JP2014503560A5 - - Google Patents
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- JP2014503560A5 JP2014503560A5 JP2013550556A JP2013550556A JP2014503560A5 JP 2014503560 A5 JP2014503560 A5 JP 2014503560A5 JP 2013550556 A JP2013550556 A JP 2013550556A JP 2013550556 A JP2013550556 A JP 2013550556A JP 2014503560 A5 JP2014503560 A5 JP 2014503560A5
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- Prior art keywords
- composition
- optionally substituted
- compound
- item
- pharmaceutically acceptable
- Prior art date
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- 239000000203 mixture Substances 0.000 claims description 24
- 150000001875 compounds Chemical class 0.000 claims description 22
- 125000000217 alkyl group Chemical group 0.000 claims description 15
- 150000003839 salts Chemical class 0.000 claims description 12
- 229910052739 hydrogen Inorganic materials 0.000 claims description 11
- 239000001257 hydrogen Substances 0.000 claims description 11
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 claims description 6
- 206010012601 diabetes mellitus Diseases 0.000 claims description 5
- 210000002966 serum Anatomy 0.000 claims description 5
- 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 claims description 4
- 239000008103 glucose Substances 0.000 claims description 4
- 229910052736 halogen Inorganic materials 0.000 claims description 4
- 150000002367 halogens Chemical class 0.000 claims description 4
- 208000002249 Diabetes Complications Diseases 0.000 claims description 3
- 206010012655 Diabetic complications Diseases 0.000 claims description 3
- 102000004877 Insulin Human genes 0.000 claims description 3
- 108090001061 Insulin Proteins 0.000 claims description 3
- 238000009472 formulation Methods 0.000 claims description 3
- 125000001475 halogen functional group Chemical group 0.000 claims description 3
- 229940125396 insulin Drugs 0.000 claims description 3
- 201000001320 Atherosclerosis Diseases 0.000 claims description 2
- 102000017011 Glycated Hemoglobin A Human genes 0.000 claims description 2
- 208000006011 Stroke Diseases 0.000 claims description 2
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 claims description 2
- 108091005995 glycated hemoglobin Proteins 0.000 claims description 2
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims description 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 208000010444 Acidosis Diseases 0.000 claims 1
- 206010010071 Coma Diseases 0.000 claims 1
- 208000003790 Foot Ulcer Diseases 0.000 claims 1
- 206010027417 Metabolic acidosis Diseases 0.000 claims 1
- 208000017442 Retinal disease Diseases 0.000 claims 1
- 206010038923 Retinopathy Diseases 0.000 claims 1
- 206010040943 Skin Ulcer Diseases 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 208000017169 kidney disease Diseases 0.000 claims 1
- 208000031225 myocardial ischemia Diseases 0.000 claims 1
- 208000033808 peripheral neuropathy Diseases 0.000 claims 1
- 238000013268 sustained release Methods 0.000 claims 1
- 239000012730 sustained-release form Substances 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 238000000034 method Methods 0.000 description 24
- 208000001145 Metabolic Syndrome Diseases 0.000 description 11
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 description 11
- 125000000304 alkynyl group Chemical group 0.000 description 10
- 125000004435 hydrogen atom Chemical group [H]* 0.000 description 10
- 125000001072 heteroaryl group Chemical group 0.000 description 9
- 125000003118 aryl group Chemical group 0.000 description 8
- 125000004452 carbocyclyl group Chemical group 0.000 description 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 8
- 125000000623 heterocyclic group Chemical group 0.000 description 8
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 8
- 208000035475 disorder Diseases 0.000 description 7
- 125000000739 C2-C30 alkenyl group Chemical group 0.000 description 6
