RU96105063A - OXATIOLANES, METHOD OF THEIR PRODUCTION AND CONTAINING THEIR PHARMACEUTICAL COMPOSITION - Google Patents
OXATIOLANES, METHOD OF THEIR PRODUCTION AND CONTAINING THEIR PHARMACEUTICAL COMPOSITIONInfo
- Publication number
- RU96105063A RU96105063A RU96105063/04A RU96105063A RU96105063A RU 96105063 A RU96105063 A RU 96105063A RU 96105063/04 A RU96105063/04 A RU 96105063/04A RU 96105063 A RU96105063 A RU 96105063A RU 96105063 A RU96105063 A RU 96105063A
- Authority
- RU
- Russia
- Prior art keywords
- compounds according
- radical
- formula
- general formula
- acyl
- Prior art date
Links
- 239000008194 pharmaceutical composition Substances 0.000 title claims 2
- 150000001875 compounds Chemical class 0.000 claims 7
- 125000002950 monocyclic group Chemical group 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 3
- 239000011780 sodium chloride Substances 0.000 claims 3
- 125000005354 acylalkyl group Chemical group 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 125000004435 hydrogen atoms Chemical group [H]* 0.000 claims 2
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 2
- 229910052500 inorganic mineral Inorganic materials 0.000 claims 2
- 239000011707 mineral Substances 0.000 claims 2
- 150000007522 mineralic acids Chemical class 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- 230000003287 optical Effects 0.000 claims 2
- 150000007524 organic acids Chemical class 0.000 claims 2
- 150000002891 organic anions Chemical class 0.000 claims 2
- 125000002943 quinolinyl group Chemical class N1=C(C=CC2=CC=CC=C12)* 0.000 claims 2
- SNICXCGAKADSCV-JTQLQIEISA-N Nicotine Chemical class CN1CCC[C@H]1C1=CC=CN=C1 SNICXCGAKADSCV-JTQLQIEISA-N 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- 230000000840 anti-viral Effects 0.000 claims 1
- 125000003710 aryl alkyl group Chemical group 0.000 claims 1
- 125000002619 bicyclic group Chemical group 0.000 claims 1
- 125000004432 carbon atoms Chemical group C* 0.000 claims 1
- 150000001732 carboxylic acid derivatives Chemical class 0.000 claims 1
- 125000004925 dihydropyridyl group Chemical class N1(CC=CC=C1)* 0.000 claims 1
- 125000005044 dihydroquinolinyl group Chemical class N1(CC=CC2=CC=CC=C12)* 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 150000002367 halogens Chemical group 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 230000003000 nontoxic Effects 0.000 claims 1
- 231100000252 nontoxic Toxicity 0.000 claims 1
- 239000000546 pharmaceutic aid Substances 0.000 claims 1
Claims (1)
в которой R является ацильным или аралкильным радикалом, происходящим из моно- или бициклического азотсодержащего гетероцикла, а оксиметильная группа в положении 2 находится в цис-положении по отношению к плоскости, определяемой положениями 2 и 5.1. 5- (Cytosinyl-1) -1,3-oxathiolane cis configuration (2R, 5S or 2S, 5R) of General formula I
in which R is an acyl or aralkyl radical derived from a mono- or bicyclic nitrogen-containing heterocycle, and the hydroxymethyl group in position 2 is in the cis position with respect to the plane defined by positions 2 and 5.
3. 5-(Цитозинил-1)-1,3-оксатиоланы по п. 1 конфигурации 2S,5R общей формулы II
4. Никотиновые соединения по пп.1 - 3, в которых R имеет формулу Iа
в которой X является водородом, атомом галоида, нитрогруппой, низшим алкокси или трифторметильным радикалом;
n является целым числом от 1 до 3,
и в которой ацильный остаток находится в положении 2, 3 или 4.2. 5- (Cytosinyl-1) -1,3-oxathiolane according to claim 1 configuration 2R, 5S of General formula I
3. 5- (Cytosinyl-1) -1,3-oxathiolanes according to claim 1 of configuration 2S, 5R of general formula II
4. Nicotinic compounds according to claims 1 - 3, in which R has the formula Ia
wherein X is hydrogen, a halogen atom, a nitro group, a lower alkoxy, or a trifluoromethyl radical;
n is an integer from 1 to 3,
and in which the acyl residue is in position 2, 3, or 4.
в которой R1 является алкильным радикалом, имеющим 1 - 10 атомов углерода, X и n имеют указанные выше значения ацильный радикал находится в положении 2, 3 или 4.5. Dihydropyridine compounds according to claims 1 - 3, in which R has the formula Ib
in which R 1 is an alkyl radical having 1 to 10 carbon atoms, X and n have the above values, the acyl radical is in position 2, 3 or 4.
