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1. 发明专利

CA2696021A1 MACROCYCLIC COMPOUNDS USEFUL AS INHIBITORS OF KINASES AND HSP90 未知
公开(公告)号：CA2696021A1
公开(公告)日：2008-02-21
申请号：CA2696021
申请日：2007-08-10
申请人： WINSSINGER NICOLAS , BARLUENGA SOFIA , KARPLUS MARTIN
发明人： WINSSINGER NICOLAS , BARLUENGA SOFIA , KARPLUS MARTIN
IPC分类号： A61K31/365 , C07D313/00 , C07D493/00
摘要： Disclosed are macrocyclic compounds of formulae I-V,which are analogs of the pochonin resorcylic acid lactones, and processes for the preparation of the compounds. The compounds disclosed are useful as inhibitors of kinases and Heat Shock Protein 90 (HSP 90). Also disclosed are pharmaceutical compositions comprising an effective kinase-inhibiting amount or an effective HSP90-inhibiting amount of the compounds and methods for the treatment of disorders that are mediated by kinases and HSP90.

2. 发明公开

EP2242359A4 SYNTHESIS OF RESORCYLIC ACID LACTONES USEFUL AS THERAPEUTIC AGENTS 有权
标题翻译：所产生的合成作为合适THERAPEUTICS二羟基苯甲酸内酯的
公开(公告)号：EP2242359A4
公开(公告)日：2011-11-09
申请号：EP09702521
申请日：2009-01-15
申请人： UNIV STRASBOURG , WINSSINGER NICOLAS , BARLUENGA SOFIA , KARPLUS MARTIN
发明人： WINSSINGER NICOLAS , BARLUENGA SOFIA , KARPLUS MARTIN
IPC分类号： A01N31/14 , A61K31/02 , C07D313/00 , C07D405/12 , C07D405/14
CPC分类号： C07D313/00 , A61K31/335 , A61K31/365 , A61K31/4025 , A61K31/435 , A61K31/4453 , A61K31/4523 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/541 , C07D211/14 , C07D225/06 , C07D405/12 , C07D405/14 , Y02P20/55

3. 发明专利

ES2587390T3 Síntesis de lactonas del ácido resorcílico útiles como agentes terapéuticos 未知
公开(公告)号：ES2587390T3
公开(公告)日：2016-10-24
申请号：ES09702521
申请日：2009-01-15
申请人： UNIV STRASBOURG , WINSSINGER NICOLAS , BARLUENGA SOFIA , KARPLUS MARTIN
发明人： WINSSINGER NICOLAS , BARLUENGA SOFIA , KARPLUS MARTIN
IPC分类号： A01N31/14 , A61K31/02 , C07D313/00 , C07D405/12 , C07D405/14
摘要： Un compuesto de fórmula II o II', o un tautómero del mismo, una sal, solvato o éster farmacéuticamente aceptable del mismo:**Fórmula** en la que: X es O, S o NR; Y es -OR, -O-(CH2)mCOOR, -O-(CH2)mCON(R)2, -N(R)2, -N(R)SOR o -N(R)SO2R, en el que los grupos unidos al átomo de nitrógeno pueden estar en una configuración Z o E; R1 y R2 son independientemente hidrógeno o halógeno; R3, R4, R5, R6, R7, R8, R9 y R10 son independientemente hidrógeno, halógeno, azido, nitro, ciano, alifático, alquilarilo, aralquilo, arilo, heteroalquilo, alquilheteroarilo, heterociclilo, heteroarilo, OR, N(R)2, SR, -O(CH2)mN(R)C(O)(CH2)pR, -O(CH2)mOC(O)(CH2)pR, -O(CH2)mC(O)(CH2)pN(R)2, -O(CH2)mC(O)(CH2)pOR, -O(CH2)mN(R)C(O)(CH2)pOR, -O(CH2)mN(R)C(O)(CH2)pN(R)2, -O(CH2)mOC(O)(CH2)pOR, -O(CH2)mOC(O)(CH2)pN(R)2, -NR(CH2)mN(R)C(O)(CH2)pR, -NR(CH2)mOC(O)(CH2)pR, -NR(CH2)mC(O)(CH2)pN(R)2, -NR(CH2)mC(O)(CH2)pOR, -NR(CH2)mN(R)C(O)(CH2)pOR, -NR(CH2)mN(R)C(O)(CH2)pN(R)2, -NR(CH2)mOC(O)(CH2)pOR, -NR(CH2)mOC(O)(CH2)pN(R)2, -(CH2)mN(R)C(O)(CH2)pR, -(CH2)mOC(O)(CH2)pR, -(CH2)mC(O)(CH2)pN(R)2, -(CH2)mC(O)(CH2)pOR, -(CH2)mN(R)C(O)(CH2)pOR, -(CH2)mN(R)C(O)(CH2)pN(R)2, -(CH2)mOC(O)(CH2)pOR, -(CH2)mOC(O)(CH2)pN(R)2, -(CH2)mN3, -O(CH2)mN3-(CH2)mN(R)2, -(CH2)mOR, -(CH2)mS(O)(CH2)pR, -(CH2)mS(O)2(CH2)pR, -(CH2)mSO2(CH2)pN(R)2 o -(CH2)mN(R)SO2(CH2)pR; y cada R es independientemente R11, hidrógeno, alifático, amino, azido, ciano, nitro, alquilamino, dialquilamino, OH, alcoxi, carbonilamino, aminocarbonilo, alcoxicarbonilo, carboniloxi, carboxi, acilo, arilo, alcarilo, arilalquilo que incluye bencilo, heteroalquilo, heteroarilo, heterociclilo, o un grupo protector seleccionado entre un grupo que consiste en etoximetilo, metoximetilo, terc-butildimetil sililo (TBS), fenildimetilsililo, trimetilsililo (TMS), 2-trimetilsililetoximetilo (SEM), 2-trimetilsililetilo; y bencilo; o dos R en el mismo nitrógeno se toman junto con el nitrógeno para formar un anillo heterocíclico o heteroarilo de 5-8 miembros; en el que un grupo contiene más de un sustituyente R; en el que R está opcionalmente sustituido, y cada R puede ser igual o diferente; R11 es el grupo: donde Z es un contraión inorgánico u orgánico; m y p son independientemente 0, 1, 2, 3, 4 o 5; y en el que, en la fórmula II', cuando X es O, entonces al menos uno de R5, R6, R7, R8, R9 o R10 no es hidrógeno.

