Patent US2608647A successfully refreshed from Google Patents.
Patent US5710178A successfully refreshed from Google Patents.
US5710178A
Expired / Lapsed
US
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Compositions and methods for therapy and prevention of pathologies including cancer, AIDS, and anemia
Assignee: United States Department of Health and Human Services
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Filing: 1995-06-06
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Granted: 1998-01-20
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Expires: 2015-06-06
Abstract
Abstract Compositions and methods of treating anemia, cancer, AIDS, or severe beta -chain hemoglobinopathies by administering a therapeutically effective amount of phenylacetate or pharmaceutically acceptable derivatives thereof or derivatives thereof alone or in combination or in conjunction with other therapeutic agents. Pharmacologically-acceptable salts alone or in combinations and methods of preventing AIDS and malignant conditions, and inducing cell differentiation are also aspects of this invention.
Inventors
- 👤 Dvorit Samid
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-31 20:43
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/70; A61K31/7042; A61K31/7052; A61K31/706; A61K31/7064; A61K31/7076; A61K31/185; A61K31/19; A61K31/192; A61K31/20; A61K31/33; A61K31/335; A61K31/35; A61K31/365; A61K31/7068; A61K31/7072; A61K45/00; A61K45/06; A61P; A61P35/00
Claims Analysis
Total Claims: 67
Claim 1
Independent Claim
206 words
A pharmaceutical composition for treating or preventing a neoplastic condition, inducing the differentiation of a cell, inducing the production of fetal hemoglobin, treating a pathology associated with abnormal hemoglobin activity, treating a viral infection, preventing a viral infection, inhibiting the production of IL-6 in a cell, inducing the production of TGFα, inhibiting the production of TGF-β2, treating an AIDS-associated dysfunction of the central nervous system, enhancing immunosurveillance, monitoring the bioavailability of the composition, promoting the healing of a wound, or treating a neoplastic condition in a subject resistant to radiation and chemotherapy, comprising a pharmaceutically-acceptable carrier and a pharmaceutically-effective amount of a compound of the formula: ##STR3## wherein n is an integer of from 1 to 2; R 0 is aryl or phenoxy, the aryl and phenoxy being unsubstituted or substituted with, independently, one or more halogen, hydroxy or lower alkyl; R 1 and R 2 are independently H, lower alkoxy, hydroxy, lower alkyl or halogen; and R 3 and R 4 are independently H, lower alkyl, lower alkoxy or halogen; except that if n is 2 and R 1 , R 2 , R 3 , and R 4 are H, R 0 cannot be unsubstituted phenyl; a pharmaceutically-acceptable salt thereof; or a mixture thereof.
Claim 2
Dependent Claim
206 words
A pharmaceutical composition for treating or preventing a neoplastic condition, inducing the differentiation of a cell, inducing the production of fetal hemoglobin, treating a pathology associated with abnormal hemoglobin activity, treating a viral infection, preventing a viral infection, inhibiting the production of IL-6 in a cell, inducing the production of TGFα, inhibiting the production of TGF-β2, treating an AIDS-associated dysfunction of the central nervous system, enhancing immunosurveillance, monitoring the bioavailability of the composition, promoting the healing of a wound, or treating a neoplastic condition in a subject resistant to radiation and chemotherapy, comprising a pharmaceutically-acceptable carrier and a pharmaceutically-effective amount of a compound of the formula: ##STR3## wherein n is an integer of from 1 to 2; R 0 is aryl or phenoxy, the aryl and phenoxy being unsubstituted or substituted with, independently, one or more halogen, hydroxy or lower alkyl; R 1 and R 2 are independently H, lower alkoxy, hydroxy, lower alkyl or halogen; and R 3 and R 4 are independently H, lower alkyl, lower alkoxy or halogen; except that if n is 2 and R 1 , R 2 , R 3 , and R 4 are H, R 0 cannot be unsubstituted phenyl; a pharmaceutically-acceptable salt thereof; or a mixture thereof.
Claim 3
Dependent Claim
34 words
The composition of claim 1, wherein R 0 is phenyl, naphthyl, or phenoxy, the phenyl, naphthyl and phenoxy being unsubstituted or substituted with, independently, one or more moieties of halogen, hydroxy or lower alkyl.
