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51. 发明申请

WO1989012638A1 TRICYCLIC 3-OXO-PROPANENITRILE DERIVATIVES AND PROCESS FOR THEIR PREPARATION 审中-公开
标题翻译：三氧化三氧代谢衍生物及其制备方法
公开(公告)号：WO1989012638A1
公开(公告)日：1989-12-28
申请号：PCT/EP1989000683
申请日：1989-06-16
申请人： FARMITALIA CARLO ERBA S.R.L. , DORIA, Gianfederico , ISETTA, Anna, Maria , FERRARI, Mario , TRIZIO, Domenico
发明人： FARMITALIA CARLO ERBA S.R.L.
IPC分类号： C07D491/052
CPC分类号： C07D491/04 , C07D495/04
摘要： Compounds having general formula (I), wherein X represents an oxygen atom or a -S(O)n-group, wherein n is zero, 1 or 2; R represents C1-C6 alkyl, pyridyl or substituted or unsubstituted phenyl; R2, R3 and R4 are as defined herein; and Q represents hydrogen, carboxy, C2-C7 alkoxycarbonyl or a -CON(Ra)'Rb group wherein Ra and Rb are as defined herein; and their pharmaceutically acceptable salts have immunomodulating activity and are useful in particular as immunostimulating agents, in the treatment of neoplastic diseases and acute and chronic infections of both bacterial and viral origin in mammals.
摘要翻译：具有通式（I）的化合物，其中X表示氧原子或-S（O）n - 基，其中n为0,1或2; R代表C1-C6烷基，吡啶基或取代或未取代的苯基; R2，R3和R4如本文所定义; 和Q表示氢，羧基，C 2 -C 7烷氧基羰基或-CON（R a）'R b基团，其中R a和R b如本文所定义; 其药学上可接受的盐具有免疫调节活性，并且特别可用作免疫刺激剂，用于治疗哺乳动物中肿瘤疾病和细菌和病毒来源的急性和慢性感染。

52. 发明申请

WO1989008646A1 HYPOLIPIDAEMIC IMIDAZOL-2-YL-DERIVATIVES OF BICYCLIC COMPOUNDS AND PROCESS FOR THEIR PREPARATION 审中-公开
标题翻译：双酚化合物的高分子咪唑-2-基衍生物及其制备方法
公开(公告)号：WO1989008646A1
公开(公告)日：1989-09-21
申请号：PCT/EP1989000233
申请日：1989-03-07
申请人： FARMITALIA CARLO ERBA S.R.L. , COZZI, Paolo , CARGANICO, Germano , SEVERINO, Dino , LOVISOLO, PierPaolo , CHIARI, Augusto
发明人： FARMITALIA CARLO ERBA S.R.L.
IPC分类号： C07D233/64
CPC分类号： C07D233/64 , C07D405/04
摘要： Compounds having formula (I), wherein the symbol ----- represents a single or double bond; Z is -O- or -CH2-; n is zero, 1, 2 or 3; each of R and R1, independently, is hydrogen or C1-C4 alkyl; each of R2 and R3, independently, is hydrogen or C1-C8 alkyl; and the pharmaceutically acceptable salts thereof; are useful in therapy in particular as antidislipidaemic and antiatherosclerotic agents.
摘要翻译：具有式（I）的化合物，其中符号-----表示单键或双键; Z是-O-或-CH 2 - ; n为零，1,2或3; R和R 1各自独立地是氢或C 1 -C 4烷基; R 2和R 3各自独立地是氢或C 1 -C 8烷基; 及其药学上可接受的盐; 在治疗中尤其可用作抗皮脂血症和抗动脉粥样硬化剂。

