JP2015516983A - Par4アゴニストペプチド - Google Patents
Par4アゴニストペプチド Download PDFInfo
- Publication number
- JP2015516983A JP2015516983A JP2015509095A JP2015509095A JP2015516983A JP 2015516983 A JP2015516983 A JP 2015516983A JP 2015509095 A JP2015509095 A JP 2015509095A JP 2015509095 A JP2015509095 A JP 2015509095A JP 2015516983 A JP2015516983 A JP 2015516983A
- Authority
- JP
- Japan
- Prior art keywords
- mmol
- peptide
- par4
- amino acid
- 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.)
- Pending
Links
- 0 C*c1c(C)nc(*2)[n]1N=C2*(C)C Chemical compound C*c1c(C)nc(*2)[n]1N=C2*(C)C 0.000 description 5
- ZJDGGFCBBONCDM-AWEZNQCLSA-N C[C@@H](c([s]1)n[n]2c1nc(-c1cc(c(OCc3c[s]c(-c4ccccc4)n3)cc(OC)c3)c3[o]1)c2)F Chemical compound C[C@@H](c([s]1)n[n]2c1nc(-c1cc(c(OCc3c[s]c(-c4ccccc4)n3)cc(OC)c3)c3[o]1)c2)F ZJDGGFCBBONCDM-AWEZNQCLSA-N 0.000 description 2
- NPDACUSDTOMAMK-UHFFFAOYSA-N Cc(cc1)ccc1Cl Chemical compound Cc(cc1)ccc1Cl NPDACUSDTOMAMK-UHFFFAOYSA-N 0.000 description 2
- WRWPPGUCZBJXKX-UHFFFAOYSA-N Cc(cc1)ccc1F Chemical compound Cc(cc1)ccc1F WRWPPGUCZBJXKX-UHFFFAOYSA-N 0.000 description 2
- JUXFXYQUXNXVAA-UHFFFAOYSA-N Cc(cc1)ccc1OC(F)(F)F Chemical compound Cc(cc1)ccc1OC(F)(F)F JUXFXYQUXNXVAA-UHFFFAOYSA-N 0.000 description 2
- IBSQPLPBRSHTTG-UHFFFAOYSA-N Cc(cccc1)c1Cl Chemical compound Cc(cccc1)c1Cl IBSQPLPBRSHTTG-UHFFFAOYSA-N 0.000 description 2
- YISYUYYETHYYMD-UHFFFAOYSA-N Cc1cc(F)cc(F)c1 Chemical compound Cc1cc(F)cc(F)c1 YISYUYYETHYYMD-UHFFFAOYSA-N 0.000 description 2
- LRLRAYMYEXQKID-UHFFFAOYSA-N Cc1ccc(C(F)(F)F)cc1 Chemical compound Cc1ccc(C(F)(F)F)cc1 LRLRAYMYEXQKID-UHFFFAOYSA-N 0.000 description 2
- IVSZLXZYQVIEFR-UHFFFAOYSA-N Cc1cccc(C)c1 Chemical compound Cc1cccc(C)c1 IVSZLXZYQVIEFR-UHFFFAOYSA-N 0.000 description 2
- COIOBXNSKPZVEZ-UHFFFAOYSA-N Brc([s]1)n[n]2c1nc(-c1cc(c(OCc3ccccc3)ccc3)c3[o]1)c2 Chemical compound Brc([s]1)n[n]2c1nc(-c1cc(c(OCc3ccccc3)ccc3)c3[o]1)c2 COIOBXNSKPZVEZ-UHFFFAOYSA-N 0.000 description 1
- HMDXNKYJONMJPU-UHFFFAOYSA-N COc([s]1)n[n]2c1nc(-c([o]c1cc(OC)c3)cc1c3OCc1cnn[n]1-c1ccccc1)c2 Chemical compound COc([s]1)n[n]2c1nc(-c([o]c1cc(OC)c3)cc1c3OCc1cnn[n]1-c1ccccc1)c2 HMDXNKYJONMJPU-UHFFFAOYSA-N 0.000 description 1
- KRDDTIMFUUMXBL-UHFFFAOYSA-N COc([s]1)n[n]2c1nc(-c1cc(c(OCc3ccccc3)cc(OC)c3)c3[o]1)c2 Chemical compound COc([s]1)n[n]2c1nc(-c1cc(c(OCc3ccccc3)cc(OC)c3)c3[o]1)c2 KRDDTIMFUUMXBL-UHFFFAOYSA-N 0.000 description 1
- GSJFSQJHCJBDIN-ZDUSSCGKSA-N C[C@@H](c([s]1)n[n]2c1nc(-c1cc(c(OCc3c[s]c(-c4ccccc4)n3)cc(F)c3)c3[o]1)c2)F Chemical compound C[C@@H](c([s]1)n[n]2c1nc(-c1cc(c(OCc3c[s]c(-c4ccccc4)n3)cc(F)c3)c3[o]1)c2)F GSJFSQJHCJBDIN-ZDUSSCGKSA-N 0.000 description 1
