JP2017527550A5 - - Google Patents
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- JP2017527550A5 JP2017527550A5 JP2017508482A JP2017508482A JP2017527550A5 JP 2017527550 A5 JP2017527550 A5 JP 2017527550A5 JP 2017508482 A JP2017508482 A JP 2017508482A JP 2017508482 A JP2017508482 A JP 2017508482A JP 2017527550 A5 JP2017527550 A5 JP 2017527550A5
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- JP
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- Prior art keywords
- autotaxin inhibitor
- inhibitor according
- individual
- autotaxin
- inhibitors
- 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.)
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- 239000003112 inhibitor Substances 0.000 claims 24
- 230000002401 inhibitory effect Effects 0.000 claims 24
- 102100016621 ENPP2 Human genes 0.000 claims 20
- 101700057276 ENPP2 Proteins 0.000 claims 20
- 239000003814 drug Substances 0.000 claims 9
- 210000004369 Blood Anatomy 0.000 claims 6
- WQZGKKKJIJFFOK-GASJEMHNSA-N D-Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims 6
- 239000008280 blood Substances 0.000 claims 6
- 229940079593 drugs Drugs 0.000 claims 6
- 239000008103 glucose Substances 0.000 claims 6
- 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 6
- HVYWMOMLDIMFJA-DPAQBDIFSA-N (3β)-Cholest-5-en-3-ol 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 claims 4
- 102000004877 Insulin Human genes 0.000 claims 3
- 108090001061 Insulin Proteins 0.000 claims 3
- 229920000023 polynucleotide Polymers 0.000 claims 3
- 239000002157 polynucleotide Substances 0.000 claims 3
- 150000003384 small molecules Chemical class 0.000 claims 3
- WRGQSWVCFNIUNZ-GDCKJWNLSA-N 1-oleoyl-sn-glycerol 3-phosphate Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OC[C@@H](O)COP(O)(O)=O WRGQSWVCFNIUNZ-GDCKJWNLSA-N 0.000 claims 2
- 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
- 229940107161 Cholesterol Drugs 0.000 claims 2
- 206010012601 Diabetes mellitus Diseases 0.000 claims 2
- 206010020772 Hypertension Diseases 0.000 claims 2
- 208000008338 Non-alcoholic Fatty Liver Disease Diseases 0.000 claims 2
- 108009000135 Nonalcoholic fatty liver disease Proteins 0.000 claims 2
- 102000004270 Peptidyl-Dipeptidase A Human genes 0.000 claims 2
- 108090000882 Peptidyl-Dipeptidase A Proteins 0.000 claims 2
- 102000003728 Peroxisome Proliferator-Activated Receptors Human genes 0.000 claims 2
- 108090000029 Peroxisome Proliferator-Activated Receptors Proteins 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 150000003626 triacylglycerols Chemical class 0.000 claims 2
- 208000004611 Abdominal Obesity Diseases 0.000 claims 1
- 241001553178 Arachis glabrata Species 0.000 claims 1
- 229940030609 CALCIUM CHANNEL BLOCKERS Drugs 0.000 claims 1
- 208000008787 Cardiovascular Disease Diseases 0.000 claims 1
- 206010065941 Central obesity Diseases 0.000 claims 1
- 229940030606 DIURETICS Drugs 0.000 claims 1
- 102100003818 GCG Human genes 0.000 claims 1
- 101710042131 GCG Proteins 0.000 claims 1
- 208000004104 Gestational Diabetes Diseases 0.000 claims 1
