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US 6,187,806 B1Granted
N-linked sulfone of heterocyclic thioester hair growth compositions and uses
AssigneeGPI NIL Holdings, Inc.
InventorsJoseph P. Steiner, Gregory S. Hamilton
Life of this patent
Estimating the term…
Abstract
This invention relates to pharmaceutical compositions and methods for treating alopecia and promoting hair growth using N-linked sulfonamides of heterocyclic thioesters.
Claims15
A pharmaceutical composition which comprises:
- (i) an effective amount of an N-linked sulfone of a heterocyclic thioester compound for treating alopecia or promoting hair growth in an animal;
- (ii) a alopecia treating or hair growth promoting compound second hair revitalizing agent;
- and
- (iii) a pharmaceutically acceptable carrier.
1 more element
A pharmaceutical composition which comprises:
- (i) a compound of formula V
- or a pharmaceutically acceptable salt, ester, or solvate thereof, wherein:
- V is C, N, or S;
- A and B, taken together with the nitrogen and carbon atoms to which they are respectively attached, form a 5-7 membered saturated or unsaturated heterocyclic ring comprising one or more O, S, SO, SO2, N, or NR2 heteroatom(s);
- X is either O or S;
- Y is a direct bond, C1-C6 straight or branched chain alkyl, or C2-C6 straight or branched chain alkenyl,
- wherein any carbon atom of said alkyl or alkenyl is optionally substituted in one or more positions) with amino, halo, haloalkyl, thiocarbonyl, ester, thioester, alkoxy, alkenoxy, cyano, nitro, imino, alkylamino, aminoalkyl, sulfhydryl, thioalkyl, sulfonyl, or oxygen to form a carbonyl,
- or wherein any carbon atom of said alkyl or alkenyl is optionally replaced with O, NR2, S, SO, or SO2;
- R, is selected from the group consisting of hydrogen, C1-C4 straight or branched chain alkyl, C3-C4 straight or branched chain alkenyl or alkynyl, and C1-C4 bridging alkyl,
- wherein a bridge is formed between the nitrogen and a carbon atom of said alkyl or alkenyl chain comprising said heteroatom to form a ring,
- wherein said ring is optionally fused to an Ar group;
- Ar is an alicyclic or aromatic, mono-, bi- or tricyclic, carbo- or heterocyclic ring,
- wherein the ring is either unsubstituted or substituted with one or more substituent(s),
- wherein the individual ring size is 5-8 members,
- wherein the heterocyclic ring contains 1-6 heteroatom(s) independently selected from the group consisting of O, N, and S,
- wherein an aromatic or tertiary alkyl amine is optionally oxidized to a corresponding N-oxide;
- Z is a direct bond, C1-C6 straight or branched chain alkyl, or C2-C6 straight or branched chain alkenyl,
- wherein any carbon atom of said alkyl or alkenyl is optionally substituted in one or more position(s) with amino, halo, haloalkyl, thiocarbonyl, ester, thioester, alkoxy, alkenoxy, cyano, nitro, imino, alkylamino, aminoalkyl, sulfhydryl, thioalkyl, sulfonyl, or oxygen to form a carbonyl,
- or wherein any atom of said alkyl or alkenyl is optionally replaced with O, NR2, S, SO, or SO2;
- C and D are independently hydrogen, Ar, C1-C6 straight or branched chain alkyl, or C2-C6 straight or branched chain alkenyl,
- wherein said alkyl or alkenyl is optionally substituted with one or more substituent(s) independently selected from the group consisting of C3-C8 cycloalkyl, C5-C7 cycloalkenyl, oxygen to form a carbonyl, Ar, C1-C6 alkyl, C2-C6 alkenyl, hydroxy, amino, halo, haloalkyl, thiocarbonyl, ester, thioester, alkoxy, alkenoxy, cyano, nitro, imino, alkylamino, aminoalkyl, sulfhydryl, thioalkyl, and sulfonyl,
- wherein said cycloalkyl or cycloalkenyl is optionally substituted with C1-C6 alkyl, C2-C6 alkenyl, hydroxy, amino, halo, haloalkyl, thiocarbonyl, ester, thioester, alkoxy, alkenoxy, cyano, nitro, imino, alkylamino, aminoalkyl, sulfhydryl, thioalkyl, or sulfonyl, or
- wherein any carbon atom of said alkyl or alkenyl is optionally replaced with O, NR2, S, SO, or SO2;
- R1 is selected from the group consisting of Ar, C3-C8 cycloalkyl, C1-C6 straight or branched chain alkyl, and C2-C6 straight or branched chain alkenyl,
- wherein said alkyl or alkenyl is optionally substituted with one or more substituent(s) independently selected from the group consisting of Ar, C3-C8 cycloalkyl, amino, halo, haloalkyl, hydroxy, trifluoromethyl, C1-C6 straight or branched chain alkyl, C2-C6 straight or branched chain alkenyl, carbonyl, thiocarbonyl, ester, thioester, alkoxy, alkenoxy, cyano, nitro, imino, alkylamino, aminoalkyl, sulfhydryl, thioalkyl, and sulfonyl,
- wherein any carbon atom of said alkyl or alkenyl is optionally replaced with O, NR2, S, SO, or SO2, for treating alopecia or promoting hair growth in an animal;
- (ii) a second alopecia treating or hair growth promoting compound;
- and
- (iii) a pharmaceutically acceptable carrier.
26 more elements
Dependencies are inferred from the claim text.