公开(公告)号：WO1994001435A1

公开(公告)日：1994-01-20

申请号：PCT/EP1993001743

申请日：1993-07-06

Applicant: FIDIA S.P.A. ,  BARTOLINI, Alessandro ,  GHELARDINI, Carla ,  GIOTTI, Alberto ,  GUALTIERI, Fulvio ,  SCAPECCHI, Serena ,  TOFFANO, Gino

Inventor： FIDIA S.P.A.

IPC: C07D451/10

CPC classification number: C07D451/04 ,  C07D451/10

Abstract: Compounds of general formula (I), where Ar = phenyl or beta-naphtyl, R1 = one or more substituents of the phenyl or beta-naphtyl nucleus, preferably in para position, and selected out of the group consisting of H, CH3, C(CH3)3, CH2-CH-(CH3)2, O-CH3, C1, F, Br, CF3, NH2, S-CH3, SO-CH3, CN, NO2; R2 = H, CH3, C2H5, CH(CH3)2, CH2OH, C6H5; R3 = (a); where R4 = H, CH3, C2H5, CH(CH3)2, CH2-C6H5; R5 = H, CH3; X = none O, S, NH, NCH3; Y = O, NH, both in the racemic form and in the isomeric enantiomeric forms, which produce a nootropic effect, i.e. memory enhancement and learning facilitation, as well as an analgesic effect.

Abstract translation: 通式（I）的化合物，其中Ar =苯基或β-萘基，R1 =苯基或β-萘基核的一个或多个取代基，优选在对位，并选自H，CH 3，C （CH 3）3，CH 2 -CH-（CH 3）2，O-CH 3，C 1，F，Br，CF 3，NH 2，S-CH 3，SO-CH 3，CN，NO 2; R2 = H，CH3，C2H5，CH（CH3）2，CH2OH，C6H5; R3 =（a）; 其中R 4 = H，CH 3，C 2 H 5，CH（CH 3）2，CH 2 -C 6 H 5; R5 = H，CH3; X =不是O，S，NH，NCH 3; Y = O，NH，均以外消旋形式和异构对映异构体形式产生，其产生向异性作用，即记忆增强和学习促进作用以及止痛作用。

公开(公告)号：WO1993017691A2

公开(公告)日：1993-09-16

申请号：PCT/EP1993000571

申请日：1993-03-12

Applicant: FIDIA S.P.A. ,  TOFFANO, Gino ,  ROMEO, Aurelio ,  SKAPER, Stephen, Drake

Inventor： FIDIA S.P.A.

IPC: A61K31/70

CPC classification number: A61K31/70 ,  A61K31/7032 ,  A61K38/185 ,  A61K31/195 ,  A61K38/18 ,  A61K2300/00 ,  A61K31/19

Abstract: The present invention refers to pharmaceutical compositions containing monosialoganglioside GM1 or a derivative thereof, namely, the inner ester AGF2 and the methyl ester AGF4, suitable for the treatment of Parkinson's disease. A further object of the present invention is a therapy for Parkinson's disease based on the associated administration of the aforesaid compounds and, in addition, the N-dichloroacetyl lyso GM1 (LIGA 20) with known pharmaceuticals active in the aforesaid treatment, in particular with L-dopa and/or BDNF.

Abstract translation: 本发明涉及含有单唾液酸神经节苷脂GM1或其衍生物，即适合治疗帕金森病的内酯AGF2和甲酯AGF4的药物组合物。 本发明的另一个目的是基于上述化合物的相关施用和另外在上述治疗中具有活性的已知药物的N-二氯乙酰溶菌素GM1（LIGA 20），特别是L -Dopa和/或BDNF。

公开(公告)号：WO1992011294A1

公开(公告)日：1992-07-09

申请号：PCT/EP1991002479

申请日：1991-12-20

Applicant: FIDIA S.P.A.

Inventor： FIDIA S.P.A. ,  DELLA VALLE, Francesco ,  ROMEO, Aurelio ,  KIRSCHNER, Günter

IPC: C08B37/10

CPC classification number: C08B37/0075

Abstract: Low molecular weight heparin derivatives and salts thereof are prepared by treating a quaternary ammonium salt of a heparin, dissolved in a heterocyclic organic solvent or in an aprotic solvent, with an alkylating agent having from 6 to 30 carbon atoms at a temperature of about 20 DEG to 60 DEG C for a prolonged period of time, treating the resultant reaction product at a temperature of about 5 DEG to 120 DEG C with an inorganic or organic base, such as an alkaline hydroxide, in aqueous solution, and isolating the obtained heparin derivatives in their free form or as alkaline salts thereof. The heparin derivatives obtained according to the procedure of the invention constitute a mixture of mostly depolymerized products with a narrow range of molecular weight. These products are useful as anti-thrombotic agents.

