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1. 发明授权

US4424351A Pyrido�3,4-e!-as-triazines 失效
标题翻译：吡啶并[3,4-e] -as-三嗪
公开(公告)号：US4424351A
公开(公告)日：1984-01-03
申请号：US123807
申请日：1980-02-22
申请人： Pal Benko , Gyo/ rgyi nee Lax Kovanyi , Judit nee Gergely Timar , Maria nee Lakatos Sigmond , Lujza Petocz , Peter Go/ ro/ g , Ibolya Kosoczky , Eniko nee Kiszelly Szirt , Hristone Toncsev
发明人： Pal Benko , Gyo/ rgyi nee Lax Kovanyi , Judit nee Gergely Timar , Maria nee Lakatos Sigmond , Lujza Petocz , Peter Go/ ro/ g , Ibolya Kosoczky , Eniko nee Kiszelly Szirt , Hristone Toncsev
IPC分类号： A61K31/53 , A61P25/04 , A61P29/00 , C07D471/04
CPC分类号： C07D471/04
摘要： Acylated pyrido �3,4-e!-as-triazines of the formula (I), ##STR1## wherein R.sub.1 stands for alkyl, alkoxy, haloalkyl, furyl, pyridyl, phenyl, phenyl-(C.sub.1-4 alkyl) or phyenyl-(C.sub.2-4 alkenyl) optionally substituted. R.sub.2 stands for hydrogen or a group of the formula R.sub.1 --CO--, R.sub.3 stands for hydrogen, a phenyl group or a naphthy6l group optionally substituted, or a phenyl-(C.sub.1-4 alkyl) group, pyridyl group or a C.sub.1-20 alkyl group, and R.sub.4 stands for hydrogen or a group of the formula R.sub.1 --CO--, and R.sub.5 forms together with R.sub.2 or R.sub.4 a valence bond, wherein R.sub.2 or R.sub.4 taking part in forming said valence bond may not have the above meaning, and pharmaceutically acceptable acid addition salts thereof, which are prepared by reacting a pyrido �3,4-e!-as-triazine of the formula (II) or an acid addition salt thereof ##STR2## R.sub.6 stands for hydrogen, and R.sub.5 forms together with R.sub. and R.sub.4 a valence bond, with an acylating agent of the formula (III). R.sub.1 --CO--X (III) The compounds exert favourable effects on the central nervous system, and can be applied primarily as analgesic and antiphlogistic agents.
摘要翻译：式（I）的酰化吡啶并[3,4-e] -as-三嗪，其中R1代表烷基，烷氧基，卤代烷基，呋喃基，吡啶基，苯基，苯基 - （C1-4烷基）或（烯基）（C 2-4烯基）任意取代。 R2代表氢或式R1-CO-的基团，R3代表氢，苯基或任选取代的萘基，或苯基 - （C 1-4烷基）基，吡啶基或C 1-20烷基， R4代表氢或式R1-CO-基团，R5与R2或R4一起形成价键，其中参与形成所述价键的R2或R4可能不具有上述含义，并且其药学上可接受的酸通过使式（II）的吡啶并[3,4-e]-α-三嗪或其酸加成盐反应制备的加成盐，其中R6代表氢，R5与兰德R4是价键，具有式（III）的酰化剂。 R1-CO-X（III）该化合物对中枢神经系统具有有利的作用，可主要用作镇痛药和消炎药。

