JP2017515899A5 - - Google Patents
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- Publication number
- JP2017515899A5 JP2017515899A5 JP2017511558A JP2017511558A JP2017515899A5 JP 2017515899 A5 JP2017515899 A5 JP 2017515899A5 JP 2017511558 A JP2017511558 A JP 2017511558A JP 2017511558 A JP2017511558 A JP 2017511558A JP 2017515899 A5 JP2017515899 A5 JP 2017515899A5
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- JP
- Japan
- Prior art keywords
- optionally substituted
- compound according
- alkyl
- cycloalkyl
- following structure
- 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.)
- Granted
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- 150000001875 compounds Chemical class 0.000 claims description 68
- 125000003107 substituted aryl group Chemical group 0.000 claims description 22
- 125000000547 substituted alkyl group Chemical group 0.000 claims description 21
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims description 21
- 125000000217 alkyl group Chemical group 0.000 claims description 19
- 125000001072 heteroaryl group Chemical group 0.000 claims description 19
- -1 Q is H Chemical group 0.000 claims description 16
- 229910052736 halogen Inorganic materials 0.000 claims description 14
- 150000002367 halogens Chemical class 0.000 claims description 14
- 125000005415 substituted alkoxy group Chemical group 0.000 claims description 14
- 125000002252 acyl group Chemical group 0.000 claims description 12
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 12
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims description 12
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 10
- 125000005328 phosphinyl group Chemical group [PH2](=O)* 0.000 claims description 10
- 125000005499 phosphonyl group Chemical group 0.000 claims description 10
- 125000005017 substituted alkenyl group Chemical group 0.000 claims description 10
- 125000004426 substituted alkynyl group Chemical group 0.000 claims description 10
- 208000008589 Obesity Diseases 0.000 claims description 6
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 6
- 235000020824 obesity Nutrition 0.000 claims description 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 6
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 6
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 5
- DLFVBJFMPXGRIB-UHFFFAOYSA-N Acetamide Chemical compound CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 claims description 4
- 239000000654 additive Substances 0.000 claims description 4
- 230000000996 additive effect Effects 0.000 claims description 4
- 125000003118 aryl group Chemical group 0.000 claims description 4
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 4
- 206010012601 diabetes mellitus Diseases 0.000 claims description 4
- 150000002148 esters Chemical class 0.000 claims description 4
- 125000005842 heteroatom Chemical group 0.000 claims description 4
- 239000008194 pharmaceutical composition Substances 0.000 claims description 4
- 150000003839 salts Chemical class 0.000 claims description 4
- 230000001225 therapeutic effect Effects 0.000 claims description 4
- 150000003573 thiols Chemical class 0.000 claims description 4
- 206010003211 Arteriosclerosis coronary artery Diseases 0.000 claims description 2
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims description 2
- 208000032928 Dyslipidaemia Diseases 0.000 claims description 2
- 201000005569 Gout Diseases 0.000 claims description 2
- 208000017170 Lipid metabolism disease Diseases 0.000 claims description 2
- 210000000577 adipose tissue Anatomy 0.000 claims description 2
- 230000002411 adverse Effects 0.000 claims description 2
- 208000026594 alcoholic fatty liver disease Diseases 0.000 claims description 2
- 125000003282 alkyl amino group Chemical group 0.000 claims description 2
- 230000003510 anti-fibrotic effect Effects 0.000 claims description 2
