JP2016510784A5 - - Google Patents
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- Publication number
- JP2016510784A5 JP2016510784A5 JP2015562112A JP2015562112A JP2016510784A5 JP 2016510784 A5 JP2016510784 A5 JP 2016510784A5 JP 2015562112 A JP2015562112 A JP 2015562112A JP 2015562112 A JP2015562112 A JP 2015562112A JP 2016510784 A5 JP2016510784 A5 JP 2016510784A5
- Authority
- JP
- Japan
- Prior art keywords
- alkylene
- alkyl
- ring
- haloalkyl
- independently selected
- 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
- 229910052717 sulfur Inorganic materials 0.000 claims description 74
- 229910052757 nitrogen Inorganic materials 0.000 claims description 64
- 125000004432 carbon atom Chemical group C* 0.000 claims description 50
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 44
- 229910052760 oxygen Inorganic materials 0.000 claims description 43
- 150000001875 compounds Chemical class 0.000 claims description 38
- 125000005842 heteroatom Chemical group 0.000 claims description 36
- 229910052739 hydrogen Inorganic materials 0.000 claims description 33
- 229910052736 halogen Inorganic materials 0.000 claims description 30
- 150000002367 halogens Chemical class 0.000 claims description 30
- 229910052799 carbon Inorganic materials 0.000 claims description 27
- 125000003118 aryl group Chemical group 0.000 claims description 26
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims description 20
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 19
- 150000003839 salts Chemical class 0.000 claims description 19
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 16
- 229920006395 saturated elastomer Polymers 0.000 claims description 16
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims description 15
- 239000003112 inhibitor Substances 0.000 claims description 14
- 125000006173 tetrahydropyranylmethyl group Chemical group 0.000 claims description 13
- 229910052731 fluorine Inorganic materials 0.000 claims description 12
- 125000001072 heteroaryl group Chemical group 0.000 claims description 10
- 239000008194 pharmaceutical composition Substances 0.000 claims description 8
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims description 5
- 229910052794 bromium Inorganic materials 0.000 claims description 4
- 229910052801 chlorine Inorganic materials 0.000 claims description 4
- 230000001225 therapeutic effect Effects 0.000 claims description 4
- 239000005557 antagonist Substances 0.000 claims description 3
- 239000003814 drug Substances 0.000 claims description 3
- 230000000694 effects Effects 0.000 claims description 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 3
- 201000001320 Atherosclerosis Diseases 0.000 claims description 2
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims description 2
- 102100029921 Dipeptidyl peptidase 1 Human genes 0.000 claims description 2
- 101710087078 Dipeptidyl peptidase 1 Proteins 0.000 claims description 2
- 208000027004 Eosinophilic disease Diseases 0.000 claims description 2
- 208000017189 Gastrointestinal inflammatory disease Diseases 0.000 claims description 2
- 229940122236 Histamine receptor antagonist Drugs 0.000 claims description 2
- 101000577881 Homo sapiens Macrophage metalloelastase Proteins 0.000 claims description 2
- 101000990902 Homo sapiens Matrix metalloproteinase-9 Proteins 0.000 claims description 2
- 102100027998 Macrophage metalloelastase Human genes 0.000 claims description 2
- 102100030412 Matrix metalloproteinase-9 Human genes 0.000 claims description 2
- 229940121948 Muscarinic receptor antagonist Drugs 0.000 claims description 2
- 229940123932 Phosphodiesterase 4 inhibitor Drugs 0.000 claims description 2
- 108050000258 Prostaglandin D receptors Proteins 0.000 claims description 2
- 102100024218 Prostaglandin D2 receptor 2 Human genes 0.000 claims description 2
- 208000026935 allergic disease Diseases 0.000 claims description 2
- 208000006673 asthma Diseases 0.000 claims description 2
- 230000003454 betamimetic effect Effects 0.000 claims description 2
- 239000000812 cholinergic antagonist Substances 0.000 claims description 2
- 239000003246 corticosteroid Substances 0.000 claims description 2
- 229940121647 egfr inhibitor Drugs 0.000 claims description 2
- 208000015181 infectious disease Diseases 0.000 claims description 2
- 244000000010 microbial pathogen Species 0.000 claims description 2
- 239000002587 phosphodiesterase IV inhibitor Substances 0.000 claims description 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 4
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 239000000739 antihistaminic agent Substances 0.000 claims 1