Claim 4
Dependent Claim
108 words
The composition of claim 1, wherein R 0 is phenyl, naphthyl, or phenoxy, the phenyl, naphthyl and phenoxy being unsubstituted or substituted with, independently, from 1 to 4 moieties of halogen, hydroxy or lower alkyl of from 1 to 4 carbon atoms; R 1 and R 2 are, independently, H, hydroxy, lower alkoxy of from 1 to 2 carbon atoms, lower straight or branched chain alkyl of from 1 to 4 carbon atoms or halogen; and R 3 and R 4 are, independently, H, lower alkoxy of from 1 to 2 carbon atoms, lower straight or branched chain alkyl of from 1 to 4 carbon atoms or halogen.
Claim 5
Dependent Claim
9 words
The composition of claim 1, wherein n is 1.
Claim 6
Dependent Claim
11 words
The composition of claim 4, wherein the compound is phenoxypropionic acid.
Claim 7
Dependent Claim
9 words
The composition of claim 1, wherein n is 2.
Claim 8
Dependent Claim
10 words
The composition of claim 6, wherein R 0 is phenyl.
Claim 9
Dependent Claim
11 words
The composition of claim 6, wherein R 0 is substituted phenyl.
Claim 10
Dependent Claim
21 words
The composition of claim 6, wherein the substitution on the phenyl at R 0 is from 1 to 4 halogen moieties.
Claim 11
Dependent Claim
20 words
The composition of claim 9, wherein the compound is 4-chlorophenylbutyric acid, 4-iodophenylbutyric acid, 4-fluorophenylbutyric acid, 3-chlorophenylbutyric acid, or 2-chlorophenylbutyric acid.
Claim 12
Dependent Claim
19 words
The composition of claim 1, wherein the pharmaceutically-acceptable salt is an alkali metal salt or alkaline earth metal salt.
Claim 13
Dependent Claim
14 words
The composition of claim 1, wherein the pharmaceutically-acceptable salt is an alkali metal salt.
Claim 14
Dependent Claim
13 words
The composition of claim 1, wherein the pharmaceutically-acceptable salt is the sodium salt.
Claim 15
Dependent Claim
15 words
The composition of claim 1, wherein all of the halogens are, independently, Cl or F.
Claim 16
Dependent Claim
14 words
The composition of claim 1, wherein R 3 and R 4 are both H.
Claim 17
Dependent Claim
193 words
A pharmaceutical composition for treating or preventing a neoplastic condition, inducing the differentiation of a cell, inducing the production of fetal hemoglobin, treating a pathology associated with abnormal hemoglobin activity, treating a viral infection, preventing a viral infection, inhibiting the production of IL-6 in a cell, inducing the production of TGF-α, inhibiting the production of TGF-β2, treating an AIDS-associated dysfunction of the central nervous system, enhancing immunosurveillance, monitoring the bioavailability of the composition, promoting the healing of a wound, or treating a neoplastic condition in a subject resistant to radiation and chemotherapy, consisting essentially of a pharmaceutically-acceptable carrier and a pharmacologically-effective amount of a compound of the formula: ##STR4## wherein n is 0; R 0 is phenyl, the phenyl being unsubstituted or substituted with, independently, one or more halogen, hydroxy, or lower alkyl; R 1 and R 2 are independently H, lower alkoxy, hydroxy, halogen, or lower alkyl; R 3 and R 4 are, independently, H, lower alkyl, lower alkoxy or halogen; except that if R 1 , R 2 , R 3 and R 4 are H, then R 0 cannot be unsubstituted phenyl; a pharmaceutically-acceptable salt thereof; or a mixture thereof.
Claim 18
Dependent Claim
193 words
A pharmaceutical composition for treating or preventing a neoplastic condition, inducing the differentiation of a cell, inducing the production of fetal hemoglobin, treating a pathology associated with abnormal hemoglobin activity, treating a viral infection, preventing a viral infection, inhibiting the production of IL-6 in a cell, inducing the production of TGF-α, inhibiting the production of TGF-β2, treating an AIDS-associated dysfunction of the central nervous system, enhancing immunosurveillance, monitoring the bioavailability of the composition, promoting the healing of a wound, or treating a neoplastic condition in a subject resistant to radiation and chemotherapy, consisting essentially of a pharmaceutically-acceptable carrier and a pharmacologically-effective amount of a compound of the formula: ##STR4## wherein n is 0; R 0 is phenyl, the phenyl being unsubstituted or substituted with, independently, one or more halogen, hydroxy, or lower alkyl; R 1 and R 2 are independently H, lower alkoxy, hydroxy, halogen, or lower alkyl; R 3 and R 4 are, independently, H, lower alkyl, lower alkoxy or halogen; except that if R 1 , R 2 , R 3 and R 4 are H, then R 0 cannot be unsubstituted phenyl; a pharmaceutically-acceptable salt thereof; or a mixture thereof.
