IL40338A - 2-(4-aminophenylimino)thiazines and thiazolidines,their preparation and veterinary and pharmaceutical compositions containing them - Google Patents

2-(4-aminophenylimino)thiazines and thiazolidines,their preparation and veterinary and pharmaceutical compositions containing them

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Publication number
IL40338A
IL40338A IL40338A IL4033872A IL40338A IL 40338 A IL40338 A IL 40338A IL 40338 A IL40338 A IL 40338A IL 4033872 A IL4033872 A IL 4033872A IL 40338 A IL40338 A IL 40338A
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Israel
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general formula
compound
group
process according
reacted
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IL40338A
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IL40338A0 (en
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Bayer Ag
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Publication date
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Publication of IL40338A0 publication Critical patent/IL40338A0/en
Publication of IL40338A publication Critical patent/IL40338A/en

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/08Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D277/12Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/18Nitrogen atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • A61P33/10Anthelmintics
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C335/00Thioureas, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C335/04Derivatives of thiourea
    • C07C335/16Derivatives of thiourea having nitrogen atoms of thiourea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C335/20Derivatives of thiourea having nitrogen atoms of thiourea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by nitrogen atoms, not being part of nitro or nitroso groups

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

2-(4-Aminophenylimino) derivatives of thiazolidine and -4H-5,6-dihydro-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. [US3860590A]

Claims (9)

