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 Title: |
US6093734:
Prodrugs of proton pump inhibitors
[ Derwent Title ]
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| Country: |
US United States of America
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| Inventor: |
Garst, Michael E.; Newport Beach, CA
Sachs, George; Encino, CA
Shin, Jai Moo; Northridge, CA
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| Assignee: |
Partnership of Michael E. Garst, George Sachs, and Jai Moo Shin, Newport Beach, CA
other patents from PARTNERSHIP OF MICHAEL E. GARST, GEORGE SACHS, AND JAI MOO SHIN (770885) (approx. 1)
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| Published / Filed: |
2000-07-25
/ 1998-08-10
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| Application Number: |
US1998000131481
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| IPC Code: |
Advanced:
C07D 235/28;
C07D 401/12;
C07D 401/14;
C07D 409/14;
C07D 417/14;
C07D 471/04;
C07F 9/6558;
Core:
C07D 235/00;
C07D 401/00;
C07D 409/00;
C07D 417/00;
C07D 471/00;
C07F 9/00;
IPC-7:
A61K 31/4439;
A61K 31/445;
C07D 401/12;
C07D 401/14;
C07D 413/12;
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| ECLA Code: |
C07D401/12; C07D235/28; C07D401/14; C07D409/14; C07D417/14; C07D471/04; C07F9/6558B; M07D401/12+235C+213; M07D401/14+235C+213+213; M07D401/14+249+235C+213; M07D409/14+333B+235C+213; M07D417/14+277B+235C+213; M07D471/04+235B+221B; M07D235/28; M07D401/12; M07D401/14; M07D409/14; M07D417/14; M07D471/04;
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| U.S. Class: |
Current:
514/338;
514/235.2;
514/318;
544/124;
546/194;
546/273.7;
Original:
514/338;
514/318;
514/235.2;
544/124;
546/273.7;
546/194;
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| Field of Search: |
546/273.7
514/338,318,235.2
544/124
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| Priority Number: |
| 1998-08-10 |
US1998000131481 |
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| Abstract: |
Prodrugs of the pyridyl methyl sulfinyl benzimidazole type proton pump inhibitor drugs have a hydrolyzable sulfinyl or arylsulfonyl group attached to the benzimidazole nitrogen, or include a group that forms a Mannich base with the benzimidazole nitrogen. The prodrugs of the invention hydrolyze under physiological conditions to provide the proton pump inhibitors with a half life measurable in hours, and are capable of providing sustained plasma concentrations of the proton pump inhibitor drugs for longer time than presently used drugs. The generation of the proton pump inhibitor drugs from the prodrugs of the invention under physiological conditions allows for more effective treatment of several diseases and conditions caused by gastric acid secretion.
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| Attorney, Agent or Firm: |
Klein & Szekeres, LLP ;
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| Primary / Asst. Examiners: |
Rotman, Alan L.;
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| Maintenance Status: |
CC Certificate of Correction issued
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| INPADOC Legal Status: |
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Family Legal Status Report
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| Designated Country: |
AE AL AM AP AZ BA BB BG BY CA CR CU CZ DM EA EE GD GE GH GM HR HU ID IL AT BE CH CY DE DK ES FR GB GR IE
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| Family: |
Show 45 known family members
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First Claim:
Show all 10 claims |
What is claimed is:
