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Azacycloalkane derivatives, absorption promoters containing the derivatives as the effective ingredient and external preparations containing the absorption promoters

Assignee: Hisamitsu Pharmaceutical Co Inc
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Filing: 1987-11-18
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Granted: 1989-11-21
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Expires: 2007-11-18
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Abstract

Abstract An azacycloalkane derivative useful for promoting the absorption of a medicine, an absorption promoting agent comprising at least one of the azacycloalkane derivatives as the effective ingredient for promoting the absorption and an external preparation containing the absorption promoting agent, the derivative being represented by the following formula ##STR1## wherein A is --CH 2 -- or --S-- for example, B is sulfur or oxygen, R is --SR" in which R" is an alkyl group or alkylthioalkyl group for example, or --OR" in which R" is as defined above, an alkyl group or substituted amino group, R' is a hydrogen atom, alkyl group or alkyloxy group for example, m is an integer of 0-5 and n is an integer of 1-15.

Inventors

  • 👤 Akira Nakagawa
  • 👤 Michinori Sakai

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-27 22:44
CPC Classifications
C; C07; C07D; C07D207/00; C07D207/02; C07D207/18; C07D207/22; C07D207/24; C07D207/26; C07D207/263; C07D207/267; A; A61; A61P; A61P43/00; C07D207/27; C07D211/00; C07D211/04; C07D211/68; C07D211/72; C07D211/74; C07D211/76; C07D223/00; C07D223/02; C07D223/06; C07D223/08; C07D223/10; C07D263/00; C07D263/02; C07D263/08; C07D263/16; C07D263/18; C07D265/00; C07D265/28; C07D265/30; C07D265/32; C07D277/00; C07D277/02; C07D277/08; C07D277/12; C07D277/14; C07D279/00; C07D279/10; C07D279/12; C07D281/00; C07D281/02; C07D281/04; C07D281/06

Claims Analysis

Total Claims: 12
Claim 1
Independent Claim 92 words
An absorption promoting agent for application to live body membranes, comprising at least one member as the effective ingredient for promoting absorption, selected from azacycloalkane derivatives represented by the following general formula (I) ##STR53## wherein R is --SR" in which R" is alkyl of 1-15 carbon atoms or --OR" in which R" alkyl of 1-15 carbon atoms, R' is hydrogen, alkyl or an alkyloxycarbonyl having 1-12 carbon atoms, m is 1 or 3, and n is an integer of 2-8 or 3-10 with the proviso that m is 1 or 3 respectively.
Claim 2
Dependent Claim 92 words
An absorption promoting agent for application to live body membranes, comprising at least one member as the effective ingredient for promoting absorption, selected from azacycloalkane derivatives represented by the following general formula (I) ##STR53## wherein R is --SR" in which R" is alkyl of 1-15 carbon atoms or --OR" in which R" alkyl of 1-15 carbon atoms, R' is hydrogen, alkyl or an alkyloxycarbonyl having 1-12 carbon atoms, m is 1 or 3, and n is an integer of 2-8 or 3-10 with the proviso that m is 1 or 3 respectively.
Claim 3
Dependent Claim 53 words
An absorption promoting agent according to claim 1, wherein m is 1, n is an integer of 2-8, R is --SR" in which R" is an alkyl group having 5-11 or 3-11 carbon atoms with the proviso that n is an integer of 2-3 or 4-8 respectively, and R' is a hydrogen atom.
Claim 4
Dependent Claim 53 words
An absorption promoting agent according to claim 1, wherein m is 3, n is an integer of 3-10, R is --SR" in which R" is an alkyl group having 5-12 or 2-12 carbon atoms with the proviso that n is 3 or an integer of 4-10 respectively, and R' is a hydrogen atom.
Claim 5
Dependent Claim 38 words
An absorption promoting agent according to claim 1, wherein m is 1, n is an integer of 2-8, R is --OR" in which R" is an alkyl group having 5-11 carbon atoms, and R' is a hydrogen atom.
Claim 6
Dependent Claim 38 words
An absorption promoting agent according to claim 1, wherein m is 3, n is an integer of 3-10, R is --OR" in which R" is an alkyl group having 4-10 carbon atoms, and R' is a hydrogen atom.
Claim 7
Dependent Claim 64 words
An absorption promoting agent according to claim 1, wherein R is --SR" in which R" in an alkyl group or --OR" in which R" is as defined above, R' is an alkyl group or alkyloxycarbonyl having 1-12 carbon atoms, m is 1 or 3, and n is an integer of 2-8 when m is 1 or an integer of 3-10 when m is 3.
Claim 8
Dependent Claim 16 words
The absorption promoting agent according to claim 1, wherein said effective ingredient is 1-[2-(n-decylthio) ethyl] azacyclopentane-2-one.
Claim 9
Dependent Claim 106 words
An external preparation for application to live body membranes, comprising a pharmaceutially-active agent and an absorption promoting agent comprising 0.001-25% of at least one member as the effective ingredient for promoting absorption, selected from azacycloalkane derivatives represented by the following general formula (I) ##STR54## wherein R is --SR" in which R" is alkyl of 1-15 carbon atoms or --OR" in which R" is alkyl of 1-15 carbon atoms, R' is hydrogen, alkyl or an alkyloxycarbonyl having 1-12 carbon atoms, m is 1 or 3 and n is an integer of 2-8 or 3-10 with the proviso that m is 1 or 3 respectively and inert excipients.
Claim 10
Dependent Claim 106 words
An external preparation for application to live body membranes, comprising a pharmaceutially-active agent and an absorption promoting agent comprising 0.001-25% of at least one member as the effective ingredient for promoting absorption, selected from azacycloalkane derivatives represented by the following general formula (I) ##STR54## wherein R is --SR" in which R" is alkyl of 1-15 carbon atoms or --OR" in which R" is alkyl of 1-15 carbon atoms, R' is hydrogen, alkyl or an alkyloxycarbonyl having 1-12 carbon atoms, m is 1 or 3 and n is an integer of 2-8 or 3-10 with the proviso that m is 1 or 3 respectively and inert excipients.
Claim 11
Dependent Claim 25 words
An external preparation according to claim 8 which is in the form of suppository, plaster, cataplasma, tape, paste, ointment, gel, cream, lotion, liniment or film.
Claim 12
Dependent Claim 106 words
An external preparation according to claim 8 wherein the pharmaceutically-active agent is an antibiotic, a chemotherapeutic agent, a bacteriostatic agent, an antimicrobial, a disinfectant, an antifungal agent, a non-steroidal anti-inflammatory agent, a steroidal anti-inflammatory agent, a carcinostatic agent, a psychotropic drug, a local anesthetic, an antiparkinsonian drug, a sex hormone drug, an anti-sudorific agent, a sunscreen, an antiallergic agent, an antiarrhythmic agent, an hypotensive agent, a vasodilator, a capillary stabilizer, a skeletal muscle relaxant, an antiemetic, an antipsoriatic drug, a skin softener, an emollient, a prostaglandin, a liposoluble vitamin, an enzyme, a peptide hormone, an antidiabetic drug, an insect repellent, an insecticide or an agricultural chemical.

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1992-11-20 1993-05-22 1993-11-21 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1996-11-20 1997-05-22 1997-11-21 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 2000-11-20 2001-05-22 2001-11-21 $7700.00 Window Closed / Lapsed

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