1. CLAIMS 1. 2-(Aminophenylimino)-thiazolines and thiazolid-ines of the following general formula or their salts: in which R is a straight-chain or branched alkyl or alkenyl group ~ and R1 is a hydrogen atom or a straight-chain or 6 7 branched alkyl or alkenyl group, or a -COR or. -S02R group; in which R is a hydrogen atom or a straight-chain or branched alkyl, alkenyl, alkoxy, alkoxyalkyl, phenoxy-alkyl, furyl or. phenyl optionally substituted with riitro, chlorine, bromine ; fluorine, alkyl, alkoxy or trifluoro- 7 methyl; R is a straight-chain or branched alkyl group; 2 3 R and R can be identical or different and are each a hydrogen atom or a straight-chain or branched alkyl, alkenyl or alkoxy group, or a halogen, atom or trifluoro-methyl radical; R^ and ^ are each a hydrogen atom and n is 2 or 3. 2. Compounds according to Claim 1 in which R is an alkyl group with 1 or 2 carbon atoms or an ally! or meth-allyl or crotyl group; R1 is an alkyl group with 1 to 3 6 7 carbon atoms, or an allyl, -COR or -S02 group; in 6 which R is a hydrogen atom or a straight .chain or branched alkyl or alkenyl group with up to 3 carbon atoms or the furyl, or phenyl radical, or an alkoxy radical with up to 7 4 carbon atoms; R is an alkyl group^ with 1 or 2 carbon 2 3 atoms;. R is a hydrogen atom; R is a hydrogen or chlorine 4 5 i · - 55 - 40338/2 13. 2-[4-(4-nltrobenzoylamino)-phenylimino]~N-methyl-thiazolidine. 14. 2-(4-Isobutylaminophenylimino)-N-methyi-thiazolidine. 1 . 2-[ 4-( 4-chlorobenzoylaraino)-phenylimino]-N-methy1-thiazolidine hydrochloride. 16. 2-[4-(3-Chlorohenzoylamino)-pheriylimino]-N-methyl-thiazolidine hydrochloride. , 17. 2-[ 4-( 2-Chlorobenzoylamino)-phenyl-imino]-N-methy1-thiazolidine hydrochloride. 18. 2-[ 4-( 4-me h l-benzoylaraino)-phenylimino]-N-methyl-thiazolidine hydrochloride. 19. 2-[ 4-(3-methylbenzoylamino)-phenylimino]-N-methy1-thiazolidine hydrochloride. 20. 2-[4-( 2-methylbenzoylamino)-phenylimino]-N-methyl-thiazolidine hydrochloride. 21. 2-[4-(2f6-dichlorobenzoylamino)-phenylimino]-N-methyl-thiazolidine hydrochloride. 22. The compound according to claim 1 that is set forth in Example 7a. 23.. Compounds according to claim 1 , 2 or 3 that are hereinbefore specifically mentioned, other than those claimed in any of claims 4 to 22. 24. process for the production of a compound according to any of claims 1 to 23 in which: -(A) a phenylthiourea of the general formula:- . (in which R, R1 , R2, 5, R^, R5 and n are as defined in claim 1 or 2 and X is a halogen, sulphonyloxy, or hydroxyl is cycl sed under the influence of a hydroxylic solvent or under the influence of an acid; or (B) a phe is cyclized by reaction with a compound of the general formula:- (in which general formulae. R, R1 , R2, R^, R4, R5, X and n are as defined in (A) and Y" is X or an KH2 group); or (C) a 2-(aminophenylimino)-3-aza-1 -thia-cycloalkane of the general formula is reacted with an alkylating agent of the general formula:- B - R (VI) (in which general formulae (V) and (VI) R, R1 , R2, R5, R4, R5 and n are as defined in claim 1 or 2 and B is a radical which is eliminated as HB); or (D) a 2-(4-nitrophenylimino)-3-aza-1 -thia-cycloalkane of -..'J - 57 - 40338/2 is reduced to produce an amine of the general formula:- (in which general formulae R, R2, R5, R4", R5 and n are as defined in claim 1 or 2) and, when a compound of any preceding claim is required in which R1 is not hydrogen, this amine is then either (aa) [when a compound of any preceding claim in which is a straight or branched-chain alkyl or alkenyl. group is required] reacted with an alkylating agent of the general formula B - R10 (IX) [in which B is as defined in (C) and R10 is a straight-chain or branched alkyl or alkenyl group ] ; or (bb) [when a compound of any preceding claim in which R1 is an alkyl group is required] reacted with ah oxo compound, of the general formula:- - 58 - 40338/2 (i which R is a hydrogen atom or an alkyl group and I is an alkyl group) to produce a Schiff *s, base which is then reduced to produce the required compound of any preceding claim; or (cc) [whe a compound of any preceding claim in which R 6 7 ie a -COR or -CO group is required] reacted with an acylating or sulphonylating agent of the general formula:- Y - 2 (XI) 6 7 ( in which Z is a -COR or -S02 ' , group as required and Y is a group which is eliminated as HY) ; or (dd) [when a compound Of any preceding claim in which R1 is a straight-chain or branched alkyl,or alkenyl group —; '—— :— is required] reacted with an aliphatic or aromatic aldehyde to give a Schiff's base, which is then quaternised with a compound of the general formula:- B - R10 (IX) [in which B and are as defined in (aa)] and thereafter the aldehyde group is split off hydrolytically to give the required compound of any preceding claim; [when a compound of any preceding claim in which R quired] a compound of the general formula (i which R, R2, .R^, ^, ^, ^ and n are as defined in claim 1 or 2) is hydrolysed. 