JP2018515594A5 - - Google Patents
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- Publication number
- JP2018515594A5 JP2018515594A5 JP2017567558A JP2017567558A JP2018515594A5 JP 2018515594 A5 JP2018515594 A5 JP 2018515594A5 JP 2017567558 A JP2017567558 A JP 2017567558A JP 2017567558 A JP2017567558 A JP 2017567558A JP 2018515594 A5 JP2018515594 A5 JP 2018515594A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- alkyloxy
- fluoro
- chloro
- acceptable salt
- 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
- 125000003545 alkoxy group Chemical group 0.000 claims 21
- 125000000217 alkyl group Chemical group 0.000 claims 19
- 150000001875 compounds Chemical class 0.000 claims 19
- 125000001153 fluoro group Chemical group F* 0.000 claims 14
- 150000003839 salts Chemical class 0.000 claims 13
- 229910052736 halogen Inorganic materials 0.000 claims 11
- 150000002367 halogens Chemical class 0.000 claims 10
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 7
- 125000004769 (C1-C4) alkylsulfonyl group Chemical group 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- DLFVBJFMPXGRIB-UHFFFAOYSA-N Acetamide Chemical compound CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- IVOMOUWHDPKRLL-KQYNXXCUSA-N Cyclic adenosine monophosphate Chemical compound C([C@H]1O2)OP(O)(=O)O[C@H]1[C@@H](O)[C@@H]2N1C(N=CN=C2N)=C2N=C1 IVOMOUWHDPKRLL-KQYNXXCUSA-N 0.000 claims 3
- IVOMOUWHDPKRLL-UHFFFAOYSA-N UNPD107823 Natural products O1C2COP(O)(=O)OC2C(O)C1N1C(N=CN=C2N)=C2N=C1 IVOMOUWHDPKRLL-UHFFFAOYSA-N 0.000 claims 3
- 125000001309 chloro group Chemical group Cl* 0.000 claims 3
- 229940095074 cyclic amp Drugs 0.000 claims 3
- 230000003834 intracellular effect Effects 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 230000011664 signaling Effects 0.000 claims 3
- 238000002560 therapeutic procedure Methods 0.000 claims 3
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 3
- 125000006284 3-fluorobenzyl group Chemical group [H]C1=C([H])C(=C([H])C(F)=C1[H])C([H])([H])* 0.000 claims 2
- 208000010061 Autosomal Dominant Polycystic Kidney Diseases 0.000 claims 2
- 208000002814 Autosomal Recessive Polycystic Kidney Diseases 0.000 claims 2
- 208000017354 Autosomal recessive polycystic kidney disease Diseases 0.000 claims 2
- 108091006027 G proteins Proteins 0.000 claims 2
- 102000030782 GTP binding Human genes 0.000 claims 2
- 108091000058 GTP-Binding Proteins 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 206010060862 Prostate cancer Diseases 0.000 claims 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 2
- 208000022185 autosomal dominant polycystic kidney disease Diseases 0.000 claims 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 230000001404 mediated effect Effects 0.000 claims 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 2
- 125000004847 2-fluorobenzyl group Chemical group [H]C1=C([H])C(F)=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 125000002774 3,4-dimethoxybenzyl group Chemical group [H]C1=C([H])C(=C([H])C(OC([H])([H])[H])=C1OC([H])([H])[H])C([H])([H])* 0.000 claims 1
- 125000003852 3-chlorobenzyl group Chemical group [H]C1=C([H])C(=C([H])C(Cl)=C1[H])C([H])([H])* 0.000 claims 1
- 125000006497 3-methoxybenzyl group Chemical group [H]C1=C([H])C(=C([H])C(OC([H])([H])[H])=C1[H])C([H])([H])* 0.000 claims 1
- 125000004176 4-fluorobenzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1F)C([H])([H])* 0.000 claims 1
- 208000030507 AIDS Diseases 0.000 claims 1
- 208000003200 Adenoma Diseases 0.000 claims 1
- 208000006468 Adrenal Cortex Neoplasms Diseases 0.000 claims 1
- 241000193738 Bacillus anthracis Species 0.000 claims 1
- 231100000699 Bacterial toxin Toxicity 0.000 claims 1
- 201000009030 Carcinoma Diseases 0.000 claims 1
- 206010007572 Cardiac hypertrophy Diseases 0.000 claims 1
- 208000006029 Cardiomegaly Diseases 0.000 claims 1
- 206010008631 Cholera Diseases 0.000 claims 1
- 201000003874 Common Variable Immunodeficiency Diseases 0.000 claims 1
- 206010058314 Dysplasia Diseases 0.000 claims 1
