DK0752987T3 - Pyrimidinylderivater som interleukininhibitorer - Google Patents
Pyrimidinylderivater som interleukininhibitorerInfo
- Publication number
- DK0752987T3 DK0752987T3 DK95915448T DK95915448T DK0752987T3 DK 0752987 T3 DK0752987 T3 DK 0752987T3 DK 95915448 T DK95915448 T DK 95915448T DK 95915448 T DK95915448 T DK 95915448T DK 0752987 T3 DK0752987 T3 DK 0752987T3
- Authority
- DK
- Denmark
- Prior art keywords
- beta
- compounds
- aspartic acid
- protease activity
- pyrimidinyl
- Prior art date
Links
- 229940046732 interleukin inhibitors Drugs 0.000 title 1
- 125000000714 pyrimidinyl group Chemical group 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 108091005804 Peptidases Proteins 0.000 abstract 2
- 239000004365 Protease Substances 0.000 abstract 2
- 102100037486 Reverse transcriptase/ribonuclease H Human genes 0.000 abstract 2
- 230000000694 effects Effects 0.000 abstract 2
- TVZJDRYAFYBTRU-YFKPBYRVSA-N (2s)-2-(pyrimidin-2-ylamino)butanedioic acid Chemical compound OC(=O)C[C@@H](C(O)=O)NC1=NC=CC=N1 TVZJDRYAFYBTRU-YFKPBYRVSA-N 0.000 abstract 1
- LOGFVTREOLYCPF-KXNHARMFSA-N (2s,3r)-2-[[(2r)-1-[(2s)-2,6-diaminohexanoyl]pyrrolidine-2-carbonyl]amino]-3-hydroxybutanoic acid Chemical compound C[C@@H](O)[C@@H](C(O)=O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](N)CCCCN LOGFVTREOLYCPF-KXNHARMFSA-N 0.000 abstract 1
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical class CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 abstract 1
- 102000004190 Enzymes Human genes 0.000 abstract 1
- 108090000790 Enzymes Proteins 0.000 abstract 1
- 102000003777 Interleukin-1 beta Human genes 0.000 abstract 1
- 108090000193 Interleukin-1 beta Proteins 0.000 abstract 1
- 241000124008 Mammalia Species 0.000 abstract 1
- 235000003704 aspartic acid Nutrition 0.000 abstract 1
- -1 aspartic acid aldehydes Chemical class 0.000 abstract 1
- OQFSQFPPLPISGP-UHFFFAOYSA-N beta-carboxyaspartic acid Natural products OC(=O)C(N)C(C(O)=O)C(O)=O OQFSQFPPLPISGP-UHFFFAOYSA-N 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 230000000144 pharmacologic effect Effects 0.000 abstract 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
- C07K5/06139—Dipeptides with the first amino acid being heterocyclic
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- 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
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/645—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
- C07F9/6509—Six-membered rings
- C07F9/6512—Six-membered rings having the nitrogen atoms in positions 1 and 3
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
- C07K5/0202—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
-
- 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
- C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
-
- 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)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Crystallography & Structural Chemistry (AREA)
- Immunology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Enzymes And Modification Thereof (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US22171294A | 1994-03-31 | 1994-03-31 | |
| PCT/US1995/003909 WO1995026958A1 (en) | 1994-03-31 | 1995-03-29 | Pyrimidinyl derivatives as interleukin inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DK0752987T3 true DK0752987T3 (da) | 2004-03-15 |
Family
ID=22829018
