Claims Analysis
Total Claims: 10
Claim 1
Independent Claim
236 words
(1) A process for the preparation of a compound of formula (I): wherein R¹ is hydrogen, C 1-4 alkyl, acetyl or formyl; R² and R³ are the same or different and are hydrogen or C 1-4 alkyl; R⁴ is NR¹¹R¹²; R¹¹, R¹², R⁵ and R⁶ are the same or different and are hydrogen, C 1-4 alkyl or C 1-12 acyl; R⁷, R⁸, R⁹ and R¹⁰ are the same or different and are hydrogen, halo, C 1-4 haloalkyl, C 1-4 alkyl and C 1-4 alkoxy; and n is 2, 3, 4 or 5; m is o or an integer from 1 to 6; or a salt thereof, which comprises deacylating a compound of formula (II): wherein R¹ is hydrogen or C 1-4 alkyl; R², R³, R⁷, R⁸, R⁹ and R¹⁰ and n and m are as defined in herein; one of the groups R⁵, R⁶, R¹¹, R¹² being C 1-12 acyl, the other groups R⁵, R⁶, R¹¹, and R¹² being the same or different and are hydrogen or C 1-12 acyl, and optionally thereafter (i) in the case where, in the resulting compound of formula (I) R¹ is hydrogen, formylating the compound so as to prepare the corresponding compound of formula (I), wherein R¹ is formyl; and/or (ii) converting R², R³, R⁵, R⁶, R¹¹ and R¹² in the resulting compound of formula (I) into another R², R³, R⁵, R⁶, R¹¹ and R¹²; and optionally forming a salt.
Claim 2
Dependent Claim
22 words
(2) A process for the preparation of a compound of formula (I) according to Claim 1, wherein NR¹ is NH or NCHO.
Claim 3
Dependent Claim
23 words
(3) A process for the preparation of a compound of formula (I) according to Claim 1, wherein R⁴ and NR⁵R⁶ are both NH₂.
Claim 4
Dependent Claim
27 words
(4) A process for the preparation of a compound of formula (I) according to Claim 1, wherein R², R³, R⁷, R⁸, R⁹ and R¹⁰ are all hydrogen.
Claim 5
Dependent Claim
22 words
(5) A process for the preparation of a compound of formula (I) according to Claim 1, wherein n is 3 or 4.
Claim 6
Dependent Claim
20 words
(6) A process for the preparation of a compound of formula (I) according to Claim 1, wherein m is 0.
Claim 7
Dependent Claim
39 words
(7) A process according to Claim 1 for preparing a compound selected from the group comprising: N-[4-[3-(2,4-diamino-1,6-dihydro-6-oxo-5-pyrimidinyl)propylamino]-benzoyl]- L -glutamic acid, N-[4-[3-(2,4-diamino-1,6-dihydro-6-oxo-5-pyrimidinyl)-N-methyl-propylamino]benzoyl]- L -glutamic acid, N-[4-[3-(2,4-diamino-1,6-dihydro-6-oxo-5-pyrimidinyl)-N-formyl-propylamino]benzoyl]- L -glutamic acid, N-[4-[2-(2,4-diamino-1,6-dihydro-6-oxo-5-pyrimidinyl)ethylamino]-benzoyl]- L -glutamic acid, N-[4-[2-(2,4-diamino-1,6-dihydro-6-oxo-5-pyrimidinyl)ethyl-N-methylamino]benzoyl]- L -glutamic acid, or salts thereof,
Claim 8
Dependent Claim
24 words
(8) A pharmaceutical formulation, which comprises a compound according to Claim 1, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier therefor.
Claim 9
Dependent Claim
23 words
(9) A compound of formula (I) or a salt thereof, as defined in Claim 1, for use in the manufacture of a medicament.
Claim 10
Dependent Claim
39 words
(10) A novel chemical intermediate of formula (II), (III), (IV) or (V). wherein R¹, R², R³, R⁵, R⁶, R⁷, R⁸, R⁹, R¹⁰, R¹¹, R¹² and n are as defined in Claim 1, and R¹³ is a C 1-4 alkyl.