- 239000000883 anti-obesity agent Substances 0.000 claims description 2
- 229940125708 antidiabetic agent Drugs 0.000 claims description 2
- 239000003472 antidiabetic agent Substances 0.000 claims description 2
- 239000002246 antineoplastic agent Substances 0.000 claims description 2
- 229940125710 antiobesity agent Drugs 0.000 claims description 2
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 2
- 210000004556 brain Anatomy 0.000 claims description 2
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 2
- 239000003795 chemical substances by application Substances 0.000 claims description 2
- 230000008021 deposition Effects 0.000 claims description 2
- 208000033679 diabetic kidney disease Diseases 0.000 claims description 2
- 229940039227 diagnostic agent Drugs 0.000 claims description 2
- 239000000032 diagnostic agent Substances 0.000 claims description 2
- 239000002552 dosage form Substances 0.000 claims description 2
- 230000000694 effects Effects 0.000 claims description 2
- 125000004404 heteroalkyl group Chemical group 0.000 claims description 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 2
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims description 2
- 230000036470 plasma concentration Effects 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 12
- 0 C**C1=CC=CC(S(N=C(C2=NN(*)C(*)(*)C2)NC(*I)=N)(=O)=O)=CC1 Chemical compound C**C1=CC=CC(S(N=C(C2=NN(*)C(*)(*)C2)NC(*I)=N)(=O)=O)=CC1 0.000 description 4
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461991333P | 2014-05-09 | 2014-05-09 | |
| US61/991,333 | 2014-05-09 | ||
| PCT/US2015/029946 WO2015172059A1 (en) | 2014-05-09 | 2015-05-08 | Pyrazole derivatives and their use as cannabinoid receptor mediators |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017515899A JP2017515899A (ja) | 2017-06-15 |
| JP2017515899A5 true JP2017515899A5 (enExample) | 2018-06-14 |
| JP6762930B2 JP6762930B2 (ja) | 2020-09-30 |
Family
ID=53385930
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017511558A Active JP6762930B2 (ja) | 2014-05-09 | 2015-05-08 | カンナビノイド受容体メディエータとしてのピラゾール誘導体およびそれらの使用 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US10329259B2 (enExample) |
| EP (1) | EP3140288B1 (enExample) |
| JP (1) | JP6762930B2 (enExample) |
| CN (1) | CN106660968B (enExample) |
| AU (2) | AU2015255765A1 (enExample) |
| CA (1) | CA2948349C (enExample) |
| WO (1) | WO2015172059A1 (enExample) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014078309A1 (en) | 2012-11-13 | 2014-05-22 | The United States Of America, As Represented By The Secretary, Department Of Health & Human Services | Cannabinoid receptor mediating compounds |
| US11155521B2 (en) | 2012-11-13 | 2021-10-26 | The United States Of America As Represented By The Secretary, Department Of Health And Human Services | Cannabinoid receptor mediating compounds |
| CN106660968B (zh) | 2014-05-09 | 2020-02-07 | 美国政府(由卫生和人类服务部的部长所代表) | 吡唑衍生物及其作为大麻素受体介体的用途 |
| CN112511569B (zh) * | 2021-02-07 | 2021-05-11 | 杭州筋斗腾云科技有限公司 | 网络资源访问请求的处理方法、系统及计算机设备 |
| WO2025040089A1 (zh) * | 2023-08-21 | 2025-02-27 | 德睿智药(苏州)新药研发有限公司 | 用于选择性调节大麻素cb1功能的新型杂环类化合物 |
Family Cites Families (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4675189A (en) | 1980-11-18 | 1987-06-23 | Syntex (U.S.A.) Inc. | Microencapsulation of water soluble active polypeptides |
| JPS60100516A (ja) | 1983-11-04 | 1985-06-04 | Takeda Chem Ind Ltd | 徐放型マイクロカプセルの製造法 |
| CA1256638A (en) | 1984-07-06 | 1989-06-27 | Motoaki Tanaka | Polymer and its production |
| JP2551756B2 (ja) | 1985-05-07 | 1996-11-06 | 武田薬品工業株式会社 | ポリオキシカルボン酸エステルおよびその製造法 |
| UA74367C2 (uk) * | 2000-03-23 | 2005-12-15 | Сольве Фармас'Ютікалз Б.В. | ПОХІДНІ 4,5-ДИГІДРО-1Н-ПІРАЗОЛУ, ЩО ВИЯВЛЯЮТЬ АНТАГОНІСТИЧНУ АКТИВНІСТЬ ЩОДО СВ<sub>1</sub>, СПОСІБ ЇХ ОДЕРЖАННЯ, ФАРМАЦЕВТИЧНА КОМПОЗИЦІЯ ТА СПОСІБ ЇЇ ВИГОТОВЛЕННЯ, СПОСІБ ЛІКУВАННЯ ЗАХВОРЮВАНЬ (ВАРІАНТИ) |