- CHLICZRVGGXEOD-UHFFFAOYSA-N Cc(cc1)ccc1OC Chemical compound Cc(cc1)ccc1OC CHLICZRVGGXEOD-UHFFFAOYSA-N 0.000 description 1
- JQUPVYKQQXTQIW-UHFFFAOYSA-N Cc(cc1)n[n]2c1nc(-c1cc(c(OCc3c[s]c(-c4ccccc4)n3)cc(OC)c3)c3[o]1)c2 Chemical compound Cc(cc1)n[n]2c1nc(-c1cc(c(OCc3c[s]c(-c4ccccc4)n3)cc(OC)c3)c3[o]1)c2 JQUPVYKQQXTQIW-UHFFFAOYSA-N 0.000 description 1
- MMZYCBHLNZVROM-UHFFFAOYSA-N Cc(cccc1)c1F Chemical compound Cc(cccc1)c1F MMZYCBHLNZVROM-UHFFFAOYSA-N 0.000 description 1
- VJYXZJGDFJJDGF-UHFFFAOYSA-N Cc1cc(C(F)(F)F)ccc1 Chemical compound Cc1cc(C(F)(F)F)ccc1 VJYXZJGDFJJDGF-UHFFFAOYSA-N 0.000 description 1
- BTQZKHUEUDPRST-UHFFFAOYSA-N Cc1cc(F)ccc1 Chemical compound Cc1cc(F)ccc1 BTQZKHUEUDPRST-UHFFFAOYSA-N 0.000 description 1
- FXLOVSHXALFLKQ-UHFFFAOYSA-N Cc1ccc(C=O)cc1 Chemical compound Cc1ccc(C=O)cc1 FXLOVSHXALFLKQ-UHFFFAOYSA-N 0.000 description 1
- SWYJSAXHEMNYLQ-UHFFFAOYSA-N Cc1cccc([F]C)c1 Chemical compound Cc1cccc([F]C)c1 SWYJSAXHEMNYLQ-UHFFFAOYSA-N 0.000 description 1
- CTQNGGLPUBDAKN-UHFFFAOYSA-N Cc1ccccc1C Chemical compound Cc1ccccc1C CTQNGGLPUBDAKN-UHFFFAOYSA-N 0.000 description 1
- KRCIFTBSQKDYMH-UHFFFAOYSA-N Cc1nc(CO)c[s]1 Chemical compound Cc1nc(CO)c[s]1 KRCIFTBSQKDYMH-UHFFFAOYSA-N 0.000 description 1
Images
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/04—Linear peptides containing only normal peptide links
- C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/705—Receptors; Cell surface antigens; Cell surface determinants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Genetics & Genomics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- General Health & Medical Sciences (AREA)
- Zoology (AREA)
- Immunology (AREA)
- Toxicology (AREA)
- Gastroenterology & Hepatology (AREA)
- Cell Biology (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261638577P | 2012-04-26 | 2012-04-26 | |
| US61/638,577 | 2012-04-26 | ||
| US201361781538P | 2013-03-14 | 2013-03-14 | |
| US61/781,538 | 2013-03-14 | ||
| PCT/US2013/037897 WO2013163248A1 (en) | 2012-04-26 | 2013-04-24 | Par4 agonist peptides |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2015516983A true JP2015516983A (ja) | 2015-06-18 |
| JP2015516983A5 JP2015516983A5 (enExample) | 2015-08-20 |
Family
ID=48289680
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015509095A Pending JP2015516983A (ja) | 2012-04-26 | 2013-04-24 | Par4アゴニストペプチド |
Country Status (9)
| Country | Link |
|---|---|
| US (3) | US8927688B2 (enExample) |
| EP (1) | EP2841448A1 (enExample) |
| JP (1) | JP2015516983A (enExample) |
| CN (1) | CN104411713A (enExample) |
| BR (1) | BR112014026644A2 (enExample) |
| CA (1) | CA2871640A1 (enExample) |
| EA (1) | EA201491959A1 (enExample) |
| MX (1) | MX2014012803A (enExample) |
