JP2012509892A5 - - Google Patents
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- JP2012509892A5 JP2012509892A5 JP2011537692A JP2011537692A JP2012509892A5 JP 2012509892 A5 JP2012509892 A5 JP 2012509892A5 JP 2011537692 A JP2011537692 A JP 2011537692A JP 2011537692 A JP2011537692 A JP 2011537692A JP 2012509892 A5 JP2012509892 A5 JP 2012509892A5
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- 239000008194 pharmaceutical composition Substances 0.000 claims 17
- 230000000580 secretagogue Effects 0.000 claims 11
- 125000000217 alkyl group Chemical group 0.000 claims 7
- 230000002124 endocrine Effects 0.000 claims 5
- 125000004404 heteroalkyl group Chemical group 0.000 claims 5
- 230000000968 intestinal Effects 0.000 claims 5
- 102100003818 GCG Human genes 0.000 claims 4
- 101710042131 GCG Proteins 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 4
- 239000003613 bile acid Substances 0.000 claims 3
- DTHNMHAUYICORS-KTKZVXAJSA-N 107444-51-9 Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(N)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC=1N=CNC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 DTHNMHAUYICORS-KTKZVXAJSA-N 0.000 claims 2
- KXGVEGMKQFWNSR-LLQZFEROSA-N Deoxycholic acid Chemical compound C([C@H]1CC2)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CCC(O)=O)C)[C@@]2(C)[C@@H](O)C1 KXGVEGMKQFWNSR-LLQZFEROSA-N 0.000 claims 2
- TWSALRJGPBVBQU-PKQQPRCHSA-N Glucagon-like peptide 2 Chemical compound C([C@@H](C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(O)=O)C(O)=O)[C@@H](C)CC)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@H](CC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)CC)C1=CC=CC=C1 TWSALRJGPBVBQU-PKQQPRCHSA-N 0.000 claims 2
- RFDAIACWWDREDC-FRVQLJSFSA-N Glycocholic acid Chemical compound C([C@H]1C[C@H]2O)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CCC(=O)NCC(O)=O)C)[C@@]2(C)[C@@H](O)C1 RFDAIACWWDREDC-FRVQLJSFSA-N 0.000 claims 2
- 102100017653 PPY Human genes 0.000 claims 2
- 102100002332 PYY Human genes 0.000 claims 2
- 108010052776 Pancreatic Polypeptide Proteins 0.000 claims 2
- 108010088847 Peptide YY Proteins 0.000 claims 2
- SSJGXNSABQPEKM-SBUIBGKBSA-N Pyy peptide Chemical compound C([C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCCCN)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(=O)NCC(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=1NC=NC=1)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(O)=O)C1=CC=C(O)C=C1 SSJGXNSABQPEKM-SBUIBGKBSA-N 0.000 claims 2
- WBWWGRHZICKQGZ-HZAMXZRMSA-N Taurocholic acid Chemical compound C([C@H]1C[C@H]2O)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CCC(=O)NCCS(O)(=O)=O)C)[C@@]2(C)[C@@H](O)C1 WBWWGRHZICKQGZ-HZAMXZRMSA-N 0.000 claims 2
- 239000003833 bile salt Substances 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 229960003964 deoxycholic acid Drugs 0.000 claims 2
- 101710038873 glc-1 Proteins 0.000 claims 2
