公开(公告)号：US3925470A

公开(公告)日：1975-12-09

申请号：US51562674

申请日：1974-10-17

申请人： BAYER AG

发明人： WOLLWEBER HARTMUND ,  FLUCKE WINFRIED

IPC分类号： A61K31/155 ,  C07C123/00

CPC分类号： A61K31/155

摘要： 4-Amino substituted phenylamidine are anthelmintics. The compounds, of which N-(4-aminophenyl)-N'',N''-dimethylacetamidine is a representative embodiment, can be prepared through treatment of a 4-amino aniline with a carboxylic acidamide or thioamide, reduction of an appropriately substituted 4-aminophenyl-amidine, optionally followed by alkylation of the resultant 4-aminophenylamidine, formation of a Schiff base followed by quaternization and hydrolysis, or hydrolysis of a 4-acylaminophenylamidine.

摘要翻译： 4-氨基取代的苯脒是驱虫剂。 可以通过用羧酸酰胺或硫代酰胺处理4-氨基苯胺来制备其中N-（4-氨基苯基）-N'，N'-二甲基乙脒是其代表性实施方案的化合物，还原适当取代的4- 任选随后将所得4-氨基苯基 - 脒烷基化，形成希夫碱，然后季铵化和水解，或4-酰氨基苯基脒的水解。

公开(公告)号：US3860590A

公开(公告)日：1975-01-14

申请号：US28909272

申请日：1972-09-14

申请人： BAYER AG

发明人： WOLLWEBER HARTMUND ,  FLUCKE WINFRIED ,  SCHULZ HANS PETER ,  THOMAS HERBERT

IPC分类号： C07D277/10 ,  A61K31/426 ,  A61K31/54 ,  A61P33/10 ,  C07C335/20 ,  C07D277/18 ,  C07D279/06 ,  C07D417/12 ,  C07D91/16 ,  C07D93/06

CPC分类号： C07D277/18 ,  C07C335/20

摘要： 2-(4-Aminophenylimino) derivatives of thiazolidine and -4H-5,6dihydro-1,3-thiazines, the corresponding amide and sulfonamide derivatives, and the salts thereof are anthelmintic agents. The compounds, of which 2-(4-aminophenylimino)-N-methylthiazolidine is a typical embodiment, are prepared through cyclization of a thiourea, optionally with subsequent hydrolysis, alkylation or acetylation.

摘要翻译： 噻唑烷和-4H-5,6-二氢-1,3-噻嗪的2-（4-氨基苯基亚氨基）衍生物，相应的酰胺和磺酰胺衍生物及其盐是驱肠剂。 其中2-（4-氨基苯基亚氨基）-N-甲基噻唑烷是典型的实施方案，通过硫脲环化，任选随后的水解，烷基化或乙酰化来制备。

公开(公告)号：US3629442A

公开(公告)日：1971-12-21

申请号：US3629442D

申请日：1969-05-29

申请人： BAYER AG

发明人： HORSTMANN HARALD ,  WOLLWEBER HARTMUND ,  MENG KARL

IPC分类号： C07D307/33 ,  A61K27/00

CPC分类号： C07D307/33

摘要： PHARMACEUTICAL COMPOSITIONS ARE PRODUCED WHICH COMPRISE A COMPOUND OF THE FORMULA:

R IS HYDROGEN OR METHYL; R'' IS HYDROGEN OR LOWER ALKYL. R" IS HYDROGEN OR LOWER ALKYL; AND N IS 0 OR 1; OR A PHARMACEUTICALLY ACCEPTABLE NON-TOXIC SALT THEREOF, IN COMBINATION WITH A PHARMACEUTICALLY ACCEPTABLE INERT DILUENT OR CARRIER. THESE COMPOSITIONS ARE USEFUL FOR THEIR SALURETIC EFFECT AND ARE USEFUL IN TREATING EDEMA AND HYPERTENSION.

