JP2002503674A - βシート模倣物およびその使用に関する方法 - Google Patents
βシート模倣物およびその使用に関する方法Info
- Publication number
- JP2002503674A JP2002503674A JP2000531467A JP2000531467A JP2002503674A JP 2002503674 A JP2002503674 A JP 2002503674A JP 2000531467 A JP2000531467 A JP 2000531467A JP 2000531467 A JP2000531467 A JP 2000531467A JP 2002503674 A JP2002503674 A JP 2002503674A
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- Pending
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- 239000004945 silicone rubber Substances 0.000 description 1
- URGAHOPLAPQHLN-UHFFFAOYSA-N sodium aluminosilicate Chemical compound [Na+].[Al+3].[O-][Si]([O-])=O.[O-][Si]([O-])=O URGAHOPLAPQHLN-UHFFFAOYSA-N 0.000 description 1
- WXMKPNITSTVMEF-UHFFFAOYSA-M sodium benzoate Chemical compound [Na+].[O-]C(=O)C1=CC=CC=C1 WXMKPNITSTVMEF-UHFFFAOYSA-M 0.000 description 1
- 239000004299 sodium benzoate Substances 0.000 description 1
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- 235000011006 sodium potassium tartrate Nutrition 0.000 description 1
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- 229940075582 sorbic acid Drugs 0.000 description 1
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- 238000001228 spectrum Methods 0.000 description 1
- 238000013222 sprague-dawley male rat Methods 0.000 description 1
- 206010041823 squamous cell carcinoma Diseases 0.000 description 1
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- 108010087686 src-Family Kinases Proteins 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- 238000010561 standard procedure Methods 0.000 description 1
- HKSZLNNOFSGOKW-FYTWVXJKSA-N staurosporine Chemical compound C12=C3N4C5=CC=CC=C5C3=C3CNC(=O)C3=C2C2=CC=CC=C2N1[C@H]1C[C@@H](NC)[C@@H](OC)[C@]4(C)O1 HKSZLNNOFSGOKW-FYTWVXJKSA-N 0.000 description 1
- CGPUWJWCVCFERF-UHFFFAOYSA-N staurosporine Natural products C12=C3N4C5=CC=CC=C5C3=C3CNC(=O)C3=C2C2=CC=CC=C2N1C1CC(NC)C(OC)C4(OC)O1 CGPUWJWCVCFERF-UHFFFAOYSA-N 0.000 description 1
- 230000004936 stimulating effect Effects 0.000 description 1
- 210000002784 stomach Anatomy 0.000 description 1
- 229960005202 streptokinase Drugs 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- RVEZZJVBDQCTEF-UHFFFAOYSA-N sulfenic acid Chemical compound SO RVEZZJVBDQCTEF-UHFFFAOYSA-N 0.000 description 1
- BUUPQKDIAURBJP-UHFFFAOYSA-N sulfinic acid Chemical compound OS=O BUUPQKDIAURBJP-UHFFFAOYSA-N 0.000 description 1
- 239000011593 sulfur Substances 0.000 description 1
- 238000001356 surgical procedure Methods 0.000 description 1
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- 230000002195 synergetic effect Effects 0.000 description 1
- 230000002194 synthesizing effect Effects 0.000 description 1
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- 235000020357 syrup Nutrition 0.000 description 1
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- 208000009056 telangiectasis Diseases 0.000 description 1
- DSPYCWLYGXGJNJ-UHFFFAOYSA-N tert-butyl n-prop-2-ynylcarbamate Chemical compound CC(C)(C)OC(=O)NCC#C DSPYCWLYGXGJNJ-UHFFFAOYSA-N 0.000 description 1
- BCNZYOJHNLTNEZ-UHFFFAOYSA-N tert-butyldimethylsilyl chloride Chemical compound CC(C)(C)[Si](C)(C)Cl BCNZYOJHNLTNEZ-UHFFFAOYSA-N 0.000 description 1
