公开(公告)号：US20100016324A1

公开(公告)日：2010-01-21

申请号：US12567045

申请日：2009-09-25

申请人： Massimiliana LANDINI ,  Sandro Guiliani ,  Alessandro Giolitti

发明人： Massimiliana LANDINI ,  Sandro Guiliani ,  Alessandro Giolitti

IPC分类号： A61K31/50 ,  A61K31/35 ,  A61P43/00 ,  A61K31/415 ,  A61K31/444

CPC分类号： A61K31/00 ,  A61K8/4926 ,  A61K8/494 ,  A61K31/4166 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/47 ,  A61K31/4704 ,  A61K2800/782 ,  A61Q19/06

摘要： There are disclosed pharmaceutical compositions for topical administration or for use in mesotherapy, containing a PDE3 inhibitor as active ingredient, and their use in the treatment of cellulite.

摘要翻译： 公开了用于局部给药或用于含有PDE3抑制剂作为活性成分的中等疗法中的药物组合物及其在治疗脂肪团中的用途。

公开(公告)号：US20080004283A1

公开(公告)日：2008-01-03

申请号：US11792912

申请日：2005-12-06

申请人： Massimiliana Landini ,  Sandro Giuliani ,  Alessandro Giolitti

发明人： Massimiliana Landini ,  Sandro Giuliani ,  Alessandro Giolitti

IPC分类号： A61K31/4166 ,  A61K31/437 ,  A61K31/444 ,  A61K31/4709 ,  A61K31/501 ,  A61K31/519 ,  A61K8/49 ,  A61P17/00 ,  A61Q19/06

CPC分类号： A61K31/4166 ,  A61K8/4926 ,  A61K8/494 ,  A61K8/4946 ,  A61K8/4953 ,  A61K31/437 ,  A61K31/444 ,  A61K31/4709 ,  A61K31/501 ,  A61K31/519 ,  A61Q19/06

摘要： There are disclosed pharmaceutical compositions for topical administration or for use in mesotherapy, containing a PDE3 inhibitor as active ingredient, and their use in the treatment of cellulite.

摘要翻译： 公开了用于局部给药或用于含有PDE3抑制剂作为活性成分的中等疗法中的药物组合物及其在治疗脂肪团中的用途。

公开(公告)号：US20060205712A1

公开(公告)日：2006-09-14

申请号：US10516681

申请日：2003-06-05

申请人： Federico Calvani ,  Fernando Catrambone ,  Patrizia Felicetti ,  Christopher Fincham ,  Alessandro Giolitti ,  Carlo Maggi ,  Laura Quartara ,  Cristina Rossi ,  Rosa Terracciano

发明人： Federico Calvani ,  Fernando Catrambone ,  Patrizia Felicetti ,  Christopher Fincham ,  Alessandro Giolitti ,  Carlo Maggi ,  Laura Quartara ,  Cristina Rossi ,  Rosa Terracciano

IPC分类号： A61K31/551 ,  A61K31/496 ,  A61K31/4709 ,  C07D403/02 ,  C07D401/02

CPC分类号： C07D401/12 ,  C07D215/26

摘要： Non-peptide compounds of formula (I) having activity as specific antagonists of bradykinin (BK) B2 receptor. The compounds are chemically characterized by the presence of an alpha, alpha-disubstituted amino acid at least one amino group, free or salified, or the corresponding ammonium quaternary salt. These BK receptor antagonists are a novel class of medicaments which can be used in all the disorders in which said receptors are involved

摘要翻译： 具有活性作为缓激肽（BK）B2受体的特异性拮抗剂的式（I）的非肽化合物。 化合物的化学特征在于存在α，α-二取代的氨基酸至少一个氨基，游离或盐化，或相应的铵季盐。 这些BK受体拮抗剂是一类新的药物，可用于所有受体参与的所有疾病中

