JP2009538327A5 - - Google Patents
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- Publication number
- JP2009538327A5 JP2009538327A5 JP2009512222A JP2009512222A JP2009538327A5 JP 2009538327 A5 JP2009538327 A5 JP 2009538327A5 JP 2009512222 A JP2009512222 A JP 2009512222A JP 2009512222 A JP2009512222 A JP 2009512222A JP 2009538327 A5 JP2009538327 A5 JP 2009538327A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- optionally substituted
- alkyl
- piperidinyl
- activating protease
- 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.)
- Pending
Links
- 150000001875 compounds Chemical class 0.000 claims description 31
- 238000000034 method Methods 0.000 claims description 12
- 108091005804 Peptidases Proteins 0.000 claims description 11
- 239000004365 Protease Substances 0.000 claims description 11
- 230000003213 activating effect Effects 0.000 claims description 11
- 239000008194 pharmaceutical composition Substances 0.000 claims description 8
- 150000003839 salts Chemical class 0.000 claims description 8
- 239000003814 drug Substances 0.000 claims description 7
- 229940124597 therapeutic agent Drugs 0.000 claims description 6
- 210000004027 cell Anatomy 0.000 claims description 4
- 241001465754 Metazoa Species 0.000 claims description 3
- 230000001404 mediated effect Effects 0.000 claims description 3
- 230000000954 anitussive effect Effects 0.000 claims description 2
- 229940121363 anti-inflammatory agent Drugs 0.000 claims description 2
- 239000002260 anti-inflammatory agent Substances 0.000 claims description 2
- 239000000739 antihistaminic agent Substances 0.000 claims description 2
- 229940124584 antitussives Drugs 0.000 claims description 2
- 210000000424 bronchial epithelial cell Anatomy 0.000 claims description 2
- 229940124630 bronchodilator Drugs 0.000 claims description 2
- 125000000217 alkyl group Chemical group 0.000 claims 16
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 10
- 102000035195 Peptidases Human genes 0.000 claims 9
- 229910052799 carbon Inorganic materials 0.000 claims 8
- -1 methylenecyclohexyl Chemical group 0.000 claims 8
- 125000003386 piperidinyl group Chemical group 0.000 claims 8
- 229910052739 hydrogen Inorganic materials 0.000 claims 7
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 6
- 101000798702 Homo sapiens Transmembrane protease serine 4 Proteins 0.000 claims 6
- 102100032471 Transmembrane protease serine 4 Human genes 0.000 claims 6
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 5
- 125000000623 heterocyclic group Chemical group 0.000 claims 5
- 125000001544 thienyl group Chemical group 0.000 claims 5
- 125000006705 (C5-C7) cycloalkyl group Chemical group 0.000 claims 4
- 102100029500 Prostasin Human genes 0.000 claims 4
- 102100037942 Suppressor of tumorigenicity 14 protein Human genes 0.000 claims 4
- 125000003118 aryl group Chemical group 0.000 claims 4
- 229910052760 oxygen Inorganic materials 0.000 claims 4
- 108010031970 prostasin Proteins 0.000 claims 4
- HPXRVTGHNJAIIH-UHFFFAOYSA-N cyclohexanol Chemical compound OC1CCCCC1 HPXRVTGHNJAIIH-UHFFFAOYSA-N 0.000 claims 3
- 125000002541 furyl group Chemical group 0.000 claims 3
- 125000001072 heteroaryl group Chemical group 0.000 claims 3
- 125000002883 imidazolyl group Chemical group 0.000 claims 3
- 125000002950 monocyclic group Chemical group 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- 102100022046 Brain-specific serine protease 4 Human genes 0.000 claims 2
