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1. 发明授权

KR780000694B1 PROCESS FOR PREPARATION OF PHYRAZOL-5-ONES 失效
公开(公告)号：KR780000694B1
公开(公告)日：1978-12-27
申请号：KR780003261
申请日：1978-10-31
申请人： BAYER AG
发明人： MENG K , HORSTMANN H , WEHINGER E , MOLLER E

2. 发明授权

KR790000301B1 PRODUCTION OF 1-SUBSTITUTED PYRAZOL-5-ONES 失效
公开(公告)号：KR790000301B1
公开(公告)日：1979-04-23
申请号：KR790000087
申请日：1979-01-13
申请人： BAYER AG
发明人： MENG K , WEHINGER E , MOELLER E
摘要： The title compds. (I;R-H, NH2, Ph, CF3, alkyl, alkeny1, R1=H, alkenyl, alkyl, allyl, R2 = alkyl, R3 = 4-MeC6H4, 3,4-Cl2C6H3, 4-FC6H4, 4-pyridyl, 2-naphthyl) were prepd. by reacting a derivative of pyrazol-5-one with NH3 in a inactive solvent at 20-220≦̸C. I (R-R3=Me) at 3mg/kg orally in dogs caused elimination of 1158μ equiv. Na, 358μ equiv. K, and 10.5ml H2O/kghr, compared with control values of 168, 136, and 2.4, resp.

3. 发明授权

KR780000147B1 PROCESSES FOR THE MANUFACTURE OF 3-AMINO-PYRAZOLONES-(5) AND THEIR USE AS MEDICINE 失效
公开(公告)号：KR780000147B1
公开(公告)日：1978-04-19
申请号：KR730001005
申请日：1973-06-23
申请人： BAYER AG
发明人： HORSTMANN H , WEHINGER E , MENG K
IPC分类号： C07D231/44 , C07D231/52

4. 发明授权

KR790000417B1 PYRAZOLE DERIVATIVES 失效
公开(公告)号：KR790000417B1
公开(公告)日：1979-05-14
申请号：KR740004111
申请日：1974-11-20
申请人： BAYER AG
发明人： MOELLER E , MENG K
摘要： Pyrazoles and their salts with diuretic and hypotensive action were manufd. The pyrazoles (I; R=H, CF3, alkyl, R1 = H, alkyl, R2 = alkyl, R3 = halogen, CF3 , substituted alkyl, alkenyl or alkoxy, naphthyl, pyridyl, R4 = acyl, sulfonyl) were produced by the reaction of pyrazolons-5 derivs. and carboxylic or carbonic acid derivs., or sulfonic acid derivs. The reaction with sulfonic acid derivs. were carried out at -20-150≦̸C in the presence of inactive solvent, and alk. metallic or earth metallic hydroxide or carbonate or triethylamine or pyridine.

5. 发明授权

KR790000300B1 PROCESS FOR 1-SUBSTITUTED PYRAZOL-5-ONES THEIR PRODUCTION 失效
公开(公告)号：KR790000300B1
公开(公告)日：1979-04-23
申请号：KR790000086
申请日：1979-01-13
申请人： BAYER AG
发明人： MENG K , MOELLER E , WEHINGER E
摘要： 1-Substituted-pyrazol-5-ones (I; R = hydrogen, amino, alkyl, alkenyl, phenyl, trifluoromethyl group, R1 = hydrogen, alkyl, alkenyl, substituted aryl or alkyl group, R2 = alkyl, R3 = substituted pyridyl or aryl group) and their salts, useful as diuretic and antihypertensive, were prepd. by hydrolysing derivs. of I. Thus pyrazol-5-one deriv. (II; Z1 = t-butyl, phenyl, benzyl group) was hydrolysed by acid or base in inert solvent at 50-200≦̸C to give I.

6. 发明授权

KR790000097B1 PROCESS FOR PREPARATION OF 1-SUBSTITUTED PYRAZOL -5ONES 失效
公开(公告)号：KR790000097B1
公开(公告)日：1979-03-15
申请号：KR740001930
申请日：1974-03-23
申请人： BAYER AG
发明人： EIKE MOELLER , WEHINGER E , MENG K , HORSTMANN H
摘要： Pyrazolones(I ; R = H, NH2, R1 = H, Me Bu, CHMeEt, Ph, R2 = alkyl, R3 = Ph, PhO, PhS, PhCH:CH, 3-ClC6-H4OCH2CHMe, 2-naphtyloxy), which are diuretics and hypotensive agents, were prepd. by condensing R3R2CH2NHNH2 with RCOCHR' CO2Et, H2NC (OET) :CR' CO2Et and NCCHR2CO2 Et. Oral administration of 3-8 kg I(R, R2 = H, R1 = Me, R3 = 3-Cl C6H4) in dogs caused total elimationation of 5,275 equiv. Na, 1,065 eqiv. K and 45.4 ml N2O/kg, resp. compared with 336, 352 and 7.2 in those of control.

7. 发明授权

US3787431A Certain 3,4,5-triphenylthiazol-2-ones 失效
标题翻译：某些3,4,5-三苯基二苯并[2-ONES]
公开(公告)号：US3787431A
公开(公告)日：1974-01-22
申请号：US3787431D
申请日：1971-10-12
申请人： BAYER AG
发明人： LINKE S , HORSTMANN H , MENG K
IPC分类号： C07D277/34 , C07D91/24
CPC分类号： C07D277/34
摘要： 4.5-DIPHENYLTHIAZOLONES-(2) BEARING AN UNSUBSTITUTED OR SUBSTITUTED ARYL GROUP IN THE 3-POSITION ARE PREPARED FROM THE REACTION OF A DESYL HALIDE AND AN N-ARYLTHIOCARBAMIC ACID O-ESTER. THE COMPOUNDS, OW WHICH 3-(4NITROPHENYL)-4.5-DIPHENYLTHIAZOLONE-(2) IS A REPRESENTATIVE EMBODIMENT, ARE HYPOLIPEMIC AGENTS.