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK95915448T DK0752987T3 (da) | 1994-03-31 | 1995-03-29 | Pyrimidinylderivater som interleukininhibitorer |
Country Status (18)
| Country | Link |
|---|---|
| US (3) | US5670494A (da) |
| EP (1) | EP0752987B1 (da) |
| JP (1) | JP3703836B2 (da) |
| CN (2) | CN1504462A (da) |
| AT (1) | ATE254111T1 (da) |
| AU (1) | AU703451B2 (da) |
| CA (1) | CA2186511C (da) |
| DE (1) | DE69532113T2 (da) |
| DK (1) | DK0752987T3 (da) |
| ES (1) | ES2210289T3 (da) |
| FI (1) | FI112943B (da) |
| HK (1) | HK1012623A1 (da) |
| HU (1) | HU224731B1 (da) |
| MX (1) | MX9604420A (da) |
| NO (1) | NO308603B1 (da) |
| NZ (1) | NZ283876A (da) |
| PT (1) | PT752987E (da) |
| WO (1) | WO1995026958A1 (da) |
Families Citing this family (46)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5874424A (en) * | 1995-12-20 | 1999-02-23 | Vertex Pharmaceuticals Incorporated | Inhibitors of interleukin-1β converting enzyme |
| US6008217A (en) * | 1995-12-20 | 1999-12-28 | Vertex Pharmaceuticals Incorporated | Inhibitors of interleukin-1β converting enzyme |
| US6204261B1 (en) | 1995-12-20 | 2001-03-20 | Vertex Pharmaceuticals Incorporated | Inhibitors of interleukin-1β Converting enzyme inhibitors |
| US5714484A (en) * | 1993-12-08 | 1998-02-03 | Prototek, Inc. | α-(1,3-dicarbonylenol ether) methyl ketones as cysteine protease inhibitors |
| JP3703836B2 (ja) | 1994-03-31 | 2005-10-05 | バーテックス ファーマシューティカルズ インコーポレイティド | インターロイキン阻害剤としてのピリミジニル誘導体 |
| US6420522B1 (en) | 1995-06-05 | 2002-07-16 | Vertex Pharmaceuticals Incorporated | Inhibitors of interleukin-1β converting enzyme |
| US5716929A (en) * | 1994-06-17 | 1998-02-10 | Vertex Pharmaceuticals, Inc. | Inhibitors of interleukin-1β converting enzyme |
| US5756466A (en) * | 1994-06-17 | 1998-05-26 | Vertex Pharmaceuticals, Inc. | Inhibitors of interleukin-1β converting enzyme |
| US5847135A (en) * | 1994-06-17 | 1998-12-08 | Vertex Pharmaceuticals, Incorporated | Inhibitors of interleukin-1β converting enzyme |
| US6001814A (en) * | 1994-11-21 | 1999-12-14 | Cortech Inc. | Serine protease inhibitors |
| ATE217321T1 (de) * | 1994-12-13 | 2002-05-15 | Corvas Int Inc | Aromatische heterocyclische derivate als enzyminhibitoren |
| US6011158A (en) * | 1994-12-13 | 2000-01-04 | Corvas International, Inc. | Aromatic heterocyclic derivatives as enzyme inhibitors |
| EP0820464A2 (en) * | 1995-03-31 | 1998-01-28 | Takeda Chemical Industries, Ltd. | Cysteine protease inhibitor |
| CA2219364A1 (en) * | 1995-04-27 | 1996-10-31 | Hideki Okunishi | Heterocyclic amide compounds and pharmaceutical use thereof |
| US5843904A (en) * | 1995-12-20 | 1998-12-01 | Vertex Pharmaceuticals, Inc. | Inhibitors of interleukin-1βconverting enzyme |
| EP0900791A1 (en) * | 1995-12-27 | 1999-03-10 | Ono Pharmaceutical Co., Ltd. | Tetrazole derivatives and drugs containing the same as the active ingredient |
| EP0932600B1 (en) * | 1996-10-11 | 2006-02-08 | Warner-Lambert Company Llc | Sulfonamide substituted aspartic acid interleukin-1beta converting enzyme inhibitors |
| US6316415B1 (en) | 1996-10-11 | 2001-11-13 | Basf Aktiengesellschaft | Sulfonamide interleukin-1β converting enzyme inhibitors |
| US5919790A (en) * | 1996-10-11 | 1999-07-06 | Warner-Lambert Company | Hydroxamate inhibitors of interleukin-1β converting enzyme |
| EP1049703B1 (en) * | 1998-01-20 | 2003-02-12 | Warner-Lambert Company | N-[2-(5-benzyloxycarbonyl-amino-6-oxo-2-(4-fluorophenyl)-1,6-dihydro-1-pyrimidinyl)acetoxyl]-l-aspartic acid aldehyde as an in vivo inhibitor of interleukin-1beta converting enzyme |