- 230000003278 mimic Effects 0.000 claims 2
- 230000003232 mucoadhesive Effects 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 239000011780 sodium chloride Substances 0.000 claims 2
- 239000000126 substance Substances 0.000 claims 2
- AWDRATDZQPNJFN-VAYUFCLWSA-N taurodeoxycholic acid Chemical compound C([C@H]1CC2)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CCC(=O)NCCS(O)(=O)=O)C)[C@@]2(C)[C@@H](O)C1 AWDRATDZQPNJFN-VAYUFCLWSA-N 0.000 claims 2
- LNAZSHAWQACDHT-XIYTZBAFSA-N (2R,3R,4S,5R,6S)-4,5-dimethoxy-2-(methoxymethyl)-3-[(2S,3R,4S,5R,6R)-3,4,5-trimethoxy-6-(methoxymethyl)oxan-2-yl]oxy-6-[(2R,3R,4S,5R,6R)-4,5,6-trimethoxy-2-(methoxymethyl)oxan-3-yl]oxyoxane Chemical group CO[C@@H]1[C@@H](OC)[C@H](OC)[C@@H](COC)O[C@H]1O[C@H]1[C@H](OC)[C@@H](OC)[C@H](O[C@H]2[C@@H]([C@@H](OC)[C@H](OC)O[C@@H]2COC)OC)O[C@@H]1COC LNAZSHAWQACDHT-XIYTZBAFSA-N 0.000 claims 1
- MIJYXULNPSFWEK-GTOFXWBISA-N 3β-hydroxy-Olean-12-en-28-oic acid Chemical compound C1C[C@H](O)C(C)(C)[C@@H]2CC[C@@]3(C)[C@]4(C)CC[C@@]5(C(O)=O)CCC(C)(C)C[C@H]5C4=CC[C@@H]3[C@]21C MIJYXULNPSFWEK-GTOFXWBISA-N 0.000 claims 1
- BHQCQFFYRZLCQQ-UMZBRFQRSA-N 4-[(3R,5S,7R,12S)-3,7,12-trihydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoic acid Chemical class C([C@H]1C[C@H]2O)[C@H](O)CCC1(C)C1C2C2CCC(C(CCC(O)=O)C)C2(C)[C@@H](O)C1 BHQCQFFYRZLCQQ-UMZBRFQRSA-N 0.000 claims 1
- 229940093761 Bile Salts Drugs 0.000 claims 1
- 229960001091 Chenodeoxycholic Acid Drugs 0.000 claims 1
- RUDATBOHQWOJDD-BSWAIDMHSA-N Chenodeoxycholic acid Chemical compound C([C@H]1C[C@H]2O)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CCC(O)=O)C)[C@@]2(C)CC1 RUDATBOHQWOJDD-BSWAIDMHSA-N 0.000 claims 1
- 239000004380 Cholic acid Substances 0.000 claims 1
- BHQCQFFYRZLCQQ-OELDTZBJSA-N Cholic acid Chemical compound C([C@H]1C[C@H]2O)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CCC(O)=O)C)[C@@]2(C)[C@@H](O)C1 BHQCQFFYRZLCQQ-OELDTZBJSA-N 0.000 claims 1
- 210000001072 Colon Anatomy 0.000 claims 1
- 101700062901 DPP Proteins 0.000 claims 1
- 102100012353 DPP4 Human genes 0.000 claims 1
- 101700039720 DPP4 Proteins 0.000 claims 1
- 206010012601 Diabetes mellitus Diseases 0.000 claims 1
- 229940095399 Enema Drugs 0.000 claims 1
- 241000792859 Enema Species 0.000 claims 1
- 108010007979 Glycocholic Acid Proteins 0.000 claims 1
- 229940099347 Glycocholic Acid Drugs 0.000 claims 1
- 108010035713 Glycodeoxycholic Acid Proteins 0.000 claims 1
- 210000003405 Ileum Anatomy 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 229940100243 Oleanolic Acid Drugs 0.000 claims 1
- MIJYXULNPSFWEK-LXLHWSNGSA-N Oleanolic acid Natural products C1C[C@H](O)C(C)(C)[C@H]2CC[C@@]3(C)[C@]4(C)CC[C@@]5(C(O)=O)CCC(C)(C)C[C@@H]5C4=CC[C@H]3[C@]21C MIJYXULNPSFWEK-LXLHWSNGSA-N 0.000 claims 1
- 229950005134 Polycarbophil Drugs 0.000 claims 1
- 229920000148 Polycarbophil calcium Polymers 0.000 claims 1
