DE69828682D1 - Nanomolare, non-peptidische inhibitoren von cathepsin d - Google Patents
Nanomolare, non-peptidische inhibitoren von cathepsin dInfo
- Publication number
- DE69828682D1 DE69828682D1 DE69828682T DE69828682T DE69828682D1 DE 69828682 D1 DE69828682 D1 DE 69828682D1 DE 69828682 T DE69828682 T DE 69828682T DE 69828682 T DE69828682 T DE 69828682T DE 69828682 D1 DE69828682 D1 DE 69828682D1
- Authority
- DE
- Germany
- Prior art keywords
- cathepsin
- nanomolar
- peptidic inhibitors
- peptidic
- inhibitors
- 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.)
- Expired - Lifetime
Links
Classifications
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/357—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
- A61K31/36—Compounds containing methylenedioxyphenyl groups, e.g. sesamin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/4035—Isoindoles, e.g. phthalimide
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
- A61K31/423—Oxazoles condensed with carbocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
- C07D263/54—Benzoxazoles; Hydrogenated benzoxazoles
- C07D263/58—Benzoxazoles; Hydrogenated benzoxazoles 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 in position 2
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D317/00—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
- C07D317/08—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
- C07D317/44—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems
- C07D317/46—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems condensed with one six-membered ring
- C07D317/48—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring
- C07D317/50—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to atoms of the carbocyclic ring
- C07D317/58—Radicals substituted by nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D317/00—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
- C07D317/08—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
- C07D317/44—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems
- C07D317/46—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems condensed with one six-membered ring
- C07D317/48—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring
- C07D317/50—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to atoms of the carbocyclic ring
- C07D317/60—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D317/00—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
- C07D317/08—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
- C07D317/44—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems
- C07D317/46—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems condensed with one six-membered ring
- C07D317/48—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring
- C07D317/62—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring 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 atoms of the carbocyclic ring
-
- 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
- C07D405/02—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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen 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
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US3690397P | 1997-02-04 | 1997-02-04 | |
US36903P | 1997-02-04 | ||
PCT/US1998/002199 WO1998033795A1 (en) | 1997-02-04 | 1998-02-03 | Nanomolar, non-peptide inhibitors of cathepsin d |
Publications (2)
Publication Number | Publication Date |
---|---|
DE69828682D1 true DE69828682D1 (de) | 2005-02-24 |
DE69828682T2 DE69828682T2 (de) | 2006-04-06 |
Family
ID=21891303
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
DE69828682T Expired - Lifetime DE69828682T2 (de) | 1997-02-04 | 1998-02-03 | Nanomolare, non-peptidische inhibitoren von cathepsin d |
Country Status (8)
Country | Link |
---|---|
US (1) | US6150416A (de) |
EP (1) | EP0958293B1 (de) |
JP (1) | JP2001510474A (de) |
