JP2016520561A5 - - Google Patents
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- Publication number
- JP2016520561A5 JP2016520561A5 JP2016507645A JP2016507645A JP2016520561A5 JP 2016520561 A5 JP2016520561 A5 JP 2016520561A5 JP 2016507645 A JP2016507645 A JP 2016507645A JP 2016507645 A JP2016507645 A JP 2016507645A JP 2016520561 A5 JP2016520561 A5 JP 2016520561A5
- Authority
- JP
- Japan
- Prior art keywords
- fat
- compound
- pharmaceutical composition
- release formulation
- sustained
- 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
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- 239000000203 mixture Substances 0.000 claims description 41
- 238000013268 sustained release Methods 0.000 claims description 24
- 239000012730 sustained-release form Substances 0.000 claims description 24
- 238000009472 formulation Methods 0.000 claims description 22
- 239000007943 implant Substances 0.000 claims description 22
- LLKFNPUXQZHIAE-UHFFFAOYSA-N 5-(3-aminopropyl)-8-bromo-3-methyl-2h-pyrazolo[4,3-c]quinolin-4-one Chemical compound O=C1N(CCCN)C2=CC=C(Br)C=C2C2=C1C(C)=NN2 LLKFNPUXQZHIAE-UHFFFAOYSA-N 0.000 claims description 13
- 238000002347 injection Methods 0.000 claims description 12
- 239000007924 injection Substances 0.000 claims description 12
- 239000002904 solvent Substances 0.000 claims description 10
- 150000001875 compounds Chemical class 0.000 claims description 7
- 239000004005 microsphere Substances 0.000 claims description 7
- KIUKXJAPPMFGSW-DNGZLQJQSA-N (2S,3S,4S,5R,6R)-6-[(2S,3R,4R,5S,6R)-3-Acetamido-2-[(2S,3S,4R,5R,6R)-6-[(2R,3R,4R,5S,6R)-3-acetamido-2,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-2-carboxy-4,5-dihydroxyoxan-3-yl]oxy-5-hydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,4,5-trihydroxyoxane-2-carboxylic acid Chemical compound CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O[C@H]3[C@@H]([C@@H](O)[C@H](O)[C@H](O3)C(O)=O)O)[C@H](O)[C@@H](CO)O2)NC(C)=O)[C@@H](C(O)=O)O1 KIUKXJAPPMFGSW-DNGZLQJQSA-N 0.000 claims description 6
- 229920002674 hyaluronan Polymers 0.000 claims description 6
- 229960003160 hyaluronic acid Drugs 0.000 claims description 6
- 239000000725 suspension Substances 0.000 claims description 5
- 210000001596 intra-abdominal fat Anatomy 0.000 claims description 3
- 210000004003 subcutaneous fat Anatomy 0.000 claims description 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 14
- 210000000579 abdominal fat Anatomy 0.000 claims 2
- BXWNKGSJHAJOGX-UHFFFAOYSA-N hexadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCO BXWNKGSJHAJOGX-UHFFFAOYSA-N 0.000 claims 2
- 206010003694 Atrophy Diseases 0.000 claims 1
- 210000001789 adipocyte Anatomy 0.000 claims 1
- 230000037444 atrophy Effects 0.000 claims 1
- 230000003796 beauty Effects 0.000 claims 1
- 210000001593 brown adipocyte Anatomy 0.000 claims 1
- 230000002459 sustained effect Effects 0.000 claims 1
- 230000000699 topical effect Effects 0.000 claims 1
- 210000000636 white adipocyte Anatomy 0.000 claims 1
- AQOKCDNYWBIDND-FTOWTWDKSA-N bimatoprost Chemical compound CCNC(=O)CCC\C=C/C[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1\C=C\[C@@H](O)CCC1=CC=CC=C1 AQOKCDNYWBIDND-FTOWTWDKSA-N 0.000 description 27
- 229960002470 bimatoprost Drugs 0.000 description 26
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 10
- 239000000499 gel Substances 0.000 description 9
- 229920000642 polymer Polymers 0.000 description 8
- 229940079593 drug Drugs 0.000 description 6
- 239000003814 drug Substances 0.000 description 6
- 229910052688 Gadolinium Inorganic materials 0.000 description 5
- SECXISVLQFMRJM-UHFFFAOYSA-N N-Methylpyrrolidone Chemical compound CN1CCCC1=O SECXISVLQFMRJM-UHFFFAOYSA-N 0.000 description 5
- 150000003180 prostaglandins Chemical class 0.000 description 5
- 210000003205 muscle Anatomy 0.000 description 4