25. A process according to claim 24(A) or 24(B) in which the thiourea of general formula (II) or (III) is cyclized by' heating in an inert diluent at the boiling point of the diluent. 26. A process according to claim 24(A), 24(B), or 25, in which X is chlorine, bromine, or tosyloxy. 27. A process according to claim 24(C) in which the alkylating agen of general formula (VI) and the compound of general formula (V) are reacted at 20 to 80¾ in the presence of an inert organic diluent. 28. A process according to claim 24(C) or 27 in which B is a halogen, ar lsulphonyloxy, or alk ls lphonyloxy radical. 29. A process according to claim 28 in which B is a chlorine, bromine, benzenesulphonyloxy or methanesulphonyloxy radical· 30. . A process according to claim 24(D) in which the compou of general formula (VII) is reduced with hydrogen in the presence of a noble metal catalyst at 20 to 80°C and 60 to 80 atmospheres gauge. 31 i A. process according to claim 24(D) in which the compou of general formula (VII) is reduced with zinc/hydrochloric , ; • 5 . . '■" 1 0 , -'. " ' radical. .1 5 3β . A process according to claim .24(D-^) or any of claims 3Q to 33 in which the amine of general formula (VIII) and the oxo compound of general formula X are reacted in ..... substantially mola amounts in the presence of an organic ■':.' ·■■ solvent. 20 : 37. A process according to claim 24(1^) or any of claims 30 to 33 and 36 , in which the Schiff's base is reduced. by ', hydrogen with a. noble metal catalyst at about 20°C and about v.- ■ . 1 to 80 atmospheres gauge in the presence of a solvent. 38. A process according to claim 24(D _) or any of claims 25 30 to 33 in which the acylating or sulphonating agent of the general formula (XI) and the amine of general formula (X) are reacted in substantially molar amounts at 20 to 90°C in an - inert organic solvent, • 39. A process according to claim 2 (D^d) or any of claims 30 30 to .33 in which the aldehyde and the amine of general ' . . formula; (VIII ) are reacted in substantially molar amounts at ' 20 to 40°G in an inert organic solvent to produce the 23 or 46 in the form of a sterile or isotonic aqueous ' solution. , , ' 49. A composition according to claim 47 or 48 containing . from 0.5 to 90 of active ingredient by weight. 50. Pharmaceutical compositions substantially as hereinbefore described or specifically .exemplified. 51. , A medicament in dosage unit form comprising a compound according to any of claims .1 to 21 , .23 or 46 either alone or in admixture with a diluent. 5.
2. A medicament in the form of tablets, pills, dragees, capsul.es, ampoules or suppositories comprising, a compound according to any of claims 1 to 21 , 2 or 46 , either alone or in admixture with a diluent. , 5
3. A medicament in dosage unit form according to claim 51 or 52, adapted for a daily dose of 50 to 9/000 mg. 5
4. A medicament in dosage uni form, substantially as ■hereinbefore described or specifically exemplified. 5
5. A method of combatting parasites in human and non-human animals which comprises administering to the animals an active compound according to any of claims 1 to 21, 23 or 46 either alone or- in admixture with a diluent or in the form of a medicament according to. an of claims 51 to 54. 5
6. A method according to claim 55 in which the parasite is - ' a helminth. 5
7. A method according to claim 56 in which the parasite is a nematode. · .5
8. A method according to claim 55, 56 or 57 in which the active compound is administered in an amount of 1 to 100 mg per body weight per day. ; . 5
9. A method of combatting parasites substantially as hereinbefore described or specifically exemplified.
IL40338A 1971-09-14 1972-09-12 2-(4-aminophenylimino)thiazines and thiazolidines,their preparation and veterinary and pharmaceutical compositions containing them IL40338A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE2145807A DE2145807A1 (en) 1971-09-14 1971-09-14 2- (AMINOPHENYLIMINO) -3-AZA-1-THIACYCLOALKANE, METHOD OF MANUFACTURING AND USE AS A MEDICINAL PRODUCT