53. 发明申请

WO1995003409A1 ANALOGUES OF AN ANTI-THROMBIN POLYPEPTIDE AND PROCESS FOR THEIR PREPARATION 审中-公开
标题翻译：抗凝血多肽的模拟物及其制备方法
公开(公告)号：WO1995003409A1
公开(公告)日：1995-02-02
申请号：PCT/EP1994001979
申请日：1994-06-17
申请人： FARMITALIA CARLO ERBA S.R.L.
发明人： FARMITALIA CARLO ERBA S.R.L. , SCACHERI, Emanuela , VISCO, Carlo , MOLINARI, Antonio , GERNA, Marco , BOLIS, Giorgio
IPC分类号： C12N15/15
CPC分类号： C07K14/005 , A61K38/00 , C07K14/815 , C07K2319/02 , C12N2760/20222
摘要： The present invention relates to analogues of anti-thrombin polypeptides and to a process for their preparation. The analogues have been obtained by a C-terminal modification of anti-thrombin polypeptides isolated from the leech Hirudinaria manillensis and are characterized by an improved biological activity in comparison to the polypeptides from which they are derived. The analogues of the invention may be prepared by: 1) isolating the anti-thrombin polypeptide from the tissue or secretions of the leech Hirudinaria manillensis and 2) subsequently modifying the C-terminal end of such polypeptide. Alternatively, the analogues may also be synthetized by recombinant DNA methods. According to this latter aspect, the invention provides DNA sequences, expression vectors and host cell lines for the recombinant preparation of the analogues. The analogues of the invention find a useful application in the treatment of venous thrombosis, vascular shunt occlusion and thrombin-induced disseminated intravascular coagulation.
摘要翻译：本发明涉及抗凝血酶多肽的类似物及其制备方法。类似物已经通过从水蛭Hirudinaria manillensis分离的抗凝血酶多肽的C末端修饰获得，并且与从其衍生的多肽相比具有改善的生物学活性。本发明的类似物可以通过以下方法制备：1）从水蛭水蛭属的组织或分泌物中分离抗凝血酶多肽，和2）随后修饰该多肽的C-末端。或者，类似物也可以通过重组DNA方法合成。根据后一方面，本发明提供用于重组制备类似物的DNA序列，表达载体和宿主细胞系。本发明的类似物在治疗静脉血栓形成，血管分流闭塞和凝血酶诱导的弥散性血管内凝血方面发现有用。

54. 发明申请

WO1994028003A1 TRICYCLIC DEFEM SULPHONES AS ELASTASE INHIBITORS 审中-公开
标题翻译： TRICYCLIC DEFEM SULPHONES as ELASTASE INHIBITORS
公开(公告)号：WO1994028003A1
公开(公告)日：1994-12-08
申请号：PCT/EP1994001643
申请日：1994-05-17
申请人： FARMITALIA CARLO ERBA S.R.L. , ALPEGIANI, Marco , BISSOLINO, Pierluigi , PERRONE, Ettore , RIZZO, Vincenzo
发明人： FARMITALIA CARLO ERBA S.R.L.
IPC分类号： C07D501/00
CPC分类号： C07D501/00
摘要： The present invention provides compounds of formula (I) and pharmaceutically or veterinarily salts thereof; wherein R1 is hydrogen or halogen or an organic group; R2 is hydrogen or an optionally substituted C1-C6 alkyl, C3-C6 cycloalkyl, C6-C10 aryl or C7-C14 aralkyl group; R3 is hydrogen or halogen, or an organic group; R4 is hydrogen or a group defined as R2 above or R4 taken together with R3 constitutes a C2-C6 alkanediyl or an alkanediyl radical optionally substituted by methyl or phenyl and X is either oxygen or sulphur or NR6, wherein R6 is either hydrogen or a group as defined for R2. A process for their preparation by cyclization of appropriate intermediates is also described. The compounds of formula (I) and the pharmaceutically and veterinarily acceptable salts thereof are elastase inhibitors.
摘要翻译：本发明提供式（I）化合物及其药学上或兽用盐; 其中R1是氢或卤素或有机基团; R 2是氢或任选取代的C 1 -C 6烷基，C 3 -C 6环烷基，C 6 -C 10芳基或C 7 -C 14芳烷基; R3是氢或卤素，或有机基团; R 4是氢或被定义为R 2或R 4与R 3一起构成的基团构成任选被甲基或苯基取代的C 2 -C 6烷二基或烷二基，X是氧或硫或NR 6，其中R 6是氢或基团如R2所定义。还描述了通过合适的中间体的环化制备其方法。式（I）化合物及其药学上和兽医学上可接受的盐是弹性蛋白酶抑制剂。

