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101. 发明授权

US5064849A Heterocyclic derivatives useful as radiosensitizing agents and antiviral agents 失效
标题翻译：用作放射增敏剂和抗病毒剂的杂环衍生物
公开(公告)号：US5064849A
公开(公告)日：1991-11-12
申请号：US510869
申请日：1990-04-18
申请人： Toshimitsu Suzuki , Masakazu Sakaguchi , Yoshiyuki Miyata , Tomoyuki Mori
发明人： Toshimitsu Suzuki , Masakazu Sakaguchi , Yoshiyuki Miyata , Tomoyuki Mori
IPC分类号： C07D249/14 , A61K31/41 , A61K31/415 , A61K31/505 , A61P31/12 , A61P35/00 , A61P43/00 , C07C69/16 , C07D233/91 , C07D239/54 , C07D239/553 , C07D249/10
CPC分类号： C07D233/91 , C07D249/10
摘要： A novel heterocyclic derivative of formula (I): ##STR1## wherein R.sub.1 represents ##STR2## and R.sub.2 represents hydrogen or acyl. When R.sub.2 is acyl, the derivative can be prepared, for example, by the following process: ##STR3## wherein R.sub.4 is acyl and R.sub.1 is ##STR4## The derivative is less toxic and has radiosensitizing activity and antiviral activity even at a low concentration.Radiosensitizing agents and antiviral agents containing the derivative as active component are also disclosed.

102. 发明授权

US5064826A Novel triazolo-pyrimidine derivatives 失效
标题翻译：新型三唑衍生物衍生物
公开(公告)号：US5064826A
公开(公告)日：1991-11-12
申请号：US487412
申请日：1990-03-02
申请人： Klara Reiter nee Esses , Jozsef Reiter , Zoltan Budai , Endre Rivo , Peter Trinka , Lujza Petocz , Gabor Gigler , Istvan Gyertyan , Istvan Gacsalyi
发明人： Klara Reiter nee Esses , Jozsef Reiter , Zoltan Budai , Endre Rivo , Peter Trinka , Lujza Petocz , Gabor Gigler , Istvan Gyertyan , Istvan Gacsalyi
IPC分类号： A61K31/505 , A61K31/519 , A61P25/04 , A61P25/24 , A61P25/26 , A61P29/00 , C07D249/14 , C07D495/14
CPC分类号： C07D495/14
摘要： This invention relates to novel triazolopyrimidine derivatives of formulae (Ia) and (Ib), ##STR1## wherein Q represents hydrogen, a heterocyclic group optionally substituted by a C.sub.1-4 alkyl group and containing one or more oxygen and/or nitrogen atoms or a group of formula--SR.sup.1 wherein R.sup.1 is alkyl or aralkyl, or a group of formula--NR.sup.2 R.sup.3 wherein R.sup.2 and R.sup.3 are independently hydrogen, alkyl, alkenyl, cycloalkyl, aralkyl, aryl or a heterocyclic group,m and n are independently 0, 1, 2, 3 or 4, with the provision that if m stands for 0, then n is different from 0, and if both n and m are 1 or m stands for 0 and n is 2, the Q is different from methylthio or morpholino group, their mixtures or pharmaceutically acceptable salts. Furthermore, the invention relates to a process for preparing these compounds.The compounds of formulae (Ia) and (Ib) are able to inhibit the ptosis caused by tetrabenazine and they have analgetic activity.
摘要翻译：本发明涉及式（Ia）和（Ib）的新型三唑并嘧啶衍生物，其中Q表示氢，任选被C 1-4烷基取代并含有一个或多个氧和/ 或氮原子或式-SR1的基团，其中R 1是烷基或芳烷基，或式-NR 2 R 3基团，其中R 2和R 3独立地是氢，烷基，烯基，环烷基，芳烷基，芳基或杂环基，m和n是独立地0,1,2,3或4，条件是如果m代表0，则n不同于0，并且如果n和m都是1或m代表0并且n是2，则Q不同甲硫基或吗啉代基，它们的混合物或药学上可接受的盐。此外，本发明涉及一种制备这些化合物的方法。式（Ia）和（Ib）的化合物能够抑制由丁苯那嗪引起的下垂并具有止痛活性。

