CN1431904A - 蛋白酶抑制剂 - Google Patents
蛋白酶抑制剂 Download PDFInfo
- Publication number
- CN1431904A CN1431904A CN01808290A CN01808290A CN1431904A CN 1431904 A CN1431904 A CN 1431904A CN 01808290 A CN01808290 A CN 01808290A CN 01808290 A CN01808290 A CN 01808290A CN 1431904 A CN1431904 A CN 1431904A
- Authority
- CN
- China
- Prior art keywords
- base
- pyridine
- alkyl
- azepan
- carboxylic acid
- 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
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- 229910052736 halogen Inorganic materials 0.000 claims description 3
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- 125000003545 alkoxy group Chemical group 0.000 claims description 2
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- WCNFFKHKJLERFM-UHFFFAOYSA-N thiomorpholinyl sulfone group Chemical group N1(CCSCC1)S(=O)(=O)N1CCSCC1 WCNFFKHKJLERFM-UHFFFAOYSA-N 0.000 description 1
- ZCAGUOCUDGWENZ-UHFFFAOYSA-N thiomorpholinyl sulfoxide group Chemical group N1(CCSCC1)S(=O)N1CCSCC1 ZCAGUOCUDGWENZ-UHFFFAOYSA-N 0.000 description 1
- 230000008354 tissue degradation Effects 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 1
- 230000017105 transposition Effects 0.000 description 1
- 125000001425 triazolyl group Chemical group 0.000 description 1
- 229910052722 tritium Inorganic materials 0.000 description 1
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 description 1
- 239000004474 valine Substances 0.000 description 1
Classifications
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
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- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
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- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- C—CHEMISTRY; METALLURGY
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
- C07D223/02—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings
- C07D223/06—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D223/08—Oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
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- 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
- C07D405/02—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 two hetero rings
- C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
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- 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
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- 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
- C07D409/12—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 linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D421/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having selenium, tellurium, or halogen atoms as ring hetero atoms
- C07D421/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having selenium, tellurium, or halogen atoms as ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
Landscapes
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Diabetes (AREA)
- Immunology (AREA)
- Hematology (AREA)
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- Pain & Pain Management (AREA)
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Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
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US19849300P | 2000-04-18 | 2000-04-18 | |
US60/198,493 | 2000-04-18 | ||
US27381101P | 2001-03-07 | 2001-03-07 | |
US60/273,811 | 2001-03-07 |
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CN1431904A true CN1431904A (zh) | 2003-07-23 |
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CN01808290A Pending CN1431904A (zh) | 2000-04-18 | 2001-04-17 | 蛋白酶抑制剂 |
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EP (1) | EP1278502A4 (es) |
JP (1) | JP2004526662A (es) |
KR (1) | KR20020089482A (es) |
CN (1) | CN1431904A (es) |
AR (1) | AR032319A1 (es) |
AU (1) | AU9050701A (es) |
BR (1) | BR0108954A (es) |
CA (1) | CA2406829A1 (es) |
CO (1) | CO5280088A1 (es) |
CZ (1) | CZ20023460A3 (es) |
HK (1) | HK1053785A1 (es) |
HU (1) | HUP0301781A2 (es) |
IL (1) | IL151087A0 (es) |
MX (1) | MXPA02010276A (es) |
NO (1) | NO20025005L (es) |
PL (1) | PL366040A1 (es) |
WO (1) | WO2001089451A2 (es) |
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EP1401453A4 (en) * | 2001-05-17 | 2005-04-06 | Smithkline Beecham Corp | PROTEASE INHIBITORS |
US20050030912A1 (en) * | 2002-08-22 | 2005-02-10 | Enikia L.L.C. | Use of hybrid (HW/DSP/MCU/SW) architectures for powerline OFDM communication field |
PL375053A1 (en) | 2002-09-24 | 2005-11-14 | Novartis Ag | Sphingosine-1-phosphate receptor agonists in the treatment of demyelinating disorders |
JP2006504719A (ja) * | 2002-10-08 | 2006-02-09 | メルク フロスト カナダ アンド カンパニー | 骨粗しょう症の治療において有用なカテプシンk阻害剤としての4−アミノ−アゼパン−3−オン化合物 |
US7297714B2 (en) * | 2003-10-21 | 2007-11-20 | Irm Llc | Inhibitors of cathepsin S |
US20100292298A1 (en) * | 2006-02-21 | 2010-11-18 | Agency For Science, Technology And Research | Method and reagents for treating hepatic fibrosis and inflammation |
US20100331545A1 (en) * | 2007-10-24 | 2010-12-30 | Nippon Chemiphar Co., Ltd. | Regulator for signaling toll-like receptor, which comprises cathepsin inhibitor as active ingredient |
RU2562571C2 (ru) | 2008-06-20 | 2015-09-10 | Новартис Аг | Педиатрические композиции для лечения рассеянного склероза |
LV15485B (lv) * | 2018-09-13 | 2020-06-20 | Latvijas Organiskās Sintēzes Institūts | Selenofēnhromenonu hidroksāmskābes, to izgatavošana un izmantošana angioģenēzes inhibīcijā |
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Publication number | Priority date | Publication date | Assignee | Title |
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US4518528A (en) * | 1983-05-19 | 1985-05-21 | Rasnick David W | α Amino fluoro ketones |
TW494094B (en) * | 1993-04-29 | 2002-07-11 | Vertex Pharma | Peptide analogs as irreversible interleukin-1β protease inhibitors and pharmaceutical compositions comprising the same |
DZ2285A1 (fr) * | 1996-08-08 | 2002-12-25 | Smithkline Beecham Corp | Inhibiteurs de protéase de la cystéine. |
TR200101869T2 (tr) * | 1998-12-23 | 2002-01-21 | Smithkline Beecham Corporation | Proteaz İnhibitörleri. |
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 |
JP2004509083A (ja) * | 2000-09-01 | 2004-03-25 | スミスクライン・ビーチャム・コーポレイション | 治療方法 |
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Also Published As
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AR032319A1 (es) | 2003-11-05 |
PL366040A1 (en) | 2005-01-24 |
NO20025005D0 (no) | 2002-10-17 |
BR0108954A (pt) | 2006-05-09 |
CZ20023460A3 (en) | 2004-03-17 |
WO2001089451A2 (en) | 2001-11-29 |
EP1278502A4 (en) | 2003-05-21 |
HK1053785A1 (zh) | 2003-11-07 |
AU9050701A (en) | 2001-12-03 |
IL151087A0 (en) | 2003-04-10 |
NO20025005L (no) | 2002-12-06 |
CO5280088A1 (es) | 2003-05-30 |
JP2004526662A (ja) | 2004-09-02 |
HUP0301781A2 (hu) | 2003-09-29 |
MXPA02010276A (es) | 2003-04-25 |
EP1278502A2 (en) | 2003-01-29 |
WO2001089451A3 (en) | 2002-04-04 |
CA2406829A1 (en) | 2001-11-29 |
KR20020089482A (ko) | 2002-11-29 |
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