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32 条记录 (耗时 0.056 秒)

    Bis-platinum complexes with antitumor activity
    23.
    发明授权
    Bis-platinum complexes with antitumor activity 有权
    具有抗肿瘤活性的双铂配合物

    公开(公告)号：US08426625B2

    公开(公告)日：2013-04-23

    申请号：US12086547

    申请日：2006-12-21

    申请人： Alberto Bernareggi ,  Mario Grugni ,  Giulio Mariotti ,  Ernesto Menta ,  Gianluca Pardi ,  Paolo Pavesi ,  Gabriella Pezzoni ,  Paolo Nicoli ,  Sergio De Munari

    发明人： Alberto Bernareggi ,  Mario Grugni ,  Giulio Mariotti ,  Ernesto Menta ,  Gianluca Pardi ,  Paolo Pavesi ,  Gabriella Pezzoni ,  Paolo Nicoli ,  Sergio De Munari

    IPC分类号： C07F15/00 ,  A61K31/28

    CPC分类号： C07F15/0093

    摘要： A compound of general formula (I): in which: R is selected from the group consisting of (C1-C25)alkyl, (C2-C25)alkenyl, aryl, (C7-C10)aralkyl; n and m are each independently an integer of two to eight; p is one or two; A is selected from the group consisting of —B—, —B—(CH2)r—B—, —B—(CH2)r—B—(CH2)z—B—, wherein r and z are an integer from 2 to 8, B is a —NR1— or —N(R2)2+1/pQ−p group, in which R1 is selected from hydrogen, (C1-C4)alkyl, (C1-C4)acyl, tert-butoxycarbonyl, and R2 is selected from hydrogen and (C1-C4)alkyl; Q−p is an anion selected from chloride, bromide, iodide, nitrate, sulphate, hydrogen sulphate, perchlorate, R3COO− wherein R3 has the same meanings as R, independently from one another and R4—O—SO3− wherein R4 is (C2-C14)alkyl with the proviso that, when Q−p is selected from chloride, bromide, iodide, nitrate, sulphate, hydrogen sulphate, perchlorate, R is not (C1-C4)alkyl.

    摘要翻译： 通式（I）的化合物：其中：R选自（C 1 -C 25）烷基，（C 2 -C 25）烯基，芳基，（C 7 -C 10）芳烷基; n和m各自独立地为2至8的整数; p是一两个; A选自-B-，-B-（CH2）rB-，-B-（CH2）rB-（CH2）zB-，其中r和z是2至8的整数，B是 -NR 1 - 或-N（R 2）2 + 1 / pQ-p基团，其中R 1选自氢，（C 1 -C 4）烷基，（C 1 -C 4）酰基，叔丁氧基羰基和R 2选自氢 和（C 1 -C 4）烷基; Qp是选自氯化物，溴化物，碘化物，硝酸盐，硫酸盐，硫酸氢盐，高氯酸盐，R 3 COO-中的一种阴离子，其中R 3具有与R相同的含义，R 4 -O-SO 3 - 其中R 4是（C 2 -C 14 ）烷基，条件是当Qp选自氯化物，溴化物，碘化物，硝酸盐，硫酸盐，硫酸氢盐，高氯酸盐时，R不是（C 1 -C 4）烷基。

    PROCESS FOR THE PREPARATION OF POLY-alpha-GLUTAMIC ACID AND DERIVATIVES THEREOF
    24.
    发明申请
    PROCESS FOR THE PREPARATION OF POLY-alpha-GLUTAMIC ACID AND DERIVATIVES THEREOF 有权
    制备聚α-谷氨酸及其衍生物的方法

    公开(公告)号：US20110196123A1

    公开(公告)日：2011-08-11

    申请号：US12965510

    申请日：2010-12-10

    申请人： Marc McKENNON ,  Giovanni Da Re ,  Luca Feliciotti ,  Marco Artico ,  Gianluca Pardi ,  Mario Grugni

    发明人： Marc McKENNON ,  Giovanni Da Re ,  Luca Feliciotti ,  Marco Artico ,  Gianluca Pardi ,  Mario Grugni

    IPC分类号： C08G69/10

    CPC分类号： C07K14/001 ,  C08G69/10

    摘要： The invention relates to an improved process for the preparation of poly-α-glutamic acids which comprises the polymerization of tertiary γ-esters of α-glutamic acid N-carboxy anhydride with appropriate solvents and initiators, followed by acid hydrolysis of the resulting poly-α-glutamic acid-γ-ester. The process is particularly advantageous in that it allows one to carefully control the molecular weight of the resulting poly-α-glutamic acid. The invention also relates to poly-α-glutamic acids capped at the amino terminus with carboxylic acids or amino acids and to a process for the preparation thereof.

