JP2015536997A5 - - Google Patents
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- JP2015536997A5 JP2015536997A5 JP2015542015A JP2015542015A JP2015536997A5 JP 2015536997 A5 JP2015536997 A5 JP 2015536997A5 JP 2015542015 A JP2015542015 A JP 2015542015A JP 2015542015 A JP2015542015 A JP 2015542015A JP 2015536997 A5 JP2015536997 A5 JP 2015536997A5
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- JP
- Japan
- Prior art keywords
- optionally substituted
- alkyl
- compound
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- item
- 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 57
- -1 nitro, hydroxy Chemical group 0.000 claims description 22
- 125000002252 acyl group Chemical group 0.000 claims description 20
- 229910052736 halogen Inorganic materials 0.000 claims description 19
- 150000002367 halogens Chemical class 0.000 claims description 19
- 125000001072 heteroaryl group Chemical group 0.000 claims description 19
- 125000000547 substituted alkyl group Chemical group 0.000 claims description 16
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 15
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 14
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 14
- 125000001841 imino group Chemical group [H]N=* 0.000 claims description 14
- 125000001181 organosilyl group Chemical group [SiH3]* 0.000 claims description 14
- 125000005328 phosphinyl group Chemical group [PH2](=O)* 0.000 claims description 14
- 125000005499 phosphonyl group Chemical group 0.000 claims description 14
- 125000005017 substituted alkenyl group Chemical group 0.000 claims description 14
- 125000005415 substituted alkoxy group Chemical group 0.000 claims description 14
- 125000004426 substituted alkynyl group Chemical group 0.000 claims description 14
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims description 14
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims description 14
- 125000000217 alkyl group Chemical group 0.000 claims description 12
- 125000003107 substituted aryl group Chemical group 0.000 claims description 12
- 125000005621 boronate group Chemical class 0.000 claims description 10
- 125000003739 carbamimidoyl group Chemical group C(N)(=N)* 0.000 claims description 8
- 208000008589 Obesity Diseases 0.000 claims description 5
- 235000020824 obesity Nutrition 0.000 claims description 5
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 4
- ZADPBFCGQRWHPN-UHFFFAOYSA-N boronic acid Chemical compound OBO ZADPBFCGQRWHPN-UHFFFAOYSA-N 0.000 claims description 4
- 150000002148 esters Chemical class 0.000 claims description 4
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 4
- 150000003839 salts Chemical class 0.000 claims description 4
- 230000002411 adverse Effects 0.000 claims description 3
- 206010012601 diabetes mellitus Diseases 0.000 claims description 3
- 230000000694 effects Effects 0.000 claims description 3
- 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
- 239000000654 additive Substances 0.000 claims description 2
- 230000000996 additive effect Effects 0.000 claims description 2
- 210000000577 adipose tissue Anatomy 0.000 claims description 2
- 208000026594 alcoholic fatty liver disease Diseases 0.000 claims description 2
- 210000005013 brain tissue Anatomy 0.000 claims description 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 2
- 230000008021 deposition Effects 0.000 claims description 2
- 208000033679 diabetic kidney disease Diseases 0.000 claims description 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 2
- 125000002757 morpholinyl group Chemical group 0.000 claims description 2
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims description 2
