JP2010515729A5 - - Google Patents
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- JP2010515729A5 JP2010515729A5 JP2009545545A JP2009545545A JP2010515729A5 JP 2010515729 A5 JP2010515729 A5 JP 2010515729A5 JP 2009545545 A JP2009545545 A JP 2009545545A JP 2009545545 A JP2009545545 A JP 2009545545A JP 2010515729 A5 JP2010515729 A5 JP 2010515729A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- pharmaceutically acceptable
- acceptable salt
- alkyl
- phenyl
- 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.)
- Ceased
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- 150000001875 compounds Chemical class 0.000 claims description 36
- 150000003839 salts Chemical class 0.000 claims description 17
- 239000003814 drug Substances 0.000 claims description 3
- 229940124597 therapeutic agent Drugs 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
- 229940124630 bronchodilator Drugs 0.000 claims description 2
- 125000000217 alkyl group Chemical group 0.000 claims 13
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 8
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 5
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 5
- 125000003386 piperidinyl group Chemical group 0.000 claims 5
- 125000001475 halogen functional group Chemical group 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 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 2
- 239000003242 anti bacterial agent Substances 0.000 claims 1
- 229940088710 antibiotic agent Drugs 0.000 claims 1
- 229940125715 antihistaminic agent Drugs 0.000 claims 1
- 239000003434 antitussive agent Substances 0.000 claims 1
- 239000000168 bronchodilator agent Substances 0.000 claims 1
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 102000035195 Peptidases Human genes 0.000 description 19
- 108091005804 Peptidases Proteins 0.000 description 19
- 239000004365 Protease Substances 0.000 description 19
- 108010031970 prostasin Proteins 0.000 description 19
- 108091006146 Channels Proteins 0.000 description 18
- 102100029500 Prostasin Human genes 0.000 description 18
- 230000003213 activating effect Effects 0.000 description 15
- 101000798702 Homo sapiens Transmembrane protease serine 4 Proteins 0.000 description 13
- 102100032471 Transmembrane protease serine 4 Human genes 0.000 description 13
- 102100037942 Suppressor of tumorigenicity 14 protein Human genes 0.000 description 11
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 11
- 201000010099 disease Diseases 0.000 description 10
- 238000000034 method Methods 0.000 description 10
- 230000000694 effects Effects 0.000 description 7
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- 102000004190 Enzymes Human genes 0.000 description 6
- 108090000790 Enzymes Proteins 0.000 description 6
- 101000661807 Homo sapiens Suppressor of tumorigenicity 14 protein Proteins 0.000 description 6
- 102100022046 Brain-specific serine protease 4 Human genes 0.000 description 5
- 108010059081 Cathepsin A Proteins 0.000 description 5
- 102000005572 Cathepsin A Human genes 0.000 description 5
- 101000897856 Homo sapiens Adenylyl cyclase-associated protein 2 Proteins 0.000 description 5
- 101000896891 Homo sapiens Brain-specific serine protease 4 Proteins 0.000 description 5
- 101000836079 Homo sapiens Serpin B8 Proteins 0.000 description 5
- 101000836075 Homo sapiens Serpin B9 Proteins 0.000 description 5
- 101000798707 Homo sapiens Transmembrane protease serine 13 Proteins 0.000 description 5
- 108010028275 Leukocyte Elastase Proteins 0.000 description 5
- 108010091175 Matriptase Proteins 0.000 description 5
- 102100033174 Neutrophil elastase Human genes 0.000 description 5
- 102100032467 Transmembrane protease serine 13 Human genes 0.000 description 5
- 102000004142 Trypsin Human genes 0.000 description 5
- 108090000631 Trypsin Proteins 0.000 description 5
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- 239000012588 trypsin Substances 0.000 description 5
- 101000598054 Homo sapiens Transmembrane protease serine 11B Proteins 0.000 description 4
