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Claims for Patent: 5,387,603

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Claims for Patent: 5,387,603

Title: 1,5,7-trisubstituted indoline compounds and salts thereof
Abstract:Indoline compounds represented by the formula: ##STR1## wherein R represents a saturated or unsaturated aliphatic acyl group which may have one or more halogen atoms, a hydroxy group, a lower alkoxy group, a carboxy group, a lower alkoxycarbonyl group, a cycloalkyl group or an aryl group as substituents; a hydroxyalkyl group; an aliphatic acyloxyalkyl group; a lower alkyl group having a lower alkoxy group, a carboxy group, a lower alkoxycarbonyl group, an aryl substituted lower alkoxycarbonyl group, a carbamoyl group, a mono- or dialkyl substituted carbamoyl group or a cyano group as substituents; an aromatic acyl group which may have one or more halogen atoms as substituents; a furoyl group or a pyridylcarbonyl group; R.sup.1 represents a lower alkyl group which may have one or more halogen atoms or an aryl group as substituents; and pharmaceutically acceptable salts thereof, exhibit a selective suppressive action on urethral contractions, and thus are useful as therapeutic agents for the treatment of dysuria with less hypotension including postural hypotension.
Inventor(s): Kitazawa; Makio (Nagano, JP), Ban; Masaaki (Nagano, JP), Okazaki; Kosuke (Nagano, JP), Ozawa; Motoyasu (Nagano, JP), Yazaki; Toshikazu (Nagano, JP), Yamagishi; Ryoichi (Nagano, JP)
Assignee: Kissei Pharmaceutical Co., Ltd. (Nagano, JP)
Application Number:08/159,624
Patent Claims: 1. A compound represented by the formula: ##STR28## wherein R represents a saturated or unsaturated aliphatic acyl group which may be optionally substituted by a halogen atom, a hydroxy group, a lower alkoxy group, a carboxy group, a lower alkoxycarbonyl group, a cycloalkyl group or an aryl group; a hydroxyalkyl group; an aliphatic acyloxyalkyl group; a lower alkyl group which may be optionally substituted by a lower alkoxy group, a carboxy group, a lower alkoxycarbonyl group, an aryl substituted lower alkoxycarbonyl group, a carbamoyl group, a mono- or dialkyl substituted carbamoyl group or a cyano group; an aromatic acyl group which may be optionally substituted by a halogen atom; a furoyl group or a pyridylcarbonyl group; R.sup.1 represents a lower alkyl group which may be optionally substituted by a halogen atom or an aryl group; the carbon atom marked with * represents a carbon atom in (R) configuration, (S) configuration or a mixture thereof; or a salt thereof.

2. A compound as claimed in claim 1, represented by the formula: ##STR29## wherein R represents a saturated or unsaturated aliphatic acyl group which may be optionally substituted with a halogen atom, a hydroxy group, a lower alkoxy group, a carboxy group, a lower alkoxycarbonyl group, a cycloalkyl group or an aryl group; a hydroxalkyl group; an aliphatic acyloxyalkyl group; a lower alkyl group which may be optionally substituted by a lower alkoxy group, a carboxy group, a lower alkoxycarbonyl group, an aryl substituted lower alkoxycarbonyl group, a carbamoyl group, a mono- or dialkyl substituted carbamoyl group or a cyano group; an aromatic acyl group which may be optionally substituted by a halogen atom; a furoyl group or a pyridylcarbonyl group; R.sup.10 represents a lower alkyl group which may be optionally substituted by a halogen atom; the carbon atom marked with * represents a carbon atom in (R) configuration, (S) configuration or a mixture thereof; or a salt thereof.

3. A compound as claimed in claim 2, represented by the formula: ##STR30## wherein R.sup.11 represents a saturated or unsaturated aliphatic acyl group which may be optionally substituted by a carboxy group; a hydroxyalkyl group; an aliphatic acyloxyalkyl group or a lower alkyl group which may be optionally substituted by a lower alkoxy group, a carboxy group or a lower alkoxycarbonyl group; R.sup.10 represents a lower alkyl group which may be optionally substituted by a halogen atom; the carbon atom marked with * represents a carbon atom in (R) configuration, (S) configuration or a mixture thereof; or a salt thereof.