- 230000002093 peripheral effect Effects 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 125000004076 pyridyl group Chemical group 0.000 claims description 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 2
- 229910052711 selenium Inorganic materials 0.000 claims description 2
- 229910052717 sulfur Inorganic materials 0.000 claims description 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 2
- 210000001519 tissue Anatomy 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 7
- 125000001309 chloro group Chemical group Cl* 0.000 claims 3
- 206010022489 Insulin Resistance Diseases 0.000 claims 1
- 208000019425 cirrhosis of liver Diseases 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 230000004761 fibrosis Effects 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 150000003573 thiols Chemical class 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
- 102000005962 receptors Human genes 0.000 description 4
- 108020003175 receptors Proteins 0.000 description 4
- 230000001225 therapeutic effect Effects 0.000 description 4
- 229910052799 carbon Inorganic materials 0.000 description 3
- 229910052739 hydrogen Inorganic materials 0.000 description 3
- 239000000883 anti-obesity agent Substances 0.000 description 2
- 229940125708 antidiabetic agent Drugs 0.000 description 2
- 239000003472 antidiabetic agent Substances 0.000 description 2
- 239000002246 antineoplastic agent Substances 0.000 description 2
- 229940125710 antiobesity agent Drugs 0.000 description 2
- 125000000717 hydrazino group Chemical group [H]N([*])N([H])[H] 0.000 description 2
- 230000001404 mediated effect Effects 0.000 description 2
- VZBVDTBDJCBVGH-UHFFFAOYSA-N N',3-diphenylpyrazole-1-carboximidamide Chemical group C1=CC(C=2C=CC=CC=2)=NN1C(N)=NC1=CC=CC=C1 VZBVDTBDJCBVGH-UHFFFAOYSA-N 0.000 description 1
- 210000004556 brain Anatomy 0.000 description 1
- 230000036470 plasma concentration Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261725949P | 2012-11-13 | 2012-11-13 | |
| US61/725,949 | 2012-11-13 | ||
| PCT/US2013/069686 WO2014078309A1 (en) | 2012-11-13 | 2013-11-12 | Cannabinoid receptor mediating compounds |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015536997A JP2015536997A (ja) | 2015-12-24 |
| JP2015536997A5 true JP2015536997A5 (enExample) | 2016-12-28 |
| JP6272626B2 JP6272626B2 (ja) | 2018-01-31 |
Family
ID=49725346
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015542015A Active JP6272626B2 (ja) | 2012-11-13 | 2013-11-12 | カンナビノイド受容体媒介性化合物 |
Country Status (7)
| Country | Link |
|---|---|
| US (6) | US9765031B2 (enExample) |
| EP (1) | EP2919779B1 (enExample) |
| JP (1) | JP6272626B2 (enExample) |
| CN (1) | CN104884057B (enExample) |
| CA (1) | CA2889697C (enExample) |
| IN (1) | IN2015DN03733A (enExample) |
| WO (1) | WO2014078309A1 (enExample) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2919779B1 (en) | 2012-11-13 | 2021-01-06 | The U.S.A. as represented by the Secretary, Department of Health and 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 |
| WO2015172059A1 (en) * | 2014-05-09 | 2015-11-12 | The United States Of America, As Represented By The Secretary, Department Of Health & Human Services | Pyrazole derivatives and their use as cannabinoid receptor mediators |
| 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 |
| EP3423448B1 (en) * | 2016-03-04 | 2024-12-04 | The U.S.A. as represented by the Secretary, Department of Health and Human Services | Cannabinoid receptor mediating compounds |
| RU2703484C1 (ru) * | 2018-05-22 | 2019-10-17 | Федеральное государственное бюджетное образовательное учреждение высшего образования "Саратовский государственный аграрный университет имени Н.И. Вавилова" | Способ производства безоболочных колбасок для функционального питания |
