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1. 发明申请

WO1998014451A1 FUSED PYRAZOLE DERIVATIVE AND PROCESS FOR ITS PREPARATION 审中-公开
标题翻译：熔融吡唑衍生物及其制备方法
公开(公告)号：WO1998014451A1
公开(公告)日：1998-04-09
申请号：PCT/EP1997005377
申请日：1997-09-30
申请人： NOVARTIS AG , BOLD, Guido , FREI, Jörg , LANG, Marc , TRAXLER, Peter , FURET, Pascal
发明人： NOVARTIS AG
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： 3-(3-Aminobenzylamino)-4-(3-chlorophenylamino)-1H-pyrazolo[3,4-d]pyrim idine of formula (I) is described. The compound of formula (I) inhibits, in particular, tyrosine-kinase activity of the receptor for the epidermal growth factor and can be used, for example, as antitumour agent and in cases of epidermal hyperproliferation (psoriasis).
摘要翻译：描述了式（I）的3-（3-氨基苄基氨基）-4-（3-氯苯基氨基）-1H-吡唑并[3,4-d]嘧啶。式（I）的化合物特别地抑制表皮生长因子受体的酪氨酸激酶活性，并且可以用作例如抗肿瘤剂和表皮过度增生（牛皮癣）的情况。

2. 发明申请

WO1997027199A1 PYRROLOPYRIMIDINES AND PROCESSES FOR THEIR PREPARATION 审中-公开
标题翻译：吡咯并嘧啶及其制备方法
公开(公告)号：WO1997027199A1
公开(公告)日：1997-07-31
申请号：PCT/EP1997000127
申请日：1997-01-13
申请人： NOVARTIS AG , TRAXLER, Peter , FREI, Jörg , BOLD, Guido
发明人： NOVARTIS AG
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： There are described compounds of formula (I) wherein R1 and R2 are as defined in the description, Q is heterocyclyl bonded via a ring nitrogen atom and having formula (IA) wherein R3 and R4 and m and n are as defined in the description, the ring marked A is a heterocyclyl having from 5 to 9 ring atoms and having at least one saturated bond, it being possible for a further ring hetero atom selected from O and S to be present in addition to the bonding nitrogen atom, the ring system marked B is a free or benzo-, thieno-, furo-, pyrrolo- or dihydropyrrolo-fused carbocyclic ring having from 5 to 9 carbon atoms that is fused to the ring A and may be unsaturated, partially saturated or fully saturated, and the bond marked by a parallel dotted line between the ring systems marked A and B is either a single bond or a double bond, and a salt thereof where at least one salt-forming group is present. The compounds are inhibitors of protein kinases and have, for example, antitumour activity.
摘要翻译：描述了式（I）的化合物，其中R 1和R 2如描述中所定义，Q是通过环氮原子并具有式（IA）的杂环基，其中R 3和R 4以及m和n如说明书中所定义，标记为A的环是具有5至9个环原子并且具有至少一个饱和键的杂环基，除了键合氮原子之外，还可以存在另外的选自O和S的环杂原子，环系标记的B是具有5至9个碳原子的游离或苯并 - ，噻吩并 - 呋喃并 - 吡咯并 - 二氢吡咯并 - 稠合的碳环，其与环A稠合并且可以是不饱和的，部分饱和的或完全饱和的，并且标记为A和B的环系统之间的平行虚线标记的键是单键或双键，以及其中存在至少一个成盐基团的盐。这些化合物是蛋白激酶的抑制剂，并且具有例如抗肿瘤活性。

