EP0181833A1
Expired / Lapsed
EP
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Substituted propane-phosphonous acid compounds
Assignee: Novartis AG
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Filing: 1985-10-07
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Granted: —
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Expires: 2005-10-07
Abstract
Abstract The compounds of the formulain which one of the groups R', R<sup>2</sup> and R<sup>3</sup> represents hydrogen, C<sub>1-8</sub>-alkyl, C<sub>3-6</sub>-cycloalkyl, phenyl optionally substituted by halogeno, C<sub>1-4</sub>-alykl. C<sub>1-4</sub>-alkoxy and/or trifluoromethyl, or C<sub>7-10</sub>-phenylalkyl optionally substituted in the phenyl moiety by halogeno, C<sub>1-4</sub>-alkyl, C<sub>1-4</sub>-alkoxy and/or trifluormethyl, and the other two are hydrogen, or salts thereof.These compounds have valuable pharmaceutical properties.
Inventors
- 👤 John Grey Dr. Dingwall
- 👤 Josef Dr. Ehrenfreund
- 👤 Roger Graham Dr. Hall
- 👤 James Dr. Jack
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-02 03:37
CPC Classifications
C; C07; C07F; C07F9/00; C07F9/02; C07F9/28; C07F9/48; A; A61; A61P; A61P21/00; A61P25/00; A61P25/04; A61P25/24; A61P25/26; A61P25/28; C07F9/30; C07F9/32; C07F9/3205; C07F9/3211; C07F9/4808; C07F9/4816; Y; Y02; Y02P; Y02P20/00; Y02P20/50; Y02P20/55
Claims Analysis
Total Claims: 40
Claim 1
Independent Claim
81 words
Compounds of the formula I, in which one of the groups R 1 , R 2 and R 3 represents hydrogen, C l -a-alkyl, C 3 - 6 -cycloalkyl, phenyl optionally substituted by halogeno, C 1 - 4 -alkyl, C 1 - 4 -alkoxy and/or trifluoromethyl, or C 7 - 10 -phenylalkyl optionally substituted in the phenyl moiety by halogeno, C 1 - 4 -alkyl, C 1 - 4 -alkoxy and/or trifluoromethyl, and the other two are hydrogen, or salts thereof.
Claim 2
Dependent Claim
81 words
Compounds of the formula I, in which one of the groups R 1 , R 2 and R 3 represents hydrogen, C l -a-alkyl, C 3 - 6 -cycloalkyl, phenyl optionally substituted by halogeno, C 1 - 4 -alkyl, C 1 - 4 -alkoxy and/or trifluoromethyl, or C 7 - 10 -phenylalkyl optionally substituted in the phenyl moiety by halogeno, C 1 - 4 -alkyl, C 1 - 4 -alkoxy and/or trifluoromethyl, and the other two are hydrogen, or salts thereof.
Claim 3
Dependent Claim
47 words
A compound according to claim 1 and having the formula I, in which R 1 and R 3 are hydrogen, and R 2 is hydrogen or phenyl, optionally substituted by halogeno, C 1 - 4 -alkyl, C 1 - 4 -alkoxy and/or trifluoromethyl, or a salt thereof.
Claim 4
Dependent Claim
31 words
A compound according to claim 1 and having the formula I, in which R 1 and R 3 are hydrogen, and R 2 is hydrogen or halogenophenyl, or a salt thereof.
Claim 5
Dependent Claim
32 words
A compound according to claim 1 and having the formula I, in which R 1 and R 3 are hydrogen, and R 2 is hydrogen, 4-chloro-phenyl or 4-fluorophenyl, or a salt thereof.
Claim 6
Dependent Claim
16 words
A compound as claimed in claim 1 and being 3-aminopropylphos- phonous acid or a salt thereof.
Claim 7
Dependent Claim
16 words
A compound as claimed in claim 1 and being 3-amino-2-(4-chloro- phenyl)propylphosphonous acid or a salt therof.
Claim 8
Dependent Claim
28 words
The compounds of claims 1 to 4 and 6 having an asymmetric carbon atom in the form of a racemate or of the optical antipodes, and salts therof.
Claim 9
Dependent Claim
10 words
The acid addition salts of the compounds of formula I.
Claim 10
Dependent Claim
10 words
The acid addition salts of the compounds of formula I.
Claim 11
Dependent Claim
10 words
The pharmaceutically acceptable salts of the compounds of formula I.
Claim 12
Dependent Claim
10 words
The pharmaceutically acceptable salts of the compounds of formula I.
Claim 13
Dependent Claim
210 words
Process for the production of a compound of formula I which comprises, in a compound of formula II, in which R l , R 2 and R 3 are as defined in claim 1, Z is -NH 2 or a protected amino group Z o , Q is hydrogen or a protecting group Q and R c is hydrogen, C l - 4 -alkyl or an alkali metal or ammonium cation, replacing the group R c by hydrogen or by an alkali metal or ammonium cation, and replacing the group Q when it is Q 0 by hydrogen and converting the group Z when it is a protected amino group Z o into -NHz, or, in a compound having the formula VIII, wherein R 1 and R 2 are as defined in claim 1 and X is a group capable of conversion into a group of formula Id, in which R 3 is as defined in claim 1, converting the group X into a group of formula Id, and wherein, if desired, any resulting salt is converted into the free compound or into another salt and/or, if desired, any resulting free compound is converted into a salt and/or, if desired resulting mixture of isomers is separated into the single isomers.
