Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1997-08-21
1999-07-27
Dees, Jose' G.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
540485, 540527, A61K 3155, C07D22310, C07D22312
Patent
active
059290676
DESCRIPTION:
BRIEF SUMMARY
The invention relates to compounds of formula I ##STR2## wherein R.sub.1 is aryl or heteroaryl; -C.sub.7 alkanedienylene, and disubstituted amino group being understood as including also an amino group in which the amino nitrogen is bonded into a ring, pharmaceutical compositions comprising those compounds, and to the use of those compounds in the therapeutic treatment of the human or animal body or in the manufacture of pharmaceutical compositions.
The general terms used hereinabove and hereinbelow preferably have the following meanings within the scope of this Application:
As already mentioned, a disubstituted amino group Am is to be understood as being also an amino group in which the amino nitrogen is bonded into a ring. That ring may be, for example, a saturated, partially unsaturated or aromatic ring. Such a ring contains--including the amino nitrogen--preferably from 3 to 8 ring members. In addition to the amino nitrogen, the ring may contain further hetero atoms, for example nitrogen, oxygen and/or sulfur atoms, and is unsubstituted or substituted.
Am is especially an amino group --NR.sub.5 R.sub.6 wherein R.sub.5 is hydrogen, unsubstituted or substituted lower alkyl, unsubstituted or substituted lower alkenyl, unsubstituted or substituted lower alkynyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted (aza, oxa or thia)-cycloalkyl, unsubstituted or substituted benzo-(aza, oxa or thia)-cycloalkyl, aryl, partially hydrated heteroaryl, heteroaryl or (unsubstituted or substituted lower alkyl, unsubstituted or substituted lower alkenyl, aryl or heteroaryl)-sulfonyl; and R.sub.6 is hydrogen, unsubstituted or substituted lower alkyl, unsubstituted or substituted lower alkenyl, unsubstituted or substituted lower alkynyl, aryl, heteroaryl or acyl; or a ring--Am may also be an aza-(cycloalkyl, cycloalkenyl, cycloalkynyl, partially hydrated heteroaryl or heteroaryl) radical, bonded via a ring nitrogen atom, which in addition to the amino nitrogen may contain further hetero atoms selected from nitrogen, oxygen and sulfur atoms and which is unsubstituted or substituted.
The term "lower" denotes a radical having up to and including 7 and especially up to and including 4 carbon atoms.
Lower alkyl is, for example, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl, neopentyl, n-hexyl or n-heptyl, preferably ethyl or methyl.
Substituted lower alkyl is to be understood as being lower alkyl that is substituted one or more times, especially from 1 to 3 times, by any desired substituent(s). Substituents that may be mentioned by way of example are: aryl, partially hydrated heteroaryl, heteroaryl, cycloalkyl, (aza, oxa or thia)-cycloalkyl, benzo-(aza, oxa or thia)-cycloalkyl, carboxy, lower alkoxycarbonyl, carbamoyl, lower alkylcarbamoyl, di-lower alkylcarbamoyl, cyano, amino, lower alkylamino, di-lower alkylamino, piperidino, morpholino, thiomorpholino, hydroxy, lower alkoxy, halogen, lower alkanoyl and benzoyl.
Substituted lower alkenyl is to be understood as being lower alkenyl that is substituted one or more times, especially once, by any desired substituent(s). Substituents that may be mentioned by way of example are: aryl, heteroaryl, carboxy and lower alkoxycarbonyl.
Substituted lower alkynyl is to be understood as being lower alkynyl that is substituted one or more times, especially once, by any desired substituent(s). Substituents that may be mentioned by way of example are: aryl, heteroaryl, carboxy and lower alkoxycarbonyl.
Halogen is, for example, chlorine, bromine or fluorine, but may also be iodine.
Acyl is, for example, lower alkanoyl, substituted lower alkanoyl, e.g. halo-lower alkanoyl, aryl-carbonyl, aryl-lower alkanoyl, heteroaryl-carbonyl or heteroaryl-lower alkanoyl. In particular, acyl is lower alkanoyl.
Lower alkanoyl is, for example, acetyl, propionyl or pivaloyl, but may also be, for example, formyl.
Carbamoyl is --CONH.sub.2. Oxo is a group .dbd.O.
Aryl is, for example, phenyl or naphthyl, each of which is unsubstituted or substituted, for example as in
REFERENCES:
patent: 5217996 (1993-06-01), Ksander
Angus M. MacLeod, et al., J. Med. Chem. vol. 36, 1993, pp. 2044-2045.
Cs. Somlai and L. Balaspiri, J. Prakt. Chem., vol. 336, 1994, pp. 525-529.
S. Natarajan, et al., "Nonhydrolyzable Tripeptide Analogs as Angiotensin-Converting Enzyme Inhibitors," The Squibb Institute for Medical Research, Princeton, NJ, pp. 429-433.
Macleod et al., (J. Med. Chem., vol. 36, No. 14 1993, pp. 2044-2045).
Somlai et al., (CVA 122:291495, J. Prakt. Chem./Chem.-Ztg. (1994), vol. 336(6), 525-9.
Auberson Yves
Betschart Claudia
Gerspacher Marc
Mah Robert
Ofner Silvio
Dees Jos,e G.
Loeschorn Carol A.
Novartis AG
Qazi Sabiha N.
LandOfFree
1-aryl-2-acylamino-ethane compounds and their use as neurokinin does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with 1-aryl-2-acylamino-ethane compounds and their use as neurokinin , we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and 1-aryl-2-acylamino-ethane compounds and their use as neurokinin will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-878928