JP2016505512A5 - - Google Patents
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- Publication number
- JP2016505512A5 JP2016505512A5 JP2015539801A JP2015539801A JP2016505512A5 JP 2016505512 A5 JP2016505512 A5 JP 2016505512A5 JP 2015539801 A JP2015539801 A JP 2015539801A JP 2015539801 A JP2015539801 A JP 2015539801A JP 2016505512 A5 JP2016505512 A5 JP 2016505512A5
- Authority
- JP
- Japan
- Prior art keywords
- compound according
- lower alkyl
- pde4
- cyano
- compound
- 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
Links
- 150000001875 compounds Chemical class 0.000 claims 43
- 125000000217 alkyl group Chemical group 0.000 claims 27
- 108060002038 Pde4 Proteins 0.000 claims 18
- -1 trifluoromethoxy, hydroxyl Chemical group 0.000 claims 18
- 125000004093 cyano group Chemical group *C#N 0.000 claims 16
- 229910052736 halogen Inorganic materials 0.000 claims 16
- 150000002367 halogens Chemical class 0.000 claims 16
- 239000008194 pharmaceutical composition Substances 0.000 claims 14
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 13
- 125000003545 alkoxy group Chemical group 0.000 claims 12
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 11
- 201000010099 disease Diseases 0.000 claims 10
- 230000001404 mediated Effects 0.000 claims 10
- 125000001424 substituent group Chemical group 0.000 claims 10
- 229910052739 hydrogen Inorganic materials 0.000 claims 9
- 239000001257 hydrogen Substances 0.000 claims 9
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 8
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 8
- 239000003814 drug Substances 0.000 claims 7
- XOQABDOICLHPIS-UHFFFAOYSA-N 1-hydroxy-2,1-benzoxaborole Chemical compound C1=CC=C2B(O)OCC2=C1 XOQABDOICLHPIS-UHFFFAOYSA-N 0.000 claims 6
- 125000004179 3-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(Cl)=C1[H] 0.000 claims 6
- 101700057678 PDE4B Proteins 0.000 claims 6
- 102100018800 PDE4B Human genes 0.000 claims 6
- 101700057277 PDE4D Proteins 0.000 claims 6
- 102100018798 PDE4D Human genes 0.000 claims 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 6
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 5
- 125000001887 cyclopentyloxy group Chemical group C1(CCCC1)O* 0.000 claims 5
- 150000002431 hydrogen Chemical class 0.000 claims 5
- 238000004519 manufacturing process Methods 0.000 claims 5
- 230000003920 cognitive function Effects 0.000 claims 4
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 4
- 125000004438 haloalkoxy group Chemical group 0.000 claims 4
- 125000001188 haloalkyl group Chemical group 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 125000006578 monocyclic heterocycloalkyl group Chemical group 0.000 claims 4
- 125000004043 oxo group Chemical group O=* 0.000 claims 4
- 125000004076 pyridyl group Chemical group 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 239000011780 sodium chloride Substances 0.000 claims 4
- 230000000051 modifying Effects 0.000 claims 3
- 230000000694 effects Effects 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- OKKJLVBELUTLKV-UHFFFAOYSA-N methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 230000001430 anti-depressive Effects 0.000 claims 1
- 239000000935 antidepressant agent Substances 0.000 claims 1
