Arylglycinamide derivatives and preparative processes therefor

{
  "publication_number": "US5439919A",
  "country": "US",
  "kind": "A",
  "title": "Arylglycinamide derivatives and preparative processes therefor",
  "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, R 1 and R 4 denote identically or differently hydrogen atoms or lower alkyl groups with 1 to 3 carbon atoms, R 2 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, R 3 denotes a hydrogen atom or lower alkyl group with 1 to 6 carbon atoms or it may form a ring constituting alkylene together with R 2, R 5 denotes a lower alkyl group with 1 to 6 carbon atoms or cycloalkyl group with 5 or 6 carbon atoms, R 6 denotes a hydrogen atom or lower alkyl group with 1 to 6 carbon atoms or it may form a ring constituting alkylene together with R 5, 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, R 1 and R 4 denote identically or differently hydrogen atoms or lower alkyl groups with 1 to 3 carbon atoms, R 2 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, R 3 denotes a hydrogen atom or lower alkyl group with 1 to 6 carbon atoms or it may form a ring constituting alkylene together with R 2, R 5 denotes a lower alkyl group with 1 to 6 carbon atoms or cycloalkyl group with 5 or 6 carbon atoms, R 6 denotes a hydrogen atom or lower alkyl group with 1 to 6 carbon atoms or it may form a ring constituting alkylene together with R 5, 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, R 1 and R 4 denote identically or differently hydrogen atoms or lower alkyl groups with 1 to 3 carbon atoms, R 2 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, R 3 denotes a hydrogen atom or lower alkyl group with 1 to 6 carbon atoms or it may form a ring constituting alkylene together with R 2, R 5 denotes a lower alkyl group with 1 to 6 carbon atoms or cycioalkyl group with 5 or 6 carbon atoms, R 6 denotes a hydrogen atom or lower alkyl group with 1 to 6 carbon atoms or it may form a ring constituting alkylene together with R 5, and m denotes 2 or 3), and their salts as effective ingredients."
  ],
  "description_excerpt": "The present invention relates to novel arylglycinamide derivatives and their salts effective as therapeutic agents for the dysurias such as urinary incontinence and pollakiuria.\n\nUrinary incontinence and pollakiuria give mental pains to the patients predisposing them to social isolation. These neurogenic bladder dysfunctions are characterized by overactive detrusor, in part.\n\nAnticholinergic drugs are used in treatment of urinary bladder dysfunctions associated with overactive detrusor, including oxybutynin hydrochloride and terodiline hydrochloride. Clinically, these drugs are effective for treatment of syndrome elicited by bladder activity, but they frequently cause the adverse effects such as dry mouth and urinary retention. The occurrence of such adverse effects is considered to be caused by non-selective anticholinergic action of these drugs, in part. Hence, new therapeutic drugs for urinary incontinence and pollakiuria that cause no serious adverse effects such as dry mouth, anuresis and difficulty in micturition have been desired strongly.\n\nAs for the arylglycinamide derivatives, there are reports on phenylglycine ester (Yakugaku Zasshi, 73, 1327 (1953)) and mandelic ester derivatives (J. Am. Chem. Soc., 70, 4214 (1948)) having an antispasmodic action, but they are different in structure from the novel compounds of the present invention. Moreover, there are no reports on the arylglycinamide derivatives having the therapeutic effect on the dysurias such as urinary incontinence and pollakiuria.",
  "cpc": [
    "C07D 295/185",
    "A61P 13/02",
    "A61P 15/00",
    "C07C 237/00",
    "C07C 237/20",
    "C07C 2601/02",
    "C07C 2601/08",
    "C07C 2601/14",
    "C07C 2602/42",
    "C07C 2603/74",
    "C07D 295/13"
  ],
  "ipc": [
    "A61K 31/16",
    "A61P 13/02",
    "A61P 15/00",
    "C07C 231/12",
    "C07C 237/00",
    "C07C 237/20",
    "C07D 295/12",
    "C07D 295/13",
    "C07D 295/185"
  ],
  "assignees": [
    "Kyorin Pharmaceutical Co Ltd"
  ],
  "inventors": [
    "Hiroyuki Miyachi",
    "Mitsuru Segawa",
    "Emiko Tagami",
    "Hideo Okubo"
  ],
  "filing_date": "1993-07-20",
  "publication_date": "1995-08-08",
  "grant_date": "1995-08-08",
  "priority_date": "1992-07-27",
  "application_number": "US-9385493-A",
  "family_id": "26510045",
  "cited_by_count": 7,
  "citations": [
    "FR1269556A",
    "EP0222099A2",
    "US5153226A"
  ]
}