WHEREIN:

N(-R)-O2S-)BENZENE (VII) WITH R'' ATTACHED AS IN III

1-(H2N-O2S-),2-CL,5-(HOOC-CH(-R")-(CH2)N-CH2-CH(-OH)-CH2-

CH2-N(-R)-O2S-)BENZENE (III)

1-(H2N-O2S-),2-CL,5-((-CH2-(CH2)N-CH(-R")-CO-O-)(-R'')>CH2-

公开(公告)号：US3911010A

公开(公告)日：1975-10-07

申请号：US39869273

申请日：1973-09-19

申请人： BAYER AG

发明人： WOLLWEBER HARTMUND ,  FLUCKE WINFRIED

IPC分类号： C07C259/14 ,  C07D209/42 ,  C07C123/00

CPC分类号： C07C259/14 ,  C07D209/42

摘要： The present invention relates to new aminophenylamidines, to processes for their production, and to their pharmaceutical use. These new compounds are useful as paraciticides, especially as anthelmintics. Some acylaminophenylformamidines, such as N-(p-acetamidophenyl)N'',N''-dimethylformamidine (U.S. Pat. No. 3,184,482) and N-phenylacetamidines, such as N-(p-chlorophenyl)-N'',N''dimethylacetamidine, are already known. These compounds are however inactive against the helminths mentioned below.

摘要翻译： 本发明涉及新的氨基苯基脒，其制备方法及其药物用途。 这些新化合物可用作杀螨剂，特别是作为驱肠虫剂。

公开(公告)号：US3594477A

公开(公告)日：1971-07-20

申请号：US3594477D

申请日：1969-01-14

申请人： BAYER AG

发明人： WOLLWEBER HARTMUND ,  HILTMANN RUDOLF ,  HOFFMEISTER FRIEDRICH ,  KRONEBERG HANS-GUENTHER

IPC分类号： A61K31/44 ,  C07D401/12 ,  A61K27/00

CPC分类号： C07D401/12 ,  A61K31/44

摘要： DEXTRO-ROTATORY AND LEVO-ROTATORY ISOMERS OF N-ACYL-N(2''-PYRIDYL)-1-PIPERIDINO-2-AMINOPROPANES OF THE FORMULA:

2-(PIPERIDINO-CH2-CH(-CH3)-N(-CO-R)-)PYRIDINE

WHEREIN R IS METHYL OR ETHYL OR A PHARMACEUTICALLY ACCEPTABLE NON-TOXIC ACID SALT THEREOF EXHIBIT PHARMACEUTICAL PROPERTIES WHICH DIFFER QUALITATIVELY FROM THE RACEMATE. THE L-ISOMER EXHIBITS APPROXIMATELY THE SAME ANALGESIC ACTIVITY AS THE RACEMATE BUT ALSO EXHIBITS A STRONG SEDATIVE EFFECT. THE D-ISOMER EXHIBITS APPROXIMATELY THE SAME ANALGESIC ACTIVITY AS THE RACEMATE BUT EXHIBITS ALSO A CENTRAL NERVOUS SYSTEM STIMULANT EFFECT.

公开(公告)号：US3563994A

公开(公告)日：1971-02-16

申请号：US3563994D

申请日：1968-04-11

申请人： BAYER AG

发明人： WOLLWEBER HARTMUND ,  HILTMANN RUDOLF ,  STOEPEL KURT

IPC分类号： C07D207/22 ,  C07D211/72 ,  C07D29/28

CPC分类号： C07D211/72 ,  C07D207/22

摘要： THERE ARE PROVIDED 2-PHENYL-IMINO-1-AZA-CYCLOALKANES HAVING AN O-SUBSTITUENT ON THE PHENYL NUCLEUS COMPRISING ALKYL, ALKOXY, HALOGEN, TRIFLUOROMETHYL, ALKANOYL AND MERCAPTOALKYL, WHEREIN ALKYL, ALKOXY AND ALKANOYL HAVE 1-4 CARBON ATOMS. THE COMPOUNDS ARE USEFUL FOR THEIR BLOOD PRESSURE DEPRESSANT ACTIVITY AND THEIR CNS DAMPING EFFECT. THEY CAN BE PREPARED BY REACTING SUBSTITUTED ANILINES WITH SELECTED LACTAMS. A REPRESENTATIVE COMPOUND IS 2(2'',6''-DIMETHYLPHENYL)-IMINO-1-AZA-CYCLOPENTANE AND ITS HCI ACID ADDITION SALT.