公开(公告)号：US07491825B2

公开(公告)日：2009-02-17

申请号：US10516681

申请日：2003-06-05

申请人： Federico Calvani ,  Fernando Catrambone ,  Patrizia Felicetti ,  Christopher Ingo Fincham ,  Alessandro Giolitti ,  Carlo Alberto Maggi ,  Laura Quartara ,  Cristina Rossi ,  Rosa Terracciano

发明人： Federico Calvani ,  Fernando Catrambone ,  Patrizia Felicetti ,  Christopher Ingo Fincham ,  Alessandro Giolitti ,  Carlo Alberto Maggi ,  Laura Quartara ,  Cristina Rossi ,  Rosa Terracciano

IPC分类号： C07D215/38 ,  A61K31/47

CPC分类号： C07D401/12 ,  C07D215/26

摘要： Non-peptide compounds of formula (I) having activity as specific antagonists of bradykinin (BK) B2 receptor. The compounds are chemically characterized by the presence of an alpha, alpha-disubstituted amino acid at least one amino group, free or salified, or the corresponding ammonium quaternary salt. These BK receptor antagonists are a novel class of medicaments which can be used in all the disorders in which the receptors are involved.

摘要翻译： 具有活性作为缓激肽（BK）B2受体的特异性拮抗剂的式（I）的非肽化合物。 化合物的化学特征在于存在α，α-二取代的氨基酸至少一个氨基，游离或盐化，或相应的铵季盐。 这些BK受体拮抗剂是一类新型的药物，可用于涉及受体的所有疾病。

公开(公告)号：US4503075A

公开(公告)日：1985-03-05

申请号：US441101

申请日：1982-11-12

申请人： Vittorio Pestellini ,  Mario Ghelardoni ,  Danilo Giannotti ,  Alessandro Giolitti ,  Carlo A. Maggi ,  Stefano Manzini ,  Guglielmo Grimaldi ,  Alberto Meli

发明人： Vittorio Pestellini ,  Mario Ghelardoni ,  Danilo Giannotti ,  Alessandro Giolitti ,  Carlo A. Maggi ,  Stefano Manzini ,  Guglielmo Grimaldi ,  Alberto Meli

IPC分类号： A61K31/165 ,  C07C233/12 ,  C07C103/82

CPC分类号： A61K31/165 ,  C07C233/12

摘要： The invention comprises: a derivative of 1-alkylamine-3-[4(p-alkyloxy-benzamide)phenoxy]-2-propanol of general formula I: ##STR1## where R.sub.1 is a linear or branched alkyl chain with 1 to 8 carbon atoms included, an alkenyl chain with 2 to 8 carbon atoms included, or an arylalkyl chain with 7 to 10 carbon atoms included, and R is a linear or branched alkyl group with 1 to 8 carbon atoms included;a compound as above, in an optically active form;pharmaceutically acceptable, non toxic salts of the above compounds;synthesis processes for obtaining the above compounds; anda pharmaceutical composition based on a compound as defined above.

摘要翻译： 本发明包括：通式I的1-烷基胺-3- [4（对 - 烷氧基 - 苯甲酰胺）苯氧基] -2-丙醇的衍生物：其中R 1是具有1至8个碳的直链或支链烷基链 包含的碳原子数为2〜8的烯基链或碳原子数为7〜10的芳烷基链，R为碳原子数为1〜8的直链或支链烷基， 如上所述的化合物，为光学活性形式; 上述化合物的药学上可接受的无毒盐; 用于获得上述化合物的合成方法; 以及基于上述化合物的药物组合物。

公开(公告)号：US07273856B2

公开(公告)日：2007-09-25

申请号：US10494077

申请日：2002-10-28

申请人： Alessandro Sisto ,  Valerio Caciagli ,  Maria Altamura ,  Alessandro Giolitti ,  Valentina Fedi ,  Antonio Guidi ,  Danilo Giannotti ,  Nicholas Harmat ,  Rossano Nannicini ,  Franco Pasqui ,  Carlo Alberto Maggi