Claim 14
Dependent Claim
8 words
The new compounds obtainable according to claim 10.
Claim 15
Dependent Claim
19 words
A process for producing a compound of formula I substantially as described with reference to any of the Examples.
Claim 16
Dependent Claim
19 words
A process for producing a compound of formula I substantially as described with reference to any of the Examples.
Claim 17
Dependent Claim
18 words
A compound of formula I when produced by a process described in any of claims 10 to 12.
Claim 18
Dependent Claim
14 words
Compounds of formula I substantially as described with reference to any of the Examples.
Claim 19
Dependent Claim
14 words
Compounds of formula I substantially as described with reference to any of the Examples.
Claim 20
Dependent Claim
24 words
A pharmaceutical preparation comprising a compound claimed in any one of claims 1 to 9, in admixture or conjunction with a pharmaceutically suitable carrier.
Claim 21
Dependent Claim
22 words
A compound named in any one of claims 1 to 9 for use in a therapeutic method of treating humans and animals.
Claim 22
Dependent Claim
15 words
A compound named in any one of claims 1 to 9 as muscle relaxant agent.
Claim 23
Dependent Claim
14 words
A compound named in any one of claims 1 to 9 as anticonvulsant agent.
Claim 24
Dependent Claim
14 words
A compound named in any one of claims 1 to 9 as analgesic agent.
Claim 25
Dependent Claim
19 words
The use of a compound of any one of claims 1 to 9 in producing of a pharmaceutical preparation.
Claim 26
Dependent Claim
27 words
Process for the manufacture of a pharmaceutical preparation, wherein a product as claimed in any of claims 1 to 9 is worked up with a pharmaceutical carrier.
Claim 27
Dependent Claim
25 words
The use of a compound of any one of claims 1 to 9 for the manufacture of a pharmaceutical preparation for application as muscle relaxant.
Claim 28
Dependent Claim
68 words
Compounds having the formula II, wherein R 1 , R 2 and R 3 are as defined in claim 1 and Q, Z and R c are as defined in claim 10, provided that, at least one of Q and R c is other than hydrogen and/or Z is other than NH 2 and that when R 2 and Q are each hydrogen, R c is not alkyl.
Claim 29
Dependent Claim
124 words
Process for the production of compounds of formula II comprising reacting in the presence of a basic catalyst or in the presence of agents forming free radicals, a compound of the formula III, in which R c and Q are as defined in claim 10, with a compound of formula IV, in which R 1 and R 2 are as defined in claim 1 and X is a group capable of being converted into a group of formula la, wherein R 3 is as defined in claim 1 and Z is as defined in claim 10, in order to produce a compound of formula V and then converting the group X into a group of formula la, to produce a compound of formula II.
Claim 30
Dependent Claim
44 words
Compounds of the formula, in which Q o is as defined in claim 10, R co is C 1 - 4 -alkyl and each R d is independently C 1 - 6 -alkyl, the groups, R co and R being the same or different.
Claim 31
Dependent Claim
17 words
Compounds of formula VI as claimed in claim 25 wherein R is C 1 - 2 -alkyl.
Claim 32
Dependent Claim
38 words
Compounds of formula VIA, in which R co and R d are as defined in claim 25 and R a , R b and R 4 are the same or different and are C 1 - 4 -alkyl.
Claim 33
Dependent Claim
3 words
Ethyl trimethylsilyl (diethoxymethyl)phosphonite.
Claim 34
Dependent Claim
3 words
Ethyl trimethylsilyl (diethoxymethyl)phosphonite.
Claim 35
Dependent Claim
45 words
Process for producing compounds of formula VI as defined in claim 25 comprising reacting, optionally in the presence of a basic catalyst, a compound of formula IIIa, in which Q o and R co are as defined in claim 25, with a suitable silylating agent.
Claim 36
Dependent Claim
12 words
Process according to claim 29 wherein the silylating agent is hexamethyl disilazane.
Claim 37
Dependent Claim
14 words
Compounds of formula VI substantially as described with reference to any of the Examples.
Claim 38
Dependent Claim
14 words
Compounds of formula VI substantially as described with reference to any of the Examples.
Claim 39
Dependent Claim
37 words
Compounds having the formula IX wherein R l , R 2 and R 3 are as defined in claim 1, Q o is as defined in claim 10 and R co is as defined in claim 25.
Claim 40
Dependent Claim
73 words
Process for the production of a compound of formula IX comprising reacting a compound having the formula X, in which R 1 , Q o and R co are as defined in claim 32, in form of the anion of formula XI, wherein M is an alkali or transition metal atom, with a compound of formula XII, wherein R 2 and R 3 are as defined in claim 1. FO 7.4 JL/eg *
References Cited (Backward Citations)
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