC INC , LEE JAEKYOO , SONG HO-JUHN , KOH JONG SUNG , LEE HEE KYU , KIM YOUNGSAM , KIM HONG WOO , CHANG SUNHWA , LIM SUN-HEE , CHOI JANG-SIK , KIM JUNG-HO , KIM SE-WON
发明人： LEE JAEKYOO , SONG HO-JUHN , KOH JONG SUNG , LEE HEE KYU , KIM YOUNGSAM , KIM HONG WOO , CHANG SUNHWA , LIM SUN-HEE , CHOI JANG-SIK , KIM JUNG-HO , KIM SE-WON
IPC分类号： A01N43/54 , A61K31/505
CPC分类号： A61K31/505 , C07D403/04 , C07D403/14 , C07D405/14 , C07D417/14 , C07D487/08
摘要： The present invention provides a new group of protein kinase inhibitors, pyrropyrimidine and pyrazolopyrimidine derivatives, and pharmaceutically acceptable salts and prodrugs thereof that are useful for treating 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 pyrropyrimidine and pyrazolopyrimidine derivatives.
摘要翻译：本发明提供了一组新的蛋白激酶抑制剂，吡咯嘧啶和吡唑并嘧啶衍生物及其药学上可接受的盐和前药，其可用于治疗细胞增殖性疾病和病症如癌症，自身免疫性疾病，感染，心血管疾病和神经变性疾病和病症。本发明提供了合成和施用蛋白激酶抑制剂化合物的方法。本发明还提供了药物制剂，其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。本发明还提供了在合成pyrropyrimidine和吡唑并嘧啶衍生物期间产生的有用中间体。

2. 发明申请

WO2011132967A3 ALPHA-ARYLMETHOXYACRYLATE DERIVATIVE, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME 审中-公开
标题翻译： ALPHA-ARYLMETHOXYACRYLATE衍生物，其制备方法和含有其的药物组合物
公开(公告)号：WO2011132967A3
公开(公告)日：2012-03-08
申请号：PCT/KR2011002892
申请日：2011-04-21
申请人： OSCOTEC INC , KIM SE-WON , KIM JUNG HO , KIM SE-NYUN , KANG DAE-PIL , HAN YOUN HO , JIN GUO FAN , JUNG DONG-SIK , PARK SUNG-HO , KIM JI MIN , ZHENG JHI
发明人： KIM SE-WON , KIM JUNG HO , KIM SE-NYUN , KANG DAE-PIL , HAN YOUN HO , JIN GUO FAN , JUNG DONG-SIK , PARK SUNG-HO , KIM JI MIN , ZHENG JHI
IPC分类号： C07C251/48 , A61K31/15 , A61P35/00 , C07C251/50
CPC分类号： A61K31/216 , A61K31/24 , A61K31/336 , A61K31/40 , A61K31/415 , A61K31/421 , A61K31/4402 , A61K31/4409 , A61K31/4453 , A61K31/5375 , C07C69/736 , C07C217/20 , C07C251/48 , C07C251/86 , C07C2601/02 , C07C2601/08 , C07D213/30 , C07D231/12 , C07D261/08 , C07D295/088 , C07D295/30 , C07D303/12
摘要： The present invention relates to an alpha-arylmethoxyacrylate derivative, a preparation method thereof, and a pharmaceutical composition containing same. The alpha-arylmethoxyacrylate derivative compound of the present invention inhibits an HIF which is a protein playing an important role in the regulation of the expression of genes involved in energy metabolism, vasomotor control, angiogenesis and apoptosis, and in the cell reaction in low oxygen conditions, and thus can be used as an agent for preventing or treating diseases such as cancer, arthritis, psoriasis, diabetic retinopathy, macular degeneration or the like.
摘要翻译：本发明涉及α-芳基甲氧基丙烯酸酯衍生物，其制备方法和含有它们的药物组合物。本发明的α-芳基甲氧基丙烯酸酯衍生化合物抑制HIF，其是在调节涉及能量代谢，血管运动控制，血管发生和凋亡的基因的表达以及在低氧条件下的细胞反应中起重要作用的蛋白质因此可以用作预防或治疗诸如癌症，关节炎，牛皮癣，糖尿病性视网膜病变，黄斑变性等疾病的药剂。