- 206010018429 Glucose tolerance impaired Diseases 0.000 claims 1
- SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Natural products C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 claims 1
- 206010022489 Insulin resistance Diseases 0.000 claims 1
- 102000036849 Islet amyloid polypeptide Human genes 0.000 claims 1
- 108010041872 Islet amyloid polypeptide Proteins 0.000 claims 1
- 206010025650 Malignant melanoma Diseases 0.000 claims 1
- 208000008466 Metabolic Disease Diseases 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 206010053219 Non-alcoholic steatohepatitis Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 102000035443 Peptidases Human genes 0.000 claims 1
- 108091005771 Peptidases Proteins 0.000 claims 1
- 210000002381 Plasma Anatomy 0.000 claims 1
- 210000002966 Serum Anatomy 0.000 claims 1
- 102000000070 Sodium-Glucose Transport Proteins Human genes 0.000 claims 1
- 108010080361 Sodium-Glucose Transport Proteins Proteins 0.000 claims 1
- 229940090121 Sulfonylureas for blood glucose lowering Drugs 0.000 claims 1
- 208000001072 Type 2 Diabetes Mellitus Diseases 0.000 claims 1
- 239000000556 agonist Substances 0.000 claims 1
- 239000003888 alpha glucosidase inhibitor Substances 0.000 claims 1
- 239000002333 angiotensin II receptor antagonist Substances 0.000 claims 1
- 230000001396 anti-anti-diuretic Effects 0.000 claims 1
- 230000000692 anti-sense Effects 0.000 claims 1
- 102000004965 antibodies Human genes 0.000 claims 1
- 108090001123 antibodies Proteins 0.000 claims 1
- 239000002876 beta blocker Substances 0.000 claims 1
- 229940058933 biguanide antimalarials Drugs 0.000 claims 1
- 229940090145 biguanide blood glucose lower drugs Drugs 0.000 claims 1
- 150000004283 biguanides Chemical class 0.000 claims 1
- 229940090127 blood glucose lowering Alpha glucosidase inhibitors Drugs 0.000 claims 1
- 229940090129 blood glucose lowering drugs Thiazolidinediones Drugs 0.000 claims 1
- 239000000480 calcium channel blocker Substances 0.000 claims 1
- 230000001112 coagulant Effects 0.000 claims 1
- 239000000701 coagulant Substances 0.000 claims 1
- 239000002934 diuretic Substances 0.000 claims 1
- 230000004064 dysfunction Effects 0.000 claims 1
- 235000020828 fasting Nutrition 0.000 claims 1
- 125000001041 indolyl group Chemical group 0.000 claims 1
- 230000002452 interceptive Effects 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 239000000816 peptidomimetic Substances 0.000 claims 1
- 201000010065 polycystic ovary syndrome Diseases 0.000 claims 1
- 229920001184 polypeptide Polymers 0.000 claims 1
- 235000019833 protease Nutrition 0.000 claims 1
- 102000004169 proteins and genes Human genes 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
- 230000036454 renin-angiotensin system Effects 0.000 claims 1
- 230000000580 secretagogue Effects 0.000 claims 1
- 150000001467 thiazolidinediones Chemical class 0.000 claims 1
- 238000005303 weighing Methods 0.000 claims 1
Claims (15)
- 代謝障害の個体の血糖値を下げるのに使用するためのオートタキシン阻害剤。
- 個体における血糖値は前記オートタキシン阻害剤の投与後に少なくとも１０％下がる、請求項１に記載のオートタキシン阻害剤。