103. 发明授权

US5049477A Radiation responsive composition 失效
标题翻译：辐射响应组合物
公开(公告)号：US5049477A
公开(公告)日：1991-09-17
申请号：US338089
申请日：1989-04-14
申请人： Koki Nakamura , Masayoshi Tsuboi , Keizo Koya
发明人： Koki Nakamura , Masayoshi Tsuboi , Keizo Koya
IPC分类号： G03C1/00 , C07D231/24 , C07D231/46 , C07D249/12 , C07D249/14 , C07D261/12 , C07D261/14 , C07D265/02 , C07D271/06 , C07D271/10 , C07D273/01 , C07D273/04 , C07D285/125 , C07D421/00 , C09K9/02 , G03C1/675 , G03C1/73 , G03C7/00 , G03C8/12 , G03C8/40 , G03F7/004
CPC分类号： G03C1/73
摘要： A radiation responsive composition containing a compound represented by the following formula (I) and a photoreducing agent capable of forming a redox couple together with said compound for many uses, e.g., image formation, etching, plating, etc.: ##STR1## wherein N represents a nitrogen atom; X represents an oxygen atom (--O--), a sulfur atom (--S--), or a nitrogen-containing group of formula, ##STR2## R.sup.1, R.sup.2, R.sup.3 and R.sup.4 each represents a mere bond, a substituted or unsubstituted alkyl, aryl, heterocyclic, acyl, aralkyl, alkenyl, alkynyl or carbamoyl group, or a sulfonyl group into which a substituted or unsubstituted alkyl or aryl group has been introduced, provided that at least one of the substituents R.sup.1 to R.sup.3 be a substituted or unsubstituted aryl or heterocyclic group and that two or more of R.sup.1, R.sup.2 and R.sup.3, or of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 when X represents a nitrogen containing group of formula, ##STR3## may be taken together to form a ring; UG represents a group to be released from said compound of formula (I) taking advantage of the N--X bond cleavage as a trigger, which takes place when a redox couple is formed between said compound of formula (I) and the photoreducing agent irradiated with radiant rays; and the solid lines represent bonds, while broken lines indicate that a bond may or may not be present, but at least one of the broken lines forms a bond.
摘要翻译：含有由下式（I）表示的化合物和能够与所述化合物一起形成氧化还原对的许多用途的光致变化组合物，例如图像形成，蚀刻，电镀等。）其中N表示氮原子; X表示氧原子（-O-），硫原子（-S-）或式的含氮基团，R 1，R 2，R 3和R 4各自表示单键，取代或未取代的烷基，芳基，杂环，酰基，芳烷基，烯基，炔基或氨基甲酰基，或其中引入取代或未取代的烷基或芳基的磺酰基，条件是至少一个取代基R 1至R 3为取代或未取代的芳基或杂环基，当X代表含氮基团时，R 1，R 2和R 3，或R 1，R 2，R 3和R 4中的两个或多个可以一起形成环; UG表示利用NX键断裂作为触发剂从式（I）化合物释放的基团，当在所述式（I）化合物与用辐射剂照射的光还原剂之间形成氧化还原对时发生射线而实线表示键，而虚线表示键可以存在或不存在，但至少一个虚线形成键。

104. 发明授权

US5002698A Sulfur- and nitrogen-containing lubricant additives 失效
标题翻译：含硫和含氮润滑剂添加剂
公开(公告)号：US5002698A
公开(公告)日：1991-03-26
申请号：US375759
申请日：1989-07-05
申请人： Hermann O. Wirth , Hans-Helmut Friedrich
发明人： Hermann O. Wirth , Hans-Helmut Friedrich
IPC分类号： C07D295/08 , C07C67/00 , C07C313/00 , C07C323/25 , C07D207/34 , C07D209/08 , C07D213/74 , C07D215/06 , C07D223/10 , C07D233/72 , C07D249/08 , C07D249/14 , C07D263/28 , C07D277/20 , C07D277/36 , C07D295/088 , C10M135/24 , C10M135/28 , C10M135/30 , C10M135/32 , C10M135/34 , C10M135/36 , C10N30/06 , C10N40/08 , C10N40/20
CPC分类号： C07D213/74 , C07C323/25 , C07D249/14 , C07D295/088 , C10M135/24 , C10M135/28 , C10M135/32 , C10M135/34 , C10M135/36 , C10M2201/02 , C10M2219/084 , C10M2219/086 , C10M2219/09 , C10M2219/10 , C10M2219/102 , C10M2219/104 , C10M2219/106 , C10N2240/08 , C10N2240/40
摘要： Compositions containing a lubricant, a hydraulic fluid or a metal-working fluid and at least one compound of the formula I ##STR1## in which R, R.sup.4, R.sup.5 and n are as defined in claim 1, are described. The compounds of the formula I are suitable for use as anti-wear agents and as extreme-pressure additives for lubricants, hydraulic fluids and metal-working fluids. Novel compounds of the formula I are also described.

