Patent EP0170105A2 successfully refreshed from Google Patents.
EP0170105A2
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EP
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Benzoic acid derivatives
Assignee: Research Foundation Itsuu Laboratory
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Filing: 1985-07-05
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Granted: —
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Expires: 2005-07-05
Abstract
Abstract A benzoic acid derivative represented by the formula (I): wherein R 1 , R 2 , R 3 , R 4 and R s may be the same or different, each represents hydrogen, middle and lower alkyl, and cycloalkyl harring 3 - 7 atoms with proviso each can not be hydrogen simultaneously, and both neighbouring substituents may be combined with each other to form a ring having 5 to 12 carbon atoms, R 6 represents hydroxyl, lower alkoxyl, a group of the formula -NR 7 'R 8 ', wherein R 7 ' and R e ' each represents hydrogen or lower alkyl, X represents a group of the formula wherein R 7 and R 8 represent hydrogen or lower alkyl. Furtheron a process to prepare this substances and a method to determ the type of leukemia is described.
Inventors
- 👤 Koichi Prof. Dr. Shudo
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-30 07:17
CPC Classifications
C; C07; C07D; C07D303/00; C07D303/02; C07D303/38; C07C; C07C233/00; C07C233/64; C07C233/65; C07C65/00; C07C65/32; C07C65/38; C07C65/40; C07D303/40
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
120 words
(1) A benzoic acid derivative represented by the formula (I): wherein R 1 , R 2 , R 3 , R 4 and R 5 may be the same or different, each represents hydrogen, middle and lower alkyl, and cycloalkyl harring 3 -7 atoms with proviso each can not be hydrogen simultaneously, and both neighboring substituents may be combined with each other to form a ring having 5 to 12 carbon atoms, R 6 represents hydroxyl, lower alkoxyl, a group of the formula -NR 7 'R 8 ', wherein R 7 ' and R 8 ' each represents hydrogen or lower alkyl, X represents a group of the formula wherein R 7 and R 8 represent hydrogen or lower alkyl.
Claim 2
Dependent Claim
3 words
(2) p-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthylcarbamoyl)benzoic acid.
Claim 3
Dependent Claim
2 words
(3) 3',5'-Di-tert-butyl-4-carboxychalcone.
Claim 4
Dependent Claim
4 words
(4) p-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalen carboxyamid)benzoic acid.
Claim 5
Dependent Claim
3 words
(5) Methyl p-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthyl)azobenzoate.
Claim 6
Dependent Claim
3 words
(6) l-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthyl)-2-4-(methoxycarbonylphenyl)ethylene oxide.
Claim 7
Dependent Claim
3 words
(7) p-(3,4-diisopropylphenylcarbamoyl)benzoic acid.
Claim 8
Dependent Claim
22 words
(8) A differentiation-inducing agent for neoplastic cells, especially leukemia cells comprising as active ingredient one or more benzoic acids of claim 1.
Claim 9
Dependent Claim
49 words
(9) Method for diagnosis to determe the type of leukemia which comprises the incubation of the blood of a patient with leukemia in vitro in the presence of a compound of claim 1, and the observation of morphological changes and / or of colony formation of the leukemia cell.
Claim 10
Dependent Claim
33 words
(10) Use of one or more benzoic acids of claim 1 as a method for treatment of human or animal leukemia which comprises administring an effective amount of a compound of claim 1.
Claim 11
Dependent Claim
350 words
(11) A process for preparation of a benzoic acid derivative represented by the formula (I) : wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and X are as defined in claim 1, comprising the step of; (a) a compound represented by the formula (I), wherein X represents a group of the formula -CO-C(R 7 )=CH 8 -, is prepared by condensation of a corresponding acetophenone derivative with a terephthalaldehyde acid ester or its derivative in the presence of a base, .(b) a compound represented by the formula (I), wherein X represents a group of the formula is prepared by oxidation of a corresponding compound, wherein X represents a group of the formula with an agent for epoxidation, . (c) a compound represented by the formula (I), wherein X represents a group of the formula -N=N-, is prepared by condensation of a corresponding aniline derivative with a p-nitroso-benzoic acid ester in the presence or absence of an acidic catalyst, (d) a compound represented by the formula (I), wherein X represents a group of the formula -N(O)=N- or -N=N(O)-, is prepared by condensation of a corresponding phenyl- hydroxylamine with a p-nitroso-benzoic acid or its derivative, as described in item (c), (e) a compound represented by the formula (I), wherein X represents a group of the formula -N=N(O)- or -N(O)=N-, is prepared by condensation of a nitroso benzene derivative with p-hydroxylamino benzoic acid or its derivative, as described in item (c), (f) a compound represented by the formula (I), wherein X represents a group of the formula -N{R 7 )-CO-, is prepared by acylation of a corresponding aniline derivative with a functional derivative of terephthalic acid (acid halogemide or ester of the acid), and (g) a compound represented by the formula (I), wherein X represents a group of the formula -CO-N(R 7 )-, is prepared by acylation of a p-amino benzoic acid or its derivative with a functional derivative of a corresponding benzoic acid (acid halogenide or ester thereof) in the usual manner and, if necessary or desirable, the obtained compound is hydrolized.
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