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1. 发明申请

WO1980000342A1 ANALGESIC PENTAPEPTIDES 审中-公开
标题翻译：有害物质
公开(公告)号：WO1980000342A1
公开(公告)日：1980-03-06
申请号：PCT/US1979000531
申请日：1979-07-23
申请人： AMERICAN HOME PROD CORP
发明人： AMERICAN HOME PROD CORP , GARSKY V
IPC分类号： C07C103/52
CPC分类号： C07K14/702 , A61K38/00 , Y10S514/809
摘要： Pentapeptides of the formula: (FORMULA) wherein R1 is hydrogen, methyl, ethyl, propyl, 2-methyl-2-pentenyl, 2-methyl-1-pentenyl, cyclopropylmethyl, or cyclobutylmethyl; R2, R3, and R4 are, independently, hydrogen or methyl; and X is -OH, -NH2, -NHCnH2n+1 where n is 1,2,3, and 4, -0R5, or CH2OR5, where R5 is hydrogen or lower alkyl of from 1 to 4 carbon atoms; or a pharmaceutically acceptable salt thereof; have analgesic activity upon administration to warm-blooded animals.

2. 发明申请

WO1980002025A1 BICYCLIC OXO-THIOLACTONES 审中-公开
标题翻译：双酚OXO-THIOLACTONES
公开(公告)号：WO1980002025A1
公开(公告)日：1980-10-02
申请号：PCT/US1980000352
申请日：1980-03-20
申请人： AMERICAN HOME PROD CORP
发明人： AMERICAN HOME PROD CORP , KIM D
IPC分类号： C07D513/04
CPC分类号： C07D513/04 , C07C323/00 , C07C327/00 , C07D207/16
摘要： Bicyclic oxo-thiolactones of the formula: (FORMULA) in which R u is hydrogen or lower alkyl; R u and R u are, independently, hydrogen, hydroxy, halogen, lower alkyl, lower alkoxy, or aryl; and R u, R u, and R u are, independently, hydrogen, lower alkyl, lower hydroxyalkyl, aryl, or arylalkyl, except that R u and R u may not both be aryl. These compounds act as inhibitors of angiotensin converting enzyme and are useful as agents for the treatment of hypertension in mammals. The compounds are stable against oxidation of the sulfur. Also disclosed is a method of preparation of such compounds.
摘要翻译：下式的双环氧代 - 硫代内酯：其中R u是氢或低级烷基的式（式） R u和R u独立地是氢，羟基，卤素，低级烷基，低级烷氧基或芳基; 并且R u，R u和R u独立地是氢，低级烷基，低级羟基烷基，芳基或芳烷基，不同之处在于R u和R u可以不是都是芳基。这些化合物作为血管紧张素转化酶的抑制剂，可用作哺乳动物高血压治疗剂。该化合物对硫的氧化是稳定的。还公开了这种化合物的制备方法。

3. 发明申请

WO1980000025A1 DERIVATIVES OF 4,5-DIHYDRO-4-OXOFURAN-2-CARBOXYLIC ACID,PREPARATIONS AND USE THEREOF AND TETRAHYDROPYRAN-2,3,5-TRIONE INTERMEDIATES 审中-公开
标题翻译： 4,5-二羟基-4-氧代呋喃-2-羧酸的制备及其用途及其衍生物和四氢噻吩-2,3,5-三羧酸中间体
公开(公告)号：WO1980000025A1
公开(公告)日：1980-01-10
申请号：PCT/US1979000376
申请日：1979-05-29
申请人： AMERICAN HOME PROD CORP
发明人： AMERICAN HOME PROD CORP , JIRKOVSKY I , CAYEN M , DVORNIK D
IPC分类号： C07D495/10
CPC分类号： C07D309/36 , C07C33/30 , C07C45/31 , C07D307/68 , C07C49/245
摘要： Compounds of formula I (FORMULA) in which R1 and R2 each is lower alkyl, cyclo (lower) alkyl, lower alkoxy (lower) alkylene, phenyl or phenyl mono- or disubstituted with lower alkyl, lower alkoxy, halo, nitro or trifluoromethyl; or R1 and R2 together form a -(CH2)m-X-(CH2)n- chain wherein m and n each is an integer from one to four and X is methylene, oxa or thia; or R1 and R2 together with the carbon atom to which they are joined form a spiro(1,2,3,4-tetrahydro napthalene)-1 or spiro(indan)-1 radical; R3 is hydrogen or lower alkyl; and R4 is hydrogen, lower alkyl, cyclo (lower) alkyl, phenyl (lower) alkylene, amino (lower) alkylene, lower alkyl-amino (lower) alkylene, di (lower alkyl) amino (lower) alkylene or 3-pyridinyl (lower) alkylene, or a therapeutically acceptable addition salt thereof are disclosed which possess hypolipidemic activity, and can be used in pharmaceutical compositions. The compounds of formula I may be prepared by cyclising a corresponding compound of formula X (FORMULA) and if desired esterifying. Tetrahydropyran-2,3,5-trione intermediates are also disclosed.

