RU96120189A - NEW PHARMACEUTICAL DRUGS AND METHODS FOR PRODUCING THEM - Google Patents
NEW PHARMACEUTICAL DRUGS AND METHODS FOR PRODUCING THEMInfo
- Publication number
- RU96120189A RU96120189A RU96120189/14A RU96120189A RU96120189A RU 96120189 A RU96120189 A RU 96120189A RU 96120189/14 A RU96120189/14 A RU 96120189/14A RU 96120189 A RU96120189 A RU 96120189A RU 96120189 A RU96120189 A RU 96120189A
- Authority
- RU
- Russia
- Prior art keywords
- alkaline
- dosage form
- enteric coating
- groups
- form according
- Prior art date
Links
- 229940079593 drugs Drugs 0.000 title 1
- 239000002552 dosage form Substances 0.000 claims 22
- 239000002702 enteric coating Substances 0.000 claims 12
- 238000009505 enteric coating Methods 0.000 claims 12
- 150000001875 compounds Chemical class 0.000 claims 10
- 239000011162 core material Substances 0.000 claims 9
- 230000003482 proton pump inhibitor Effects 0.000 claims 9
- 239000000612 proton pump inhibitor Substances 0.000 claims 9
- 125000000217 alkyl group Chemical group 0.000 claims 6
- 159000000011 group IA salts Chemical class 0.000 claims 6
- 229910052739 hydrogen Inorganic materials 0.000 claims 6
- 239000001257 hydrogen Substances 0.000 claims 6
- 239000010410 layer Substances 0.000 claims 6
- 229920000642 polymer Polymers 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- 239000011780 sodium chloride Substances 0.000 claims 5
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 150000002367 halogens Chemical class 0.000 claims 4
- 239000000463 material Substances 0.000 claims 4
- 241000124008 Mammalia Species 0.000 claims 3
- 210000002784 Stomach Anatomy 0.000 claims 3
- 239000002253 acid Substances 0.000 claims 3
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 150000002431 hydrogen Chemical class 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 150000002894 organic compounds Chemical class 0.000 claims 3
- 230000028327 secretion Effects 0.000 claims 3
- 238000000926 separation method Methods 0.000 claims 3
- SBQLYHNEIUGQKH-UHFFFAOYSA-N Omeprazole Chemical compound N1=C2[CH]C(OC)=CC=C2N=C1S(=O)CC1=NC=C(C)C(OC)=C1C SBQLYHNEIUGQKH-UHFFFAOYSA-N 0.000 claims 2
- 150000008044 alkali metal hydroxides Chemical class 0.000 claims 2
- 150000001412 amines Chemical class 0.000 claims 2
- 150000001413 amino acids Chemical class 0.000 claims 2
- 150000003863 ammonium salts Chemical class 0.000 claims 2
- 125000005586 carbonic acid group Chemical group 0.000 claims 2
- 239000008187 granular material Substances 0.000 claims 2
- 238000011065 in-situ storage Methods 0.000 claims 2
- 229960000381 omeprazole Drugs 0.000 claims 2
- 239000000546 pharmaceutic aid Substances 0.000 claims 2
- 125000005624 silicic acid group Chemical class 0.000 claims 2
- 235000012239 silicon dioxide Nutrition 0.000 claims 2
- VUKAUDKDFVSVFT-UHFFFAOYSA-N 2-[6-[4,5-bis(2-hydroxypropoxy)-2-(2-hydroxypropoxymethyl)-6-methoxyoxan-3-yl]oxy-4,5-dimethoxy-2-(methoxymethyl)oxan-3-yl]oxy-6-(hydroxymethyl)-5-methoxyoxane-3,4-diol Chemical compound COC1C(OC)C(OC2C(C(O)C(OC)C(CO)O2)O)C(COC)OC1OC1C(COCC(C)O)OC(OC)C(OCC(C)O)C1OCC(C)O VUKAUDKDFVSVFT-UHFFFAOYSA-N 0.000 claims 1
- LENZDBCJOHFCAS-UHFFFAOYSA-N 2-amino-2-(hydroxymethyl)propane-1,3-diol Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 claims 1
- 239000004475 Arginine Substances 0.000 claims 1
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims 1