- 125000004429 atoms Chemical group 0.000 claims 1
- 239000002775 capsule Substances 0.000 claims 1
- 125000006448 cycloalkyl cycloalkyl group Chemical group 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- KFZMGEQAYNKOFK-UHFFFAOYSA-N iso-propanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims 1
- DKGAVHZHDRPRBM-UHFFFAOYSA-N t-BuOH Chemical compound CC(C)(C)O DKGAVHZHDRPRBM-UHFFFAOYSA-N 0.000 claims 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261718285P | 2012-10-25 | 2012-10-25 | |
| US61/718,285 | 2012-10-25 | ||
| US201261733675P | 2012-12-05 | 2012-12-05 | |
| US61/733,675 | 2012-12-05 | ||
| US201361776937P | 2013-03-12 | 2013-03-12 | |
| US61/776,937 | 2013-03-12 | ||
| PCT/US2013/066645 WO2014066659A1 (en) | 2012-10-25 | 2013-10-24 | Heteroaryl inhibitors of pde4 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016505512A JP2016505512A (ja) | 2016-02-25 |
| JP2016505512A5 true JP2016505512A5 (US06780888-20040824-C00057.png) | 2016-12-15 |
| JP6289485B2 JP6289485B2 (ja) | 2018-03-07 |
Family
ID=50545269
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015539801A Active JP6289485B2 (ja) | 2012-10-25 | 2013-10-24 | Ｐｄｅ４のヘテロアリール阻害剤 |
Country Status (23)
Families Citing this family (52)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI633087B (zh) | 2012-06-13 | 2018-08-21 | 赫孚孟拉羅股份公司 | 新穎二氮雜螺環烷及氮雜螺環烷 |
| SI2900669T1 (sl) | 2012-09-25 | 2019-12-31 | F. Hoffmann-La Roche Ag | Derivati heksahidropirolo(3,4-C)pirola in sorodne spojine kot zaviralci avtotaksina (ATX) in kot zaviralci tvorbe lizofosfatidne kisline (LPA) za zdravljenje npr. bolezni ledvic |
| SI3842420T1 (sl) * | 2012-10-25 | 2023-04-28 | Tetra Discovery Partners Llc | Heteroarilni zaviralci PDE4 |
| ES2637716T3 (es) * | 2013-02-04 | 2017-10-16 | Grünenthal GmbH | Nuevos compuestos de pirimidina condensados sustituidos |
| EP2951161A1 (en) | 2013-02-04 | 2015-12-09 | Grünenthal GmbH | 4-amino substituted condensed pyrimidine compounds as pde4 inhibitors |
| AR095079A1 (es) | 2013-03-12 | 2015-09-16 | Hoffmann La Roche | Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo |
| SI3074400T1 (en) | 2013-11-26 | 2018-03-30 | F. Hoffmann-La Roche Ag | Octahydro-cyclobut (1,2-c, 3,4-cy) dipyrrole derivatives as autoantaxine inhibitors |
| AU2015238541B2 (en) | 2014-03-26 | 2019-09-19 | F. Hoffmann-La Roche Ag | Condensed [1,4]diazepine compounds as autotaxin (ATX) and lysophosphatidic acid (LPA) production inhibitors |
| AU2015238537B2 (en) | 2014-03-26 | 2019-08-01 | F. Hoffmann-La Roche Ag | Bicyclic compounds as autotaxin (ATX) and lysophosphatidic acid (LPA) production inhibitors |
| WO2016161268A1 (en) | 2015-04-01 | 2016-10-06 | Enanta Pharmaceuticals, Inc. | Hepatitis b antviral agents |
| MA41898A (fr) | 2015-04-10 | 2018-02-13 | Hoffmann La Roche | Dérivés de quinazolinone bicyclique |
| WO2016183266A1 (en) | 2015-05-13 | 2016-11-17 | Enanta Pharmaceuticals, Inc. | Ehpatitis b antiviral agents |
| US10179131B2 (en) | 2015-07-13 | 2019-01-15 | Enanta Pharmaceuticals, Inc. | Hepatitis B antiviral agents |
| US10301255B2 (en) | 2015-07-22 | 2019-05-28 | Enanta Pharmaceuticals, Inc. | Hepatitis B antiviral agents |