4. 发明申请

WO1979001037A1 1-HYDROXYALKANAMINE PYRANO(3,4-B)INDOLE DERIVATIVES 审中-公开
标题翻译： 1-羟基烷胺吡咯烷（3,4-B）吲哚衍生物
公开(公告)号：WO1979001037A1
公开(公告)日：1979-11-29
申请号：PCT/US1979000256
申请日：1979-04-19
申请人： AMERICAN HOME PROD CORP
发明人： AMERICAN HOME PROD CORP , ASSELIN A , FAILLI A , DIONNE G , REVESZ C , HUMBER L
IPC分类号： A61K31/40
CPC分类号： C07D491/04 , C07D495/04 , Y10S514/869
摘要： New compounds of formula I (FORMULA) in which R1 is lower alkyl; R2 is hydrogen or lower alkyl; R3 and R4 each independently is hydrogen, lower alkyl halo, nitro, trifluoromethyl or lower alkoxy; R5 and R6 each independently is hydrogen or lower alkyl or R5 and R6 together with the nitrogen atom form a pyrrol-1-yl, piperidino or morpholino ring; R7 is hydrogen or lower alkyl; Alk1 and Alk2 each independently is a straight or branched chain lower alkylene having one to six carbon atoms; and X is oxa or thia, and therapeutically acceptable acid addition salts thereof. The above compounds are diuretic agents, which also possess anti-hypertensive activity. They may be used alone or with other diuretic agents. Pharmaceutical compositions containing the compounds and processes for preparing the compounds are also described.

5. 发明申请

WO1982001187A1 CNS STIMULANTS 审中-公开
公开(公告)号：WO1982001187A1
公开(公告)日：1982-04-15
申请号：PCT/US1981001243
申请日：1981-09-14
申请人： AMERICAN HOME PROD CORP
发明人： AMERICAN HOME PROD CORP , STEIN R
IPC分类号： C07D271/04
CPC分类号： C07F7/1804 , C07D271/04
摘要： The invention provides a process for preparing compound of the formula: in which the enantiomeric form is l- when R is hydrogen (in the presence or absence of d form), and l-threo when R is other than hydrogen (in the presence or absence of the d-threo form), R , R , R , R and R are defined groups or a non-toxic acid addition salt thereof, which are central nervous system stimulants. The invention also provides intermediates for preparing the compounds of formula I having a substituted hydroxyl group, their preparation and pharmaceutical compositions containing the intermediates having CNS stimulant activity.

6. 发明申请

WO1982001184A1 SYDNONE IMINE DERIVATIVES,INTERMEDIATES THEREFORE AND METHODS OF PREPARATION 审中-公开
标题翻译：赛奈酮衍生物，其中间体及其制备方法
公开(公告)号：WO1982001184A1
公开(公告)日：1982-04-15
申请号：PCT/US1981001205
申请日：1981-09-08
申请人： AMERICAN HOME PROD CORP
发明人： AMERICAN HOME PROD CORP , STEIN R
IPC分类号： C07C111/00
CPC分类号： C07C255/00 , C07D271/04
摘要： Les derives de (2-(amino substitue)-2-phenyle ethyle) nitrosoamino) acetonitrile decrits et leurs sels d'oxadiazolium a cycle ferme ainsi que leurs sels d'addition d'acide pharmaceutiquement acceptables sont des agents utiles dans le traitement de l'hypertension et servent de produits intermediaires dans la production des derives de la 3-(2-(dimethylamino)-2-phenylethyle)-N-((phenylamino) carbonyle) sydnone imine qui sont des stimulants utiles du systeme nerveux central.

