JP2017531692A5 - - Google Patents
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- Publication number
- JP2017531692A5 JP2017531692A5 JP2017538176A JP2017538176A JP2017531692A5 JP 2017531692 A5 JP2017531692 A5 JP 2017531692A5 JP 2017538176 A JP2017538176 A JP 2017538176A JP 2017538176 A JP2017538176 A JP 2017538176A JP 2017531692 A5 JP2017531692 A5 JP 2017531692A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- pharmaceutically acceptable
- composition
- carbonyl
- 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
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- -1 benzothiazol-2-yl-carbonyl Chemical group 0.000 claims description 57
- 150000001875 compounds Chemical class 0.000 claims description 57
- 150000003839 salts Chemical class 0.000 claims description 54
- 229910052739 hydrogen Inorganic materials 0.000 claims description 31
- 239000001257 hydrogen Substances 0.000 claims description 31
- 125000000217 alkyl group Chemical group 0.000 claims description 30
- 125000003118 aryl group Chemical group 0.000 claims description 24
- 125000001072 heteroaryl group Chemical group 0.000 claims description 22
- 125000000623 heterocyclic group Chemical group 0.000 claims description 22
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims description 16
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims description 16
- 201000010099 disease Diseases 0.000 claims description 16
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 16
- 150000002431 hydrogen Chemical class 0.000 claims description 15
- 229910052736 halogen Inorganic materials 0.000 claims description 13
- 150000002367 halogens Chemical class 0.000 claims description 13
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 12
- 239000003814 drug Substances 0.000 claims description 12
- 229940124597 therapeutic agent Drugs 0.000 claims description 12
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 claims description 10
- 208000014644 Brain disease Diseases 0.000 claims description 8
- 125000002947 alkylene group Chemical group 0.000 claims description 8
- 125000006242 amine protecting group Chemical group 0.000 claims description 8
- 125000005347 halocycloalkyl group Chemical group 0.000 claims description 8
- 150000003573 thiols Chemical group 0.000 claims description 8
- 125000003545 alkoxy group Chemical group 0.000 claims description 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 6
- 125000001424 substituent group Chemical group 0.000 claims description 6
- 206010028980 Neoplasm Diseases 0.000 claims description 5
- 208000017442 Retinal disease Diseases 0.000 claims description 5
- 201000011510 cancer Diseases 0.000 claims description 5
- 208000019423 liver disease Diseases 0.000 claims description 5
- 125000006648 (C1-C8) haloalkyl group Chemical group 0.000 claims description 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 4
- 208000024827 Alzheimer disease Diseases 0.000 claims description 4
- 208000024172 Cardiovascular disease Diseases 0.000 claims description 4
- 208000005107 Premature Birth Diseases 0.000 claims description 4
- 125000000218 acetic acid group Chemical group C(C)(=O)* 0.000 claims description 4
- 206010003246 arthritis Diseases 0.000 claims description 4
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 4
- 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 description 4
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 4
- 206010012601 diabetes mellitus Diseases 0.000 claims description 4
- 125000001475 halogen functional group Chemical group 0.000 claims description 4
