 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 ... |
|
| Geldanamycin derivatives and antitumor drug |
| OF THE PREFERRED EMBODIMENTS The Geldanamycin derivatives having the formula (I) can be produced ... |
|
|
N-naphthoylglycine derivatives
| Details |
Inventors: Sestanj, Kazimir; Abraham, Nedumparambil A.; Bellini, Francesco; Treasurywala, Adi;
Assignee: Ayerst, McKenna & Harrison, Inc. (Montreal, CA)
Primary Examiner:
Assistant Examiner:
Attorney, Agent or Firm:
Herein disclosed are N-naphthoylglycine derivatives having aldose reductase inhibiting activity. The derivatives are useful for treating diabetic complications. |
|
DETAILED DESCRIPTION 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 character to the carbon-nitrogen bond of the thioamide group.
This partial double bond character leads to restricted rotation about the carbon nitrogen bond giving rise to cis and trans rotamers, the restricted rotation being augmented by the bulkiness of neighboring groups.
Interconversion of the rotamers is possible and is dependent on the physical environment.
As evidenced by its physical properties, the thermodynamically more stable rotamer exists exclusively in the crystalline state of the compound and is the predominant isomer present in equilabrated solutions.
Furthermore, the more stable rotamer is the more pharmacologically active.
The less stable rotamer can be separated from the more stable rotamer by high performance liquid chromatography or by thin layer chromatography.
The rotameric forms are included within the scope of this invention.
For brevity, the compounds of this invention, including their rotameric forms, are referred to herein as compounds of formula I.
The term "lower alkyl" as used herein means a straight chain alkyl radical containing from one to four carbon atoms or a branched chain alkyl radical containing three or four carbon atoms and includes methyl, ethyl, propyl, 1-methylethyl, butyl, 2-methylpropyl and 1,1-dimethylethyl.
Preferred lower alkyl radicals contain from one to three carbon atoms.
The term "lower alkenyl" as used herein means a straight chain alkenyl radical containing from two to six carbon atoms, or a branched chain alkenyl radical containing from four to six carbon atoms and includes, for example, ethenyl, 2-propenyl, 2-methyl-2-propenyl and 2-ethyl-3-butenyl.
Preferred lower alkenyl radicals contain two to three carbon atoms.
The term "lower alkoxy" as used herein means a straight chain alkoxy radical containing from one to six carbon atoms, preferably one to three carbon atoms, or a branched chain alkoxy radical containing three or four carbon atoms, and includes methoxy, ethoxy, 1-methylethoxy, butoxy and hexanoxy
|
| Related patents |
|
|
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 ...
|
|
|
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 independently hydrogen, alkyl containining 1 to 6 carbon atoms, halogen, ...
|
|
|
Novel alpha-glucosidase inhibitor, pradimicin Q
OF THE INVENTION One aspect of the present invention provides the compound pradimicin Q and its pharmaceutically acceptable base salts. "Pharmaceutically acceptable ...
|
|
|
.alpha.-glucosidase inhibitors
What is claimed is: 1. 1-deoxy nojirimycin derivatives of the formula ##STR5## and the pharmaceutically acceptable acid addition salts thereof wherein n is zero, 1 or 2 ...
|
|
|
Oxetanones
OF THE INVENTION As used herein, the term "alkyl" denotes a straight or branched chain alkyl containing the number of carbon atoms designated. Examples of C.sub.1 -C....
|
|
|
Weight Loss and Supplements 