- 229940096976 Rectal Foam Drugs 0.000 claims 1
- 229940041666 Rectal Gel Drugs 0.000 claims 1
- 210000000664 Rectum Anatomy 0.000 claims 1
- 238000010521 absorption reaction Methods 0.000 claims 1
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 150000001413 amino acids Chemical class 0.000 claims 1
- 150000001450 anions Chemical class 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- JISBOJIHFHAQPL-UHFFFAOYSA-N benzyl 6-methyl-2-oxo-4-thiophen-2-yl-3,4-dihydro-1H-pyrimidine-5-carboxylate Chemical compound N1C(=O)NC(C)=C(C(=O)OCC=2C=CC=CC=2)C1C1=CC=CS1 JISBOJIHFHAQPL-UHFFFAOYSA-N 0.000 claims 1
- 239000001768 carboxy methyl cellulose Substances 0.000 claims 1
- 150000001768 cations Chemical class 0.000 claims 1
- 229950001904 chenodiol Drugs 0.000 claims 1
- 229940099352 cholate Drugs 0.000 claims 1
- 229960002471 cholic acid Drugs 0.000 claims 1
- 235000019416 cholic acid Nutrition 0.000 claims 1
- 125000003716 cholic acid group Chemical group 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- 239000007920 enema Substances 0.000 claims 1
- 238000009472 formulation Methods 0.000 claims 1
- WVULKSPCQVQLCU-BUXLTGKBSA-N glycodeoxycholic acid Chemical compound C([C@H]1CC2)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CCC(=O)NCC(O)=O)C)[C@@]2(C)[C@@H](O)C1 WVULKSPCQVQLCU-BUXLTGKBSA-N 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 229920000609 methyl cellulose Polymers 0.000 claims 1
- 239000001923 methylcellulose Substances 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims 1
- 230000028327 secretion Effects 0.000 claims 1
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 claims 1
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 claims 1
- 239000000829 suppository Substances 0.000 claims 1
Claims (14)
- 個人における肥満症又は糖尿病の治療に使用するための、回腸、結腸及び/又は直腸への経口投与又は直腸内投与に適した医薬組成物であって、
当該医薬組成物が、胆汁酸、胆汁酸塩、胆汁酸模擬物質、胆汁酸塩模擬物質、及び、これらの組合せからなる群から選択される腸内分泌ペプチド分泌促進剤を含有し、
当該医薬組成物は体内吸収が10%wt/wt未満に調製されている、医薬組成物。 - 前記腸内分泌ペプチド分泌促進剤が、次の式(I)で表される化合物であり、
式中、
それぞれのR 1 は独立した、H、OH、低級アルキル又は低級へテロアルキルであり、
Lは、置換若しくは非置換アルキル、又は、置換若しくは非置換へテロアルキルであり、
それぞれのR 2 は独立した、H、OH、低級アルキル又は低級へテロアルキルであり、
R 3 は、H、OH、O−低級アルキル、低級アルキル又は低級へテロアルキルであり、
Aは、COOR 4 、S(O) n R 4 、又は、OR 5 であり、
ここで、R 4 は、H、アニオン、薬学的に許容可能なカチオン、置換若しくは非置換アルキル、置換若しくは非置換へテロアルキル、置換若しくは非置換アリール、置換若しくは非置換へテロアリール、又は、アミノ酸であり、
nは、1〜3であり、
R 5 は低級アルキル又はHである、
請求項1に記載の医薬組成物。 - 治療有効量のDPP−IV阻害剤を更に含有する、請求項1に記載の医薬組成物。
- 前記腸内分泌ペプチド分泌促進剤が、グルカゴン様ペプチド分泌促進剤である、
請求項1に記載の医薬組成物。 - 前記グルカゴン様ペプチド分泌促進剤が、グルカゴン様ペプチド−1(GLP−1)分泌促進剤、又は、グルカゴン様ペプチド−2(GLP−2)分泌促進剤である、
請求項4に記載の医薬組成物。 - 前記腸内分泌ペプチド分泌促進剤が、膵臓ポリペプチド折り畳みペプチド分泌促進剤である、請求項1に記載の医薬組成物。
- 前記膵臓ポリペプチド折り畳みペプチド分泌促進剤が、ペプチドYY(PYY)分泌促進剤である、請求項6に記載の医薬組成物。
- 前記胆汁酸模擬物質が、TGR−5結合類似体、6−メチル−2−オキソ−4−チオフェン−2−イル−1,2,3,4−テトラヒドロ−ピリミジン−5−カルボン酸ベンジルエステル、又は、オレアノール酸である、請求項1に記載の医薬組成物。
- 粘膜接着剤を更に含有する、請求項1に記載の医薬組成物。
- 前記粘膜接着剤が、メチルセルロース、ポリカルボフィル、ポリビニルピロリドン、カルボキシメチルセルロースナトリウム、及びこれらの組み合わせから選択される、
