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    Aminophenylamidines their production and their medicinal use
    12.
    发明授权
    Aminophenylamidines their production and their medicinal use 失效
    氨基苯基脒的生产及其药用

    公开(公告)号：US3925471A

    公开(公告)日：1975-12-09

    申请号：US51562774

    申请日：1974-10-17

    Applicant: BAYER AG

    Inventor： WOLLWEBER HARTMUND ,  FLUCKE WINFRIED

    IPC: A61K31/155 ,  C07C123/00

    CPC classification number: A61K31/155

    Abstract: 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.

    Abstract translation: 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。

    Aminophenylamidines, their production and their medicinal use
    13.
    发明授权
    Aminophenylamidines, their production and their medicinal use 失效
    氨基苯基脒，其生产和药用

    公开(公告)号：US3923888A

    公开(公告)日：1975-12-02

    申请号：US39981373

    申请日：1973-09-24

    Applicant: BAYER AG

    Inventor： WOLLWEBER HARTMUND ,  FLUCKE WINFRIED

    IPC: A61K31/155 ,  C07C123/00

    CPC classification number: A61K31/155

    Abstract: The present invention relates to new aminophenylamidines and cycloamidines and salts thereof, to processes for their production, and to their use as medicines, especially as parasiticides. Acylaminophenylformamidines, such as N-(p-acetamidophenyl)-N'', N''-dimethylformamidine (U.S. Pat. No. 3,184,482) are already known. This compound, as well as other formamidine derivatives, are, however, ineffective against helminths. Furthermore, Nphenylacetamidines, such as N-(p-chlorophenyl)-N'',N''dimethylacetamidine, are known. These compounds are also ineffective against helminths.

    Abstract translation: 本发明涉及新的氨基苯基脒和环脒及其盐，其生产方法及其用作药物，特别是作为杀寄生物剂。

    New aminophenylamidines, their production and their medicinal use
    14.
    发明授权
    New aminophenylamidines, their production and their medicinal use 失效
    新型氨基苯脒，其生产及其药用

    公开(公告)号：US3919315A

    公开(公告)日：1975-11-11

    申请号：US42225873

    申请日：1973-12-06

    Applicant: BAYER AG

    Inventor： WOLLWEBER HARTMUND ,  FLUCKE WINFRIED

    IPC: A61K31/155 ,  C07C123/00

    CPC classification number: A61K31/155

    Abstract: 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-amino-phenylamidine, optionally followed by alkylation of the resultant 4aminophenylamidine, formation of a Schiff base followed by quaternization and hydrolysis, or hydrolysis of a 4acylaminophenylamidine.

    Abstract translation: 4-氨基取代的苯脒是驱虫剂。 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可以通过用羧酸酰胺或硫代酰胺处理4-氨基苯胺来制备，还原适当取代的4-氨基 - 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。

    Aminophenylamidines, their production and their medicinal use
    15.
    发明授权
    Aminophenylamidines, their production and their medicinal use 失效
    氨基苯基脒，其生产和药用

    公开(公告)号：US3911014A

    公开(公告)日：1975-10-07

    申请号：US51557774

    申请日：1974-10-17

    Applicant: BAYER AG

    Inventor： WOLLWEBER HARTMUND ,  FLUCKE WINFRIED

    IPC: A61K31/155 ,  C07C123/00

    CPC classification number: A61K31/155

    Abstract: 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.

    Abstract translation: 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。

    Aminophenylamidines as anthelmintic agents
    16.
    发明授权
    Aminophenylamidines as anthelmintic agents 失效
    氨基苯基脒作为驱虫剂

    公开(公告)号：US3903302A

    公开(公告)日：1975-09-02

    申请号：US32814673

    申请日：1973-01-30

    Applicant: BAYER AG

    Inventor： WOLLWEBER HARTMUND ,  FLUCKE WINFRIED

    IPC: A61K31/155 ,  A61K27/00

    CPC classification number: A61K31/155

    Abstract: 4-Amino substituted phenylamidines as 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-amino-phenylamidine, optionally followed by alkylation of the resultant 4aminophenylamidine, formation of a Schiff base followed by quaternization and hydrolysis, or hydrolysis of a 4acylaminophenylamidine.

    Abstract translation: 4-氨基取代的苯脒作为驱肠虫剂。 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可以通过用羧酸酰胺或硫代酰胺处理4-氨基苯胺来制备，还原适当取代的4 任选随后将所得4-氨基苯基脒烷基化，形成席夫碱，然后季铵化和水解，或4-酰氨基苯基脒的水解。

    N-substituted-2-arylimino oxazolidines
    17.
    发明授权
    N-substituted-2-arylimino oxazolidines 失效
    N-取代-2-亚胺基氧杂环丁烷

    公开(公告)号：US3686199A

    公开(公告)日：1972-08-22

    申请号：US3686199D

    申请日：1970-12-17

    Applicant: BAYER AG

    Inventor： WOLLWEBER HARTMUND ,  HILTMANN RUDOLF ,  STENDEL WILHELM

    IPC: A01N43/76 ,  C07D263/28 ,  C07D85/26

    CPC classification number: C07D263/28

    Abstract: 2-((2-R,(R'')N-PHENYL)-N=),3-R"-OXAZOLIDINE

    AND SALTS THEREOF, WHICH POSSESS ACARICIDAL PROPERTIES.

