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61. 发明申请

WO1994018207A1 RAPAMYCIN-LIKE MACROLIDE AND A NEW STRAIN OF STREPTOMYCES WHICH PRODUCES IT 审中-公开
标题翻译： RAPAMYCIN-LIKE MACROLIDE和一种生产线的新型菌株
公开(公告)号：WO1994018207A1
公开(公告)日：1994-08-18
申请号：PCT/EP1994000284
申请日：1994-02-01
申请人： SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT M.B.H. , SANDOZ-PATENT-GMBH , SANDOZ LTD. , FEHR, Theodor , SANGLIER, Jean-Jacques , SCHULER, Walter
发明人： SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT M.B.H. , SANDOZ-PATENT-GMBH , SANDOZ LTD.
IPC分类号： C07D498/18
CPC分类号： C07D498/18
摘要： A macrolide of formula (I) that has FK506 and rapamycin antagonistic properties. The macrolide is a metabolite of a newly isolated Streptomyces strain, Streptomyces sp. A 91-261 402.
摘要翻译：具有FK506和雷帕霉素拮抗性质的式（I）的大环内酯。大环内酯是新分离的链霉菌菌株Streptomyces sp。 A 91-261 402。

62. 发明申请

WO1993017039A1 ISO-CYCLOSPORIN SALTS 审中-公开
公开(公告)号：WO1993017039A1
公开(公告)日：1993-09-02
申请号：PCT/EP1993000407
申请日：1993-02-20
申请人： SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT M.B.H. , SANDOZ-PATENT-GMBH , SANDOZ LTD. , WENGER, Roland
发明人： SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT M.B.H. , SANDOZ-PATENT-GMBH , SANDOZ LTD.
IPC分类号： C07K07/64
CPC分类号： C07K7/645 , A61K38/13 , Y02A50/423
摘要： Acid addition salts of iso-cyclosporins are found to have surprisingly improved galenical characteristics, e.g., enhanced solubility and stability, and to demonstrate an improved pharmacologic profile compared to cyclosporins, making them useful as pharmaceuticals, e.g., as immunosuppressants, particularly as pro-drugs for cyclosporins. Novel iso-cyclosporins, which are useful, e.g., for making the iso-cyclosporin acid addition salts of the invention, are also provided, as are methods of production, pharmaceutical formulations, and therapeutic applications for the compounds of the invention.
摘要翻译：发现异环孢菌素的酸加成盐具有令人惊讶的改善的盖仑特性，例如增强的溶解度和稳定性，并且与环孢菌素相比显示出改善的药理学特征，使得它们可用作药物，例如作为免疫抑制剂，特别是作为前药用于环孢菌素。本发明化合物的制备方法，药物制剂和治疗应用也可提供新的异环孢菌素，其可用于制备本发明的异环孢菌素酸加成盐。

63. 发明申请

WO1993017037A1 TREATMENT OF ACUTE MIGRAINE OR CLUSTER HEADACHE ATTACKS 审中-公开
标题翻译：治疗急性脑膜炎或丛集性耳聋
公开(公告)号：WO1993017037A1
公开(公告)日：1993-09-02
申请号：PCT/EP1993000366
申请日：1993-02-16
申请人： SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT M.B.H. , SANDOZ-PATENT-GMBH , SANDOZ LTD. , HIRT, Dorothea , LATASTE, Xavier
发明人： SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT M.B.H. , SANDOZ-PATENT-GMBH , SANDOZ LTD.
IPC分类号： C07K07/06
CPC分类号： A61K9/0043 , A61K38/31
摘要： Nasal administration of a somatostatin peptide analogue or derivative for treating acute attacks of migraine or cluster headache.
摘要翻译：鼻内给予生长抑素肽类似物或衍生物用于治疗偏头痛或丛集性头痛的急性发作。