55. 发明申请

WO1994014806A1 SEROTONINERGIC ERGOLINE DERIVATIVES 审中-公开
标题翻译：丝氨酸蛋白衍生物
公开(公告)号：WO1994014806A1
公开(公告)日：1994-07-07
申请号：PCT/EP1993003337
申请日：1993-11-26
申请人： FARMITALIA CARLO ERBA S.R.L.
发明人： FARMITALIA CARLO ERBA S.R.L. , MANTEGANI, Sergio , BRAMBILLA, Enzo , CACCIA, Carla , CARFAGNA, Nicola
IPC分类号： C07D457/04
CPC分类号： C07D457/04 , C07D457/02 , C07D457/08 , C07D457/12
摘要： The present invention provides compounds of formula (I) wherein A represents OH, NH2, COOR3', OCONHR4, CONHR4, NHCOR4, NHCO2R4, NHC(X)NHR4, NHC(X)NHCOR4, (a) or (b), R1 is hydrogen or C1-4 linear or branched alkyl; R2 is hydrogen, chlorine, bromine or an S-C1-4 alkyl group; R3 and R3' are, independently, C1-5 alkyl or hydrogen, n is 0,1 or 2, m is 1 or 2; R4 is hydrogen, C1-7 alkyl, C3-7 cycloalkyl, adamantidyl (tricyclo 3.3.1.1. ) decan-1-yl, C1-5 alkylphenyl, C2 alkenylphenyl; C2 alkynylphenyl, phenyl optionally substituted by one or more groups selected from C1-4 alkyl, C1-3 alkoxy, methylendioxy, cyano, trifluoromethyl, hydroxy, nitro and acetyl; an optionally substituted naphthyl ring or phenyl condensed with a heterocyclic ring system having 5- or 6- ring members including 1 to 4 heteroatoms selected from nitrogen, oxygen and sulphur; a heterocyclic ring having 5 or 6 ring members including 1 or 2 heteroatoms selected from nitrogen, oxygen and sulphur which is optionally substituted by a group selected from C1-4 alkyl, phenyl optionally substituted as defined above, C1-3 alkoxy and halogen; R5 is hydrogen, C1-4 alkyl or a phenyl group and X is NH, O, S; or a pharmaceutically acceptable salt thereof. A process for their preparation and the pharmaceutical compositions comprising them are also provided.
摘要翻译：本发明提供式（I）化合物，其中A代表OH，NH2，COOR3'，OCONHR4，CONHR4，NHCOR4，NHCO2R4，NHC（X）NHR4，NHC（X）NHCOR4，（a）或（b）氢或C 1-4直链或支链烷基; R2是氢，氯，溴或S-C1-4烷基; R3和R3'独立地为C1-5烷基或氢，n为0,1或2，m为1或2; R4是氢，C1-7烷基，C3-7环烷基，金刚烷基（三环3.3.1.1。<3,7>）癸烷-1-基，C1-5烷基苯基，C2链烯基苯基; C 2炔基苯基，任选被一个或多个选自C 1-4烷基，C 1-3烷氧基，甲氧基，氰基，三氟甲基，羟基，硝基和乙酰基的基团取代的苯基; 任选取代的萘基环或与具有5-或6-个环成员的杂环系统缩合的苯基，包括1至4个选自氮，氧和硫的杂原子; 具有5或6个环成员的杂环，包括1或2个选自氮，氧和硫的杂原子，其任选被选自C 1-4烷基，任选如上所定义的苯基，C 1-3烷氧基和卤素的基团取代; R5是氢，C1-4烷基或苯基，X是NH，O，S; 或其药学上可接受的盐。还提供了其制备方法和包含它们的药物组合物。

