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公开(公告)号：EP0351435B1
公开(公告)日：1993-08-04
申请号：EP88909359.7
申请日：1988-10-29
IPC分类号： C07D237/36 , C07D495/04 , A61K31/50
CPC分类号： C07D401/04 , C07D237/36 , C07D491/04 , C07D495/04
摘要： Novel fused pyridazine compounds represented by general formula (I) (wherein R1, R2, R3 and R4, which may be the same or different, each represents hydrogen, halogen, hydroxy, nitro, amino, cyano, trifluoromethyl, alkyl, alkoxy or alkanoylamino, one of Ra and Rb represents -O-Y-NR5R6 (wherein R5 and R6, which may be the same or different, each represents hydrogen, alkyl, phenylalkyl or substituted phenylalkyl or, when taken together, R5 and R6 represent a group capable of forming a heterocyclic ring together with the adjacent nitrogen atom, and Y represents straight-chain or branched alkylene optionally having hydroxy group(s) on the chain as the substituent) and the other represents H, or Ra and Rb, which may be the same or different, each represents -O-Y-NR5R6 (wherein R5 and R6 are as defined above), W represents =CH- or =N-, X represents CH2, S, SO, SO2 or O, and the bond represented by a dotted line represents a single bond or a double bond), pharmaceutically acceptable salts or hydrates thereof, and their medicinal uses are disclosed. These compounds have the action of increasing phagocytosis of leucocytes, that of increasing phagocytosis of macrophage, that of restoring the number of leucocytes, an infection protective action, an antitumor action, etc., and can be used for prophylaxis or treatment of diseases including human immunodeficiency.
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公开(公告)号：EP0308515A1
公开(公告)日：1989-03-29
申请号：EP88902569.8
申请日：1988-03-17
发明人： NAKAO, Toru , MORITA, Kenji , HISADOME, Masao , TAKEHARA, Shuzo
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： Thienocinnoline compounds represented by general for-
(wherein R represents hydrogen, halogen or lower alkyl, Ar represents aryl, heteroaryl, or aryl or heteroaryl having at least one substituent selected from the group consisting of halogen, lower alkyl, lower alkoxy, nitro, amino, hydroxy, trifluoromethyl and lower alkanoylamino, and between 5a-position and 6-position represents either a single or a double bond) useful as anti-anxious agents, amnesia treating agents, brain function activating agents, anti-dement agents or bioprotection accelerating agents.摘要翻译： （其中R代表氢，卤素或低级烷基，Ar代表具有至少一个选自卤素，低级烷基，低级烷氧基，硝基，氨基的取代基的芳基，杂芳基或芳基或杂芳基的噻吩并喹啉化合物 ，羟基，三氟甲基和低级烷酰基氨基，以及5a-位和6-位之间代表单键或双键），用作抗焦虑剂，遗忘症治疗剂，脑功能活化剂，抗痴呆剂或生物保护促进剂 。
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3.发明公开FUSED PYRIDAZINE COMPOUNDS AND THEIR MEDICINAL USES 失效KENENSIERTE PYRIDAZIN-VERBINDUNGEN UND DEREN VERWENDUNG ALS ARZNEIMITTEL。
公开(公告)号：EP0351435A1
公开(公告)日：1990-01-24
申请号：EP88909359.7
申请日：1988-10-29
IPC分类号： C07D237/36 , C07D495/04 , A61K31/50
CPC分类号： C07D401/04 , C07D237/36 , C07D491/04 , C07D495/04
摘要： Novel fused pyridazine compounds represented by general formula (1) (wherein R 1 , R 2 , R 3 and R 4 , which may be the same or different, each represents hydrogen, halogen, hydroxy, nitro, amino, cyano, trifluoromethyl, alkyl, alkoxy or alkanoylamino, one of Ra and Rb represents -O-Y-NR 5 R 6 , (wherein R 5 and R 6 , which may be the same or different, each represents hydrogen, alkyl, phenylalkyl or substituted phenylalkyl or, when taken together, R 5 and R 6 represent a group capable of forming a heterocyclic ring together with the adjacent nitrogen atom, and Y represents straight-chain or branched alkylene optionally having hydroxy group(s) on the chain as the substituent) and the other represents H, or Ra and Rb, which may be the same or different, each represents -0-Y-NR 5 R 6 (wherein R 5 and R 6 are as defined above), W represents = CH- or = N-, X represents CH 2 , S, SO, SO 2 or 0, and the bond represented by a dotted line represents a single bond or a double bond), pharmaceutically acceptable salts or hydrates thereof and their medicinal uses are disclosed. These compounds have the action of increasing phagocytosis of leucocytes, that of increasing phagocytosis of macrophage, that of restoring the number of leucocytes, an infection protective action, an antitumor action, etc., and can be used for prophylaxis or treatment of diseases including human immunodeficiency.