| WO (1) | WO2013163248A1 (enExample) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2015514808A (ja) * | 2012-04-26 | 2015-05-21 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | 血小板凝集を治療するためのプロテアーゼ活性化受容体4(par4)阻害剤としてのイミダゾチアジアゾールおよびイミダゾピラジン誘導体 |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2015061733A1 (en) * | 2013-10-25 | 2015-04-30 | Bristol-Meyers Squibb Company | Diagnostic methods for par4 antagonist therapy |
| WO2016134450A1 (en) | 2015-02-26 | 2016-09-01 | Université de Montréal | Imidazopyridazine and imidazothiadiazole compounds |
| US9789087B2 (en) | 2015-08-03 | 2017-10-17 | Thomas Jefferson University | PAR4 inhibitor therapy for patients with PAR4 polymorphism |
| US9963466B2 (en) | 2016-03-07 | 2018-05-08 | Vanderbilt University | Substituted 5-membered heterocyclic analogs as protease activated receptor 4 (PAR-4) antagonists |
| US20190119300A1 (en) * | 2016-04-18 | 2019-04-25 | Vanderbilt University | Substituted and fused 6-membered protease activated receptor 4 (par-4) antagonists |
| WO2019149205A1 (zh) * | 2018-01-31 | 2019-08-08 | 江苏恒瑞医药股份有限公司 | 苯并杂芳基类衍生物、其制备方法及其在医药上的应用 |
| CN110218218B (zh) * | 2018-03-01 | 2022-04-08 | 江苏恒瑞医药股份有限公司 | 苯并呋喃类衍生物、其制备方法及其在医药上的应用 |
| CN110627817B (zh) * | 2018-06-25 | 2022-03-29 | 中国药科大学 | 咪唑并环类par4拮抗剂及其医药用途 |
| CN111349105B (zh) * | 2018-12-24 | 2023-04-07 | 江苏恒瑞医药股份有限公司 | 苯并呋喃类衍生物、其制备方法及其在医药上的应用 |
| CN111362970A (zh) * | 2018-12-25 | 2020-07-03 | 天津药物研究院有限公司 | 苯并呋喃类衍生物及其制备方法和用途 |
| US12077607B2 (en) | 2021-09-23 | 2024-09-03 | University Of Utah Research Foundation | Functional and therapeutic effects of PAR4 cleavage by cathepsin G |
| CN117285527A (zh) * | 2023-09-25 | 2023-12-26 | 中国药科大学 | 一种噌啉类par4拮抗剂及其医药应用 |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0667345A1 (en) * | 1994-02-14 | 1995-08-16 | Yung Shin Pharm. Ind. Co. Ltd. | 1-Benzyl-3-(substituted aryl)-condensed pyrazole derivatives as inhibitors of platelet aggregation |
| WO2001058930A1 (en) * | 2000-02-09 | 2001-08-16 | Zymogenetics, Inc. | Par4 peptides and polypeptides |
| WO2001094411A1 (en) * | 2000-06-05 | 2001-12-13 | The Regents Of The University Of California | Peptides modulating protease activated receptors and methods of using same |
| EP1166785A1 (en) * | 2000-06-19 | 2002-01-02 | Yung Shin Pharmeutical Ind. Co., Ltd. | Use of pyrazole derivatives for inhibiting thrombin-induced platelet aggregation |
| WO2003033515A1 (en) * | 2001-10-15 | 2003-04-24 | Corixa Corporation | Compositions and methods for the therapy and diagnosis of acne vulgaris |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE602004006529T2 (de) | 2003-10-31 | 2008-01-31 | Janssen Pharmaceutica N.V. | Phenoxyessigsäure-derivate als peroxisom-proliferator-aktivierte rezeptor (ppar) dual-agonisten |