56. 发明申请

WO1993023406A1 HYDROXY PROTECTING GROUP REMOVAL IN PENEMS 审中-公开
标题翻译：保护组中的羟基保护基
公开(公告)号：WO1993023406A1
公开(公告)日：1993-11-25
申请号：PCT/EP1993000935
申请日：1993-04-15
申请人： FARMITALIA CARLO ERBA S.R.L.
发明人： FARMITALIA CARLO ERBA S.R.L. , BEDESCHI, Angelo , ZARINI, Franco
IPC分类号： C07D499/88
CPC分类号： C07D499/88 , Y02P20/55
摘要： The present invention relates to removal of t-butyldimethylsilyl protecting groups in the preparation of penems which are useful antibiotics. The invention provides a process for preparing a compound of formula (I), wherein R is a free or protected hydroxy or amino group or an alkoxy, acyloxy or an optionally substituted carbamoyloxy group, and R1 is selected from: a) hydrogen; b) a C2-C4 alkenyl group; c) a p-NO2 benzyl group; d) a linear or branched alkanoyloxy C1-C2 alkyl group; and e) (2-oxo-1,3-dioxolen-4-yl)methyl optionally substituted by C1-C4 alkyl at the 5-position or a pharmaceutically acceptable salt thereof, which process comprises reacting a compound of formula (II).
摘要翻译：本发明涉及在用作抗生素的青霉烯的制备中除去叔丁基二甲基甲硅烷基保护基。本发明提供了制备式（I）化合物的方法，其中R为游离或保护的羟基或氨基或烷氧基，酰氧基或任选取代的氨基甲酰氧基，R 1选自：a）氢; b）C 2 -C 4烯基; c）p-NO 2苄基; d）直链或支链烷酰氧基C 1 -C 2烷基; 和e）任选被5位的C 1 -C 4烷基取代的（2-氧代-1,3-二氧杂环戊烯-4-基）甲基或其药学上可接受的盐，该方法包括使式（II）化合物反应。

57. 发明申请

WO1993005799A1 LYOPHILIZED STABLE PHARMACEUTICAL COMPOSITIONS CONTAINING A GRANULOCYTE MACROPHAGE COLONY STIMULATING FACTOR 审中-公开
标题翻译：含有粒细胞巨噬细胞集落刺激因子的LYOPHILIZED稳定的药物组合物
公开(公告)号：WO1993005799A1
公开(公告)日：1993-04-01
申请号：PCT/EP1992002084
申请日：1992-09-10
申请人： FARMITALIA CARLO ERBA S.R.L. , CAVALLO, Alessandra , DALLA CASA, Rosanna , MAGRINI, Roberto , MELLA, Lorena
发明人： FARMITALIA CARLO ERBA S.R.L.
IPC分类号： A61K37/02
CPC分类号： A61K47/183 , A61K9/19 , A61K38/193 , A61K47/26
摘要： The invention relates to a lyophilized composition which comprises a granulocyte macrophage colony stimulating factor (GM-CSF), a pharmaceutically acceptable bulking agent, a polyoxyethylene sorbitan fatty acid ester and a basic amino acid. The compositions according to the present invention are useful in a method of treatment of the human or animal body, e.g. in the treatment of neutropenic disorders of cancer patients after chemotherapy.
摘要翻译：本发明涉及包含粒细胞巨噬细胞集落刺激因子（GM-CSF），药学上可接受的填充剂，聚氧乙烯山梨糖醇酐脂肪酸酯和碱性氨基酸的冻干组合物。根据本发明的组合物可用于治疗人或动物体的方法，例如，治疗化疗后癌症患者的中性粒细胞减少症。

58. 发明申请

WO1993002096A1 PROCESS FOR THE PREPARATION OF 17'beta'-SUBSTITUTED-4-AZA-5'alpha'-ANDROSTAN-3-ONE DERIVATIVES 审中-公开
标题翻译：制备17（BETA）-SUBSTITUTED-4-AZA-5（ALPHA）-ANDROSTAN-3-ONE衍生物的方法
公开(公告)号：WO1993002096A1
公开(公告)日：1993-02-04
申请号：PCT/EP1992001620
申请日：1992-07-16
申请人： FARMITALIA CARLO ERBA S.R.L. , PANZERI, Achille , CERIANI, Lucio , GRIGGI, Pierluigi , NESI, Marcella
发明人： FARMITALIA CARLO ERBA S.R.L.
IPC分类号： C07J73/00
CPC分类号： C07J73/005 , C07J41/0066
摘要： The preparation of a compound of formula (I) wherein X is oxygen or sulphur; R1 is hydrogen or C1-C6 alkyl; each of R2 and R3 is, independently, hydrogen, C1-C6 alkyl, C5 or C6 cycloalkyl or C6-C9 cycloalkylalkyl; R4 is hydrogen, C1-C6 alkyl, C5 or C6 cycloalkyl, C6-C9 cycloalkylalkyl or aryl; and the symbol ----- represents a single or a double bond; by a multistep process is disclosed.