摘要翻译： 由通式（I）表示的新型稠合哒嗪化合物（其中R 1，R 2，R 3和R 4可以相同或不同，各自表示氢，卤素，羟基，硝基 ，氨基，氰基，三氟甲基，烷基，烷氧基或烷酰基氨基，Ra和Rb之一表示-OY-NR 5 R 6（其中R 5和R 6可以相同或不同， 各自表示氢，烷基，苯基烷基或取代的苯基烷基，或者当R 5和R 6一起表示能够与相邻氮原子一起形成杂环的基团，Y表示直链或支链亚烷基 任选地在链上具有羟基作为取代基），另一个表示H，或可以相同或不同的R a和R b各自表示-OY-NR 5 R 6（其中R' 5＆gt;和R 6如上定义），W表示= CH-或= N-，X表示CH 2，S，SO，SO 2或O，虚线表示的键表示单键或双键 债券），药品 公开了其可接受的盐或水合物及其药用用途。 这些化合物具有增加白细胞吞噬作用，增加巨噬细胞吞噬作用，恢复白细胞数，感染保护作用，抗肿瘤作用等作用，可用于预防或治疗包括人类在内的疾病 免疫缺陷。
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公开(公告)号：EP0066628B1
公开(公告)日：1986-04-02
申请号：EP82900034.8
申请日：1981-12-09
发明人： OE, Takanori , TSURUDA, Mineo , GOTO, Kazuhiro , HISADOME, Masao
IPC分类号： C07D213/63 , C07D213/70 , C07D401/14 , A61K31/44
CPC分类号： C07D213/64 , C07D213/61 , C07D213/70 , C07D231/12 , C07D233/56 , C07D249/08
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5.发明公开FUSED PYRAZOLE COMPOUNDS, PROCESS FOR THEIR PREPARATION, AND THEIR MEDICINAL USE 失效熔化在一起的准备和吡唑方法及其使用药物。
公开(公告)号：EP0338087A1
公开(公告)日：1989-10-25
申请号：EP88908755.7
申请日：1988-10-11
IPC分类号： C07D231/56 , C07D471/04 , A61K31/495
CPC分类号： C07D231/56 , C07D471/04
摘要： Novel fused pyrazole compounds represented by general formula (I) (wherein X represents =N- or =CH-, R represents H, alkyl, alkoxy or halogen, Y¹ represents α, phenyl or phenyl substituted by halogen, alkyl or alkoxy, Y² represents β, -A²-B², H, alkyl, substituted alkyl, phenyl or phenyl substituted by a substituent selected from the group consisting of halogen, alkyl and alkoxy, provided that at least one of Y¹ and Y² represents α or β, Z¹ and Z² each represents -O-, -S- or -NR³ (wherein R³ represents H or alkyl), A¹ and A² each represents alkylene, B¹ and B² each represents carboxyl, alkoxycarbonyl or phenylalkoxycarbonyl wherein the phenyl group may optionally be substituted by a substituent selected from the group consisting of halogen, alkyl and alkoxy, acyl, -OH, acyloxy, γ or λ (wherein R¹ and R² represents H, alkyl, dialkylaminoalkyl, hydroxyalkyl or, when taken together, R¹ and R² represent a group forming a heterocyclic ring together with the adjacent nitrogen atom), and L¹ and L² each represents halogen, alkyl or alkoxy) and salts thereof, a process for their preparation and a medicinal composition containing same are disclosed. The compounds have the action of increasing phagocytosis of leucocytes, that of increasing phagocytosis of macrophage, that of restoring the number of leucocytes, that of activating infection protective function, that of improving immunological competence, an antitumor action, etc.