- 前記個体における血中のリゾホスファチジン酸（ＬＰＡ）レベルは、前記オートタキシン阻害剤の投与後に少なくとも２０％下がる、請求項１に記載のオートタキシン阻害剤。
- オートタキシン阻害剤は、タンパク質薬、ペプチド薬、ポリペプチド薬、ペプチド模倣薬、抗体薬、小分子薬、低分子干渉ＲＮＡコード化ポリヌクレオチド、アンチセンスＲＮＡコード化ポリヌクレオチド、またはリボザイムコード化ポリヌクレオチドからなる群から選択される薬剤である、請求項１に記載のオートタキシン阻害剤。
- オートタキシン阻害剤は、インドール含有小分子である小分子である、請求項１に記載のオートタキシン阻害剤。
- 個体は血糖値が上昇している、請求項１に記載のオートタキシン阻害剤。
- 個体の血糖値は、前記オートタキシン阻害剤の投与前、１００ｍｇ／ｄＬよりも高い、請求項１に記載のオートタキシン阻害剤。
- 個体はメタボリック症候群を抱えている、請求項１乃至７の何れか１つに記載のオートタキシン阻害剤。
- 個体は、腹部肥満、高血圧、空腹時の高血漿グルコース、高血清トリグリセリド、および低い高密度コレステロールレベル（ＨＤＬ）からなる群から選択される少なくとも１つの医学的状態を抱えている、請求項１乃至７の何れか１つに記載のオートタキシン阻害剤。
- 個体はインスリン抵抗性、２型糖尿病、少なくとも６．０％以上のＡ１Ｃレベルを有し、非アルコール性脂肪肝疾患（ＮＡＦＬＤ）、または非アルコール性の脂肪性肝炎と診断されたことがあり、耐糖能障害を抱えており、且つ前糖尿病性である、請求項１乃至７の何れか１つに記載のオートタキシン阻害剤。
- 個体は、少なくとも２５ｋｇ／ｍ ２ の肥満度指数を有するとともに、運動不足、糖尿病の一等親血縁者、リスクの高い人種または民族性、４．０８キログラムを超える重さの赤ん坊を出産した女性、以前に妊娠性糖尿病と診察されたことがある女性、高血圧、少なくとも０．９ｍｍｏｌ／Ｌ（３５ｍｇ／ｄＬ）よりも低いＨＤＬコレステロールレベル、少なくとも２．８２ｍｍｏｌ／Ｌ（２５０ｍｇ／ｄＬ）以上のトリグリセリドレベル、多嚢胞性卵巣症候群、重度の肥満、黒色表皮腫、および心血管疾患の女性からなる群から選択される糖尿病の危険因子の少なくとも１つ以上を有する、請求項１乃至７の何れか１つに記載のオートタキシン阻害剤。
- 個体は肥満である、請求項１乃至７の何れか１つに記載のオートタキシン阻害剤。
- 追加の治療薬をさらに含む、血糖値を下げるのに使用するための請求項１乃至７の何れか１つに記載のオートタキシン阻害剤。
- 追加の治療薬は、ペルオキシソーム増殖因子活性化受容体（ＰＰＡＲ）アゴニスト（ガンマ、デュアル、またはパン）、ジペプチジルペプチダーゼ（ＩＶ）阻害剤、グルカゴン様ペプチド−１（ＧＬＰ−Ｉ）アナログ、インスリンまたはインスリンアナログ、インスリン分泌促進物質、ナトリウムグルコース共輸送体２（ＳＧＬＴ２）阻害剤、ヒトアミリンアナログ、ビグアニド、グルコファージ、アルファ−グルコシダーゼ阻害剤、メグリチニド、チアゾリジンジオン、およびスルホニル尿素、またはこれらの任意の組み合わせからなる群から選択される、請求項１３に記載のオートタキシン阻害剤。
- 追加の治療薬は、アンジオテンシン変換酵素（ＡＣＥ）阻害剤、アンジオテンシンＩＩ受容体拮抗薬（ＡＲＢ）、β−遮断薬、利尿薬、カルシウムチャネル遮断薬、レニン−アンジオテンシン系（ＲＡＳ）の阻害剤、抗凝血薬、スタチン、および、フィブラート系薬剤、または、これらの任意の組み合わせからなる群から選択される、請求項１３に記載のオートタキシン阻害剤。
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US14/462,459 | 2014-08-18 | ||
| US14/462,459 US9051320B1 (en) | 2014-08-18 | 2014-08-18 | Methods for the treatment of metabolic disorders by a selective small molecule autotaxin inhibitor |
| PCT/US2015/045518 WO2016028686A1 (en) | 2014-08-18 | 2015-08-17 | Methods and compositions for the treatment of metabolic disorders |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017527550A JP2017527550A (ja) | 2017-09-21 |
| JP2017527550A5 true JP2017527550A5 (ja) | 2018-09-27 |
| JP6817190B2 JP6817190B2 (ja) | 2021-01-20 |
Family
ID=53267810
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017508482A Active JP6817190B2 (ja) | 2014-08-18 | 2015-08-17 | 代謝障害の処置のための方法と組成物 |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US9051320B1 (ja) |
| EP (1) | EP3183005A4 (ja) |
| JP (1) | JP6817190B2 (ja) |
| WO (1) | WO2016028686A1 (ja) |
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|---|---|---|---|---|
| EP3046905A4 (en) | 2013-09-17 | 2017-03-22 | Pharmakea Inc. | Vinyl autotaxin inhibitor compounds |
| JP2016530210A (ja) | 2013-09-17 | 2016-09-29 | ファーマケア，インク． | ヘテロ環式ビニルオートタキシン阻害剤化合物 |
| US9850203B2 (en) | 2013-09-26 | 2017-12-26 | Pharmakea, Inc. | Autotaxin inhibitor compounds |
| AU2014352887A1 (en) | 2013-11-22 | 2016-06-09 | Pharmakea, Inc. | Tetracyclic autotaxin inhibitors |
| AU2014352888B2 (en) | 2013-11-22 | 2019-05-09 | Sabre Therapeutics Llc | Autotaxin inhibitor compounds |