- 101000637855 Homo sapiens Transmembrane protease serine 11E Proteins 0.000 description 4
- 101000638154 Homo sapiens Transmembrane protease serine 2 Proteins 0.000 description 4
- 101000798700 Homo sapiens Transmembrane protease serine 3 Proteins 0.000 description 4
- 101100069392 Mus musculus Gzma gene Proteins 0.000 description 4
- 102100037023 Transmembrane protease serine 11B Human genes 0.000 description 4
- 102100032001 Transmembrane protease serine 11E Human genes 0.000 description 4
- 102100031989 Transmembrane protease serine 2 Human genes 0.000 description 4
- 238000003556 assay Methods 0.000 description 4
- 210000004027 cell Anatomy 0.000 description 4
- 239000000137 peptide hydrolase inhibitor Substances 0.000 description 4
- 210000001519 tissue Anatomy 0.000 description 4
- 229940124158 Protease/peptidase inhibitor Drugs 0.000 description 3
- 210000001124 body fluid Anatomy 0.000 description 3
- 239000010839 body fluid Substances 0.000 description 3
- 210000000981 epithelium Anatomy 0.000 description 3
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- 210000003734 kidney Anatomy 0.000 description 3
- 210000004072 lung Anatomy 0.000 description 3
- 210000003097 mucus Anatomy 0.000 description 3
- 239000008194 pharmaceutical composition Substances 0.000 description 3
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- 108010036927 trypsin-like serine protease Proteins 0.000 description 3
- 102000003837 Epithelial Sodium Channels Human genes 0.000 description 2
- 108090000140 Epithelial Sodium Channels Proteins 0.000 description 2
- 108090000862 Ion Channels Proteins 0.000 description 2
- 102000004310 Ion Channels Human genes 0.000 description 2
- 241000124008 Mammalia Species 0.000 description 2
- 208000004880 Polyuria Diseases 0.000 description 2
- 206010036790 Productive cough Diseases 0.000 description 2
- 238000009825 accumulation Methods 0.000 description 2
- 230000033228 biological regulation Effects 0.000 description 2
- 210000000424 bronchial epithelial cell Anatomy 0.000 description 2
- -1 bronchodilator Substances 0.000 description 2
- 230000035619 diuresis Effects 0.000 description 2
- 230000037427 ion transport Effects 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- 210000004379 membrane Anatomy 0.000 description 2
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- 230000035479 physiological effects, processes and functions Effects 0.000 description 2
- 230000000241 respiratory effect Effects 0.000 description 2
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- 210000003802 sputum Anatomy 0.000 description 2
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- 238000012360 testing method Methods 0.000 description 2
- 241000894006 Bacteria Species 0.000 description 1
- 208000035143 Bacterial infection Diseases 0.000 description 1
- 206010006458 Bronchitis chronic Diseases 0.000 description 1
- 0 CS(N[C@@](CCC1CCNCC1)C(N(CC(*Cc(cc1)ccc1Cl)C1)[C@@]1C(NCc1c(CN)ccc(*)c1)=O)=O)(=C)=O Chemical compound CS(N[C@@](CCC1CCNCC1)C(N(CC(*Cc(cc1)ccc1Cl)C1)[C@@]1C(NCc1c(CN)ccc(*)c1)=O)=O)(=C)=O 0.000 description 1
- 241000700199 Cavia porcellus Species 0.000 description 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 description 1
- 201000003883 Cystic fibrosis Diseases 0.000 description 1
- 102000016911 Deoxyribonucleases Human genes 0.000 description 1
- 108010053770 Deoxyribonucleases Proteins 0.000 description 1
- 208000003556 Dry Eye Syndromes Diseases 0.000 description 1
- 206010013774 Dry eye Diseases 0.000 description 1
- 206010020772 Hypertension Diseases 0.000 description 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 description 1
- 229940123991 Prostasin inhibitor Drugs 0.000 description 1
- 206010057190 Respiratory tract infections Diseases 0.000 description 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 description 1
- 241000700605 Viruses Species 0.000 description 1
- 230000002159 abnormal effect Effects 0.000 description 1
- 230000005856 abnormality Effects 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 239000000443 aerosol Substances 0.000 description 1