4. 发明专利

AU2009206097B2 Synthesis of resorcylic acid lactones useful as therapeutic agents 未知
公开(公告)号：AU2009206097B2
公开(公告)日：2014-08-14
申请号：AU2009206097
申请日：2009-01-15
申请人： BARLUENGA SOFIA , KARPLUS MARTIN , UNIV STRASBOURG , WINSSINGER NICOLAS
发明人： BARLUENGA SOFIA , WINSSINGER NICOLAS , KARPLUS MARTIN
IPC分类号： C07D313/00 , A01N31/14 , A61K31/02
摘要： Disclosed are macrocyclic compounds of formulae I, I', II, II', III, III', IV, and V, which are analogs of the pochonin resorcylic acid lactones, pharmaceutical compositions comprising the compounds, and methods and uses comprising the compounds for the treatment of diseases mediated by kinases and Heat Shock Protein 90 HSP90.

5. 发明申请

WO2008149244A3 COMPOSITIONS AND METHODS COMPRISING ANALOGUES OF RADICICOL A 审中-公开
标题翻译：包含RADICICOL A类似物的组合物和方法A
公开(公告)号：WO2008149244A3
公开(公告)日：2009-03-12
申请号：PCT/IB2008002497
申请日：2008-06-05
申请人： WINSSINGER NICOLAS , BARLUENGA SOFIA
发明人： WINSSINGER NICOLAS , BARLUENGA SOFIA
IPC分类号： C07D313/08 , A61K31/365 , A61K31/39 , A61P25/00 , A61P29/00 , A61P31/04 , A61P35/00 , C07D321/10 , C07D327/02
CPC分类号： C07D313/00 , C07D321/00 , C07D327/02
摘要： Disclosed are novel analogues of the natural product radicicol A of formulae I,.Ia, pi, Ha, lib and HI, pharmaceutical compositions comprising the compounds. The compounds of the invention are kinase and phosphatase inhibitors and find utility in the treatment or prevention of kinase and phosphatase -mediated disorders. Also provided are uses and methods for the treatment or prevention of kinase- and phosphatase -mediated disorders and synthetic processes for the preparation of the compounds.
摘要翻译：公开了式I，.Ia，pi，Ha，lib和HI的天然产物根赤虫胺A的新类似物，包含该化合物的药物组合物。本发明的化合物是激酶和磷酸酶抑制剂，可用于治疗或预防激酶和磷酸酶介导的病症。还提供了用于治疗或预防激酶和磷酸酶介导的病症的用途和方法以及用于制备化合物的合成方法。

6. 发明授权

EP2242359B1 SYNTHESIS OF RESORCYLIC ACID LACTONES USEFUL AS THERAPEUTIC AGENTS 有权
标题翻译：所产生的合成作为合适THERAPEUTICS二羟基苯甲酸内酯的
公开(公告)号：EP2242359B1
公开(公告)日：2016-06-01
申请号：EP09702521.7
申请日：2009-01-15
申请人： Université de Strasbourg , WINSSINGER, Nicolas , BARLUENGA, Sofia , KARPLUS, Martin
发明人： WINSSINGER, Nicolas , BARLUENGA, Sofia , KARPLUS, Martin
IPC分类号： A01N31/14 , A61K31/02 , C07D313/00 , C07D405/12 , C07D405/14
CPC分类号： C07D313/00 , A61K31/335 , A61K31/365 , A61K31/4025 , A61K31/435 , A61K31/4453 , A61K31/4523 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/541 , C07D211/14 , C07D225/06 , C07D405/12 , C07D405/14 , Y02P20/55