3. 发明申请

WO2011065800A3 PYRIMIDINE DERIVATIVE, METHOD FOR PREPARING SAME AND PHARMACEUTICAL COMPOSITION CONTAINING SAME 审中-公开
标题翻译：嘧啶衍生物，其制备方法及含有该组合物的药物组合物
公开(公告)号：WO2011065800A3
公开(公告)日：2011-10-27
申请号：PCT/KR2010008522
申请日：2010-11-30
申请人： OSCOTEC INC , KIM SE-WON , KIM JUNG-KEUN , KIM SE-NYUN , KANG DAE-PIL , HWANG HEA-JUN , KIM YOUNG-SAM
发明人： KIM SE-WON , KIM JUNG-KEUN , KIM SE-NYUN , KANG DAE-PIL , HWANG HEA-JUN , KIM YOUNG-SAM
IPC分类号： C07D239/10 , A61K31/505 , A61P19/10 , C07D403/04
CPC分类号： C07D239/10 , C07D403/04
摘要： A pyridimine derivative compound of the present invention can be usefully used in bone formation during the growth period as well as in prevention and treatment of metabolic bone diseases such as osteoporosis as a result of increasing bone density by promoting differentiation of osteroblasts. In addition, a pharmaceutical composition of the prevent invention can be used as a therapeutic agent for various metabolic bone diseases such as renal osterodystrophy, osteromalacia, Paget's disease, anostosis, and the like. The pharmaceutical composition also treats fracture and can be used as a therapeutic agent that suppresses bone metastasis of cancer.
摘要翻译：本发明的吡啶亚胺衍生物化合物可以有效用于生长期间的骨形成以及由于促进成骨细胞的分化而增加骨密度的结果，预防和治疗代谢性骨疾病如骨质疏松症。另外，本发明的药物组合物可以用作各种代谢性骨疾病如肾性骨营养不良症，软骨病，佩吉特病，骨关节病等的治疗剂。该药物组合物还可治疗骨折并可用作抑制癌症骨转移的治疗剂。

4. 发明专利

HUE056048T2 Helyettesített pirimidin vegyületek és SYK inhibitorként való alkalmazásuk 未知
公开(公告)号：HUE056048T2
公开(公告)日：2022-01-28
申请号：HUE14856054
申请日：2014-10-21
申请人： GENOSCO , OSCOTEC INC
发明人： LEE JAEKYOO , CHOI JANG-SIK , HWANG HAE-JUN , SONG HO-JUHN , KIM JUNG-HO , KIM SE-WON , KOH JONG , LEE JAESANG , LEE TAE-IM , CHOI YUNG-GEUN , PARK SUNG-HO , LEE IN , SUH BYUNG-CHUL , SALGAONKAR PARESH DEVIDAS , JUNG DONG-SIK
IPC分类号： C07D413/14 , A61P35/00 , C07D413/04

5. 发明专利

SG10201407453TA KINASE INHIBITORS 未知
公开(公告)号：SG10201407453TA
公开(公告)日：2014-12-30
申请号：SG10201407453T
申请日：2010-11-12
申请人： GENOSCO , OSCOTEC INC
发明人： LEE JAEKYOO , SONG HO-JUHN , KOH JONG SUNG , LEE HEE KYU , KIM YOUNGSAM , KIM HONG WOO , CHANG SUNHWA , LIM SUN-HEE , CHOI JANG-SIK , KIM JUNG-HO , KIM SE-WON
摘要： - 125 - KINASE INHIBITORS Abstract The present invention provides a new group of protein kinase inhibitors, pyrropyrimidine and pyrazolopyrimidine derivatives, and pharmaceutical^ acceptable salts and prodrugs thereof that are useful for treating 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 pyrropyrimidine and pyrazolopyrimidine derivatives. Figure: None

6. 发明专利

PL3060562T3 PODSTAWIONE ZWIĄZKI PIRYMIDYNOWE I ICH ZASTOSOWANIE JAKO INHIBITORY SYK 未知
公开(公告)号：PL3060562T3
公开(公告)日：2022-01-10
申请号：PL14856054
申请日：2014-10-21
申请人： GENOSCO , OSCOTEC INC
发明人： LEE JAEKYOO , CHOI JANG-SIK , HWANG HAE-JUN , SONG HO-JUHN , KIM JUNG-HO , KIM SE-WON , KOH JONG SUNG , LEE JAESANG , LEE TAE-IM , CHOI YUNG-GEUN , PARK SUNG-HO , LEE IN YONG , SUH BYUNG-CHUL , SALGAONKAR PARESH DEVIDAS , JUNG DONG-SIK
IPC分类号： C07D413/14 , A61K31/505 , A61K31/506 , A61P35/00 , C07D413/04