- 125000005931 tert-butyloxycarbonyl group Chemical group [H]C([H])([H])C(OC(*)=O)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- GMRIOAVKKGNMMV-UHFFFAOYSA-N tetrabutylazanium;azide Chemical compound [N-]=[N+]=[N-].CCCC[N+](CCCC)(CCCC)CCCC GMRIOAVKKGNMMV-UHFFFAOYSA-N 0.000 description 1
- DPKBAXPHAYBPRL-UHFFFAOYSA-M tetrabutylazanium;iodide Chemical compound [I-].CCCC[N+](CCCC)(CCCC)CCCC DPKBAXPHAYBPRL-UHFFFAOYSA-M 0.000 description 1
- RAOIDOHSFRTOEL-UHFFFAOYSA-N tetrahydrothiophene Chemical compound C1CCSC1 RAOIDOHSFRTOEL-UHFFFAOYSA-N 0.000 description 1
- 125000004301 thiazolin-2-yl group Chemical group [H]C1([H])SC(*)=NC1([H])[H] 0.000 description 1
- 229960000103 thrombolytic agent Drugs 0.000 description 1
- 230000002537 thrombolytic effect Effects 0.000 description 1
- 210000001685 thyroid gland Anatomy 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
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- 230000000699 topical effect Effects 0.000 description 1
- 230000002103 transcriptional effect Effects 0.000 description 1
- 238000012546 transfer Methods 0.000 description 1
- 230000014616 translation Effects 0.000 description 1
- 102000035160 transmembrane proteins Human genes 0.000 description 1
- 108091005703 transmembrane proteins Proteins 0.000 description 1
- 238000002054 transplantation Methods 0.000 description 1
- 150000003852 triazoles Chemical class 0.000 description 1
- YFMZQCCTZUJXEB-UHFFFAOYSA-N tris(methylsulfanyl)methane Chemical compound CSC(SC)SC YFMZQCCTZUJXEB-UHFFFAOYSA-N 0.000 description 1
- 239000002753 trypsin inhibitor Substances 0.000 description 1
- 239000002750 tryptase inhibitor Substances 0.000 description 1
- 230000005748 tumor development Effects 0.000 description 1
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- 239000004474 valine Substances 0.000 description 1
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- 210000004509 vascular smooth muscle cell Anatomy 0.000 description 1
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- 230000007998 vessel formation Effects 0.000 description 1
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- 210000002845 virion Anatomy 0.000 description 1
- 230000029302 virus maturation Effects 0.000 description 1
- PJVWKTKQMONHTI-UHFFFAOYSA-N warfarin Chemical compound OC=1C2=CC=CC=C2OC(=O)C=1C(CC(=O)C)C1=CC=CC=C1 PJVWKTKQMONHTI-UHFFFAOYSA-N 0.000 description 1
- 229960005080 warfarin Drugs 0.000 description 1
- 239000008215 water for injection Substances 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/44—Iso-indoles; Hydrogenated iso-indoles
- C07D209/48—Iso-indoles; Hydrogenated iso-indoles with oxygen atoms in positions 1 and 3, e.g. phthalimide
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06139—Dipeptides with the first amino acid being heterocyclic
-
- 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
-
- 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)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Indole Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Peptides Or Proteins (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/US1998/002891 WO1999041276A1 (en) | 1998-02-12 | 1998-02-12 | β-SHEET MIMETICS AND METHODS RELATING TO THE USE THEREOF |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2002503674A true JP2002503674A (ja) | 2002-02-05 |
| JP2002503674A5 JP2002503674A5 (enExample) | 2005-12-22 |
Family
ID=22266392