3. 发明申请

WO1998014450A1 PYRIMIDINE DERIVATIVES AND PROCESSES FOR THE PREPARATION THEREOF 审中-公开
标题翻译：吡嗪衍生物及其制备方法
公开(公告)号：WO1998014450A1
公开(公告)日：1998-04-09
申请号：PCT/EP1997005369
申请日：1997-09-30
申请人： NOVARTIS AG , BOLD, Guido , FREI, Jörg , LANG, Marc , TRAXLER, Peter
发明人： NOVARTIS AG
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： 4-Amino-1H-pyrazolo[3,4-d]pyrimidine derivatives of formula (I) wherein the substituents are as defined in claim 1, are described. These compounds inhibit the tyrosine kinase activity of the receptor for epidermal growth factor (EGF) and c-erbB2 kinase and can be used as anti-tumour agents.
摘要翻译：描述了其中取代基如权利要求1中所定义的式（I）的4-氨基-1H-吡唑并[3,4-d]嘧啶衍生物。这些化合物抑制表皮生长因子（EGF）和c-erbB2激酶受体的酪氨酸激酶活性，可用作抗肿瘤剂。

4. 发明申请

WO1998007726A1 SUBSTITUTED PYRROLOPYRIMIDINES AND PROCESSES FOR THEIR PREPARATION 审中-公开
标题翻译：取代的吡咯并嘧啶及其制备方法
公开(公告)号：WO1998007726A1
公开(公告)日：1998-02-26
申请号：PCT/EP1997004564
申请日：1997-08-21
申请人： NOVARTIS AG , TRAXLER, Peter , BOLD, Guido , LANG, Marc , FREI, Jörg
发明人： NOVARTIS AG
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： There are described 7H-pyrrolo[2,3-d]pyrimidine derivatives of formula (I) in which the substituents are as defined in claim 1. These compounds inhibit the tyrosine kinase activity of the receptor for the epidermal growth factor (EGF) and c-erbB2kinase and can be used as anti-tumour agents.
摘要翻译：描述了式（I）的7H-吡咯并[2,3-d]嘧啶衍生物，其中取代基如权利要求1中所定义。这些化合物抑制表皮生长因子（EGF）受体的酪氨酸激酶活性和 c-erbB2激酶，可用作抗肿瘤药物。

5. 发明申请

WO1998014449A1 FUSED PYRAZOLE DERIVATIVES AND PROCESSES FOR THEIR PREPARATION 审中-公开
标题翻译：熔化的吡唑衍生物及其制备方法
公开(公告)号：WO1998014449A1
公开(公告)日：1998-04-09
申请号：PCT/EP1997005368
申请日：1997-09-30
申请人： NOVARTIS AG , BOLD, Guido , FREI, Jörg , LANG, Marc , TRAXLER, Peter , FURET, Pascal
发明人： NOVARTIS AG
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： 4-Amino-1H-pyrazolo[3,4-d]pyrimidine derivatives of formula (I) in which m, n and v are each, independently of one another, 0 or 1, R is hydrogen or methyl, R1 is chlorine or methyl which is in each case located in position 3 of the phenyl radical, X is the group NH(CH-R7)t in which t is 0, 1 or 2 and R7 is hydrogen, or the group (C[R3]-R4)q, in which q is 0, and R2 is nitro, cyano, amino, dimethylamino-lower-alkyleneamino, 4-pyridylcarbonylamino, 2-methylpropanoylamino, tert-butyloxycarbonylamino, or methyl which is substituted by amino, C1-C5-alkanoylamino, tert-butyloxycarbonylamino or benzoylamino, with the exception of 3-(3-aminobenzylamino)-4-(3-chlorophenylamino)-1H-pyrazolo[3,4-d]pyrimidine are described. The compounds of formula (I) inhibit in particular the tyrosine kinase activity of the receptor for epidermal growth factor and can be used, for example, for epidermal hyperproliferation (psoriasis) and as antitumor agents.
摘要翻译：式（I）的4-氨基-1H-吡唑并[3,4-d]嘧啶衍生物，其中m，n和v各自彼此独立地为0或1，R为氢或甲基，R 1为氯或甲基，其各自位于苯基的位置3，X为基团NH（CH-R 7）t，其中t为0,1或2，R7为氢，或基团（C [R3] -R4 ）q，其中q为0，R 2为硝基，氰基，氨基，二甲基氨基 - 低级亚烷基氨基，4-吡啶基羰基氨基，2-甲基丙酰基氨基，叔丁氧基羰基氨基或被氨基，C 1 -C 5 - 烷酰基氨基，叔丁氧基羰基氨基或苯甲酰基氨基，但3-（3-氨基苄基氨基）-4-（3-氯苯基氨基）-1H-吡唑并[3,4-d]嘧啶除外。式（I）化合物特别地抑制表皮生长因子受体的酪氨酸激酶活性，并且可以用于例如表皮过度增殖（牛皮癣）和抗肿瘤剂。