Abstract translation: 低分子量肝素衍生物及其盐通过在约20℃的温度下处理溶解于杂环有机溶剂或非质子溶剂中的肝素季铵盐与6-30个碳原子的烷基化剂来制备 在60℃〜60℃下，用无水或有机碱如碱性氢氧化物在水溶液中处理所得反应产物在约5℃至120℃的温度下，分离得到的肝素衍生物 以其游离形式或其碱性盐。 根据本发明的方法获得的肝素衍生物构成具有窄范围分子量的大多数解聚产物的混合物。 这些产品可用作抗血栓形成剂。

公开(公告)号：WO1994020516A1

公开(公告)日：1994-09-15

申请号：PCT/US1994001966

申请日：1994-03-04

Applicant: FIDIA S.P.A. ,  ROMEO, Aurelio ,  KIRSCHNER, Gunter ,  CHIZZOLINI, Carlo ,  MANEV, Hari ,  FACCI, Laura

Inventor： FIDIA S.P.A.

IPC: C07H15/10

CPC classification number: C07H15/10

Abstract: Semisynthetic analogues of gangliosides selected from the group consisting of N-sulfo-, N-hydrocarbyl-sulfonyl- and N-hydrocarbyloxy-sulfonyl-N,N'-dilyso-gangliosides and the N'-acyl derivatives thereof, N'-sulfo-, N'-hydrocarbylsulfonyl- and N'-hydrocarbyloxy-sulfonyl-N,N'-dilyso-gangliosides and the N-acyl derivatives thereof, N,N'-di or polysulfo-N,N'-di- or poly-lyso-gangliosides, N,N'-di- or polyhydrocarbylsulfonyl-N,N'-di- or poly-lyso-gangliosides and N,N'-di- or polyhydrocarbyloxy-N,N'-di- or poly-lyso-gangliosides, and functional derivatives thereof, and salts of these compounds, have protective activity against neurotoxicity induced by excitatory amino acids and are foreseen to be used in therapy in the nervous system and in modulating of the expression of determinants such as CD4 on the surface of human cells in the immune system.

Abstract translation: 神经节苷脂的半合成类似物，其选自N-磺基，N-烃基 - 磺酰基和N-烃氧基 - 磺酰基-N，N'-二甘氨酸神经节苷脂及其N'-酰基衍生物，N'-磺酰基 - ，N'-烃基磺酰基 - 和N'-烃氧基 - 磺酰基-N，N'-二甘氨酸神经节苷脂及其N-酰基衍生物，N，N'-二或多磺基-N，N'-二 - 或多 - 神经节苷脂，N，N'-二 - 或多烃基磺酰基-N，N'-二 - 或多溶血神经节苷脂和N，N'-二 - 或多羟基氧基-N，N'-二 - 或多溶解神经节苷脂 及其功能性衍生物和这些化合物的盐具有针对由兴奋性氨基酸诱导的神经毒性的保护作用，并且预期用于神经系统的治疗和调节人类表面上的诸如CD4的决定簇的表达 免疫系统中的细胞。

公开(公告)号：WO1993021190A1

公开(公告)日：1993-10-28

申请号：PCT/EP1993000915

申请日：1993-04-16

Applicant: FIDIA S.P.A. ,  DI MARTINO, Alessandro ,  CALLEGARO, Lanfranco ,  TOFFANO, Gino

Inventor： FIDIA S.P.A.

IPC: C07F09/10

CPC classification number: A61K31/685 ,  A61K35/30 ,  C07F9/103

Abstract: A phospholipid mixture in which the biological and pharmacological properties are maintained but from which unconventional viruses causing e.g. bovine spongiform encephalopathy are selectively eliminated may be prepared by extraction of phospholipids from bovine brain by a mixture of organic solvents of which one is a chlorinated hydrocarbon or by silica gel chromatography with elution with a succession of eluents consisting of chloroform, lower alcohols and water, or by a combination of extraction and silica gel chromatography. Purified phospholipids can be used in pharmaceutical compositions.

Abstract translation: 一种磷脂混合物，其中保持生物和药理学性质，但是由非常规病毒引起，例如， 选择性地消除牛海绵状脑病可以通过其中一种是氯代烃的有机溶剂的混合物或通过硅胶色谱法从牛脑中提取磷脂来制备，用一系列由氯仿，低级醇和水组成的洗脱液洗脱， 或通过萃取和硅胶色谱法的组合。 纯化的磷脂可用于药物组合物中。

公开(公告)号：WO1993020824A1

公开(公告)日：1993-10-28

申请号：PCT/EP1993000894

申请日：1993-04-13

Applicant: FIDIA S.P.A. ,  ROMEO, Aurelio ,  TOFFANO, Gino

Inventor： FIDIA S.P.A.

IPC: A61K31/70

CPC classification number: A61K31/70

Abstract: Pharmaceutical compositions containing monosialoganglioside derivatives suitable for the treatment of spinal cord injury caused by hypoxic-ischaemic or traumatic events, in which said derivatives are selected from the group consisting of the inner ester (AGF2) and the methyl ester (AGF4) of the monosialoganglioside (GM1).

