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    Cyclic dinucleoside diphosphorothioates, related compounds and pharmaceutical compositions
    1.
    发明授权
    Cyclic dinucleoside diphosphorothioates, related compounds and pharmaceutical compositions 失效
    环状二核苷二磷酸硫酸酯，相关化合物和药物组合物

    公开(公告)号：US5547941A

    公开(公告)日：1996-08-20

    申请号：US354888

    申请日：1994-12-09

    申请人： Carlo Battistini ,  Silvia Fustinoni ,  Maria G. Brasca ,  Domenico Ungheri

    发明人： Carlo Battistini ,  Silvia Fustinoni ,  Maria G. Brasca ,  Domenico Ungheri

    IPC分类号： A61K31/70 ,  A61P31/12 ,  A61P31/18 ,  C07H19/10 ,  C07H19/20 ,  C07H21/00 ,  C07H21/04 ,  C07H19/213 ,  C07H21/02

    CPC分类号： C07H19/10 ,  C07H19/20

    摘要： There are provided compounds of formula (I) ##STR1## wherein each group B is, independently, a naturally occurring or modified heterocyclic base linked through a nitrogen or a carbon atom of the ring to the sugar moiety;each group X is a, independently, hydrogen, fluorine, hydroxy, or a C.sub.1 -C.sub.6 alkoxy group;each group Y is, independently, hydrogen, sulphidryl or hydroxy; and the pharmaceutically acceptable salts thereof.A process for their preparation and pharmaceutical compositions comprising them are also described. The compounds of this invention can be useful as antivirals, particularly as anti-HIV (Human Immunodeficiency Virus) agents, namely as drugs to be used against AIDS (Acquired Immunodeficiency Syndrome) therapeutically and/or prophylatically.

    摘要翻译： 提供式（I）化合物（I）其中每个基团B独立地是通过环的氮或碳原子与糖部分连接的天然存在或修饰的杂环碱基; 每个基团X独立地是氢，氟，羟基或C 1 -C 6烷氧基; 每个基团Y独立地是氢，硫代或羟基; 及其药学上可接受的盐。 还描述了其制备方法和包含它们的药物组合物。 本发明的化合物可用作抗病毒剂，特别是作为抗HIV（人类免疫缺陷病毒）试剂，即用于治疗和/或预防用于抗艾滋病（获得性免疫缺陷综合征）的药物）。

    Paromomycin containing compounds and method of use
    4.
    发明授权
    Paromomycin containing compounds and method of use 失效
    含有溴霉素的化合物及其使用方法

    公开(公告)号：US4337248A

    公开(公告)日：1982-06-29

    申请号：US156478

    申请日：1980-06-04

    申请人： Carlo Battistini ,  Giuseppe Cassinelli ,  Giovanni Franceschi ,  Rosanna Mazzoleni ,  Federico Arcamone

    发明人： Carlo Battistini ,  Giuseppe Cassinelli ,  Giovanni Franceschi ,  Rosanna Mazzoleni ,  Federico Arcamone

    IPC分类号： C07H5/06 ,  A61K31/70 ,  A61K31/702 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/7036 ,  A61P31/04 ,  C07H15/232 ,  A61K31/71 ,  C07H15/22

    CPC分类号： C07H15/232

    摘要： Compounds are disclosed of the formula ##STR1## wherein R.sub.1 represents a hydrogen or chlorine atom, as well as intermediates. These include 4'-deoxy-paromomycin; 4'-deoxy-4'-epi-chloro-paromomycin; 4'-deoxy-4'-epi-chloro-penta-N-benzyloxycarbonylparomomycin; 4'-deoxy-penta-N-benzyloxycarbonylparomomycin; 6,3',2",5",3"',4"'-hexa-O-acetyl-6'-O-benzoyl-4'-deoxy-penta-N-benzyloxycarbonylparomomycin; 6,3',2",5",3"',4"'-hexa-O-acetyl-6'-O-benzoyl-4'-epi-chloro-4'-deoxy-penta-N-benzyloxycarbonylparomomycin; 6,3',2",5",3"',4"'-hexa-O-acetyl-6'-O-benzyl-penta-N-benzyloxycarbonylparomomycin; 6,3',2",5",3"',4"'-hexa-O-acetyl-6'-O-benzoyl-4'-O-[(methylthio)-thiocarbonyl]-penta-N-benzyloxycarbonylparomomycin; and 6,3',2",5",3"',4"'-hexa-O-acetyl-6'-O-benzoyl-4'-O-[(phenylthio)-thiocarbonyl]-penta-N-benzyloxycarbonylparomomycin. The compounds illustrated by the structural formula are useful in treating amoebic dysentery in man and animals.

