JP2017531692A5 - - Google Patents
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- 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 (https=) | 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 (https=) |
| EP (1) | EP3204352B1 (https=) |
| JP (1) | JP6642948B2 (https=) |
| KR (1) | KR20170068521A (https=) |
| CN (2) | CN111349053A (https=) |
| AU (1) | AU2015328385B2 (https=) |
| BR (1) | BR112017006920A8 (https=) |
| CA (1) | CA2963305A1 (https=) |
| CL (1) | CL2017000845A1 (https=) |
| CO (1) | CO2017003321A2 (https=) |
| CY (1) | CY1123532T1 (https=) |
| DK (1) | DK3204352T3 (https=) |
| ES (1) | ES2819218T3 (https=) |
| HR (1) | HRP20201473T1 (https=) |
| HU (1) | HUE050876T2 (https=) |
| IL (2) | IL251501B (https=) |
| MX (1) | MX378266B (https=) |
| PE (1) | PE20171335A1 (https=) |
| PH (1) | PH12017500637A1 (https=) |
| PL (1) | PL3204352T3 (https=) |
| PT (1) | PT3204352T (https=) |
| RU (1) | RU2728785C2 (https=) |
| SG (1) | SG11201702797RA (https=) |
| WO (1) | WO2016057413A2 (https=) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX378266B (es) | 2014-10-06 | 2025-03-10 | Lighthouse Pharmaceuticals Inc | Inhibidores de gingipaina de lisina. |
| CN108602787A (zh) | 2015-11-09 | 2018-09-28 | 库特克希米公司 | 精氨酸牙龈卟啉菌蛋白酶的抑制剂 |
| 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 |
| CN110944637A (zh) * | 2017-05-10 | 2020-03-31 | 库特克希米公司 | 氨基吡啶化合物及其制备方法和使用方法 |
| US20210355527A1 (en) * | 2018-09-27 | 2021-11-18 | Cortexyme, Inc. | Methods for detection of microbial nucleic acids in body fluids |
| US20240400654A1 (en) * | 2020-11-03 | 2024-12-05 | 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 |
|---|---|---|---|---|
| ZA86746B (en) | 1985-02-04 | 1986-09-24 | Merrell Dow Pharma | 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 |
| AU2299592A (en) | 1991-07-02 | 1993-02-11 | 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 |
| AP9701004A0 (en) | 1994-12-22 | 1997-07-31 | Iaf Biochem Int | Low molecular weight bicyclic thrombin inhibitors. |
| JPH10508034A (ja) | 1995-03-24 | 1998-08-04 | モレキュメティックス リミテッド | βシート模倣物および生物学的に活性なペプチドまたはタンパク質のインヒビターとしてのその使用 |
| WO1996030396A1 (en) | 1995-03-24 | 1996-10-03 | Molecumetics Ltd. | β-SHEET MIMETICS AND USE THEREOF AS PROTEASE INHIBITORS |
| GB9510264D0 (en) | 1995-05-22 | 1995-07-19 | Iaf Biochem Int | Low molecular weight bicyclic-urea type thrombin inhibitors |
| US5827860A (en) | 1995-06-07 | 1998-10-27 | Ortho Pharmaceutical Corporation | 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 |
| US5523308A (en) | 1995-06-07 | 1996-06-04 | Costanzo; Michael J. | 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 |
| NZ334227A (en) | 1996-08-05 | 2000-10-27 | Molecumetics Ltd | Use of beta-sheet mimetics as protease and kinase inhibitors and as inhibitors of transcription factors |
| AU4172397A (en) | 1996-09-06 | 1998-03-26 | Biochem Pharma Inc. | Lactam inhibitors of thrombin |
| WO1999026925A1 (en) | 1997-11-26 | 1999-06-03 | Yoshitomi Pharmaceutical Industries, Ltd. | Tryptase inhibitors comprising heterocyclic amide compounds |
| DE69810513T2 (de) | 1998-02-12 | 2004-03-18 | Molecumetics, Ltd., Bellevue | Mimetika von beta-faltblatt und verfahren zur verwendung davon |
| 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 |
| CZ20012722A3 (cs) * | 1999-01-27 | 2002-08-14 | Ortho-Mcneil Pharmaceutical, Inc. | Peptidylové heterocyklické ketony pouľitelné jako inhibitory typtasy |
| AU2847200A (en) * | 1999-01-27 | 2000-08-18 | G.D. Searle & Co. | Novel hydroxyamidino carboxylate derivatives useful as nitric oxide synthase inhibitors |
| HK1039110A1 (zh) | 1999-03-15 | 2002-04-12 | Axys Pharmaceuticals, Inc. | 以新颖的合成物及组分作为蛋白酶抑制剂 |
| 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 |
| CA2586086A1 (en) | 2004-07-23 | 2006-01-23 | Robert E.(Deceased) Smith | 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 |
| AU2013305759C1 (en) * | 2012-08-23 | 2018-01-18 | Janssen Biopharma, Inc. | Compounds for the treatment of paramoxyvirus viral infections |
| US10100037B2 (en) | 2013-03-15 | 2018-10-16 | The Board Of Trustees Of The Leland Stanford Junior University | Activity-based probe compounds, compositions, and methods of use |
| MX378266B (es) | 2014-10-06 | 2025-03-10 | Lighthouse Pharmaceuticals Inc | Inhibidores de gingipaina de lisina. |
-
2015
- 2015-10-05 MX MX2017004569A patent/MX378266B/es unknown
- 2015-10-05 US US14/875,416 patent/US9758473B2/en active Active
- 2015-10-05 PE PE2017000557A patent/PE20171335A1/es unknown
- 2015-10-05 PL PL15849799T patent/PL3204352T3/pl unknown
- 2015-10-05 ES ES15849799T patent/ES2819218T3/es active Active
- 2015-10-05 CN CN201911258644.XA patent/CN111349053A/zh active Pending
- 2015-10-05 SG SG11201702797RA patent/SG11201702797RA/en unknown
- 2015-10-05 CA CA2963305A patent/CA2963305A1/en not_active Abandoned
- 2015-10-05 CN CN201580062146.1A patent/CN107108468B/zh not_active Expired - Fee Related
- 2015-10-05 AU AU2015328385A patent/AU2015328385B2/en not_active Ceased
- 2015-10-05 JP JP2017538176A patent/JP6642948B2/ja not_active Expired - Fee Related
- 2015-10-05 WO PCT/US2015/054050 patent/WO2016057413A2/en not_active Ceased
- 2015-10-05 KR KR1020177012278A patent/KR20170068521A/ko not_active Ceased
- 2015-10-05 EP EP15849799.0A patent/EP3204352B1/en active Active
- 2015-10-05 HU HUE15849799A patent/HUE050876T2/hu unknown
- 2015-10-05 BR BR112017006920A patent/BR112017006920A8/pt not_active Application Discontinuation
- 2015-10-05 DK DK15849799.0T patent/DK3204352T3/da active
- 2015-10-05 HR HRP20201473TT patent/HRP20201473T1/hr unknown
- 2015-10-05 RU RU2017115726A patent/RU2728785C2/ru active
- 2015-10-05 PT PT158497990T patent/PT3204352T/pt unknown
-
2017
- 2017-04-02 IL IL251501A patent/IL251501B/en unknown
- 2017-04-05 CO CONC2017/0003321A patent/CO2017003321A2/es unknown
- 2017-04-06 CL CL2017000845A patent/CL2017000845A1/es unknown
- 2017-04-06 PH PH12017500637A patent/PH12017500637A1/en 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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