 Spiro-isoquinoline-pyrrolidines and analogs thereof useful as aldose reductase inhibitors |
| We claim: 1. The compounds of structural formula (I) ##STR5## wherein R.sup.1 and R.sup.2 are ... |
|
| Novel alpha-glucosidase inhibitor, pradimicin Q |
| OF THE INVENTION One aspect of the present invention provides the compound pradimicin Q and its ... |
|
| .alpha.-glucosidase inhibitors |
| What is claimed is: 1. 1-deoxy nojirimycin derivatives of the formula ##STR5## and the ... |
|
| Oxetanones |
| OF THE INVENTION As used herein, the term "alkyl" denotes a straight or branched chain alkyl ... |
|
| Process for the preparation of .alpha.-glucosidase inhibitor, pradimicin Q |
| OF THE INVENTION One aspect of the present invention provides the compound pradimicin Q and its ... |
|
| Inhibitor of absorption of digestion product of food and drink |
| OF THE INVENTION The following examples are to explain this invention in detail, not to limit its ... |
|
| Hydantoin derivatives for treating complications of diabetes |
| OF PREFERRED EMBODIMENTS The invention will now be further explained with reference to M... |
|
| Oral composition |
| OF THE INVENTION Although the present invention is described below with reference to examples, the ... |
|
| Formulation for administration of steroid compounds |
| OF THE INVENTION By 5.beta. steroid is meant .alpha. ET, .beta. ET, and ED. In addition certain ... |
|
|
Phthalazin-4-ylacetic acid derivatives
| Details |
Inventors: Brittain, David R.; Wood, Robin;
Assignee: Imperial Chemical Industries Limited (London, GB2)
Primary Examiner: Rizzo; Nicholas S.
Assistant Examiner:
Attorney, Agent or Firm: Cushman, Darby & Cushman
This invention relates to enzyme inhibitory, novel phthalazin-4-ylacetic acid derivatives of the general formula I: ##STR1## and pharmaceutically acceptable salts as appropriate, to pharmaceutical compositions thereof, and to analogy processes for their manufacture. The compounds of formula I are inhibitors of the enzyme aldose reductase in vivo and as such may be useful in the reduction or prevention of the development of the peripheral effects such as macular oedema, cataract, retinopathy or impaired neural conduction. A preferred compound is 2-(2-fluoro-4-bromobenzyl)-1,2-dihydro-1-oxophthalazin-4-ylacetic acid. |
|
DETAILED DESCRIPTION What is claimed is: 1.
A phthalazin-4-ylacetic acid derivative of the formula: ##STR20## wherein R.
sup.
1 is a hydroxy or benzyloxy radical, or a C.
sub.
1-4 -alkoxy radical optionally bearing an N-morpholino or di-C.
sub.
1-4 -alkylamino radical; the substituents R.
sup.
2, R.
sup.
3, R.
sup.
4 and R.
sup.
5 on benzene ring A are selected from any one of the following combinations: (a) R.
sup.
2 is a fluoro or methoxy radical, R.
sup.
3 is hydrogen, R.
sup.
4 is a chloro, bromo or iodo radical, and R.
sup.
5 is hydrogen or a halogeno radical; (b) R.
sup.
2, R.
sup.
3 and R.
sup.
5 are hydrogen, and R.
sup.
4 is a bromo or iodo radical; (c) R.
sup.
2 is hydrogen or a fluoro radical, R.
sup.
3 and R.
sup.
5 are the same or different halogeno radicals, and R.
sup.
4 is hydrogen; (d) R.
sup.
2 is hydrogen or a fluoro radical, R.
sup.
3 and R.
sup.
4 are the same or different halogeno radicals, and R.
sup.
5 is hydrogen; and (e) R.
sup.
2 is hydrogen, R.
sup.
3 and R.
sup.
5 are independently fluoro or chlororadicals, and R.
sup.
4 is a chloro, bromo or iodo radical; and wherein, on benzene ring B, R.
sup.
6, R.
sup.