2. 发明授权

US4697013A Condensed as-triazine derivatives 失效
标题翻译：浓缩的三嗪衍生物
公开(公告)号：US4697013A
公开(公告)日：1987-09-29
申请号：US652613
申请日：1984-09-20
申请人： Andras Messmer , Sandor Batori , Gyorgy Hajos , Pal Benko , Laszlo Pallos , Lujza Petocz , Grasser Katalin , Ibolya Kosoczky
发明人： Andras Messmer , Sandor Batori , Gyorgy Hajos , Pal Benko , Laszlo Pallos , Lujza Petocz , Grasser Katalin , Ibolya Kosoczky
IPC分类号： C07D253/08 , C07D471/04
CPC分类号： C07D471/04
摘要： A one step process for the preparation of compounds having antidepressant activity of the formula I ##STR1## and isomers thereof, wherein R.sub.1, R.sub.2, Z and A.sup.- have the meanings indicated in the claims, which process comprises: heating a compound of the formula II ##STR2## wherein Z, A.sup.-, R.sub.1 and R.sub.2 have the meanings set out in the claims and R.sub.3 stands for hydrogen or C.sub.1-4 alkyl, in the presence of a dehydrating agent to split off a compound of the formula R.sub.3 OH. The invention is also directed to compounds of the formula I, wherein R.sub.2 is halogen and to compositions containing a compound of the formula I which exhibit antidepressant activity.
摘要翻译：制备具有式I的抗抑郁活性的化合物及其异构体的一步法，其中R1，R2，Z和A具有权利要求中所示的含义，该方法包括：将式II其中Z，A，R 1和R 2具有权利要求中所述的含义，R 3代表氢或C 1-4烷基，在脱水剂的存在下分离式R 3 OH的化合物。本发明还涉及式I化合物，其中R 2是卤素，以及含有表现出抗抑郁活性的式I化合物的组合物。

3. 发明授权

US4871846A Process for the preparation of condensed as-triazine derivatives 失效
标题翻译：缩合的三嗪衍生物的制备方法
公开(公告)号：US4871846A
公开(公告)日：1989-10-03
申请号：US43600
申请日：1987-04-28
申请人： Sandor Batori , Gyorgy Hajos , Andras Messmer , Pal Benko , Laszlo Pallos , Lujza Petocz , Katalin Grasser , Ibolya Kosoczky , Eniko Szirt nee Kiszelly
发明人： Sandor Batori , Gyorgy Hajos , Andras Messmer , Pal Benko , Laszlo Pallos , Lujza Petocz , Katalin Grasser , Ibolya Kosoczky , Eniko Szirt nee Kiszelly
IPC分类号： C07D215/12 , C07D215/58 , C07D217/16 , C07D217/18 , C07D471/04
CPC分类号： C07D471/04 , C07D215/58 , C07D217/18
摘要： A process for the preparation of condensed as-triazinium derivatives of the formula I ##STR1## and isomers thereof, wherein R.sub.1 inter alia is an alkyl group, R.sub.2 inter alia is hydrogen or an alkyl group and R.sub.3 is hydrogen and where Z is a group of the formula a or b ##STR2## which comprises reacting a compound of the formula II ##STR3## where Y is a group of the formula c or d ##STR4## with a compound of the formula IIaNH.sub.2 --CO--R.sub.2 (IIa)in the presence of a dehydrating agent. The advantage of the process is that it consists of fewer reaction steps and provides higher yields than the known methods. The compounds of formula I are pharmaceutically active known derivatives.
摘要翻译：一种制备式I（I）的缩合的三嗪鎓衍生物及其异构体的方法，其中R1特别是烷基，R 2特别是氢或烷基，R 3是氢，并且其中Z 是式a或b的基团（a）（b），其包括使式II的化合物（II）其中Y是式c的基团或d （c）在脱水剂存在下，用式IIa NH 2 -CO-R 2（IIa）化合物与（d）化合物反应。该方法的优点在于其由较少的反应步骤组成，并提供比已知方法更高的产率。式I的化合物是药学活性的已知衍生物。

