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1. 发明申请

WO1995020603A1 INHIBITORS OF SERINE PROTEASES, BEARING A CHELATING GROUP 审中-公开
标题翻译：丝氨酸蛋白酶抑制剂，支撑组
公开(公告)号：WO1995020603A1
公开(公告)日：1995-08-03
申请号：PCT/EP1995000269
申请日：1995-01-25
申请人： SANDOZ LTD. , SANDOZ-PATENT-GMBH , SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT MBH , METTERNICH, Rainer , TAPPARELLI, Carlo , WIENAND, Anette
发明人： SANDOZ LTD. , SANDOZ-PATENT-GMBH , SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT MBH
IPC分类号： C07K14/81
CPC分类号： A61K51/088 , A61K38/00 , C07K5/06191 , C07K5/0827
摘要： A trypsin-like serine protease inhibiting peptide or pseudo-peptide bearing a chelating group capable of complexing a detectable element, the chelating group being linked to an amino group of the peptide or pseudo-peptide such that the chelating group does not interfere with or prevent the binding of the peptide or pseudo-peptide to thrombin, preferably a compound of formula (I) or (II) in free form, in salt form or in the form of a complex, e.g. a complex with a detectable element, its preparation, its use as a medicament or, when complexed with a UPSILON -emitting radionuclide, as a radiopharmaceutical, e.g. for thrombus imaging, and pharmaceutical compositions containing such a compound.
摘要翻译：胰蛋白酶样丝氨酸蛋白酶抑制肽或携带能够络合可检测元素的螯合基团的假性肽，所述螯合基团与肽或假肽的氨基连接，使得螯合基团不干扰或预防肽或假肽与盐形式或复合物形式的凝血酶，优选游离形式的式（I）或（II）化合物的结合，例如具有可检测元素的复合物，其制备，其作为药物的用途，或当与UPSILON发射放射性核素复合时，作为放射性药物，例如，用于血栓成像，以及含有这种化合物的药物组合物。

2. 发明申请

WO1997005161A1 BORONIC ACID DERIVATIVES 审中-公开
标题翻译：硼酸衍生物
公开(公告)号：WO1997005161A1
公开(公告)日：1997-02-13
申请号：PCT/EP1996003314
申请日：1996-07-26
申请人： SANDOZ LTD. , SANDOZ-PATENT-GMBH , SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT MBH , WIENAND, Anette
发明人： SANDOZ LTD. , SANDOZ-PATENT-GMBH , SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT MBH
IPC分类号： C07K05/06
CPC分类号： C07K5/06191 , A61K38/00
摘要： A compound of formula (I) wherein each of Q1 and Q2 is OH or Q1 and Q2 form together a residue of formula (a) have interesting pharmacological properties.
摘要翻译：式（I）化合物其中Q 1和Q 2各自为OH或Q 1和Q 2，式（a）残基具有有趣的药理学性质。

3. 发明申请

WO1996041807A1 RAPAMYCIN DERIVATIVES 审中-公开
标题翻译： RAPAMYCIN衍生物
公开(公告)号：WO1996041807A1
公开(公告)日：1996-12-27
申请号：PCT/EP1996002441
申请日：1996-06-05
申请人： SANDOZ LTD. , SANDOZ-PATENT-GMBH , SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT MBH , COTTENS, Sylvain , SEDRANI, Richard
发明人： SANDOZ LTD. , SANDOZ-PATENT-GMBH , SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT MBH
IPC分类号： C07D498/18
CPC分类号： C07D498/18 , C07F7/1804
摘要： Compounds of Formula (I), wherein R2 is selected from formula (II) or formula (III), and X is OH or H show immunosuppressant activity.
摘要翻译：式（I）化合物，其中R 2选自式（II）或式（III），X是OH或H表示免疫抑制剂活性。