ABSTRACT
Novel fused pyrazole compounds of the general formula
wherein all the symbols are as defined in the specification or its pharmaceutically acceptable salt which possesses a stimulating action on phagocytosis of leukocytes, a stimulating action on phagocytosis of macrophages, a restorative action on leukopenia, a stimulating action on non-specific resistance to infection, an antitumour action, an activating action on immune responses and the like, and therefore is of use as a pharmaceutical.摘要翻译： 由通式表示的新的稠合的吡唑化合物（I）（其中，X darstellt = N-或= CH-，R代表H，烷基，烷氧基或卤素，Y <1>表示由卤素，烷基或烷氧基取代的α-，苯基或苯基 ，Y <2> darstellt-β，-A <2> -B <2>，H，烷基，substituiertem烷基，苯基或苯基substituiertem由选自卤素，烷基和烷氧基中选择的取代基，条件是至少一个没有 的Y <1>和Y <2> darstelltα或β，Z <1>和Z <2>每个darstellt -O - ， - S-或-NR <3>（worin - [R <3>表示H或烷基） ，A <1>和A <2>每个darstellt亚烷基，B <1>和B <2>每个darstellt羧基，烷氧基羰基或phenylalkoxycarbonyl worin苯基可以任选地被选自卤素选自取代基substituiertem，烷基 和烷氧基，酰基，-OH，酰氧基，γ-或λ（worin - [R <1>和R <2>表示H，烷基，二烷基氨基烷基，羟基烷基或，当结合在一起，R <1>和R <2>表示基团 形成heteroC yclic环与氮原子相邻的一起），并且L <1>和L <2>每个darstellt卤素，烷基或烷氧基），以及它们的盐，它们的制备和处理的药物组合物包含相同的游离缺失光盘。 所述化合物具有增加白细胞的吞噬作用的作用下，没有增加巨噬细胞的吞噬作用的，没恢复白细胞数量的，做过活化感染的保护功能的，没有提高免疫能力，抗肿瘤作用等的
摘要<的 / H0>通式的新的稠合的吡唑化合物 worin所有符号如，其中在白细胞吞噬作用具有刺激作用说明书或其药学上可接受的盐所定义，对巨噬细胞的吞噬刺激作用，恢复性动作 上白细胞减少，到感染的非特异性抵抗力刺激作用，以抗肿瘤作用上激活免疫应答作用等，因此，是作为药物使用的。 -
公开(公告)号：EP0043858B1
公开(公告)日：1984-04-18
申请号：EP81900262.7
申请日：1981-01-13
IPC分类号： C07D471/04 , C07D513/04 , A61K31/425 , A61K31/435
CPC分类号： C07D471/04 , C07D513/04
摘要： Hetero ring-substituted oxoalkanoic acid derivatives having an immunity-controlling action and represented by the following general formula: (FORMULA) wherein R1 represents a hydrogen atom, a lower alkyl group, or a phenyl, thienyl or furyl group optionally having in an optional position of the nucleus at least one substitutent of halogen, lower alkyl, lower alkoxy, mono- or di-lower alkylamino-substituted lower alkoxy, lower alkylthio, lower alkylsulfinyl, amino, nitro or cyano, R2 and R3 each represents a hydrogen atom or a lower alkyl group, A represents a lower alkylene group, X represents a sulfur atom or a vinylene group, Y represents a nitrogen atom or a methine group optionally having lower alkyl as a substituent, and Z represents a carbonyl group or a single bond.