| US20230174493A1 (en) * | 2020-03-24 | 2023-06-08 | Inversago Pharma Inc. | Solid Dispersions of Amorphous 3,4-Diphenyl-4,5-Dihydro-1H-Pyrazole Derivatives, Compositions Comprising them and Uses Thereof as Cannabinoid CB1 Receptor Inhibitors |
| CA3169745A1 (en) | 2020-04-07 | 2021-10-14 | Inversago Pharma Inc. | Process for producing 4,5-dihydro-1h-pyrazoles and intermediates |
| CN118829427A (zh) * | 2022-02-24 | 2024-10-22 | 诺和诺德股份有限公司 | 治疗腹型肥胖、高甘油三酯血症和/或血糖受损受试者的方法 |
| EP4493547A1 (en) * | 2022-03-14 | 2025-01-22 | The United States of America, as represented by the Secretary, Department of Health and Human Services | Cannabinoid receptor modulating compounds |
| WO2025257151A1 (en) | 2024-06-10 | 2025-12-18 | Institut National de la Santé et de la Recherche Médicale | Methods and pharmaceutical composition for treating ciliopathies |
Family Cites Families (22)
| 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 |
| PL208098B1 (pl) * | 2000-03-23 | 2011-03-31 | Solvay Pharm Bv | Pochodne 4,5-dihydro-1H-pirazolu, kompozycja farmaceutyczna, sposób wytwarzania związków oraz ich zastosowanie |
| CZ2003698A3 (cs) * | 2001-03-22 | 2003-06-18 | Solvay Pharmaceuticals B. V. | 4,5-Dihydro-1H-pyrazolové deriváty mající CB1-antagonistickou účinnost |
| CN101659639A (zh) * | 2001-09-21 | 2010-03-03 | 索尔瓦药物有限公司 | 具有cb1-拮抗活性的新的4,5-二氢-1h-吡唑衍生物 |
| KR100950430B1 (ko) | 2001-09-21 | 2010-04-02 | 솔베이 파마슈티칼스 비. 브이 | 효력있는 ｃｂ1-길항 작용을 가지는4,5-디하이드로-1ｈ-피라졸 유도체 |
| 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 |
| EP1713475B1 (en) | 2004-01-30 | 2008-07-30 | 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 |
| EP2023920B1 (en) | 2006-05-05 | 2012-06-13 | Jenrin Discovery | Cannabinoid receptor antagonists/inverse agonists |
| 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 |
| CA2708706A1 (en) | 2007-12-10 | 2009-06-18 | 7Tm Pharma A/S | Cannabinoid receptor modulators |
| WO2010111573A1 (en) | 2009-03-27 | 2010-09-30 | Abbott Laboratories | Compounds as cannabinoid receptor ligands |
| US8217038B2 (en) | 2009-10-07 | 2012-07-10 | Jenrin Discovery, Inc. | Cannabinoid receptor antagonists/inverse agonists useful for treating metabolic disorders, including obesity and diabetes |
| WO2012068529A2 (en) | 2010-11-18 | 2012-05-24 | Jenrin Discovery | Cannabinoid receptor antagonists-inverse agonists useful for treating metabolic disorders, including obesity and diabetes |
| EP2919779B1 (en) | 2012-11-13 | 2021-01-06 | The U.S.A. as represented by the Secretary, Department of Health and 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 |
| WO2015172059A1 (en) | 2014-05-09 | 2015-11-12 | The United States Of America, As Represented By The Secretary, Department Of Health & Human Services | Pyrazole derivatives and their use as cannabinoid receptor mediators |
| 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 |
-
2013
- 2013-11-12 EP EP13802153.0A patent/EP2919779B1/en active Active
- 2013-11-12 CA CA2889697A patent/CA2889697C/en active Active
- 2013-11-12 US US14/442,383 patent/US9765031B2/en active Active
- 2013-11-12 WO PCT/US2013/069686 patent/WO2014078309A1/en not_active Ceased
- 2013-11-12 IN IN3733DEN2015 patent/IN2015DN03733A/en unknown
- 2013-11-12 JP JP2015542015A patent/JP6272626B2/ja active Active
- 2013-11-12 CN CN201380069389.9A patent/CN104884057B/zh active Active
-
2017
- 2017-08-10 US US15/674,333 patent/US10787419B2/en active Active
- 2017-08-10 US US15/674,365 patent/US10683270B2/en active Active
-
2020
- 2020-05-08 US US16/870,093 patent/US11485709B2/en active Active
-
2022
- 2022-09-29 US US17/956,313 patent/US20230202983A1/en not_active Abandoned
-
2023
- 2023-02-10 US US18/108,264 patent/US11939297B2/en active Active
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