| PE20180479A1 (es) | 2015-09-04 | 2018-03-07 | Hoffmann La Roche | Nuevos derivados de fenoximetilo |
| JP6845230B2 (ja) | 2015-09-24 | 2021-03-17 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | デュアルａｔｘ／ｃａ阻害剤としての新規な二環式化合物 |
| PE20180552A1 (es) | 2015-09-24 | 2018-04-02 | Hoffmann La Roche | Nuevos compuestos biciclicos como inhibidores duales de atx/ca |
| MA42919A (fr) | 2015-09-24 | 2018-08-01 | Hoffmann La Roche | Composés bicycliques utilisés en tant qu'inhibiteurs d'atx |
| RU2018114289A (ru) | 2015-09-24 | 2019-10-24 | Ф. Хоффманн-Ля Рош Аг | Бициклические соединения в качестве ингибиторов аутотаксина (atx) |
| WO2017136403A1 (en) | 2016-02-02 | 2017-08-10 | Enanta Pharmaceuticals, Inc. | Hepatitis b antiviral agents |
| ES2938341T3 (es) | 2016-03-07 | 2023-04-10 | Enanta Pharm Inc | Agentes antivirales contra la hepatitis B |
| JP2019521972A (ja) * | 2016-06-10 | 2019-08-08 | エナンタ ファーマシューティカルズ インコーポレイテッド | Ｂ型肝炎抗ウイルス剤 |
| WO2018167001A1 (en) | 2017-03-16 | 2018-09-20 | F. Hoffmann-La Roche Ag | Heterocyclic compounds useful as dual atx/ca inhibitors |
| CN110382484B (zh) | 2017-03-16 | 2022-12-06 | 豪夫迈·罗氏有限公司 | 新的作为atx抑制剂的二环化合物 |
| CA3073986A1 (en) | 2017-08-28 | 2019-03-07 | Enanta Pharmaceuticals, Inc. | Hepatitis b antiviral agents |
| JP7216719B2 (ja) | 2017-09-20 | 2023-02-01 | ユニオン・セラピューティクス・アクティエセルスカブ | 置換ジヒドロチエノピリミジンおよびホスホジエステラーゼ阻害剤としてのその使用 |
| TW201936192A (zh) | 2017-12-06 | 2019-09-16 | 美商因那塔製藥公司 | B 型肝炎抗病毒試劑 |
| WO2019113173A1 (en) | 2017-12-06 | 2019-06-13 | Enanta Pharmaceuticals, Inc. | Hepatitis b antiviral agents |
| EP3724196B9 (en) | 2017-12-15 | 2023-03-22 | UNION therapeutics A/S | Substituted azetidine dihydrothienopyridines and their use as phosphodiesterase inhibitors |
| EP3724194B1 (en) | 2017-12-15 | 2023-12-27 | UNION therapeutics A/S | Substituted azetidine dihydrothienopyrimidines and their use as phosphodiesterase inhibitors |
| US11058678B2 (en) | 2018-01-22 | 2021-07-13 | Enanta Pharmaceuticals, Inc. | Substituted heterocycles as antiviral agents |
| WO2019191166A1 (en) | 2018-03-29 | 2019-10-03 | Enanta Pharmaceuticals, Inc. | Hepatitis b antiviral agents |
| CA3135420A1 (en) * | 2018-04-05 | 2019-10-10 | Universiteit Hasselt | Selective pde4d inhibitors against demyelinating diseases |
| CN108997394A (zh) * | 2018-06-12 | 2018-12-14 | 广州百霆医药科技有限公司 | 苯并氧杂硼杂环戊烷类化合物及其制备方法 |
| CN112955142A (zh) | 2018-09-21 | 2021-06-11 | 英安塔制药有限公司 | 官能化杂环化合物作为抗病毒剂 |
| CR20210163A (es) * | 2018-10-05 | 2021-06-24 | Pfizer | Inhibidores de pde4 que contienen boro |
| UY38483A (es) | 2018-11-21 | 2020-06-30 | Enanta Pharm Inc | Heterociclos funcionalizados como agentes antivirales |
| CN111635400A (zh) | 2019-03-02 | 2020-09-08 | 察略盛医药科技(上海)有限公司 | 吡唑并[1,5-a]吡啶类衍生物、及其制备方法和用途 |
| JP2022529698A (ja) * | 2019-04-18 | 2022-06-23 | テトラ ディスカバリー パートナーズ インコーポレイテッド | Ｐｄｅ４阻害剤の塩および多形 |
| EP3969458A4 (en) | 2019-05-13 | 2023-05-17 | Borah, Inc. | CHEMICAL COMPOUNDS |
| US11236111B2 (en) | 2019-06-03 | 2022-02-01 | Enanta Pharmaceuticals, Inc. | Hepatitis B antiviral agents |
| WO2020247575A1 (en) | 2019-06-04 | 2020-12-10 | Enanta Pharmaceuticals, Inc. | Hepatitis b antiviral agents |
| WO2020247561A1 (en) | 2019-06-04 | 2020-12-10 | Enanta Pharmaceuticals, Inc, | Hepatitis b antiviral agents |