8. 发明专利

YU169281A PROCESS FOR PREPARING 1-(2-(BETA-NAPHTHYLOXY)-ETHYL)-3-METHYL-PYRAZOLONE-(5) 未知
公开(公告)号：YU169281A
公开(公告)日：1982-02-28
申请号：YU169281
申请日：1981-07-08
申请人： BAYER AG
发明人： MOELLER E , MENG K , HORSTMANN H , SEUTER F , WEHINGER E
IPC分类号： A61K31/415 , A61P7/02 , C07D231/20 , C07D231/08
摘要： 1454733 1 - (2 - Beta - naphthoxyethyl)- 3 - methylpyrazolin - 5 - one BAYER AG 6 May 1975 [6 June 1974 11 July 1974] 18970/75 Heading C2C The invention comprises the title compound and its salts. In examples, it is prepared by reacting (1) 2-beta-naphthoxyethylhydrazine with an alkyl or benzyl acetoacetate or tetrolate, or (2) a 2-beta-naphthoxyethyl halide with 3-methylpyrazolin-5-one or its sodium derivative. Therapeutic compositions having antithrombotic and thrombolytic activity comprise the above compound or its salts, and may be administered orally, parenterally or rectally.

9. 发明专利

SE408552B 未知
公开(公告)号：SE408552B
公开(公告)日：1979-06-18
申请号：SE7405079
申请日：1974-04-16
申请人： BAYER AG
发明人： MOLLER E , MENG K , WEHINGER E , HORSTMANN H
IPC分类号： A61K31/415 , A61P7/02 , A61P7/10 , A61P9/12 , C07D231/20 , C07D231/24 , C07D231/52
摘要： 1-Substituted pyrazole-5-ones of the formula AND PHARMACEUTICALLY ACCEPTABLE, NONTOXIC SALTS THEREOF, WHEREIN R is hydrogen or amino; R1 is hydrogen, alkyl, alkenyl, unsubstituted or substituted aryl or unsubstituted or substituted aralky; X is A. ETHYLENE, ETHYLENE WHEREIN 1 HYDROGEN ATOM ON ONE OF THE CARBON ATOMS IS SUBSTITUTED BY ALKYL OF 1 TO 4 CARBON ATOMS, ETHYLENE WHEREIN 1 HYDROGEN ATOM ON EACH OF THE TWO CARBON ATOMS IS SUBSTITUTED BY ALKYL OF 1 TO 4 CARBON ATOMS OR SAID ETHYLENE WHICH IS LINKED TO R2 via an oxygen or sulphur atom; B. PROPENYL, PROPENYL WHEREIN 1 HYDROGEN ATOM ON ONE, TWO OR THREE OF THE CARBON ATOMS IS SUBSTITUTED BY ALKYL OF 1 TO 4 CARBON ATOMS, SAID PROPENYL BEING LINKED TO THE N1 atom of the pyrazol ring via its methylene moiety; or C. METHYLENE; PROVIDED THAT WHEN X is methylene, R1 is not hydrogen if R is amino; R2 is aryl unsubstituted or substituted by:

10. 发明专利

SE408301B 未知
公开(公告)号：SE408301B
公开(公告)日：1979-06-05
申请号：SE7405078
申请日：1974-04-16
申请人： BAYER AG
发明人： MOLLER E , MENG K , WEHINGER E , HORSTMANN H
IPC分类号： A61K31/415 , A61P7/02 , C07D231/18 , A61P7/10 , A61P9/12 , C07D231/20 , C07D231/24 , C07D231/52 , C07D401/06
摘要： 1429141 Pyrazolin-5-ones BAYER AG 16 April 1974 [17 April 1973 19 Dec 1973] 16507/74 Heading C2C The invention comprises compounds of formula (including tautomers thereof, especially when R is amino), wherein R is H, amino, alkyl, alkenyl, CF 3 or Ph; R 1 is H, alkyl, alkenyl or an optionally substituted aryl or aralkyl radical; R 2 is an alkyl group; and R 3 is a pyridyl radical or an aryl radical carrying 1 or 2 identical or different substituents, which are selected from halogen, CF 3 , alkyl, alkenyl, and alkoxy radicals, or carrying one mono- or di-alkylamino, CF 3 O, nitro, nitrile, carbamoyl, alkyl- or dialkylcarbamoyl, sulphamyl, or alkyl- or dialkylsulphamyl radical, or a group -B, -CO.B or -SO 2 .B (in which B is a saturated ring containing a nitrogen atom in the 1-position) or a -SO n alkyl group (in which n=0, 1 or 2), optionally together with 1 or 2 substituents selected from alkyl, alkenyl, alkoxy, halogen and CF 3 , or carrying none or 1 only of these substituents and a fused branched or unbranched, saturated or unsaturated 5-, 6- or 7- membered ring optionally containing 1 or 2 oxygen or sulphur atoms. In examples, these compounds are prepared by (a) reacting R 2 R 3 CHNHNH 2 with an appropriate ring-forming co-reactant, (2) replacing a compound in which R is halogen, by amino, (3) hydrolysing a compound in which R is (e.g.) NHCO 2 Et, or (4) introducing the R 2 R 3 CH group by N 1 -substitution. Therapeutic compositions having diuretic, saluretic, antihypertensive and antithrombotic activity comprise compounds of the above formula, and may be administered orally, parenterally, rectally, topically, or by spray.

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