| DE69925581T2 (de) | 1998-03-09 | 2006-04-27 | Vertex Pharmaceuticals Inc., Cambridge | 1,2-diazepanderivate als inhibitoren des interleukin-1beta umwandelnden enzyms |
| ATE410439T1 (de) | 1998-03-19 | 2008-10-15 | Vertex Pharma | Caspase inhibitoren |
| JP2003535022A (ja) * | 1998-06-03 | 2003-11-25 | コーテック インコーポレーテッド | セリンプロテアーゼ阻害剤としてのアルファー‐ケトオキサジアゾール含有ペプトイド及び非ペプトイド |
| EP1098902A4 (en) | 1998-07-23 | 2002-07-24 | Yeda Res & Dev | TREATMENT OF AUTOIMMUNE DISEASES BY COPOLYMER 1 AND SIMILAR COPOLYMERS AND PEPTIDES |
| ES2527760T3 (es) * | 1998-07-23 | 2015-01-29 | Yeda Research And Development Co., Ltd. | Tratamiento de enfermedad de Crohn con copolímero 1 y polipéptidos |
| US6800287B2 (en) * | 1998-09-25 | 2004-10-05 | Yeda Research And Development Co., Ltd. | Copolymer 1 related polypeptides for use as molecular weight markers and for therapeutic use |
| US6972296B2 (en) | 1999-05-07 | 2005-12-06 | Encysive Pharmaceuticals Inc. | Carboxylic acid derivatives that inhibit the binding of integrins to their receptors |
| US7022663B2 (en) * | 2000-02-18 | 2006-04-04 | Yeda Research And Development Co., Ltd. | Oral, nasal and pulmonary dosage formulations of copolymer 1 |
| EP2329842A3 (en) | 2000-05-12 | 2011-07-27 | Immunex Corporation | Interleukin-1 inhibitors in the treatment of diseases |
| PE20011350A1 (es) | 2000-05-19 | 2002-01-15 | Vertex Pharma | PROFARMACO DE UN INHIBIDOR DE ENZIMA CONVERTIDORA DE INTERLEUCINA-1ß (ICE) |
| US20020077278A1 (en) | 2000-06-05 | 2002-06-20 | Yong V. Wee | Use of glatiramer acetate (copolymer 1) in the treatment of central nervous system disorders |
| WO2002076503A1 (en) * | 2000-06-20 | 2002-10-03 | Mayo Foundation For Medical Education And Research | Treatment of central nervous system diseases by antibodies against glatiramer acetate |
| JP2004504302A (ja) * | 2000-07-18 | 2004-02-12 | ニューロジェン・コーポレーション | ５−置換２−アリール−４−ピリミジノン |
| ES2349033T3 (es) * | 2001-12-04 | 2010-12-22 | Teva Pharmaceutical Industries, Ltd. | Procedimientos para la medida de la actividad del acetato de glatiramer. |
| EP1485107A1 (en) * | 2002-02-11 | 2004-12-15 | Vertex Pharmaceuticals Incorporated | Phospholipids as caspase inhibitor prodrugs |
| US7001899B2 (en) * | 2002-06-10 | 2006-02-21 | The Procter & Gamble Company | Interleukin converting enzyme inhibitors |
| EP1553090A4 (en) * | 2002-06-14 | 2006-07-05 | Ajinomoto Kk | PROCESS FOR PREPARING A PYRIMIDINE COMPOUND |
| PE20050159A1 (es) | 2003-05-27 | 2005-04-19 | Vertex Pharma | Derivados de acido 3-[2-(3-amino-2-oxo-2h-piridin-1-il)-acetilamino]-4-oxo-pentanoico como inhibidores de caspasa |
| WO2005115362A1 (en) * | 2004-05-15 | 2005-12-08 | Vertex Pharmaceuticals Incorporated | Treating seizures using ice inhibitors |
| CA2567080A1 (en) | 2004-05-27 | 2005-12-15 | Vertex Pharmaceuticals Incorporated | Ice inhibitors for the treatment of autoinflammatory diseases |
| AU2005309776B2 (en) | 2004-11-24 | 2011-12-22 | Vertex Pharmaceuticals Incorporated | 3-[2-(3-acylamino-2-oxo-2h-pyridin-1-yl)-acetylamino]-4-oxo-pentanoic acid derivatives and their use as caspase inhibitors |
| KR20100072167A (ko) | 2007-08-03 | 2010-06-30 | 사노피-아벤티스 | 카스파제 이미징 프로브 |
| EP2262783A2 (en) * | 2008-02-21 | 2010-12-22 | Sanofi-Aventis | Covalently binding imaging probes |
