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
- Authority
- 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 (OSRAM) | 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 (OSRAM) |
| EP (1) | EP3140288B1 (OSRAM) |
| JP (1) | JP6762930B2 (OSRAM) |
| CN (1) | CN106660968B (OSRAM) |
| AU (2) | AU2015255765A1 (OSRAM) |
| CA (1) | CA2948349C (OSRAM) |
| WO (1) | WO2015172059A1 (OSRAM) |
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 |
| US10329259B2 (en) | 2014-05-09 | 2019-06-25 | The United States Of America, As Represented By The Secretary, Department Of Health & Human Services | Pyrazole derivatives and their use as cannabinoid receptor mediators |
| 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 |
| HK1052349B (zh) * | 2000-03-23 | 2005-09-23 | 索尔瓦药物有限公司 | 具有cb1-拮抗活性的4，5-二氢-1h-吡唑衍生物 |
| JP4373675B2 (ja) | 2001-03-22 | 2009-11-25 | ソルベイ・フアーマシユーチカルズ・ベー・ブイ | Ｃｂ１−拮抗活性を有する４，５−ジヒドロ−１ｈ−ピラゾール誘導体 |
| BR0212044A (pt) * | 2001-09-21 | 2004-08-17 | Solvay Pharm Bv | Compostos, composições farmacêuticas, método de preparação das mesmas, e, uso de um composto |
| PL367814A1 (en) * | 2001-09-21 | 2005-03-07 | Solvay Pharmaceuticals B.V. | 4,5-dihydro-1h-pyrazole derivatives having potent cb1-antagonistic activity |
| 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. |
| AU2005210163B2 (en) * | 2004-01-30 | 2010-05-13 | Solvay Pharmaceuticals B.V. | 1,3,5-trisubstituted 4,5-dihydro-1H-pyrazole derivatives having CB1-antagonistic activity |
| 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 |
| PL1902034T3 (pl) * | 2005-06-02 | 2011-09-30 | Glenmark Pharmaceuticals Sa | Nowe ligandy receptorów kanabinoidowych, kompozycja farmaceutyczna je zawierająca oraz proces ich wytwarzania |
| AU2007247878B2 (en) | 2006-05-05 | 2012-05-31 | Jenrin Discovery | Cannabinoid receptor antagonists/inverse agonists |
| 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 |
| ES2540119T3 (es) | 2009-03-27 | 2015-07-08 | Abbvie Inc. | Compuestos como ligandos de receptores cannabinoides |
| WO2011044370A1 (en) * | 2009-10-07 | 2011-04-14 | Jenrin Discovery | Cannabinoid receptor antagonists/inverse agonists useful for treating metabolic disorders, including obesity and diabetes |
| US8580768B2 (en) | 2010-11-18 | 2013-11-12 | Jenrin Discovery, Inc. | Cannabinoid receptor antagonists-inverse agonists useful for treating metabolic disorders, including obesity and diabetes |
| 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 |
| 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 |
| US10329259B2 (en) | 2014-05-09 | 2019-06-25 | The United States Of America, As Represented By The Secretary, Department Of Health & Human Services | Pyrazole derivatives and their use as cannabinoid receptor mediators |
| US20180273485A1 (en) | 2015-06-04 | 2018-09-27 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Serv | Cannabinoid receptor mediating compounds |
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2015
- 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 CN CN201580028788.XA patent/CN106660968B/zh active Active
- 2015-05-08 CA CA2948349A patent/CA2948349C/en active Active
- 2015-05-08 JP JP2017511558A patent/JP6762930B2/ja active Active
- 2015-05-08 WO PCT/US2015/029946 patent/WO2015172059A1/en not_active Ceased
- 2015-05-08 EP EP15728668.3A patent/EP3140288B1/en active Active
-
2019
- 2019-09-10 AU AU2019227889A patent/AU2019227889B2/en active Active