6. 发明申请

WO1998003476A1 ANILINOPEPTIDE DERIVATIVES 审中-公开
标题翻译：抗胰岛素衍生物
公开(公告)号：WO1998003476A1
公开(公告)日：1998-01-29
申请号：PCT/EP1997003804
申请日：1997-07-16
申请人： NOVARTIS AG , FÄSSLER, Alexander , BOLD, Guido , CAPRARO, Hans-Georg , LANG, Marc
发明人： NOVARTIS AG
IPC分类号： C07C271/22
CPC分类号： C07D295/135 , C07C271/22 , C07D231/12 , C07D233/56 , C07D249/08
摘要： The invention relates to compounds of formula (I), in which R1 and R2 are, independently of each other, lower alkyl or lower alkoxy-lower alkyl; R3 and R4 are, independently of each other, sec-lower alkyl or tert-lower alkyl; R5 is phenyl or cyclohexyl; and R6 and R7 are, independently of each other, lower alkyl, or, together with the linking nitrogen atom, pyrrolidino, piperidino, 4-lower alkylpiperidino, 1,2,4-triazol-1-yl or 1,2,4-triazol-4-yl; or a salt thereof, provided that at least one salt-forming group is present. These compounds are inhibitors of HIV protease and are therefore suitable, for example, for treating AIDS or its preliminary stages.
摘要翻译：本发明涉及式（I）化合物，其中R 1和R 2彼此独立地为低级烷基或低级烷氧基 - 低级烷基; R 3和R 4彼此独立地为低级烷基或叔 - 低级烷基; R5是苯基或环己基; 和R 6和R 7彼此独立地为低级烷基，或与连接氮原子一起为吡咯烷子基，哌啶子基，4-低级烷基哌啶子基，1,2,4-三唑-1-基或1,2,4-三唑-1-基，三唑-4-基; 或其盐，条件是存在至少一个成盐基团。这些化合物是HIV蛋白酶的抑制剂，因此适用于例如用于治疗AIDS或其初级阶段。

7. 发明申请

WO1997019055A1 AZAHEXANE DERIVATIVES AS SUBSTRATE ISOSTERS OF RETROVIRAL ASPARATE PROTEASES 审中-公开
标题翻译：作为替代天竺葵蛋白的基质间隔物的阿拉伯糖衍生物
公开(公告)号：WO1997019055A1
公开(公告)日：1997-05-29
申请号：PCT/EP1996004968
申请日：1996-11-13
申请人： NOVARTIS AG , FÄSSLER, Alexander , BOLD, Guido , CAPRARO, Hans-Georg , LANG, Marc
发明人： NOVARTIS AG
IPC分类号： C07C271/22
CPC分类号： C07C271/22 , Y10S514/934
摘要： The invention relates to compounds of formula (I): wherein R1 and R10 are each independently of the other lower alkoxycarbonyl; either R2, R3 and R4 are each independently of the other C1-C4alkyl and R7, R8 and R9 are each selected from hydrogen and C1-C4alkyl, with not more than 2 of the radicals being hydrogen; or R7, R8 and R9 are each independently of the other C1-C4alkyl and R2, R3 and R4 are each selected from hydrogen and C1-C4alkyl, with 1 or 2 of the radicals being hydrogen; R5 is phenyl or cyclohexyl; and R6 is phenyl or cyanophenyl; or salts thereof; those compounds are inhibitors of retroviral aspartate proteases and are effective, for example, against HIV.
摘要翻译：本发明涉及式（I）化合物：其中R 1和R 10各自独立地为低级烷氧基羰基; R 2，R 3和R 4各自独立地为C 1 -C 4烷基，R 7，R 8和R 9各自选自氢和C 1 -C 4烷基，不超过2个基团为氢; 或R 7，R 8和R 9各自独立地为C 1 -C 4烷基，R 2，R 3和R 4各自选自氢和C 1 -C 4烷基，其中1或2个是氢; R5是苯基或环己基; R6为苯基或氰基苯基; 或其盐; 这些化合物是逆转录病毒天冬氨酸蛋白酶的抑制剂，并且是有效的，例如针对HIV。