- 239000007787 solid Substances 0.000 description 4
- FXHOOIRPVKKKFG-UHFFFAOYSA-N N,N-Dimethylacetamide Chemical compound CN(C)C(C)=O FXHOOIRPVKKKFG-UHFFFAOYSA-N 0.000 description 3
- 238000000034 method Methods 0.000 description 3
- 229920001606 poly(lactic acid-co-glycolic acid) Polymers 0.000 description 3
- 239000000243 solution Substances 0.000 description 3
- LZDKZFUFMNSQCJ-UHFFFAOYSA-N 1,2-diethoxyethane Chemical compound CCOCCOCC LZDKZFUFMNSQCJ-UHFFFAOYSA-N 0.000 description 2
- 102000008186 Collagen Human genes 0.000 description 2
- 108010035532 Collagen Proteins 0.000 description 2
- 108010010803 Gelatin Proteins 0.000 description 2
- ALNHYDLSRWZMHE-MJNWZANWSA-N NC(CCC/C=C\C[C@@H]([C@H](C[C@H]1O)O)[C@H]1/C=C/[C@H](CCc(cc([s]1)Cl)c1Cl)O)=O Chemical compound NC(CCC/C=C\C[C@@H]([C@H](C[C@H]1O)O)[C@H]1/C=C/[C@H](CCc(cc([s]1)Cl)c1Cl)O)=O ALNHYDLSRWZMHE-MJNWZANWSA-N 0.000 description 2
- 210000000577 adipose tissue Anatomy 0.000 description 2
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 description 2
- 229920001436 collagen Polymers 0.000 description 2
- 239000008273 gelatin Substances 0.000 description 2
- 229920000159 gelatin Polymers 0.000 description 2
- 235000019322 gelatine Nutrition 0.000 description 2
- 235000011852 gelatine desserts Nutrition 0.000 description 2
- 238000000338 in vitro Methods 0.000 description 2
- 238000011065 in-situ storage Methods 0.000 description 2
- 230000003993 interaction Effects 0.000 description 2
- 229960001160 latanoprost Drugs 0.000 description 2
- GGXICVAJURFBLW-CEYXHVGTSA-N latanoprost Chemical compound CC(C)OC(=O)CCC\C=C/C[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1CC[C@@H](O)CCC1=CC=CC=C1 GGXICVAJURFBLW-CEYXHVGTSA-N 0.000 description 2
- 229940094443 oxytocics prostaglandins Drugs 0.000 description 2
- 239000000546 pharmaceutical excipient Substances 0.000 description 2
- 229920001610 polycaprolactone Polymers 0.000 description 2
- 229920001223 polyethylene glycol Polymers 0.000 description 2
- 238000002360 preparation method Methods 0.000 description 2
- 210000002027 skeletal muscle Anatomy 0.000 description 2
- 230000007704 transition Effects 0.000 description 2
- SQDAZGGFXASXDW-UHFFFAOYSA-N 5-bromo-2-(trifluoromethoxy)pyridine Chemical compound FC(F)(F)OC1=CC=C(Br)C=N1 SQDAZGGFXASXDW-UHFFFAOYSA-N 0.000 description 1
- 229920001287 Chondroitin sulfate Polymers 0.000 description 1
- 229920001244 Poly(D,L-lactide) Polymers 0.000 description 1
- 229920002562 Polyethylene Glycol 3350 Polymers 0.000 description 1
- 229920001710 Polyorthoester Polymers 0.000 description 1
- 229920002385 Sodium hyaluronate Polymers 0.000 description 1
- 238000005411 Van der Waals force Methods 0.000 description 1
- 239000013543 active substance Substances 0.000 description 1
- 229940006138 antiglaucoma drug and miotics prostaglandin analogues Drugs 0.000 description 1
- 239000003125 aqueous solvent Substances 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 235000012000 cholesterol Nutrition 0.000 description 1
- 229940059329 chondroitin sulfate Drugs 0.000 description 1
- 239000006184 cosolvent Substances 0.000 description 1
- 238000009792 diffusion process Methods 0.000 description 1
- 238000012377 drug delivery Methods 0.000 description 1
- 210000002468 fat body Anatomy 0.000 description 1
- 150000002191 fatty alcohols Chemical class 0.000 description 1
- 150000004676 glycans Chemical class 0.000 description 1
- 229910052739 hydrogen Inorganic materials 0.000 description 1
- 239000001257 hydrogen Substances 0.000 description 1
- 230000002209 hydrophobic effect Effects 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- WFKAJVHLWXSISD-UHFFFAOYSA-N isobutyramide Chemical compound CC(C)C(N)=O WFKAJVHLWXSISD-UHFFFAOYSA-N 0.000 description 1
