JP2019503340A5 - - Google Patents
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- Publication number
- JP2019503340A5 JP2019503340A5 JP2018524794A JP2018524794A JP2019503340A5 JP 2019503340 A5 JP2019503340 A5 JP 2019503340A5 JP 2018524794 A JP2018524794 A JP 2018524794A JP 2018524794 A JP2018524794 A JP 2018524794A JP 2019503340 A5 JP2019503340 A5 JP 2019503340A5
- Authority
- JP
- Japan
- Prior art keywords
- compound according
- amino acid
- proteinogenic
- aryl
- lower alkyl
- 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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- 150000001875 compounds Chemical class 0.000 claims 20
- 125000000217 alkyl group Chemical group 0.000 claims 13
- 125000003118 aryl group Chemical group 0.000 claims 11
- 150000001413 amino acids Chemical group 0.000 claims 7
- 235000001014 amino acid Nutrition 0.000 claims 6
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 5
- 125000001072 heteroaryl group Chemical group 0.000 claims 5
- 125000001424 substituent group Chemical group 0.000 claims 5
- 125000003342 alkenyl group Chemical group 0.000 claims 4
- 208000003167 cholangitis Diseases 0.000 claims 4
- 206010009887 colitis Diseases 0.000 claims 4
- 125000000623 heterocyclic group Chemical group 0.000 claims 4
- 125000004103 aminoalkyl group Chemical group 0.000 claims 3
- 208000006673 asthma Diseases 0.000 claims 3
- -1 cyclic secondary amine Chemical class 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 208000004396 mastitis Diseases 0.000 claims 3
- 229930182852 proteinogenic amino acid Natural products 0.000 claims 3
- 208000023275 Autoimmune disease Diseases 0.000 claims 2
- 206010006458 Bronchitis chronic Diseases 0.000 claims 2
- 206010009137 Chronic sinusitis Diseases 0.000 claims 2
- 208000015943 Coeliac disease Diseases 0.000 claims 2
- 206010009900 Colitis ulcerative Diseases 0.000 claims 2
- 208000011231 Crohn disease Diseases 0.000 claims 2
- 206010017993 Gastrointestinal neoplasms Diseases 0.000 claims 2
- 208000009329 Graft vs Host Disease Diseases 0.000 claims 2
- 241000725303 Human immunodeficiency virus Species 0.000 claims 2
- 206010033645 Pancreatitis Diseases 0.000 claims 2
- 208000002389 Pouchitis Diseases 0.000 claims 2
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 2
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000002877 alkyl aryl group Chemical group 0.000 claims 2
- 235000008206 alpha-amino acids Nutrition 0.000 claims 2
- 206010006451 bronchitis Diseases 0.000 claims 2
- 238000002512 chemotherapy Methods 0.000 claims 2
- 201000001352 cholecystitis Diseases 0.000 claims 2
- 208000007451 chronic bronchitis Diseases 0.000 claims 2
- 208000027157 chronic rhinosinusitis Diseases 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000024908 graft versus host disease Diseases 0.000 claims 2
- 208000027866 inflammatory disease Diseases 0.000 claims 2
- 230000002757 inflammatory effect Effects 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 208000008275 microscopic colitis Diseases 0.000 claims 2
- 201000010315 pericholangitis Diseases 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- 238000001959 radiotherapy Methods 0.000 claims 2
- 208000011580 syndromic disease Diseases 0.000 claims 2
- 208000036487 Arthropathies Diseases 0.000 claims 1