发明人： Alessandro Sisto ,  Valerio Caciagli ,  Maria Altamura ,  Alessandro Giolitti ,  Valentina Fedi ,  Antonio Guidi ,  Danilo Giannotti ,  Nicholas Harmat ,  Rossano Nannicini ,  Franco Pasqui ,  Carlo Alberto Maggi

IPC分类号： A61K31/455 ,  A61K31/535 ,  C07D265/30 ,  C07D211/82 ,  C07D207/00

CPC分类号： C07D409/12 ,  A61K38/00 ,  C07D333/70 ,  C07K5/06026 ,  C07K5/06034 ,  C07K5/06078

摘要： Described herein are compounds of formula (I) useful as antagonists of tachykinins in general, and in particular of neurokinin A; and the pharmaceutical formulations comprising the compounds of formula (I)

摘要翻译： 本文描述的是通式（I）的化合物，其通常用作速激肽拮抗剂，特别是神经激肽A; 和包含式（I）化合物的药物制剂，

公开(公告)号：US4551451A

公开(公告)日：1985-11-05

申请号：US639687

申请日：1984-08-10

申请人： Vittorio Pestellini ,  Mario Ghelardoni ,  Alessandro Giolitti ,  Giovanna Volterra ,  Martino Furio ,  Alberto Meli

发明人： Vittorio Pestellini ,  Mario Ghelardoni ,  Alessandro Giolitti ,  Giovanna Volterra ,  Martino Furio ,  Alberto Meli

IPC分类号： C07D215/38 ,  A61K31/55 ,  A61P25/08 ,  A61P25/20 ,  C07D223/20 ,  A61K31/53

CPC分类号： C07D223/20

摘要： A pharmacologically active compound has the general formula ##STR1## in which R is a hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms; R.sub.1 and R.sub.2, which can be different, represent a hydrogen atom, a hydroxyl group, an alkyl group, an alkoxy group, an arylalkyl group, or an arylalkoxy group, or can jointly represent an oxygen atom or a CHCOOR.sub.1 ' group where R.sub.1 ' is a hydrogen atom or an alkyl group; and R.sub.3 represents a hydrogen or halogen atom or an alkyl, NH.sub.2, NO.sub.2, NHCO-alkyl, NHCO-aryl, NHCONH-alkyl or NHCOHN-aryl group.These compounds act on the central nervous system and have an anti-convulsant sedative activity.

摘要翻译： 药理活性化合物具有通式“IMAGE”，其中R是氢原子或含有1至4个碳原子的烷基; R 1和R 2可以不同，表示氢原子，羟基，烷基，烷氧基，芳基烷基或芳基烷氧基，或者可以共同表示氧原子或CHCOOR1'基团，其中R1' 是氢原子或烷基; 并且R 3表示氢或卤素原子或烷基，NH 2，NO 2，NHCO-烷基，NHCO-芳基，NHCONH-烷基或NHCOHN-芳基。 这些化合物作用于中枢神经系统，具有抗惊厥镇静作用。

公开(公告)号：US07645759B2

公开(公告)日：2010-01-12

申请号：US11786041

申请日：2007-04-10

申请人： Patrizia Felicetti ,  Christopher Ingo Fincham ,  Alessandro Giolitti ,  Carlo Alberto Maggi ,  Laura Quartara ,  Cristina Rossi

发明人： Patrizia Felicetti ,  Christopher Ingo Fincham ,  Alessandro Giolitti ,  Carlo Alberto Maggi ,  Laura Quartara ,  Cristina Rossi

IPC分类号： A61K31/4709 ,  C07D405/12 ,  A61K31/47 ,  C07D215/26

CPC分类号： C07D215/26

摘要： Non-peptide compounds having activity as selective antagonists of bradykinin (BK) B2 receptor are disclosed. The compounds have the general formula (I) in which R is hydrogen or methyl; W is a single bond or an oxygen atom; n=3; X is hydrogen or a —NR1R2 amino group in which R1 and R2 can be independently hydrogen or a group which is methyl, ethyl, n-propyl, or isopropyl; Y is a —NR3R4R5 quaternary ammonium group in which R3, R4, R5 can be independently a group which is methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, or n-pentyl; and the enantiomers and enantiomeric mixtures thereof. Pharmaceutical compositions containing these compounds and methods of using the compounds to treat patients having conditions, disorders or diseases involving activation of bradykinin B2 receptors are also disclosed.