- -1 latexes Polymers 0.000 description 1
- 238000002844 melting Methods 0.000 description 1
- 230000008018 melting Effects 0.000 description 1
- 229920005615 natural polymer Polymers 0.000 description 1
- 230000002085 persistent effect Effects 0.000 description 1
- 150000003014 phosphoric acid esters Chemical class 0.000 description 1
- 229920000117 poly(dioxanone) Polymers 0.000 description 1
- 229920000728 polyester Polymers 0.000 description 1
- 229920002959 polymer blend Polymers 0.000 description 1
- 229920001282 polysaccharide Polymers 0.000 description 1
- 239000005017 polysaccharide Substances 0.000 description 1
- 229920001296 polysiloxane Polymers 0.000 description 1
- 229940002612 prodrug Drugs 0.000 description 1
- 239000000651 prodrug Substances 0.000 description 1
- 235000021391 short chain fatty acids Nutrition 0.000 description 1
- 150000004666 short chain fatty acids Chemical class 0.000 description 1
- 229940010747 sodium hyaluronate Drugs 0.000 description 1
- YWIVKILSMZOHHF-QJZPQSOGSA-N sodium;(2s,3s,4s,5r,6r)-6-[(2s,3r,4r,5s,6r)-3-acetamido-2-[(2s,3s,4r,5r,6r)-6-[(2r,3r,4r,5s,6r)-3-acetamido-2,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-2-carboxy-4,5-dihydroxyoxan-3-yl]oxy-5-hydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,4,5-trihydroxyoxane-2- Chemical compound [Na+].CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O[C@H]3[C@@H]([C@@H](O)[C@H](O)[C@H](O3)C(O)=O)O)[C@H](O)[C@@H](CO)O2)NC(C)=O)[C@@H](C(O)=O)O1 YWIVKILSMZOHHF-QJZPQSOGSA-N 0.000 description 1
- 230000001954 sterilising effect Effects 0.000 description 1
- 238000004659 sterilization and disinfection Methods 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 239000001993 wax Substances 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361811682P | 2013-04-12 | 2013-04-12 | |
| US61/811,682 | 2013-04-12 | ||
| PCT/US2014/033558 WO2014169075A1 (en) | 2013-04-12 | 2014-04-09 | Sustained release of bimatoprost, bimatoprost analogs, prostamides and prostaglandins for fat reduction |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2016520561A JP2016520561A (ja) | 2016-07-14 |
| JP2016520561A5 true JP2016520561A5 (https=) | 2017-06-15 |
Family
ID=51686960
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016507645A Pending JP2016520561A (ja) | 2013-04-12 | 2014-04-09 | 脂肪減少のためのビマトプロスト、ビマトプロスト類似体、プロスタミド及びプロスタグランジンの持続放出 |
Country Status (18)
| Country | Link |
|---|---|
| US (2) | US20140308354A1 (https=) |
| EP (2) | EP3656375A1 (https=) |
| JP (1) | JP2016520561A (https=) |
| KR (1) | KR20150141972A (https=) |
| CN (2) | CN110840899A (https=) |
| AU (2) | AU2014250937A1 (https=) |
| BR (1) | BR112015025915A8 (https=) |
| CA (1) | CA2908731A1 (https=) |
| CL (1) | CL2015003023A1 (https=) |
| DK (1) | DK2983663T3 (https=) |
| ES (1) | ES2785382T3 (https=) |
| IL (1) | IL242006B (https=) |
| MX (1) | MX381097B (https=) |
| MY (1) | MY187802A (https=) |
| RU (1) | RU2015143859A (https=) |
| SG (2) | SG10201701938PA (https=) |
| WO (1) | WO2014169075A1 (https=) |
| ZA (1) | ZA201507217B (https=) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX385254B (es) * | 2015-04-30 | 2025-03-14 | Allergan Inc | Uso de analogos de bimatoprost para el tratamiento de la reduccion de grasa corporal en un sujeto. |
| US11452703B2 (en) * | 2020-05-21 | 2022-09-27 | Peregrine Ophthalmic PTE LTD. | Methods and compositions for reducing adipocyte numbers |
| TW202216159A (zh) * | 2020-07-21 | 2022-05-01 | 美商歐樂根公司 | 具高負載前列腺素醯胺之眼內植入物 |
| WO2024218609A1 (en) * | 2023-04-18 | 2024-10-24 | Welfare Concepts Limited | Composition and method for inducing luteolysis |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2218424A (en) * | 1931-05-07 | 1940-10-15 | Teleregister Corp | Transmitter and code translator |