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2000531467A Pending JP2002503674A (ja) | 1998-02-12 | 1998-02-12 | βシート模倣物およびその使用に関する方法 |
Country Status (9)
| Country | Link |
|---|---|
| EP (1) | EP1053246B1 (enExample) |
| JP (1) | JP2002503674A (enExample) |
| KR (1) | KR20010040939A (enExample) |
| AT (1) | ATE230414T1 (enExample) |
| AU (1) | AU748887B2 (enExample) |
| CA (1) | CA2319766A1 (enExample) |
| DE (1) | DE69810513T2 (enExample) |
| ES (1) | ES2192764T3 (enExample) |
| WO (1) | WO1999041276A1 (enExample) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2005526722A (ja) * | 2002-02-14 | 2005-09-08 | ミリアド・ジェネティックス・インコーポレイテッド | β−シートミメティックならびにそれに関連する組成物および方法 |
| JP2011525927A (ja) * | 2008-06-25 | 2011-09-29 | シェーリング コーポレイション | 複素環式抗菌剤の合成および使用 |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6699855B2 (en) * | 2000-02-29 | 2004-03-02 | Bristol-Myers Squibb Company | Inhibitors of hepatitis C virus NS3 protease |
| US6534651B2 (en) | 2000-04-06 | 2003-03-18 | Inotek Pharmaceuticals Corp. | 7-Substituted isoindolinone inhibitors of inflammation and reperfusion injury and methods of use thereof |
| US7122679B2 (en) | 2000-05-09 | 2006-10-17 | Cephalon, Inc. | Multicyclic compounds and the use thereof |
| US20060276497A1 (en) | 2000-05-09 | 2006-12-07 | Cephalon, Inc. | Novel multicyclic compounds and the use thereof |
| RU2728785C2 (ru) | 2014-10-06 | 2020-07-31 | Кортексим, Инк. | Ингибиторы лизинспецифичного гингипаина |
| 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 |
| PT3486242T (pt) | 2016-08-31 | 2022-01-06 | Jiangsu Hengrui Medicine Co | Derivado de oxopicolinamida, método de preparação para esse fim e utilização farmacêutica do mesmo |
| PE20190473A1 (es) | 2016-09-16 | 2019-04-04 | Cortexyme Inc | Inhibidores cetonicos de gingipain de lisina |
| WO2020007256A1 (zh) | 2018-07-02 | 2020-01-09 | 江苏恒瑞医药股份有限公司 | 一种氧代吡啶酰胺类衍生物的晶型及制备方法 |
| MX2022003649A (es) | 2019-09-27 | 2022-06-08 | Shenzhen Salubris Pharm Co Ltd | Inhibidores del fxia y metodo de preparacion de los mismos y uso farmaceutico de los mismos. |
Citations (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH06340691A (ja) * | 1993-03-08 | 1994-12-13 | Sandoz Ag | ペプチド類 |
| WO1996019483A1 (en) * | 1994-12-22 | 1996-06-27 | Biochem Pharma Inc. | Low molecular weight bicyclic thrombin inhibitors |
| WO1996030396A1 (en) * | 1995-03-24 | 1996-10-03 | Molecumetics Ltd. | β-SHEET MIMETICS AND USE THEREOF AS PROTEASE INHIBITORS |
| WO1996030035A1 (en) * | 1995-03-24 | 1996-10-03 | Molecumetics Ltd. | β-SHEET MIMETICS AND USE THEREOF AS INHIBITORS OF BIOLOGICALLY ACTIVE PEPTIDES OR PROTEINS |
| JPH08325152A (ja) * | 1995-05-17 | 1996-12-10 | Bristol Myers Squibb Co | Aceおよびnepの抑制に有用なベンゾ縮合アゼピノンおよびピペリジノン化合物 |
| WO1997005160A1 (en) * | 1995-08-01 | 1997-02-13 | A. Menarini Industrie Farmaceutiche Riunite S.R.L. | Bicyclic lactam derivatives as thrombin inhibitors |
| 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 |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU668707B2 (en) * | 1992-02-14 | 1996-05-16 | Merrell Pharmaceuticals Inc. | Aminoacetylmercaptoacetylamide derivatives useful as inhibitors of enkephalinase and ACE |
| CA2133963C (en) * | 1992-05-15 | 1998-07-07 | Gary A. Flynn | Novel mercaptoacetylamido pyridazo[1,2]pyridazine, pyrazolo[1,2]pyridazine, pyridazo[1,2-a][1,2]diazepine and pyrazolo[1,2-a][1,2]diazepine derivatives useful as inhibitors of enkephalinase and ace |