7 and R.
sup.
8 are independently selected from hydrogen, halogeno, C.
sub.
1-4 -alkyl and C.
sub.
1-4 -alkoxy radicals; or R.
sup.
6 and R.
sup.
7 together constitute a C.
sub.
1-4 -alkenedioxy diradical; provided that at least one of R.
sup.
6, R.
sup.
7 and R.
sup.
8 is hydrogen; and X is oxygen or sulphur; or a pharmaceutically acceptable base-addition salt of a compound of formula I wherein R.
sup.
1 is a hydroxy radical; or a pharmaceutically acceptable acid-addition salt of a compound of formula I wherein R.
sup.
1 is a C.
sub.
1-4 -alkoxy radical bearing an N-morpholino or di-C.
sub.
1-4 -alkylamino radical.
2.
A compound of formula I as claimed in claim 1 wherein R.
sup.
1 is a hydroxy, methoxy, ethoxy, benzyloxy, 2-(N-morpholino)ethoxy or 2-(N,N-dimethylamino)ethoxy radical; the combinations (a), (c) and (d) of R.
sup.
2, R.
sup.
3, R.
sup.
4 and R.
sup.
5 on benzene ring A have the values: (a) R.
sup.
2 is a fluoro or methoxy radical, R.
sup
|
| Related patents |
|
|
Food or dietetic substances having an alveolar structure and process of preparing same
What is claimed is: 1. A process for preparing a dietetic bakery product having an aveolar structure which consists essentially of the steps of (a) kneading a mixture ...
|
|
|
Method of inhibiting aldose reductase activity
What is claimed is: 1. A method for treating diabetic complications in mammals comprising administering an effective amount of spiro-(fluoren-9,4'-imidazolidine)-2',5'-...
|
|
|
Rhodanine derivatives, process for their preparation, and aldose reductase inhibitor containing the rhodanine derivatives as active ingredient
We claim: 1. An aldose reductase inhibitor containing, as an active ingredient, 3-carboxymethyl-5-(2-methylcinnamylidene)rhodanine or non-toxic salts of an acid thereof. ...
|
|
|
N-naphthoylglycine derivatives
OF THE INVENTION The compounds of this invention, represented by formula I, can exist in rotameric forms. More explictly, mesomerism imparts a partial double bond ...
|
|
|
Antidiabetic 3,4,5-trihydroxypiperidines
What is claimed is: 1. A compound of the formula ##STR264## in which R.sub.1 is C.sub.5 -C.sub.30 alkyl, C.sub.2 -C.sub.18 alkenyl, C.sub.2 -C.sub.18 alkinyl, C.sub.3 -C....
|
|
|
N-substituted pseudo-aminosugars, their production and use
What is claimed is: 1. A compound of the formula: ##STR35## wherein A is a chain hydrocarbon group having 1 to 10 carbon atoms which may be substituted by hydroxyl, ...
|
|
|
Thiolactam-n-acetic acid derivatives
We claim: 1. A compound of the formula: ##STR11## wherein, R.sup.1 and R.sup.2 are, the same or different, hydrogen, a halogen, a lower alkyl, a cycloalkyl having 3....
|
|
|
Rhodanine derivatives, process for their preparation, and aldose reductase inhibitor containing the rhodanine derivatives as active ingredient
I claim: 1. A rhodanine derivative represented by the general formula: ##STR13## wherein R.sup.11 represents a hydrogen atom; R.sup.22 represents: (1) a 5- to 10-...
|
|
|
Fuel supply systems
We claim: 1. A liquid fuel pump arrangement for delivering liquid fuel to an engine comprising a liquid-ring pump including a motor-driven bladed impeller rotor which is ...
|
|
|
Heterocyclic oxophthalazinyl acetic acids
OF THE INVENTION The numbering system of the compounds of formula I is as shown: ##STR5## The term "(C.sub.1 -C.sub.4)alkyl" whenever used in the definitions of R.sub.1 ...
|
|
|
Weight Loss and Supplements 
