公开(公告)号：KR800001135B1

公开(公告)日：1980-10-12

申请号：KR790004569

申请日：1979-12-22

Applicant: HOECHST AG

Inventor： MANIA D ,  BORMANN D ,  MERKEL W

IPC: C07D207/04

Abstract: This patent refers mainly to the method how to manuf. sulfamyl-benzoic acid (I) by reacting formula II or III with L-CH2-A-CH2-L and hydro-analyze B in formula III. In I, A represents hydrocarbon like Z1-Z2C-(CH2)n-CZ3-Z4, Z2C-Z1, where Z means double bond, X bears OR2, SR2, SOR2, SO2R2, where R2 means alkyl, phenyl, cyclic compound, sometimes also bears disubstituted amino group, R shows alkyl group, L represents isolating radical, B means a protecting group like CR4-NR5-Rb. R means alkyl group of low grade and the three of R's can form a ring.

公开(公告)号：KR800001132B1

公开(公告)日：1980-10-12

申请号：KR790002788

申请日：1979-08-16

Applicant: HOECHST AG

Inventor： BORMANN D ,  MERKEL W ,  MUSHABECK R

IPC: C07D207/00

Abstract: Heterocylic group substituted 5-sulfamoyl benzoic acid and its salts (I; R1, R2 = H, C1-4 alkyl; when R1 is H, R2 is C2-5 alkoxymethyl, phenoxymethyl or phenylthiomethyl; R3 = H, C1-4 alkyls, C5-6 cycloalkyl, phenyl, benzyl; X = halogen, CF3, CCl3, C1-6 satd. or unsatd. alkyl or alkoxy, benzyl, OR4, SR4, SOR4, SO2R4 (R4 = Hal, OH, NH2, CF3, NO2); A= halogen, alkyl, aralkyl or side chain aryl group substituted C1-3 alkylene or singled bond; L = eliminatig group), useful as diuretic agent, were prepd. by treating sulfamoyl benzoic acid derivs. (II) with acid or base for eliminating HL group.

公开(公告)号：KR800001130B1

公开(公告)日：1980-10-12

申请号：KR750001561

申请日：1975-07-18

Applicant: HOECHST AG

Inventor： BORMANN D ,  MANIA D ,  MERKEL W

IPC: C07D207/04

Abstract: Sulfamylbenzoic acid derivs [I; R = C1-10 alkyl; X = OR2, SR2, SOR2, SO2R2(R2 = C1-5 branched alkyl, etc.), A = Z1-C-Z2(Z1 = Z2 or other H, C1-4 lower alkyl, aryl, halogen) are useful as diuretics and saluretics were prepd. by nitration of II [Y = halogen, B = protected gp. of CR4-NR5R6(R4 = R5 = R6 or other alkyl gp., R4, R5, R6 is joined to each other) , reducting, followed by redn. with NaBH4 to give III. Hydrolysis of III with acid or alkali give I.

公开(公告)号：KR810000981B1

公开(公告)日：1981-08-25

申请号：KR780000611

申请日：1978-03-09

Applicant: HOECHST AG

Inventor： BORMANN D ,  WORM M ,  SCHRINNER E ,  KNABE B

IPC: A61K31/545 ,  C07D501/36

Abstract: Title compds. [I; R1 = H, lower alkoxy; R2=H, alkyl, phthalide; X = O, S, Me; A = H, alkoxy, halogen, CH2Y(Y = H, acyloxy, alkoxy, carbamoyloxy, or acyl, alkyl, 5-6membered heterocyclic compd. -substituted thionyl group) were prepd. by reaction of II and III, and removing protected-group of amino from IV. Thus, III(R = 2-triphenylmethyl) in MeCl, Et3N and pivaloylchloride were mixed and reacted with II(R1,R2,A = H) and Et3N to give IV(R = 2-triphenylmethyl; R1,R2,A = H). IV was reacted with formic acid to give yellow crystal-form I.

公开(公告)号：KR800001133B1

公开(公告)日：1980-10-12

申请号：KR740003720

申请日：1974-09-28

Applicant: HOECHST AG

Inventor： BORMANN D ,  MERKEL W ,  MUSHABECK R

IPC: C07D207/00

Abstract: Title compds. (I; R1, R2 = H, C1-4 alkyl, alkoxymethyl, phenoxymethyl, phenylthiomethyl; R3 = H, C1-4 alkyl, C5-6 cycloalkyl, Ph, benzyl, benzhydryl, C3-5 alkanoyloxymethyl; x = halogen, CF3, CCl3, alkyl, alkoxy; A = single bond, substituted alkylene), useful diuretic, were prepd. from 3-substituted sulfamoyl benzoic acid derivs.(II, z = two H, one O) by redn. with HB complex in the presence of Lewis acid or various methods.

