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1. 发明公开

EP0228893A3 Arylalkyl-heterocyclic amines, n-substituted by aryloxyalkyl group in allergy treatment 失效
标题翻译：在过敏治疗中被芳氧基烷基基团取代的芳基烷基 - 杂环胺
公开(公告)号：EP0228893A3
公开(公告)日：1990-01-03
申请号：EP86310047.5
申请日：1986-12-22
申请人： A.H. ROBINS COMPANY, INCORPORATED (a Delaware corporation)
发明人： Yanni, John Michael , Walsh, David Allan
IPC分类号： A61K31/445 , A61K31/47
CPC分类号： C07D207/08 , C07D211/14 , C07D211/18 , C07D211/22 , C07D211/70 , C07D401/06 , C07D401/12 , C07D405/06 , C07D405/12
摘要： 57 Allergy can be treated with substituted heterocyclic amines, wherein the active agents are expressed generally by the formula:
wherein p is zero, one or two; m is one to six inclusive; A is selected from hydrogen, hydroxy or cyano; d is zero or one; Q is -CH-, -CH 2 -, or
n is zero or one and when Q is -CH- and n is one, a douo!e bond is formed with one of the adjacent carbons but not both at the same time, and when n and d are zero at the same time, a double bond is formed between the a carbon and a carbon of the central heterocyclic amine ring Ar, D and R are selected from phenyl, substituted phenyl, pyridinyl, thienyl, furanyl or naphthyl and in addition. R may have the values benzyl, substituted benzyl, cycloalkyl or loweralkyl and D may additionally have the values; 2H-1-benzopyran-2-one, 4-oxo-4H-1-benzopyran-2-carboxylic acid loweralkyl ester, 2,3-dihydro-4N-1-benzopyran-4-one or 1,4-benzodioxan-loweralkyl-2-yl, and the pharmaceutically acceptable salts thereof.
摘要翻译：过敏症可以用取代的杂环胺治疗，其中活性剂通常由下式表示：其中p是0,1或2; m是一至六（含）; A选自氢，羟基或氰基; d是零或一个; Q是-CH - ， - CH 2 - ，或者n是零或1，并且当Q是-CH-并且n是1时，与邻近的碳中的一个形成双键但不同时形成双键，以及当n和d同时为零时，在中心杂环胺环Ar的碳和碳之间形成双键，D和R选自苯基，取代的苯基，吡啶基，噻吩基，呋喃基或萘基，和此外。 R可具有苄基，取代的苄基，环烷基或低级烷基值，并且D可另外具有这些值; 2H-1-苯并吡喃-2-酮，4-氧代-4H-1-苯并吡喃-2-羧酸低级烷基酯，2,3-二氢-4N-1-苯并吡喃-4-酮或1,4-苯并二恶烷 - 低级烷基 -2-基及其药学上可接受的盐。

2. 发明公开

EP0279707A3 Aryloxymethyl derivatives of nitrogenous heterocyclic methanols and ethers thereof having cardiovascular activity 失效
标题翻译：亚硝基甲基衍生物和其他具有心血管活性的异戊二烯甲醇
公开(公告)号：EP0279707A3
公开(公告)日：1989-07-19
申请号：EP88301479.7
申请日：1988-02-22
申请人： A.H. ROBINS COMPANY, INCORPORATED
发明人： Shanklin, JNR., James Robert , Johnson, Christopher Peter
IPC分类号： C07D207/08 , C07D211/22 , C07D213/30 , C07D223/04 , C07D498/04 , A61K31/395
CPC分类号： C07D207/08 , C07D211/22 , C07D213/30 , C07D223/04
摘要： Novel heterocyclicmethanols are disclosed having the formula:
wherein Z is pyrrolidinyl, piperidinyl, homopiperidinyl or pyridinyl;
R¹ is hydrogen, loweralkyl or carbethoxymethyl;
R² is hydrogen, loweralkyl or cycloalkyl, phenyl or phenyl-loweralkyl;
R³ is 1 or 2-naphthalenyl, 2,3-dihydroinden-4 or 5-yl, phenyl or phenyl substituted by loweralkyl, loweralkoxy, halogen, trifluoromethyl, phenyl, methylenedioxy, nitro, amino, loweralkylamino, diloweralkylamino, loweracylamino;
the 1-position of 2-pyrrolidinyl, 2-piperidinyl or 2-homopiperidinyl may be substituted by an R⁴ loweralkyl group, or R¹ may form methylene or -CH₂-C(O)- bridges with R⁴;
the pharmaceutically acceptable salts and diastereomers thereof, which compounds have antiarrhythmic and/or hypotensive activity in animals.

