4-(Alkylamino-2-hydroxypropoxy)-indenes and method of use

{
  "publication_number": "US4127675A",
  "country": "US",
  "kind": "A",
  "title": "4-(Alkylamino-2-hydroxypropoxy)-indenes and method of use",
  "abstract": "Novel indene derivatives represented by the general formula wherein R represents lower alkyl, phenylloweralkyl or lower cycloalkyl, and acid addition salts thereof useful as beta -receptor antagonists.",
  "claims": [
    "1. A method of establishing an adrenergic β-receptor blockade which comprises administering to a patient in which such blockade is desired a pharmaceutically effective amount of a compound selected from the group consisting of 4-(3-isopropylamino-2-hydroxypropoxy)indene, 4-(3-tert-butylamino-2-hydroxypropoxy)indene and a non-toxic acid addition salt thereof.",
    "2. A method according to claim 1, wherein the compound is 4-(3-isopropylamino-2-hydroxypropoxy)indene.",
    "3. A method according to claim 1, wherein the compound is 4-(3-tert-butylamino-2-hydroxypropoxy)indene.",
    "4. A compound selected from the group consisting of 4-(3-tert-butylamino-2-hydroxypropoxy)indene and a non-toxic acid addition salt thereof.",
    "5. A pharmaceutical composition which comprises, as active ingredient, a compound selected from the group consisting of 4-(3-isopropylamino-2-hydroxypropoxy)indene, 4-(3-tert-butylamino-2-hydroxypropoxy)indene and a non-toxic acid addition salt thereof, and a pharmaceutically acceptable carrier therefor.",
    "6. A composition as claimed in claim 5, wherein the active ingredient is 4-(3-isopropylamino-2-hydroxypropoxy)indene.",
    "7. A composition as claimed in claim 5, wherein the active ingredient is 4-(3-tert-butylamino-2-hydroxypropoxy)indene."
  ],
  "description_excerpt": "This application is a divisional of Ser. No. 568,097, filed Apr. 14, 1975, now U.S. Pat. No. 4,045,482 which is a continuation of Ser. No. 141,936, filed May 10, 1971, now abandoned, which is a continuation-in-part of Ser. No. 876,070, filed Nov. 12, 1969, now abandoned.\n\nThis invention relates to novel indene derivatives having valuable therapeutic properties, non-toxic salts thereof, and to processes for their production.\n\nThe therapeutically active compounds of this invention are represented by the general formula ##STR2## wherein R represents a lower alkyl, phenylloweralkyl or lower cycloalkyl group.\n\nThe term \"lower alkyl\" as used herein means both straight and branched chain aliphatic hydrocarbon groups such as methyl, ethyl, propyl, isopropyl, butyl, isobutyl, t-butyl, amyl, hexyl, etc. The term \"phenylloweralkyl\", which may contain more than one phenyl group, is represented by groups such as benzyl, diphenylmethyl, β-phenylisopropyl, etc. The term \"lower cycloalkyl\" is represented by groups such as cyclopentyl and cyclohexyl, etc.\n\nThe compounds I of the present invention can be prepared by reacting a compound of the general formula ##STR3## wherein A represents a hydrogen atom or a 2,3-epoxypropyl group with an amine of the general formula\n\nwherein R is defined as above and B represents a 3-halogeno-2-hydroxypropyl group when A is a hydrogen atom; and when A is a 2,3-epoxypropyl group, B is a hydrogen atom.",
  "cpc": [
    "A61K 31/135",
    "F16B 2/06"
  ],
  "ipc": [
    "A61K 31/135",
    "F16B 2/06"
  ],
  "assignees": [
    "Yamanouchi Pharmaceutical Co Ltd"
  ],
  "inventors": [
    "Masuo Murakami",
    "Kiyoshi Murase",
    "Kunihiro Niigata",
    "Shiro Tachikawa",
    "Toichi Takenaka"
  ],
  "filing_date": "1976-10-21",
  "publication_date": "1978-11-28",
  "grant_date": "1978-11-28",
  "priority_date": "1968-11-12",
  "application_number": "US-73451476-A",
  "family_id": "27300987",
  "cited_by_count": 5,
  "citations": [
    "US3051709A",
    "US3234211A",
    "US3415873A"
  ]
}