JP2013536858A5 - - Google Patents
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- Publication number
- JP2013536858A5 JP2013536858A5 JP2013527262A JP2013527262A JP2013536858A5 JP 2013536858 A5 JP2013536858 A5 JP 2013536858A5 JP 2013527262 A JP2013527262 A JP 2013527262A JP 2013527262 A JP2013527262 A JP 2013527262A JP 2013536858 A5 JP2013536858 A5 JP 2013536858A5
- Authority
- JP
- Japan
- Prior art keywords
- tetrahydro
- chloro
- methyl
- benzazepine
- composition
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 150000003839 salts Chemical class 0.000 claims description 73
- 238000000034 method Methods 0.000 claims description 30
- 239000008194 pharmaceutical composition Substances 0.000 claims description 27
- 239000002552 dosage form Substances 0.000 claims description 26
- 230000037221 weight management Effects 0.000 claims description 26
- 206010033307 Overweight Diseases 0.000 claims description 15
- XTTZERNUQAFMOF-QMMMGPOBSA-N lorcaserin Chemical compound C[C@H]1CNCCC2=CC=C(Cl)C=C12 XTTZERNUQAFMOF-QMMMGPOBSA-N 0.000 claims description 14
- 235000012054 meals Nutrition 0.000 claims description 14
- 239000003814 drug Substances 0.000 claims description 12
- 235000012631 food intake Nutrition 0.000 claims description 12
- 230000004580 weight loss Effects 0.000 claims description 10
- 239000000883 anti-obesity agent Substances 0.000 claims description 8
- 229940125708 antidiabetic agent Drugs 0.000 claims description 8
- 239000003472 antidiabetic agent Substances 0.000 claims description 8
- 229940125710 antiobesity agent Drugs 0.000 claims description 8
- 238000004519 manufacturing process Methods 0.000 claims description 8
- 230000037406 food intake Effects 0.000 claims description 7
- 230000036186 satiety Effects 0.000 claims description 7
- 235000019627 satiety Nutrition 0.000 claims description 7
- 239000012453 solvate Substances 0.000 claims description 7
- 208000024172 Cardiovascular disease Diseases 0.000 claims description 5
- 208000032928 Dyslipidaemia Diseases 0.000 claims description 5
- 206010020772 Hypertension Diseases 0.000 claims description 5
- 208000017170 Lipid metabolism disease Diseases 0.000 claims description 5
- 235000003642 hunger Nutrition 0.000 claims description 5
- 150000004677 hydrates Chemical class 0.000 claims description 5
- XZWYZXLIPXDOLR-UHFFFAOYSA-N metformin Chemical group CN(C)C(=N)NC(N)=N XZWYZXLIPXDOLR-UHFFFAOYSA-N 0.000 claims description 5
- 229960003105 metformin Drugs 0.000 claims description 5
- 201000002859 sleep apnea Diseases 0.000 claims description 5
- JXPLVDIOYCZMCL-QRPNPIFTSA-N (5r)-7-chloro-5-methyl-2,3,4,5-tetrahydro-1h-3-benzazepine;2-hydroxyacetic acid Chemical compound OCC(O)=O.C[C@H]1CNCCC2=CC=C(Cl)C=C12 JXPLVDIOYCZMCL-QRPNPIFTSA-N 0.000 claims description 4
- QJTAECMTXJHPIE-QRPNPIFTSA-N (5r)-7-chloro-5-methyl-2,3,4,5-tetrahydro-1h-3-benzazepine;hexanedioic acid Chemical compound OC(=O)CCCCC(O)=O.C[C@H]1CNCCC2=CC=C(Cl)C=C12 QJTAECMTXJHPIE-QRPNPIFTSA-N 0.000 claims description 4
