ZA200303848B - Protease inhibitors. - Google Patents
Protease inhibitors. Download PDFInfo
- Publication number
- ZA200303848B ZA200303848B ZA200303848A ZA200303848A ZA200303848B ZA 200303848 B ZA200303848 B ZA 200303848B ZA 200303848 A ZA200303848 A ZA 200303848A ZA 200303848 A ZA200303848 A ZA 200303848A ZA 200303848 B ZA200303848 B ZA 200303848B
- Authority
- ZA
- South Africa
- Prior art keywords
- galkyl
- substituted
- group
- methyl
- phenyl
- Prior art date
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- 229940042399 direct acting antivirals protease inhibitors Drugs 0.000 title description 8
- 239000000137 peptide hydrolase inhibitor Substances 0.000 title description 8
- -1 pentanonyl Chemical group 0.000 claims description 331
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- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 55
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- 108010005843 Cysteine Proteases Proteins 0.000 claims description 45
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 claims description 38
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 38
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- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 20
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- 229960002429 proline Drugs 0.000 description 1
- 230000001681 protective effect Effects 0.000 description 1
- 230000017854 proteolysis Effects 0.000 description 1
- 239000003586 protic polar solvent Substances 0.000 description 1
- 125000004309 pyranyl group Chemical group O1C(C=CC=C1)* 0.000 description 1
- 125000003373 pyrazinyl group Chemical group 0.000 description 1
- 125000003072 pyrazolidinyl group Chemical group 0.000 description 1
- 125000003226 pyrazolyl group Chemical group 0.000 description 1
- 125000002098 pyridazinyl group Chemical group 0.000 description 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 description 1
- 125000000168 pyrrolyl group Chemical group 0.000 description 1
- 150000003242 quaternary ammonium salts Chemical class 0.000 description 1
- 238000005956 quaternization reaction Methods 0.000 description 1
- 125000004621 quinuclidinyl group Chemical group N12C(CC(CC1)CC2)* 0.000 description 1
- 150000003254 radicals Chemical group 0.000 description 1
- 230000002441 reversible effect Effects 0.000 description 1
- 238000006798 ring closing metathesis reaction Methods 0.000 description 1
- 102200029256 rs121964925 Human genes 0.000 description 1
- 102220030673 rs59931416 Human genes 0.000 description 1
- 230000022932 ruffle assembly Effects 0.000 description 1
- 229910052707 ruthenium Inorganic materials 0.000 description 1
- 229920006395 saturated elastomer Polymers 0.000 description 1
- 238000007789 sealing Methods 0.000 description 1
- 150000003335 secondary amines Chemical class 0.000 description 1
- 229960001153 serine Drugs 0.000 description 1
- 239000003001 serine protease inhibitor Substances 0.000 description 1
- 210000002966 serum Anatomy 0.000 description 1
- 238000007086 side reaction Methods 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 239000001632 sodium acetate Substances 0.000 description 1
- 235000017281 sodium acetate Nutrition 0.000 description 1
- 239000012279 sodium borohydride Substances 0.000 description 1
- 229910000033 sodium borohydride Inorganic materials 0.000 description 1
- 239000001509 sodium citrate Substances 0.000 description 1
- NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 description 1
- 239000007790 solid phase Substances 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000007858 starting material Substances 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 239000000758 substrate Substances 0.000 description 1
- 229940124530 sulfonamide Drugs 0.000 description 1
- 150000003456 sulfonamides Chemical class 0.000 description 1
- 150000003871 sulfonates Chemical class 0.000 description 1
- YBBRCQOCSYXUOC-UHFFFAOYSA-N sulfuryl dichloride Chemical compound ClS(Cl)(=O)=O YBBRCQOCSYXUOC-UHFFFAOYSA-N 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 238000013268 sustained release Methods 0.000 description 1
- 239000012730 sustained-release form Substances 0.000 description 1
- 210000001258 synovial membrane Anatomy 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 235000012222 talc Nutrition 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- JGQSREKJPFNXQH-UHFFFAOYSA-N tert-butyl 1-aminocyclohexane-1-carboxylate Chemical compound CC(C)(C)OC(=O)C1(N)CCCCC1 JGQSREKJPFNXQH-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
- 125000001412 tetrahydropyranyl group Chemical group 0.000 description 1
- 125000005247 tetrazinyl group Chemical group N1=NN=NC(=C1)* 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 125000001113 thiadiazolyl group Chemical group 0.000 description 1
- 125000006090 thiamorpholinyl sulfone group Chemical group 0.000 description 1
- 125000006089 thiamorpholinyl sulfoxide group Chemical group 0.000 description 1
