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1. 发明申请

WO2008007210A2 NITROGENOUS N-SUBSTITUTED 4-SPIRO-HETEROCYCLIC 2, 2 -DIMETHYLCHROMANE DERIVATIVES 审中-公开
标题翻译： N-取代的4-取代的4-甲氧基-2-二甲基喹啉衍生物
公开(公告)号：WO2008007210A2
公开(公告)日：2008-01-17
申请号：PCT/IB2007/001957
申请日：2007-07-11
申请人： UNIVERSITA' DI PISA , BALSAMO, Aldo , CALDERONE, Vincenzo , RAPPOSELLI, Simona
发明人： BALSAMO, Aldo , CALDERONE, Vincenzo , RAPPOSELLI, Simona
IPC分类号： C07D498/10 , A61K31/537 , A61P9/14
CPC分类号： C07D498/10
摘要： A compound having the following general formula:(I) wherein - * represents a chiral center; - R0 is selected from the group comprised of : a carbonyl or thiocarbonyl group, an alkyl group (methylene, ethylene, or methylcarbonyl or methyl-thiocarbonyl group; - Y is selected from the group comprised of: a CH2 group, a C=O group, a C=S group, a C=NH group; - A is selected from the group comprised of: a -CONH- group, a - COO- group, a -CO- group, an alkyl group (C1-C3), alkylcarbonyl group, a carbonyl group, a thiocarbonyl group, an alkylthiocarbonyl group, a sulphonic group, an alkylsulphonic group; - R1 is selected from the group comprised of: a hydrogen atom, an alkyl group, (methyl, ethyl, propyl, isopropyl, butyl, iso-butyl or tert-butyl, an alkoxy group (methoxy, ethoxy, n-propyloxy, iso-propyloxy), an halide atom (F, Cl, Br, I), a trifluoromethyl group, a cyanide group, a nitro group, a hydroxy group, an amine group, an alkylamine group, an alkylamide (acetamide, trifluoroacetamide, propionamide) or alkylsulphonamide (methanesulphonamide, ethanesulphonamide) group. - -R2 is selected from the group comprised of: a hydrogen atom, an alkyl group with C1-C4 carbon atoms (methyl, ethyl, propyl, isopropyl, butyl, isobutyl or terbutyl), a carboxyl group, an alkoxy group (methoxy, ethoxy, n-propyloxy, iso-propyloxy), an halide atom (F, Cl, Br, I), a cyanide group, a nitro group, a trifluoromethyl group, a hydroxy group, a thioalkyl group (C1, C2, C3); an amine group of NR3R4 type where R3 and R4 can be indifferently a hydrogen atom, an alkyl, alkylsulphonic (methanesulphonic, ethanesulphonic), acyl (acetyl, propionyl), trifluoroalkyl group.
摘要翻译：具有以下通式的化合物：（I）其中 - *表示手性中心; - R 0选自羰基或硫代羰基，烷基（亚甲基，亚乙基或甲基羰基或甲基 - 硫代羰基）; -Y选自：CH 2基，C = O 基团，C = S基团，C = NH基团; -A选自-CONH-基团，-OCO-基团，-CO-基团，烷基（C1-C3），烷基羰基，羰基，硫代羰基，烷硫基羰基，磺酸基，烷基磺酸基; -R1选自氢原子，烷基，（甲基，乙基，丙基，异丙基），丁基，异丁基或叔丁基，烷氧基（甲氧基，乙氧基，正丙氧基，异丙氧基），卤素原子（F，Cl，Br，I），三氟甲基，氰基，硝基，羟基，胺基，烷基胺基，烷基酰胺（乙酰胺，三氟乙酰胺，丙酰胺）或烷基磺酰胺（甲磺酰胺，乙磺酰胺）基团-R 2 i （甲基，乙基，丙基，异丙基，丁基，异丁基或叔丁基）的羧基，烷氧基（甲氧基，乙氧基，n 丙氧基，异丙氧基），卤素原子（F，Cl，Br，I），氰化物基，硝基，三氟甲基，羟基，硫代烷基（C1，C2，C3）其中R 3和R 4可以是氢原子，烷基，烷基磺酸（甲磺酸，乙磺酸），酰基（乙酰基，丙酰基），三氟烷基的NR 3 R 4型胺基。