摘要翻译： 具有活性作为缓激肽（BK）B2受体的选择性拮抗剂的非肽化合物被公开。 所述化合物具有通式（I），其中R是氢或甲基; W是单键或氧原子; n = 3; X是氢或-NR 1 R 2氨基，其中R 1和R 2可以独立地是氢或甲基，乙基，正丙基或异丙​​基的基团; Y是-NR 3 R 4 R 5季铵基，其中R 3，R 4，R 5可以独立地是甲基，乙基，正丙基，异丙基，正丁基，异丁基或正戊基的基团。 及其对映体和对映体混合物。 还公开了含有这些化合物的药物组合物和使用该化合物治疗患有缓激肽B2受体活化的病症或病症或疾病的患者的方法。

公开(公告)号：US20070281944A1

公开(公告)日：2007-12-06

申请号：US11786041

申请日：2007-04-10

申请人： Patrizia Felicetti ,  Christopher Fincham ,  Alessandro Giolitti ,  Carlo Maggi ,  Laura Quartara ,  Cristina Rossi

发明人： Patrizia Felicetti ,  Christopher Fincham ,  Alessandro Giolitti ,  Carlo Maggi ,  Laura Quartara ,  Cristina Rossi

IPC分类号： A61K31/496 ,  A61P29/00 ,  A61P37/00 ,  C07D405/14

CPC分类号： C07D215/26

摘要： Disclosed are non-peptide compounds having activity as selective antagonists of bradykinin (BK) B2 receptor. The compounds are chemically characterized by the presence of an amino acid alpha substituted with a cyclic group and by a tetraalkylammonium group. Also disclosed are pharmaceutical compositions containing the compound, and methods of using the compounds to treat patients having conditions, disorders or diseases involving activation of bradykinin B2 receptor.

摘要翻译： 公开了作为缓激肽（BK）B2受体的选择性拮抗剂的活性的非肽化合物。 化合物的化学特征在于存在被环状基团和四烷基铵基团取代的氨基酸α。 还公开了含有该化合物的药物组合物，以及使用该化合物治疗患有缓激肽B2受体活化的病症，疾病或疾病的患者的方法。

公开(公告)号：US4800208A

公开(公告)日：1989-01-24

申请号：US85067

申请日：1987-08-13

申请人： Vittorio Pestellini ,  Mario Ghelardoni ,  Danilo Giannotti ,  Alessandro Giolitti ,  Adriano Barzanti ,  Rossella Ciappi ,  Carlo Ortolani

发明人： Vittorio Pestellini ,  Mario Ghelardoni ,  Danilo Giannotti ,  Alessandro Giolitti ,  Adriano Barzanti ,  Rossella Ciappi ,  Carlo Ortolani

IPC分类号： C07D405/06 ,  A61K31/343 ,  A61K31/415 ,  A61K31/4178 ,  A61P31/04 ,  A61P31/10 ,  C07D521/00 ,  A61K31/34 ,  C07D403/06

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

摘要： Compounds corresponding to the general formula ##STR1## wherein: R and R1, that may be different, represent a hydrogen atom, a halogen, an alkyl group, an alkoxy radical in which the alkyl group contains one to four carbon atoms, a nitro group, a cyano group, an amino group, an acetamino group, a sulfamidic or N-substituted sulfamidic group; R2 represents a hydrogen atom, a halogen, an alkoxy radical, an alkyl group, a phenyl group, a phenylalkyl group, a phenylalkylene or phenylalkenyl group in which the alkylene or alkenyl radical contains two to four carbon atoms, a nitro group, a cyano group, an amino group, an acetamino group, an N-substituted suylfamidic group; and R3 represents a hydrogen atom, an alkyl group, preferably containing one to three carbon atoms or a cyano group.