4. 发明申请

WO1996015227A1 METHODS OF INDUCING CELL DEATH OF PRIMITIVE HEMATOPOIETIC CELLS AND COMPOSITIONS FOR INDUCTION THEREOF 审中-公开
标题翻译：诱导原代细胞凋亡细胞死亡的方法及其诱导组合物
公开(公告)号：WO1996015227A1
公开(公告)日：1996-05-23
申请号：PCT/EP1995004479
申请日：1995-11-14
申请人： SANDOZ LTD. , SANDOZ-PATENT-GMBH , SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT MBH , SYSTEMIX, INC.
发明人： SANDOZ LTD. , SANDOZ-PATENT-GMBH , SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT MBH , SYSTEMIX, INC. , BRANDT, John , TSUKAMOTO, Ann, S. , HOFFMAN, Ronald, H. , BAZIL, Vladimir
IPC分类号： C12N05/08
CPC分类号： C12N5/0647 , A61K38/00 , C07K16/2896 , C12N2501/125 , C12N2501/23 , C12N2501/48 , C12N2501/599
摘要： The present invention encompasses methods for inducing cell death in hematopoietic cells expressing CD43. The methods can be used in conjunction with therapeutic treatments such as chemotherapy and hematopoietic stem cell transplantation. The method is also useful in obtaining a highly enriched population of hematopoietic stem cells.
摘要翻译：本发明包括在表达CD43的造血细胞中诱导细胞死亡的方法。这些方法可以与化疗和造血干细胞移植等治疗性治疗结合使用。该方法在获得高度富集的造血干细胞群体中也是有用的。

5. 发明申请

WO1996013273A1 PHARMACEUTICAL COMPOSITIONS 审中-公开
标题翻译：药物组合物
公开(公告)号：WO1996013273A1
公开(公告)日：1996-05-09
申请号：PCT/EP1995004187
申请日：1995-10-25
申请人： SANDOZ LTD. , SANDOZ-PATENT-GMBH , SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT MBH , COTTENS, Sylvain , HAEBERLIN, Barbara , SEDRANI, Richard , VONDERSCHER, Jacky
发明人： SANDOZ LTD. , SANDOZ-PATENT-GMBH , SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT MBH
IPC分类号： A61K38/13
CPC分类号： A61K9/0019 , A61K9/1075 , A61K9/4858 , A61K31/436 , A61K38/13 , A61K47/12
摘要： This invention provides a microemulsion pre-concentrate comprising a difficultly soluble active agent and a carrier medium comprising: 1) a hydrophilic phase which comprises dimethylisosorbide and/or a lower alkyl alkanoic ester, 2) a lipophilic phase, and 3) a surfactant. The active agent may be a cyclosporin or a macrolide. In another aspect, this invention provides a pharmaceutical composition for enteral or parenteral administration comprising a macrolide and an acid.
摘要翻译：本发明提供了包含难溶性活性剂和载体介质的微乳液预浓缩物，其包含：1）亲水相，其包含二甲基异山梨醇酯和/或低级烷基链烷酸酯，2）亲油相，和3）表面活性剂。活性剂可以是环孢菌素或大环内酯。另一方面，本发明提供了包含大环内酯和酸的肠内或肠胃外给药的药物组合物。

6. 发明申请

WO1996013249A1 PHARMACEUTICAL COMPOSITIONS 审中-公开
标题翻译：药物组合物
公开(公告)号：WO1996013249A1
公开(公告)日：1996-05-09
申请号：PCT/EP1995004208
申请日：1995-10-26
申请人： SANDOZ LTD. , SANDOZ-PATENT-GMBH , SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT MBH , JACKMAN, Martin , POPP, Xue-Ping , RICHTER, Friedrich , SCHMOOK, Fritz
发明人： SANDOZ LTD. , SANDOZ-PATENT-GMBH , SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT MBH
IPC分类号： A61K09/107
CPC分类号： A61K31/55 , A61K9/0014 , A61K9/107 , A61K31/436 , A61K47/06 , A61K47/10 , A61K47/14
摘要： This invention provides a topical composition, in the form of an emulsion, that comprises a compound of the FK506 class; a physiologically acceptable alkanediol, ether diol or diether alcohol containing up to 8 carbon atoms as solvent for the compound of the FK506 class; an unsaturated fatty alcohol and water. In another aspect, this invention provides a topical pharmaceutical composition that comprises a macrolide in suspension. In a further aspect, this invention provides the use of an unsaturated fatty alcohol to stabilise a macrolide in a pharmaceutical composition.
摘要翻译：本发明提供乳状液形式的局部组合物，其包含FK506类化合物; 含有至多8个碳原子的生理学上可接受的链烷二醇，醚二醇或二醚醇作为FK506类化合物的溶剂; 不饱和脂肪醇和水。另一方面，本发明提供了一种局部药物组合物，其包含悬浮液中的大环内酯。在另一方面，本发明提供不饱和脂肪醇在药物组合物中稳定大环内酯的用途。

