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121. 发明申请

WO1998003497A1 COVALENTLY IMMOBILISED FLUOROIONOPHORES FOR OPTICAL ION SENSORS 审中-公开
标题翻译：用于光离子传感器的共同固定氟化物
公开(公告)号：WO1998003497A1
公开(公告)日：1998-01-29
申请号：PCT/EP1997003913
申请日：1997-07-21
申请人： NOVARTIS AG , BARNARD, Steven, Mark , BEERLI, René , BERGER, Joseph , REINHOUDT, David , WALDNER, Adrian
发明人： NOVARTIS AG
IPC分类号： C07D311/90
CPC分类号： C07D493/08 , C07C69/00 , C07C2603/00 , C07D219/08 , C07D311/90 , G01N33/52 , G01N33/84 , Y10S436/80
摘要： Compounds, constructed in modular manner, of formula (I), wherein I is the monovalent residue of an ionophore, F is the monovalent residue of a fluorophore, G is a functional group, T is a trivalent organic radical and R01, R02 and R03 are each independently of the others a direct bond or a bridging group. The compounds may be used in immobilised form as active components in polymer membranes of optical sensors for the detection of ions. The sensors are distinguished by a long usable life and a high degree of sensitivity.
摘要翻译：以式（I）的方式构建的化合物，其中I是离子载体的单价残基，F是荧光团的一价残基，G是官能团，T是三价有机基团，R01，R02和R03 各自独立于其他直接键或桥接基团。化合物可以以固定形式用作用于检测离子的光学传感器的聚合物膜中的活性组分。传感器的使用寿命长，灵敏度高。

122. 发明申请

WO1997048408A2 METHOD FOR THE PREVENTION AND TREATMENT OF MASTITIS 审中-公开
标题翻译：预防和治疗主体的方法
公开(公告)号：WO1997048408A2
公开(公告)日：1997-12-24
申请号：PCT/EP1997003212
申请日：1997-06-19
申请人： NOVARTIS AG , SURI, Bruno , GEORGES, Catherine , PEEL, John, Edmondson
发明人： NOVARTIS AG
IPC分类号： A61K38/05
CPC分类号： C07K5/06139 , A01N43/90 , A23C9/123 , A23C19/05 , A61K31/425 , A61K38/05
摘要： A method for treating or preventing mastitis in mammals is disclosed. The method contemplates the intramammary injection or dipping the teat with micrococcin antibiotics, preferably micrococcin P1 or P2, which do not interfere with the production of cheese and yoghurt using milk from treated animals. Hydrophobic antibiotics such as micrococcin P1 or P2 can be administered prior to infection to effectively suppress the rate, severity, and duration of subsequent bacterial infection, or can be administered subsequent to infection to effectively treat mastitis.
摘要翻译：公开了一种治疗或预防哺乳动物乳腺炎的方法。该方法考虑乳内注射或用乳球菌素抗生素，优选青霉素P1或P2浸泡乳头，其不影响使用经处理的动物的牛奶生产奶酪和酸奶。疏水性抗生素如微球菌素P1或P2可以在感染之前施用以有效抑制随后细菌感染的速率，严重性和持续时间，或者可以在感染后施用以有效治疗乳腺炎。