Publications (2)

Publication Number Publication Date
IL40338A0 IL40338A0 (en) 1972-11-28
IL40338A true IL40338A (en) 1976-01-30

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Country Status (22)

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US (1) US3860590A (en)
JP (2) JPS4836169A (en)
AT (1) AT322548B (en)
AU (1) AU464649B2 (en)
BE (1) BE788743A (en)
CA (1) CA1007638A (en)
CH (2) CH569724A5 (en)
DD (2) DD103898A5 (en)
DE (1) DE2145807A1 (en)
EG (1) EG11037A (en)
ES (4) ES406622A1 (en)
FR (1) FR2154512B1 (en)
GB (1) GB1377265A (en)
HU (1) HU167410B (en)
IE (1) IE36698B1 (en)
IL (1) IL40338A (en)
NL (1) NL7212419A (en)
PL (4) PL89701B1 (en)
RO (4) RO68389A (en)
SE (1) SE412756B (en)
SU (3) SU556728A3 (en)
ZA (1) ZA726271B (en)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HU167761B (en) * 1973-07-12 1975-12-25
IL52927A (en) * 1976-09-17 1980-01-31 Ciba Geigy Ag 2-(n-methylcarbamoyloxyphenyl imino)-4-thiazoline derivatives their production and their use as pesticides
US4140784A (en) * 1976-09-17 1979-02-20 Ciba-Geigy Corporation Novel thiazolidines
DE2758005A1 (en) 1977-12-24 1979-06-28 Bayer Ag PHOSPHONYLUREIDOBENZOL DERIVATIVES, METHOD FOR THE PRODUCTION THEREOF AND THEIR USE AS MEDICINAL PRODUCTS
DE3632042A1 (en) * 1986-03-08 1987-09-10 Bayer Ag DIARYLSULFID DERIVATIVES
US6353006B1 (en) 1999-01-14 2002-03-05 Bayer Corporation Substituted 2-arylimino heterocycles and compositions containing them, for use as progesterone receptor binding agents
WO2001019807A1 (en) 1999-09-14 2001-03-22 Shionogi & Co., Ltd. 2-imino-1,3-thiazine derivatives
DE102008030764A1 (en) * 2008-06-28 2009-12-31 Bayer Animal Health Gmbh Combination of amidine derivatives with cyclic depsipeptides

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US327708A (en) * 1885-10-06 Wet-ore concentrator
US2877232A (en) * 1957-12-31 1959-03-10 Ciba Pharm Prod Inc 2-(4-isopentyloxyphenyl)-imino, 3 (4-isopentyloxyphenyl)-thiazolidine and therapeutically useful salts
US3297708A (en) * 1965-10-06 1967-01-10 American Cyanamid Co Method of preparing thiazolidines
FR1516854A (en) * 1966-12-20 1968-02-05 Aquitaine Petrole Process for the production of imino-thiazolidines

Also Published As

Publication number Publication date
RO84247B (en) 1984-07-30
AU4660472A (en) 1974-03-21
GB1377265A (en) 1974-12-11
IL40338A0 (en) 1972-11-28
EG11037A (en) 1977-12-31
SE412756B (en) 1980-03-17
SU505363A3 (en) 1976-02-28
RO84248B (en) 1984-07-30
PL93588B1 (en) 1977-06-30
PL93690B1 (en) 1977-06-30
ZA726271B (en) 1973-06-27
NL7212419A (en) 1973-03-16
PL89701B1 (en) 1976-12-31
CH569724A5 (en) 1975-11-28
AT322548B (en) 1975-05-26
RO84247A (en) 1984-05-23
JPS4836169A (en) 1973-05-28
JPS4836168A (en) 1973-05-28
ES436202A1 (en) 1977-02-16
FR2154512B1 (en) 1976-04-23
SU455544A3 (en) 1974-12-30
SU556728A3 (en) 1977-04-30
RO68389A (en) 1981-09-24
SU439988A3 (en) 1974-08-15
CA1007638A (en) 1977-03-29
ES436200A1 (en) 1977-01-16
RO84248A (en) 1984-05-23
DD103898A5 (en) 1974-02-12
US3860590A (en) 1975-01-14
ES436201A1 (en) 1977-01-16
FR2154512A1 (en) 1973-05-11
CH587258A5 (en) 1977-04-29
AU464649B2 (en) 1975-09-04
ES406622A1 (en) 1976-01-16
PL93669B1 (en) 1977-06-30
DD105990A5 (en) 1974-05-20
DE2145807A1 (en) 1973-03-22
IE36698L (en) 1973-03-14
HU167410B (en) 1976-04-28
IE36698B1 (en) 1977-02-02
BE788743A (en) 1973-03-13
RO68372A (en) 1981-06-26

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