4. 发明授权

US4324786A Pyrido[2,3-e]-as-triazine derivatives and pharmaceutical compositions 失效
标题翻译：吡啶并[2,3-e] -as-三嗪衍生物和药物组合物
公开(公告)号：US4324786A
公开(公告)日：1982-04-13
申请号：US143778
申请日：1980-04-25
申请人： Andras Messmer , Pal Benko , Gyorgy Hajos , Lujza Petocz , Ibolya Kosoczky , Peter Gorog
发明人： Andras Messmer , Pal Benko , Gyorgy Hajos , Lujza Petocz , Ibolya Kosoczky , Peter Gorog
IPC分类号： A61K31/53 , A61K31/535 , A61P25/00 , A61P25/04 , A61P25/20 , A61P29/00 , C07D221/04 , C07D253/10 , C07D471/04 , C07D471/14
CPC分类号： C07D471/04
摘要： New pyrido[2,3-e]-as-triazine derivatives of the general formula (I), ##STR1## wherein R.sup.1 and R.sup.2 each stand for a C.sub.1-20 alkylcarbonyl, halogenated (C.sub.1-4 alkyl)-carbonyl, C.sub.1-4 alkoxycarbonyl, benzoyl, phenyl-(C.sub.1-4 alkyl)-carbonyl or phenyl-(C.sub.2-4 alkenyl)-carbonyl group or a 5-10-membered mono- or bicyclic nitrogen-containing heterocyclic acid residue (preferably a pyridylcarbonyl group) containing optionally one or more additional nitrogen, oxygen and/or sulfur atoms in the heterocyclic ring, and optionally one or more identical or different substituents selected from the group consisting of halogen, C.sub.1-4 alkoxy, nitro and hydroxy are attached to the aromatic or heterocyclic rings, furthermore one of R.sup.1 and R.sup.2 may also stand for hydrogen atom, orR.sup.1 and R.sup.2 may form, together with the adjacent nitrogen atoms, a pyrazole-2,4 ring having optionally a C.sub.1-6 alkyl substituent in position 3, andR.sup.3 stands for hydrogen, halogen, C.sub.1-4 alkoxy, amino, mono-(C.sub.1-6 alkyl)-amino, di-(C.sub.1-6 alkyl)-amino, hydroxy, alkylated or acylated hydroxy, morpholino, piperazino, N-(C.sub.1-6 alkyl)-piperazino, N-benzylpiperazino or N-pyridylpiperazino group,and pharmaceutically acceptable acid addition salts thereof are prepared by acylating the respective 1,2-unsubstituted 1,2-dihydro-pyrido[2,3-e]-as-triazine derivatives.The new compounds according to the invention act on the central nervous system and exert sedative, analgesic, narcosis potentiating, tetrabenazine antagonizing and antiphlogistic effects. The new compounds according to the invention can be applied to advantage in the therapy.
摘要翻译：通式（I）的新的吡啶并[2,3-e] -as-三嗪衍生物，其中R 1和R 2各自代表C 1-20烷基羰基，卤代（C 1-4烷基） - 羰基，C 1-4烷氧基羰基，苯甲酰基，苯基 - （C 1-4烷基） - 羰基或苯基 - （C 2-4烯基） - 羰基或5-10元单环或双环含氮杂环酸残基（优选含有任选的一个或多个杂环中的一个或多个另外的氮，氧和/或硫原子，以及任选地一个或多个相同或不同的选自卤素，C 1-4烷氧基，硝基和羟基的取代基被连接到芳族或杂环，此外，R 1和R 2中的一个也可以代表氢原子，或者R 1和R 2可以与相邻的氮原子一起形成具有任选地C 1-6烷基取代基的吡唑-2,4环的位置 3，R3代表氢，卤素，C1-4烷氧基，氨基，单 - （C1-6烷基） - 氨基，二 - （C1-6烷基） - 氨羟基，烷基化或酰化羟基，吗啉代，哌嗪子基，N-（C 1-6烷基） - 哌嗪基，N-苄基哌嗪子基或N-吡啶基哌嗪子基及其药学上可接受的酸加成盐，未取代的1,2-二氢 - 吡啶并[2,3-e] -as-三嗪衍生物。根据本发明的新化合物作用于中枢神经系统，并施加镇静，止痛，麻醉增强，丁苯那嗪拮抗和消炎作用。根据本发明的新化合物可以在治疗中有利地应用。