- 239000003073 chemokine receptor CCR9 antagonist Substances 0.000 claims 1
- 230000006806 disease prevention Effects 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 1
- 201000010099 disease Diseases 0.000 description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- 102100022718 Atypical chemokine receptor 2 Human genes 0.000 description 1
- 101000678892 Homo sapiens Atypical chemokine receptor 2 Proteins 0.000 description 1
- 101000716070 Homo sapiens C-C chemokine receptor type 9 Proteins 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 239000013543 active substance Substances 0.000 description 1
- 125000000217 alkyl group Chemical group 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP13159245 | 2013-03-14 | ||
| EP13159245.3 | 2013-03-14 | ||
| EP13170008.0 | 2013-05-31 | ||
| EP13170008 | 2013-05-31 | ||
| PCT/EP2014/054798 WO2014140078A1 (en) | 2013-03-14 | 2014-03-12 | Substituted 2-aza-bicyclo[2.2.1]heptane-3-carboxylic acid (cyano-methyl)-amides inhibitors of cathepsin c |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016510784A JP2016510784A (ja) | 2016-04-11 |
| JP2016510784A5 true JP2016510784A5 (https=) | 2017-04-13 |
| JP6441830B2 JP6441830B2 (ja) | 2018-12-19 |
Family
ID=50241452
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015562112A Active JP6441830B2 (ja) | 2013-03-14 | 2014-03-12 | カテプシンｃの置換２−アザ−ビシクロ［２．２．１］ヘプタン−３−カルボン酸（シアノ−メチル）−アミド阻害剤 |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US8871783B2 (https=) |
| EP (1) | EP2970228B1 (https=) |
| JP (1) | JP6441830B2 (https=) |
| WO (1) | WO2014140078A1 (https=) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NO2699580T3 (https=) | 2014-01-24 | 2018-02-24 | ||
| HUE070049T2 (hu) | 2018-03-01 | 2025-05-28 | Astrazeneca Ab | (2S)-{(1S)-1-ciano-2-[4-(3-metil-2-oxo-2,3-dihidro-1,3-benzoxazol-5-il)fenil]etil} -1,4-oxazepán-2-karboxamidot tartalmazó gyógyászati készítmények |
| WO2020018547A1 (en) | 2018-07-17 | 2020-01-23 | Insmed Incorporated | Certain (2s)-n-[(1s)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides for treating lupus nephritis |
| US11399231B2 (en) | 2019-09-27 | 2022-07-26 | United States Of America As Represented By The Administrator Of Nasa | Extreme low frequency microphone/hydrophone for exploration of oceanic and atmospheric dynamics |
| CN118496197A (zh) | 2019-12-20 | 2024-08-16 | 拜耳公司 | 取代的噻吩甲酰胺、噻吩甲酸及其衍生物 |
| EP4182700A4 (en) | 2020-07-20 | 2024-11-13 | Insmed Incorporated | METHODS FOR EXTRACTING NEUTROPHIL SERINE PROTEASES AND TREATMENT OF DIPETIDYL PEPTIDASE-1-MEDIATED DISEASES |
| CN115996923B (zh) * | 2020-08-26 | 2025-07-18 | 海思科医药集团股份有限公司 | 一种作为二肽基肽酶1抑制剂的腈衍生物及其用途 |
| EP4450497A4 (en) * | 2022-01-11 | 2025-11-26 | Shanghai Yidian Pharmaceutical Tech Development Co Ltd | NITRILE PEPTIDYL COMPOUND AND ITS USES |
| US20240124450A1 (en) | 2022-09-21 | 2024-04-18 | Pfizer Inc. | Novel SIK Inhibitors |
| JP2026503035A (ja) | 2023-01-06 | 2026-01-27 | インスメッド インコーポレイテッド | 新規な可逆性ｄｐｐ１阻害剤及びその用途 |
| EP4688750A1 (en) | 2023-04-06 | 2026-02-11 | Pfizer Inc. | Substituted indazole propionic acid derivative compounds and uses thereof as ampk activators |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2439415C (en) * | 2001-03-02 | 2011-09-20 | Merck Frosst Canada & Co. | Cathepsin cysteine protease inhibitors |
| JP2006527704A (ja) * | 2003-06-18 | 2006-12-07 | プロザイメックス・アクティーゼルスカブ | プロテアーゼ阻害剤 |
| WO2009047829A1 (ja) | 2007-10-12 | 2009-04-16 | Fujitsu Limited | Ｉｐ電話自動試験システム及び方法 |
| US7902181B2 (en) * | 2007-12-12 | 2011-03-08 | Astrazeneca Ab | Compounds 010 |
| MX2011011661A (es) | 2009-05-07 | 2011-11-18 | Astrazeneca Ab | Compuestos 1-cianoetilheterociclilcarboxamida sustituidos 750. |
| WO2010142985A1 (en) | 2009-06-10 | 2010-12-16 | Astrazeneca Ab | Substituted n-[1-cyano-2-(phenyl)ethyl]piperidin-2-ylcarboxmide compounds 761 |
| WO2011154677A1 (en) * | 2010-06-09 | 2011-12-15 | Astrazeneca Ab | Substituted n-[1-cyano-2-(phenyl)ethyl] 1-aminocycloalk-1-ylcarboxamide compounds - 760 |
| WO2012119941A1 (en) | 2011-03-04 | 2012-09-13 | Prozymex A/S | Peptidyl nitrilcompounds as peptidase inhibitors |
| US8999975B2 (en) | 2011-09-19 | 2015-04-07 | Boehringer Ingelheim International Gmbh | Substituted N- [1-cyano-2- (phenyl) ethyl] -2-azabicyclo [2.2.1] heptane-3-carboxamide inhibitors of cathepsin C |
-
2014
- 2014-03-12 EP EP14709317.3A patent/EP2970228B1/en active Active
- 2014-03-12 JP JP2015562112A patent/JP6441830B2/ja active Active
- 2014-03-12 WO PCT/EP2014/054798 patent/WO2014140078A1/en not_active Ceased
- 2014-03-12 US US14/205,881 patent/US8871783B2/en active Active
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