- 206010008609 Cholangitis sclerosing Diseases 0.000 claims 1
- 208000000094 Chronic Pain Diseases 0.000 claims 1
- 208000031879 Chédiak-Higashi syndrome Diseases 0.000 claims 1
- 102000008186 Collagen Human genes 0.000 claims 1
- 108010035532 Collagen Proteins 0.000 claims 1
- 206010064212 Eosinophilic oesophagitis Diseases 0.000 claims 1
- 208000007882 Gastritis Diseases 0.000 claims 1
- 229920002527 Glycogen Polymers 0.000 claims 1
- 241001320695 Hermas Species 0.000 claims 1
- 208000012659 Joint disease Diseases 0.000 claims 1
- ROHFNLRQFUQHCH-YFKPBYRVSA-N L-leucine Chemical compound CC(C)C[C@H](N)C(O)=O ROHFNLRQFUQHCH-YFKPBYRVSA-N 0.000 claims 1
- ROHFNLRQFUQHCH-UHFFFAOYSA-N Leucine Natural products CC(C)CC(N)C(O)=O ROHFNLRQFUQHCH-UHFFFAOYSA-N 0.000 claims 1
- 229910003827 NRaRb Inorganic materials 0.000 claims 1
- 208000001132 Osteoporosis Diseases 0.000 claims 1
- 208000002193 Pain Diseases 0.000 claims 1
- ONIBWKKTOPOVIA-UHFFFAOYSA-N Proline Natural products OC(=O)C1CCCN1 ONIBWKKTOPOVIA-UHFFFAOYSA-N 0.000 claims 1
- 206010062164 Seronegative arthritis Diseases 0.000 claims 1
- 208000021017 Weight Gain Diseases 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 150000001370 alpha-amino acid derivatives Chemical class 0.000 claims 1
- 150000001408 amides Chemical class 0.000 claims 1
- 125000005001 aminoaryl group Chemical group 0.000 claims 1
- 125000005214 aminoheteroaryl group Chemical group 0.000 claims 1
- 230000003872 anastomosis Effects 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 125000004104 aryloxy group Chemical group 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 150000001576 beta-amino acids Chemical class 0.000 claims 1
- 210000004899 c-terminal region Anatomy 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 238000012321 colectomy Methods 0.000 claims 1
- 229920001436 collagen Polymers 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 201000000708 eosinophilic esophagitis Diseases 0.000 claims 1
- 201000001564 eosinophilic gastroenteritis Diseases 0.000 claims 1
- 150000002148 esters Chemical class 0.000 claims 1
- 230000002496 gastric effect Effects 0.000 claims 1
- 210000001035 gastrointestinal tract Anatomy 0.000 claims 1
- 229940096919 glycogen Drugs 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 125000005553 heteroaryloxy group Chemical group 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 238000007455 ileostomy Methods 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 230000015788 innate immune response Effects 0.000 claims 1
- 201000008105 leukocyte adhesion deficiency 1 Diseases 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 201000000742 primary sclerosing cholangitis Diseases 0.000 claims 1
- 108090000765 processed proteins & peptides Proteins 0.000 claims 1
- 125000001500 prolyl group Chemical group [H]N1C([H])(C(=O)[*])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
- 230000005855 radiation Effects 0.000 claims 1
- 238000002271 resection Methods 0.000 claims 1
- 208000010157 sclerosing cholangitis Diseases 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 230000000699 topical effect Effects 0.000 claims 1
- 230000004584 weight gain Effects 0.000 claims 1
- 235000019786 weight gain Nutrition 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562254003P | 2015-11-11 | 2015-11-11 | |
| US62/254,003 | 2015-11-11 | ||