3. 发明公开

EP0315433A2 3-amino-5-methyl-1H-pyrazole-4-carboxylic acids and esters thereof as anticonvulsants, muscle relaxants and anxiolytics 失效
标题翻译： 3-氨基-5-甲基-1H-吡唑-4-酮和酯类davon als Antikrampfmittel，Muskelrelaxans und Anti-Beklemmungsmittel。
公开(公告)号：EP0315433A2
公开(公告)日：1989-05-10
申请号：EP88310307.9
申请日：1988-11-02
申请人： A.H. ROBINS COMPANY, INCORPORATED
发明人： Taylor, Chandler Roy, Jr. , Stauffer, Harold Fisher, Jr.
IPC分类号： C07D231/38 , A01N43/56 , C07D401/12 , A01N43/40
CPC分类号： C07D231/38 , C07D401/12
摘要： Pharmaceutical compositions which comprise a compound represented by the formula
where
R¹ represents a hydrogen atom, a lower alkyl group or a pharmaceutically acceptable cation;
R² and R³ independently represent a hydrogen atom, a lower alkyl group, an aryl group, a cycloalkyl group, a lower alkenyl group, a 1-adamantyl group, a heterocyclicaminoalkyl group, a diloweralkylaminoloweralkyl group, or R² together with R³ and the adjacent nitrogen atom may form a heterocyclic ring structure;
and/or a pharmaceutically acceptable acid salt thereof; the use of such compounds in medicine; and the use of such compounds in the preparation of anticonvulsant agents, muscle relaxants and anxiolytic agents, are disclosed.
摘要翻译：药物组合物，其包含由式CHEM表示的化合物，其中R 1表示氢原子，低级烷基或药学上可接受的阳离子; R 2和R 3独立地表示氢原子，低级烷基，芳基，环烷基，低级烯基，1-金刚烷基，杂环氨基烷基，二低级烷基氨基低级烷基或R' 2>与R 3一起，并且相邻的氮原子可以形成杂环结构; 和/或其药学上可接受的酸盐; 在药物中使用这些化合物; 并且公开了这些化合物在制备抗惊厥剂，肌肉松弛剂和抗焦虑剂中的用途。

4. 发明公开

EP0299663A2 Antihistaminic aromatic tetrahydroazepinones (and thiones) 失效
标题翻译：抗组胺药四氢吖庚因酮（十二酮）。
公开(公告)号：EP0299663A2
公开(公告)日：1989-01-18
申请号：EP88306109.5
申请日：1988-07-05
申请人： A.H. ROBINS COMPANY, INCORPORATED (a Delaware corporation)
发明人： Cale, Albert Duncan, Jr.
IPC分类号： C07D471/04 , C07D223/16 , C07D403/06 , A61K31/55 , C07D401/06
CPC分类号： C07D223/16 , C07D471/04
摘要： Aromatic tetrahydroazepinones and thiones having the formula:
wherein
Q is carbon or nitrogen;
B is oxygen or sulfur;
R is loweralkyl, cycloalkyl or phenylloweralkyl;
Z is an amino or a heterocyclic amino containing radical; and
Y is halo, loweralkyl, loweralkoxy, diloweralkylamino, nitro, phenyl or trifluorophenyl;
and having antihistaminic utility, a process for the preparation thereof and chemical intermediates therefor are disclosed.
摘要翻译：具有下式的芳香族四氮杂吖庚因酮和硫酮：其中Q是碳或氮; B是氧或硫; R是低级烷基，环烷基或苯基低级烷基; Z是含氨基或杂环氨基的基团; Y为卤素，低级烷基，低级烷氧基，二低级烷基氨基，硝基，苯基或三氟苯基; 并具有抗组胺功效，其制备方法及其化学中间体。