- 125000004474 heteroalkylene group Chemical group 0.000 claims description 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 4
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 4
- 208000028169 periodontal disease Diseases 0.000 claims description 4
- 125000003386 piperidinyl group Chemical group 0.000 claims description 4
- 125000004076 pyridyl group Chemical group 0.000 claims description 4
- QZAYGJVTTNCVMB-UHFFFAOYSA-N serotonin Chemical compound C1=C(O)C=C2C(CCN)=CNC2=C1 QZAYGJVTTNCVMB-UHFFFAOYSA-N 0.000 claims description 4
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims description 4
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims description 4
- 125000000335 thiazolyl group Chemical group 0.000 claims description 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 4
- 206010003805 Autism Diseases 0.000 claims description 3
- 208000020706 Autistic disease Diseases 0.000 claims description 3
- 208000004051 Chronic Traumatic Encephalopathy Diseases 0.000 claims description 3
- 208000020401 Depressive disease Diseases 0.000 claims description 3
- 201000010374 Down Syndrome Diseases 0.000 claims description 3
- 201000011240 Frontotemporal dementia Diseases 0.000 claims description 3
- 208000023105 Huntington disease Diseases 0.000 claims description 3
- 208000009829 Lewy Body Disease Diseases 0.000 claims description 3
- 201000002832 Lewy body dementia Diseases 0.000 claims description 3
- 208000001089 Multiple system atrophy Diseases 0.000 claims description 3
- 208000018737 Parkinson disease Diseases 0.000 claims description 3
- 208000006011 Stroke Diseases 0.000 claims description 3
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims description 3
- 208000010877 cognitive disease Diseases 0.000 claims description 3
- 208000017004 dementia pugilistica Diseases 0.000 claims description 3
- 206010015037 epilepsy Diseases 0.000 claims description 3
- 201000006517 essential tremor Diseases 0.000 claims description 3
- 125000004970 halomethyl group Chemical group 0.000 claims description 3
- 208000015181 infectious disease Diseases 0.000 claims description 3
- 208000027061 mild cognitive impairment Diseases 0.000 claims description 3
- 201000000980 schizophrenia Diseases 0.000 claims description 3
- 102000013918 Apolipoproteins E Human genes 0.000 claims description 2
- 108010025628 Apolipoproteins E Proteins 0.000 claims description 2
- 208000010412 Glaucoma Diseases 0.000 claims description 2
- HOKKHZGPKSLGJE-GSVOUGTGSA-N N-Methyl-D-aspartic acid Chemical compound CN[C@@H](C(O)=O)CC(O)=O HOKKHZGPKSLGJE-GSVOUGTGSA-N 0.000 claims description 2
- 206010035664 Pneumonia Diseases 0.000 claims description 2
- 206010044688 Trisomy 21 Diseases 0.000 claims description 2
- 239000013543 active substance Substances 0.000 claims description 2
- 239000000654 additive Substances 0.000 claims description 2
- 230000000996 additive effect Effects 0.000 claims description 2
- HSFWRNGVRCDJHI-UHFFFAOYSA-N alpha-acetylene Natural products C#C HSFWRNGVRCDJHI-UHFFFAOYSA-N 0.000 claims description 2
- 239000002260 anti-inflammatory agent Substances 0.000 claims description 2
- 229940121363 anti-inflammatory agent Drugs 0.000 claims description 2
- 230000008499 blood brain barrier function Effects 0.000 claims description 2
- 210000001218 blood-brain barrier Anatomy 0.000 claims description 2
- 239000000544 cholinesterase inhibitor Substances 0.000 claims description 2
- 230000000295 complement effect Effects 0.000 claims description 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 2
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 claims description 2