4. A compound as claimed in claim 3, represented by the formula: ##STR31## wherein R.sup.12 represents a butyryl group, a 3-hydroxypropyl group, a 3-ethyoxycarbonylpropyl group or a 3-methoxypropyl group; R.sup.10 represents a lower alkyl group which may be optionally substituted by a halogen atom; the carbon atom marked with * represents a carbon atom in (R) configuration, (S) configuration or a mixture thereof; or a salt thereof.

5. A compound as claimed in claim 4, represented by the formula: ##STR32## wherein R.sup.12 represents a butyryl group, a 3-hydroxypropyl group, a 3-ethyoxycarbonylpropyl group or a 3-methoxypropyl group; R.sup.13 represents a 2,2,2-trifluoroethyl group or an isopropyl group; the carbon atom marked with * represents a carbon atom in (R) configuration, (S) configuration or a mixture thereof; or a salt thereof.

6. The compound as claimed in claim 5, represented by the formula: ##STR33## wherein the carbon atom marked with * represents a carbon atom in (R) configuration, (S) configuration or a mixture thereof; or a salt thereof.

7. The compound as claimed in claim 5, represented by the formula: ##STR34## wherein the carbon atom marked with * represents a carbon atom in (R) configuration, (S) configuration or a mixture thereof; or a salt thereof.

8. The compound as claimed in claim 5, represented by the formula: ##STR35## wherein the carbon atom marked with * represents a carbon atom in (R) configuration, (S) configuration or a mixture thereof; or a salt thereof.

9. The compound as claimed in claim 5, represented by the formula: ##STR36## wherein the carbon atom marked with * represents a carbon atom in (R) configuration, (S) configuration or a mixture thereof; or a salt thereof.

10. The compound as claimed in claim 5, represented by the formula: ##STR37## wherein the carbon atom marked with * represents a carbon atom in (R) configuration, (S) configuration or a mixture thereof; or a salt thereof.

11. The compound as claimed in claim 5, represented by the formula: ##STR38## wherein the carbon atom marked with (R) represents a carbon atom in (R) configuration; or a salt thereof.

12. A pharmaceutical composition for the treatment of dysuria containing, as an active ingredient, a compound represented by the formula: ##STR39## wherein R represents a saturated or unsaturated aliphatic acyl group which may be optionally substituted by a halogen atom, a hydroxy group, a lower alkoxy group, a carboxy group, a lower alkoxycarbonyl group, a cycloalkyl group or an aryl group; a hydroxyalkyl group; an aliphatic acyloxyalkyl group; a lower alkyl group which may be optionally substituted by a lower alkoxy group, a carboxy group, a lower alkoxycarbonyl group, an aryl substituted lower alkoxycarbonyl group, a carbamoyl group, a mono- or dialkyl substituted carbamoyl group or a cyano group; an aromatic acyl group which may be optionally substituted by a halogen atom; a furoyl group or a pyridylcarbonyl group; R.sup.1 represents a lower alkyl group which may be optionally substituted by a halogen atom or an aryl group; the carbon atom marked with * represents a carbon atom in (R) configuration, (S) configuration or a mixture thereof; or a salt thereof.

13. A pharmaceutical composition as claimed in claim 12, wherein said active ingredient is represented by the formula: ##STR40## wherein the carbon atom marked with (R) represents a carbon atom in (R) configuration; or a salt thereof.

14. A method for the treatment of dysuria which comprises administering to a mammal or a human afflicted with dysuria a therapeutically effective amount of a compound of claim 1.

15. The method as claimed in claim 14, wherein said compound is represented by the formula: ##STR41## wherein the carbon atom marked with (R) represents a carbon atom in (R) configuration; or a salt thereof.
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