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公开(公告)号：EP0308515B1
公开(公告)日：1994-01-26
申请号：EP88902569.8
申请日：1988-03-17
发明人： NAKAO, Toru , MORITA, Kenji , HISADOME, Masao , TAKEHARA, Shuzo
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： Thienocinnoline compounds represented by general formula (I) (wherein R represents hydrogen, halogen or lower alkyl, Ar represents aryl, heteroaryl, or aryl or heteroaryl having at least one substituent selected from the group consisting of halogen, lower alkyl, lower alkoxy, nitro, amino, hydroxy, trifluoromethyl and lower alkanoylamino, and ----- between 5a-position and 6-position represents either a single or a double bond) useful as anti-anxious agents, amnesia treating agents, brain function activating agents, anti-dement agents or bioprotection accelerating agents.
摘要翻译： 由通式（I）表示的噻吩并喹啉化合物（其中R代表氢，卤素或低级烷基，Ar代表具有至少一个选自卤素，低级烷基，低级烷氧基，硝基的取代基的芳基，杂芳基或芳基或杂芳基 ，氨基，羟基，三氟甲基和低级烷酰基氨基，以及在5a-位和6-位之间代表单键或双键），用作抗焦虑剂，遗忘症治疗剂，脑功能活化剂，抗 代谢剂或生物保护促进剂。
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公开(公告)号：EP0066628A1
公开(公告)日：1982-12-15
申请号：EP82900034.8
申请日：1981-12-09
发明人： OE, Takanori , TSURUDA, Mineo , GOTO, Kazuhiro , HISADOME, Masao
IPC分类号： C07D213/63 , C07D213/70 , C07D401/14 , A61K31/44
CPC分类号： C07D213/64 , C07D213/61 , C07D213/70 , C07D231/12 , C07D233/56 , C07D249/08
摘要： Pyridine derivatives represented by the following general formula
wherein R 1 , R 2 , R3, and R 4 , which may the same or different, each represents a hydrogen atom or a lower alkyl group, or R 1 and R 2 , or R 3 and R 4 , are taken together to form a hetero ring together with the adjacent nitrogen atom, A 1 and A 2 , which may be the same or different, each represents an alkylene or hydroxy-substituted alkylene group, Y' and Y 2 , which may be the same or different, each represents an oxygen or sulfur atom, and Z represents
or the pharmaceutically acceptable acid addition salts thereof. These compounds show pharmacological effects such as acceleration of leukocyte phagocytosis, acceleration of macrophage phagocytosis, acceleration of production of rosette forming cells of spleen, and depression of adjuvant arthritis, thus being useful as medicines.-
公开(公告)号：EP0043858A1
公开(公告)日：1982-01-20
申请号：EP81900262.7
申请日：1981-01-13
IPC分类号： C07D471/04 , C07D513/04 , A61K31/425 , A61K31/435
CPC分类号： C07D471/04 , C07D513/04
摘要： Hetero ring-substituted oxoalkanoic acid derivatives having an immunity-controlling action and represented by the following general formula:
wherein R' represents a hydrogen atom, a lower alkyl group, or a phenyl, thienyl or furyl group optionally having in an optional position of the nucleus at least one substitutent of halogen, lower alkyl, lower alkoxy, mono- or di-lower alkylamino-substituted lower alkoxy, lower alkylthio, lower alkylsulfinyl, amino, nitro or cyano, R 2 and R 3 each represents a hydrogen atom or a lower alkyl group, A represents a lower alkylene group, X represents a sulfur atom or a vinylene group, Y represents a nitrogen atom or a methine group optionally having lower alkyl as a substituent, and Z represents a carbonyl group or a single bond.摘要翻译： 具有免疫控制作用并由下列通式表示的杂环取代的氧代链烷酸衍生物：其中R'表示氢原子，低级烷基或苯基，噻吩基或呋喃基，其任选地在 低级烷基，低级烷氧基，一或二低级烷基氨基取代的低级烷氧基，低级烷硫基，低级烷基亚磺酰基，氨基，硝基或氰基，R2和R3分别代表氢原子或低级烷基 A表示低级亚烷基，X表示硫原子或亚乙烯基，Y表示氮原子或可以具有低级烷基作为取代基的次甲基，Z表示羰基或单键。
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