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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

WO2011053861A8 KINASE INHIBITORS 审中-公开
标题翻译：激酶抑制剂
公开(公告)号：WO2011053861A8
公开(公告)日：2011-10-27
申请号：PCT/US2010054853
申请日：2010-10-29
申请人： GENOSCO , OSCOTEC INC , KIM HONG WOO , KOH JONG SUNG , LEE JAEKYOO , SONG HO-JUHN , KIM YOUNGSAM , LEE HEE KYU , CHOI JANG-SIK , LIM SUN-HEE , CHANG SUNHWA
发明人： KIM HONG WOO , KOH JONG SUNG , LEE JAEKYOO , SONG HO-JUHN , KIM YOUNGSAM , LEE HEE KYU , CHOI JANG-SIK , LIM SUN-HEE , CHANG SUNHWA
IPC分类号： A01N43/90 , A61K31/519
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，心血管疾病和神经退行性疾病和病症。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吡啶并[4,3，-d]嘧啶-5-酮衍生物期间产生的有用中间体。

3. 发明专利

CA2779105C KINASE INHIBITORS 未知
公开(公告)号：CA2779105C
公开(公告)日：2016-08-16
申请号：CA2779105
申请日：2010-10-29
申请人： GENOSCO , OSCOTEC INC
发明人： KIM HONG WOO , LEE JAEKYOO , SONG HO-JUHN , KIM YOUNGSAM , LEE HEE KYU , CHOI JANG-SIK , LIM SUN-HEE , CHANG SUNHWA , KOH JONG SUNG
IPC分类号： C07D471/04 , A61K31/519 , C07D519/00
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.

4. 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

5. 发明专利

SG10201407012XA KINASE INHIBITORS 未知
公开(公告)号：SG10201407012XA
公开(公告)日：2014-11-27
申请号：SG10201407012X
申请日：2010-10-29
申请人： GENOSCO , OSCOTEC INC
发明人： KIM HONG WOO , KOH JONG SUNG , LEE JAEKYOO , SONG HO-JUHN , KIM YOUNGSAM , LEE HEE KYU , CHOI JANG-SIK , LIM SUN-HEE , CHANG SUNHWA
IPC分类号： A01N43/90 , A61K31/519
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.

6. 发明专利

EA029273B1 КИНАЗНЫЕ ИНГИБИТОРЫ 未知
公开(公告)号：EA029273B1
公开(公告)日：2018-03-30
申请号：EA201290237
申请日：2010-10-29
申请人： GENOSCO , OSCOTEC INC
发明人： KIM HONG WOO , KOH JONG SUNG , LEE JAEKYOO , SONG HO-JUHN , KIM YOUNGSAM , LEE HEE KYU , CHOI JANG-SIK , LIM SUN-HEE , CHANG SUNHWA
IPC分类号： A01N43/90 , A61K31/519
摘要： Заявляетсяноваягруппапротеинкиназныхингибиторов, производныхпиридо[4,3-d]пиримидин-5-она, иихфармацевтическиприемлемыесолии пролекарства, которыеприменяютдлялеченияклеточныхпролиферативныхзаболеванийи расстройств, такихкакрак, аутоиммунныезаболевания, инфекции, сердечно-сосудистыезаболеванияи нейродегенеративныезаболеванияи расстройства, атакжеихприменениедлялечениямедиированногопротеинкиназойзаболевания. Вданномизобретениитакжезаявленыфармацевтическиекомпозиции, содержащиепоменьшеймереодносоединениеингибиторапротеинкиназывместес фармацевтическиприемлемымносителем, разбавителемилинаполнителем, атакжеихприменениедлялечениямедиированногопротеинкиназойзаболевания.

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

NZ630860A Bissubstituted pyrido[4,3-d]-pyrimindin-5-one kinase nhibitors and medical uses 未知
公开(公告)号：NZ630860A
公开(公告)日：2016-03-31
申请号：NZ63086010
申请日：2010-10-29
申请人： GENOSCO , OSCOTEC INC
发明人： CHOI JANG-SIK , SONG HO-JUHN , KIM HONG WOO , LIM SUN-HEE , KIM YOUNGSAM , LEE JAEKYOO , KOH JONG SUNG , CHANG SUNHWA , LEE HEE KYU
IPC分类号： A61K31/519 , A61K31/4375 , C07D471/04
摘要： Disclosed are bi-substituted -amino-pyrido[4,3-d]pyrimidine-5(6H)-one derivatives as represented by the general formula (I), wherein the variables are as defined in the specification. These compounds are suitable for treating neurodegenerative disease such as Parkinson’s disease or Alzheimer’s disease, and inflammatory disease selected from asthma, chronic obstructive pulmonary disease (COPD), adult respiratory distress syndrome (ARDs), ulcerative colitis, Crohn’s disease, bronchitis, dermatitis, allergic rhinitis, psorasis, scleroderma, urticaria, rheumatoid arthritis, multiple sclerosis, or cancer.

9. 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.

10. 发明专利

NZ599040A 2,4-disubstituted pyrido[4,3-d]pyrimidin-5(6h)-one compounds for selective inhibitors of lrrk2 and syk kinases 未知
公开(公告)号：NZ599040A
公开(公告)日：2014-11-28
申请号：NZ59904010
申请日：2010-10-29
申请人： GENOSCO , OSCOTEC INC
发明人： CHOI JANG-SIK , SONG HO-JUHN , KIM HONG WOO , LIM SUN-HEE , KIM YOUNGSAM , LEE JAEKYOO , KOH JONG SUNG , CHANG SUNHWA , LEE HEE KYU
IPC分类号： A61K31/519 , A61K31/4375 , C07D471/04
摘要： Disclosed are 2-(piperidin-1-yl)-4-amino-pyrido[4,3-d]pyrimidine-5(6H)-one and 2-(benzylamino)-4-amino-pyrido[4,3-d]pyrimidine-5(6H)-one derivatives as represented by the general formula (I), wherein: R1 is H; X is NR2R3 or NR4R5; Y is NHR6; Z is selected from H, halogen, alkyl, alkynyl, aryl, heteroaryl, or cycloalkyl, wherein the alkyl, cycloalkyl, aryl, alkynyl or heteroaryl is optionally substituted; R2 and R3, taken together with the nitrogen atom to which they are bonded form: i) a 3-8 membered saturated or partially unsaturated monocyclic group having no heteroatom other than the nitrogen atom to which R2 and R3 are bonded, wherein said 3-8 membered saturated or partially unsaturated monocyclic group is substituted at one or more carbon atoms with 1-2 R7; or ii) an 8-10 membered bicyclic aryl group having 0-5 heteroatoms independently selected from nitrogen, oxygen, sulfur, sulfoxide, or sulfone; R4 is selected from H, alkyl, or hydroxyalkyl; R5 is arylalkyl, wherein the aryl group is independently substituted at one or more carbon atoms with 1-3 R11; R11 is independently selected from OR9, NR9R9, NR9COR9, or NR9S(O)nR9; R6 is selected from alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, cycloalkenyl, aryl, arylalkyl, or heteroaryl, wherein the heterocycloalkyl, aryl, or heteroaryl is optionally substituted; and wherein the remaining substituents are as defined herein. Representative compounds include 2-(4-hydroxypiperidin-1-yl)-4-(3-(trifluoromethyl)phenylamino)pyrido[4,3-d] pyrimidine-5(6H)-one and 2-(4-hydroxy-4-(hydroxymethyl)piperidin-1-yl)-4-(4-methoxy-3-(trifluromethyl) phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one.

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