в которой A является минеральным или органическим анионом, R1, X и n имеют указанные выше значения и ацильный радикал находится в положении 2, 3 или 4.6. Quaternized nicotine compounds according to claims 1 - 3, in which R has the formula Ib
in which A is a mineral or organic anion, R 1 , X and n have the above values and the acyl radical is in position 2, 3 or 4.
в которой карбонильный радикал находится в положении 2, 3 или 4, X является водородом, галоидом, трифторметильным радикалом, низшим алкокси или нитрогруппой и n' является целым числом от 1 до 6.7. Quinoline compounds according to one of claims 1 to 3, in which R has the general formula Ig
wherein the carbonyl radical is in the 2, 3 or 4 position, X is hydrogen, halogen, a trifluoromethyl radical, a lower alkoxy or a nitro group, and n 'is an integer from 1 to 6.
в которой R1 и X имеют указанные выше значения и n' является целым числом от 1 до 6.8. Dihydroquinoline compounds according to claims 1 - 3, in which R has the general formula Id
in which R 1 and X have the above values and n 'is an integer from 1 to 6.
в которой R1, X и n' имеют указанные выше значения, ацильный радикал находится в положении 2, 3 или 4 и A является минеральным или органическим анионом.9. Quaternized quinoline compounds according to claims 1 - 3, in which R has the general formula I
in which R 1 , X and n 'are as defined above, the acyl radical is in position 2, 3 or 4 and A is a mineral or organic anion.
в которой R1, X и n имеют указанные ранее значения и m является числом от 1 до 6.10. (Dihydropyridylamine) compounds according to claims 1 - 3, in which R has the formula I (g)
in which R 1 , X and n have the previously specified values and m is a number from 1 to 6.
в которой R является ацильным или аралкильным радикалом, происходящим из моно- или бициклического, азотсодержащего ароматического или дигидроароматического гетероцикла, и оксиметильная группа в положении 2 находится в цис-положении по отношению к плоскости, определяемой положениями 2 и 5, или одну из солей присоединения кислоты в рацемической или оптически активной форме, в смеси или ассоциации с инертным, нетоксичным, фармацевтически приемлемым экципиентом.15. Pharmaceutical composition of antiviral action, characterized in that it contains as active principle at least one compound of general formula I
in which R is an acyl or aralkyl radical derived from a mono- or bicyclic, nitrogen-containing aromatic or dihydroaromatic heterocycle, and the hydroxymethyl group in position 2 is in the cis-position relative to the plane defined by positions 2 and 5, or one of the acid addition salts in racemic or optically active form, in mixture or association with an inert, non-toxic, pharmaceutically acceptable excipient.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
FR9406262 | 1994-05-24 | ||
FR9406262A FR2720397B1 (en) | 1994-05-24 | 1994-05-24 | New oxathiolanes, process for their preparation and pharmaceutical compositions containing them. |
PCT/FR1995/000683 WO1995032200A1 (en) | 1994-05-24 | 1995-05-24 | Oxathiolanes, method for their preparation and pharmaceutical compositions containing same |
Publications (2)
Publication Number | Publication Date |
---|---|
RU96105063A true RU96105063A (en) | 1998-05-20 |
RU2142462C1 RU2142462C1 (en) | 1999-12-10 |
Family
ID=9463449
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
RU96105063A RU2142462C1 (en) | 1994-05-24 | 1995-05-24 | 5-(cytosinyl-1)-1,3-oxathiolanes, method of their synthesis and pharmaceutical composition |
Country Status (19)
Country | Link |
---|---|
US (1) | US5708000A (en) |
EP (1) | EP0733053A1 (en) |
JP (1) | JPH09502453A (en) |
KR (1) | KR100242891B1 (en) |
CN (1) | CN1080264C (en) |
AP (1) | AP612A (en) |
AU (1) | AU688052B2 (en) |
BR (1) | BR9506244A (en) |
CA (1) | CA2167930A1 (en) |
CZ (1) | CZ21996A3 (en) |
FI (1) | FI960316A (en) |
FR (1) | FR2720397B1 (en) |
HU (1) | HU219299B (en) |
NO (1) | NO306299B1 (en) |
NZ (1) | NZ287478A (en) |
OA (1) | OA10258A (en) |
PL (1) | PL181713B1 (en) |
RU (1) | RU2142462C1 (en) |
WO (1) | WO1995032200A1 (en) |