    摘要翻译： 本发明涉及一种制备聚-α-谷氨酸的改进方法，其包括用适当的溶剂和引发剂将α-谷氨酸N-羧酸酐的叔γ-酯聚合，然后酸化所得的聚 - α-谷氨酸-γ-酯。 该方法特别有利的是，它允许仔细控制所得聚-α-谷氨酸的分子量。 本发明还涉及在氨基末端被羧酸或氨基酸封端的聚-α-谷氨酸及其制备方法。

    Process for the preparation of poly-alpha-glutamic acid and derivatives thereof
    25.
    发明申请
    Process for the preparation of poly-alpha-glutamic acid and derivatives thereof 审中-公开
    制备聚-α-谷氨酸及其衍生物的方法

    公开(公告)号：US20080051603A1

    公开(公告)日：2008-02-28

    申请号：US11818056

    申请日：2007-06-12

    申请人： Marc McKennon ,  Giovanni Da Re ,  Luca Feliciotti ,  Marco Artico ,  Gianluca Pardi ,  Mario Grugni

    发明人： Marc McKennon ,  Giovanni Da Re ,  Luca Feliciotti ,  Marco Artico ,  Gianluca Pardi ,  Mario Grugni

    IPC分类号： C07C269/00

    CPC分类号： C07K14/001 ,  C08G69/10

    摘要： The invention relates to an improved process for the preparation of poly-α-glutamic acids which comprises the polymerization of tertiary γ-esters of α-glutamic acid N-carboxy anhydride with appropriate solvents and initiators, followed by acid hydrolysis of the resulting poly-α-glutamic acid-γ-ester. The process is particularly advantageous in that it allows one to carefully control the molecular weight of the resulting poly-α-glutamic acid. The invention also relates to poly-α-glutamic acids capped at the amino terminus with carboxylic acids or amino acids and to a process for the preparation thereof.

    摘要翻译： 本发明涉及一种改进的制备聚-α-谷氨酸的方法，其包括用适当的溶剂和引发剂聚合α-谷氨酸N-羧酸酐的叔γ-酯，然后酸化所得的聚 - α-谷氨酸-γ-酯。 该方法特别有利的是，其允许仔细控制所得聚-α-谷氨酸的分子量。 本发明还涉及在氨基末端被羧酸或氨基酸封端的聚-α-谷氨酸及其制备方法。

    Process for the preparation of poly-α-glutamic acid and derivatives thereof
    26.
    发明授权
    Process for the preparation of poly-α-glutamic acid and derivatives thereof 有权
    聚-α-谷氨酸及其衍生物的制备方法

    公开(公告)号：US08329853B2

    公开(公告)日：2012-12-11

    申请号：US12965510

    申请日：2010-12-10

    申请人： Marc McKennon ,  Giovanni Da Re ,  Luca Feliciotti ,  Marco Artico ,  Gianluca Pardi ,  Mario Grugni

    发明人： Marc McKennon ,  Giovanni Da Re ,  Luca Feliciotti ,  Marco Artico ,  Gianluca Pardi ,  Mario Grugni

    IPC分类号： C08G69/10

    CPC分类号： C07K14/001 ,  C08G69/10

    摘要： The invention relates to an improved process for the preparation of poly-α-glutamic acids which comprises the polymerization of tertiary γ-esters of α-glutamic acid N-carboxy anhydride with appropriate solvents and initiators, followed by acid hydrolysis of the resulting poly-α-glutamic acid-γ-ester. The process is particularly advantageous in that it allows one to carefully control the molecular weight of the resulting poly-α-glutamic acid. The invention also relates to poly-α-glutamic acids capped at the amino terminus with carboxylic acids or amino acids and to a process for the preparation thereof.

    摘要翻译： 本发明涉及一种制备聚-α-谷氨酸的改进方法，其包括用适当的溶剂和引发剂将α-谷氨酸N-羧酸酐的叔γ-酯聚合，然后酸化所得的聚 - α-谷氨酸-γ-酯。 该方法特别有利的是，它允许仔细控制所得聚-α-谷氨酸的分子量。 本发明还涉及在氨基末端被羧酸或氨基酸封端的聚-α-谷氨酸及其制备方法。

    Bis-Platinum Complexes With Antitumor Activity
    28.
    发明申请
    Bis-Platinum Complexes With Antitumor Activity 有权
    具有抗肿瘤活性的双铂配合物

    公开(公告)号：US20100292322A1

    公开(公告)日：2010-11-18

    申请号：US12086547

    申请日：2006-12-21

    申请人： Alberto Bernareggi ,  Mario Grugni ,  Giulio Mariotti ,  Ernesto Menta ,  Gianluca Pardi ,  Paolo Pavesi ,  Gabriella Pezzoni ,  Paolo Nicoli ,  Sergio De Munari

    发明人： Alberto Bernareggi ,  Mario Grugni ,  Giulio Mariotti ,  Ernesto Menta ,  Gianluca Pardi ,  Paolo Pavesi ,  Gabriella Pezzoni ,  Paolo Nicoli ,  Sergio De Munari