5. 发明授权

US4419355A Condensed as-triazine derivatives and method of using the same 失效
标题翻译：缩合三嗪衍生物及其使用方法
公开(公告)号：US4419355A
公开(公告)日：1983-12-06
申请号：US283971
申请日：1981-07-16
申请人： Ibolya Kosoczky , Eva Toncsev, nee Ravasz , Pal Benko , Laszlo Pallos , Lujza Petocz , Sandor Batori , Gyorgy Hajos , Andras Messmer , Katalin Grasser
发明人： Ibolya Kosoczky , Eva Toncsev, nee Ravasz , Pal Benko , Laszlo Pallos , Lujza Petocz , Sandor Batori , Gyorgy Hajos , Andras Messmer , Katalin Grasser
IPC分类号： C07D471/04 , A61K31/53 , A61P25/24 , A61P25/26 , C07D253/10 , C07D487/04 , C07D253/08
CPC分类号： C07D487/04
摘要： The invention relates to new condensed as-triazine derivatives of the general formula (I) ##STR1## wherein Z represents a buta-1,3-dienyl group or a group of the formula (a), (b), (c) or (d) ##STR2## R.sub.1 denotes a C.sub.1-10 alkyl group, an oxo group or a C.sub.6-10 aryl or C.sub.6-10 aryl-(C.sub.1-3 alkyl) group optionally substituted by one or more identical or different substituents selected from the group consisting of amino, nitro, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy and halogen,R.sub.2 stands for hydrogen, C.sub.1-10 alkyl or amino,R.sub.3 represents hydrogen, C.sub.1-10 alkyl or C.sub.6-10 aryl or C.sub.6-10 aryl-(C.sub.1-3 alkyl) optionally substituted by one or more identical or different substituents selected from the group consisting of nitro, amino, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy and halogen,X.sup.- denotes an anion, andn is 0 or 1,with the proviso that if n is O, R.sub.1 is other than an oxo group and R.sub.1 ' and R.sub.2 ' form together a double bond, and with the further provisos that if n is 1, R.sub.1 represents an oxo group and the symbols R.sub.1 ' and R.sub.2 ' are not present, and if Z is a buta-1,3-dienyl group and R.sub.1 denotes an oxo group, R.sub.3 is other than unsubstituted phenyl.The new compounds of the general formula (I) can be prepared by cyclizing the compounds of the general formula (II) or (V), wherein R.sub.1, Z, R.sub.3 and X.sup.- have the above defined meanings, R.sub.4 is a leaving group and R.sub.7 represents hydrogen or C.sub.1-10 alkyl.The new compounds of the general formula (I) possess a valuable antidepressant effect and can advantageously be used in the therapy.
摘要翻译：本发明涉及通式（I）的新的缩合的三嗪衍生物，其中Z代表丁-1,3-二烯基或式（a），（b），（ c）或（d）R1表示任选被一个或多个相同的C 1-6烷基，氧代基或C 6-10芳基或C 6-10芳基 - （C 1-3烷基）或选自氨基，硝基，C 1-6烷基，C 1-6烷氧基，羟基和卤素的不同取代基，R 2代表氢，C 1-10烷基或氨基，R 3表示氢，C 1-10烷基或C 6- 芳基或任选被一个或多个相同或不同的选自硝基，氨基，C 1-6烷基，C 1-6烷氧基，羟基和卤素的取代基取代的芳基或C 6-10芳基 - （C 1-3烷基）表示阴离子，n为0或1，条件是如果n为O，则R1不是氧代基，R1'和R2'一起形成双键，另外条件是，如果n为1， R1代表氧代基团， mbols R1'和R2'不存在，并且如果Z是丁-1,3-二烯基并且R 1表示氧代基，则R 3不是未取代的苯基。通式（I）的新化合物可以通过使通式（II）或（V）的化合物环化来制备，其中R1，Z，R3和X具有上述定义，R4是离去基团， R 7表示氢或C 1-10烷基。通式（I）的新化合物具有有价值的抗抑郁作用，可有利地用于治疗。

6. 发明授权

US4324894A Aminoisoquinoline derivatives 失效
标题翻译：氨基异喹啉衍生物
公开(公告)号：US4324894A
公开(公告)日：1982-04-13
申请号：US138843
申请日：1980-04-10
申请人： Pal Benko , Andras Gelleri , Gyorgy Hajos , Andras Messmer , Laszlo Pallos , Lujza Petocz , Ibolya Kosoczky , Katalin Grasser , Peter Gorog , Eniko Szirt nee Kiszelly
发明人： Pal Benko , Andras Gelleri , Gyorgy Hajos , Andras Messmer , Laszlo Pallos , Lujza Petocz , Ibolya Kosoczky , Katalin Grasser , Peter Gorog , Eniko Szirt nee Kiszelly
IPC分类号： A61K31/47 , A61K31/472 , A61K31/4725 , A61K31/495 , A61P25/00 , A61P25/04 , C07D217/22 , C07D217/24 , C07D401/12 , C07D413/04 , C07D403/14
CPC分类号： C07D217/22 , C07D217/24
摘要： Novel aminoisoquinoline derivatives of the general formula (I) ##STR1## wherein R.sub.1 represents a hydrogen atom or a C.sub.1-4 alkyl group,R.sub.2 represents a hydrogen atom,R.sub.3 represents a hydrogen atom,R.sub.4 represents a morpholinyl group or a piperazinyl group substituted with a pyridyl group, andpharmaceutically acceptable acid addition salts and quaternary derivatives thereof have been prepared. The novel compounds exert narcosis potentiating effects.
摘要翻译：通式（I）的新型氨基异喹啉衍生物其中R 1表示氢原子或C 1-4烷基，R 2表示氢原子，R 3表示氢原子，R 4表示吗啉基或哌嗪基已经制备了被吡啶基取代的基团，以及其药学上可接受的酸加成盐和其季衍生物。新型化合物发挥麻醉加强作用。