105. 发明授权

US4969948A Herbicidal and plant growth-regulating substituted phenoxyphenylsulphonylazoles, compositions and use 失效
标题翻译：除草和植物生长调节取代苯氧基苯基磺酰基唑，组成和用途
公开(公告)号：US4969948A
公开(公告)日：1990-11-13
申请号：US413349
申请日：1989-09-27
申请人： Michael Haug , Theodor Pfister , Hans-Joachim Santel , Robert R. Schmidt , Klaus Lurssen , Harry Strang
发明人： Michael Haug , Theodor Pfister , Hans-Joachim Santel , Robert R. Schmidt , Klaus Lurssen , Harry Strang
IPC分类号： A01N43/56 , C07D231/12 , C07D231/16 , C07D231/18 , C07D231/38 , C07D233/56 , C07D233/64 , C07D233/66 , C07D233/68 , C07D233/70 , C07D233/84 , C07D233/88 , C07D233/90 , C07D249/04 , C07D249/08 , C07D249/10 , C07D249/12 , C07D249/14 , C07D521/00
CPC分类号： C07D231/12 , C07D231/16 , C07D233/56 , C07D249/08
摘要： Herbicidal and plant growth-regulating substituted phenoxyphenylsulphonylazoles of the formula ##STR1## in which R.sup.1 represents hydrogen, halogen, cyano or trifluoromethyl,R.sup.2 represents hydrogen or halogen,R.sup.3 represents halogen, cyano, trifluoromethyl, trifluoromethoxy or trifluoromethylsulphonyl,R.sup.4 represents hydrogen or halogen,R.sup.5 represents hydrogen or halogen,R.sup.6 represents hydrogen, halogen, cyano, nitro or amino andAz represents optionally substituted azolyl.
摘要翻译：式（I）的除草剂和植物生长调节性取代的苯氧基苯基磺酰基唑其中R1代表氢，卤素，氰基或三氟甲基，R2代表氢或卤素，R3代表卤素，氰基，三氟甲基，三氟甲氧基或三氟甲基磺酰基，R4代表氢或卤素，R 5表示氢或卤素，R 6表示氢，卤素，氰基，硝基或氨基，而Az表示任选取代的唑基。

106. 发明授权

US4942114A Silver halide photographic materials with reducible brightening agent releaser 失效
标题翻译：卤化银照相材料与可还原增亮剂释放剂
公开(公告)号：US4942114A
公开(公告)日：1990-07-17
申请号：US189003
申请日：1988-05-02
申请人： Keisuke Shiba , Keizo Koya
发明人： Keisuke Shiba , Keizo Koya
IPC分类号： G03C7/26 , C07D213/64 , C07D213/70 , C07D215/38 , C07D249/12 , C07D249/14 , C07D249/20 , C07D249/22 , C07D251/20 , C07D251/42 , C07D251/52 , C07D261/12 , C07D261/14 , C07D261/20 , C07D263/56 , C07D271/06 , C07D273/01 , C07D273/04 , C07D311/86 , C07D311/92 , G03C1/06 , G03C1/815 , G03C7/305
CPC分类号： G03C1/8155 , G03C7/30541 , Y10S430/134 , Y10S430/156
摘要： A silver halide photographic material having at least one silver halide emulsion layer on a support, comprising a compound of formula (I):PWR--(Time).sub.t --FWA (I)in which PWR represents a group capable of releasing (Time).sub.t --FWA upon reduction; FWA represents a group which functions as a brightening agent; Time represents a group capable of releasing FWA through a reaction which follows the release of (Time).sub.t --FWA from PWR; and t represents an integer of 0 or 1.
摘要翻译：一种卤化银照相材料，其在载体上具有至少一个卤化银乳剂层，其包含式（I）化合物：PWR-（时间）t-FWA（I），其中PWR表示能够释放（时间）t -FWA减量 FWA表示作为增白剂起作用的基团; 时间表示能够通过PWR释放（Time）t-FWA后的反应释放FWA的组; t表示0或1的整数。