| JP5980790B2 (ja) | 2010-11-05 | 2016-08-31 | ブランダイス ユニバーシティＢｒａｎｄｅｉｓ Ｕｎｉｖｅｒｓｉｔｙ | バイオマーカーとしての、ｉｃｅ切断されたアルファ−シヌクレイン |
| US9956260B1 (en) | 2011-07-22 | 2018-05-01 | The J. David Gladstone Institutes | Treatment of HIV-1 infection and AIDS |
| EP2848696A1 (en) | 2013-09-13 | 2015-03-18 | Sanofi-Aventis Deutschland GmbH | Caspase-1 imaging probes |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5441960A (en) * | 1992-04-16 | 1995-08-15 | Zeneca Limited | 1-pyrimidinylacetamide human leukocyte elastate inhibitors |
| JP3703836B2 (ja) * | 1994-03-31 | 2005-10-05 | バーテックス ファーマシューティカルズ インコーポレイティド | インターロイキン阻害剤としてのピリミジニル誘導体 |
-
1995
- 1995-03-29 JP JP52582195A patent/JP3703836B2/ja not_active Expired - Fee Related
- 1995-03-29 AT AT95915448T patent/ATE254111T1/de not_active IP Right Cessation
- 1995-03-29 CA CA002186511A patent/CA2186511C/en not_active Expired - Fee Related
- 1995-03-29 CN CNA031452183A patent/CN1504462A/zh active Pending
- 1995-03-29 EP EP95915448A patent/EP0752987B1/en not_active Expired - Lifetime
- 1995-03-29 AU AU22323/95A patent/AU703451B2/en not_active Ceased
- 1995-03-29 CN CN95193258A patent/CN1118458C/zh not_active Expired - Fee Related
- 1995-03-29 DE DE69532113T patent/DE69532113T2/de not_active Expired - Lifetime
- 1995-03-29 NZ NZ283876A patent/NZ283876A/en not_active IP Right Cessation
- 1995-03-29 WO PCT/US1995/003909 patent/WO1995026958A1/en active IP Right Grant
- 1995-03-29 MX MX9604420A patent/MX9604420A/es active IP Right Grant
- 1995-03-29 DK DK95915448T patent/DK0752987T3/da active
- 1995-03-29 ES ES95915448T patent/ES2210289T3/es not_active Expired - Lifetime
- 1995-03-29 PT PT95915448T patent/PT752987E/pt unknown
- 1995-03-29 HU HU9602664A patent/HU224731B1/hu not_active IP Right Cessation
- 1995-11-20 US US08/559,870 patent/US5670494A/en not_active Expired - Lifetime
-
1996
- 1996-09-26 NO NO964058A patent/NO308603B1/no unknown
- 1996-09-27 FI FI963897A patent/FI112943B/fi not_active IP Right Cessation
-
1997
- 1997-06-17 US US08/877,380 patent/US6162800A/en not_active Expired - Lifetime
-
1998
- 1998-12-16 HK HK98113788A patent/HK1012623A1/xx not_active IP Right Cessation
-
2000
- 2000-12-19 US US09/740,623 patent/US6407080B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| NZ283876A (en) | 2001-03-30 |
| CN1118458C (zh) | 2003-08-20 |
| AU2232395A (en) | 1995-10-23 |
| NO964058D0 (no) | 1996-09-26 |
| DE69532113T2 (de) | 2004-07-29 |
| CA2186511A1 (en) | 1995-10-12 |
| EP0752987B1 (en) | 2003-11-12 |
| EP0752987A4 (en) | 1997-04-09 |
| US6407080B2 (en) | 2002-06-18 |
| DE69532113D1 (de) | 2003-12-18 |
| US20010003750A1 (en) | 2001-06-14 |
| US6162800A (en) | 2000-12-19 |
| EP0752987A1 (en) | 1997-01-15 |
| HU224731B1 (en) | 2006-01-30 |
| WO1995026958A1 (en) | 1995-10-12 |
| PT752987E (pt) | 2004-03-31 |
| ES2210289T3 (es) | 2004-07-01 |
| AU703451B2 (en) | 1999-03-25 |
| NO964058L (no) | 1996-09-26 |
| CN1149292A (zh) | 1997-05-07 |
| FI112943B (fi) | 2004-02-13 |
| HK1012623A1 (en) | 1999-08-06 |
| FI963897A (fi) | 1996-09-27 |
| CN1504462A (zh) | 2004-06-16 |
| NO308603B1 (no) | 2000-10-02 |
| JP3703836B2 (ja) | 2005-10-05 |
| JPH09511249A (ja) | 1997-11-11 |
| ATE254111T1 (de) | 2003-11-15 |
| HU9602664D0 (en) | 1996-11-28 |
| CA2186511C (en) | 2009-02-10 |
| HUT75715A (en) | 1997-05-28 |
| US5670494A (en) | 1997-09-23 |
| FI963897A0 (fi) | 1996-09-27 |
| MX9604420A (es) | 1997-12-31 |
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