-
1998
- 1998-02-12 AU AU66557/98A patent/AU748887B2/en not_active Ceased
- 1998-02-12 JP JP2000531467A patent/JP2002503674A/ja active Pending
- 1998-02-12 KR KR1020007008856A patent/KR20010040939A/ko not_active Ceased
- 1998-02-12 CA CA002319766A patent/CA2319766A1/en not_active Abandoned
- 1998-02-12 EP EP98908551A patent/EP1053246B1/en not_active Expired - Lifetime
- 1998-02-12 DE DE69810513T patent/DE69810513T2/de not_active Expired - Lifetime
- 1998-02-12 ES ES98908551T patent/ES2192764T3/es not_active Expired - Lifetime
- 1998-02-12 AT AT98908551T patent/ATE230414T1/de not_active IP Right Cessation
- 1998-02-12 WO PCT/US1998/002891 patent/WO1999041276A1/en not_active Ceased
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH06340691A (ja) * | 1993-03-08 | 1994-12-13 | Sandoz Ag | ペプチド類 |
| WO1996019483A1 (en) * | 1994-12-22 | 1996-06-27 | Biochem Pharma Inc. | Low molecular weight bicyclic thrombin inhibitors |
| WO1996030396A1 (en) * | 1995-03-24 | 1996-10-03 | Molecumetics Ltd. | β-SHEET MIMETICS AND USE THEREOF AS PROTEASE INHIBITORS |
| WO1996030035A1 (en) * | 1995-03-24 | 1996-10-03 | Molecumetics Ltd. | β-SHEET MIMETICS AND USE THEREOF AS INHIBITORS OF BIOLOGICALLY ACTIVE PEPTIDES OR PROTEINS |
| JPH08325152A (ja) * | 1995-05-17 | 1996-12-10 | Bristol Myers Squibb Co | Aceおよびnepの抑制に有用なベンゾ縮合アゼピノンおよびピペリジノン化合物 |
| WO1997005160A1 (en) * | 1995-08-01 | 1997-02-13 | A. Menarini Industrie Farmaceutiche Riunite S.R.L. | Bicyclic lactam derivatives as thrombin inhibitors |
| 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 |
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| ADAM, W. ET AL., J. ORG. CHEM., vol. 58, no. 6, JPN6009008779, 1993, pages 1477 - 1482, ISSN: 0001259947 * |
| BALDWIN, J.E. ET AL., HETEROCYCLES, vol. 34, no. 5, JPN6009008787, 1992, pages 903 - 906, ISSN: 0001259951 * |
| BERNABEU, M.C. ET AL., TETRAHEDRON LETT., vol. 37, no. 20, JPN6009008789, 1996, pages 3595 - 3598, ISSN: 0001259952 * |
| HANESSIAN, S. ET AL., BIOORG. MED. CHEM. LETT., vol. 4, no. 11, JPN6009008781, 1994, pages 1397 - 1400, ISSN: 0001259948 * |
| NAKANISHI, H. ET AL., PROC. NATL. ACAD. SCI. USA, vol. 89, JPN6009008785, March 1992 (1992-03-01), pages 1705 - 1709, ISSN: 0001259950 * |
| SALIMBENI, A. ET AL., BIOORG. MED. CHEM. LETT., vol. 7, no. 17, JPN6009008783, 1997, pages 2205 - 2210, ISSN: 0001259949 * |
| SLOMCZYNSKA, U. ET AL., J. ORG. CHEM., vol. 61, no. 4, JPN6009008777, 1996, pages 1198 - 1204, ISSN: 0001259946 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2005526722A (ja) * | 2002-02-14 | 2005-09-08 | ミリアド・ジェネティックス・インコーポレイテッド | β−シートミメティックならびにそれに関連する組成物および方法 |
| JP2011525927A (ja) * | 2008-06-25 | 2011-09-29 | シェーリング コーポレイション | 複素環式抗菌剤の合成および使用 |
Also Published As
| Publication number | Publication date |
|---|---|
| EP1053246B1 (en) | 2003-01-02 |
| DE69810513T2 (de) | 2004-03-18 |
| CA2319766A1 (en) | 1999-08-19 |
| AU6655798A (en) | 1999-08-30 |
| DE69810513D1 (de) | 2003-02-06 |
| WO1999041276A1 (en) | 1999-08-19 |
| EP1053246A1 (en) | 2000-11-22 |
| KR20010040939A (ko) | 2001-05-15 |
| AU748887B2 (en) | 2002-06-13 |
| ATE230414T1 (de) | 2003-01-15 |
| ES2192764T3 (es) | 2003-10-16 |
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