Families Citing this family (12)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
FR2720397B1 (en) * | 1994-05-24 | 1996-08-23 | Laphal Laboratoires Sa | New oxathiolanes, process for their preparation and pharmaceutical compositions containing them. |
IT1290447B1 (en) * | 1997-03-28 | 1998-12-03 | Zambon Spa | 1,3-OSSATIOLANIC DERIVATIVES FOR ANTI-VIRAL ACTIVITY |
US20100074949A1 (en) | 2008-08-13 | 2010-03-25 | William Rowe | Pharmaceutical composition and administration thereof |
US8354427B2 (en) * | 2004-06-24 | 2013-01-15 | Vertex Pharmaceutical Incorporated | Modulators of ATP-binding cassette transporters |
NZ587551A (en) | 2004-06-24 | 2012-01-12 | Vertex Pharma | 5-Amino-phenol derivatives such as 5-amino-2,4-di-tert-butyl-phenol |
CN101374849A (en) * | 2005-12-24 | 2009-02-25 | 沃泰克斯药物股份有限公司 | Quinoline-4-ketones derivates as ABC transport protein regulation/control agent |
SI3219705T1 (en) | 2005-12-28 | 2020-08-31 | Vertex Pharmaceuticals Incorporated | Pharmaceutical compositions of the amorphous form of n-(2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl)-1,4-dihydro-4-oxoquinoline-3-carboxamide |
PE20071025A1 (en) * | 2006-01-31 | 2007-10-17 | Mitsubishi Tanabe Pharma Corp | TRISUSTITUTED AMINE COMPOUND |
RU2543714C2 (en) | 2009-03-20 | 2015-03-10 | Вертекс Фармасьютикалз Инкорпорейтед | Method of obtaining modulators of cystic fibrousis transmembrane conductance regulator |
US8802700B2 (en) | 2010-12-10 | 2014-08-12 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-Binding Cassette transporters |
BR112014021090B1 (en) | 2012-02-27 | 2023-01-24 | Vertex Pharmaceuticals Incorporated | PHARMACEUTICAL COMPOSITION AND USE OF N-[2,4-BIS(1,1-DIMETHYLethyl)-5-HYDROXYPHENYL]-1,4-DIHYDRO-4-OXOQUINOLINE3-CARBOXAMIDE IN THE PREPARATION OF THE SAME |
RU2749213C2 (en) | 2014-10-07 | 2021-06-07 | Вертекс Фармасьютикалз Инкорпорейтед | Co-crystals of transmembrane conduction regulator modulators in cystic fibrosis |
Family Cites Families (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5047407A (en) * | 1989-02-08 | 1991-09-10 | Iaf Biochem International, Inc. | 2-substituted-5-substituted-1,3-oxathiolanes with antiviral properties |
DE69122264T2 (en) * | 1990-11-13 | 1997-02-06 | Biochem Pharma Inc., Laval, Quebec | SUBSTITUTED 1,3-OXATHIOLANS WITH ANTIVIRAL PROPERTIES |
WO1992020344A1 (en) * | 1991-05-16 | 1992-11-26 | Glaxo Group Limited | Antiviral combinations containing nucleoside analogs |
GB9110874D0 (en) * | 1991-05-20 | 1991-07-10 | Iaf Biochem Int | Medicaments |
FR2720397B1 (en) * | 1994-05-24 | 1996-08-23 | Laphal Laboratoires Sa | New oxathiolanes, process for their preparation and pharmaceutical compositions containing them. |
-
1994
- 1994-05-24 FR FR9406262A patent/FR2720397B1/en not_active Expired - Fee Related
-
1995
- 1995-05-24 CN CN95190647A patent/CN1080264C/en not_active Expired - Fee Related
- 1995-05-24 WO PCT/FR1995/000683 patent/WO1995032200A1/en not_active Application Discontinuation
- 1995-05-24 JP JP7530108A patent/JPH09502453A/en not_active Ceased
- 1995-05-24 KR KR1019960700446A patent/KR100242891B1/en not_active IP Right Cessation
- 1995-05-24 RU RU96105063A patent/RU2142462C1/en active
- 1995-05-24 CZ CZ96219A patent/CZ21996A3/en unknown
- 1995-05-24 EP EP95920986A patent/EP0733053A1/en not_active Withdrawn
- 1995-05-24 CA CA002167930A patent/CA2167930A1/en not_active Abandoned
- 1995-05-24 BR BR9506244A patent/BR9506244A/en active Search and Examination
- 1995-05-24 US US08/586,892 patent/US5708000A/en not_active Expired - Fee Related
- 1995-05-24 HU HU9600155A patent/HU219299B/en not_active IP Right Cessation
- 1995-05-24 AU AU26209/95A patent/AU688052B2/en not_active Ceased
- 1995-05-24 PL PL95312693A patent/PL181713B1/en unknown
- 1995-05-25 NZ NZ287478A patent/NZ287478A/en unknown
-
1996
- 1996-01-23 AP APAP/P/1996/000784A patent/AP612A/en active
- 1996-01-23 FI FI960316A patent/FI960316A/en unknown
- 1996-01-23 NO NO960272A patent/NO306299B1/en not_active IP Right Cessation
- 1996-01-24 OA OA60770A patent/OA10258A/en unknown
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