- 102000003688 G-Protein-Coupled Receptors Human genes 0.000 claims 1
- 108090000045 G-Protein-Coupled Receptors Proteins 0.000 claims 1
- 206010064571 Gene mutation Diseases 0.000 claims 1
- 101001014590 Homo sapiens Guanine nucleotide-binding protein G(s) subunit alpha isoforms XLas Proteins 0.000 claims 1
- 101001014594 Homo sapiens Guanine nucleotide-binding protein G(s) subunit alpha isoforms short Proteins 0.000 claims 1
- 101001014610 Homo sapiens Neuroendocrine secretory protein 55 Proteins 0.000 claims 1
- 101000797903 Homo sapiens Protein ALEX Proteins 0.000 claims 1
- 206010020850 Hyperthyroidism Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 201000005702 Pertussis Diseases 0.000 claims 1
- 208000010067 Pituitary ACTH Hypersecretion Diseases 0.000 claims 1
- 208000007913 Pituitary Neoplasms Diseases 0.000 claims 1
- 201000005746 Pituitary adenoma Diseases 0.000 claims 1
- 206010061538 Pituitary tumour benign Diseases 0.000 claims 1
- 208000020627 Pituitary-dependent Cushing syndrome Diseases 0.000 claims 1
- 208000012287 Prolapse Diseases 0.000 claims 1
- 208000024313 Testicular Neoplasms Diseases 0.000 claims 1
- 206010057644 Testis cancer Diseases 0.000 claims 1
- 230000004913 activation Effects 0.000 claims 1
- 210000004404 adrenal cortex Anatomy 0.000 claims 1
- 208000021033 autosomal dominant polycystic liver disease Diseases 0.000 claims 1
- 239000000688 bacterial toxin Substances 0.000 claims 1
- 210000000845 cartilage Anatomy 0.000 claims 1
- -1 chloro, methoxy Chemical group 0.000 claims 1
- 230000007812 deficiency Effects 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 229940088597 hormone Drugs 0.000 claims 1
- 239000005556 hormone Substances 0.000 claims 1
- 230000003902 lesion Effects 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 125000003564 m-cyanobenzyl group Chemical group [H]C1=C([H])C(=C([H])C(C#N)=C1[H])C([H])([H])* 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 230000035772 mutation Effects 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 208000021310 pituitary gland adenoma Diseases 0.000 claims 1
- 208000030761 polycystic kidney disease Diseases 0.000 claims 1
- 208000028589 polycystic liver disease Diseases 0.000 claims 1
- 208000001061 polyostotic fibrous dysplasia Diseases 0.000 claims 1
- 102000005962 receptors Human genes 0.000 claims 1
- 108020003175 receptors Proteins 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 201000003120 testicular cancer Diseases 0.000 claims 1
- 201000008827 tuberculosis Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB1504763.2 | 2015-03-20 | ||
| GBGB1504763.2A GB201504763D0 (en) | 2015-03-20 | 2015-03-20 | Compounds and uses |
| PCT/GB2016/050766 WO2016151300A1 (en) | 2015-03-20 | 2016-03-18 | Triazole derivatives and their use as pde4 activators |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018515594A JP2018515594A (ja) | 2018-06-14 |
| JP2018515594A5 true JP2018515594A5 (https=) | 2019-04-25 |
| JP6694452B2 JP6694452B2 (ja) | 2020-05-13 |
Family
ID=53052153
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017567558A Active JP6694452B2 (ja) | 2015-03-20 | 2016-03-18 | トリアゾール誘導体およびｐｄｅ４活性化体としてその使用 |
Country Status (5)
| Country | Link |
|---|---|
| US (2) | US10385027B2 (https=) |
| EP (1) | EP3271338B1 (https=) |
| JP (1) | JP6694452B2 (https=) |
| GB (1) | GB201504763D0 (https=) |
| WO (1) | WO2016151300A1 (https=) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201504763D0 (en) | 2015-03-20 | 2015-05-06 | Mironid Ltd | Compounds and uses |
| GB201616439D0 (en) * | 2016-09-28 | 2016-11-09 | Mironid Limited | Compounds and uses |
| GB201805527D0 (en) * | 2018-04-04 | 2018-05-16 | Mironid Ltd | Compounds and their use as pde4 activators |
| WO2021127190A1 (en) | 2019-12-17 | 2021-06-24 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
| GB202102088D0 (en) | 2021-02-15 | 2021-03-31 | Mironid Ltd | Compounds and their use as pde4 activators |
| GB202212000D0 (en) | 2022-08-17 | 2022-09-28 | Mironid Ltd | Compounds and their use as PDE4 activators |