    摘要翻译： 公开了下式的化合物：其中R 1表示氢或氯原子，以及中间体。 这些包括4'-脱氧巴马霉素; 4'-脱氧-4'-表 - 氯 - 巴龙霉素; 4'-脱氧-4'-表 - 氯 - 五-N-苄氧羰基巴霉素; 4'-脱氧 - 五-N-苄氧羰基巴霉素; 6,3'，2“，5”，3“，4”' - 六-O-乙酰基-6'-O-苯甲酰基-4'-脱氧-5-N-苄氧基羰基巴霉素; 6,3'，2“，5”，3“，4” - 六-O-乙酰基-6'-O-苯甲酰基-4'-表氯 - 4'-脱甲基 - 五 -N-苄氧羰基巴霉素; 6,3'，2“，5”，3“，4”' - 六-O-乙酰基-6'-O-苄基 - 五-N-苄氧基氨基辛基巴霉素; 6,3'，2“，5”，3“，4” - 六-O-乙酰基-6'-O-苯甲酰基-4'-O - [（甲硫基） - 噻吩基] 五-N-苄氧羰基巴霉素; 和6,3'，2“，5”，3“，4” - 六-O-乙酰基-6'-O-苯甲酰基-4'-O - [（苯硫基） - 噻吩基] - 五-N-苄氧羰基巴霉素。 由结构式表示的化合物可用于治疗人和动物中的阿米巴痢疾。

    PROCESS FOR THE PREPARATION OF 5-(2-AMINO-PYRIMIDIN-4-YL)-2-ARYL-1H-PYRROLE-3-CARBOXAMIDES
    5.
    发明申请
    PROCESS FOR THE PREPARATION OF 5-(2-AMINO-PYRIMIDIN-4-YL)-2-ARYL-1H-PYRROLE-3-CARBOXAMIDES 有权
    制备5-（2-氨基 - 嘧啶-4-基）-2-芳基-1H-吡咯-3-羧酸的方法

    公开(公告)号：US20110040090A1

    公开(公告)日：2011-02-17

    申请号：US12989518

    申请日：2009-04-30

    申请人： Matteo D'Anello ,  Carlo Battistini ,  Maria Gioia Fornaretto ,  Ermes Vanotti

    发明人： Matteo D'Anello ,  Carlo Battistini ,  Maria Gioia Fornaretto ,  Ermes Vanotti

    IPC分类号： C07D403/04 ,  C07D207/416

    CPC分类号： C07D403/04

    摘要： The present invention relates to a process for the preparation of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxamides and to the useful intermediate compounds of such process. 5-(2-Amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxamides are described and claimed in W02007110344, which also discloses processes for their preparation. These compounds can be advantageously prepared through a process which allows to obtain the desired products in high yields and purity and with a limited number of steps. The synthesis is starting from a cyano pyrrole derivative, and is characterized from the final hydrolysis of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carbonitrile. The compounds prepared according to the process of the present invention are endowed with protein kinase inhibiting activity and, more particularly, Cdc7 or Cdc7/Cdks inhibiting activity. The compounds are therefore useful in the treatment of a variety of cancers, cell proliferative disorders and diseases associated with protein kinases.

    摘要翻译： 本发明涉及制备5-（2-氨基 - 嘧啶-4-基）-2-芳基-1H-吡咯-3-甲酰胺的方法和该方法的有用的中间体化合物。 5-（2-氨基 - 嘧啶-4-基）-2-芳基-1H-吡咯-3-甲酰胺在WO2007110344中进行了描述和要求保护，其也公开了其制备方法。 这些化合物可以有利地通过允许以高产率和纯度以及有限数量的步骤获得所需产物的方法制备。 合成起始于氰基吡咯衍生物，其特征在于5-（2-氨基 - 嘧啶-4-基）-2-芳基-1H-吡咯-3-甲腈的最终水解。 根据本发明的方法制备的化合物具有蛋白激酶抑制活性，更具体地，赋予Cdc7或Cdc7 / Cdks抑制活性。 因此，这些化合物可用于治疗多种癌症，细胞增殖性疾病和与蛋白激酶相关的疾病。