123. 发明申请

WO1997047765A1 METHOD FOR DETERMINING RNA STRUCTURE 审中-公开
标题翻译：确定RNA结构的方法
公开(公告)号：WO1997047765A1
公开(公告)日：1997-12-18
申请号：PCT/EP1997002998
申请日：1997-06-09
申请人： NOVARTIS AG , NAGAMINE, Yoshikuni
发明人： NOVARTIS AG
IPC分类号： C12Q01/68
CPC分类号： C12N15/1096 , C12Q1/6811 , C12Q2531/113 , C12Q2525/197
摘要： A method is provided for determining the structure of a target RNA molecule in a living cell, comprising the steps of: (a) treating cells containing the target RNA with a base-modifying agent capable of disrupting Watson-Crick base pairing; (b) isolating RNA from treated cells; (c) hybridising the isolated RNA with a target RNA-specific first primer and reverse transcribing the target RNA molecules; and (d) assaying the length of the transcripts. The method allows the identification of nucleosides in the target RNA molecule which are exposed to attack by the base-modifying agents, since modification of a nucleoside will cause arrest of the reverse transcription reaction. Differences in exposure of particular nucleosides in an RNA molecule subjected to differing conditions in vivo represent differences in the secondary structure of the molecule, particularly differences in RNA:protein interactions. The method of the invention thus allows the comparison of the structure of RNA exposed to different influences.
摘要翻译：提供了一种确定活细胞中靶RNA分子结构的方法，包括以下步骤：（a）用能够破坏沃森 - 克里克碱基配对的碱修饰剂处理含有靶RNA的细胞; （b）从处理的细胞中分离RNA; （c）将分离的RNA与靶RNA特异性第一引物杂交并逆转转录靶RNA分子; 和（d）测定转录物的长度。该方法允许鉴定受到碱改性剂侵袭的靶RNA分子中的核苷，因为核苷的修饰将导致逆转录反应的停止。在体内不同条件的RNA分子中特定核苷的暴露差异表示分子的二级结构的差异，特别是RNA：蛋白质相互作用的差异。因此，本发明的方法可以比较暴露于不同影响的RNA的结构。

124. 发明申请

WO1997047593A3 PEPTIDES 审中-公开
公开(公告)号：WO1997047593A3
公开(公告)日：1997-12-18
申请号：PCT/EP1997003077
申请日：1997-06-12
申请人： NOVARTIS AG , SEEBACH, Dieter
发明人： NOVARTIS AG
IPC分类号： C07C271/22

125. 发明申请

WO1997047592A1 PESTICIDES 审中-公开
标题翻译：农药
公开(公告)号：WO1997047592A1
公开(公告)日：1997-12-18
申请号：PCT/EP1997002889
申请日：1997-06-04
申请人： NOVARTIS AG , SZCZEPANSKI, Henry , ZELLER, Martin , HÜTER, Ottmar, Franz
发明人： NOVARTIS AG
IPC分类号： C07C251/60
CPC分类号： C07D213/53 , A01N37/36 , A01N37/42 , A01N37/50 , A01N43/40 , A01N43/50 , A01N43/80 , C07C251/60 , C07C2601/16 , C07D211/76 , C07D233/86 , C07D261/08 , C07D295/155
摘要： Pesticidally active compounds of formula (I) wherein: X is CH or N; Y is O, S, S=O or NR5; Z is OR2, SR2 or N(R3)R4; n is 0, 1, 2, 3, 4 or 5; or Y and Z together form a 5- to 7-membered ring containing 2 or 3 hetero atoms O and/or N that is unsubstituted or mono- or poly-substituted by C1-C4alkyl, halo-C1-C4alkyl, halogen, =O or by cyclopropyl; W is an aldimino or ketimino group; R1 is cyclopropyl, C1-C6alkyl or halo-C1-C6alkyl; R2 and R3 are each independently of the other C1-C6alkyl or halo-C1-C6alkyl; R4 and R5 are each independently of the other hydrogen, C1-C6alkyl or C1-C6alkoxy; R8 and R9 are each independently of the other hydrogen or C1-C3alkyl; or R8 and R9 together are C2-C6alkenyl or C3-C6cycloalkyl; R21 and R22 are each independently of the other hydrogen, halogen, C1-C8alkyl, C1-C8alkoxy or C1-C8alkylthio; and R23, R24, R25 and R26 are each independently of the others hydrogen, halogen, C1-C8alkyl or C1-C8alkoxy. The compounds may be used in the control of pests, especially as fungicides, acaricides and insecticides in plant protection.
摘要翻译：式（I）的杀虫活性化合物，其中：X是CH或N; Y是O，S，S = O或NR5; Z是OR 2，SR 2或N（R 3）R 4; n为0，1，2，3，4或5; 或Y和Z一起形成含有2或3个未被取代或被C1-C4烷基，卤代C1-C4烷基，卤素= O的单取代或多取代的2或3个杂原子的5至7元环或环丙基; W是阿霉素或酮咪基; R1是环丙基，C1-C6烷基或卤代-C1-C6烷基; R2和R3各自独立地为C 1 -C 6烷基或卤代-C 1 -C 6烷基; R 4和R 5各自独立地为氢，C 1 -C 6烷基或C 1 -C 6烷氧基; R 8和R 9各自独立地为氢或C 1 -C 3烷基; 或R8和R9一起是C 2 -C 6烯基或C 3 -C 6环烷基; R 21和R 22各自独立地为氢，卤素，C 1 -C 8烷基，C 1 -C 8烷氧基或C 1 -C 8烷硫基; R 23，R 24，R 25和R 26各自独立地为氢，卤素，C 1 -C 8烷基或C 1 -C 8烷氧基。这些化合物可用于防治害虫，尤其是作为杀真菌剂，杀螨剂和杀虫剂的植物保护。