7. 发明申请

WO1997011052A1 UREA DERIVATIVES AND THEIR USE AS ANALGESICS AND ANTIINFLAMMATORY AGENTS 审中-公开
标题翻译：尿素衍生物及其用作治疗和抗炎药物
公开(公告)号：WO1997011052A1
公开(公告)日：1997-03-27
申请号：PCT/EP1996004129
申请日：1996-09-20
申请人： SANDOZ LTD. , SANDOZ-PATENT-GMBH , SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT MBH , SANDOZ PHARMACEUTICALS (UK) LTD. , CAMPBELL, Elizabeth, Anne , WALPOLE, Christopher, Simon, John
发明人： SANDOZ LTD. , SANDOZ-PATENT-GMBH , SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT MBH , SANDOZ PHARMACEUTICALS (UK) LTD.
IPC分类号： C07C275/24
CPC分类号： C07C275/34 , C07C275/24 , C07C275/28 , C07C275/30
摘要： Compounds of formula (I) wherein: R1 is C1-4 alkyl, C1-4 alkoxy, halogen or trifluoromethyl; R2 is hydrogen or has any of the meanings given for R1; R3 is hydrogen or C1-4 alkyl and n is zero, 1 or 2, or physiologically hydrolysable and acceptable amide or salt thereof, processes for their production, their use as pharmaceuticals, e.g. as analgesics and antiinflammatory agents, and pharmaceutical compositions comprising them.
摘要翻译：式（I）的化合物，其中：R 1是C 1-4烷基，C 1-4烷氧基，卤素或三氟甲基; R2是氢或具有对R1给出的任何含义; R 3是氢或C 1-4烷基，n是0,1或2，或其生理上可水解和可接受的酰胺或其盐，它们的制备方法，它们作为药物的用途。作为止痛剂和抗炎剂，以及包含它们的药物组合物。

8. 发明申请

WO1996040875A1 METHODS FOR OBTAINING COMPOSITIONS ENRICHED FOR HEMATOPOIETIC STEM CELLS AND ANTIBODIES FOR USE THEREIN 审中-公开
标题翻译：用于获得用于HEMATOPOIETIC STEM细胞的组合物和用于其的抗体的方法
公开(公告)号：WO1996040875A1
公开(公告)日：1996-12-19
申请号：PCT/EP1996002463
申请日：1996-06-06
申请人： SANDOZ LTD. , SYSTEMIX, INC. , SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT MBH , SANDOZ-PATENT-GMBH
发明人： SANDOZ LTD. , SYSTEMIX, INC. , SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT MBH , SANDOZ-PATENT-GMBH , HILL, Beth, Louise , ROZLER, Elen , CHEN, Benjamin, P.
IPC分类号： C12N05/08
CPC分类号： C12N5/0647 , A61K35/28 , C07K16/28 , Y10S530/809
摘要： A method for obtaining human hematopoietic stem cells is provided by enrichment for stem cells using a novel stem cell marker. Compositions obtained thereby and reagents for use therein are also provided.
摘要翻译：通过使用新型干细胞标记物对干细胞进行富集来提供获得人类造血干细胞的方法。还提供了由此获得的组合物和其中使用的试剂。