2. 发明申请

WO2023001942A1 14-3-3 PROTEIN MODULATORS AS ANTITUMOR AGENTS 审中-公开
公开(公告)号：WO2023001942A1
公开(公告)日：2023-01-26
申请号：PCT/EP2022/070443
申请日：2022-07-21
申请人： RAPPOSELLI, Simona , GAUDIO, Eugenio , DAL PIAZ, Fabrizio
发明人： RAPPOSELLI, Simona , GAUDIO, Eugenio , DAL PIAZ, Fabrizio
IPC分类号： A61K31/404 , A61K31/4155 , A61K31/4178 , A61P35/00 , A61P35/02
摘要： The invention relates to a 2-oxoindole compound of Formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are, independently from each other, hydrogen,1H-imidazolyl, thienyl and 1-methyl-1H-imidazolyl, 2-methyl-1H-imidazolyl,2-aminopyridinyl, 1H-pyrazolyl, with the proviso that one of R1 and R2 is hydrogen; or R1 and R2 together form 9H-fluorene R3 is hydrogen, (C1-C3)alkyl, halogen or NO2; for use as a 14-3-3 protein modulator of a tumor selected from the group consisting of a lymphoma, chronic lymphocytic leukaemia (CLL), Ewing sarcoma, colon cancer, melanoma and anaplastic thyroid cancer (ATC). The invention relates also new 2-oxoindole compound of Formula (I) or a pharmaceutically acceptable salt thereof..

3. 发明公开

EP4373488A1 14-3-3 PROTEIN MODULATORS AS ANTITUMOR AGENTS 审中-实审
公开(公告)号：EP4373488A1
公开(公告)日：2024-05-29
申请号：EP22753691.9
申请日：2022-07-21
申请人： Rapposelli, Simona , Gaudio, Eugenio , Dal Piaz, Fabrizio
发明人： Rapposelli, Simona , Gaudio, Eugenio , Dal Piaz, Fabrizio
IPC分类号： A61K31/404 , A61K31/4155 , A61K31/4178 , A61P35/00 , A61P35/02
CPC分类号： A61P35/02 , A61P35/00 , A61K31/4155 , A61K31/4178 , A61K31/404

4. 发明申请

WO2008017925A3 PHARMACODYNAMIC HYBRIDS ENDOWED OF HYPOGLYCEMIC AND NO-DONOR ACTIVITIES OBTAINED COMBINING HYDROXYLATED DERIVATIVES OF GLIBENCLAMIDE AND NITROOXY-SUBSTITUTED CARBOXYLIC ACIDS 审中-公开
标题翻译：获得的低血糖和无供体活性的药物动力学混合物，其与羟基环酰胺和硝基取代的羧酸的羟基衍生物
公开(公告)号：WO2008017925A3
公开(公告)日：2008-11-06
申请号：PCT/IB2007002259
申请日：2007-08-06
申请人： UNIV PISA , BALSAMO ALDO , CALDERONE VINCENZO , RAPPOSELLI SIMONA , MARCHETTI PIERO , TORRI SCILLA
发明人： BALSAMO ALDO , CALDERONE VINCENZO , RAPPOSELLI SIMONA , MARCHETTI PIERO , TORRI SCILLA
IPC分类号： C07C311/59 , A61K31/64 , A61P3/10
CPC分类号： C07C311/59
摘要： Compound featuring a hypoglycemic action and in the meantime a release of nitric oxide (NO), said compound having the following general formula (I) : where at least one among R, R1, and R2 is a substitute comprising an nitroxy-ester group bound to a acyl aliphatic, aromatic or aliphatic-aromatic group. The compound can be in particular, used to treat patients affected by NO endogenous deficit responsive to diabetes mellitus of type 2.
摘要翻译：具有降血糖作用并同时释放一氧化氮（NO）的化合物，所述化合物具有以下通式（I）：其中R，R1和R2中的至少一个是包含硝酰氧基酯基团结合的取代基到酰基脂族，芳族或脂族 - 芳族基团。该化合物可以特别用于治疗受2型糖尿病反应的NO内源性缺陷影响的患者。