| MX2022000140A (es) * | 2019-07-03 | 2022-04-27 | Borah Inc | Compuestos quimicos. |
| WO2021007488A1 (en) | 2019-07-11 | 2021-01-14 | Enanta Pharmaceuticals, Inc. | Substituted heterocycles as antiviral agents |
| WO2021055425A2 (en) | 2019-09-17 | 2021-03-25 | Enanta Pharmaceuticals, Inc. | Functionalized heterocycles as antiviral agents |
| US11802125B2 (en) | 2020-03-16 | 2023-10-31 | Enanta Pharmaceuticals, Inc. | Functionalized heterocyclic compounds as antiviral agents |
| CN114149410A (zh) * | 2020-09-07 | 2022-03-08 | 四川科伦博泰生物医药股份有限公司 | 吡啶并环类化合物及其制备方法和用途 |
| WO2022099284A1 (en) * | 2020-11-05 | 2022-05-12 | Young Biopharma, Llc | Novel capsaicin analogs and uses thereof |
| CN115521946B (zh) * | 2022-10-14 | 2024-06-21 | 浙江玖世生物科技有限公司 | 一种TiOx基光酶催化剂合成(R)-1-[3,5-二(三氟甲基)]苯乙醇的方法 |
| WO2024135840A1 (ja) * | 2022-12-23 | 2024-06-27 | 塩野義製薬株式会社 | Ｐｄｅ４阻害剤を含有するカプセル剤または顆粒 |
| WO2024179493A1 (zh) * | 2023-02-28 | 2024-09-06 | 上海翊石医药科技有限公司 | 二氢噻吩并嘧啶衍生物的制备方法和用途 |
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| DK23392D0 (da) | 1992-02-24 | 1992-02-24 | Novo Nordisk As | Heterocykliske forbindelser, deres anvendelse og fremstilling |
| FR2754260B1 (fr) | 1996-10-04 | 1998-10-30 | Adir | Nouveaux derives substitues de biphenyle ou de phenylpyridine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| AU5648599A (en) * | 1998-09-11 | 2000-04-03 | Kyorin Pharmaceutical Co. Ltd. | Phosphonic ester derivatives and process for producing the same |
| ES2289274T3 (es) | 2002-03-08 | 2008-02-01 | Eli Lilly And Company | Derivados de pirrol-2,5-diona y su uso como inhibidores de gsk-3. |
| US20050014767A1 (en) | 2003-01-29 | 2005-01-20 | Magnus Pfahl | Benzoxazole, benzothiazole, and benzimidazole derivatives for the treatment of cancer and other diseases |
| JP2006123639A (ja) | 2004-10-27 | 2006-05-18 | Mitsubishi Electric Corp | ホームドア状態認識システム |
| WO2006123639A1 (ja) * | 2005-05-18 | 2006-11-23 | Asahi Kasei Pharma Corporation | ピリミジン誘導体 |
| US20060293343A1 (en) | 2005-05-18 | 2006-12-28 | Asahi Kasei Pharma Corporation | Pyrimidine derivatives |
| US7919519B2 (en) | 2005-11-23 | 2011-04-05 | Epix Pharmaceuticals Inc. | S1P receptor modulating compounds and use thereof |
| WO2009146388A1 (en) | 2008-05-28 | 2009-12-03 | The Trustees Of Columbia University In The City Of New York | Voxel-based methods for assessing subjects using positron emission tomography |
| EP2348863A4 (en) * | 2008-09-04 | 2012-03-07 | Anacor Pharmaceuticals Inc | BORN SMALL MOLECULES |
| RU2380890C1 (ru) | 2008-10-17 | 2010-02-10 | Государственное образовательное учреждение высшего профессионального образования Марийский государственный технический университет | Способ испытания травяного покрова на прирусловой пойме реки |
| WO2010059838A2 (en) | 2008-11-20 | 2010-05-27 | Decode Genetics Ehf | Pde4 inhibitors selective for the long form of pde4 for treating inflammation and avoiding side effects |
| JP2012519160A (ja) * | 2009-02-27 | 2012-08-23 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Ｐｄｅ４阻害剤及びｎｓａｉｄを含有する組み合わせ薬 |
| EP2380890A1 (en) * | 2010-04-23 | 2011-10-26 | Almirall, S.A. | New 7,8-dihydro-1,6-naphthyridin-5(6h)-one-derivatives as PDE4 inhibitors |