- 208000017169 kidney disease Diseases 0.000 claims description 2
- 210000000274 microglia Anatomy 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 125000004483 piperidin-3-yl group Chemical group N1CC(CCC1)* 0.000 claims description 2
- 201000002212 progressive supranuclear palsy Diseases 0.000 claims description 2
- 229940076279 serotonin Drugs 0.000 claims description 2
- 229920002554 vinyl polymer Polymers 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 29
- 208000026139 Memory disease Diseases 0.000 claims 1
- 206010038923 Retinopathy Diseases 0.000 claims 1
- 208000034189 Sclerosis Diseases 0.000 claims 1
- 206010027175 memory impairment Diseases 0.000 description 2
- 201000006417 multiple sclerosis Diseases 0.000 description 2
- 206010006187 Breast cancer Diseases 0.000 description 1
- 208000026310 Breast neoplasm Diseases 0.000 description 1
- 201000010915 Glioblastoma multiforme Diseases 0.000 description 1
- 208000003445 Mouth Neoplasms Diseases 0.000 description 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 description 1
- 206010033799 Paralysis Diseases 0.000 description 1
- 206010064930 age-related macular degeneration Diseases 0.000 description 1
- 208000005017 glioblastoma Diseases 0.000 description 1
- 208000012987 lip and oral cavity carcinoma Diseases 0.000 description 1
- 208000002780 macular degeneration Diseases 0.000 description 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 description 1
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 description 1
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 description 1
- 201000002528 pancreatic cancer Diseases 0.000 description 1
- 208000008443 pancreatic carcinoma Diseases 0.000 description 1
- 230000000750 progressive effect Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462060483P | 2014-10-06 | 2014-10-06 | |
| US62/060,483 | 2014-10-06 | ||
| PCT/US2015/054050 WO2016057413A2 (en) | 2014-10-06 | 2015-10-05 | Inhibitors of lysine gingipain |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017531692A JP2017531692A (ja) | 2017-10-26 |
| JP2017531692A5 true JP2017531692A5 (enExample) | 2018-09-27 |
| JP6642948B2 JP6642948B2 (ja) | 2020-02-12 |
Family
ID=55632328
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017538176A Expired - Fee Related JP6642948B2 (ja) | 2014-10-06 | 2015-10-05 | リシンジンジパインの阻害剤 |
Country Status (24)
| Country | Link |
|---|---|
| US (5) | US9758473B2 (enExample) |
| EP (1) | EP3204352B1 (enExample) |
| JP (1) | JP6642948B2 (enExample) |
| KR (1) | KR20170068521A (enExample) |
| CN (2) | CN107108468B (enExample) |
| AU (1) | AU2015328385B2 (enExample) |
| BR (1) | BR112017006920A8 (enExample) |
| CA (1) | CA2963305A1 (enExample) |
| CL (1) | CL2017000845A1 (enExample) |
| CO (1) | CO2017003321A2 (enExample) |
| CY (1) | CY1123532T1 (enExample) |
| DK (1) | DK3204352T3 (enExample) |
| ES (1) | ES2819218T3 (enExample) |
| HR (1) | HRP20201473T1 (enExample) |
| HU (1) | HUE050876T2 (enExample) |
| IL (2) | IL251501B (enExample) |
| MX (1) | MX378266B (enExample) |
| PE (1) | PE20171335A1 (enExample) |
| PH (1) | PH12017500637A1 (enExample) |
| PL (1) | PL3204352T3 (enExample) |
| PT (1) | PT3204352T (enExample) |
| RU (1) | RU2728785C2 (enExample) |
| SG (1) | SG11201702797RA (enExample) |
| WO (1) | WO2016057413A2 (enExample) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2728785C2 (ru) | 2014-10-06 | 2020-07-31 | Кортексим, Инк. | Ингибиторы лизинспецифичного гингипаина |
| CA3004095A1 (en) | 2015-11-09 | 2017-05-18 | Cortexyme, Inc. | Inhibitors of arginine gingipain |
| WO2017201322A1 (en) * | 2016-05-19 | 2017-11-23 | Cortexyme, Inc. | Treatment of osteoarthritis with gingipain blocking agents |