8. 发明申请

WO1997027179A2 ANTIRETROVIRAL BASES 审中-公开
标题翻译：抗逆转基因
公开(公告)号：WO1997027179A2
公开(公告)日：1997-07-31
申请号：PCT/EP1997000139
申请日：1997-01-14
申请人： NOVARTIS AG , FREI, Jörg , FÄSSLER, Alexander , FLÖRSHEIMER, Andreas , HAMY, François , KLIMKAIT, Thomas
发明人： NOVARTIS AG
IPC分类号： C07D219/12
CPC分类号： C07D221/14 , A61K31/473 , C07D219/04 , C07D219/12 , C07D271/12 , C07D473/40
摘要： The invention relates to the use of a compound of formula (I), wherein R1 and R2 are independently amino, N-alkylamino, N,N-dialkylamino, cycloalkylamino, amidino, N-lower alkylamidino, N,N-di-lower alkylamidino, guanidino, N-lower alkylguanidino, N,N-di-lower alkylguanidino or (a); X and Y are independently selected from the group consisting of -(CH2)b-, (b), (c) and -(CH2)g-Cycloalkylen-(CH2)h-; Z is, independently of X and Y, -(CH2)b-, (d) or (e), wherein R is hydrogen or lower alkyl; Q is aryl, arylcarbonyl, arylaminocarbonyl, heterocyclyl, heterocyclylcarbonyl or heterocyclylaminocarbonyl, aryl or heterocyclyl whenever mentioned containing 2 or more annelated rings, a is 2 to 4, b is 2-7, c, d, e and f is 1 to 3, respectively, g and h is 0 to 3, respectively, i is 2 to 7 and k is 1 to 3, with the proviso that Q is arylcarbonyl, arylaminocarbonyl, heterocyclylcarbonyl or heterocyclylaminocarbonyl only if Z is a bivalent radical of formula (f) or (g); a tautomer thereof, or a salt thereof, as antiretroviral therapeutic (also for prophylaxis) inhibiting the interaction of transcriptional regulators with retroviral response elements.
摘要翻译：本发明涉及式（I）化合物的用途，其中R 1和R 2独立地是氨基，N-烷基氨基，N，N-二烷基氨基，环烷基氨基，脒基，N-低级烷基脒基，N，N-二低级烷基脒基胍基，N-低级烷基胍基，N，N-二低级烷基胍基或（a）; X和Y独立地选自 - （CH 2）b - ，（b），（c）和 - （CH 2）g-环烷基 - （CH 2）h - ; Z独立于X和Y， - （CH 2）b - ，（d）或（e），其中R是氢或低级烷基; Q为芳基，芳基羰基，芳基氨基羰基，杂环基，杂环基羰基或杂环基氨基羰基，芳基或杂环基，每当提到含有2个或更多个环状环时，a为2至4，b为2-7，c，d，e和f为1至3， g和h分别为0至3，i为2至7，k为1至3，条件是Q为芳基羰基，芳基氨基羰基，杂环基羰基或杂环基氨基羰基，只要Z是式（f）的二价基团或（G）; 其互变异构体或其盐作为抗转录病毒治疗剂（也用于预防）抑制转录调节物与逆转录病毒应答元件的相互作用。