Abstract translation: 含有适用于治疗由缺氧缺血性或创伤性事件引起的脊髓损伤的单唾液酸神经节苷脂衍生物的药物组合物，其中所述衍生物选自单唾液酸神经节苷脂的内酯（AGF2）和甲酯（AGF4） GM1）。

公开(公告)号：WO1991007417A1

公开(公告)日：1991-05-30

申请号：PCT/EP1990001960

申请日：1990-11-16

Applicant: FIDIA S.P.A. ,  DELLA VALLE, Francesco ,  CALLEGARO, Lanfranco ,  LORENZI, Silvana

Inventor： FIDIA S.P.A.

IPC: C07H15/10

CPC classification number: C07H15/10 ,  C07H1/08

Abstract: The process of the invention relates to a process for the preparation of a ganglioside mixture, free from contaminants associated with non-conventional, life-threatening viruses, without altering the biological and pharmacological characteristics of the mixture on the central and peripheral nervous systems.

Abstract translation: 本发明的方法涉及制备神经节苷脂混合物的方法，所述神经节苷脂混合物没有与非传统的危及生命的病毒相关的污染物，而不改变中枢和周围神经系统上混合物的生物学和药理学特征。

公开(公告)号：WO1989010941A1

公开(公告)日：1989-11-16

申请号：PCT/EP1989000519

申请日：1989-05-12

Applicant: FIDIA S.P.A.

Inventor： FIDIA S.P.A. ,  DELLA VALLE, Francesco ,  ROMEO, Aurelio

IPC: C08B15/00

CPC classification number: A61K9/0014 ,  A61K8/0208 ,  A61K8/73 ,  A61K8/731 ,  A61K8/733 ,  A61K8/735 ,  A61K8/736 ,  A61K47/36 ,  A61K47/38 ,  A61K2800/57 ,  A61L15/28 ,  A61L15/425 ,  A61L17/10 ,  A61L27/20 ,  A61L27/58 ,  A61L31/042 ,  A61Q19/00 ,  C08B11/20 ,  C08B15/005 ,  C08B37/003 ,  C08B37/0072 ,  C08B37/0084 ,  C08L5/00

Abstract: Inter and/or intramolecular cross-linked esters of acid polysaccharides are disclosed in which a part or all of the carboxy groups are esterified with hydroxyl groups of the same molecule and/or of different molecules of the acid polysaccharide. These inner cross-linked esters of polysaccharide acids are useful in the field of biodegradable plastic materials, to manufacture sanitary and surgical articles, in the cosmetic and pharmaceutical fields, in the food industry and in many other industrial fields.

Abstract translation: 公开了酸多糖的间和/或分子内交联的酯，其中部分或全部羧基用同一分子的羟基和/或酸多糖的不同分子酯化。 这些多糖酸的内部交联酯可用于可生物降解的塑料材料领域，在食品工业和许多其他工业领域的化妆品和制药领域中制造卫生和外科用品。

公开(公告)号：WO1998017285A1

公开(公告)日：1998-04-30

申请号：PCT/IB1997001288

申请日：1997-10-17

Applicant: FIDIA S.P.A. ,  ROMEO, Aurelio ,  SILVESTRINI, Bruno ,  KIRSCHNER, Gunter

Inventor： FIDIA S.P.A.

IPC: A61K31/715

CPC classification number: A61K31/728 ,  A61K31/416 ,  A61K31/445

Abstract: Pharmaceutical preparations are described, comprised of salts of hyaluronic acid with a basic anaesthetic containing aliphatics and/or amino groups, particularly salts with benzydamine or bupivacaine.

Abstract translation: 描述了药物制剂，其由透明质酸盐与含有脂肪族和/或氨基的碱性麻醉剂组成，特别是与苯甲胺或布比卡因的盐。

公开(公告)号：WO1995000142A1

公开(公告)日：1995-01-05

申请号：PCT/EP1994002008

申请日：1994-06-20

Applicant: FIDIA S.P.A. ,  DI ROSA, Massimo ,  CIRILLO, Rocco ,  HORNBY, Edward, Joseph ,  PROSDOCIMI, Marco

Inventor： FIDIA S.P.A.

IPC: A61K31/37

CPC classification number: A61K31/37

Abstract: A pharmaceutical composition which comprises as an active ingredient, an effective amount of 8-chloro-3(beta-diethylaminoethyl)-4-methyl-7-ethoxycarbonylmethoxy coumarin or a pharmaceutically acceptable salt thereof, for the treatment of pathological conditions involving high release of nitric oxide (NO).

Abstract translation: 一种药物组合物，其包含作为活性成分的有效量的8-氯-3（β-二乙基氨基乙基）-4-甲基-7-乙氧基羰基甲氧基香豆素或其药学上可接受的盐，用于治疗涉及高释放的病理状态 一氧化氮（NO）。