7. 发明授权

US4395413A Oxime ethers and pharmaceutical compositions containing the same 失效
标题翻译：肟醚和含有它的药物组合物
公开(公告)号：US4395413A
公开(公告)日：1983-07-26
申请号：US162674
申请日：1980-06-24
申请人： Zoltan Budai , Aranka Lay nee Konya , Tibor Mezei , Lujza Petocz , Katalin Grasser , Ibolya Kosoczky , Eniko Szirt nee Kiszelly , Peter Gorog
发明人： Zoltan Budai , Aranka Lay nee Konya , Tibor Mezei , Lujza Petocz , Katalin Grasser , Ibolya Kosoczky , Eniko Szirt nee Kiszelly , Peter Gorog
IPC分类号： A61K31/15 , A61K31/495 , A61P25/04 , C07C67/00 , C07C239/00 , C07C249/10 , C07C251/58 , C07D295/02 , C07D295/088 , C07D295/08
CPC分类号： C07D295/088 , Y10S514/926 , Y10S514/927
摘要： The invention relates to novel oxime ethers of the general formula /I/ and acid addition salts and quaternary ammonium derivatives thereof, ##STR1## wherein A represents a C.sub.2-6 straight or branched alkylene chain,R and R.sup.1 each represent a C.sub.1-6 alkyl group or they form together with the adjacent nitrogen atom a heterocyclic ring containing 4 to 7 carbon atoms and optionally a further hetero atom, i.e. an oxygen, sulfur or nitrogen atom, and said ring may be optionally substituted by a C.sub.1-3 alkyl, phenyl or benzyl group,R.sup.2 and R.sup.3 each denote a hydrogen atom or together form a valency bond,R.sup.4 denotes a C.sub.1-10 alkyl or C.sub.2-10 alkenyl group, andn denotes an integer from 3 to 7.The compounds of the general formula /I/ are prepared according to the invention by reacting a cycloalkane derivative of the general formula /II/ ##STR2## wherein R.sup.2, R.sup.3, R.sup.4 and n have the same meaning as above, whereasY denotes an oxygen or sulphur atom or a .dbd.N--OH group with an aminoalkyl derivative of the general formula /III/ ##STR3## wherein R, R.sup.1 and A have the same meaning as stated above andZ means a halogen atom or a H.sub.2 N--O-- group or a salt thereof in the presence of a basic condensing agent.The new compounds of the general formula /I/ possess valuable nicotine-lethality inhibiting, local anaesthetic, analgesic effects, which are, in case of certain compounds, complemented by anti-hypertensive, maximum electroshock and tetracorspasm inhibiting, ulcus inhibiting and motility inhibiting effects, and can be applied to advantage in the therapy.
摘要翻译：本发明涉及通式I I的新型肟醚及其酸加成盐和季铵衍生物，其中A表示C2-6直链或支链亚烷基链，R和R1各自表示C1 -6烷基，或者它们与相邻的氮原子一起与含有4至7个碳原子的杂环和任选的另外的杂原子（即氧，硫或氮原子）一起形成，并且所述环可以任选地被C 1-3 烷基，苯基或苄基，R2和R3各自表示氢原子或一起形成价键，R4表示C1-10烷基或C2-10烯基，n表示3至7的整数。根据本发明通过使通式/ II / IMAGE / II /的环烷烃衍生物与其中R2，R3，R4和n具有与上述相同的含义反应制备通式/ I / I，而Y表示氧或硫原子或a =具有氨基烷基衍生物的N-OH基团通式/ III / / III /其中R，R 1和A具有与上述相同的含义，Z表示在碱性缩合剂存在下的卤素原子或H 2 N-O-基或其盐。新型化合物/ I /具有有价值的尼古丁杀伤力抑制，局部麻醉，止痛作用，在某些化合物的情况下，补充有抗高血压，最大电休克和四疣抑制作用，抑制溃疡和运动抑制作用，并且可以在治疗中有利地应用。