- 108010059081 Cathepsin A Proteins 0.000 claims 2
- 102000005572 Cathepsin A Human genes 0.000 claims 2
- 101000897856 Homo sapiens Adenylyl cyclase-associated protein 2 Proteins 0.000 claims 2
- 101000896891 Homo sapiens Brain-specific serine protease 4 Proteins 0.000 claims 2
- 101000836079 Homo sapiens Serpin B8 Proteins 0.000 claims 2
- 101000836075 Homo sapiens Serpin B9 Proteins 0.000 claims 2
- 101000661807 Homo sapiens Suppressor of tumorigenicity 14 protein Proteins 0.000 claims 2
- 101000598054 Homo sapiens Transmembrane protease serine 11B Proteins 0.000 claims 2
- 101000637855 Homo sapiens Transmembrane protease serine 11E Proteins 0.000 claims 2
- 101000798707 Homo sapiens Transmembrane protease serine 13 Proteins 0.000 claims 2
- 101000638154 Homo sapiens Transmembrane protease serine 2 Proteins 0.000 claims 2
- 101000798700 Homo sapiens Transmembrane protease serine 3 Proteins 0.000 claims 2
- 108010028275 Leukocyte Elastase Proteins 0.000 claims 2
- 108010091175 Matriptase Proteins 0.000 claims 2
- 101100069392 Mus musculus Gzma gene Proteins 0.000 claims 2
- 102100033174 Neutrophil elastase Human genes 0.000 claims 2
- XYFCBTPGUUZFHI-UHFFFAOYSA-N Phosphine Chemical compound P XYFCBTPGUUZFHI-UHFFFAOYSA-N 0.000 claims 2
- 102100037023 Transmembrane protease serine 11B Human genes 0.000 claims 2
- 102100032001 Transmembrane protease serine 11E Human genes 0.000 claims 2
- 102100032467 Transmembrane protease serine 13 Human genes 0.000 claims 2
- 102100031989 Transmembrane protease serine 2 Human genes 0.000 claims 2
- 108090000631 Trypsin Proteins 0.000 claims 2
- 102000004142 Trypsin Human genes 0.000 claims 2
- 125000001475 halogen functional group Chemical group 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 239000012588 trypsin Substances 0.000 claims 2
- 206010006458 Bronchitis chronic Diseases 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 201000003883 Cystic fibrosis Diseases 0.000 claims 1
- 102000016911 Deoxyribonucleases Human genes 0.000 claims 1
- 108010053770 Deoxyribonucleases Proteins 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000016285 Movement disease Diseases 0.000 claims 1
- 206010036790 Productive cough Diseases 0.000 claims 1
- 206010057190 Respiratory tract infections Diseases 0.000 claims 1
- GUGOEEXESWIERI-UHFFFAOYSA-N Terfenadine Chemical compound C1=CC(C(C)(C)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 GUGOEEXESWIERI-UHFFFAOYSA-N 0.000 claims 1
- 238000009825 accumulation Methods 0.000 claims 1
- 239000000654 additive Substances 0.000 claims 1
- 230000000996 additive effect Effects 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 230000001387 anti-histamine Effects 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims 1
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 claims 1
- 230000003115 biocidal effect Effects 0.000 claims 1
- 206010006451 bronchitis Diseases 0.000 claims 1
- 208000007451 chronic bronchitis Diseases 0.000 claims 1
- 230000001886 ciliary effect Effects 0.000 claims 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 125000005959 diazepanyl group Chemical group 0.000 claims 1
- PCHPORCSPXIHLZ-UHFFFAOYSA-N diphenhydramine hydrochloride Chemical compound [Cl-].C=1C=CC=CC=1C(OCC[NH+](C)C)C1=CC=CC=C1 PCHPORCSPXIHLZ-UHFFFAOYSA-N 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 210000000981 epithelium Anatomy 0.000 claims 1
- 239000012530 fluid Substances 0.000 claims 1
- 150000004677 hydrates Chemical class 0.000 claims 1