-
2013
- 2013-04-24 BR BR112014026644A patent/BR112014026644A2/pt not_active IP Right Cessation
- 2013-04-24 WO PCT/US2013/037897 patent/WO2013163248A1/en not_active Ceased
- 2013-04-24 CN CN201380034451.0A patent/CN104411713A/zh active Pending
- 2013-04-24 JP JP2015509095A patent/JP2015516983A/ja active Pending
- 2013-04-24 CA CA2871640A patent/CA2871640A1/en not_active Abandoned
- 2013-04-24 EP EP13720698.3A patent/EP2841448A1/en not_active Withdrawn
- 2013-04-24 MX MX2014012803A patent/MX2014012803A/es unknown
- 2013-04-24 US US13/869,093 patent/US8927688B2/en active Active
- 2013-04-24 EA EA201491959A patent/EA201491959A1/ru unknown
-
2014
- 2014-11-26 US US14/554,387 patent/US9303065B2/en active Active
-
2016
- 2016-02-23 US US15/051,067 patent/US9605024B2/en active Active
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0667345A1 (en) * | 1994-02-14 | 1995-08-16 | Yung Shin Pharm. Ind. Co. Ltd. | 1-Benzyl-3-(substituted aryl)-condensed pyrazole derivatives as inhibitors of platelet aggregation |
| WO2001058930A1 (en) * | 2000-02-09 | 2001-08-16 | Zymogenetics, Inc. | Par4 peptides and polypeptides |
| WO2001094411A1 (en) * | 2000-06-05 | 2001-12-13 | The Regents Of The University Of California | Peptides modulating protease activated receptors and methods of using same |
| EP1166785A1 (en) * | 2000-06-19 | 2002-01-02 | Yung Shin Pharmeutical Ind. Co., Ltd. | Use of pyrazole derivatives for inhibiting thrombin-induced platelet aggregation |
| WO2003033515A1 (en) * | 2001-10-15 | 2003-04-24 | Corixa Corporation | Compositions and methods for the therapy and diagnosis of acne vulgaris |
Non-Patent Citations (1)
| Title |
|---|
| JPN6016023672; T.R.Faruqi, et al., J Biol Chem., 2000, 275(26), pp19728-19734 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2015514808A (ja) * | 2012-04-26 | 2015-05-21 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | 血小板凝集を治療するためのプロテアーゼ活性化受容体4(par4)阻害剤としてのイミダゾチアジアゾールおよびイミダゾピラジン誘導体 |
Also Published As
| Publication number | Publication date |
|---|---|
| CA2871640A1 (en) | 2013-10-31 |
| EP2841448A1 (en) | 2015-03-04 |
| US8927688B2 (en) | 2015-01-06 |
| US20160304560A1 (en) | 2016-10-20 |
| CN104411713A (zh) | 2015-03-11 |
| MX2014012803A (es) | 2015-01-15 |
| US20130289238A1 (en) | 2013-10-31 |
| BR112014026644A2 (pt) | 2017-06-27 |
| US9303065B2 (en) | 2016-04-05 |
| EA201491959A1 (ru) | 2016-05-31 |
| US9605024B2 (en) | 2017-03-28 |
| US20150158910A1 (en) | 2015-06-11 |
| WO2013163248A1 (en) | 2013-10-31 |
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