| CN109983012B (zh) * | 2016-09-16 | 2023-12-01 | 莱特豪斯制药公司 | 赖氨酸牙龈蛋白酶的酮抑制剂 |
| JP7079794B2 (ja) * | 2017-05-10 | 2022-06-02 | コーテクシーミー， インコーポレイテッド | アミノピリジン化合物ならびにその調製および使用のための方法 |
| WO2020069397A1 (en) * | 2018-09-27 | 2020-04-02 | Cortexyme, Inc. | Methods for detection of microbial nucleic acids in body fluids |
| WO2022098661A1 (en) * | 2020-11-03 | 2022-05-12 | Keystone Bio, Inc. | Antigen-binding molecules that bind to porphyromonas gingivalis |
| KR102779135B1 (ko) * | 2023-06-19 | 2025-03-12 | 한국과학기술연구원 | 신규한 형광 화합물 및 이를 이용한 진지페인 검출용 조성물, 포르피로모나스 진지발리스 감염 진단용 조성물 또는 포르피로모나스 진지발리스에 대한 항균용 조성물 |
| CN119912460A (zh) * | 2025-03-31 | 2025-05-02 | 上海光声制药有限公司 | 卟啉衍生物、其制备方法及其用于抑菌的用途 |
Family Cites Families (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU600226B2 (en) | 1985-02-04 | 1990-08-09 | Merrell Pharmaceuticals Inc. | Novel peptidase inhibitors |
| US5055451A (en) | 1986-12-22 | 1991-10-08 | Syntex Inc. | Aryloxy and arylacyloxy methyl ketones as thiol protease inhibitors |
| JPH01163162A (ja) * | 1987-12-18 | 1989-06-27 | Showa Denko Kk | アミノ酸誘導体および酵素阻害剤 |
| US5451410A (en) * | 1993-04-22 | 1995-09-19 | Emisphere Technologies, Inc. | Modified amino acids for encapsulating active agents |
| GB9019558D0 (en) | 1990-09-07 | 1990-10-24 | Szelke Michael | Enzyme inhibitors |
| WO1993000926A1 (en) | 1991-07-02 | 1993-01-21 | Children's Medical Center Corporation | Treatment of periodontal disease with protease inhibitors |
| SE9102462D0 (sv) | 1991-08-28 | 1991-08-28 | Astra Ab | New isosteric peptides |
| US5374623A (en) | 1992-08-20 | 1994-12-20 | Prototek, Inc. | Cysteine protease inhibitors effective for in vivo use |
| PL320965A1 (en) | 1994-12-22 | 1997-11-24 | Iaf Biochem Int | Bicyclic thrombin inhibitors of low molecular weight |
| WO1996030396A1 (en) | 1995-03-24 | 1996-10-03 | Molecumetics Ltd. | β-SHEET MIMETICS AND USE THEREOF AS PROTEASE INHIBITORS |
| AU712581B2 (en) | 1995-03-24 | 1999-11-11 | Molecumetics, Ltd. | Beta-sheet mimetics and use thereof as inhibitors of biologically active peptides or proteins |
| GB9510264D0 (en) | 1995-05-22 | 1995-07-19 | Iaf Biochem Int | Low molecular weight bicyclic-urea type thrombin inhibitors |
| US5523308A (en) | 1995-06-07 | 1996-06-04 | Costanzo; Michael J. | Peptidyl heterocycles useful in the treatment of thrombin related disorders |
| US5827866A (en) | 1995-06-07 | 1998-10-27 | Ortho Pharmaceutical Corporation | Peptidyl heterocycles useful in the treatment of thrombin related disorders |
| US5827860A (en) | 1995-06-07 | 1998-10-27 | Ortho Pharmaceutical Corporation | Peptidyl heterocycles useful in the treatment of thrombin related disorders |
| IL119466A (en) * | 1995-11-03 | 2001-08-26 | Akzo Nobel Nv | Thrombin inhibitors, their preparation and pharmaceutical compositions containing them |
| JP2001524931A (ja) | 1996-08-05 | 2001-12-04 | モレキュメティクス リミテッド | プロテアーゼおよびキナーゼのインヒビターとしてならびに転写因子のインヒビターとしてのβシート模倣物の使用 |
| WO1998009987A1 (en) | 1996-09-06 | 1998-03-12 | Biochem Pharma, Inc. | Lactam inhibitors of thrombin |
| AU1176299A (en) | 1997-11-26 | 1999-06-15 | Yoshitomi Pharmaceutical Industries, Ltd. | Tryptase inhibitors comprising heterocyclic amide compounds |
| EP1053246B1 (en) | 1998-02-12 | 2003-01-02 | Molecumetics, Ltd. | Beta-sheet mimetics and methods relating to the use thereof |
| US6323219B1 (en) | 1998-04-02 | 2001-11-27 | Ortho-Mcneil Pharmaceutical, Inc. | Methods for treating immunomediated inflammatory disorders |
| US7053056B2 (en) * | 1998-07-02 | 2006-05-30 | Idun Pharmaceuticals, Inc. | C-terminal modified oxamyl dipeptides as inhibitors of the ICE/ced-3 family of cysteine proteases |