- LBPRUTQSXUUQDQ-QRPNPIFTSA-N (5r)-7-chloro-5-methyl-2,3,4,5-tetrahydro-1h-3-benzazepine;hydrobromide Chemical compound Br.C[C@H]1CNCCC2=CC=C(Cl)C=C12 LBPRUTQSXUUQDQ-QRPNPIFTSA-N 0.000 claims description 4
- OAKWIZZGLJXXQZ-QRPNPIFTSA-N (5r)-7-chloro-5-methyl-2,3,4,5-tetrahydro-1h-3-benzazepine;methanesulfonic acid Chemical compound CS(O)(=O)=O.C[C@H]1CNCCC2=CC=C(Cl)C=C12 OAKWIZZGLJXXQZ-QRPNPIFTSA-N 0.000 claims description 4
- BOKGRJHFZCLFOV-QRPNPIFTSA-N (5r)-7-chloro-5-methyl-2,3,4,5-tetrahydro-1h-3-benzazepine;nitric acid Chemical compound O[N+]([O-])=O.C[C@H]1CNCCC2=CC=C(Cl)C=C12 BOKGRJHFZCLFOV-QRPNPIFTSA-N 0.000 claims description 4
- PHUPWGHNZALQEV-QRPNPIFTSA-N (5r)-7-chloro-5-methyl-2,3,4,5-tetrahydro-1h-3-benzazepine;propanedioic acid Chemical compound OC(=O)CC(O)=O.C[C@H]1CNCCC2=CC=C(Cl)C=C12 PHUPWGHNZALQEV-QRPNPIFTSA-N 0.000 claims description 4
- ZEZBZHACNLTZNP-QRPNPIFTSA-N (5r)-7-chloro-5-methyl-2,3,4,5-tetrahydro-1h-3-benzazepine;sulfuric acid Chemical compound OS(O)(=O)=O.C[C@H]1CNCCC2=CC=C(Cl)C=C12 ZEZBZHACNLTZNP-QRPNPIFTSA-N 0.000 claims description 4
- 239000003937 drug carrier Substances 0.000 claims description 4
- 241001465754 Metazoa Species 0.000 claims description 3
- 235000005911 diet Nutrition 0.000 claims description 3
- 238000002560 therapeutic procedure Methods 0.000 claims description 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 3
- 230000000378 dietary effect Effects 0.000 claims description 2
- 235000015872 dietary supplement Nutrition 0.000 claims description 2
- VCSZKSHWUBFOOE-UHFFFAOYSA-N dioxidanium;sulfate Chemical compound O.O.OS(O)(=O)=O VCSZKSHWUBFOOE-UHFFFAOYSA-N 0.000 claims description 2
- WRZCAWKMTLRWPR-VSODYHHCSA-N lorcaserin hydrochloride hemihydrate Chemical compound O.Cl.Cl.C[C@H]1CNCCC2=CC=C(Cl)C=C12.C[C@H]1CNCCC2=CC=C(Cl)C=C12 WRZCAWKMTLRWPR-VSODYHHCSA-N 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 24
- 208000002705 Glucose Intolerance Diseases 0.000 claims 2
- 208000008589 Obesity Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 230000001939 inductive effect Effects 0.000 claims 2
- 235000020824 obesity Nutrition 0.000 claims 2
- 201000009104 prediabetes syndrome Diseases 0.000 claims 2
- 102000005962 receptors Human genes 0.000 claims 2
- 108020003175 receptors Proteins 0.000 claims 2
- OFOBLEOULBTSOW-UHFFFAOYSA-L Malonate Chemical compound [O-]C(=O)CC([O-])=O OFOBLEOULBTSOW-UHFFFAOYSA-L 0.000 claims 1
- 239000013078 crystal Substances 0.000 claims 1
- 235000013305 food Nutrition 0.000 claims 1
- 238000012423 maintenance Methods 0.000 claims 1
- 238000007726 management method Methods 0.000 claims 1
- 239000000047 product Substances 0.000 claims 1
- 238000000634 powder X-ray diffraction Methods 0.000 description 10