59. 发明申请

WO1992021691A1 2',5'-NUCLEOTIDE ANALOGS AS ANTIVIRAL AGENTS 审中-公开
标题翻译： 2'，5'-NUCLEOTIDE ANALOGS作为抗病毒剂
公开(公告)号：WO1992021691A1
公开(公告)日：1992-12-10
申请号：PCT/EP1992001058
申请日：1992-05-14
申请人： FARMITALIA CARLO ERBA S.R.L.
发明人： FARMITALIA CARLO ERBA S.R.L. , BATTISTINI, Carlo , BRASCA, Maria, Gabriella , GIORDANI, Antonio , FUSTINONI, Silvia , ERMOLI, Antonella
IPC分类号： C07H21/00
CPC分类号： A61K31/70 , C07H21/00 , C07H21/04
摘要： There is provided the use of a nucleotide analog of formula (I) wherein R1 represents (i) a hydrogen atom, (ii) a 2' or 3'-P-thionucleotidyl residue conjugated at its 5' position with an acyl group, (iii) a phosphoryl group, a P-thiophosphoryl group, a PO2R H group optionally esterified with a linear or branched, cyclic or acyclic aliphatic hydroxy alkyl group having from 1 to 6 carbon atoms or with a lipophilic moiety or (iv) an acyl group; R represents a C1-C6 alkyl group or hydrogen atom, and the pharmaceutically acceptable salts thereof, in the manufacture of a medicament for use as an antiviral, antitumour, immunomodulatory, interferon-enhancing or interferon-inducing agent. Some compounds of formula (I) are new. A process for their preparation and pharmaceutical compositions comprising them are also provided.
摘要翻译：提供式（I）的核苷酸类似物的用途，其中R 1表示（i）氢原子，（ii）在其5'位与酰基共轭的2'或3'-对 - 硫代核苷酸残基（ iii）磷酸基，P-硫代磷酰基，任选用具有1至6个碳原子的直链或支链，环状或无环脂族羟基烷基或与亲油部分酯化的PO 2 R 2 H基团，或（iv）酰基; R 2表示C1-C6烷基或氢原子及其药学上可接受的盐，用于制备用作抗病毒，抗肿瘤，免疫调节，干扰素增强或干扰素诱导剂的药物。一些式（I）化合物是新的。还提供了其制备方法和包含它们的药物组合物。

60. 发明申请

WO1992004362A1 2-HYDROXY- AND 2-ACYLOXY-4-MORPHOLINYL ANTHRACYCLINES 审中-公开
标题翻译： 2-羟基 - 和2-乙酰氧基-4-吗啉酰基蒽醌
公开(公告)号：WO1992004362A1
公开(公告)日：1992-03-19
申请号：PCT/EP1991001506
申请日：1991-08-08
申请人： FARMITALIA CARLO ERBA S.R.L. , FAIARDI, Daniela , BARGIOTTI, Alberto , SUARATO, Antonino
发明人： FARMITALIA CARLO ERBA S.R.L.
IPC分类号： C07H15/252
CPC分类号： C07H15/252
摘要： Anthracycline glycosides of formula (1) wherein R1 is hydrogen or methoxy group; R2 is hydrogen or hydroxy; both R3 and R4 represent hydrogen or one of R3 and R4 is hydroxy and the other of R3 and R4 represents hydrogen; R5 represents hydrogen atom or an acyl residue -COX in which X is a C1-C8 linear or branched alkyl chain, an aryl, an aryl lower alkyl, or a 5- or 6-membered heteroaromatic group are anti-tumour agents.

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