64. 发明申请

WO1991001144A1 LABELED POLYPEPTIDE DERIVATIVES 审中-公开
标题翻译：标签多肽衍生物
公开(公告)号：WO1991001144A1
公开(公告)日：1991-02-07
申请号：PCT/EP1990001169
申请日：1990-07-12
申请人： SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT M.B.H. , SANDOZ-PATENT-GMBH , SANDOZ LTD , ALBERT, Rainer , BAUER, Wilfried , PLESS, Janos
发明人： SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT M.B.H. , SANDOZ-PATENT-GMBH , SANDOZ LTD
IPC分类号： A61K43/00
CPC分类号： A61K51/088 , A61K47/62 , A61K47/6425 , A61K2121/00 , A61K2123/00
摘要： A biologically active peptide selected from growth factors, peptide hormones, interferons and cytokines and analogues and derivatives thereof, and bearing at least one chelating group linked to an amino group of said peptide, the chelating group being capable of complexing a detectable element and such amino group having no significant binding affinity to target receptors, are complexed with a detectable element and are useful as a pharmaceutical, e.g. a radiopharmaceutical for in vivo imaging of target tissues or for therapy.
摘要翻译：选自生长因子，肽激素，干扰素和细胞因子及其类似物和衍生物的生物活性肽，并且具有与所述肽的氨基连接的至少一个螯合基团，所述螯合基团能够络合可检测元件，并且所述氨基与靶受体没有显着结合亲和力的基团与可检测元件复合并且可用作药物，例如，用于靶组织的体内成像或用于治疗的放射性药物。

65. 发明申请

WO1984000547A1 FLUORALKYLATEDCARBAPENEM DERIVATIVES 审中-公开
标题翻译：氟代甲基丙烯酸衍生物
公开(公告)号：WO1984000547A1
公开(公告)日：1984-02-16
申请号：PCT/EP1983000193
申请日：1983-07-23
申请人： SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT M.B.H. , SANDOZ AG , SANDOZ-PATENT-GMBH
发明人： SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT M.B.H. , SANDOZ AG , SANDOZ-PATENT-GMBH , MAK, Ching, Pong , FLIRI, Hans
IPC分类号： C07D487/04
CPC分类号： C07D477/20 , C07D205/08 , C07D477/10 , C07D499/88 , C07F7/10
摘要： Compounds of formula (I), wherein, R1 represents hydrogen or methyl and R2 represents hydrogen or lower alkyl, lower alkenyl or cycloalkyl each of which may be unsubstituted or mono- or polysubstituted by amino, mono- or di-(lower)-alkylamino, lower acylamino, carboxy, lower alkoxycarbonyl or carbamoyl; a group of formula IIc: (CH2)p-R7, wherein R7 represents phenyl or a 5- or 6-membered saturated or unsaturated heterocycle containing one or more heteroatoms selected from 0, S and/or N and which may be unsubstituted or mono- or polysubstituted by fluoro, chloro, bromo, amino, mono- or di-(lower)-alkylamino, hydroxy, lower alkoxy, mercapto, alkylthio, phenylthio, sulfamoyl, guanidino, nitro, cyano, lower acylamino, carboxyl, alkoxycarbonyl or carbamoyl and p is 0, 1, 2 or 3; or a group of formula (II), (IIa), (IIb), wherein R4, R5 and R6 may be the same or different and each represents hydrogen or lower alkyl or R4 and R6 and/or R5 and one of the CH2 groups may be joined to form a ring as may R5 and R6 in formula II and R4 and R5 in IIa and IIb, which rings may be unsubstituted or mono- or poly-substituted by alkyl, hydroxy, carboxy or di-(lower)-alkylamino, m is 2 or 3, and n is 1, 2 or 3 with the proviso that when R1 is hydrogen and the group containing it has R-configuration, R2 is other than acetylaminoethyl; or protected forms and/or physiologically-hydrolysable and acceptable ester forms thereof; in free acid or salt form or in the form of zwitter-ions. The compounds exhibit chemotherapeutic properties and are particularly indicated for use as anti-bacterially active antibiotics.
摘要翻译：式（I）化合物，其中R 1表示氢或甲基，R 2表示氢或低级烷基，低级烯基或环烷基，其各自可以是未取代的或被氨基，单 - 或二 - （低级） - 烷基氨基，低级酰基氨基，羧基，低级烷氧基羰基或氨基甲酰基; 式IIc的基团：（CH 2）p -R 7，其中R 7表示苯基或含有一个或多个选自O，S和/或N的杂原子的5或6元饱和或不饱和杂环，并且其可以是未取代的或单羟基，低级烷氧基，巯基，烷硫基，苯硫基，氨磺酰基，胍基，硝基，氰基，低级酰氨基，羧基，烷氧基羰基或氨基甲酰基 p为0,1,2或3; 或式（II），（IIa），（IIb）的基团，其中R 4，R 5和R 6可以相同或不同，并且各自表示氢或低级烷基或R 4和R 6和/或R 5和一个CH 2基团可以结合形成环，如式II中的R 5和R 6，以及IIa和IIb中的R 4和R 5，该环可以是未被取代的或被烷基，羟基，羧基或二（低级） - 烷基氨基，m为2或3，n为1,2或3，条件是当R 1为氢且含有R基团时，R 2为乙酰氨基乙基; 或受保护的形式和/或其生理上可水解和可接受的酯形式; 以游离酸或盐的形式或以两性离子的形式存在。该化合物具有化学治疗性质，特别指出用作抗细菌活性抗生素。