126. 发明申请

WO1997047317A1 COMBINATION OF A SOMATOSTATIN ANALOGUE AND A RAPAMYCIN 审中-公开
标题翻译： SOMATOSTATIN ANALOGUE和RAPAMYCIN的组合
公开(公告)号：WO1997047317A1
公开(公告)日：1997-12-18
申请号：PCT/EP1997003036
申请日：1997-06-11
申请人： NOVARTIS AG , WECKBECKER, Gisbert
发明人： NOVARTIS AG
IPC分类号： A61K38/31
CPC分类号： A61K38/31 , A61K2300/00
摘要： A combination of a compound of the somatostatin class and a rapamycin macrolide is useful for the prevention or treatment of cell hyperproliferation.
摘要翻译：生长抑素类化合物和雷帕霉素大环内酯的组合可用于预防或治疗细胞过度增殖。

127. 发明申请

WO1997045119A1 USE OF SUBSTANCE P ANTAGONISTS FOR TREATING SOCIAL PHOBIA 审中-公开
标题翻译：使用物质治疗社会焦虑症
公开(公告)号：WO1997045119A1
公开(公告)日：1997-12-04
申请号：PCT/EP1997002481
申请日：1997-05-15
申请人： NOVARTIS AG , STRUCK, Michael , VASSOUT, Annick , KATZ, Richard , BENNETT, Deborah , KRAMER, Lynn , HAUSER, Kathleen
发明人： NOVARTIS AG
IPC分类号： A61K31/47
CPC分类号： A61K31/4525 , A61K31/4468 , A61K31/453 , A61K31/4535 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/517
摘要： The invention relates to the use of a compound of formula (I) or of a pharmaceutically utilizable salt thereof, in which R1 is an unsubstituted or substituted aralkyl, aryloxyalkyl, heteroaralkyl, aroyl, heteroaroyl, cycloalkylcarbonyl, aralkanoyl, heteroarylalkanoyl, aralkoxycarbonyl or arylcarbamoyl radical or the acyl radical of an alpha -amino acid which is unsubstituted or N-substituted by lower alkanoyl or carbamoyl-lower-alkanoyl; R2 is cycloalkyl or an unsubstituted or substituted aryl or heteroaryl radical; R3 is hydrogen, alkyl, carbamoyl or an alkanoyl or alkenoyl radical which is unsubstituted or substituted by carboxyl or esterified or amidated carboxyl; R4 is an unsubstituted or substituted aryl or unhydrogenated or partially hydrogenated heteroaryl radical; X1 is methylene, ethylene, a direct linkage, a carbonyl group which may be ketalized, or an unetherified or etherified hydroxymethylene group; X2 is alkylene, carbonyl or a direct linkage; and X3 is carbonyl, oxo-lower-alkylene, oxo(aza)-lower-alkylene or an alkylene radical which is unsubstituted or substituted by phenyl, hydroxymethyl, carboxyl which may be esterified or amidated, or by hydroxyl in a position higher than alpha ; for producing pharmaceutical products for the treatment of social phobia.
摘要翻译：本发明涉及式（I）化合物或其可药用盐的用途，其中R 1为未取代或取代的芳烷基，芳氧基烷基，杂芳烷基，芳酰基，杂芳酰基，环烷基羰基，芳烷酰基，杂芳基烷酰基，芳烷氧基羰基或芳基氨基甲酰基或未被取代或被低级烷酰基或氨基甲酰基 - 低级 - 烷酰基取代的α-氨基酸的酰基; R2是环烷基或未取代或取代的芳基或杂芳基; R3是氢，烷基，氨基甲酰基或未取代或被羧基或酯化或酰胺化羧基取代的烷酰基或烯酰基; R4是未取代或取代的芳基或未氢化或部分氢化的杂芳基; X1是亚甲基，乙烯，直接连接，可被缩醛化的羰基，或未醚化或醚化羟基亚甲基; X2是亚烷基，羰基或直链; 并且X 3是羰基，氧代 - 低级 - 亚烷基，氧代（氮杂） - 低级 - 亚烷基或亚烷基，其未被取代或被苯基，羟甲基，可被酯化或酰胺化的羧基或羟基在高于α ; 用于生产用于治疗社交恐惧症的药品。