    Process for the preparation of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxamides
    8.
    发明授权
    Process for the preparation of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxamides 有权
    制备5-（2-氨基 - 嘧啶-4-基）-2-芳基-1H-吡咯-3-甲酰胺的方法

    公开(公告)号：US08399668B2

    公开(公告)日：2013-03-19

    申请号：US12989518

    申请日：2009-04-30

    申请人： Matteo D'Anello ,  Carlo Battistini ,  Maria Gioia Fornaretto ,  Ermes Vanotti

    发明人： Matteo D'Anello ,  Carlo Battistini ,  Maria Gioia Fornaretto ,  Ermes Vanotti

    IPC分类号： C07D403/04

    CPC分类号： C07D403/04

    摘要： The present invention relates to a process for the preparation of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxamides and to the useful intermediate compounds of such process. 5-(2-Amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxamides are described and claimed in WO2007110344, which also discloses processes for their preparation. These compounds can be advantageously prepared through a process which allows to obtain the desired products in high yields and purity and with a limited number of steps. The synthesis is starting from a cyano pyrrole derivative, and is characterized from the final hydrolysis of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carbonitrile. The compounds prepared according to the process of the present invention are endowed with protein kinase inhibiting activity and, more particularly, Cdc7 or Cdc7/Cdks inhibiting activity. The compounds are therefore useful in the treatment of a variety of cancers, cell proliferative disorders and diseases associated with protein kinases.

    摘要翻译： 本发明涉及制备5-（2-氨基 - 嘧啶-4-基）-2-芳基-1H-吡咯-3-甲酰胺的方法和该方法的有用的中间体化合物。 在WO2007110344中描述和要求保护5-（2-氨基 - 嘧啶-4-基）-2-芳基-1H-吡咯-3-甲酰胺，其也公开了其制备方法。 这些化合物可以有利地通过允许以高产率和纯度以及有限数量的步骤获得所需产物的方法制备。 合成起始于氰基吡咯衍生物，其特征在于5-（2-氨基 - 嘧啶-4-基）-2-芳基-1H-吡咯-3-甲腈的最终水解。 根据本发明的方法制备的化合物具有蛋白激酶抑制活性，更具体地，赋予Cdc7或Cdc7 / Cdks抑制活性。 因此，这些化合物可用于治疗多种癌症，细胞增殖性疾病和与蛋白激酶相关的疾病。

    Peptide antagonists of cellular mitogenesis and motogenesis and their therapeutic use
    9.
    发明授权
    Peptide antagonists of cellular mitogenesis and motogenesis and their therapeutic use 失效
    细胞有丝分裂和机制的肽拮抗剂及其治疗用途

    公开(公告)号：US06245742B1

    公开(公告)日：2001-06-12

    申请号：US08930616

    申请日：1997-10-15

    申请人： Carlo Battistini ,  Patrizia Giordano ,  Sabrina De Rosa ,  Fabio Corradi ,  Paolo Comoglio ,  Alberto Bardelli

    发明人： Carlo Battistini ,  Patrizia Giordano ,  Sabrina De Rosa ,  Fabio Corradi ,  Paolo Comoglio ,  Alberto Bardelli

    IPC分类号： A61K3800

    CPC分类号： C07K5/0827 ,  C07K5/0202 ,  C07K5/1016 ,  C07K5/1027 ,  C07K14/71

    摘要： The present invention relates to peptides and peptidomimetic compounds and pharmaceutical compositions containing them as useful pharmacological agents in the control or treatment of proliferative diseases such as cancer, against tumor growing and/or tumoral metastasis, and psoriasis and in the control or treatment of inflammatory, allergic, autoimmune, viral, and cardiovascular diseases. These new compounds have the unique property to inhibit the recognition of several phosphotyrosine containing motifs within all the cellular receptors and cytosolic transducers by a wide spectrum of SH2 domains contained in cytosolic transducers and other effector proteins laying along different pathways of the signal transduction process and with a particularly high affinity for the SH2 domain of the adaptor transducer Grb2, a key element along the pathway to mitogenesis and motogenesis, this last activity leading to invasiveness and to metastasis. The invention also relates to methods for production of the compounds and methods of treatment employing the compounds.