107. 发明授权

US4925863A Antifugal azole compounds 失效
标题翻译：防腐唑化合物
公开(公告)号：US4925863A
公开(公告)日：1990-05-15
申请号：US156017
申请日：1988-02-16
申请人： Richard W. Bayles , Francis T. Boyle , Michael B. Gravestock , James M. Wapdleworth
发明人： Richard W. Bayles , Francis T. Boyle , Michael B. Gravestock , James M. Wapdleworth
IPC分类号： A01N43/653 , A01N20060101 , A01N47/02 , A61K20060101 , A61K31/41 , A61K31/44 , A61K31/4427 , A61P31/04 , C07D20060101 , C07D213/00 , C07D233/22 , C07D233/24 , C07D233/26 , C07D249/00 , C07D249/08 , C07D249/14 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D521/00
CPC分类号： C07D231/12 , A01N43/653 , A01N47/02 , C07D233/56 , C07D249/08
摘要： 1,3-Diazolyl-2-propanol derivatives of the formula ##STR1## wherein X and Y are N or CH, R.sup.1 is phenyl, heterocyclyl, heterocyclyl-alkyl, -alkenyl or -alkynyl, optionally substituted, R.sup.2 and R.sup.3 are hydrogen or alkyl, and R.sup.4 and R.sup.5 are hydrogen, amino, alkoxyalkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, or alkenyl, or phenyl, phenylalkyl or phenylalkenyl, heterocycyl, heterocyclyalkyl or heterocyclylalkenyl, each optionally substituted, provided that when R.sup.1 is optionally substituted phenyl at least one of R.sup.1, R.sup.4 and R5 is, or contains, a phenyl ring bearing at least one substitutent selected from cyano, cyanoalkyl, nitro, aminocarbonylalkyl, halogeneoalkoxy and radicals of the formulae --CONR.sup.6 R.sup.7, --NHCOR.sup.8 or OR.sup.9 as defined herein, and the acid addition salts of compounds which contain a basic substituent; together with processes for their manufacture, pharmaceutical, veterinary and plant antifungal compositions, a method of treating fungal diseases in plants, and the use of the compounds for the manufacture of pharmacuetical or veterinary antifungal compositions.
摘要翻译：其中X和Y是N或CH，R 1是苯基，杂环基，杂环基 - 烷基， - 烯基或 - 炔基，任选地被取代，R 2和R 3是氢或烷基，和R 4和R 5是氢，氨基，烷氧基烷基，氨基烷基，烷基氨基烷基，二烷基氨基烷基或链烯基，或苯基，苯基烷基或苯基烯基，杂环基，杂环烷基或杂环烯基，各自任选取代，条件是当R 1是任选取代的苯基时，的R 1，R 4和R 5是或含有带有至少一个选自氰基，氰基烷基，硝基，氨基羰基烷基，卤代烷氧基的取代基的苯环，以及如本文所定义的式-CONR 6 R 7，-NHCOR 8或OR 9的基团，含有碱性取代基的化合物的盐; 以及其制造方法，药物，兽医和植物抗真菌组合物，在植物中治疗真菌疾病的方法，以及该化合物用于制备药物或兽医抗真菌组合物的用途。

108. 再颁专利

USRE33125E 3- and 5-[3-(1-arylureido)]-1,2,4-triazoles 失效
标题翻译： 3-和5- [3-（1-芳基脲基）] - 1,2,4-三唑
公开(公告)号：USRE33125E
公开(公告)日：1989-12-05
申请号：US884765
申请日：1986-07-11
申请人： Henry F. Campbell , Thomas H. Scholtz , George H. Douglas
发明人： Henry F. Campbell , Thomas H. Scholtz , George H. Douglas
IPC分类号： A61K31/41 , C07D249/14 , C07D251/42 , C07D401/04 , C07D401/12
CPC分类号： C07D401/04 , A61K31/41 , C07D249/14 , C07D251/42 , C07D401/12
摘要： ##STR1## This invention relates to .[.1-aryl-4-hydrazinyl-1,2-dihydro-1,3,5-triazin-2-ones and 2-thiones.]. .Iadd.3.Iaddend.- .Iadd.and 5.Iaddend.-.Iadd.[3.Iaddend.-(.Iadd.1.Iaddend.-.Iadd.arylureido.Iaddend.)]-.Iadd.1,2,4.Iaddend.-.Iadd.triazoles and 3.Iaddend.- .Iadd.and 5.Iaddend.-.Iadd.[3.Iaddend.-(.Iadd.1.Iaddend.-(.Iadd.arylthioureido.Iaddend.)]-.Iadd.triazoles .Iaddend.of Formula I, processes for their preparation, isobiuret and 4-alkoxy-s-triazinone preparative intermediates, and methods of treating physiological disorders in humans and animals, in particular, cardiovascular disorders, including hypertension.