5. 发明公开

EP0279543A1 Process for the preparation of an azetidine and intermediates therefor 失效
标题翻译： Verfahren zur Herstellung eines Azetidins und Zwischenprodukt。
公开(公告)号：EP0279543A1
公开(公告)日：1988-08-24
申请号：EP88300744.5
申请日：1988-01-28
申请人： A.H. ROBINS COMPANY, INCORPORATED (a Delaware corporation)
发明人： Lo, Young Sek , Causey, David Hudson , Shamblee, Dwight Allen , Mays, Richard Puckett
IPC分类号： C07D205/04 , C07C211/29
CPC分类号： C07D205/04
摘要： A novel process is described for preparing azetidine and 2 or 3 methyl and ethyl azetidine free bases by reacting primary arylmethylamine having suitable bulk providing substituents attached to the methyl carbon and an appropriate propane derivative having leaving groups in the one and three position in hot organic solvent containing a non-nucleophilic base and an amount of water sufficient to promote azetidine ring formation to give N-protected-azetidines and deprotecting by hydrogenolysis under acidic conditions to give an acid salt of the azetidines and thereafter flashing off vaporized azetidine from a hot, agitated strong base solution or slurry and condensing to give the liquid azetidine free bases.
摘要翻译：描述了一种制备氮杂环丁烷和2或3个甲基和乙基氮杂环丁烷游离碱的新方法，该方法是通过使具有连接到甲基碳上的合适体积的主要芳基甲基胺和在热的有机溶剂中在一个和三个位置上具有离去基团的合适的丙烷衍生物含有非亲核碱和一定量的足以促进氮杂环丁烷环形成的水，得到N-保护的氮杂环丁烷，并在酸性条件下通过氢解脱保护，得到氮杂环丁烷的酸式盐，然后从热的搅拌下闪蒸汽化的氮杂环丁烷强碱溶液或浆液冷凝，得到液氮氮杂环丁烷碱。

6. 发明授权

EP0161074B1 Gastrokinetic and antiemetic n-(1-substituted-4,5-dihydro-1h-pyrazol-4-yl)benzamides 失效
标题翻译：胃肠动力学和抗N-（1-取代-4,5-二氢-1H-吡唑-4-基）苯甲酸酯
公开(公告)号：EP0161074B1
公开(公告)日：1988-08-03
申请号：EP85302461.0
申请日：1985-04-09
申请人： A.H. ROBINS COMPANY, INCORPORATED
发明人： Turnbull, Lennox Birckhead , Donohue, John Alexander , Jagdmann, Gunnar Erik, Jr.
IPC分类号： C07D231/06 , A61K31/415
CPC分类号： C07D231/06

7. 发明公开

EP0178946A3 1-(Aminoalkyl)-alpha, alpha-diaryl pyrrolidine-piperidine- and homopiperidine- acetamides and acetonitriles 失效
标题翻译： 1-（氨基甲酰基）-ALPHA，ALPHA-二元吡咯烷 - 哌啶酮和HOMOPIPERIDINE-乙酰胺和乙酰胺
公开(公告)号：EP0178946A3
公开(公告)日：1988-06-22
申请号：EP85307553
申请日：1985-10-18
申请人： A.H. ROBINS COMPANY, INCORPORATED
发明人： Welstead, William John, Jr.
IPC分类号： C07D207/09 , C07D211/34 , C07D223/04 , C07D401/06 , A61K31/40 , A61K31/44 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/55 , C07D207/416 , C07D207/12 , C07D211/96 , C07D211/46 , C07D223/08
CPC分类号： C07D207/08 , C07D207/09 , C07D211/34 , C07D223/04 , C07D401/06
摘要： 1-Aminoalkyl)-α, α-diaryl pyrrolidinyl, piperidino and homopiperidinoacetamides and acetonitriles having the formula
wherein:
n is 0, 1 or 2; Ar 1 and Ar 2 are 2, 3 or 4-pyrido, phenyl or substituted phenyl; Y is aminocarbonyl or cyano; x is 2 to 5 ; R is H or loweralkyl; R 1 and R 2 are hydrogen, cycloalkyl, loweralkyl, and R 2 and R 3 taken with the adjacent nitrogen may form a heterocyclic residue (including their diastereoisomers when possible) and pharmaceutical salts; have cardiac antiarrhythmic activity.

