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1. 发明授权

US4247551A N-Pyrrolyl-pyridazineamines and their use as antihypertensive agents 失效
标题翻译： N-吡咯基 - 哒嗪胺及其作为抗高血压药的用途
公开(公告)号：US4247551A
公开(公告)日：1981-01-27
申请号：US76114
申请日：1979-09-17
申请人： Elvio Bellasio , Nunzio Di Mola , Ambrogio Campi , Emiliana Baldoli
发明人： Elvio Bellasio , Nunzio Di Mola , Ambrogio Campi , Emiliana Baldoli
IPC分类号： A61K31/505 , C07D237/20 , C07D403/12 , C07D413/14 , A61K31/50 , A61K31/535
CPC分类号： C07D413/14 , A61K31/505 , C07D237/20 , C07D403/12
摘要： New-pyrrolyl-3-pyridazineamines having a further aminic substituent in the position 6. The compounds are useful as antihypertensive agents and may be prepared from 6-amino substituted-3-hydrazino pyridazines and .beta.-dicarbonyl compounds. The use of the novel compounds as antihypertensives and compositions containing the novel compounds as active ingredients are also claimed.
摘要翻译：在该位置6具有另外的氨基取代基的新的吡咯基-3-哒嗪胺。该化合物可用作抗高血压药，并可由6-氨基取代的3-肼基哒嗪和β-二羰基化合物制备。还要求使用新化合物作为抗高血压药和含有新化合物作为活性成分的组合物。

2. 发明授权

US4232017A Treatment of psychic disorders and inflammation with fused isoquinolines 失效
标题翻译：治疗心理障碍和炎症与融合异喹啉
公开(公告)号：US4232017A
公开(公告)日：1980-11-04
申请号：US41356
申请日：1979-05-22
申请人： Giorgio Winters , Nunzio Di Mola
发明人： Giorgio Winters , Nunzio Di Mola
IPC分类号： A61K31/47 , A61P25/20 , A61P29/00 , C07D231/38 , C07D471/04 , C07D513/04 , A61K31/54
CPC分类号： C07D231/38 , C07D471/04 , C07D513/04
摘要： New tricyclic ortho-fused heterocyclic compounds of formula ##STR1## wherein A is the group ##STR2## or the group ##STR3## in which R represents hydrogen, (C.sub.1-4)alkyl, phenyl or tolyl and R.sub.1 and may be (C.sub.1-4)alkyl, phenyl or tolyl, R.sub.2 is selected from (C.sub.1-4)alkyl, (C.sub.2-4)alkanoylmethyl, carbo(C.sub.1-3)alkoxymethyl, hydroxy(C.sub.2-4)alkyl, halo(C.sub.2-4)alkyl and a group ##STR4## wherein R.sub.3 is an alkylene group from 2 to 4 carbon atoms and R.sub.4 and R.sub.5 independently represent hydrogen or (C.sub.1-4)alkyl or, taken together with the nitrogen atom, a fully hydrogenated 5 or 6 membered heterocyclic radical which may contain a further heteroatom selected from O, N and S and be optionally substituted by a (C.sub.1-4)alkyl or phenyl group, or R.sub.2 may represent, nil the dotted lines x and y may represent nil or additional bonds; with the proviso that, when the symbol R.sub.2 linked to the oxygen atom is different from nil, x is an additional bond and y and the other symbol R.sub.2 represent nil; with the further proviso that, when the symbol R.sub.2 linked to the nitrogen atom is different from nil, y is an additional bond and x and the other symbol R.sub.2 represent nil; and salts therewith of pharmaceutically acceptable acids. The compounds possess antiinflammatory, CNS-depressent and anti-anxiety utility.
摘要翻译：新的式（I）所示的三环邻 - 稠合杂环化合物，其中A为基团（a）或基团（b），其中R表示氢，（C 1-4）烷基，苯基或甲苯基， R1可以是（C1-4）烷基，苯基或甲苯基，R2选自（C1-4）烷基，（C2-4）烷酰基甲基，碳（C1-3）烷氧基甲基，羟基（C2-4）（C 2-4）烷基和基团，其中R 3是2至4个碳原子的亚烷基，且R 4和R 5独立地表示氢或（C 1-4）烷基，或者与氮原子一起完全氢化 5或6元杂环基，其可以含有选自O，N和S的另外的杂原子，并且任选地被（C 1-4）烷基或苯基取代，或者R 2可以表示，虚线x和y可以表示nil 或附加债券; 条件是当连接到氧原子的符号R2不同于nil时，x是附加键，y和其它符号R2表示nil; 进一步的条件是当连接到氮原子的符号R2不同于nil时，y是附加键，x和其它符号R2表示nil; 以及其与药学上可接受的酸的盐。该化合物具有抗炎，CNS抑制和抗焦虑效用。