| US8889123B2 (en) * | 2010-08-19 | 2014-11-18 | Allergan, Inc. | Compositions and soft tissue replacement methods |
| SI3842420T1 (sl) * | 2012-10-25 | 2023-04-28 | Tetra Discovery Partners Llc | Heteroarilni zaviralci PDE4 |
| ES2637716T3 (es) * | 2013-02-04 | 2017-10-16 | Grünenthal GmbH | Nuevos compuestos de pirimidina condensados sustituidos |
| WO2015048407A1 (en) | 2013-09-26 | 2015-04-02 | Tetra Discovery Partners, LLC | Heteroaryl inhibitors of pde4 |
| WO2016049595A1 (en) | 2014-09-26 | 2016-03-31 | Tetra Discovery Partners, LLC | Heteroaryl inhibitors of pde4 |
| JP2022529698A (ja) * | 2019-04-18 | 2022-06-23 | テトラ ディスカバリー パートナーズ インコーポレイテッド | Ｐｄｅ４阻害剤の塩および多形 |
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2013
- 2013-10-24 SI SI201332034T patent/SI3842420T1/sl unknown
- 2013-10-24 KR KR1020157010502A patent/KR102189560B1/ko active IP Right Grant
- 2013-10-24 PT PT138487392T patent/PT2912019T/pt unknown
- 2013-10-24 CN CN201380055959.9A patent/CN104768932B/zh active Active
- 2013-10-24 EP EP13848739.2A patent/EP2912019B1/en active Active
- 2013-10-24 PL PL13848739T patent/PL2912019T3/pl unknown
- 2013-10-24 SG SG11201502050XA patent/SG11201502050XA/en unknown
- 2013-10-24 JP JP2015539801A patent/JP6289485B2/ja active Active
- 2013-10-24 ES ES13848739T patent/ES2871821T3/es active Active
- 2013-10-24 HR HRP20230162TT patent/HRP20230162T1/hr unknown
- 2013-10-24 CA CA2886263A patent/CA2886263C/en active Active
- 2013-10-24 DK DK13848739.2T patent/DK2912019T3/da active
- 2013-10-24 MX MX2015005015A patent/MX368959B/es active IP Right Grant
- 2013-10-24 WO PCT/US2013/066645 patent/WO2014066659A1/en active Application Filing
- 2013-10-24 LT LTEP21156065.1T patent/LT3842420T/lt unknown
- 2013-10-24 EP EP21156065.1A patent/EP3842420B1/en active Active
- 2013-10-24 BR BR112015009168-7A patent/BR112015009168B1/pt active IP Right Grant
- 2013-10-24 US US14/349,688 patent/US9221843B2/en active Active
- 2013-10-24 NZ NZ705881A patent/NZ705881A/en unknown
- 2013-10-24 HU HUE13848739A patent/HUE056251T2/hu unknown
- 2013-10-24 AU AU2013334236A patent/AU2013334236B2/en active Active
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2015
- 2015-04-21 IL IL238409A patent/IL238409A/en active IP Right Grant
- 2015-04-24 CL CL2015001068A patent/CL2015001068A1/es unknown
- 2015-09-04 HK HK15108659.8A patent/HK1208026A1/xx unknown
- 2015-11-11 US US14/938,544 patent/US9777024B2/en active Active
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2017
- 2017-08-18 US US15/680,842 patent/US10093686B2/en active Active
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2018
- 2018-08-24 US US16/111,700 patent/US10364258B2/en active Active
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2019
- 2019-04-26 US US16/396,457 patent/US10626129B2/en active Active
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2020
- 2020-02-04 US US16/781,748 patent/US11401286B2/en active Active
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2022
- 2022-06-23 US US17/808,439 patent/US11767334B2/en active Active
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2023
- 2023-07-11 US US18/350,452 patent/US20230348501A1/en active Pending