8. 发明授权

US4208410A Dibenzo[d,g][1,3,6]dioxazocine derivatives 失效
标题翻译：二苯并[d，g] [1,3,6]二氧杂吖庚因衍生物
公开(公告)号：US4208410A
公开(公告)日：1980-06-17
申请号：US927934
申请日：1978-07-25
申请人： Laszlo Rozsa , Lujza Petocz , Katalin Grasser , Ibolya Kosoczky , Eniko Kiszelly , Jozsef Nagy
发明人： Laszlo Rozsa , Lujza Petocz , Katalin Grasser , Ibolya Kosoczky , Eniko Kiszelly , Jozsef Nagy
IPC分类号： A61K31/553 , C07D273/00 , C07D273/01 , C07D267/22 , A61K31/395
CPC分类号： C07D273/00 , Y10S514/818
摘要： This invention relates to novel dibenzo[d,g][1,3,6]dioxazocine derivatives represented by the general formula I ##STR1## wherein R.sub.1 and R.sub.2 independently represent hydrogen, halogen, cyano or trifluoromethyl,Y stands for hydrogen or a group of formula ##STR2## wherein A stands for a straight or branched chained alkylene having from 2 to 5 carbon atoms andR.sub.3 and R.sub.4 independently stand for an alkyl having from 1 to 4 carbon atoms, orR.sub.3 and R.sub.4 together with the nitrogen atom they are attached to and optionally together with a further nitrogen atom or with an additional oxygen atom may form a five- or six-membered heterocyclic ring optionally substituted with an alkyl having from 1 to 4 carbon atoms,and pharmaceutically acceptable acid addition salts thereof formed with an inorganic or organic acid.The above compounds possess valuable pharmaceutical properties, for instance they are effective local anaesthetics and can be used for treating Parkinson syndrome.
摘要翻译：本发明涉及由通式I（I）表示的新的二苯并[d，g] [1,3,6]二氧杂吖庚因衍生物，其中R 1和R 2独立地表示氢，卤素，氰基或三氟甲基，Y代表氢或一组式（I）其中A代表具有2至5个碳原子的直链或支链链状亚烷基，R3和R4独立代表具有1至4个碳原子的烷基，或R3和R4与氮原子一起它们与另外的氮原子或与另外的氧原子连接并且可选地与另外的氧原子连接的原子可以形成任选被具有1至4个碳原子的烷基取代的五元或六元杂环，及其药学上可接受的酸加成盐由无机或有机酸形成。上述化合物具有有价值的药物性质，例如它们是有效的局部麻醉剂，并且可用于治疗帕金森综合征。

9. 发明授权

US4342766A Novel dihydro-as-triazino[5,6-c]quinoline derivatives and a process for the preparation thereof 失效
标题翻译：新型二氢 - 三嗪并[5,6-c]喹啉衍生物及其制备方法
公开(公告)号：US4342766A
公开(公告)日：1982-08-03
申请号：US254763
申请日：1981-04-16
申请人： Edit Berenyi nee Poldermann , Peter Gorog , Katalin Grasser , Ibolya Kosoczky , Agnes Koracs nee Palotay , Lujza Petocz
发明人： Edit Berenyi nee Poldermann , Peter Gorog , Katalin Grasser , Ibolya Kosoczky , Agnes Koracs nee Palotay , Lujza Petocz
IPC分类号： A61K31/4745 , A61K31/53 , A61P23/00 , A61P25/04 , A61P25/08 , A61P25/20 , A61P29/00 , C07D471/04 , A61K31/395
CPC分类号： C07D471/04
摘要： New compounds are disclosed of the formulae ##STR1## or pharmaceutically effective salts thereof, wherein R is hydrogen, C.sub.1-12 alkyl, or R is phenyl or phenyl-C.sub.1 to C.sub.4 alkyl wherein the phenyl can be substituted with 1 to 3 halogen, C.sub.1 to C.sub.4 alkyl, or C.sub.1 to C.sub.4 alkoxy substituents; andX.sub.1, X.sub.2 and X.sub.3 are hydrogen, C.sub.1 to C.sub.6 alkanoyl, or C.sub.1 to C.sub.6 haloalkanoyl; and where X.sub.1 is hydrogen, X.sub.2 and X.sub.3 are not simultaneously hydrogen. The compounds possess antiphlogistic, analgesic, anticonvulsive, or tranquilizing properties.
摘要翻译：公开了新的化合物或其药学有效盐，其中R是氢，C 1-12烷基或R是苯基或苯基-C 1至C 4烷基，其中苯基可被1至3个卤素取代，C 1 至C 4烷基或C 1至C 4烷氧基取代基; 且X 1，X 2和X 3为氢，C 1至C 6烷酰基或C 1至C 6卤代烷酰基; 并且其中X1为氢，X2和X3不同时为氢。该化合物具有消炎，镇痛，抗惊厥或镇静作用。