Claim 19
Dependent Claim
20 words
The composition of claim 16, wherein R 1 , R 2 , R 3 , and R 4 are H.
Claim 20
Dependent Claim
14 words
The composition of claim 17, wherein the pharmaceutically-acceptable salt is an alkali metal salt.
Claim 21
Dependent Claim
22 words
The composition of claim 16, wherein R 1 is lower straight or branched chain alkyl of from 1 to 4 carbon atoms.
Claim 22
Dependent Claim
14 words
The composition of claim 19, wherein the compound is α-methylphenylacetic acid or α-ethylphenylacetic acid.
Claim 23
Dependent Claim
20 words
The composition of claim 16, wherein R 1 is hydroxy or lower alkoxy of from 1 to 2 carbon atoms.
Claim 24
Dependent Claim
14 words
The composition of claim 16, wherein the compound is α-hydroxyphenylacetic acid or α-methoxyphenylacetic acid.
Claim 25
Dependent Claim
11 words
The composition of claim 16, wherein R 0 is substituted phenyl.
Claim 26
Dependent Claim
21 words
The composition of claim 16, wherein the substitution on the phenyl at R 0 is from 1 to 4 halogen moieties.
Claim 27
Dependent Claim
22 words
The composition of claim 16, wherein the compound is 4-chlorophenylacetic acid, 4-iodophenylacetic acid, 4-fluorophenylacetic acid, 3-chlorophenylacetic acid, 2-chlorophenylacetic acid or 2,6-dichlorophenylacetic acid.
Claim 28
Dependent Claim
29 words
The composition of claim 23, wherein the substitution on the phenyl at R 0 is a lower straight or branched chain alkyl of from 1 to 4 carbon atoms.
Claim 29
Dependent Claim
16 words
The composition of claim 26, wherein the compound is 2-methylphenylacetic acid, 3-methylphenylacetic acid, or 4-methylphenylacetic acid.
Claim 30
Dependent Claim
13 words
The composition of claim 16, wherein the pharmaceutically-acceptable salt is the sodium salt.
Claim 31
Dependent Claim
19 words
The composition of claim 16, wherein R 0 is phenyl, unsubstituted or substituted with from 1 to 4 halogens.
Claim 32
Dependent Claim
16 words
The composition of claim 29, wherein for R 0 the halogens are, independently, F or Cl.
Claim 33
Dependent Claim
87 words
A pharmaceutical composition, comprising a pharmaceutically-acceptable carrier and a pharmaceutically-effective amount of a compound of the formula: ##STR5## wherein n is an integer of from 0 to 2; R 0 is naphthyl or phenoxy, the phenoxy being unsubstituted or substituted with, independently, one or more halogen, hydroxy or lower alkyl; R 1 and R 2 are independently H, lower alkoxy, hydroxy, or lower alkyl; and R 3 and R 4 are independently H, lower alkyl, lower alkoxy or halogen; a pharmaceutically-acceptable salt thereof, or a mixture thereof.
Claim 34
Dependent Claim
87 words
A pharmaceutical composition, comprising a pharmaceutically-acceptable carrier and a pharmaceutically-effective amount of a compound of the formula: ##STR5## wherein n is an integer of from 0 to 2; R 0 is naphthyl or phenoxy, the phenoxy being unsubstituted or substituted with, independently, one or more halogen, hydroxy or lower alkyl; R 1 and R 2 are independently H, lower alkoxy, hydroxy, or lower alkyl; and R 3 and R 4 are independently H, lower alkyl, lower alkoxy or halogen; a pharmaceutically-acceptable salt thereof, or a mixture thereof.
Claim 35
Dependent Claim
10 words
The composition of claim 31, wherein R 0 is naphthyl.
Claim 36
Dependent Claim
11 words
The composition of claim 32, wherein the compound is 1-naphthylacetic acid.
Claim 37
Dependent Claim
11 words
The composition of claim 31, wherein R 0 is substituted phenoxy.
Claim 38
Dependent Claim
36 words
A pharmaceutical dosage form for oral administration to a subject, comprising a pharmaceutically-effective amount of the compound of the formula of claim 1, wherein the pharmaceutically-effective amount is from 50 to 1,000 mg/kg. of the subject.