公开(公告)号：US3513182A

公开(公告)日：1970-05-19

申请号：US3513182D

申请日：1966-07-18

申请人： BAYER AG

发明人： WOLLWEBER HARTMUND ,  HILTMANN RUDOLF ,  BEHRENZ WOLFGANG ,  MULLER GERHARD

IPC分类号： A01N9/16 ,  C07C143/80

公开(公告)号：US3911013A

公开(公告)日：1975-10-07

申请号：US51557674

申请日：1974-10-17

申请人： BAYER AG

发明人： WOLLWEBER HARTMUND ,  FLUCKE WINFRIED

IPC分类号： A61K31/155 ,  C07C123/00

CPC分类号： A61K31/155

摘要： 4-Amino substituted phenylamidine are anthelmintics. The compounds, of which N-(4-aminophenyl)-N'',N''-dimethylacetamidine is a representative embodiment, can be prepared through treatment of a 4-amino aniline with a carboxylic acidamide or thioamide, reduction of an appropriately substituted 4-aminophenylamidine, optionally followed by alkylation of the resultant 4-aminophenylamidine, formation of a Schiff base followed by quaternization and hydrolysis, or hydrolysis of a 4-acylaminophenylamidine.

摘要翻译： 4-氨基取代的苯脒是驱虫剂。 可以通过用羧酸酰胺或硫代酰胺处理4-氨基苯胺来制备其中N-（4-氨基苯基）-N'，N'-二甲基乙脒是其代表性实施方案的化合物，还原适当取代的4- 任选地随后将所得4-氨基苯基 - 脒烷基化，形成希夫碱，然后季铵化和水解，或4-酰氨基苯基脒的水解。

公开(公告)号：US3897488A

公开(公告)日：1975-07-29

申请号：US43274474

申请日：1974-01-11

申请人： BAYER AG

发明人： HORSTMANN HARALD ,  WOLLWEBER HARTMUND ,  MENG KARL

IPC分类号： C07D207/08 ,  C07C143/40

CPC分类号： C07D207/08

摘要： Pharmaceutical compositions are produced which comprise a compound of the formula:

WHEREIN: R is hydrogen or methyl; R'' is hydrogen or lower alkyl; R'''' is hydrogen or lower alkyl; and N IS 0 OR 1; OR A PHARMACEUTICALLY ACCEPTABLE NON-TOXIC SALT THEREOF, IN COMBINATION WITH A PHARMACEUTICALLY ACCEPTABLE INERT DILUENT OR CARRIER. These compositions are useful for their saluretic effect and are useful in treating edema and hypertension.

摘要翻译： 制备药物组合物，其包含下式的化合物：

公开(公告)号：US3894039A

公开(公告)日：1975-07-08

申请号：US27869972

申请日：1972-08-07

申请人： BAYER AG

发明人： HILTMANN RUDOLF ,  WOLLWEBER HARTMUND ,  HERMANN GUNTHER

IPC分类号： A01N43/50 ,  C07D233/42 ,  C07D233/46 ,  C07D233/48 ,  C07D49/30 ,  C07D49/34

CPC分类号： C07D233/46 ,  C07D233/42 ,  C07D233/48

摘要： 1-HALOPHENYL-2-IMINO-IMIDAZOLIDINES OF THE FORMULA

IN WHICH Hal is halogen, R is hydrogen, halogen, lower alkyl, lower alkoxy or halo-lower alkyl, R'' and R'''' each independently is hydrogen or alkyl of one to six carbon atoms, and N IS 1, 2, 3 OR 4, AND THEIR SALTS, WHICH POSSESS BIRD REPELLENT PROPERTIES.

摘要翻译： 其中Hal是卤素，R是氢，卤素，低级烷基，低级烷氧基或卤素 - 低级烷基，式中R'和R“各自独立地是氢或一个烷基的烷基， 六个碳原子和N个IS 1,2,3或4，以及它们的销售，具有良好的性能。