- ODKSFYDXXFIFQN-BYPYZUCNSA-P L-argininium(2+) Chemical compound NC(=[NH2+])NCCC[C@H]([NH3+])C(O)=O ODKSFYDXXFIFQN-BYPYZUCNSA-P 0.000 claims 1
- HNDVDQJCIGZPNO-YFKPBYRVSA-N L-histidine Chemical compound OC(=O)[C@@H](N)CC1=CN=CN1 HNDVDQJCIGZPNO-YFKPBYRVSA-N 0.000 claims 1
- KDXKERNSBIXSRK-YFKPBYRVSA-N L-lysine Chemical compound NCCCC[C@H](N)C(O)=O KDXKERNSBIXSRK-YFKPBYRVSA-N 0.000 claims 1
- AHLPHDHHMVZTML-BYPYZUCNSA-N L-ornithine Chemical compound NCCC[C@H](N)C(O)=O AHLPHDHHMVZTML-BYPYZUCNSA-N 0.000 claims 1
- SIXIIKVOZAGHPV-UHFFFAOYSA-N Lansoprazole Chemical compound CC1=C(OCC(F)(F)F)C=CN=C1CS(=O)C1=NC2=CC=C[CH]C2=N1 SIXIIKVOZAGHPV-UHFFFAOYSA-N 0.000 claims 1
- 239000004472 Lysine Substances 0.000 claims 1
- MBBZMMPHUWSWHV-BDVNFPICSA-N Meglumine Chemical compound CNC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO MBBZMMPHUWSWHV-BDVNFPICSA-N 0.000 claims 1
- 229960003104 Ornithine Drugs 0.000 claims 1
- XAPRFLSJBSXESP-UHFFFAOYSA-N Oxycinchophen Chemical compound N=1C2=CC=CC=C2C(C(=O)O)=C(O)C=1C1=CC=CC=C1 XAPRFLSJBSXESP-UHFFFAOYSA-N 0.000 claims 1
- GRHYHJAAOJVRSZ-UHFFFAOYSA-N Pantoprazole Chemical group COC1=CC=NC(CS(=O)C=2N=C3[CH]C(OC(F)F)=CC=C3N=2)=C1OC GRHYHJAAOJVRSZ-UHFFFAOYSA-N 0.000 claims 1
- 229940035504 Tromethamine Drugs 0.000 claims 1
- 125000005083 alkoxyalkoxy group Chemical group 0.000 claims 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 1
- 125000005055 alkyl alkoxy group Chemical group 0.000 claims 1
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims 1
- 125000004414 alkyl thio group Chemical group 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 125000003710 aryl alkyl group Chemical group 0.000 claims 1
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 1
- 239000002775 capsule Substances 0.000 claims 1
- 125000004432 carbon atoms Chemical group C* 0.000 claims 1
- 229920001577 copolymer Polymers 0.000 claims 1
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 125000004663 dialkyl amino group Chemical group 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- SUPCQIBBMFXVTL-UHFFFAOYSA-N ethyl 2-methylprop-2-enoate Chemical compound CCOC(=O)C(C)=C SUPCQIBBMFXVTL-UHFFFAOYSA-N 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 239000011737 fluorine Substances 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- -1 for example Chemical compound 0.000 claims 1
- 125000004438 haloalkoxy group Chemical group 0.000 claims 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims 1
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 1
- 239000004615 ingredient Substances 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 229960003174 lansoprazole Drugs 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 1
- 230000001264 neutralization Effects 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 150000002829 nitrogen Chemical group 0.000 claims 1
- 150000007524 organic acids Chemical class 0.000 claims 1
- 125000002971 oxazolyl group Chemical group 0.000 claims 1
- 229960005019 pantoprazole Drugs 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000000587 piperidin-1-yl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 125000004950 trifluoroalkyl group Chemical group 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
- 229960000281 trometamol Drugs 0.000 claims 1
Claims (20)
где Het1 представляет собой:
Het2 представляет собой:
где N в бензимидазольной части означает, что один из атомов углерода, замещенных R6-R9, необязательно, замещен на атом азота каких-либо заместителей;