Claim 39
Dependent Claim
36 words
A pharmaceutical dosage form for oral administration to a subject, comprising a pharmaceutically-effective amount of the compound of the formula of claim 1, wherein the pharmaceutically-effective amount is from 300 to 500 mg/kg. of the subject.
Claim 40
Dependent Claim
36 words
A pharmaceutical dosage form for oral administration to a subject, comprising a pharmaceutically-effective amount of the compound of the formula of claim 1, wherein the pharmaceutically-effective amount is from 150 to 250 mg/kg. of the subject.
Claim 41
Dependent Claim
42 words
An aqueous solution for parenteral administration to a subject, comprising a pharmaceutically-effective amount of the compound of the formula of claim 1, wherein the carrier is an aqueous carrier and the pharmaceutically-effective amount is from 50 to 1,000 mg/kg. of the subject.
Claim 42
Dependent Claim
39 words
An aqueous solution for parenteral administration to a subject, comprising a pharmaceutically-effective amount of the compound of claim 1, wherein the carrier is an aqueous carrier and the pharmaceutically-effective amount is from 300 to 500 mg/kg. of the subject.
Claim 43
Dependent Claim
39 words
An aqueous solution for parenteral administration to a subject, comprising a pharmaceutically-effective amount of the composition compound claim 1, wherein the carrier is an aqueous carrier and the pharmaceutically-effective amount is from 150 to 250 mg/kg. of the subject.
Claim 44
Dependent Claim
23 words
A composition for topical administration, comprising from about 0.1 mM to about 10 mM of the compound of the formula of claim 1.
Claim 45
Dependent Claim
36 words
A pharmaceutical dosage form for oral administration to a subject, comprising a pharmaceutically-effective amount of the compound of the formula of claim 16, wherein the pharmaceutically-effective amount is from 50 to 1,000 mg/kg. of the subject.
Claim 46
Dependent Claim
36 words
A pharmaceutical dosage form for oral administration to a subject, comprising a pharmaceutically-effective amount of the compound of the formula of claim 16, wherein the pharmaceutically-effective amount is from 300 to 500 mg/kg. of the subject.
Claim 47
Dependent Claim
36 words
A pharmaceutical dosage form for oral administration to a subject, comprising a pharmaceutically-effective amount of the compound of the formula of claim 16, wherein the pharmaceutically-effective amount is from 150 to 250 mg/kg. of the subject.
Claim 48
Dependent Claim
42 words
An aqueous solution for parenteral administration to a subject, comprising a pharmaceutically-effective amount of the compound of the formula of claim 16, wherein the carrier is an aqueous carrier and the pharmaceutically-effective amount is from 50 to 1,000 mg/kg. of the subject.
Claim 49
Dependent Claim
39 words
An aqueous solution for parenteral administration to a subject, comprising a pharmaceutically-effective amount of the compound of claim 16, wherein the carrier is an aqueous carrier and the pharmaceutically-effective amount is from 300 to 500 mg/kg. of the subject.
Claim 50
Dependent Claim
39 words
An aqueous solution for parenteral administration to a subject, comprising a pharmaceutically-effective amount of the composition compound claim 16, wherein the carrier is an aqueous carrier and the pharmaceutically-effective amount is from 150 to 250 mg/kg. of the subject.
Claim 51
Dependent Claim
23 words
A composition for topical administration, comprising from about 0.1 mM to about 10 mM of the compound of the formula of claim 16.
Claim 52
Dependent Claim
19 words
The composition of claim 16, wherein the pharmaceutically-acceptable salt is an alkali metal salt or alkaline earth metal salt.
Claim 53
Dependent Claim
192 words
A pharmaceutical composition for treating or preventing a neoplastic condition, inducing the differentiation of a cell, inducing the production of fetal hemoglobin, treating a pathology associated with abnormal hemoglobin activity, treating a vital infection, preventing a viral infection, inhibiting the production of lL-6 in a cell, inducing the production of TGF-α, inhibiting the production of TGF-β2, treating an AIDS-associated dysfunction of the central nervous system, enhancing immunosurveillance, monitoring the bioavailability of the composition, promoting the healing of a wound, or treating a neoplastic condition in a subject resistant to radiation and chemotherapy, comprising a pharmaceutically-acceptable carrier and a pharmacologically-effective amount of a compound of the formula: ##STR6## wherein n is 0; R 0 is phenyl, the phenyl being unsubstituted or substituted with, independently, one or more halogen, hydroxy, or lower alkyl; R 1 and R 2 are independently H, lower alkoxy, hydroxy, halogen, or lower alkyl; R 3 and R 4 are, independently, H, lower alkyl, lower alkoxy or halogen; except that if R 1 , R 2 , R 3 , and R 4 are H, then R 0 cannot be unsubstituted phenyl; a pharmaceutically-acceptable salt thereof; or a mixture thereof.