- DHHVAGZRUROJKS-UHFFFAOYSA-N phentermine Chemical compound CC(C)(N)CC1=CC=CC=C1 DHHVAGZRUROJKS-UHFFFAOYSA-N 0.000 description 6
- ZCKAMNXUHHNZLN-UHFFFAOYSA-N Chlorphentermine Chemical group CC(C)(N)CC1=CC=C(Cl)C=C1 ZCKAMNXUHHNZLN-UHFFFAOYSA-N 0.000 description 3
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 3
- 230000037396 body weight Effects 0.000 description 3
- 229950007046 chlorphentermine Drugs 0.000 description 3
- HXCXASJHZQXCKK-UHFFFAOYSA-N clortermine Chemical compound CC(C)(N)CC1=CC=CC=C1Cl HXCXASJHZQXCKK-UHFFFAOYSA-N 0.000 description 3
- 229950000649 clortermine Drugs 0.000 description 3
- 230000007423 decrease Effects 0.000 description 3
- 239000008103 glucose Substances 0.000 description 3
- UMWAUEZOGHNSCH-UHFFFAOYSA-N pentorex Chemical compound CC(N)(C)C(C)C1=CC=CC=C1 UMWAUEZOGHNSCH-UHFFFAOYSA-N 0.000 description 3
- 229950000821 pentorex Drugs 0.000 description 3
- 229960003562 phentermine Drugs 0.000 description 3
- 230000037213 diet Effects 0.000 description 1
- 239000013589 supplement Substances 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US40258910P | 2010-09-01 | 2010-09-01 | |
| US61/402,589 | 2010-09-01 | ||
| PCT/US2011/049953 WO2012030951A1 (en) | 2010-09-01 | 2011-08-31 | Fast-dissolve dosage forms of 5-ht2c agonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2013536858A JP2013536858A (ja) | 2013-09-26 |
| JP2013536858A5 true JP2013536858A5 (enExample) | 2014-10-16 |
Family
ID=44645827
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013527262A Pending JP2013536858A (ja) | 2010-09-01 | 2011-08-31 | ５−ｈｔ２ｃアゴニストの速く溶解する剤形 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20140148442A1 (enExample) |
| EP (1) | EP2611781A1 (enExample) |
| JP (1) | JP2013536858A (enExample) |
| KR (1) | KR20130138768A (enExample) |
| CN (1) | CN103189358A (enExample) |
| AU (1) | AU2011296027A1 (enExample) |
| CA (1) | CA2808900A1 (enExample) |
| IN (1) | IN2013DN02552A (enExample) |
| MX (1) | MX2013002430A (enExample) |
| SG (2) | SG188363A1 (enExample) |
| WO (1) | WO2012030951A1 (enExample) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2013539470A (ja) | 2010-09-01 | 2013-10-24 | アリーナ ファーマシューティカルズ， インコーポレイテッド | ロルカセリンと光学活性な酸との塩 |
| KR20130101524A (ko) | 2010-09-01 | 2013-09-13 | 아레나 파마슈티칼스, 인크. | 5-ｈｔ2ｃ 아고니스트의 비-흡습성 염 |
| EA201390335A1 (ru) | 2010-09-01 | 2013-09-30 | Арена Фармасьютикалз, Инк. | Введение лоркасерина индивидуумам с почечной недостаточностью |
| KR20180118801A (ko) | 2010-09-01 | 2018-10-31 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 체중 관리에 유용한 5-ｈｔ2ｃ 작동제의 변형-방출 투여 형태 |
| RU2674670C1 (ru) | 2012-10-09 | 2018-12-12 | Арена Фармасьютикалз, Инк. | Способ коррекции массы тела |
| WO2014135545A1 (en) * | 2013-03-05 | 2014-09-12 | Sandoz Ag | Solid dispersion comprising amorphous lorcaserin hydrochloride |
| WO2014187768A1 (en) * | 2013-05-20 | 2014-11-27 | Lek Pharmaceuticals D.D. | Novel synthetic processes to 8-chloro-3-benzo[d]azepine via friedel-crafts alkylation of olefin |