7. 发明专利

EA024729B1 КИНАЗНЫЕ ИНГИБИТОРЫ 未知
公开(公告)号：EA024729B1
公开(公告)日：2016-10-31
申请号：EA201290324
申请日：2010-11-12
申请人： GENOSCO , OSCOTEC INC
发明人： LEE JAEKYOO , SONG HO-JUHN , KOH JONG SUNG , LEE HEE KYU , KIM YOUNGSAM , KIM HONG WOO , CHANG SUNHWA , LIM SUN-HEE , CHOI JANG-SIK , KIM JUNG-HO , KIM SE-WON
IPC分类号： A01N43/54 , A61K31/505
摘要： Визобретениизаявленановаягруппапротеинкиназныхингибиторов, производныхпирропиримидинаи пиразолопиримидинаобщейформулы Iиихфармацевтическиприемлемыесоли, которыеприменяютдлялеченияпролиферативныхзаболеванийи расстройствклеток, такихкакрак, аутоиммунныезаболевания, инфекции, сердечно-сосудистыезаболевания, нейродегенеративныезаболеванияи расстройства. Визобретениипредставленыспособысинтезаи введениясоединенийпротеинкиназныхингибиторов. Визобретениитакжепредставленыфармацевтическиекомпозиции, содержащиепоменьшеймереодносоединениепротеинкиназногоингибиторавместес фармацевтическиприемлемымносителем, разбавителемилинаполнителем. Визобретениитакжепредставленыпромежуточныесоединения, полученныевовремясинтезапроизводныхпирропиримидинаи пиразолопиримидина.

8. 发明专利

MY184561A SUBSTITUTED PYRIMIDINE COMPOUNDS AND THEIR USE AS SYK INHIBITORS 未知
公开(公告)号：MY184561A
公开(公告)日：2021-04-03
申请号：MYPI2016701436
申请日：2014-10-21
申请人： GENOSCO , OSCOTEC INC
发明人： LEE JAEKYOO , CHOI JANG-SIK , HWANG HAE-JUN , SONG HO-JUHN , KIM JUNG-HO , KIM SE-WON , KOH JONG SUNG , LEE JAESANG , LEE TAE-IM , CHOI YUNG-GEUN , PARK SUNG-HO , LEE IN YONG , SUH BYUNG-CHUL , SALGAONKAR PARESH DEVIDAS , JUNG DONG-SIK
IPC分类号： C07D413/04 , A61K31/506 , C07D413/14
摘要： Compounds of Formula (I) and methods for inhibiting kinases, including spleen tyrosine kinases, are disclosed. Also disclosed are methods for treating a kinase-mediated disease or condition by administering to a subject a therapeutically effective amount of the compound of Formula (I).

9. 发明专利

HK1226395A1 取代的嘧啶化合物及其作為SYK抑制劑的用途未知
公开(公告)号：HK1226395A1
公开(公告)日：2017-09-29
申请号：HK16114653
申请日：2016-12-23
申请人： GENOSCO , OSCOTEC INC
发明人： LEE JAEKYOO , CHOI JANG-SIK , HWANG HAE-JUN , SONG HO-JUHN , KIM JUNG-HO , KIM SE-WON , KOH JONG SUNG , LEE JAESANG , LEE TAE-IM , CHOI YUNG-GEUN , PARK SUNG-HO , LEE IN YONG , SUH BYUNG-CHUL , SALGAONKAR PARESH DEVIDAS , JUNG DONG-SIK
IPC分类号： C07D20060101 , A61K20060101

10. 发明专利

MY160820A KINASE INHIBITORS 未知
公开(公告)号：MY160820A
公开(公告)日：2017-03-31
申请号：MYPI2012002078
申请日：2010-11-12
申请人： GENOSCO , OSCOTEC INC
发明人： LEE JAEKYOO , KIM JUNG-HO , KIM SE-WON , SONG HO-JUHN , KOH JONG SUNG , LEE HEE KYU , KIM YOUNGSAM , KIM HONG WOO , CHANG SUNHWA , LIM SUN-HEE , CHOI JANG-SIK
IPC分类号： A61K31/33 , A61K31/505 , A61K31/535 , A61K31/55 , C07D243/08 , C07D403/04 , C07D413/06
摘要： THE PRESENT INVENTION PROVIDES A NEW GROUP OF PROTEIN KINASE INHIBITORS, PYRROPYRIMIDINE AND PYRAZOLOPYRIMIDINE DERIVATIVES, AND PHARMACEUTICALLY ACCEPTABLE SALTS AND PRODRUGS THEREOF THAT ARE USEFUL FOR TREATING 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 PYRROPYRIMIDINE AND PYRAZOLOPYRIMIDINE DERIVATIVES.

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