128. 发明申请

WO1997043270A1 ISOXAZOLE DERIVATIVES AND THEIR USE AS HERBICIDES 审中-公开
标题翻译：异佛唑衍生物及其作为除草剂的用途
公开(公告)号：WO1997043270A1
公开(公告)日：1997-11-20
申请号：PCT/EP1997002442
申请日：1997-05-13
申请人： NOVARTIS AG , LEE, Shy-Fuh
发明人： NOVARTIS AG
IPC分类号： C07D261/10
CPC分类号： C07D261/10 , A01N43/80 , C07D413/04
摘要： Compounds defined by generic formula (I) or an agriculturally acceptable salt thereof, wherein the letter R represents a lower alkyl, haloalkyl, alkoxyalkyl, cycloalkyl, or alkenyl, each of which is optionally substituted, the symbol R represents a lower alkyl, haloalkyl or phenyl group, optionally substituted, X and Y are each independently a hydrogen, hydroxyl, halogen, cyano, alkylsulfenyl, alkylsulfinyl, alkylsulfonyl, acyloxy, carbamoyloxy, alkylsulfonyloxy, amino, substituted amino, acylamino, sulfamoyloxy, sulfamyl, or X and Y can be combined to be =O, -S(CH2)mS- and -O(CH2)mO-, in which m is 2 or 3, the symbol Ar represents an aromatic ring moiety optionally substituted with from one to four groups and wherein two substituents on adjacent positions of the aromatic ring may be taken together with the two atoms to which they are attached, to form a 5- to 7-membered ring optionally substituted, and the letter Z represents -S-, -SO- or -SO2-, exhibit herbicidal activity.
摘要翻译：由通式（I）或其农业上可接受的盐定义的化合物，其中字母R表示任选被取代的低级烷基，卤代烷基，烷氧基烷基，环烷基或烯基，符号R 1表示低级烷基，卤素烷基或苯基，任选取代的X和Y各自独立地为氢，羟基，卤素，氰基，烷基亚磺酰基，烷基亚磺酰基，烷基磺酰基，酰氧基，氨基甲酰氧基，烷基磺酰氧基，氨基，取代的氨基，酰氨基，氨磺酰氧基，氨磺酰基或X， Y可以组合为= O，-S（CH 2）m -S-和-O（CH 2）m O-，其中m为2或3，符号Ar表示任选被1-4个基团取代的芳环部分，其中芳族环的相邻位置上的两个取代基可以与它们所连接的两个原子一起形成任选取代的5-至7-元环，并且字母Z表示-S - ， - SO-或 -SO2-表现出除草活性。