| EP2868656A1 (en) * | 2013-11-05 | 2015-05-06 | LEK Pharmaceuticals d.d. | Stabilized amorphous lorcaserin hydrochloride |
| CN104936947B (zh) * | 2013-12-27 | 2017-03-08 | 杭州普晒医药科技有限公司 | 氯卡色林盐及其晶体、其制备方法和用途 |
| US9981912B2 (en) | 2014-04-21 | 2018-05-29 | Hangzhou Pushai Pharmaceutical Technology Co., Ltd. | Cocrystal of lorcaserin, preparation methods, pharmaceutical compositions and uses thereof |
| CN103901151A (zh) * | 2014-04-23 | 2014-07-02 | 湖北朗昕生化药业有限公司 | 一种hplc法检测氯卡色林盐酸盐含量的方法 |
| TW201618787A (zh) | 2014-10-30 | 2016-06-01 | 艾尼納製藥公司 | 組合物及方法 |
| CA3010636A1 (en) | 2016-06-29 | 2018-01-04 | CannScience Innovations Inc. | Decarboxylated cannabis resins, uses thereof and methods of making same |
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| FR2561916B1 (fr) | 1984-03-30 | 1987-12-11 | Lafon Labor | Forme galenique pour administration orale et son procede de preparation par lyophilisation d'une emission huile dans eau |
| US4642903A (en) | 1985-03-26 | 1987-02-17 | R. P. Scherer Corporation | Freeze-dried foam dosage form |
| US5073374A (en) | 1988-11-30 | 1991-12-17 | Schering Corporation | Fast dissolving buccal tablet |
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| US5219574A (en) | 1989-09-15 | 1993-06-15 | Cima Labs. Inc. | Magnesium carbonate and oil tableting aid and flavoring additive |
| US5223264A (en) | 1989-10-02 | 1993-06-29 | Cima Labs, Inc. | Pediatric effervescent dosage form |
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| WO1993000094A2 (en) * | 1991-06-21 | 1993-01-07 | Smithkline Beecham Plc | Use of tetrahydrobenzazepine derivatives for the treatment of portal hypertension and migraine |
| US5464632C1 (en) | 1991-07-22 | 2001-02-20 | Prographarm Lab | Rapidly disintegratable multiparticular tablet |
| JP3069458B2 (ja) | 1992-01-29 | 2000-07-24 | 武田薬品工業株式会社 | 口腔内崩壊型錠剤およびその製造法 |
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-
2011
- 2011-08-31 KR KR1020137008322A patent/KR20130138768A/ko not_active Withdrawn
- 2011-08-31 JP JP2013527262A patent/JP2013536858A/ja active Pending
- 2011-08-31 MX MX2013002430A patent/MX2013002430A/es not_active Application Discontinuation
- 2011-08-31 CN CN201180052517XA patent/CN103189358A/zh active Pending
- 2011-08-31 CA CA2808900A patent/CA2808900A1/en not_active Abandoned
- 2011-08-31 AU AU2011296027A patent/AU2011296027A1/en not_active Abandoned
- 2011-08-31 SG SG2013015607A patent/SG188363A1/en unknown
- 2011-08-31 EP EP11755511.0A patent/EP2611781A1/en not_active Withdrawn
- 2011-08-31 IN IN2552DEN2013 patent/IN2013DN02552A/en unknown
- 2011-08-31 US US13/820,123 patent/US20140148442A1/en not_active Abandoned
- 2011-08-31 SG SG10201506873WA patent/SG10201506873WA/en unknown
- 2011-08-31 WO PCT/US2011/049953 patent/WO2012030951A1/en not_active Ceased
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