| US9051320B1 (en) * | 2014-08-18 | 2015-06-09 | Pharmakea, Inc. | Methods for the treatment of metabolic disorders by a selective small molecule autotaxin inhibitor |
| US10183949B2 (en) * | 2014-08-29 | 2019-01-22 | The University Of Tokyo | Pyrimidinone derivative having autotaxin-inhibitory activity |
| EP3265456B1 (en) | 2015-03-06 | 2020-11-18 | Pharmakea, Inc. | Fluorinated lysyl oxidase-like 2 inhibitors and uses thereof |
| EP4026549A1 (en) * | 2015-05-27 | 2022-07-13 | Sabre Therapeutics LLC | Autotaxin inhibitors and uses thereof |
| CA2987071A1 (en) | 2015-06-10 | 2016-12-15 | Hackensack University Medical Center | Use of telmisartan to prevent and treat graft versus host disease and other alloimmune and autoimmune diseases |
| ES2870030T3 (es) * | 2015-10-30 | 2021-10-26 | Univ Muenster Westfaelische Wilhelms | Reducción del nivel de LPA para tratar trastornos del sistema nervioso central |
| CA3033863C (en) * | 2016-08-18 | 2021-09-14 | Memorial Sloan Kettering Cancer Center | Inhibition of sphingosine 1-phosphate receptor for treatment and prevention of lymphedema |
| EA201990621A1 (ru) | 2016-09-07 | 2019-09-30 | Фармакеа, Инк. | Кристаллические формы ингибитора лизилоксидаза-подобного белка 2 и способы получения |
| KR102615565B1 (ko) | 2016-09-07 | 2023-12-18 | 파마케아, 인크. | 리실 옥시다제 유사 2 억제제의 용도 |
| CN106822114B (zh) * | 2016-12-12 | 2020-08-07 | 中国科学院西北高原生物研究所 | Mtca在制备降血糖或降血脂的药物中的用途 |
| JP2021528738A (ja) * | 2018-06-14 | 2021-10-21 | アストラゼネカ・ユーケイ・リミテッドＡｓｔｒａＺｅｎｅｃａ ＵＫ Ｌｉｍｉｔｅｄ | メトホルミン医薬組成物を用いて血糖を低下させるための方法 |
| EP3807893A1 (en) * | 2018-06-14 | 2021-04-21 | AstraZeneca UK Limited | Methods for lowering blood sugar with a gliflozin sodium-glucose cotransporter 2 inhibitor pharmaceutical composition |
| GR1010570B (el) | 2022-12-22 | 2023-11-17 | Uni-Pharma Κλεων Τσετης Φαρμακευτικα Εργαστηρια Α.Β.Ε.Ε., | 4-(2-(4-((2,4-διοξοθειαζολιδιν-5-υλ)μεθυλ)φαινοξυ) παραγωγα με δραση αναστολης της αυτοταξινης |
| CN116239577A (zh) * | 2023-03-27 | 2023-06-09 | 沈阳药科大学 | 一种制备Cudetaxestat的方法 |
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| US8497371B2 (en) | 2009-10-26 | 2013-07-30 | University Of Memphis Research Foundation | Pipemidic acid derivative autotaxin inhibitors |
| EP2552914B1 (de) | 2010-03-26 | 2015-11-11 | Merck Patent GmbH | Benzonaphthyridinamine als autotaxin-inhibitoren |
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| SG11201504633PA (en) | 2012-12-19 | 2015-07-30 | Novartis Ag | Autotaxin inhibitors |
| US9409895B2 (en) | 2012-12-19 | 2016-08-09 | Novartis Ag | Autotaxin inhibitors |
| TWI499591B (zh) | 2013-01-11 | 2015-09-11 | Lilly Co Eli | 雙環嘧啶化合物 |
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-
2014
- 2014-08-18 US US14/462,459 patent/US9051320B1/en not_active Expired - Fee Related
-
2015
- 2015-08-17 JP JP2017508482A patent/JP6817190B2/ja active Active
- 2015-08-17 EP EP15833802.0A patent/EP3183005A4/en not_active Withdrawn
- 2015-08-17 WO PCT/US2015/045518 patent/WO2016028686A1/en active Application Filing
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