請求項9に記載の医薬組成物。 - 前記医薬組成物が、坐薬、浣腸溶液、直腸フォーム、直腸ゲル、又は、腸溶経口製剤として調製されている、請求項1に記載の医薬組成物。
- 前記腸内分泌ペプチド分泌促進剤が、コール酸、デオキシコール酸、グリココール酸、グリコデオキシコール酸、タウロコール酸、タウロジヒドロフシジン酸、タウロデオキシコール酸、コール酸塩、グリココール酸塩、デオキシコール酸塩、タウロコール酸塩、タウロデオキシコール酸塩、ケノデオキシコール酸もしくはその塩、又は、それらの組み合わせである、請求項1に記載の医薬組成物。
- 経口投与用の、請求項1〜12のいずれか一項に記載の医薬組成物。
- 直腸内投与用の、請求項1〜12のいずれか一項に記載の医薬組成物。
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US11832408P | 2008-11-26 | 2008-11-26 | |
US61/118,324 | 2008-11-26 | ||
US25521109P | 2009-10-27 | 2009-10-27 | |
US61/255,211 | 2009-10-27 | ||
PCT/US2009/065587 WO2010062863A2 (en) | 2008-11-26 | 2009-11-23 | Compositions containing satiogens and methods of use |
Related Child Applications (1)
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JP2014004971A Division JP2014062134A (ja) | 2008-11-26 | 2014-01-15 | サティオゲン類を含有する組成物 |
Publications (2)
Publication Number | Publication Date |
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JP2012509892A JP2012509892A (ja) | 2012-04-26 |
JP2012509892A5 true JP2012509892A5 (ja) | 2013-01-17 |
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JP2011537692A Pending JP2012509892A (ja) | 2008-11-26 | 2009-11-23 | サティオゲン類を含有する組成物及び使用の方法 |
JP2014004971A Pending JP2014062134A (ja) | 2008-11-26 | 2014-01-15 | サティオゲン類を含有する組成物 |
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JP2014004971A Pending JP2014062134A (ja) | 2008-11-26 | 2014-01-15 | サティオゲン類を含有する組成物 |
Country Status (7)
Country | Link |
---|---|
US (3) | US8318663B2 (ja) |
EP (1) | EP2364161B1 (ja) |
JP (2) | JP2012509892A (ja) |
CN (1) | CN102316889B (ja) |
CA (1) | CA2744697C (ja) |
GB (1) | GB2465677B (ja) |
WO (1) | WO2010062863A2 (ja) |
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JOP20180077A1 (ar) | 2007-06-19 | 2019-01-30 | Kythera Biopharmaceuticals Inc | تركيبات وطرق لحمض صفراوي تخليقي |
US20080318870A1 (en) | 2007-06-19 | 2008-12-25 | Kythera Biopharmaceuticals, Inc. | Synthetic bile acid compositions and methods |
US8242294B2 (en) | 2007-06-19 | 2012-08-14 | Kythera Biopharmaceuticals, Inc. | Synthetic bile acid compositions and methods |
CN102316889B (zh) | 2008-11-26 | 2014-11-26 | 萨蒂奥根制药公司 | 组合物及使用方法 |
US9339480B2 (en) * | 2008-11-26 | 2016-05-17 | Satiogen Pharmaceuticals, Inc. | Bile acid recycling inhibitors for treatment of obesity and diabetes |
US9006288B2 (en) | 2009-01-12 | 2015-04-14 | Biokier, Inc. | Composition and method for treatment of diabetes |
PL2376077T3 (pl) * | 2009-01-12 | 2017-10-31 | Biokier Inc | Kompozycja i sposób leczenia cukrzycy |
US9314444B2 (en) | 2009-01-12 | 2016-04-19 | Biokier, Inc. | Composition and method for treatment of NASH |
EP2480246A4 (en) | 2009-09-23 | 2013-02-27 | Biokier Inc | COMPOSITION AND METHOD FOR THE TREATMENT OF DIABETES |
EA201200428A1 (ru) * | 2009-10-09 | 2013-02-28 | Атеронова Оперэйшионс, Инк. | Композиция и способ для лечения ожирения |
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