1. A compound of the formula [Figure] where R1, R2 and R3 are independently selected from hydrogen, alkyl of 1 to 10 carbons, fluoro substituted alkyl of 1 to 10 carbons, alkoxy of 1 to 10 carbons, fluoro substituted alkoxy of 1 to 10 carbons, alkylthio of 1 to 10 carbons, fluoro substituted alkylthio of 1 to 10 carbons, alkoxyalkoxy of 2 to 10 carbons, amino, alkylamino and dialkylamino each of the alkyl groups in said alkylamino and dialkyl amino groups having 1 to 10 carbons, halogen, phenyl, alkyl substituted phenyl, alkoxy substituted phenyl, phenylalkoxy, each of the alkyl groups in said alkyl substituted phenyl, alkoxy substituted phenyl and phenylalkoxy having 1 to 10 carbons, piperidino, morpholino or two of the R1, R2 and R3 groups jointly forming a 5 or 6 membered ring having 0 or 1 heteroatom selected from N, S and O;
- R6 through R9 are independently selected from hydrogen, alkyl of 1 to 10 carbons, halogen substituted alkyl of 1 to 10 carbons, alkoxy of 1 to 10 carbons, halogen substituted alkoxy of 1 to 10 carbons, alkylcarbonyl, alkoxycarbonyl, the alkyl group in said alkylcarbonyl and alkoxycarbonyl having 1 to 10 carbons, oxazolyl, imidazolyl, thiazolyl, pyrazolyl, or any two adjacent ones of the R6 through R9 groups may form a ring that may optionally include a heteroatom selected from N, 0 and S and said ring may be further substituted;
- R10, is hydrogen, alkyl of 1 to 10 carbons, or R10 may form an alkylene chain together with R3 ;
- R17 is alkyl of 1 to 10 carbons, halogen substituted alkyl of 1 to 10 carbons, alkoxy having 1 to 10 carbons, halogen substituted alkoxy of 1 to 10 carbons, alkylthio having 1 to 10 carbons, halogen substituted alkylthio of 1 to 10 carbons, alkoxy carbonyl having 1 to 10 carbons, halogen substituted alkoxy carbonyl having 1 to 10 carbons, F, Cl, Br, I, NO2, CN, OCOalkyl, NH2, alkylamino and dialkylamino where in said OCOalkyl,, alkylamino and dialkylamino groups each of said alkyl group has 1 to 10 carbons, and
- n is an integer having the value 0 to 5.
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| Background / Summary: |
Show background / summary
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| Drawing Descriptions: |
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| Description: |
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| Forward References: |
Show 7 U.S. patent(s) that reference this one
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| Foreign References: |
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| Other Abstract Info: |
CHEMABS 132(14)180572P
DERABS C2000-256240
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| Other References: |
B.G. Katzung MD,PhD Basic & Clinical Pharmacology, sixth Edition, p. 952, 95.
Design of prodrugs: Bioreversible derivatives for various functional groups and chemical entities, Design of Prodrugs (Bundgaard, H., ed.) 1985 Elsevier Science Publishers B.V. (Biomedical Division), Chapter 1, H. Bundgaard et al.
Formation of Prodrugs of Amines, Amides, Ureides, and Imides, by H. Bundgaard, Methods in Enzimology, vol. 112, pp. 347-359. (1998).
International Journal of Pharmaceuticals, vol. 22, 1984, pp. 45-56 (Elsevier, H. Bundgaard et al.
International Journal of Pharmaceuticals, vol. 29, 1986, pp. 19-28 (Elsevier), H. Bundgaard et al.
Journal of Medicinal Chemistry, vol. 32, No. 12, Dec. 1989, pp. 2503-2507, H. Bundgaard et al.
Chemical Abstracts, vol. 93, 1980, abstract No. 137935y, Bundgaard et al.
Chemical Abstracts, vol. 95, 1981, abstract No. 138493f, Bundgaard et al.
Chemical Abstracts, vol. 95, 1981, abstract No. 138592n, Bundgaard et al.
Chemical Abstracts, vol. 110, 1989, abstract No. 57664, Alminger et al.
Chemical Abstracts, vol. 115, 1991, abstract No. 64029s, Buur et al.
Chemical Abstracts, vol. 115, 1991, abstract No. 189582y, Hansen et al.
Chemical Abstracts, vol. 117, 1992, abstract No. 14347q, Bundgaard et al.
Chemical Abstracts, vol. 117, 1992, abstract No. 55790x, Jensen et al.
Chemical Abstracts, vol. 123, 1995, abstract No. 17593b, Thomsen et al.
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