Arylglycinamide derivatives and preparative processes therefor

• US 5,439,919 A
• Filed: 07/20/1993
• Issued: 08/08/1995
• Est. Priority Date: 07/27/1992
• Status: Expired due to Fees

• Current Assignee: Kyorin Pharmaceutical Company Limited (Kyorin Holdings Incorporated)
• Original Assignee: Kyorin Pharmaceutical Company Limited (Kyorin Holdings Incorporated)
• Inventors: Okubo, Hideo, Tagami, Emiko, Miyachi, Hiroyuki, Segawa, Mitsuru
• Primary Examiner(s): Ivy, C. Warren
• Assistant Examiner(s): COVINGTON, RAYMOND K
• Application Number:
  US08/093,854
• Time in Patent Office: 749 Days
• Field of Search: 546/225, 546/195, 546/189, 546/203, 546/205, 546/226, 546/233, 546/234, 564/164, 564/165, 564/168, 514/330, 514/316, 514/319, 514/331, 514/325, 514/620, 514/423, 514/428, 548/540
• US Class Current: 514/316
• CPC Class Codes: A61P 13/02 of urine or of the urinary tract, e.g. urine acidifiers
• CPC Class Codes: A61P 15/00 Drugs for genital or sexual disorders for disorders of sex hormones A61P5/24; Contraceptives
• CPC Class Codes: C07C 237/20 the carbon skeleton containing six-membered aromatic rings
• CPC Class Codes: C07C 2601/02 with a three-membered ring
• CPC Class Codes: C07C 2601/08 the ring being saturated
• CPC Class Codes: C07C 2601/14 The ring being saturated
• CPC Class Codes: C07C 2602/42 the bicyclo ring system containing seven carbon atoms
• CPC Class Codes: C07C 2603/74 Adamantanes
• CPC Class Codes: C07D 295/13 to an acyclic saturated chain
• CPC Class Codes: C07D 295/185 from aliphatic carboxylic acids

Abstract

Arylglycinamide derivatives represented by a general formula (1) ##STR1## (wherein Ar denotes a phenyl group which may have 1 to 3 substituents or naphthyl group which may have 1 to 3 substituents, R₁ and R₄ denote identically or differently hydrogen atoms or lower alkyl groups with 1 to 3 carbon atoms, R₂ denotes a lower alkyl group with 1 to 6 carbon atoms, cycloalkyl group with 3 to 6 carbon atoms, lower alkyl group with 1 to 4 carbon atoms which may have a phenyl group which may have 1 to 3 substituents, norbornyl group, adamantyl group or phenyl group which may have 1 to 3 substituents, R₃ denotes a hydrogen atom or lower alkyl group with 1 to 6 carbon atoms or it may form a ring constituting alkylene together with R₂, R₅ denotes a lower alkyl group with 1 to 6 carbon atoms or cycloalkyl group with 5 or 6 carbon atoms, R₆ denotes a hydrogen atom or lower alkyl group with 1 to 6 carbon atoms or it may form a ring constituting alkylene together with R₅, and m denotes 2 or 3), and their salts, which function as effective therapeutic drugs for the dysurias such as urinary incontinence and pollakiuria, and the preparative processes therefor are presented.

Claims

1. Arylglycinamide derivatives represented by a general formula ( 1 ) ##STR85## (wherein Ar denotes a phenyl group which may have 1 to 3 substituents or naphthyl group which may have 1 to 3 substituents, R₁ and R₄ denote identically or differently hydrogen atoms or lower alkyl groups with 1 to 3 carbon atoms, R₂ denotes a lower alkyl group with 1 to 6 carbon atoms, cycloalkyl group with 3 to 6 carbon atoms, lower alkyl group with 1 to 4 carbon atoms which may have a phenyl group which may have 1 to 3 substituents, norbornyl group, adamantyl group or phenyl group which may have 1 to 3 substituents, R₃ denotes a hydrogen atom or lower alkyl group with 1 to 6 carbon atoms or it may form a ring constituting alkylene together with R₂, R₅ denotes a lower alkyl group with 1 to 6 carbon atoms or cycloalkyl group with 5 or 6 carbon atoms, R₆ denotes a hydrogen atom or lower alkyl group with 1 to 6 carbon atoms or it may form a ring constituting alkylene together with R₅, and m denotes 2 or 3), and their salts.

2. A therapeutic drug for the dysurias having at least one kind of arylglycinamide represented by a general formula ( 1 ) ##STR86## (wherein Ar denotes a phenyl group which may have 1 to 3 substituents or naphthyl group which may have 1 to 3 substituents, R₁ and R₄ denote identically or differently hydrogen atoms or lower alkyl groups with 1 to 3 carbon atoms, R₂ denotes a lower alkyl group with 1 to 6 carbon atoms, cycloalkyl group with 3 to 6 carbon atoms, lower alkyl group with 1 to 4 carbon atoms which may have a phenyl group which may have 1 to 3 substituents, norbornyl group, adamantyl group or phenyl group which may have 1 to 3 substituents, R₃ denotes a hydrogen atom or lower alkyl group with 1 to 6 carbon atoms or it may form a ring constituting alkylene together with R₂, R₅ denotes a lower alkyl group with 1 to 6 carbon atoms or cycioalkyl group with 5 or 6 carbon atoms, R₆ denotes a hydrogen atom or lower alkyl group with 1 to 6 carbon atoms or it may form a ring constituting alkylene together with R₅, and m denotes 2 or 3), and their salts as effective ingredients.