10. 发明授权

US4303660A Pyrazolo[1,5-c]quinazoline derivatives and analgesic compositions containing them 失效
标题翻译：吡唑并[1,5-c]喹唑啉衍生物和含有它们的镇痛组合物
公开(公告)号：US4303660A
公开(公告)日：1981-12-01
申请号：US150349
申请日：1980-05-16
申请人： Edit Berenyi nee Poldermann , Eniko Szirt nee Kiszelly , Peter Gorog , Lujza Petocz , Ibolya Kosoczky , Agnes Kovacs nee Palotai , Gabriella rmos nee Lassu
发明人： Edit Berenyi nee Poldermann , Eniko Szirt nee Kiszelly , Peter Gorog , Lujza Petocz , Ibolya Kosoczky , Agnes Kovacs nee Palotai , Gabriella rmos nee Lassu
IPC分类号： A61K31/4162 , A61K31/4745 , A61K31/505 , A61K31/519 , A61P1/00 , A61P1/04 , A61P25/04 , A61P29/00 , C07D231/16 , C07D487/04
CPC分类号： C07D487/04 , C07D231/16
摘要： The invention relates to novel pyrazolo[1,5-c]quinazoline derivatives of the general formula I ##STR1## wherein R represents a hydrogen atom, a C.sub.1-4 alkyl group or an acyl group,R.sub.1 represents a hydrogen atom, a C.sub.1-12 alkyl group, a C.sub.3-8 cycloalkyl group, a C.sub.2-4 alkenyl group, an aralkyl group, wherein the alkyl group has 1 to 4 carbon atoms, a phenylalkenyl group, wherein the alkenyl group has 2 to 4 carbon atoms, furthermore a carboxy group or a phenyl group optionally substituted by one or more substituents selected from the group consisting of halogen, hydroxy, C.sub.1-4 alkoxy, nitro or di(C.sub.1-4 alkyl)amino groups, orR and R.sub.1 may form together a valence bond,R.sub.2 represents a hydrogen atom, a C.sub.1-4 alkyl or a phenyl group, orR.sub.1 and R.sub.2 may form together a C.sub.2-7 alkylene group,R.sub.3 represents a nitro group, an amino group, an alkylamino group, a dialkylamino group, wherein the alkyl groups have 1 to 4 carbon atoms, an alkylideneimino group, wherein the alkylidene group has 1 to 4 carbon atoms, a benzylideneimino group or an acylamino group,and pharmaceutically acceptable acid addition salts thereof.The novel compounds of the general formula I can be employed primarily as analgesic agents.
摘要翻译：本发明涉及通式I（XIX）的新颖的吡唑并[1,5-c]喹唑啉衍生物，其中R表示氢原子，C1-4烷基或酰基，R1表示氢原子， C1-12烷基，C3-8环烷基，C2-4烯基，其中烷基具有1至4个碳原子的芳烷基，苯基烯基，其中烯基具有2至4个碳原子此外，羧基或任选被一个或多个选自卤素，羟基，C 1-4烷氧基，硝基或二（C 1-4烷基）氨基的取代基取代的苯基，或R和R 1可以一起形成价键，R2表示氢原子，C1-4烷基或苯基，或R1和R2可以一起形成C2-7亚烷基，R3表示硝基，氨基，烷基氨基，二烷基氨基基团，其中烷基具有1至4个碳原子，亚烷基亚氨基，其中亚烷基具有1至4个碳 n原子，亚苄基亚氨基或酰氨基，及其药学上可接受的酸加成盐。通式I的新化合物可以主要用作止痛剂。

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