109. 发明授权

US4822404A Sulfonamides derived from substituted 2-amino-1,2,4-triazolo (1,5-a) pyrimidines and compositions and methods of controlling undesired vegetation 失效
标题翻译：衍生自取代的2-氨基-1,2,4-三唑并（1,5-a）嘧啶的磺酰胺和控制不希望的植物的组合物和方法
公开(公告)号：US4822404A
公开(公告)日：1989-04-18
申请号：US111003
申请日：1987-10-20
申请人： William A. Kleschick
发明人： William A. Kleschick
IPC分类号： A01N43/90 , C07D249/14 , C07D487/04
CPC分类号： C07D487/04 , A01N43/90 , C07D249/14
摘要： Novel compounds, e.g., N-(5,7-dimethyl-1,2,4-triazolo [1,5-a]pyrimidin-2-yl)-2-thiophene sulfonamide and their compositions and use in the control of weeds.
摘要翻译：新型化合物，例如N-（5,7-二甲基-1,2,4-三唑并[1,5-a]嘧啶-2-基）-2-噻吩磺酰胺及其组合物并用于控制杂草。

110. 发明授权

US4795755A Heterocyclic derivatives 失效
标题翻译：杂环衍生物
公开(公告)号：US4795755A
公开(公告)日：1989-01-03
申请号：US353384
申请日：1982-03-01
申请人： Derrick F. Jones , Keith Oldham
发明人： Derrick F. Jones , Keith Oldham
IPC分类号： C07D213/73 , C07D213/75 , C07D231/16 , C07D231/40 , C07D239/42 , C07D239/46 , C07D239/54 , C07D239/545 , C07D249/04 , C07D249/08 , C07D249/14 , C07D257/06 , A61K31/495 , C07D403/04
CPC分类号： C07D213/73 , C07D213/75 , C07D231/16 , C07D231/40 , C07D239/42 , C07D239/47 , C07D239/545 , C07D249/04 , C07D249/08 , C07D249/14 , C07D257/06
摘要： This invention relates to heterocyclic derivatives which are histamine H-2 antagonists and which inhibit gastric acid secretion. According to the invention there is provided a guanidine derivative of the formula I: ##STR1## in which R.sup.1 and R.sup.2, same or different, are hydrogen or 1-10C alkyl, 3-8C cycloalkyl, 4-14C cycloalkylalkyl, each alkyl, cycloalkyl or cycloalkylalkyl optionally carrying one or more F, Cl or Br atoms, provided that one of R.sup.1 and R.sup.2 is halogen-substituted, or R.sup.2 is hydrogen and R.sup.1 is R.sup.5 -E-W- in which W is 2-6 alkylene optionally substituted by 1 or 2 1-4C alkyls, E is O,S,SO,SO.sub.2 or NR.sup.6 in which R.sup.6 is H or 1-6C alkyl, R.sup.5 is H or 1-6C alkyl optionally substituted by 1 or 2 1-4C alkyls, or R.sup.5 and R.sup.6 are joined to form a pyrrolidine, piperidine, morpholine, piperazine or N-methylpiperazine ring; ring X is a heterocyclic ring as defined in the specification; A is phenylene or 5-7C cycloalkylene, or a 1-8C alkylene into which is optionally inserted one or two groups; and R.sup.3 and R.sup.4 are a variety of radicals described in the specification: and the pharmaceutically-acceptable acid-addition salts thereof. Manufacturing processes and pharmaceutical compositions are also described.
摘要翻译：本发明涉及组胺H-2拮抗剂并抑制胃酸分泌的杂环衍生物。根据本发明，提供了式I的胍衍生物：其中R 1和R 2相同或不同，为氢或1-10C烷基，3-8C环烷基，4-14C环烷基烷基，各烷基，任选地携带一个或多个F，Cl或Br原子的环烷基或环烷基烷基，条件是R 1和R 2中的一个是卤素取代的，或者R 2是氢，R 1是R 5 -WW-，其中W是2-6个亚烷基，或2 1-4C烷基，E是其中R6是H或1-6C烷基，R5是H或任选被1或2个1-4C烷基取代的1-6C烷基的O，S，SO，SO2或NR6，或R5 R 6连接形成吡咯烷，哌啶，吗啉，哌嗪或N-甲基哌嗪环; 环X是说明书中定义的杂环; A是亚苯基或5-7C亚环烷基，或其中任选插入一个或两个基团的1-8C亚烷基; R3和R4是本说明书中描述的各种基团及其药学上可接受的酸加成盐。还描述了制造方法和药物组合物。

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