R1, R2 и R3, которые могут быть одинаковыми или различными, выбирают из водорода; алкильной группы; алкоксигруппы, необязательно замещенной фтором; алкилтио-группы; алкоксиалкокси-группы; диалкиламино-группы; пиперидино-группы; морфолино-группы; галогена; фенильной группы; и фенилакоксигруппы;
R4 и R5, которые могут быть одинаковыми или различными, выбирают из водорода, алкильной группы и аралкильной группы;
представляет собой водород, галоген, трифторметильную группу, алкильную группу и алкокси-группу;
R6-R9, которые могут быть одинаковыми или различными, выбирают из водорода; алкильной группы; алкокси-группы; галогена; галогеналкокси-группы; алкилкарбонильной группы; алкоксикарбонильной группы; оксазолильной группы, трифтор алкильной группы; либо смежные группы R6-R9 образуют кольцевые структуры, которые могут быть кроме того замещенными;
R10 является водородом; либо R10 и R3, взятые вместе, образуют алкиленовую цепь; и
R11 и R12, которые могут быть одинаковыми или различными, выбирают из водорода, галогена или алкильной группы; и алкильные группы, алкокси-группы и их части могут быть разветвленными и прямыми C1-C9-цепями, или составляют циклоалкильные группы, например, циклоалкилалкильную группу.9. The dosage form according to claim 1, characterized in that said proton pump inhibitor is a compound of general formula 1 or a pharmaceutically acceptable salt thereof or its pure enantiomer in neutral form or in the form of an alkaline salt:
where Het 1 represents:
Het 2 is:
where N in the benzimidazole moiety means that one of the carbon atoms substituted with R 6 -R 9 is optionally substituted on the nitrogen atom of any substituents;
R 1 , R 2 and R 3 , which may be the same or different, are selected from hydrogen; an alkyl group; alkoxy groups optionally substituted with fluorine; alkylthio groups; alkoxyalkoxy groups; dialkylamino groups; piperidino groups; morpholino groups; halogen; phenyl group; and phenylacoxy groups;
R 4 and R 5 , which may be the same or different, are selected from hydrogen, an alkyl group and an aralkyl group;
represents hydrogen, halogen, trifluoromethyl group, alkyl group and alkoxy group;
R 6 -R 9 , which may be the same or different, are selected from hydrogen; an alkyl group; alkoxy groups; halogen; haloalkoxy groups; an alkylcarbonyl group; alkoxycarbonyl group; oxazolyl group; trifluoroalkyl group; or adjacent R 6 -R 9 groups form ring structures which may be further substituted;
R 10 is hydrogen; or R 10 and R 3 taken together form an alkylene chain; and
R 11 and R 12 , which may be the same or different, are selected from hydrogen, halogen or an alkyl group; and alkyl groups, alkoxy groups and parts thereof may be branched and straight C 1 -C 9 chains, or form cycloalkyl groups, for example a cycloalkylalkyl group.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
SE9500478-4 | 1995-02-09 | ||
SE9500478A SE9500478D0 (en) | 1995-02-09 | 1995-02-09 | New pharmaceutical formulation and process |
Publications (2)
Publication Number | Publication Date |
---|---|
RU96120189A true RU96120189A (en) | 1998-12-27 |
RU2170090C2 RU2170090C2 (en) | 2001-07-10 |
Family
ID=20397154
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
RU96120189/14A RU2170090C2 (en) | 1995-02-09 | 1996-02-09 | Method of preparing pharmaceutical medicinal form, method of inhibition of acid secretion in stomach of mammals and humans |
Country Status (29)
Country | Link |
---|---|