9. 发明申请

WO1996034849A1 TETRALINES BEARING A PHENYL SUBSTITUANT ON THE AROMATIC RING AND THEIR USE IN THE TREATMENT OF EPILEPSY, STROKE AND BRAIN OR SPINAL TRAUMA 审中-公开
标题翻译：支撑在芳环上的苯并噻唑类替代物及其在治疗癫痫，脑脊髓和脊髓损伤中的应用
公开(公告)号：WO1996034849A1
公开(公告)日：1996-11-07
申请号：PCT/EP1996001841
申请日：1996-05-03
申请人： SANDOZ LTD. , SANDOZ-PATENT-GMBH , SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT MBH , SWOBODA, Robert
发明人： SANDOZ LTD. , SANDOZ-PATENT-GMBH , SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT MBH
IPC分类号： C07C217/54
CPC分类号： C07D295/073 , C07C211/42 , C07C215/64 , C07C217/74 , C07C237/48 , C07C255/58 , C07C2602/10 , C07D295/033
摘要： Compounds of formula (I) wherein R1 and R2, independently, are hydrogen (C1-4)alkyl, (C1-4)alkoxy, (C1-4)alkylthio, halogen, trifluoromethyl, trifluoromethoxy, cyano, (C2-5)alkanoyl, (C1-4)alkylsulfonyl or sulfamoyl; R3 is hydrogen, hydroxy, (C1-4)alkyl, (C1-4)alkoxy, halogen, cyano, (C2-5)alkanoyl, carbamoyl, (C1-4)alkylsulfonyloxy or trifluoromethylsulfonyloxy; and R4 and R5, independently, are hydrogen, (C1-4)alkyl, hydroxy(C2-4)alkyl or phenyl(C1-4)alkyl, or form together with the nitrogen atom to which they are attached a pyrrolidinyl, piperidino or piperazinyl group, in free base or acid addition salt form. Compounds according to formula (I) are useful in the treatment of epilepsy, stroke and brain or spinal trauma.
摘要翻译：式（I）化合物其中R 1和R 2独立地是氢（C 1-4）烷基，（C 1-4）烷氧基，（C 1-4）烷硫基，卤素，三氟甲基，三氟甲氧基，氰基，（C 2-5）烷酰基，（C 1-4）烷基磺酰基或氨磺酰基; R3是氢，羟基，（C1-4）烷基，（C1-4）烷氧基，卤素，氰基，（C2-5）烷酰基，氨基甲酰基，（C1-4）烷基磺酰氧基或三氟甲基磺酰氧基; 并且R 4和R 5独立地为氢，（C 1-4）烷基，羟基（C 2-4）烷基或苯基（C 1-4）烷基，或与它们所连接的氮原子一起形成吡咯烷基，哌啶子基或哌嗪基，游离碱或酸加成盐形式。根据式（I）的化合物可用于治疗癫痫，中风和脑或脊髓损伤。

10. 发明申请

WO1996029420A1 PLANTS RESISTANT TO TOSPOVIRUSES 审中-公开
标题翻译：植物抗病毒
公开(公告)号：WO1996029420A1
公开(公告)日：1996-09-26
申请号：PCT/EP1996001271
申请日：1996-03-22
申请人： SANDOZ LTD. , SANDOZ-PATENT-GMBH , SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT MBH , DE HAAN, Petrus, Theodorus
发明人： SANDOZ LTD. , SANDOZ-PATENT-GMBH , SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT MBH
IPC分类号： C12N15/82
CPC分类号： C12N15/8283
摘要： The present invention provides, inter alia, a recombinant polynucleotide, comprising a transcriptional regulatory region and a region contiguous therewith and under the transcriptional control thereof, wherein the contiguous region comprises the sequence depicted in SEQ ID No. 1 or a sequence complementary thereto or a part of the sequence or complement, characterized in that the sequence, complement or part is modified (i) by removal therefrom of translational-start encoding codons, or mutation of such codons so that they do not encode translational start or stop codons; or (ii) by insertion or deletion of nucleotides 3' of the translational start encoding codon so that the translational reading frame of the thus encoded RNA is different to that of the unmodified sequence, complement or part. The modified sequence, complement or part is capable of conferring upon plants resistance or tolerance to tospoviruses - typified by TSWV.
摘要翻译：本发明尤其提供了一种重组多核苷酸，其包含转录调节区和与其连续的区域及其转录控制，其中连续区包含SEQ ID No.1所示的序列或其互补序列或序列或补体的一部分，其特征在于修饰序列，补体或部分（i）通过从其中除去翻译起始编码密码子或这种密码子的突变，使得它们不编码翻译起始或终止密码子; 或（ii）通过插入或缺失翻译起始编码密码子的核苷酸3'，使得如此编码的RNA的翻译阅读框与未修饰的序列，补体或部分的翻译读框不同。修饰的序列，补体或部分能够赋予植物对烟草病毒的抗性或耐受性，以TSWV为代表。

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