    IN WHICH R DENOTES A HALOGEN ATOM, OR AN OPTIONALLY HALOGENSUBSTITUTED LOWER ALKYL, ALKENYL OR ALKOXY RADICAL, R'' DENOTES A HALOGEN ATOM OR AN ALKYL, ALKOXY, ALKENYL OR FLUOROMETHYL RADICAL, R" DENOTES AN ALKYL, ALKENYL OR ALKYNYL RADICAL CONTAINING UP TO 7 CARBON ATOMS, THE ALKENYL RADICAL OPTIONALLY BEING SUBSTITUTED AT THE DOUBLE BOND BY 1 OR 2 CHLORINE OR BROMINE ATOMS, AND N DENOTES 0, 1 OR 2,
    N-SUBSTITUTED-2-ARYLIMINO-OXAZOLIDINES OF THE FORMULA

    2-cycloalkylamino-oxazolines
    18.
    发明授权
    2-cycloalkylamino-oxazolines 失效
    2-环丙基氨基 - 氧杂环丁烷

    公开(公告)号：US3598833A

    公开(公告)日：1971-08-10

    申请号：US3598833D

    申请日：1967-09-22

    Applicant: BAYER AG

    Inventor： HILTMANN RUDOLF ,  WOLLWEBER HARTMUND ,  STOEPEL KURT ,  PULS WALTER

    IPC: C07C275/26 ,  C07D263/28 ,  C07D85/36

    CPC classification number: C07D263/28 ,  C07C275/26 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/18

    Abstract: 2-CYCLOALKYLAMINO-OXAZOLINES OF THE FORMULA:

    2-((R1-)-CH2-(CH2)N-CH(-R)-)>CH-NH)-2-OXAZOLINE (I)

    WHEREIN R IS LOWER ALKYL OF 1 TO 3 CARBON ATOMS, R1 IS HYDROGEN OR AT LEAST ONE LOWER ALKYL OF 1 TO 5 CARBON ATOMS AND N IS AN INTEGER FROM 2 TO 4, AND WHEREIN THE CYCLOALKYL MOIETY MAY CONTAIN A DOUBLE BOND PROVIDED THAT, IF THERE IS A DOUBLE BOND, SUCH IS NOT IN THE A,BPOSITION, ARE PREPARED BY REACTING 2-CYCLOALKYLISOCYANIDE DICHLORIDES OF THE FORMULA:

    (CL-)2C=N-CH
    WHEREIN R, R1 AND N HAVE THE ABOVE DEFINED MEANINGS AND IN WHICH THE CYCLOALKYL MOIETY MAY CONTAIN A DOUBLE BOND, WITH THE PROVISO THAT IF THERE IS A DOUBLE BOND, SUCH IS NOT IN THE A,B-POSITION, BY HEATING IN HOT WATER OPTIONALLY AT TEMPERATURES ABOVE 100*C. UNDER PRESSURE AND PRECIPITATING THE BASES BY MEANS OF AMMONIA OR ALKALI FROM THE RESULTANT AQUEOUS SOLUTION OF THE 2-CYCLOALKYLAMINO-OXAZOLINE SALTS FORMED. WHEN R1 IS HYDROGEN, THE HYDROGEN ATOM IS ATTACHED TO A CARBON ATOM SO THAT IN ALL CASES EACH CARBON ATOM MAINTAINS THE PROPER VALENCE. R AND R1 MAY BE ALL CIS, ALL TRANS, OR SOME MAY BE CIS AND THE REMAINING TRANS. THE AMINO GROUP ATTACHED TO THE CARBON ATOM IN THE 1-POSITION IN THE CYCLOALKYL RING CAN ALSO BE CIS OR TRANS. THE 2-CYCLOALKYLAMINO-OXAZOLINES ARE USEFUL AS LOCAL ANESTHETICS, SEDATIVES, VASO-CONSTRICTORS, BLOOD PRESSURE DEPRESSANTS AND THEY ALSO EXHIBIT AN INHIBITORY EFFECT ON THE SECRETION OF GASTRIC FLUID THEREBY MAKING THEM VALUABLE FOR TREATING HYPERTONIA AND ULCERS. BY VIRTUE OF THEIR BLOOD SUGAR INCREASING EFFECT, THESE COMPOUNDS CAN ALSO BE USED IN HUMANS AND ANIMALS IN THE TREATMENT OF DISEASES WHEREBY INCREASE IN BLOOD SUGAR IS DESIRABLE. THESE COMPOUNDS ARE ADMINISTERED IN THE SAME DOSAGE RANGE AND BY THE SAME ROUTES OF ADMINISTRATION AS COMPOUNDS ALREADY KNOWN TO HAVE THE ABOVE SPECIFIED EFFECTS AND PROPERTIES. THE ASYMMETRICAL 2-CYCLOALKYLAMINO-OXAZOLINES OF THE PRESENT INVENTION EXIST IN RACEMIC FORM AND AS IS KNOWN SUCH RACEMATES CAN BE RESOLVED INTO THEIR OPTICAL ISOMERS.

    HO-CH2-CH2-NH-CO-NH-CH
    WHEREIN R, R1 AND N ARE AS ABOVE DEFINED, AND IN WHICH THE CYCLOALKYL MOIETY MAY CONTAIN A DOUBLE BOND, WITH THE PROVISO THAT IF THERE IS A DOUBLE BOND, SUCH IS NOT IN THE A,B-POSITION, WITH ETHANOLAMINE IN ORGANIC SOLVENTS OR IN WATER AND, IF DESIRED, WITH THE ADDITION OF A BASE OR THEY MAY BE PREPARED BY CYCLIZING REACTIVE ESTERS OF NCYCLOALKYL-N''-B-HYDROXYETHYL-UREAS OF THE FORMULA:

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