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US4851407A Expired / Lapsed US ⏱️ 0.0 years remaining

Novel treatment

Assignee: Beecham Group PLC
•
Filing: 1988-09-16
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Granted: 1989-07-25
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Expires: 2008-09-16
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Abstract

Abstract A method of treatment of emesis, anxiety and/or IBS in mammals, including humans, which method comprises administering an effective amount of a compound of formula (I) or (II) or a pharmaceutically acceptable salt thereof: Ar--CO--Y--Z (I) wherein Ar is a group of formula (a): ##STR1## wherein: R 1 and R 2 are independently selected from hydrogen, halogen, C 1-6 alkyl, C 1-4 alkoxy, hydroxy, amino optionally substituted by one or two C 1-4 alkyl groups, thiol, C 1-4 alkylthio; X is CH 2 , NR 3 , --O-- or --S-- wherein R 3 is hydrogen, C 1-4 alkyl, C 3-5 alkenyl, phenyl or phenyl C 1-4 alkyl; or Ar is a group of formula (b): ##STR2## wherein R 4 to R 7 are independently hydrogen, halogen, C 1-6 alkyl, C 1-6 alkoxy, hydroxy, amino optionally substituted by one or two C 1-4 alkyl, by C 1-4 alkanoylamino or pyrrolyl, one of R 4 to R 7 being other than hydrogen; Y is --O-- or --NH--; and Z is a group of formula (c), (d) or (e): ##STR3## wherein n is 2, 3 or 4; R 8 is hydrogen, C 1-7 alkyl, C 3-5 alkenyl or phenyl C 1-4 alkyl optionally substituted by one or two halogen, C 1-4 alkoxy or C 1-4 alkyl; ##STR4## wherein: p is 1, 2 or 3; and R 9 is as defined above for R 8 ; and with the proviso that, when Ar is of formula (b) and Y is --NH--, Z is a group of formula (d) or (e); ##STR5## wherein R 10 is hydrogen, C 1-10 alkyl, C 3-7 cycloalkyl, C 3-6 alkenyl, phenyl or phenyl-C 1-3 alkyl; and one of the groups represented by R 11 , R 12 and R 13 is hydrogen, C 1-6 alkyl, C 3-7 cycloalkyl, C 2-6 alkenyl or phenyl-C 1-3 alkyl and each of the other groups, which may be the same or different, is hydrogen or C 1-6 alkyl.

Inventors

  • 👤 Gordon Wootton
  • 👤 Gareth J. Sanger

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-09 20:42
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/435; A61K31/40; A61K31/403; A61K31/404; A61K31/405; A61K31/41; A61K31/415; A61K31/46; A61P; A61P1/00; A61P1/08; A61P11/00; A61P25/00; A61P25/20; A61P35/00