- 239000000651 prodrug Substances 0.000 description 6
- 229940002612 prodrug Drugs 0.000 description 6
- 239000012453 solvate Substances 0.000 description 6
- 125000006649 (C2-C20) alkynyl group Chemical group 0.000 description 4
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 description 4
- 125000003358 C2-C20 alkenyl group Chemical group 0.000 description 4
- 125000004450 alkenylene group Chemical group 0.000 description 4
- 125000002947 alkylene group Chemical group 0.000 description 4
- 125000004419 alkynylene group Chemical group 0.000 description 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 4
- 150000003573 thiols Chemical class 0.000 description 4
- 239000008194 pharmaceutical composition Substances 0.000 description 3
- 208000032928 Dyslipidaemia Diseases 0.000 description 2
- 208000017170 Lipid metabolism disease Diseases 0.000 description 2
- 208000008589 Obesity Diseases 0.000 description 2
- -1 amino, monosubstituted amino Chemical group 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
- 125000004093 cyano group Chemical group *C#N 0.000 description 2
- 208000030159 metabolic disease Diseases 0.000 description 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 2
- 235000020824 obesity Nutrition 0.000 description 2
- 239000000546 pharmaceutical excipient Substances 0.000 description 2
- 125000006239 protecting group Chemical group 0.000 description 2
- 208000024891 symptom Diseases 0.000 description 2
- 238000007910 systemic administration Methods 0.000 description 2
- 206010012289 Dementia Diseases 0.000 description 1
- 208000004930 Fatty Liver Diseases 0.000 description 1
- 206010019708 Hepatic steatosis Diseases 0.000 description 1
- 208000035150 Hypercholesterolemia Diseases 0.000 description 1
- 206010061218 Inflammation Diseases 0.000 description 1
- 206010033307 Overweight Diseases 0.000 description 1
- 206010033645 Pancreatitis Diseases 0.000 description 1
- 208000018262 Peripheral vascular disease Diseases 0.000 description 1
- 210000001789 adipocyte Anatomy 0.000 description 1
- 208000026106 cerebrovascular disease Diseases 0.000 description 1
- 235000012000 cholesterol Nutrition 0.000 description 1
- 208000029078 coronary artery disease Diseases 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000010706 fatty liver disease Diseases 0.000 description 1
- 208000027866 inflammatory disease Diseases 0.000 description 1
- 230000004054 inflammatory process Effects 0.000 description 1
- 239000002207 metabolite Substances 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 231100000240 steatosis hepatitis Toxicity 0.000 description 1
- 230000009885 systemic effect Effects 0.000 description 1
- 150000003626 triacylglycerols Chemical class 0.000 description 1
- 208000019553 vascular disease Diseases 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161434337P | 2011-01-19 | 2011-01-19 | |
| US61/434,337 | 2011-01-19 | ||
| PCT/US2012/021692 WO2012099942A2 (en) | 2011-01-19 | 2012-01-18 | Methods and compositions for treating metabolic syndrome |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015086407A Division JP5881266B2 (ja) | 2011-01-19 | 2015-04-21 | 代謝症候群を治療する方法および組成物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014503560A JP2014503560A (ja) | 2014-02-13 |
| JP2014503560A5 true JP2014503560A5 (enExample) | 2015-03-05 |
| JP5778781B2 JP5778781B2 (ja) | 2015-09-16 |
Family
ID=46516342
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013550556A Expired - Fee Related JP5778781B2 (ja) | 2011-01-19 | 2012-01-18 | 代謝症候群を治療する方法および組成物 |
| JP2015086407A Expired - Fee Related JP5881266B2 (ja) | 2011-01-19 | 2015-04-21 | 代謝症候群を治療する方法および組成物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015086407A Expired - Fee Related JP5881266B2 (ja) | 2011-01-19 | 2015-04-21 | 代謝症候群を治療する方法および組成物 |
Country Status (6)
| Country | Link |
|---|---|
| US (3) | US9089579B2 (enExample) |