| GB202211999D0 (en) | 2022-08-17 | 2022-09-28 | Mironid Ltd | Compounds and their use as PDE4 activators |
Family Cites Families (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP3890453B2 (ja) | 1996-09-18 | 2007-03-07 | リードケミカル株式会社 | 新規２，４−ジオキソピロリジンおよび２，４−ジオキソテトラヒドロフラン誘導体及び該化合物を有効成分とする医薬 |
| JP2006518738A (ja) | 2003-02-12 | 2006-08-17 | トランス テック ファーマ，インコーポレイテッド | 治療薬としての置換アゾール誘導体 |
| EP1613590A2 (en) * | 2003-04-16 | 2006-01-11 | Memory Pharmaceutical Corporation | 4-(3,4-disubstituted phenyl)-pyrrolidin-2-one compounds as phosphodiesterase 4 inhibitors |
| US7056932B2 (en) | 2003-12-19 | 2006-06-06 | Hoffman-La Roche Inc. | Heterocyclyl substituted 1-alkoxy acetic acid amides |
| US20070191711A1 (en) | 2006-02-15 | 2007-08-16 | Misonix, Incorporated | Liquid processing and handling apparatus and associated method for use in medical procedures |
| EP2013176A2 (en) | 2006-02-27 | 2009-01-14 | Sterix Limited | Diaryl compounds as non-steroidal inhibitors of 17-beta hydroxysteroid dehydrogenase and/or steroid sulphatase for the treatment of oestrogen-related diseases such as hormone dependent breast cancer |
| DE102006024024A1 (de) * | 2006-05-23 | 2007-11-29 | Bayer Healthcare Aktiengesellschaft | Substituierte Arylimidazolone und -triazolone sowie ihre Verwendung |
| EP2057152A1 (de) * | 2006-08-07 | 2009-05-13 | Boehringer Ingelheim International GmbH | Enantiomerenreine betaagonisten, verfahren zu deren herstellung und deren verwendung als arzneimittel |
| WO2009131956A1 (en) | 2008-04-21 | 2009-10-29 | Institute For Oneworld Health | Compounds, compositions and methods comprising triazole derivatives |
| US20100144733A1 (en) | 2008-04-28 | 2010-06-10 | Institute For Oneworld Health | Compounds, compositions and methods comprising heteroaromatic derivatives |
| 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 |
| DE102009013642A1 (de) * | 2009-03-18 | 2010-09-23 | Bayer Schering Pharma Aktiengesellschaft | Substituierte Phenylalaninderivate und deren Verwendung |
| US8343976B2 (en) | 2009-04-20 | 2013-01-01 | Institute For Oneworld Health | Compounds, compositions and methods comprising pyrazole derivatives |
| ES2700877T3 (es) | 2009-05-12 | 2019-02-19 | Koninklijke Philips Nv | Fosfodiesterasa 4D7 como marcador de cáncer de próstata |
| ES2707598T3 (es) | 2009-05-12 | 2019-04-04 | Koninklijke Philips Nv | Fosfodiesterasa 4D7 como marcador para cáncer maligno de próstata sensible a hormonas |
| MX341050B (es) | 2010-04-07 | 2016-08-05 | Celgene Corp * | Metodos para tratar infeccion viral respiratoria. |
| EP2742030B1 (de) | 2011-08-11 | 2016-07-27 | Bayer Intellectual Property GmbH | 1,2,4-triazolyl-substituierte ketoenole zum einsatz im pflanzenschutz |
| US8642774B2 (en) * | 2011-12-08 | 2014-02-04 | Boehringer Ingelheim International Gmbh | Compounds |
| US8889677B2 (en) * | 2012-01-17 | 2014-11-18 | Boehringer Ingellheim International GmbH | Substituted triazoles useful as mGlu5 receptor modulators |
| CN105228616B (zh) | 2013-03-15 | 2019-05-03 | 实发生物医学公司 | 抗前蛋白转化酶枯草杆菌蛋白酶Kexin 9型（抗PCSK9）化合物及其用于治疗和/或预防心血管疾病的方法 |
| US20170087129A1 (en) | 2014-05-16 | 2017-03-30 | Celgene Corporation | Compositions and methods for the treatment of atherosclerotic cardiovascular diseases with pde4 modulators |
| GB201504763D0 (en) | 2015-03-20 | 2015-05-06 | Mironid Ltd | Compounds and uses |
| WO2017044828A1 (en) | 2015-09-11 | 2017-03-16 | VenatoRx Pharmaceuticals, Inc. | Beta-lactamase inhibitors |
| GB201616439D0 (en) | 2016-09-28 | 2016-11-09 | Mironid Limited | Compounds and uses |
-
2015
- 2015-03-20 GB GBGB1504763.2A patent/GB201504763D0/en not_active Ceased
-
2016
- 2016-03-18 WO PCT/GB2016/050766 patent/WO2016151300A1/en not_active Ceased
- 2016-03-18 JP JP2017567558A patent/JP6694452B2/ja active Active
- 2016-03-18 EP EP16712412.2A patent/EP3271338B1/en active Active
- 2016-03-18 US US15/559,875 patent/US10385027B2/en active Active
-
2019
- 2019-07-10 US US16/508,001 patent/US10793531B2/en active Active
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