66. 发明申请

WO1997003242A1 U.V. ABSORBER COMPOSITIONS 审中-公开
标题翻译：紫外光吸收组合物
公开(公告)号：WO1997003242A1
公开(公告)日：1997-01-30
申请号：PCT/EP1996003050
申请日：1996-07-11
申请人： CLARIANT FINANCE (BVI) LIMITED , SANDOZ-PATENT-GMBH , SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT M.B.H. , BEST, Michael , MURAT, Jean-Luc , PALACIN, Francis
发明人： CLARIANT FINANCE (BVI) LIMITED , SANDOZ-PATENT-GMBH , SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT M.B.H.
IPC分类号： D06P01/642
CPC分类号： D06P1/56 , D06P1/58 , D06P1/6135 , D06P1/6426 , D06P5/02 , D06P5/04 , D06P5/06 , D06P5/08
摘要： Compositions of water insoluble or very sparingly soluble U.V. absorbers can be improved by the addition of a non-ionic surfactant which is an addition product of ethylene oxide or propylene oxide or both ethylene oxide and propylene oxide, and a mixture of fatty alcohols, fatty acids or fatty esters having 7-20 carbon atoms, preferably 14-18 carbon atoms or either tristyrylphenol or distyrylphenol. Such compositions have a good storage stability and excellent shear stability when the substrate to be dyed is a yarn which is in packed form.
摘要翻译：水不溶或非常微溶的U.V. 可以通过加入作为环氧乙烷或环氧丙烷或环氧乙烷和环氧丙烷两者的加成产物的非离子表面活性剂和具有7-20个碳原子的脂肪醇，脂肪酸或脂肪酸酯的混合物来改善吸收剂，优选14-18个碳原子或三苯乙烯基苯酚或二苯乙烯基苯酚。当待染色的基底是填充形式的纱线时，这样的组合物具有良好的储存稳定性和优异的剪切稳定性。

67. 发明申请

WO1990006949A2 PEPTIDE DERIVATIVES 审中-公开
标题翻译：肽衍生物
公开(公告)号：WO1990006949A2
公开(公告)日：1990-06-28
申请号：PCT/EP1989001448
申请日：1989-11-30
申请人： SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT M.B.H. , SANDOZ AG , SANDOZ-PATENT-GMBH
发明人： SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT M.B.H. , SANDOZ AG , SANDOZ-PATENT-GMBH , ALBERT, Rainer , KRENNING, Eric, P. , LAMBERTS, Steven, W., J. , PLESS, Janos
IPC分类号： C07K07/26
CPC分类号： C07K14/6555 , A61K38/00
摘要： Somatostatin peptides bearing at least one chelating group for a detectable element, said chelating group being linked to an amino group of said peptide, and said amino group having no significant binding affinity for somatostatin receptors, in free or salt form, are complexed with a detectable element and are useful as a pharmaceutical, e.g. a radiopharmaceutical for in vivo imaging of somatostatin receptor positive tumors or for therapy.