- XSDQTOBWRPYKKA-UHFFFAOYSA-N amiloride Chemical compound NC(=N)NC(=O)C1=NC(Cl)=C(N)N=C1N XSDQTOBWRPYKKA-UHFFFAOYSA-N 0.000 description 1
- 229960002576 amiloride Drugs 0.000 description 1
- 230000001387 anti-histamine Effects 0.000 description 1
- 208000006673 asthma Diseases 0.000 description 1
- 208000022362 bacterial infectious disease Diseases 0.000 description 1
- 238000010256 biochemical assay Methods 0.000 description 1
- 238000003185 biochemical assay format Methods 0.000 description 1
- 230000003115 biocidal effect Effects 0.000 description 1
- 230000004531 blood pressure lowering effect Effects 0.000 description 1
- 206010006451 bronchitis Diseases 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 208000007451 chronic bronchitis Diseases 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 230000001886 ciliary effect Effects 0.000 description 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 description 1
- 229940042399 direct acting antivirals protease inhibitors Drugs 0.000 description 1
- 208000035475 disorder Diseases 0.000 description 1
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- 230000004064 dysfunction Effects 0.000 description 1
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- 230000029142 excretion Effects 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 230000013632 homeostatic process Effects 0.000 description 1
- 230000001939 inductive effect Effects 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 206010023332 keratitis Diseases 0.000 description 1
- 201000010666 keratoconjunctivitis Diseases 0.000 description 1
- 201000005296 lung carcinoma Diseases 0.000 description 1
- 210000005265 lung cell Anatomy 0.000 description 1
- 238000012423 maintenance Methods 0.000 description 1
- 230000014759 maintenance of location Effects 0.000 description 1
- 230000000420 mucociliary effect Effects 0.000 description 1
- 239000007922 nasal spray Substances 0.000 description 1
- 229940097496 nasal spray Drugs 0.000 description 1
- 239000006199 nebulizer Substances 0.000 description 1
- 108090000765 processed proteins & peptides Proteins 0.000 description 1
- 230000001737 promoting effect Effects 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 210000002345 respiratory system Anatomy 0.000 description 1
- 230000028327 secretion Effects 0.000 description 1
- 210000000582 semen Anatomy 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
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- 239000003826 tablet Substances 0.000 description 1
- 230000007306 turnover Effects 0.000 description 1
- 210000002700 urine Anatomy 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US88433407P | 2007-01-10 | 2007-01-10 | |
| US89147407P | 2007-02-23 | 2007-02-23 | |
| PCT/US2007/085366 WO2008085608A1 (en) | 2007-01-10 | 2007-11-21 | Compounds and compositions as channel activating protease inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2010515729A JP2010515729A (ja) | 2010-05-13 |
| JP2010515729A5 true JP2010515729A5 (enExample) | 2012-08-30 |
Family
ID=39148650
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009545545A Ceased JP2010515729A (ja) | 2007-01-10 | 2007-11-21 | 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 |
Country Status (32)
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007137080A2 (en) * | 2006-05-23 | 2007-11-29 | Irm Llc | Compounds and compositions as channel activating protease inhibitors |
| CA2674644A1 (en) | 2007-01-10 | 2008-07-17 | F. Hoffmann-La Roche Ag | Sulfonamide derivatives as chymase inhibitors |
| BRPI0807483A2 (pt) * | 2007-02-09 | 2014-05-13 | Irm Llc | Compostos e composições como inibidores de protease de ativação de canal |
| BRPI1011267A2 (pt) | 2009-05-18 | 2016-03-22 | Orion Corp | inibidores de protease |
| US10399940B2 (en) * | 2016-10-07 | 2019-09-03 | Abbvie S.Á.R.L. | Substituted pyrrolidines and methods of use |
| GB201805174D0 (en) * | 2018-03-29 | 2018-05-16 | Univ Leeds Innovations Ltd | Compounds |