- 230000037427 ion transport Effects 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 210000003097 mucus Anatomy 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 210000004789 organ system Anatomy 0.000 claims 1
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 1
- 229910000073 phosphorus hydride Inorganic materials 0.000 claims 1
- 210000002345 respiratory system Anatomy 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 210000003802 sputum Anatomy 0.000 claims 1
- 208000024794 sputum Diseases 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 1
- 125000003039 tetrahydroisoquinolinyl group Chemical group C1(NCCC2=CC=CC=C12)* 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 102100037486 Reverse transcriptase/ribonuclease H Human genes 0.000 description 2
- WNNNWFKQCKFSDK-SCSAIBSYSA-N (2r)-2-azaniumylpent-4-enoate Chemical compound [O-]C(=O)[C@H]([NH3+])CC=C WNNNWFKQCKFSDK-SCSAIBSYSA-N 0.000 description 1
- 241000282412 Homo Species 0.000 description 1
- 239000003242 anti bacterial agent Substances 0.000 description 1
- 229940088710 antibiotic agent Drugs 0.000 description 1
- 229940125715 antihistaminic agent Drugs 0.000 description 1
- 239000003434 antitussive agent Substances 0.000 description 1
- 239000000168 bronchodilator agent Substances 0.000 description 1
- 210000005260 human cell Anatomy 0.000 description 1
- 210000000056 organ Anatomy 0.000 description 1
- 230000001575 pathological effect Effects 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US80298306P | 2006-05-23 | 2006-05-23 | |
| US86060406P | 2006-11-22 | 2006-11-22 | |
| PCT/US2007/069059 WO2007137080A2 (en) | 2006-05-23 | 2007-05-16 | Compounds and compositions as channel activating protease inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2009538327A JP2009538327A (ja) | 2009-11-05 |
| JP2009538327A5 true JP2009538327A5 (enExample) | 2010-07-01 |
Family
ID=38565503
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009512222A Pending JP2009538327A (ja) | 2006-05-23 | 2007-05-16 | チャネル活性化プロテアーゼ阻害剤である化合物および組成物 |
Country Status (14)
| Country | Link |
|---|---|
| US (2) | US7951823B2 (enExample) |
| EP (1) | EP2027143A2 (enExample) |
| JP (1) | JP2009538327A (enExample) |
| KR (1) | KR101069051B1 (enExample) |
| AR (1) | AR061109A1 (enExample) |
| AU (1) | AU2007253819B2 (enExample) |
| BR (1) | BRPI0712021A2 (enExample) |
| CA (1) | CA2651762A1 (enExample) |
| CL (1) | CL2007001481A1 (enExample) |
| MX (1) | MX2008014839A (enExample) |
| PE (1) | PE20080708A1 (enExample) |
| RU (1) | RU2419626C2 (enExample) |
| TW (1) | TW200813094A (enExample) |
| WO (1) | WO2007137080A2 (enExample) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0507577D0 (en) * | 2005-04-14 | 2005-05-18 | Novartis Ag | Organic compounds |
| AU2007253819B2 (en) * | 2006-05-23 | 2011-02-17 | Irm Llc | Compounds and compositions as channel activating protease inhibitors |
| RU2419625C2 (ru) * | 2006-05-23 | 2011-05-27 | Айрм Ллк | Соединения и композиции в качестве ингибиторов протеазы, активирующей каналы |
| JP2010518097A (ja) * | 2007-02-09 | 2010-05-27 | アイアールエム・リミテッド・ライアビリティ・カンパニー | チャネル活性化プロテアーゼ阻害剤としての化合物および組成物 |
| US8293915B2 (en) | 2007-02-09 | 2012-10-23 | Irm Llc | Compounds and compositions as channel activating protease inhibitors |
| IE20070935A1 (en) * | 2007-12-21 | 2009-06-24 | Trinity College Dublin | Guanidine based compounds and their use in the treatment of mental and neurological disorders. |