US (5) | US6013281A (en) |
EP (2) | EP1174136A3 (en) |
JP (1) | JP3881377B2 (en) |
KR (1) | KR100405586B1 (en) |
CN (1) | CN1182841C (en) |
AT (1) | ATE218327T1 (en) |
BR (1) | BR9605121A (en) |
CA (1) | CA2186037C (en) |
CZ (1) | CZ291720B6 (en) |
DE (1) | DE69621523T2 (en) |
DK (1) | DK0752851T3 (en) |
EE (1) | EE03379B1 (en) |
ES (1) | ES2179175T3 (en) |
FI (1) | FI119141B (en) |
HK (1) | HK1008302A1 (en) |
HU (1) | HUP9603112A3 (en) |
IS (1) | IS1884B (en) |
MX (1) | MX9604497A (en) |
NO (1) | NO315925B1 (en) |
NZ (1) | NZ301424A (en) |
PL (1) | PL184433B1 (en) |
PT (1) | PT752851E (en) |
RU (1) | RU2170090C2 (en) |
SE (1) | SE9500478D0 (en) |
SK (1) | SK281202B6 (en) |
TR (1) | TR199600785T1 (en) |
UA (1) | UA44890C2 (en) |
WO (1) | WO1996024338A1 (en) |
ZA (1) | ZA961078B (en) |
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1995
- 1995-02-09 SE SE9500478A patent/SE9500478D0/en unknown
-
1996
- 1996-02-09 EP EP01125523A patent/EP1174136A3/en not_active Withdrawn
- 1996-02-09 JP JP52420996A patent/JP3881377B2/en not_active Expired - Lifetime
- 1996-02-09 ES ES96902579T patent/ES2179175T3/en not_active Expired - Lifetime
- 1996-02-09 EP EP96902579A patent/EP0752851B1/en not_active Expired - Lifetime
- 1996-02-09 TR TR96/00785T patent/TR199600785T1/en unknown
- 1996-02-09 EE EE9600148A patent/EE03379B1/en not_active IP Right Cessation
- 1996-02-09 ZA ZA9601078A patent/ZA961078B/en unknown
- 1996-02-09 KR KR1019960705620A patent/KR100405586B1/en not_active IP Right Cessation
- 1996-02-09 BR BR9605121A patent/BR9605121A/en not_active Application Discontinuation
- 1996-02-09 PL PL96316685A patent/PL184433B1/en not_active IP Right Cessation
- 1996-02-09 CA CA002186037A patent/CA2186037C/en not_active Expired - Lifetime
- 1996-02-09 AT AT96902579T patent/ATE218327T1/en active
- 1996-02-09 HU HU9603112A patent/HUP9603112A3/en unknown
- 1996-02-09 SK SK1261-96A patent/SK281202B6/en not_active IP Right Cessation
- 1996-02-09 UA UA96114336A patent/UA44890C2/en unknown
- 1996-02-09 DK DK96902579T patent/DK0752851T3/en active
- 1996-02-09 RU RU96120189/14A patent/RU2170090C2/en active
- 1996-02-09 WO PCT/SE1996/000161 patent/WO1996024338A1/en active IP Right Grant
- 1996-02-09 CZ CZ19962918A patent/CZ291720B6/en not_active IP Right Cessation
- 1996-02-09 DE DE69621523T patent/DE69621523T2/en not_active Expired - Lifetime
- 1996-02-09 PT PT96902579T patent/PT752851E/en unknown
- 1996-02-09 MX MX9604497A patent/MX9604497A/en unknown
- 1996-02-09 NZ NZ301424A patent/NZ301424A/en not_active IP Right Cessation
- 1996-02-09 US US08/612,951 patent/US6013281A/en not_active Expired - Fee Related
- 1996-02-09 CN CNB961900903A patent/CN1182841C/en not_active Expired - Lifetime
- 1996-09-17 IS IS4359A patent/IS1884B/en unknown
- 1996-10-08 NO NO19964271A patent/NO315925B1/en not_active IP Right Cessation
- 1996-10-08 FI FI964028A patent/FI119141B/en not_active IP Right Cessation
-
1998
- 1998-07-17 HK HK98109233A patent/HK1008302A1/en not_active IP Right Cessation
-
1999
- 1999-10-06 US US09/413,521 patent/US20020012676A1/en not_active Abandoned
-
2001
- 2001-12-18 US US10/023,968 patent/US20020086029A1/en not_active Abandoned
-
2002
- 2002-09-04 US US10/235,392 patent/US20030113375A1/en not_active Abandoned
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2003
- 2003-10-23 US US10/693,317 patent/US20040234594A1/en not_active Abandoned
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