| YU61401A (sh) * | 1999-01-27 | 2005-07-19 | Orto-Mcneil Pharmaceuticals Inc. U.S. | Peptidil heterociklični ketoni korisni kao inhibitori triptaze |
| WO2000044731A1 (en) * | 1999-01-27 | 2000-08-03 | G.D. Searle & Co. | Novel hydroxyamidino carboxylate derivatives useful as nitric oxide synthase inhibitors |
| EP1159260A1 (en) | 1999-03-15 | 2001-12-05 | Axys Pharmaceuticals, Inc. | Novel compounds and compositions as protease inhibitors |
| US6790989B2 (en) * | 2000-01-13 | 2004-09-14 | Idun Pharmaceuticals, Inc. | Inhibitors of the ICE/ced-3 family of cysteine proteases |
| US7205384B2 (en) | 2003-08-05 | 2007-04-17 | Ortho-Mcneil Pharmaceutical Inc. | Process for preparing peptidyl heterocyclic ketone derivatives |
| WO2007046781A1 (en) | 2004-07-23 | 2007-04-26 | Smith, Judith | Furin inhibitors |
| US7951823B2 (en) | 2006-05-23 | 2011-05-31 | Irm Llc | Compounds and compositions as channel activating protease inhibitors |
| WO2009103432A2 (en) * | 2008-02-21 | 2009-08-27 | Sanofi-Aventis | Covalently binding imaging probes |
| JP6243908B2 (ja) * | 2012-08-23 | 2017-12-06 | アリオス バイオファーマ インク． | パラミクソウイルス感染症を治療するための化合物 |
| WO2014145257A2 (en) | 2013-03-15 | 2014-09-18 | The Board Of Trustees Of The Leland Stanford Junior University | Activity-based probe compounds, compositions, and methods of use |
| RU2728785C2 (ru) | 2014-10-06 | 2020-07-31 | Кортексим, Инк. | Ингибиторы лизинспецифичного гингипаина |
-
2015
- 2015-10-05 RU RU2017115726A patent/RU2728785C2/ru active
- 2015-10-05 PT PT158497990T patent/PT3204352T/pt unknown
- 2015-10-05 HR HRP20201473TT patent/HRP20201473T1/hr unknown
- 2015-10-05 SG SG11201702797RA patent/SG11201702797RA/en unknown
- 2015-10-05 EP EP15849799.0A patent/EP3204352B1/en active Active
- 2015-10-05 HU HUE15849799A patent/HUE050876T2/hu unknown
- 2015-10-05 WO PCT/US2015/054050 patent/WO2016057413A2/en not_active Ceased
- 2015-10-05 BR BR112017006920A patent/BR112017006920A8/pt not_active Application Discontinuation
- 2015-10-05 PL PL15849799T patent/PL3204352T3/pl unknown
- 2015-10-05 KR KR1020177012278A patent/KR20170068521A/ko not_active Ceased
- 2015-10-05 JP JP2017538176A patent/JP6642948B2/ja not_active Expired - Fee Related
- 2015-10-05 MX MX2017004569A patent/MX378266B/es unknown
- 2015-10-05 CN CN201580062146.1A patent/CN107108468B/zh not_active Expired - Fee Related
- 2015-10-05 DK DK15849799.0T patent/DK3204352T3/da active
- 2015-10-05 ES ES15849799T patent/ES2819218T3/es active Active
- 2015-10-05 PE PE2017000557A patent/PE20171335A1/es unknown
- 2015-10-05 US US14/875,416 patent/US9758473B2/en active Active
- 2015-10-05 CA CA2963305A patent/CA2963305A1/en not_active Abandoned
- 2015-10-05 CN CN201911258644.XA patent/CN111349053A/zh active Pending
- 2015-10-05 AU AU2015328385A patent/AU2015328385B2/en not_active Ceased
-
2017
- 2017-04-02 IL IL251501A patent/IL251501B/en unknown
- 2017-04-05 CO CONC2017/0003321A patent/CO2017003321A2/es unknown
- 2017-04-06 PH PH12017500637A patent/PH12017500637A1/en unknown
- 2017-04-06 CL CL2017000845A patent/CL2017000845A1/es unknown
- 2017-08-22 US US15/683,348 patent/US9988375B2/en active Active
-
2018
- 2018-06-04 US US15/996,660 patent/US10301301B2/en active Active
-
2019
- 2019-04-30 US US16/399,821 patent/US10676470B2/en not_active Expired - Fee Related
-
2020
- 2020-05-04 US US16/866,022 patent/US11332464B2/en active Active
- 2020-09-29 CY CY20201100918T patent/CY1123532T1/el unknown
-
2021
- 2021-06-20 IL IL284242A patent/IL284242A/en unknown
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