7. 发明申请

WO1981000567A1 SYDNONE IMINES 审中-公开
公开(公告)号：WO1981000567A1
公开(公告)日：1981-03-05
申请号：PCT/US1980001067
申请日：1980-08-15
申请人： AMERICAN HOME PROD CORP
发明人： AMERICAN HOME PROD CORP , STEIN R
IPC分类号： C07D271/04
CPC分类号： C07D271/04
摘要： A compound of the formula: (FORMULA) in which the enantiomeric form is d, l or l- when R5 is hydrogen and d, l or l-threo when R5 is other than hydrogen; R1 and R2 are, independently, hydrogen, alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, halo, perfluoroalkyl of 1 to 3 carbon atoms, nitro, alkanoyl of 2 to 4 carbon atoms or alkoxycarbonyl of 2 to 4 carbon atoms; R3 is hydrogen, halo, nitro or alkanoyl of 2 to 4 carbon atoms; R5 and R6 are, independently, hydrogen or methyl; or a non-toxic acid addition salt thereof, are central nervous system stimulants.

8. 发明申请

WO1980002287A1 1,8-NAPHTHYRIDINE DERIVATIVES 审中-公开
标题翻译： 1,8-萘啶衍生物
公开(公告)号：WO1980002287A1
公开(公告)日：1980-10-30
申请号：PCT/US1980000319
申请日：1980-03-24
申请人： AMERICAN HOME PROD CORP
发明人： AMERICAN HOME PROD CORP , SCOTESE A , SANTILLI A
IPC分类号： C07D403/14
CPC分类号： C07D213/80 , C07D471/04
摘要： 4-Amino-3-carboxy or cyano-1,2-dihydro-2-oxo-1,8-naphthyridine derivatives are anti-secretory agents for use in the treatment of peptic ulcer disease.

9. 发明申请

WO1980000537A1 PYRIMIDO(1,6-A)INDOLE DERIVATIVES 审中-公开
标题翻译： PYRIMIDO（1,6-A）INDOLE DERIVATIVES
公开(公告)号：WO1980000537A1
公开(公告)日：1980-04-03
申请号：PCT/US1979000656
申请日：1979-08-27
申请人： AMERICAN HOME PROD CORP
发明人： AMERICAN HOME PROD CORP , JIRKOVSKY I
IPC分类号： A61K31/505
CPC分类号： C07D487/04 , C07D491/04 , C07D491/14
摘要： Pyrimido (1,6-a) indole derivatives of formula (I) (FORMULA) wherein R1-3 are optional defined substituents and R4 and R5 are defined substituents, and therapeutically acceptable acid addition salts thereof, are useful as antihypertensive agents. They may be used alone or with diuretic or other antihypertensive agents. Pharmaceutical compositions containing the compounds and processes for preparing the compounds are disclosed. Diazofluranthene chemical intermediates and processes for preparing them are also disclosed.

10. 发明申请

WO1980000151A1 N-(3-ALKYLAMINOPROPYL)-N'-PHENYLUREAS 审中-公开
标题翻译： N-（3- ALKYLAMINOPROPYL）-N'-苯脲
公开(公告)号：WO1980000151A1
公开(公告)日：1980-02-07
申请号：PCT/US1979000392
申请日：1979-06-06
申请人： AMERICAN HOME PROD CORP
发明人： AMERICAN HOME PROD CORP , SULKOWSKI T , MASCITTI A , BERGEY J
IPC分类号： C07C127/19
CPC分类号： C07C275/30 , C07C275/28
摘要： Compounds of the formula: (FORMULA) wherein: Y is 2,6-dimethylphenyl, 2,5-dimethylphenyl, 5-bromo-2-methylphenyl, or 5-chloro-2-methylphenyl; and X is propyl, isopropyl, n-butyl, or isobutyl; or a non-toxic, pharmaceutically acceptable acid addition salt thereof; possess anti-arrhythmic activity.

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