7. 发明公开

EP2242359A1 SYNTHESIS OF RESORCYLIC ACID LACTONES USEFUL AS THERAPEUTIC AGENTS 有权
标题翻译：所产生的合成作为合适THERAPEUTICS二羟基苯甲酸内酯的
公开(公告)号：EP2242359A1
公开(公告)日：2010-10-27
申请号：EP09702521.7
申请日：2009-01-15
申请人： Universite De Strasbourg , WINSSINGER, Nicolas , BARLUENGA, Sofia , KARPLUS, Martin
发明人： WINSSINGER, Nicolas , BARLUENGA, Sofia , KARPLUS, Martin
IPC分类号： A01N31/14 , A61K31/02
CPC分类号： C07D313/00 , A61K31/335 , A61K31/365 , A61K31/4025 , A61K31/435 , A61K31/4453 , A61K31/4523 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/541 , C07D211/14 , C07D225/06 , C07D405/12 , C07D405/14 , Y02P20/55
摘要： Disclosed are macrocyclic compounds of formulae I, I', II, II', III, III', IV, and V, which are analogs of the pochonin resorcylic acid lactones, pharmaceutical compositions comprising the compounds, and methods and uses comprising the compounds for the treatment of diseases mediated by kinases and Heat Shock Protein 90 HSP90.

8. 发明公开

EP2173733A2 COMPOSITIONS AND METHODS COMPRISING ANALOGUES OF RADICICOL A 审中-公开
标题翻译：组合物和方法，用起根赤壳模拟
公开(公告)号：EP2173733A2
公开(公告)日：2010-04-14
申请号：EP08807156.8
申请日：2008-06-05
申请人： WINSSINGER, Nicolas , BARLUENGA, Sofia
发明人： WINSSINGER, Nicolas , BARLUENGA, Sofia
IPC分类号： C07D313/08 , C07D321/10 , C07D327/02 , A61K31/365 , A61K31/39 , A61P25/00 , A61P29/00 , A61P31/04 , A61P35/00
CPC分类号： C07D313/00 , C07D321/00 , C07D327/02
摘要： Disclosed are novel analogues of the natural product radicicol A of formulae I,.Ia, pi, Ha, lib and HI, pharmaceutical compositions comprising the compounds. The compounds of the invention are kinase and phosphatase inhibitors and find utility in the treatment or prevention of kinase and phosphatase -mediated disorders. Also provided are uses and methods for the treatment or prevention of kinase- and phosphatase -mediated disorders and synthetic processes for the preparation of the compounds.

9. 发明专利

BRPI0905687A8 composto da fórmula i ou i', composição farmacêutica, método de tratamento de um paciente com uma doença, uso do composto 未知
公开(公告)号：BRPI0905687A8
公开(公告)日：2019-05-21
申请号：BRPI0905687
申请日：2009-01-15
申请人： BARLUENGA SOFIA , KARPLUS MARTIN , MARTIN KARPLUS , NICOLAS WINSSINGER , SOFIA BARLUENGA , UNIV STRASBOURG , WINSSINGER NICOLAS
发明人： BARLUENGA SOFIA , KARPLUS MARTIN , WINSSINGER NICOLAS
IPC分类号： A61K31/02 , A01N31/14
摘要： "composto da fórmula i ou i', composição farmacêutica, método de tratamento de um paciente com uma doença, uso do composto", trata-se a presente invenção de compostos macrociclos das fórmulas i, 1', 11, 11', 111, 111', iv e v', que são análogos das lactonas do ácido resorcílico, como, por exemplo, porchonina, e composições farmacêuticas compreendendo os compostos para o tratamento de doenças mediadas por quinase e proteína de choque térmico 90 (hsp90).

10. 发明专利

CA2696021C MACROCYCLIC COMPOUNDS USEFUL AS INHIBITORS OF KINASES AND HSP90 未知
公开(公告)号：CA2696021C
公开(公告)日：2015-09-29
申请号：CA2696021
申请日：2007-08-10
申请人： WINSSINGER NICOLAS , BARLUENGA SOFIA , KARPLUS MARTIN
发明人： WINSSINGER NICOLAS , BARLUENGA SOFIA , KARPLUS MARTIN
IPC分类号： C07D313/00 , A61K31/365 , A61K31/4427 , C07D407/10 , C07D493/04
摘要： Disclosed are macrocyclic compounds of formulae l-V, which are analogs of the pochonin resorcylic acid lactones, and processes for the preparation of the compounds. The compounds disclosed are useful as inhibitors of kinases and Heat Shock Protein 90 (HSP 90). Also disclosed are pharmaceutical compositions comprising an effective kinase-inhibiting amount or an effective HSP90-inhibiting amount of the compounds and methods for the treatment of disorders that are mediated by kinases and HSP90. (see formula I)

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