Claims Analysis

Total Claims: 15
Claim 1
Independent Claim 116 words
A method for treatment of emesis in mammals comprising administering to a mammal in need of such treatment an effective amount of a compound of the following formula, or a pharmaceutically acceptable salt thereof: ##STR23## wherein R 5 1 is halo, C 1-6 alkyl or C 1-6 alkoxy, R 6 1 is hydrogen or C 1-6 alkoxy; R 7 1 is halo, C 1-6 alkyl or C 1-6 alkoxy and Z 1 is is a group of the formula: ##STR24## wherein n is 2, 3 or 4; R 8 is hydrogen, C 1-7 alkyl, C 3-5 alkenyl or phenyl C 1-4 alkyl optionally substituted by one or two halogen, C 1-4 alkoxy or C 1-4 alkyl.
Claim 2
Independent Claim 116 words
A method for treatment of emesis in mammals comprising administering to a mammal in need of such treatment an effective amount of a compound of the following formula, or a pharmaceutically acceptable salt thereof: ##STR23## wherein R 5 1 is halo, C 1-6 alkyl or C 1-6 alkoxy, R 6 1 is hydrogen or C 1-6 alkoxy; R 7 1 is halo, C 1-6 alkyl or C 1-6 alkoxy and Z 1 is is a group of the formula: ##STR24## wherein n is 2, 3 or 4; R 8 is hydrogen, C 1-7 alkyl, C 3-5 alkenyl or phenyl C 1-4 alkyl optionally substituted by one or two halogen, C 1-4 alkoxy or C 1-4 alkyl.
Claim 3
Dependent Claim 13 words
A method according to claim 1 wherein R 8 is methyl or ethyl.
Claim 4
Dependent Claim 17 words
A method according to claim 1, wherein the compound is 3,5-dichloro-[3α-(8-methyl-8-azabicyclo(3.2.1)octyl)]-benzoate, or a pharmaceutically acceptable salt thereof.
Claim 5
Dependent Claim 17 words
A method according to claim 1, wherein the compound is 3,5-dimethyl-[3α-(8-methyl-8-azabicyclo(3.2.1)octyl)]-benzoate, or a pharmaceutically acceptable salt thereof.
Claim 6
Independent Claim 120 words
A method of treatment of cytotoxic agent induced nausea and vomiting, which method comprises administering to a mammal in need of such treatment an effective amount of a compound of the following formula, or a pharmaceutically acceptable salt thereof: ##STR25## wherein R 5 1 is halo, C 1-6 alkyl or C 1-6 alkoxy, R 6 1 is hydrogen or C 1-6 alkoxy; R 7 1 is halo, C 1-6 alkyl or C 1-6 alkoxy and Z 1 is a group of the formula: ##STR26## wherein n is 2, 3 or 4; R 8 is hydrogen, C 1-7 alkyl, C 3-5 alkenyl or phenyl C 1-4 alkyl optionally substituted by one or two halogen, C 1-4 alkoxy or C 1-4 alkyl.
Claim 7
Independent Claim 120 words
A method of treatment of cytotoxic agent induced nausea and vomiting, which method comprises administering to a mammal in need of such treatment an effective amount of a compound of the following formula, or a pharmaceutically acceptable salt thereof: ##STR25## wherein R 5 1 is halo, C 1-6 alkyl or C 1-6 alkoxy, R 6 1 is hydrogen or C 1-6 alkoxy; R 7 1 is halo, C 1-6 alkyl or C 1-6 alkoxy and Z 1 is a group of the formula: ##STR26## wherein n is 2, 3 or 4; R 8 is hydrogen, C 1-7 alkyl, C 3-5 alkenyl or phenyl C 1-4 alkyl optionally substituted by one or two halogen, C 1-4 alkoxy or C 1-4 alkyl.
Claim 8
Dependent Claim 17 words
A method according to claim 5, wherein the compound is 3,5-dimethyl-[3α-(8-methyl-8-azabicyclo(3.2.1)octyl)]-benzoate, or a pharmaceutically acceptable salt thereof.
Claim 9
Dependent Claim 17 words
A method according to claim 5, wherein the compound is 3,5-dichloro-[3α-(8-methyl-8-azabicyclo(3.2.1)octyl)]-benzoate, or a pharmaceutically acceptable salt thereof.
Claim 10
Independent Claim 121 words
A method of treatment of radiation agent induced nausea and vomiting, which method comprises administering to a mammal in need of such treatment an effective amount of a compound of the following formula , or a pharmaceutically acceptable salt thereof: ##STR27## wherein R 5 1 is halo, C 1-6 alkyl or C 1-6 alkoxy, R 6 1 is hydrogen or C 1-6 alkoxy; R 7 1 is halo, C 1-6 alkyl or C 1-6 alkoxy and Z 1 is a group of the formula: ##STR28## wherein n is 2, 3 or 4; R 8 is hydrogen, C 1-7 alkyl, C 3-5 alkenyl or phenyl C 1-4 alkyl optionally substituted by one or two halogen, C 1-4 alkoxy or C 1-4 alkyl.
Claim 11
Independent Claim 121 words
A method of treatment of radiation agent induced nausea and vomiting, which method comprises administering to a mammal in need of such treatment an effective amount of a compound of the following formula , or a pharmaceutically acceptable salt thereof: ##STR27## wherein R 5 1 is halo, C 1-6 alkyl or C 1-6 alkoxy, R 6 1 is hydrogen or C 1-6 alkoxy; R 7 1 is halo, C 1-6 alkyl or C 1-6 alkoxy and Z 1 is a group of the formula: ##STR28## wherein n is 2, 3 or 4; R 8 is hydrogen, C 1-7 alkyl, C 3-5 alkenyl or phenyl C 1-4 alkyl optionally substituted by one or two halogen, C 1-4 alkoxy or C 1-4 alkyl.
Claim 12
Dependent Claim 17 words
A method according to claim 8, wherein the compound is 3,5-dimethyl-[3α-(8-methyl-8-azabicyclo(3.2.1)octyl)]-benzoate, or a pharmaceutically acceptable salt thereof.
Claim 13
Dependent Claim 17 words
A method according to claim 8, wherein the compound is 3,5-dichloro-[3α-(8-methyl-8-azabicyclo(3.2.1)octyl)]-benzoate, or a pharmaceutically acceptable salt thereof.
Claim 14
Dependent Claim 17 words
A method according to claim 6, wherein the cytotoxic agent is selected from cisplatin, doxorubicin and cyclophosphamide.
Claim 15
Dependent Claim 17 words
A method according to claim 7, wherein the cytotoxic agent is selected from cisplatin, doxorubicin and cyclophosphamide.

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1992-07-24 1993-01-23 1993-07-25 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1996-07-24 1997-01-23 1997-07-25 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 2000-07-24 2001-01-23 2001-07-25 $7700.00 Window Closed / Lapsed

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