3. 发明授权

US3984563A Antiinflammatory 2-imino-indolines and their pharmaceutical compositions 失效
标题翻译：抗炎2-亚氨基 - 吲哚啉及其药物组合物
公开(公告)号：US3984563A
公开(公告)日：1976-10-05
申请号：US504205
申请日：1974-09-09
申请人： Giorgio Winters , Nunzio Di Mola
发明人： Giorgio Winters , Nunzio Di Mola
IPC分类号： B01J27/00 , C07B61/00 , C07C243/36 , C07D209/40 , C07D209/96 , C07D209/14 , A61K31/40
CPC分类号： C07C243/00 , C07C243/36 , C07D209/40 , C07D209/96
摘要： Compounds with antiinflammatory, analgesic and CNS depressant activity having the following general formula ##SPC1##WhereinR represents hydrogen or methoxy;R.sub.1 represents hydrogen; lower alkyl; lower alkyl substituted with a group carboxy, carbo(lower alkoxy) or carbamyl; phenyl; benzyl, lower aliphatic acyl; benzoyl; benzoyl substituted with a halo group;R.sub.2 represents hydrogen; lower alkyl; carbo(lower alkoxy); carbamyl; phenylcarbamyl; lower aliphatic acyl; benzoyl; benzoyl substituted with a halo group,R.sub.3 represents halo; lower alkyl; lower alkyl substituted with a group selected from carboxy, carbo(lower alkoxy), carbamyl, halo, amino, mono and di-lower alkylamino, phthalimido and morpholino; phenyl; phenyl substituted with a group selected from lower alkoxy, halo, nitro, amino and acetamido;R.sub.4 represents hydrogen or lower alkyl; with the proviso that when simultaneously R.sub.1 represents hydrogen, methyl, phenyl, benzyl, acetyl or benzoyl, R.sub.2 represents hydrogen, lower alkyl or acetyl,R.sub.3 represents lower alkyl or phenyl, R.sub.4 must be different from hydrogen and methyl;Or R.sub.3 and R.sub.4 taken together with the adjacent carbon atom may represent a 5-6 membered alicyclic ring.
摘要翻译：具有抗炎，镇痛和CNS抑制活性的化合物具有以下通式，其中R表示氢或甲氧基; R1表示氢; 低级烷基被羧基取代的低级烷基，碳（低级烷氧基）或氨基甲酰基; 苯基; 苄基，低级脂族酰基; 苯甲酰用卤代基取代的苯甲酰基; R2表示氢; 低级烷基碳（低级烷氧基）; 氨基甲酰苯基氨基甲酰基; 低级脂肪族酰基; 苯甲酰被卤素取代的苯甲酰基，R3代表卤素; 低级烷基被选自羧基，碳（低级烷氧基），氨基甲酰基，卤素，氨基，单和二低级烷基氨基，苯二甲酰亚氨基和吗啉代的基团取代的低级烷基; 苯基; 被选自低级烷氧基，卤素，硝基，氨基和乙酰氨基的基团取代的苯基; R4代表氢或低级烷基; 条件是当R 1代表氢，甲基，苯基，苄基，乙酰基或苯甲酰基时，R 2表示氢，低级烷基或乙酰基，R 3表示低级烷基或苯基，R 4必须不同于氢和甲基; OR 3和R 4与相邻碳原子一起可以表示5-6元脂环。

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