9. 发明申请

WO1998017662A1 PHENYL-SUBSTITUTED BICYCLIC HETEROCYCLYL DERIVATIVES AND THEIR USE 审中-公开
标题翻译：苯基取代的双环杂环衍生物及其用途
公开(公告)号：WO1998017662A1
公开(公告)日：1998-04-30
申请号：PCT/EP1997005697
申请日：1997-10-16
申请人： NOVARTIS AG , TRAXLER, Peter , SEQUIN, Urs , GREEN, Jennifer, Mary , FURET, Pascal
发明人： NOVARTIS AG
IPC分类号： C07D311/36
CPC分类号： C07D215/233 , A61K31/352 , C07D311/36
摘要： The invention relates to the use of a compound of formula (I), wherein R1 and R2, independently of each other, represent hydrogen, hydroxy or lower alkoxy, or R1 and R2 together form lower alkylenedioxy; R3 is halogen, lower alkyl, halogen-substituted lower alkyl, hydroxy, phenyloxy, C3-C7-cycloalkyloxy or lower alkoxy; any R4 is, independently of R3 and independently of any other R4 if present, selected from halogen, lower alkyl, halogen-substituted lower alkyl, hydroxy, phenyloxy, C3-C7-cycloalkyloxy or lower alkoxy; X is oxygen, imino or (halogen-substituted or unsubstituted lower alkanoyl, [lower alkyl or carboxy-, lower alkoxycarbonyl-, aminocarbonyl-, N-mono- or N,N-di-lower alkylamino carbonyl]-lower alkyl; or C6-C12-aryl)-substituted imino; and n is 0, 1, 3 or 4; or a salt thereof if at least one salt-forming group is present, in the treatment of certain diseases and the inhibition of protein kinases, as well as to new compounds of formula (I) and salts thereof.
摘要翻译：本发明涉及式（I）化合物的用途，其中R 1和R 2彼此独立地表示氢，羟基或低级烷氧基，或者R 1和R 2一起形成低级亚烷基二氧基; R3是卤素，低级烷基，卤素取代的低级烷基，羟基，苯氧基，C3-C7-环烷氧基或低级烷氧基; 任何R 4独立地为R 3，独立地为任何其它R 4（如果存在），选自卤素，低级烷基，卤素取代的低级烷基，羟基，苯氧基，C 3 -C 7 - 环烷氧基或低级烷氧基; X是氧，亚氨基或（卤素取代或未取代的低级烷酰基，[低级烷基或羧基 - ，低级烷氧基羰基 - ，氨基羰基 - ，N-单 - 或N，N-二 - 低级烷基氨基羰基] - 低级烷基;或C6 -C 12 - 芳基） - 取代的亚氨基; n为0,1,3或4; 如果存在至少一种成盐基团，则可以使用它们的盐，以治疗某些疾病和抑制蛋白激酶，以及新的式（I）化合物及其盐。

10. 发明申请

WO1998031704A2 TACHYKININ ANTAGONISTS 审中-公开
公开(公告)号：WO1998031704A2
公开(公告)日：1998-07-23
申请号：PCT/EP1997007307
申请日：1997-12-29
申请人： NOVARTIS AG , NOVARTIS PHARMACEUTICALS UK LIMITED , WALPOLE, Christopher, Simon, John , PRASHAD, Mahavir , HAR, Denis
发明人： NOVARTIS AG , NOVARTIS PHARMACEUTICALS UK LIMITED
IPC分类号： C07K05/00
CPC分类号： C07K5/06165 , A61K38/00 , C07K7/22
摘要： Compounds of formula (I) wherein X is -CH2-, -CO- or direct linkage, Y is -O-, -S- or -NH-, R1 is phenyl, R2=H or phenyl and R3 is H or -CH - and their pharmaceutically acceptable salts have tachykinin antagonist activity and are useful as pharmaceuticals e.g. for the treatment of pain and migraine.
摘要翻译：其中X为-CH 2 - ， - CO-或直接键合的式（I）化合物，Y为-O - ， - S-或-NH-，R1为苯基，R2 = H或苯基，R3为H或-CH 其药学上可接受的盐具有速激肽拮抗剂活性，并且可用作药物例如用于治疗痛苦和偏头痛。

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