Compositions and method comprising heterocyclic compounds containing two heteroatoms as membrane penetration enhancers
Patent 5030629 Issued on July 9, 1991. Estimated Expiration Date: 
August 11, 2009. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.
August 11, 2009. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.Patent ReferencesCompositions and method comprising heterocyclic compounds containing two heteroatoms Oxazolidinone penetration enhancing compounds Patent #: 4960771 InventorApplicationNo. 393584 filed on 08/11/1989US Classes:514/211.07, Nitrogen attached directly or indirectly to the ring nitrogen of the seven-membered hetero ring by acyclic nonionic bonding (e.g., Diltiazem, etc.)514/228.8, Hetero ring is six-membered and includes at least nitrogen and oxygen as ring hetero atoms (e.g., monocyclic 1,2- and 1,3-oxazines, etc.)514/256, 1,3-diazines (e.g., pyrimidines, etc.)514/275, Nitrogen bonded directly to the 1,3-diazine at 2-position by a single bond514/356, C=O in a C(=O)O group (e.g., nicotinic acid, etc.)514/374, 1,3-oxazoles (including hydrogenated)514/376, Chalcogen bonded directly to ring carbon of the oxazole ring514/377, Nitrogen bonded directly to ring carbon of the oxazole ring514/385, 1,3-diazoles514/392, Divalent chalcogen or acyclic nitrogen double bonded at 2-position, or tautomeric equivalent514/423, C=X bonded directly to the five-membered hetero ring by nonionic bonding (X is chalcogen)514/470, Chalcogen or nitrogen bonded directly to the hetero ring514/652, Alkanol group only between the amino nitrogen and an ether oxygen which is bonded directly to the aryl ring or aryl ring system (i.e., aryloxy alkanol amines)514/772, DESIGNATED ORGANIC NONACTIVE INGREDIENT CONTAINING OTHER THAN HYDROCARBON514/788, Nitrogen containing514/946, PENETRANT OR ABSORBENT (ENHANCES PENETRATION INTO SUBJECT TREATED)514/947Topical applicationExaminersPrimary: Shah, Mukund J.Assistant: Datlow, Philip I. International ClassesA61K 031/415A61K 031/42 A61K 031/495 A61K 031/535 AbstractA method and compositions for enhancing absorption of topically administered physiologically active agents through the skin and mucous membranes of humans and animals in a transdermal device or formulation for local or systemic use, comprising a therapeutically effective amount of a pharmaceutically active agent and a non-toxic, effective amount of penetration enhancing agent of the formula I: ##STR1## wherein R is a saturated or unsaturated, straight or branched, cyclic or acyclic hydrocarbon group with from 1 to 19 carbon atoms, alkoxyalkyl, haloalkyl, specifically trifluoromethyl, alkoxy, amino, alkylamino and acylamino; R' and R" are hydrogen, alkyl, trifluoromethyl, alkoxyalkyl, aminoalkyl, alkyl- and acylaminoalkyl, carboxy, carbalkoxy, hydroxyalkyl or lower alkyl ester thereof; X is O or NR1 wherein R1 is hydrogen, alkyl, alkenyl, alkoxyalkyl, carbalkoxyalkyl, aminoalkyl, alkyl- and acylaminoalkyl, hydroxyalkyl or hydroxyalkyloxyalkyl and lower alkyl ester thereof; and n is 2 or 3 are disclosed.Field of SearchDESIGNATED ORGANIC NONACTIVE INGREDIENT CONTAINING OTHER THAN HYDROCARBONNitrogen containing PENETRANT OR ABSORBENT (ENHANCES PENETRATION INTO SUBJECT TREATED) Topical application Hetero ring is six-membered and includes at least nitrogen and oxygen as ring hetero atoms (e.g., monocyclic 1,2- and 1,3-oxazines, etc.) 1,3-diazines (e.g., pyrimidines, etc.) Chalcogen bonded directly to pyrimidine at 2-position Nitrogen bonded directly to the 1,3-diazine at 2-position by a single bond C=O in a C(=O)O group (e.g., nicotinic acid, etc.) Divalent chalcogen or acyclic nitrogen double bonded at 2-position, or tautomeric equivalent C=X bonded directly to the five-membered hetero ring by nonionic bonding (X is chalcogen) Chalcogen or nitrogen bonded directly to the hetero ring Alkanol group only between the amino nitrogen and an ether oxygen which is bonded directly to the aryl ring or aryl ring system (i.e., aryloxy alkanol amines) 1,3-diazoles 1,3-oxazoles (including hydrogenated) Chalcogen bonded directly to ring carbon of the oxazole ring Nitrogen bonded directly to ring carbon of the oxazole ring | |