68. 发明申请

WO1988002756A2 PEPTIDE DERIVATIVES 审中-公开
标题翻译：肽衍生物
公开(公告)号：WO1988002756A2
公开(公告)日：1988-04-21
申请号：PCT/EP1987000593
申请日：1987-10-12
申请人： SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT M.B.H. , SANDOZ AG , SANDOZ-PATENT-GMBH
发明人： SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT M.B.H. , SANDOZ AG , SANDOZ-PATENT-GMBH
IPC分类号： C07K09/00
CPC分类号： C07K9/00 , C07K1/1077 , Y02P20/55
摘要： Sugar derivative of a biologically active peptide, which derivative has a prolonged duration of action when compared to the non-sugar modified peptide, and contains at least on one of the amino acid units a sugar residue which is attached to an amino group thereof by a coupling other than a direct N-glycosidic bond, and additionally, when it is a condensation product of a carboxyl group containing sugar and a peptide with less than 8 amino acid units, by a coupling other than a direct amide bond.
摘要翻译：生物活性肽的糖衍生物，与未修饰的糖肽相比，该衍生物具有延长的作用持续时间，并且含有至少一个氨基酸单元的糖残基，其通过除直接N-糖苷键以外的偶联而与所述单元的氨基连接，此外，当其为含有羧基的糖和肽的缩合产物时，的8个氨基酸单元，通过不同于与酰胺直接键合的偶联。

69. 发明申请

WO1986007054A1 IMIDAZOLE ANALOGS OF MEVALONOLACTONE AND DERIVATIVES THEREOF 审中-公开
标题翻译：咪唑啉酮及其衍生物的咪唑类似物
公开(公告)号：WO1986007054A1
公开(公告)日：1986-12-04
申请号：PCT/EP1986000297
申请日：1986-05-16
申请人： SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT M.B.H. , SANDOZ-PATENT-GMBH , SANDOZ AG
发明人： SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT M.B.H. , SANDOZ-PATENT-GMBH , SANDOZ AG , WAREING, James, Richard
IPC分类号： C07D233/64
CPC分类号： C07D233/64 , C07F7/1804 , C07F9/6506
摘要： Compounds of the formula and the pharmaceutically acceptable acid addition salts thereof, wherein the various substituents are defined hereinbelow, the use thereof for inhibiting cholesterol biosynthesis and lowering the blood cholesterol level and, therefore, in the treatment of hyperlipoproteinemia and atherosclerosis, pharmaceutical compositions comprising such compounds and processes for and intermediates in the synthesis of such compounds.

70. 发明申请

WO1984000759A1 DESOXYURIDINE DERIVATIVES, PROCESSES FOR THEIR PREPARATION AND THEIR USE AS PHARMACEUTICALS 审中-公开
标题翻译：脱甲基衍生物，其制备方法及其作为药物的用途
公开(公告)号：WO1984000759A1
公开(公告)日：1984-03-01
申请号：PCT/EP1983000219
申请日：1983-08-12
申请人： SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT M.B.H. , SANDOZ AG , SANDOZ-PATENT-GMBH
发明人： SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT M.B.H. , SANDOZ AG , SANDOZ-PATENT-GMBH , GRIENGL, Herfried , WANEK, Erich
IPC分类号： C07H19/06
CPC分类号： C07H19/06
摘要： Desoxyuridine derivatives such as 1-(2-desoxy-beta-D-erythropentofuranosyl)-5-(2-chloroethyl)-(1H,3H)-pyrimidine-2,4-dione which derivatives are useful as chemotherapeutical agents particularly in combatting Herpes diseases and infections.

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