公开(公告)号：US3781283A

公开(公告)日：1973-12-25

申请号：US3781283D

申请日：1971-12-28

Applicant: HOECHST AG

Inventor： BORMANN D ,  WORM M

IPC: C07D205/08 ,  C07D501/10 ,  C07F9/54 ,  C07F9/568 ,  C07D99/24

CPC classification number: C07F9/5683 ,  C07D205/08 ,  C07F9/5407

Abstract: PROCESS FOR PREPARING A CEPHEM-CARBOXYLIC ACID ESTER OF THE FORMULA

7-(R-NH-),2-(R''-OOC-),3-CH3-2-CEPHEM

BY HEATING A PENICILLIN OXIDE OF THE FORMULA

6-(R-NH-),2-(R''-OOC-),3,3-DI(CH3-)PENAM

IN A SOLVENT WITH A PHOSPHONIUM SALT OF THE FORMULA

R1-P(+)(-R2)(-R3)-R4 X(-)

IN THE FORMULAS; R IS ACYL; R'' IS ALKYL, SUBSTITUTED ALKYL, CYCLOALKYL, OR ARYL; R1, R2 ARE EACH SUBSTITUTED OR UNSUBSTITUTED HYDROCARBON; R4 IS METHYL SUBSTITUTED BY AN ELECTRON-ATTRACTING GROUP, AND MAY CONTAIN A FURTHER SUBSTITUENT; AND ? IS AN ANION.

公开(公告)号：KR800001134B1

公开(公告)日：1980-10-12

申请号：KR790004568

申请日：1979-12-22

Applicant: HOECHST AG

Inventor： MANIA D ,  MERKEL W ,  BORMANN D

IPC: C07D207/04

Abstract: Sulfamoylbenzoic acids I(R = OR2, SR2, SOR2, SO2R2; R2 = C1-5 alkyl, cycloalkyl, phenyl) X = desubstituted amino group, R = H, C1-10 alkyl) were prepd. by reducing pyrrolo-compd. II (R6, R7 = H, halogen, C1-C4 alkyl). Thus, 4-chloro-5 sulfamo- ylbenzoic acid was stirred with DMF and SOCl2 at room temp. for 2 hr to give 4-chloro-5-N, N-dimethylaminomethyleneamino-sulfonybenzoic acid. I are useful as diurecics.

公开(公告)号：KR800001131B1

公开(公告)日：1980-10-12

申请号：KR790002786

申请日：1979-08-16

Applicant: HOECHST AG

Inventor： BORMANN D ,  MERKEL W ,  MUSHABECK R

IPC: C07D207/00

Abstract: Title compds. (I; R1, R2 = H, C1-4 alkyl; R3 = H, C1-4 alkyl, phenyl, benzyl, C3-5 alkanoyloxymethyl; X = halogen, CF3, C1-6 alkyl etc.; A = single bond or C1-3 alkylene), with diuretic and saluretic action are prepd. by treating 5-halo- genosulfonyl benzoic acid derivs.(II; Hal = halogen) with III. If, necessary a process such as adding hydrogen to double bond, inducing double bond, esterifying carboxylic acid, hydrolysing carboxylic ester, separating protected group and liberating hydroxyl, amino or mercapto group and treating carboxylic acid with base or acid can be accepted.

公开(公告)号：KR790001269B1

公开(公告)日：1979-09-20

申请号：KR740003603

申请日：1974-09-16

Applicant: HOECHST AG

Inventor： BORMANN D ,  WULF MERKEL

Abstract: Title compds, (I; R1,R2 = C1-4 alkyl or H, R3 = H, C1-6 main or side-chain alkyl group, R4,R5 = H, hydroxy, C1-5 alkoxy or alkyl, amino, mono or dialkylamino, R6 = halogen, hydroxy, mercapto, cyano or amino group substituted C1-4 main or side-chain alkyl group contains O,N, or S useful as diuretic, were pprepd. by reduction of 3-acylamino-5-sulfamyl-benzoic acid with (BH3)2 in the presence of Lewis acid at room temp. or 80≦̸C.