    摘要翻译： 本发明涉及肽和拟肽化合物和药物组合物，其含有它们作为控制或治疗增殖性疾病如癌症，抗肿瘤生长和/或肿瘤转移以及牛皮癣以及控制或治疗炎症， 过敏性，自身免疫性，病毒性和心血管疾病。 这些新化合物具有独特的性质，可以通过广泛的SH2结构域抑制所有细胞受体和细胞溶质转导体中识别的含有多种含磷酸酪氨酸基序，这些SH2结构域包含在信号转导过程不同途径的细胞溶质转导和其他效应蛋白中， 对于适应器传感器Grb2的SH2结构域特别高的亲和力，Grb2是沿着有丝分裂和发育的途径的关键因素，这是导致侵袭和转移的最后一个活动。 本发明还涉及化合物的制备方法和使用该化合物的处理方法。

    Substituted tetralymethylen-Oxindoles analogues as tyrosine kinase inhibitors
    10.
    发明授权
    Substituted tetralymethylen-Oxindoles analogues as tyrosine kinase inhibitors 失效
    取代的四氢甲基 - 羟吲哚类似物作为酪氨酸激酶抑制剂

    公开(公告)号：US6147073A

    公开(公告)日：2000-11-14

    申请号：US981473

    申请日：1998-01-12

    申请人： Carlo Battistini ,  Antonella Ermoli ,  Sergio Vioglio ,  Franco Buzzetti ,  Dario Ballinari

    发明人： Carlo Battistini ,  Antonella Ermoli ,  Sergio Vioglio ,  Franco Buzzetti ,  Dario Ballinari

    IPC分类号： A61K38/00 ,  A61K31/00 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61P9/00 ,  A61P25/28 ,  A61P35/00 ,  A61P35/04 ,  A61P37/02 ,  C07D209/34 ,  C07K5/062 ,  A61K31/54 ,  C07D401/06 ,  C07D413/06

    CPC分类号： C07D209/34

    摘要： A tetralylmethylene-2-oxindole derivative having the following formula (I) ##STR1## wherein one or two of R, R.sub.1, R.sub.2 and R.sub.3 the said two being the same or different, are selected from:a) --X--(CH.sub.2).sub.m --NH.sub.2, --X--(CH.sub.2).sub.m --NR.sub.4 R.sub.5 or --X--(CH.sub.2).sub.m --NHR.sub.6, in which X is --O--, --S-- or --NH--, m is an integer of 2 to 4, one of R.sub.4 and R.sub.5 is hydrogen or C.sub.1 -C.sub.6 alkyl and the other is C.sub.1 -C.sub.6 alkyl or R.sub.4 and R.sub.5 taken together with the N atom to which they are linked form a 5 to 7 membered saturated heteromonocycle, and R.sub.6 is C.sub.2 -C.sub.6 alkanoyl or a C-terminally linked peptidyl residue containing from 1 to 3 aminoacids wherein the terminal amino group is either free or protected or in an alkylated form to provide a --NR.sub.4 R.sub.5 group in which R.sub.4 and R.sub.5 are as defined above.

    摘要翻译： PCT No.PCT / EP97 / 02672 Sec。 371日期：1998年1月12日 102（e）日期1998年1月12日PCT提交1997年5月15日PCT公布。 公开号WO97 / 45409 日期1997年12月4日具有下式（I）的四亚甲基-2-羟基吲哚衍生物，其中所述两个相同或不同的R 1，R 2，R 2和R 3中的一个或两个选自：a）-X-（ CH2）m-NH2，-X-（CH2）m-NR4R5或-X-（CH2）m-NHR6，其中X是-O - ， - S-或-NH-，m是2〜4的整数 R 4和R 5中的一个是氢或C 1 -C 6烷基，另一个是C 1 -C 6烷基或R 4和R 5与它们所连接的N原子一起形成5至7元饱和杂单环，并且R 6是C 2 - C6链烷酰基或含有1至3个氨基酸的C末端连接的肽基残基，其中末端氨基是游离的或被保护的或以烷基化形式提供，其中R4和R5如上所定义的-NR4R5基团。