| PCT/CA2016/000274 WO2017079820A1 (en) | 2015-11-11 | 2016-11-14 | CYCLIC PEPTIDES TARGETING α4β7 INTEGRIN |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019503340A JP2019503340A (ja) | 2019-02-07 |
| JP2019503340A5 true JP2019503340A5 (https=) | 2019-12-26 |
| JP6961586B2 JP6961586B2 (ja) | 2021-11-05 |
Family
ID=58694457
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018524794A Active JP6961586B2 (ja) | 2015-11-11 | 2016-11-14 | α４β７インテグリンを標的とする環状ペプチド |
Country Status (8)
| Country | Link |
|---|---|
| US (4) | US11046695B2 (https=) |
| EP (2) | EP3377471A4 (https=) |
| JP (1) | JP6961586B2 (https=) |
| KR (1) | KR102867019B1 (https=) |
| CN (2) | CN109071602B (https=) |
| AU (1) | AU2016353547B9 (https=) |
| CA (2) | CA3004714A1 (https=) |
| WO (2) | WO2017079820A1 (https=) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11046695B2 (en) | 2015-11-11 | 2021-06-29 | Zealand Pharma A/S | Fragment synthesis of substituted cyclic peptides |
| US11111273B2 (en) | 2016-11-11 | 2021-09-07 | Zealand Pharma A/S | Cyclic peptides multimers targeting alpha-4-beta-7 integrin |
| KR20230079464A (ko) | 2017-05-10 | 2023-06-07 | 질랜드 파마 에이/에스 | α4β7 인테그린을 타겟팅하는 호모데틱 사이클릭 펩타이드 |
| CN110551178B (zh) * | 2018-06-01 | 2020-07-21 | 深圳翰宇药业股份有限公司 | 一种含脯氨酸的首尾环肽合成方法 |
| WO2020185999A1 (en) * | 2019-03-14 | 2020-09-17 | Genentech, Inc. | Cyclic peptide antibiotics |
| US20230117920A1 (en) * | 2019-12-27 | 2023-04-20 | The University Of Tokyo | Library Construction Method, Cyclic Peptide, FXIIa Binder and IFNGR1 Binder |
| JP2021106565A (ja) * | 2019-12-27 | 2021-07-29 | 国立大学法人 東京大学 | ライブラリーの製造方法、環状ペプチド、ＦＸＩＩａ結合剤、及びＩＦＮＧＲ１結合剤 |
| EP4172177A1 (en) | 2020-06-29 | 2023-05-03 | Zealand Pharma A/S | Compounds targeting alpha4-beta7 integrin |
| US11957761B2 (en) | 2021-12-20 | 2024-04-16 | Zealand Pharma A/S | Compounds having α4β7 integrin inhibition activity |
| WO2026018016A1 (en) * | 2024-07-19 | 2026-01-22 | C4X Discovery Limited | Therapeutic compounds |
| WO2026018017A1 (en) * | 2024-07-19 | 2026-01-22 | C4X Discovery Limited | Therapeutic compounds |
Family Cites Families (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3219113A1 (de) * | 1982-05-21 | 1983-11-24 | Bayer Ag, 5090 Leverkusen | Verwendung von n-substituierten 2,3-diaminocarbonsaeuren in arzneimitteln und ihre herstellung |
| ZA906188B (en) | 1989-08-10 | 1991-06-26 | Merrell Dow Pharma | Cyclic neurokinin a antagonists |
| US5296604A (en) | 1992-05-15 | 1994-03-22 | Miles Inc. | Proline derivatives and compositions for their use as inhibitors of HIV protease |
| US5705481A (en) | 1992-11-06 | 1998-01-06 | Merck Patent Gesellschaft Mit Beschrankter Haftung | Cyclopeptides |
| IL109615A (en) | 1993-05-17 | 2000-12-06 | Fujisawa Pharmaceutical Co | Cyclic polypeptide derivatives processes for the preparation thereof and pharmaceutical compositions containing the same |
| US5693325A (en) | 1994-03-15 | 1997-12-02 | Molecumetics, Ltd. | Peptide vaccines and methods relating thereto |
| DE4415310A1 (de) | 1994-04-30 | 1995-11-02 | Merck Patent Gmbh | Cyclopeptide |
| GB9524630D0 (en) * | 1994-12-24 | 1996-01-31 | Zeneca Ltd | Chemical compounds |
| US5696084A (en) | 1996-08-16 | 1997-12-09 | Abbott Laboratories | Amino-lipopetide antifungal agents |