| US4525359A (en) * | 1982-12-10 | 1985-06-25 | Greenway Frank L Iii | Treatment for selective weight control |
| US6124344A (en) | 1993-12-28 | 2000-09-26 | Allergan Sales, Inc. | Cyclopentane heptan(ene)oic acid, 2-heteroarylalkenyl derivatives as therapeutic agents |
| CA2221110C (en) * | 1995-05-18 | 2009-08-04 | Allergan | Cyclopentane heptan(ene)oic acid, 2-heteroarylalkenyl derivatives as therapeutic agents for the treatment of ocular hypertension |
| DK1562604T3 (da) | 2002-10-23 | 2012-04-02 | Sucampo Ag | Prostaglandinforbindelser til behandling af fedme |
| CN100453066C (zh) * | 2002-12-04 | 2009-01-21 | 参天制药株式会社 | 利用结膜下储存库的药物释放系统 |
| EP1699432A2 (en) * | 2003-12-22 | 2006-09-13 | Aventis Pharmaceuticals, Inc. | Injectable phosphatidylcholine preparations |
| US20080038316A1 (en) | 2004-10-01 | 2008-02-14 | Wong Vernon G | Conveniently implantable sustained release drug compositions |
| WO2007111806A2 (en) * | 2006-03-23 | 2007-10-04 | Massachusetts Eye And Ear Infirmary | Cyclopentane heptanoic acid compounds for reducing body fat |
| JP2010506941A (ja) * | 2006-10-17 | 2010-03-04 | リセラ，インク． | 甲状腺眼症の治療のための方法、組成物及び製剤 |
| US8969415B2 (en) * | 2006-12-01 | 2015-03-03 | Allergan, Inc. | Intraocular drug delivery systems |
| US9095506B2 (en) * | 2008-11-17 | 2015-08-04 | Allergan, Inc. | Biodegradable alpha-2 agonist polymeric implants and therapeutic uses thereof |
| US20100247606A1 (en) * | 2009-03-25 | 2010-09-30 | Allergan, Inc. | Intraocular sustained release drug delivery systems and methods for treating ocular conditions |
| WO2011109384A2 (en) * | 2010-03-02 | 2011-09-09 | Allergan, Inc. | Biodegradable polymers for lowering intraocular pressure |
| WO2012012546A2 (en) | 2010-07-21 | 2012-01-26 | Allergan, Inc. | METHOD OF CONTROLLING INITIAL DRUG RELEASE OF siRNA FROM SUSTAINED-RELEASE IMPLANTS |
| WO2014143754A2 (en) * | 2013-03-15 | 2014-09-18 | Allergan, Inc. | Prostamide-containing intraocular implant |
| MX385254B (es) | 2015-04-30 | 2025-03-14 | Allergan Inc | Uso de analogos de bimatoprost para el tratamiento de la reduccion de grasa corporal en un sujeto. |
-
2014
- 2014-04-09 CA CA2908731A patent/CA2908731A1/en not_active Abandoned
- 2014-04-09 SG SG10201701938PA patent/SG10201701938PA/en unknown
- 2014-04-09 CN CN201910977574.7A patent/CN110840899A/zh active Pending
- 2014-04-09 DK DK14725582.2T patent/DK2983663T3/da active
- 2014-04-09 MY MYPI2015002531A patent/MY187802A/en unknown
- 2014-04-09 JP JP2016507645A patent/JP2016520561A/ja active Pending
- 2014-04-09 EP EP20152147.3A patent/EP3656375A1/en not_active Withdrawn
- 2014-04-09 ES ES14725582T patent/ES2785382T3/es active Active
- 2014-04-09 US US14/248,898 patent/US20140308354A1/en not_active Abandoned
- 2014-04-09 BR BR112015025915A patent/BR112015025915A8/pt active Search and Examination
- 2014-04-09 EP EP14725582.2A patent/EP2983663B1/en active Active
- 2014-04-09 AU AU2014250937A patent/AU2014250937A1/en not_active Abandoned
- 2014-04-09 MX MX2015014320A patent/MX381097B/es unknown
- 2014-04-09 CN CN201480020790.8A patent/CN105101962A/zh active Pending
- 2014-04-09 SG SG10202109919P patent/SG10202109919PA/en unknown
- 2014-04-09 RU RU2015143859A patent/RU2015143859A/ru not_active Application Discontinuation
- 2014-04-09 KR KR1020157029970A patent/KR20150141972A/ko not_active Ceased
- 2014-04-09 WO PCT/US2014/033558 patent/WO2014169075A1/en not_active Ceased
-
2015
- 2015-09-29 ZA ZA2015/07217A patent/ZA201507217B/en unknown
- 2015-10-09 CL CL2015003023A patent/CL2015003023A1/es unknown
- 2015-10-11 IL IL242006A patent/IL242006B/en active IP Right Grant
-
2016
- 2016-04-21 US US15/134,792 patent/US10682361B2/en active Active
-
2019
- 2019-05-08 AU AU2019203214A patent/AU2019203214B2/en not_active Ceased
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