公开(公告)号：SE425486B

公开(公告)日：1982-10-04

申请号：SE7802175

申请日：1978-02-27

Applicant: HOECHST AG

Inventor： BORMANN D ,  MERKEL W ,  MUSCHAWECK R ,  MANIA D

IPC: C07D207/04 ,  A61K20060101 ,  A61K31/125 ,  A61K31/18 ,  A61K31/33 ,  A61K31/395 ,  A61K31/397 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/402 ,  A61K31/403 ,  A61K31/4035 ,  A61K31/445 ,  A61K31/45 ,  A61K31/635 ,  A61P7/10 ,  C07C20060101 ,  C07D20060101 ,  C07D205/04 ,  C07D205/10 ,  C07D207/02 ,  C07D207/06 ,  C07D207/08 ,  C07D207/10 ,  C07D207/18 ,  C07D207/20 ,  C07D207/32 ,  C07D207/327 ,  C07D207/40 ,  C07D207/404 ,  C07D207/44 ,  C07D207/452 ,  C07D209/00 ,  C07D209/44 ,  C07D209/48 ,  C07D209/52 ,  C07D209/94 ,  C07D211/04 ,  C07D211/14 ,  C07D211/18 ,  C07D211/30 ,  C07D211/32 ,  C07D211/34 ,  C07D211/38 ,  C07D211/70 ,  C07D211/88 ,  C07D265/32 ,  C07D265/33 ,  C07D295/00 ,  C07D295/02 ,  C07D295/04 ,  C07D295/08 ,  C07D295/10 ,  C07D295/116 ,  C07D295/12 ,  C07D295/14 ,  C07D295/155 ,  C07D295/18 ,  C07D295/192 ,  C07D317/00 ,  C07D403/10 ,  C07D405/10 ,  C07D407/10 ,  C07D413/10

Abstract: 1504505 Sulphonamides HOECHST AG 25 April 1975 [25 April 1974 27 Dec 1974] 17337/75 Heading C2C The invention comprises novel compounds (I) (including salts thereof) in which R 1 and R 2 , which may be identical or different, each represents a hydrogen atom or an alkyl group having from 1 to 4 carbon atoms, and, if R 1 represents a hydrogen atom, R 2 may also represent an alkoxymethyl group having from 1 to 4 carbon atoms in the alkoxy radical, a phenoxymethyl group or a phenylthiomethyl group, R 3 represents a hydrogen atom, a straight or branched chain alkyl group having from 1 to 4 carbon atoms, a cycloalkyl group, having 5 or 6 ring members, one of which may be replaced by an oxygen or sulphur atom, a phenyl or benzyl group which may be substituted in the phenyl nucleus by one or more substituents selected from nitro groups, alkyl groups having from 1 to 3 carbon atoms, alkoxy groups having from 1 to 5 carbon atoms and halogen atoms, or represents a benzhydryl group or an alkanoyloxymethyl group having 2 to 4 carbon atoms in the alkanoyl part, X represents a halogen atom, a CF 3 or CCl 3 group, a straight or branched chain, saturated or unsaturated alkyl group having from 1 to 6 carbon atoms, a benzyl group which may be substituted in the phenyl nucleus by one or more substituents selected from halogen atoms, hydroxy and amino groups, and alkyl and alkoxy groups, or represents one of the groups -O-R 4 , -S-R 4 , SO-R 4 , SO 2 -R 4 and NR 4 R 5 , in which R 4 represents a phenyl group which may be substituted by one or more substituents selected from halogen atoms, CF 3 , OH and amino groups, alkyl and alkoxy groups having from 1 to 4 carbon atoms, and SO 2 NH 2 groups, or represents a straight or branched chain alkyl group having from 1 to 4 carbon atoms which may be substituted by a phenyl, pyridyl, furyl or thienyl group, and R 5 represents a hydrogen atom, a straight or branched chain alkyl group having from 1 to 4 carbon atoms, and the group NR 4 R 5 may represent a saturated, heterocyclic, 5- or 6-membered ring which may be interrupted by an O-, N- or S- atom, A represents a single bond, or an alkylene chain of 1 to 3 carbon atoms which may be unsaturated, interrupted by O-, N- or S-atoms or substituted by halogen atoms and/or substituted by alkyl, aralkyl, aryl groups or by mono-nuclear hetero-aromatic rings, or A represents an ortho-phenylene radical or the grouping in which Y represents a single bond or an alkylene group having from 1 to 4 carbon atoms, and R 6 and R 7 , which may be identical or different, each represents a hydrogen or halogen atom or an alkyl group having from 1 to 4 carbon atoms. They are made by standard methods. Pharmaceutical preparations having diuretic and saluretic action contain (I) as active ingredient. Administration is enterally or parenterally.