8. 发明公开

EP0160436A3 N-[(Amino)Alkyl]-1-pyrrolidine, 1-piperidine and 1-homopiperidinecarboxamides (and thiocarboxamides) with sulphur linked substitution in the 2, 3 or 4-position 失效
标题翻译： N-Û（氨基）烷基-1-吡咯烷，1-PIPERIDINE和1-HOMOPIPERIDINARARAMAMESES（和硫代烟酰胺）在2,3或4位置具有连锁取代基
公开(公告)号：EP0160436A3
公开(公告)日：1988-06-08
申请号：EP85302526
申请日：1985-04-10
申请人： A.H. ROBINS COMPANY, INCORPORATED
发明人： Shanklin, James Robert, Jr.
IPC分类号： C07D207/36 , C07D211/54 , C07D223/06
CPC分类号： C07D223/06 , C07D207/12 , C07D207/34 , C07D211/54
摘要： Pyrrolidine, piperidine and homopiperidine- carboxamide and thiocarboxamide compounds of the formula:
wherein X is -S-, -S(0)- or -S(0) 2 -; A is a loweralkalene chain and A 1 and A 2 are alkalene chains when p and d are one; R, R 1 and R 2 are hydrogen, loweralkyl, phenyl cycloalkyl or phenylalkyl and R 1 and R 2 may form a heterocyclic residue with the adjacent nitrogen atom; Q is a selected aromatic radical, and the pharmaceutically acceptable acid addition salts are useful as cardiac antiarrhythmia agents. Chemical intermediates, unsubstituted on pyrrolidine, piperidine and homopiperidine nitrogen but with the -(A 2 ) p -X-(A 2 ) d -Q side chain are also disclosed.

9. 发明授权

EP0066415B1 N-(arylthioalkyl)-N'-(aminoalkyl)ureas 失效
标题翻译： N-（芳硫基烷基）-N' - （氨基烷基）脲
公开(公告)号：EP0066415B1
公开(公告)日：1985-10-02
申请号：EP82302557.2
申请日：1982-05-19
申请人： A.H. ROBINS COMPANY, INCORPORATED
发明人： Shanklin, James Robert, Jr. , Johnson, Christopher Peter, III
IPC分类号： C07C149/437 , C07C147/00 , C07C157/00 , C07D295/12 , C07D307/38 , A61K31/17
CPC分类号： C07D209/48 , C07C255/00 , C07C317/28 , C07C323/00 , C07C323/44 , C07C335/08 , C07C2601/14 , C07D307/38

10. 发明公开

EP0152236A2 Aryloxymethylpyrrolidinols and piperidinols having antidepressant, antiarhythmic or hypotensive activity 失效
标题翻译：皮质激素和丙烯酰氧基甲基 - 吡咯烷基酯，blitdrucksenkenden，抗抑郁和抗心律失常Wirkungen。
公开(公告)号：EP0152236A2
公开(公告)日：1985-08-21
申请号：EP85300667.4
申请日：1985-01-31
申请人： A.H. ROBINS COMPANY, INCORPORATED
发明人： Taylor, Chandler Roy, Jr. , Stauffer, Harold Fisher, Jr.
IPC分类号： C07D207/12 , C07D211/46 , A61K31/395
CPC分类号： C07D211/42 , C07D207/12 , C07D211/48
摘要： Aryloxymethylpyrrolidinols and piperidinols of the formula:
wherein R' represents a hydrogen atom or a loweralkyl or phenylloweralkyl group, R 2 represents a hydrogen atom or a loweralkyl or acyl; R 3 is phenyl, naphthyl, 4-indanyl and 5-indanyl; m is 2 or 3 and n is 1 or 2; and the pharmaceutically acceptable salts thereof, having antiarrhythmic, antidepressant and antihypertensive activity.
摘要翻译：芳基氧基甲基吡咯烷醇和下式的哌啶醇：其中R 1表示氢原子或低级烷基或苯基低级烷基，R 2表示氢原子或低级烷基或酰基; R 3是苯基，萘基，4-二氢化茚基和5-二氢化茚基; m为2或3，n为1或2; 及其药学上可接受的盐，具有抗心律不齐，抗抑郁和抗高血压活性。

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