| US6492553B1 (en) | 1998-01-29 | 2002-12-10 | Aventis Pharamaceuticals Inc. | Methods for preparing N-[(aliphatic or aromatic)carbonyl)]-2-aminoaetamide compounds and for cyclizing such compounds |
| DE10107707A1 (de) | 2001-02-19 | 2002-08-29 | Wilex Biotechnology Gmbh | Antagonisten für alpha¶4¶beta¶7¶-Integrin |
| US6667407B2 (en) | 2002-05-03 | 2003-12-23 | Bayer Polymers Llc | Process of making polyaziridines |
| WO2005105827A2 (en) | 2004-04-15 | 2005-11-10 | Proteolix, Inc. | Compounds for proteasome enzyme inhibition |
| US8143375B2 (en) | 2006-10-20 | 2012-03-27 | The Governing Council Of The University Of Toronto | Aziridine aldehydes, aziridine-conjugated amino derivatives, aziridine-conjugated biomolecules and processes for their preparation |
| EP1961759A1 (en) * | 2007-02-21 | 2008-08-27 | Universita'degli Studi Di Milano | Integrin targeted cyclopeptide ligands, their preparation and use |
| EP2291390B1 (en) | 2008-05-22 | 2014-11-05 | Centre National de la Recherche Scientifique (CNRS) | New optically pure compounds for improved therapeutic efficiency |
| AU2010225426B2 (en) | 2009-03-16 | 2015-09-03 | The Governing Council Of The University Of Toronto | Cyclic amino acid molecules and methods of preparing the same |
| US20120045393A1 (en) | 2009-03-17 | 2012-02-23 | Linder Karen E | Lhrh-ii peptide analogs |
| EP2556060A1 (en) | 2010-04-08 | 2013-02-13 | Ah Usa 42 Llc | Substituted 3,5- diphenyl-isoxazoline derivatives as insecticides and acaricides |
| WO2012113803A1 (en) * | 2011-02-22 | 2012-08-30 | Leo Pharma A/S | A cyclic peptide and conjugate thereof for binding to keratinocytes |
| US9273093B2 (en) | 2012-10-11 | 2016-03-01 | Protagonist Therapeutics, Inc. | α4β7 peptide dimer antagonists |
| KR20170108936A (ko) | 2014-10-01 | 2017-09-27 | 프로타고니스트 테라퓨틱스, 인코포레이티드 | 신규한 α4β7 펩타이드 단량체 및 이량체 길항제 |
| EP3201217A4 (en) | 2014-10-01 | 2018-07-18 | Protagonist Therapeutics Inc. | Novel cyclic monomer and dimer peptides having integrin antagonist activity |
| US10281407B2 (en) | 2015-11-02 | 2019-05-07 | Jon A. Petty | Multi-fluid strip test |
| US11046695B2 (en) | 2015-11-11 | 2021-06-29 | Zealand Pharma A/S | Fragment synthesis of substituted cyclic peptides |
-
2016
- 2016-11-14 US US15/775,319 patent/US11046695B2/en not_active Expired - Fee Related
- 2016-11-14 WO PCT/CA2016/000274 patent/WO2017079820A1/en not_active Ceased
- 2016-11-14 US US15/775,309 patent/US11072616B2/en active Active
- 2016-11-14 AU AU2016353547A patent/AU2016353547B9/en active Active
- 2016-11-14 EP EP16863254.5A patent/EP3377471A4/en not_active Withdrawn
- 2016-11-14 WO PCT/CA2016/000275 patent/WO2017079821A1/en not_active Ceased
- 2016-11-14 KR KR1020187016390A patent/KR102867019B1/ko active Active
- 2016-11-14 CN CN201680079148.6A patent/CN109071602B/zh active Active
- 2016-11-14 EP EP16863253.7A patent/EP3387004B1/en active Active
- 2016-11-14 CA CA3004714A patent/CA3004714A1/en active Pending
- 2016-11-14 CA CA3004641A patent/CA3004641A1/en active Pending
- 2016-11-14 JP JP2018524794A patent/JP6961586B2/ja active Active
- 2016-11-14 CN CN201680078545.1A patent/CN109071430A/zh active Pending
-
2020
- 2020-08-04 US US16/985,096 patent/US10981921B2/en not_active Expired - Fee Related
-
2021
- 2021-03-26 US US17/214,530 patent/US20210300932A1/en not_active Abandoned
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