    IPC分类号： A61K31/28 ,  C07F15/00 ,  A61P35/00

    CPC分类号： C07F15/0093

    摘要： A compound of general formula (I): in which: R is selected from the group consisting of (C1-C25)alkyl, (C2-C25)alkenyl, aryl, (C7-C10)aralkyl; n and m are each independently an integer of two to eight; p is one or two; A is selected from the group consisting of —B—, —B—(CH2)r—B—, —B—(CH2)r—B—(CH2)z—B—, wherein r and z are an integer from 2 to 8, B is a —NR1— or —N(R2)2+ 1/pQ−p group, in which R1 is selected from hydrogen, (C1-C4)alkyl, (C1-C4)acyl, tert-butoxycarbonyl, and R2 is selected from hydrogen and (C1-C4)alkyl; Q−p is an anion selected from chloride, bromide, iodide, nitrate, sulphate, hydrogen sulphate, perchlorate, R3COO− wherein R3 has the same meanings as R, independently from one another and R4—O—SO3− wherein R4 is (C2-C14)alkyl with the proviso that, when Q−p is selected from chloride, bromide, iodide, nitrate, sulphate, hydrogen sulphate, perchlorate, R is not (C1-C4)alkyl.

    摘要翻译： 通式（I）的化合物：其中：R选自（C 1 -C 25）烷基，（C 2 -C 25）烯基，芳基，（C 7 -C 10）芳烷基; n和m各自独立地为2至8的整数; p是一两个; A选自-B-，-B-（CH2）r-B-，-B-（CH2）r-B-（CH2）z-B-，其中r和z是2的整数 至（C 1 -C 4）烷基，（C 1 -C 4）酰基，叔丁氧基羰基，C 1 -C 4烷基， 并且R 2选自氢和（C 1 -C 4）烷基; Q-p是选自氯化物，溴化物，碘化物，硝酸盐，硫酸盐，硫酸氢盐，高氯酸盐，R3COO-中的一种阴离子，其中R3具有与R相同的含义，R4-O-SO3-，其中R4是（C2 -C 14）烷基，条件是当Q-p选自氯化物，溴化物，碘化物，硝酸盐，硫酸盐，硫酸氢盐，高氯酸盐时，R不是（C 1 -C 4）烷基。

    Quinoline-4-carboxamide as NK-2 and NK-3 receptor antagonists
    30.
    发明申请
    Quinoline-4-carboxamide as NK-2 and NK-3 receptor antagonists 审中-公开

    公开(公告)号：US20060205735A1

    公开(公告)日：2006-09-14

    申请号：US11418274

    申请日：2006-05-04

    申请人： Giuseppe Maria Glardina ,  Mario Grugni ,  Davide Graziani ,  Luca Raveglia

    发明人： Giuseppe Maria Glardina ,  Mario Grugni ,  Davide Graziani ,  Luca Raveglia

    IPC分类号： A61K31/496 ,  A61K31/4709 ,  C07D403/02 ,  C07D401/02

    CPC分类号： C07D401/06 ,  C07D215/50 ,  C07D215/52 ,  C07D251/52 ,  C07D491/10 ,  C07D491/113

    摘要： A compound, or a solvate or a salt thereof, of formula (I): wherein, Ar is an optionally substituted aryl or a C5-7 cycloalkdienyl group, or a C5-7 cycloalkyl group or an optionally substituted single or fused ring aromatic heterocyclic group; R is C1-6 alkyl, C3-7 cycloalkyl, C3-7 cycloalkylalkyl, optionally substituted phenyl or phenyl C1-6 alkyl, an optionally substituted five-membered heteroaromatic ring comprising up to four heteroatoms selected from O and N, hydroxy C1-6 alkyl, amino C1-6 alkyl, C1-6 alkylaminoalkyl, di C1-6 alkylaminoalkyl, C1-6 acylaminoalkyl, C1-6 alkoxyalkyl, C1-6 alkylcarbonyl, carboxy, C1-6 alkoxycarbonyl, C1-6 alkoxycarbonyl C1-6 alkyl, aminocarbonyl, C1-6 alkylaminocarbonyl, di C1-6 alkylaminocarbonyl, halogeno C1-6 alkyl; or R is a group —(CH2)p— wherein p is 2 or 3 which group forms a ring with a carbon atom of Ar; R1 represents hydrogen or up to four optional substituents selected from the list consisting of: C1-6 alkyl, C1-6 alkenyl, aryl, C1-6 alkoxy, hydroxy, halogen, nitro, cyano, carboxy, carboxamido, sulphonamido, C1-6 alkoxycarbonyl, trifluoromethyl, acyloxy, phthalimido, amino or mono- and di-C1-6 alkylamino; R2 represents a moiety —(CH2)n—NY1Y2 wherein n is an integer in the range of from 1 to 9, Y1 and Y2 are independently selected from hydrogen; C1-6-alkyl; C1-6 alkyl substituted with hydroxy, C1-6 alkylamino or bis (C1-6 alkyl) amino; C1-6-alkenyl; aryl or aryl-C1-6-alkyl or Y1 and Y2 together with the nitrogen atom to which they are attached represent an optionally substituted N-linked single or fused ring heterocyclic group; R3 is branched or linear C1-6 alkyl, C3-7 cycloalkyl, C4-7 cycloalkylalkyl, optionally substituted aryl, or an optionally substituted single or fused ring aromatic heterocyclic group; and R4 represents hydrogen or C1-6 alkyl; a pharmaceutical composition comprising such a compound, process for preparing such a compound and the use of such a compound in medicine.