| US11584714B2 (en) | 2018-05-29 | 2023-02-21 | Omeros Corporation | MASP-2 inhibitors and methods of use |
| CN119350433A (zh) | 2018-05-29 | 2025-01-24 | 奥默罗斯公司 | Masp-2抑制剂和使用方法 |
| EP3941462A4 (en) * | 2019-03-22 | 2023-04-05 | Achillion Pharmaceuticals, Inc. | PHARMACEUTICAL COMPOUNDS FOR THE TREATMENT OF COMPLEMENT-MEDIED DISEASES |
| EP4031138A1 (en) | 2019-09-17 | 2022-07-27 | Mereo Biopharma 4 Limited | Alvelestat for use in the treatment of graft rejection, bronchiolitis obliterans syndrome and graft versus host disease |
| CA3159172A1 (en) | 2019-12-04 | 2021-06-10 | Michael Cicirelli | Masp-2 inhibitors and methods of use |
| CN115052862A (zh) | 2019-12-04 | 2022-09-13 | 奥默罗斯公司 | Masp-2抑制剂和使用方法 |
| BR112022010890A2 (pt) | 2019-12-04 | 2022-08-16 | Omeros Corp | Composto, composição farmacêutica, e, método para tratar uma doença ou distúrbio associado a serina protease-2 associada à lectina de ligação ao manan |
| CA3159159A1 (en) * | 2019-12-04 | 2021-06-10 | Neil S. Cutshall | Masp-2 inhibitors and methods of use |
| LT4106757T (lt) | 2020-04-16 | 2023-11-10 | Mereo Biopharma 4 Limited | Neutrofilų elastazės inhibitoriaus alvelestato panaudojimas kvėpavimo sistemos ligų, nulemtų alfa-1 antitripsino nepakankamumo, gydymui |
| EP4419102A1 (en) | 2021-10-20 | 2024-08-28 | Mereo Biopharma 4 Limited | Neutrophil elastase inhibitors for use in the treatment of fibrosis |
| US20250346585A1 (en) * | 2022-03-22 | 2025-11-13 | Alexion Pharmaceuticals, Inc. | Pharmaceutical compounds for the treatment of complement mediated disorders |
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-
2007
- 2007-11-21 EP EP10013675A patent/EP2279777A2/en not_active Withdrawn
- 2007-11-21 NZ NZ577939A patent/NZ577939A/en not_active IP Right Cessation
- 2007-11-21 AT AT07854747T patent/ATE493174T1/de active
- 2007-11-21 CA CA002673803A patent/CA2673803A1/en not_active Abandoned
- 2007-11-21 DK DK07854747.8T patent/DK2104535T3/da active
- 2007-11-21 MX MX2009007476A patent/MX2009007476A/es active IP Right Grant
- 2007-11-21 AU AU2007342223A patent/AU2007342223B2/en not_active Ceased
- 2007-11-21 EP EP07854747A patent/EP2104535B9/en active Active
- 2007-11-21 RS RS20110129A patent/RS51644B/sr unknown
- 2007-11-21 JP JP2009545545A patent/JP2010515729A/ja not_active Ceased
- 2007-11-21 US US11/943,845 patent/US20080176901A1/en not_active Abandoned
- 2007-11-21 PT PT07854747T patent/PT2104535E/pt unknown
- 2007-11-21 WO PCT/US2007/085366 patent/WO2008085608A1/en not_active Ceased
- 2007-11-21 EA EA200900920A patent/EA016199B1/ru not_active IP Right Cessation
- 2007-11-21 BR BRPI0720799-9A patent/BRPI0720799A2/pt not_active IP Right Cessation
- 2007-11-21 DE DE602007011670T patent/DE602007011670D1/de active Active
- 2007-11-21 PL PL07854747T patent/PL2104535T3/pl unknown
- 2007-11-21 KR KR1020097014455A patent/KR101084787B1/ko not_active Expired - Fee Related
- 2007-11-21 HR HR20110201T patent/HRP20110201T1/hr unknown
-
2008
- 2008-01-10 CL CL200800060A patent/CL2008000060A1/es unknown
- 2008-01-10 AR ARP080100104A patent/AR064841A1/es not_active Application Discontinuation
- 2008-01-10 PE PE2008000105A patent/PE20081566A1/es not_active Application Discontinuation
- 2008-01-10 TW TW097101044A patent/TW200845981A/zh unknown
-
2009
- 2009-06-30 MA MA32060A patent/MA31037B1/fr unknown
- 2009-07-08 HN HN2009001282A patent/HN2009001282A/es unknown
- 2009-07-08 TN TNP2009000294A patent/TN2009000294A1/fr unknown
- 2009-07-08 GT GT200900196A patent/GT200900196A/es unknown
- 2009-07-10 CU CU20090122A patent/CU23762B7/es not_active IP Right Cessation
- 2009-07-10 SV SV2009003330A patent/SV2009003330A/es not_active Application Discontinuation
- 2009-07-13 CO CO09072488A patent/CO6190626A2/es not_active Application Discontinuation
- 2009-07-15 EC EC2009009517A patent/ECSP099517A/es unknown
- 2009-08-10 NO NO20092817A patent/NO20092817L/no not_active Application Discontinuation
-
2011
- 2011-03-14 CY CY20111100283T patent/CY1111340T1/el unknown
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