5. 发明申请

WO2008007210A3 NITROGENOUS N-SUBSTITUTED 4-SPIRO-HETEROCYCLIC 2, 2 -DIMETHYLCHROMANE DERIVATIVES 审中-公开
标题翻译： N取代的N-取代的4-螺环 - 杂环2,2-二甲基衍生物
公开(公告)号：WO2008007210A3
公开(公告)日：2008-08-14
申请号：PCT/IB2007001957
申请日：2007-07-11
申请人： UNIV PISA , BALSAMO ALDO , CALDERONE VINCENZO , RAPPOSELLI SIMONA
发明人： BALSAMO ALDO , CALDERONE VINCENZO , RAPPOSELLI SIMONA
IPC分类号： C07D498/10 , A61K31/537 , A61P9/14
CPC分类号： C07D498/10
摘要： Compounds having the following general formula : wherein R 0 , R 1 , R 2 , A and Y are as defined in the specification. The compounds can be used for therapeutic or prophylactic treatments of biological tissues of anatomical parts, such as heart, the pancreatic beta cells, the smooth muscle, the kidney and the central nervous system, involved with ischemic episodes.
摘要翻译：具有以下通式的化合物：其中R 0，R 1，R 2，A和Y如说明书中所定义。该化合物可用于治疗或预防性处理与缺血发作有关的解剖部位如心脏，胰腺β细胞，平滑肌，肾脏和中枢神经系统的生物组织。

6. 发明申请

WO2008017925A2 PHARMACODYNAMIC HYBRIDS ENDOWED OF HYPOGLYCEMIC AND NO-DONOR ACTIVITIES OBTAINED COMBINING HYDROXYLATED DERIVATIVES OF GLIBENCLAMIDE AND NITROOXY-SUBSTITUTED CARBOXYLIC ACIDS 审中-公开
标题翻译：获得结合羟苯甲酰胺和硝基取代的羧酸的羟化衍生物的高分子化合物和非离子活性的药物动力学杂交
公开(公告)号：WO2008017925A2
公开(公告)日：2008-02-14
申请号：PCT/IB2007/002259
申请日：2007-08-06
申请人： UNIVERSITA' DI PISA , BALSAMO, Aldo , CALDERONE, Vincenzo , RAPPOSELLI, Simona , MARCHETTI, Piero , TORRI, Scilla
发明人： BALSAMO, Aldo , CALDERONE, Vincenzo , RAPPOSELLI, Simona , MARCHETTI, Piero , TORRI, Scilla
IPC分类号： C07C311/59 , A61K31/64
CPC分类号： C07C311/59
摘要： Compound featuring a hypoglycemic action and in the meantime a release of nitric oxide (NO), said compound having the following general formula (I) : where at least one among R, R1, and R2 is a substitute comprising an nitroxy-ester group bound to a acyl aliphatic, aromatic or aliphatic-aromatic group. The compound can be in particular, used to treat patients affected by NO endogenous deficit responsive to diabetes mellitus of type 2.
摘要翻译：具有降血糖作用并且同时释放一氧化氮（NO）的化合物的化合物，所述化合物具有以下通式（I）：其中R，R 1和R 2中的至少一个是包含硝基 - 酯基团的取代基酰基脂族，芳族或脂族 - 芳族基团。该化合物特别可用于治疗受2型糖尿病反应的NO内源性缺陷影响的患者。

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