- 125000004495 thiazol-4-yl group Chemical group S1C=NC(=C1)* 0.000 description 1
- 125000002769 thiazolinyl group Chemical group 0.000 description 1
- 229960002898 threonine Drugs 0.000 description 1
- ZFDIRQKJPRINOQ-UHFFFAOYSA-N transbutenic acid ethyl ester Natural products CCOC(=O)C=CC ZFDIRQKJPRINOQ-UHFFFAOYSA-N 0.000 description 1
- 230000008733 trauma Effects 0.000 description 1
- 125000004306 triazinyl group Chemical group 0.000 description 1
- WLPUWLXVBWGYMZ-UHFFFAOYSA-N tricyclohexylphosphine Chemical compound C1CCCCC1P(C1CCCCC1)C1CCCCC1 WLPUWLXVBWGYMZ-UHFFFAOYSA-N 0.000 description 1
- 229960004799 tryptophan Drugs 0.000 description 1
- 229960004441 tyrosine Drugs 0.000 description 1
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Chemical class OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 description 1
- 229960004295 valine Drugs 0.000 description 1
- 239000004474 valine Chemical class 0.000 description 1
- 230000003313 weakening effect Effects 0.000 description 1
- 229910052725 zinc Inorganic materials 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pain & Pain Management (AREA)
- Immunology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US25250800P | 2000-11-22 | 2000-11-22 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ZA200303848B true ZA200303848B (en) | 2004-06-28 |
Family
ID=22956303
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ZA200303848A ZA200303848B (en) | 2000-11-22 | 2003-05-16 | Protease inhibitors. |
Country Status (17)
| Country | Link |
|---|---|
| EP (1) | EP1392657A4 (zh) |
| JP (1) | JP2005513083A (zh) |
| KR (1) | KR20040004445A (zh) |
| CN (1) | CN1635903A (zh) |
| AR (1) | AR034278A1 (zh) |
| AU (1) | AU2001298052A1 (zh) |
| BR (1) | BR0115473A (zh) |
| CA (1) | CA2436850A1 (zh) |
| CZ (1) | CZ20031403A3 (zh) |
| HU (1) | HUP0301964A3 (zh) |
| IL (1) | IL155997A0 (zh) |
| MX (1) | MXPA03004542A (zh) |
| NO (1) | NO20032328L (zh) |
| PL (1) | PL366232A1 (zh) |
| UY (1) | UY27032A1 (zh) |
| WO (1) | WO2003053331A2 (zh) |
| ZA (1) | ZA200303848B (zh) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20030144175A1 (en) | 1998-12-23 | 2003-07-31 | Smithkline Beecham Corporation | Protease inhibitors |
| CN1416346A (zh) | 2000-03-21 | 2003-05-07 | 史密丝克莱恩比彻姆公司 | 蛋白酶抑制剂 |
| AU2001268407A1 (en) * | 2000-06-14 | 2001-12-24 | Smithkline Beecham Corporation | Protease inhibitors |
| CN101970007A (zh) | 2007-06-08 | 2011-02-09 | 日本化学医药株式会社 | 脑动脉瘤的治疗或预防药 |
| JPWO2009054454A1 (ja) | 2007-10-24 | 2011-03-03 | 国立大学法人 東京医科歯科大学 | カテプシン阻害剤を有効成分として含有するＴｏｌｌ様受容体のシグナル伝達の調整剤 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ511710A (en) * | 1998-12-23 | 2003-12-19 | Smithkline Beecham Corp | 4-Amino-azepan-3-one derivatives useful as protease inhibitors |
| CN1416346A (zh) * | 2000-03-21 | 2003-05-07 | 史密丝克莱恩比彻姆公司 | 蛋白酶抑制剂 |
| AU2001268407A1 (en) * | 2000-06-14 | 2001-12-24 | Smithkline Beecham Corporation | Protease inhibitors |
-
2001
- 2001-11-19 CN CNA018220533A patent/CN1635903A/zh active Pending
- 2001-11-19 AU AU2001298052A patent/AU2001298052A1/en not_active Abandoned
- 2001-11-19 JP JP2003554091A patent/JP2005513083A/ja not_active Withdrawn
- 2001-11-19 HU HU0301964A patent/HUP0301964A3/hu unknown
- 2001-11-19 CA CA002436850A patent/CA2436850A1/en not_active Abandoned
- 2001-11-19 MX MXPA03004542A patent/MXPA03004542A/es unknown
- 2001-11-19 WO PCT/US2001/051647 patent/WO2003053331A2/en not_active Application Discontinuation
- 2001-11-19 CZ CZ20031403A patent/CZ20031403A3/cs unknown
- 2001-11-19 IL IL15599701A patent/IL155997A0/xx unknown
- 2001-11-19 EP EP01275089A patent/EP1392657A4/en not_active Withdrawn
- 2001-11-19 PL PL01366232A patent/PL366232A1/xx not_active Application Discontinuation
- 2001-11-19 BR BR0115473-7A patent/BR0115473A/pt not_active Application Discontinuation
- 2001-11-19 KR KR10-2003-7006807A patent/KR20040004445A/ko not_active Application Discontinuation
- 2001-11-20 AR ARP010105409A patent/AR034278A1/es unknown
- 2001-11-21 UY UY27032A patent/UY27032A1/es not_active Application Discontinuation
-
2003
- 2003-05-16 ZA ZA200303848A patent/ZA200303848B/en unknown
- 2003-05-22 NO NO20032328A patent/NO20032328L/no unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CZ20031403A3 (cs) | 2003-10-15 |
| UY27032A1 (es) | 2002-07-31 |
| WO2003053331A3 (en) | 2003-11-13 |
| MXPA03004542A (es) | 2003-09-10 |
| JP2005513083A (ja) | 2005-05-12 |
| PL366232A1 (en) | 2005-01-24 |
| EP1392657A2 (en) | 2004-03-03 |
| WO2003053331A2 (en) | 2003-07-03 |
| HUP0301964A2 (en) | 2007-02-28 |
| CN1635903A (zh) | 2005-07-06 |
| EP1392657A4 (en) | 2004-03-10 |
| NO20032328L (no) | 2003-07-02 |
| KR20040004445A (ko) | 2004-01-13 |
| AU2001298052A1 (en) | 2003-07-09 |
| IL155997A0 (en) | 2003-12-23 |
| CA2436850A1 (en) | 2003-07-03 |
| NO20032328D0 (no) | 2003-05-22 |
| BR0115473A (pt) | 2004-09-28 |
| AR034278A1 (es) | 2004-02-18 |
| HUP0301964A3 (en) | 2007-09-28 |
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