RU93058290A - Thiopyranopyrrole derivatives, methods for their production and containing their pharmaceutical composition - Google Patents
Thiopyranopyrrole derivatives, methods for their production and containing their pharmaceutical compositionInfo
- Publication number
- RU93058290A RU93058290A RU93058290/04A RU93058290A RU93058290A RU 93058290 A RU93058290 A RU 93058290A RU 93058290/04 A RU93058290/04 A RU 93058290/04A RU 93058290 A RU93058290 A RU 93058290A RU 93058290 A RU93058290 A RU 93058290A
- Authority
- RU
- Russia
- Prior art keywords
- production
- methods
- pharmaceutical composition
- derivatives
- thiopyranopyrrole
- Prior art date
Links
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- ADNPLDHMAVUMIW-CUZNLEPHSA-N (2S)-2-[[(2S)-1-[(2S)-6-amino-2-[[(2S)-1-[(2S)-2-amino-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-N-[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-y Chemical compound C([C@@H](C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(N)=O)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](CCCCN)NC(=O)[C@H]1N(CCC1)C(=O)[C@@H](N)CCCN=C(N)N)C1=CC=CC=C1 ADNPLDHMAVUMIW-CUZNLEPHSA-N 0.000 claims 1
- 102100002996 TAC1 Human genes 0.000 claims 1
- 101700065588 TAC1 Proteins 0.000 claims 1
- 125000004442 acylamino group Chemical group 0.000 claims 1
- 125000004423 acyloxy group Chemical group 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 1
- 125000000278 alkyl amino alkyl group Chemical group 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 125000004414 alkyl thio group Chemical group 0.000 claims 1
- 125000004103 aminoalkyl group Chemical group 0.000 claims 1
- 230000003042 antagnostic Effects 0.000 claims 1
- 239000005557 antagonist Substances 0.000 claims 1
- 125000001584 benzyloxycarbonyl group Chemical group C(=O)(OCC1=CC=CC=C1)* 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 125000003678 cyclohexadienyl group Chemical group C1(=CC=CCC1)* 0.000 claims 1
- 125000004985 dialkyl amino alkyl group Chemical group 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- MYMOFIZGZYHOMD-UHFFFAOYSA-N oxygen Chemical group O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 239000001301 oxygen Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000011780 sodium chloride Substances 0.000 claims 1
Claims (1)
где Х - кислород или NН; R1 - фенил, при необходимости замещенный, циклогексадиенил, нафтил или гетероциклил; R2 - водород, галоген, ОН, алкил, аминоалкил, алкиламиноалкил, диалкиламиноалкил, алкилокси, алкилтио, ацилокси, карбокси, алкилоксикарбонил, при необходимости замещенный; бензилоксикарбонил, амино- или ациламино; n = 0,1 или 2, в виде их стереоизомерных форм или их смесей, при необходимости в виде их солей, когда они существуют, и способ их получения. Новые производные согласно изобретению особенно представляют интерес как антагонисты вещества Р.New derivatives of thiopyranopyrrole of the general formula
where X is oxygen or NH; R 1 is phenyl, optionally substituted, cyclohexadienyl, naphthyl or heterocyclyl; R 2 is hydrogen, halogen, OH, alkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkyloxy, alkylthio, acyloxy, carboxy, alkyloxycarbonyl, optionally substituted; benzyloxycarbonyl, amino or acylamino; n = 0.1 or 2, in the form of their stereoisomeric forms or their mixtures, if necessary, in the form of their salts, when they exist, and the method for their preparation. The novel derivatives of the invention are of particular interest as antagonists of substance P.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR91/06037 | 1991-05-17 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU93058290A true RU93058290A (en) | 1996-12-27 |
Family
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