| SI2421826T1 (sl) * | 2009-04-20 | 2014-02-28 | F. Hoffmann-La Roche Ag | Derivati prolina kot inhibitorji katepsina |
| CN102811989A (zh) * | 2010-02-03 | 2012-12-05 | Meh联合公司 | 作为具有选择性和生物活性的等排物的多取代氟甲烷 |
| RU2014123784A (ru) * | 2011-11-25 | 2015-12-27 | Ф. Хоффманн-Ля Рош Аг | Новые производные пирролидина в качестве ингибиторов катепсина |
| KR20170068521A (ko) | 2014-10-06 | 2017-06-19 | 코텍자임, 인코포레이티드 | 리신 진지페인의 억제제 |
| CN105001131A (zh) * | 2015-07-31 | 2015-10-28 | 吉尔生化（上海）有限公司 | 一种医药中间体nα-z-s-苄基-l-半胱氨酸-4-硝基苯酯的合成方法 |
| CA3004095A1 (en) | 2015-11-09 | 2017-05-18 | Cortexyme, Inc. | Inhibitors of arginine gingipain |
| WO2018053353A1 (en) | 2016-09-16 | 2018-03-22 | Cortexyme, Inc. | Ketone inhibitors of lysine gingipain |
| CN110483437B (zh) * | 2018-05-14 | 2022-12-06 | 嘉兴维眸生物科技有限公司 | 一种含五元环的化合物及其制备和应用 |
| US20220354833A1 (en) | 2019-09-17 | 2022-11-10 | Mereo Biopharma 4 Limited | Alvelestat for use in the treatment of graft rejection, bronchiolitis obliterans syndrome and graft versus host disease |
| ES2962498T3 (es) | 2020-04-16 | 2024-03-19 | Mereo Biopharma 4 Ltd | Métodos que implican el inhibidor de elastasa de neutrófilos alvelestat para el tratamiento de enfermedades respiratorias mediadas por deficiencia de alfa-1 antitripsina |
| US20240382472A1 (en) | 2021-10-20 | 2024-11-21 | Mereo Biopharma 4 Limited | Neutrophil elastase inhibitors for use in the treatment of fibrosis |
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| GB0507577D0 (en) | 2005-04-14 | 2005-05-18 | Novartis Ag | Organic compounds |
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| RU2419625C2 (ru) | 2006-05-23 | 2011-05-27 | Айрм Ллк | Соединения и композиции в качестве ингибиторов протеазы, активирующей каналы |
| AU2007253819B2 (en) * | 2006-05-23 | 2011-02-17 | Irm Llc | Compounds and compositions as channel activating protease inhibitors |
| NZ577939A (en) | 2007-01-10 | 2011-03-31 | Irm Llc | Compounds and compositions as channel activating protease inhibitors |
| US8293915B2 (en) | 2007-02-09 | 2012-10-23 | Irm Llc | Compounds and compositions as channel activating protease inhibitors |
| JP2010518097A (ja) | 2007-02-09 | 2010-05-27 | アイアールエム・リミテッド・ライアビリティ・カンパニー | チャネル活性化プロテアーゼ阻害剤としての化合物および組成物 |
-
2007
- 2007-05-16 AU AU2007253819A patent/AU2007253819B2/en not_active Ceased
- 2007-05-16 MX MX2008014839A patent/MX2008014839A/es active IP Right Grant
- 2007-05-16 WO PCT/US2007/069059 patent/WO2007137080A2/en not_active Ceased
- 2007-05-16 CA CA002651762A patent/CA2651762A1/en not_active Abandoned
- 2007-05-16 RU RU2008150615/04A patent/RU2419626C2/ru not_active IP Right Cessation
- 2007-05-16 KR KR1020087031129A patent/KR101069051B1/ko not_active Expired - Fee Related
- 2007-05-16 US US11/749,430 patent/US7951823B2/en not_active Expired - Fee Related
- 2007-05-16 JP JP2009512222A patent/JP2009538327A/ja active Pending
- 2007-05-16 EP EP07783835A patent/EP2027143A2/en not_active Withdrawn
- 2007-05-16 BR BRPI0712021-4A patent/BRPI0712021A2/pt not_active IP Right Cessation
- 2007-05-23 TW TW096118422A patent/TW200813094A/zh unknown
- 2007-05-23 PE PE2007000642A patent/PE20080708A1/es not_active Application Discontinuation
- 2007-05-23 AR ARP070102231A patent/AR061109A1/es not_active Application Discontinuation
- 2007-05-23 CL CL200701481A patent/CL2007001481A1/es unknown
-
2011
- 2011-04-19 US US13/089,973 patent/US8338469B2/en not_active Expired - Fee Related
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