129. 发明申请

WO1997041214A1 BIOCATALYSTS WITH AMINE ACYLASE ACTIVITY 审中-公开
标题翻译：生物钙与氨基酸酶活性
公开(公告)号：WO1997041214A1
公开(公告)日：1997-11-06
申请号：PCT/EP1997001866
申请日：1997-04-14
申请人： NOVARTIS AG , GHISALBA, Oreste , KITTELMANN, Matthias , LAUMEN, Kurt , WALSER-VOLKEN, Paula
发明人： NOVARTIS AG
IPC分类号： C12N09/80
CPC分类号： C12N9/80 , C12P41/007 , Y10S435/826 , Y10S435/893 , Y10S435/908
摘要： The invention belongs to the field of biotechnology. It concerns a biocatalyst, i.e. a dead or living microorganism or a polypeptide, preferably in isolated form, which exhibits acylase enzymatic activity without lipase- or esterase-activity. The biocatalyst is capable of stereoselectively hydrolysing a racemic acylamide which has an aliphatic acyl residue and which is not a derivative of a natural amino acid.
摘要翻译：本发明属于生物技术领域。它涉及生物催化剂，即死亡或活的微生物或多肽，优选分离形式，其显示没有脂肪酶或酯酶活性的酰基转移酶酶活性。该生物催化剂能够立体选择性水解具有脂肪族酰基残基并且不是天然氨基酸衍生物的外消旋酰基酰胺。

130. 发明申请

WO1997040029A1 ANTIVIRALLY ACTIVE HETEROCYCLIC AZAHEXANE DERIVATIVES 审中-公开
标题翻译：有活性的杂环亚胺衍生物
公开(公告)号：WO1997040029A1
公开(公告)日：1997-10-30
申请号：PCT/EP1997001860
申请日：1997-04-14
申请人： NOVARTIS AG
发明人： NOVARTIS AG , FÄSSLER, Alexander , BOLD, Guido , CAPRARO, Hans-Georg , LANG, Marc , KHANNA, Satish, Chandra
IPC分类号： C07D277/28
CPC分类号： C07D213/42 , C07C271/22 , C07C281/02 , C07C281/04 , C07D241/12 , C07D257/04 , C07D277/28 , C07D333/20 , Y02P20/55
摘要： There are described compounds of formula (I*) wherein R1 is lower alkoxycarbonyl, R2 is secondary or tertiary lower alkyl or lower alkylthio-lower alkyl, R3 is phenyl that is unsubsituted or substituted by one or more lower alkoxy radicals, or C4-C8cycloalkyl, R4 is phenyl or cyclohexyl each substituted in the 4-position by unsaturated heterocyclyl that is bonded by way of a ring carbon atom, has from 5 to 8 ring atoms, contains from 1 to 4 hetero atoms selected from nitrogen, oxygen, sulfur, sulfinyl (-SO-) and sulfonyl (-SO2-) and is unsubstituted or substituted by lower alkyl or by phenyl-lower alkyl, R5, independently of R2, has one of the meanings mentioned for R2, and R6, independently of R1, is lower alkoxycarbonyl, or salts thereof, provided that at least one salt-forming group is present. The compounds are inhibitors of retroviral aspartate protease and can be used, for example, in the treatment of AIDS. They exhibit outstanding pharmacodynamic properties.
摘要翻译：描述了式（I *）的化合物，其中R 1是低级烷氧基羰基，R 2是仲或叔低级烷基或低级烷硫基 - 低级烷基，R 3是未被取代或被一个或多个低级烷氧基取代的苯基或C 4 -C 8环烷基 R4是通过环碳原子键合的不饱和杂环基在4-位取代的苯基或环己基，具有5-8个环原子，含有1-4个选自氮，氧，硫，亚磺酰基（-SO-）和磺酰基（-SO 2 - ），并且是未取代的或被低级烷基或苯基 - 低级烷基取代，R 5与R 2独立地具有R2中提到的含义之一，R 6，是低级烷氧基羰基或其盐，条件是存在至少一个成盐基团。这些化合物是逆转录病毒天冬氨酸蛋白酶的抑制剂，可以用于例如艾滋病的治疗。它们具有出色的药效学性质。

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