| RU2281941C2 (ru) | 2001-03-22 | 2006-08-20 | Солвей Фармасьютикалс Б.В. | Производные 4,5-дигидро-1h-пиразола, обладающие cb1-антагонистической активностью |
| US7528162B2 (en) * | 2001-09-21 | 2009-05-05 | Solvay Pharmaceuticals, B.V. | 4,5-dihydro-1H-pyrazole derivatives having CB1-antagonistic activity |
| JP4313672B2 (ja) * | 2001-09-21 | 2009-08-12 | ソルベイ・フアーマシユーチカルズ・ベー・ブイ | 強力なｃｂ１−拮抗活性を有する４，５−ジヒドロ−１ｈ−ピラゾール誘導体 |
| US20050239859A2 (en) | 2003-09-03 | 2005-10-27 | Solvay Pharmaceuticals Gmbh | Novel medical uses of 4,5-dihydro-1h-pyrazole derivatives having cb1- antagonistic activity |
| AR047462A1 (es) * | 2004-01-30 | 2006-01-18 | Solvay Pharm Bv | Derivados 1,3,5 trisubstituidos de 4, 5 dihidro - 1h - pirazol que tienen actividad antagonista cb1. composiciones farmaceuticas. |
| ES2311972T3 (es) * | 2004-01-30 | 2009-02-16 | Solvay Pharmaceuticals B.V. | Derivados 1,3,5-trisubstituidos de 4,5-dihidro-1h-pirazol que tienen actividad antagonista de cb1. |
| EP1574211A1 (en) | 2004-03-09 | 2005-09-14 | Inserm | Use of antagonists of the CB1 receptor for the manufacture of a composition useful for the treatment of hepatic diseases |
| WO2006060192A2 (en) | 2004-11-30 | 2006-06-08 | Bayer Pharmaceuticals Corporation | Pyrazole derivatives |
| CA2613678A1 (en) * | 2005-06-02 | 2006-12-07 | Glenmark Pharmaceuticals S.A. | Novel cannabinoid receptor ligands, pharmaceutical compositions containing them, and process for their preparation |
| JP5561720B2 (ja) * | 2006-05-05 | 2014-07-30 | ジェンリン ディスカバリー | 肥満及び糖尿病を含む心臓血管障害を治療するために有用なカンナビノイド受容体アンタゴニスト／インバ−スアゴニスト |
| AU2007336219A1 (en) * | 2006-12-20 | 2008-06-26 | Solvay Pharmaceuticals B.V. | Compounds with a combination of cannabinoid-CB1 antagonism and acetylcholinesterase inhibition |
| US7655685B2 (en) | 2007-11-02 | 2010-02-02 | Jenrin Discovery, Inc. | Cannabinoid receptor antagonists/inverse agonists useful for treating metabolic disorders, including obesity and diabetes |
| CN101896465A (zh) | 2007-12-10 | 2010-11-24 | 7Tm制药联合股份有限公司 | 大麻素受体调节剂 |
| AR070898A1 (es) * | 2008-03-18 | 2010-05-12 | Solvay Pharm Bv | Derivados de arilsulfonil pirazolin carboxamidina como antagonistas de 5-ht6 |
| EP2411370B1 (en) | 2009-03-27 | 2015-04-22 | AbbVie Inc. | Compounds as cannabinoid receptor ligands |
| WO2011044370A1 (en) * | 2009-10-07 | 2011-04-14 | Jenrin Discovery | Cannabinoid receptor antagonists/inverse agonists useful for treating metabolic disorders, including obesity and diabetes |
| EP2640381A4 (en) * | 2010-11-18 | 2014-05-21 | Jenrin Discovery | CANNABINOID RECEPTOR ANTAGONISTS / INVERSAGONISTS FOR THE TREATMENT OF METABOLISM DISEASES INCLUDING ADIPOSITAS AND DIABETES |
| WO2014078309A1 (en) * | 2012-11-13 | 2014-05-22 | The United States Of America, As Represented By The Secretary, Department Of Health & Human Services | Cannabinoid receptor mediating compounds |
| US11155521B2 (en) | 2012-11-13 | 2021-10-26 | The United States Of America As Represented By The Secretary, Department Of Health And Human Services | Cannabinoid receptor mediating compounds |
| CN106660968B (zh) | 2014-05-09 | 2020-02-07 | 美国政府(由卫生和人类服务部的部长所代表) | 吡唑衍生物及其作为大麻素受体介体的用途 |
| EP3303325A1 (en) | 2015-06-04 | 2018-04-11 | The U.S.A. as represented by the Secretary, Department of Health and Human Services | Cannabinoid receptor mediating compounds |
-
2015
- 2015-05-08 CN CN201580028788.XA patent/CN106660968B/zh active Active
- 2015-05-08 JP JP2017511558A patent/JP6762930B2/ja active Active
- 2015-05-08 EP EP15728668.3A patent/EP3140288B1/en active Active
- 2015-05-08 WO PCT/US2015/029946 patent/WO2015172059A1/en not_active Ceased
- 2015-05-08 US US15/309,728 patent/US10329259B2/en active Active
- 2015-05-08 AU AU2015255765A patent/AU2015255765A1/en not_active Abandoned
- 2015-05-08 CA CA2948349A patent/CA2948349C/en active Active
-
2019
- 2019-09-10 AU AU2019227889A patent/AU2019227889B2/en active Active