Claim 54
Dependent Claim
192 words
A pharmaceutical composition for treating or preventing a neoplastic condition, inducing the differentiation of a cell, inducing the production of fetal hemoglobin, treating a pathology associated with abnormal hemoglobin activity, treating a vital infection, preventing a viral infection, inhibiting the production of lL-6 in a cell, inducing the production of TGF-α, inhibiting the production of TGF-β2, treating an AIDS-associated dysfunction of the central nervous system, enhancing immunosurveillance, monitoring the bioavailability of the composition, promoting the healing of a wound, or treating a neoplastic condition in a subject resistant to radiation and chemotherapy, comprising a pharmaceutically-acceptable carrier and a pharmacologically-effective amount of a compound of the formula: ##STR6## wherein n is 0; R 0 is phenyl, the phenyl being unsubstituted or substituted with, independently, one or more halogen, hydroxy, or lower alkyl; R 1 and R 2 are independently H, lower alkoxy, hydroxy, halogen, or lower alkyl; R 3 and R 4 are, independently, H, lower alkyl, lower alkoxy or halogen; except that if R 1 , R 2 , R 3 , and R 4 are H, then R 0 cannot be unsubstituted phenyl; a pharmaceutically-acceptable salt thereof; or a mixture thereof.
Claim 55
Dependent Claim
36 words
A pharmaceutical dosage form for oral administration to a subject, comprising a pharmaceutically-effective amount of the compound of the formula of claim 31, wherein the pharmaceutically-effective amount is from 50 to 1,000 mg/kg. of the subject.
Claim 56
Dependent Claim
36 words
A pharmaceutical dosage form for oral administration to a subject, comprising a pharmaceutically-effective amount of the compound of the formula of claim 31, wherein the pharmaceutically-effective amount is from 300 to 500 mg/kg. of the subject.
Claim 57
Dependent Claim
36 words
A pharmaceutical dosage form for oral administration to a subject, comprising a pharmaceutically-effective amount of the compound of the formula of claim 31, wherein the pharmaceutically-effective amount is from 150 to 250 mg/kg. of the subject.
Claim 58
Dependent Claim
42 words
An aqueous solution for parenteral administration to a subject, comprising a pharmaceutically-effective amount of the compound of the formula of claim 31, wherein the carrier is an aqueous carrier and the pharmaceutically-effective amount is from 50 to 1,000 mg/kg. of the subject.
Claim 59
Dependent Claim
39 words
An aqueous solution for parenteral administration to a subject, comprising a pharmaceutically-effective amount of the compound of claim 31, wherein the carrier is an aqueous carrier and the pharmaceutically-effective amount is from 300 to 500 mg/kg. of the subject.
Claim 60
Dependent Claim
39 words
An aqueous solution for parenteral administration to a subject, comprising a pharmaceutically-effective amount of the composition compound claim 31, wherein the carrier is an aqueous carrier and the pharmaceutically-effective amount is from 150 to 250 mg/kg. of the subject.
Claim 61
Dependent Claim
23 words
A composition for topical administration, comprising from about 0.1 mM to about 10 mM of the compound of the formula of claim 31.
Claim 62
Dependent Claim
19 words
The composition of claim 31, wherein the pharmaceutically-acceptable salt is an alkali metal salt or alkaline earth metal salt.
Claim 63
Dependent Claim
14 words
The composition of claim 31, wherein the pharmaceutically-acceptable salt is an alkali metal salt.
Claim 64
Dependent Claim
13 words
The composition of claim 31, wherein the pharmaceutically-acceptable salt is the sodium salt.
Claim 65
Dependent Claim
22 words
The composition of claim 31, wherein R 1 is lower straight or branched chain alkyl of from 1 to 4 carbon atoms.
Claim 66
Dependent Claim
20 words
The composition of claim 31, wherein R 1 is hydroxy or lower alkoxy of from 1 to 2 carbon atoms.
Claim 67
Dependent Claim
9 words
The composition of claim 31, wherein n is 0.
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