| EP (3) | EP2665481B1 (enExample) |
| JP (2) | JP5778781B2 (enExample) |
| CA (2) | CA2866067C (enExample) |
| ES (2) | ES2579990T3 (enExample) |
| WO (1) | WO2012099942A2 (enExample) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106075449A (zh) | 2005-07-14 | 2016-11-09 | 尼奥塞蒂克斯公司 | 用于局部脂肪组织治疗的持续释放的增强性脂肪分解性制剂 |
| CA2681668C (en) | 2006-03-23 | 2014-04-01 | Michael S. Singer | Compositions comprising prostaglandin f2-alpha analogs and methods for reducing body fat |
| US9132084B2 (en) | 2009-05-27 | 2015-09-15 | Neothetics, Inc. | Methods for administration and formulations for the treatment of regional adipose tissue |
| US20110124736A1 (en) | 2009-11-09 | 2011-05-26 | Allergan, Inc. | Compositions and methods for stimulating hair growth |
| CA2866067C (en) | 2011-01-19 | 2015-04-21 | Topokine Therapeutics, Inc. | Uses of certain f-series prostaglandin analogs for treating diabetes and dyslipidemia |
| US8426471B1 (en) * | 2011-12-19 | 2013-04-23 | Topokine Therapeutics, Inc. | Methods and compositions for reducing body fat and adipocytes |
| GB2507341A (en) * | 2012-10-29 | 2014-04-30 | Peter Kenny | Fat loss composition comprising a prostaglandin F2 alpha analogue and a fragment of amino acids 176-191 of human growth hormone |
| WO2014081941A1 (en) | 2012-11-21 | 2014-05-30 | Topokine Therapeutics, Inc. | Methods and compositions for locally increasing body fat |
| BR112015021859A2 (pt) * | 2013-03-15 | 2017-07-18 | Allergan Inc | bimatoprost para potencialização da produção de leptina |
| NO2753788T3 (enExample) | 2013-05-10 | 2018-06-16 | ||
| US9820993B2 (en) * | 2013-05-15 | 2017-11-21 | Topokine Therapeutics, Inc. | Methods and compositions for topical delivery of prostaglandins to subcutaneous fat |
| WO2015200425A1 (en) * | 2014-06-27 | 2015-12-30 | Topokine Therapeutics, Inc. | Topical dosage regimen |
| MA42953A (fr) | 2015-09-22 | 2018-08-01 | Graybug Vision Inc | Composés et compositions pour le traitement de troubles oculaires |
| US10285998B1 (en) | 2018-04-04 | 2019-05-14 | The Menopause Method, Inc. | Composition and method to aid in hormone replacement therapy |
| EP3845232B1 (en) * | 2018-08-30 | 2024-10-09 | Daisankasei Co., Ltd. | Transdermal use of phytostenone for reducing subcutaneous fat |
| US10835502B2 (en) | 2018-10-16 | 2020-11-17 | Polithera, Inc. | Alcohol-based compositions and uses thereof |
| US11452703B2 (en) * | 2020-05-21 | 2022-09-27 | Peregrine Ophthalmic PTE LTD. | Methods and compositions for reducing adipocyte numbers |
| WO2023065203A1 (en) * | 2021-10-21 | 2023-04-27 | Givaudan Sa | Organic compounds |
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| NO2753788T3 (enExample) | 2013-05-10 | 2018-06-16 | ||
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-
2012
- 2012-01-18 CA CA2866067A patent/CA2866067C/en not_active Expired - Fee Related
- 2012-01-18 EP EP12736090.7A patent/EP2665481B1/en not_active Not-in-force
- 2012-01-18 WO PCT/US2012/021692 patent/WO2012099942A2/en not_active Ceased
- 2012-01-18 EP EP18166647.0A patent/EP3378480A1/en not_active Withdrawn
- 2012-01-18 ES ES12736090.7T patent/ES2579990T3/es active Active
- 2012-01-18 CA CA2824317A patent/CA2824317C/en not_active Expired - Fee Related
- 2012-01-18 US US13/980,179 patent/US9089579B2/en active Active
- 2012-01-18 ES ES15180363.2T patent/ES2687494T3/es active Active
- 2012-01-18 EP EP15180363.2A patent/EP2982373B1/en not_active Not-in-force
- 2012-01-18 JP JP2013550556A patent/JP5778781B2/ja not_active Expired - Fee Related
-
2014
- 2014-10-08 US US14/509,680 patent/US9504695B2/en active Active
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2015
- 2015-04-21 JP JP2015086407A patent/JP5881266B2/ja not_active Expired - Fee Related
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2016
- 2016-11-22 US US15/359,061 patent/US10335418B2/en active Active
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