AT (1) | ATE287402T1 (de) |
AU (1) | AU749281B2 (de) |
CA (1) | CA2280096A1 (de) |
DE (1) | DE69828682T2 (de) |
WO (1) | WO1998033795A1 (de) |
Families Citing this family (29)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US7119105B2 (en) | 1997-02-04 | 2006-10-10 | The Regents Of The University Of California | Methods for treating neurodegenerative disorders using aspartyl protease inhibitors |
US20020010550A1 (en) | 1998-09-14 | 2002-01-24 | George M. Grass | Pharmacokinetic-based drug design tool and method |
CA2367112A1 (en) * | 1999-03-24 | 2000-09-28 | The Regents Of The University Of California | Methods for treating neurodegenerative disorders using aspartyl protease inhibitors |
JP2003519201A (ja) * | 2000-01-03 | 2003-06-17 | ザ トラスティーズ オブ プリンストン ユニバーシティ | 機能特性に対する分子変種の高能率マッピング |
EP1666452A2 (de) | 2000-06-30 | 2006-06-07 | Elan Pharmaceuticals, Inc. | Verbindungen zur Behandlung der Alzheimerischen Krankheit |
EP1586556A3 (de) * | 2000-06-30 | 2005-12-21 | Elan Pharmaceuticals, Inc. | Verbindungen zur Behandlung der Alzheimerischen Krankheit |
US6846813B2 (en) * | 2000-06-30 | 2005-01-25 | Pharmacia & Upjohn Company | Compounds to treat alzheimer's disease |
DE60112942T2 (de) * | 2000-06-30 | 2006-06-22 | Elan Pharmaceuticals, Inc., South San Francisco | Verbindungen zur behandlung der alzheimerischen krankheit |
PE20020276A1 (es) | 2000-06-30 | 2002-04-06 | Elan Pharm Inc | COMPUESTOS DE AMINA SUSTITUIDA COMO INHIBIDORES DE ß-SECRETASA PARA EL TRATAMIENTO DE ALZHEIMER |
US20030211487A1 (en) * | 2001-01-03 | 2003-11-13 | Herschel Rabitz | High efficiency mapping of molecular variations to functional properties |
AR035960A1 (es) * | 2001-04-23 | 2004-07-28 | Elan Pharm Inc | Epoxidos sustituidos y procesos para prepararlos |
ATE396174T1 (de) * | 2001-06-01 | 2008-06-15 | Elan Pharm Inc | Hydroxyalkylaminderivate als beta-secretase- inhibitoren und deren verwendung zur behandlung der alzheimerschen krankheit oder ähnlicher krankheiten |
CA2462851A1 (en) | 2001-10-04 | 2003-04-10 | Elan Pharmaceuticals, Inc. | Hydroxypropylamines |
MXPA04004428A (es) | 2001-11-08 | 2004-09-10 | Elan Pharm Inc | Derivados de 2,3-diamino-2-hidroxipropano n,n`-sustituidos. |
US7338965B2 (en) | 2001-11-19 | 2008-03-04 | Pharmacia & Upjohn Company | 3,4-disubstituted, 3,5-disubstituted and 3,4,5-substituted piperidines |
AU2003303141A1 (en) | 2002-04-30 | 2004-07-22 | Elan Pharmaceuticals, Inc. | Hydroxypropyl amides for the treatment of alzheimer's disease |
AU2003256305A1 (en) * | 2002-06-24 | 2004-01-06 | Axys Pharmaceuticals, Inc. | Peptidic compounds as cysteine protease inhibitors |
CN100384824C (zh) * | 2002-09-10 | 2008-04-30 | 艾伦药物公司 | 乙酰基2-羟基-1,3-二氨基烷烃 |
UY27967A1 (es) * | 2002-09-10 | 2004-05-31 | Pfizer | Acetil 2-hindroxi-1,3-diaminoalcanos |
GB0228410D0 (en) | 2002-12-05 | 2003-01-08 | Glaxo Group Ltd | Novel Compounds |
GB0309221D0 (en) * | 2003-04-23 | 2003-06-04 | Glaxo Group Ltd | Novel compounds |
US7408008B2 (en) | 2003-12-09 | 2008-08-05 | Janssen Pharmaceutica, N.V. | Method of producing highly functionalized 1,3-diamino-propan-2-ols from solid support |
GB0328900D0 (en) * | 2003-12-12 | 2004-01-14 | Glaxo Group Ltd | Novel compounds |
AU2006228957A1 (en) * | 2005-04-01 | 2006-10-05 | Methylgene Inc. | Inhibitors of histone deacetylase |
ES2649964T3 (es) | 2011-02-08 | 2018-01-16 | Merck Patent Gmbh | Derivados de aminoestatina para el tratamiento de la artrosis |
JP6430936B2 (ja) | 2012-07-24 | 2018-11-28 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングMerck Patent Gesellschaft mit beschraenkter Haftung | 関節症の処置のためのヒドロキシスタチン誘導体 |
WO2014084430A1 (ko) * | 2012-11-30 | 2014-06-05 | 경상대학교 산학협력단 | 병용 항암요법 |
CN105189469B (zh) | 2013-02-25 | 2018-09-25 | 默克专利股份公司 | 2-氨基-3,4-二氢喹唑啉衍生物及其作为组织蛋白酶d抑制剂的用途 |
EP3030250B1 (de) | 2013-08-06 | 2019-08-28 | Merck Patent GmbH | Intraartikuläre applikation von pepstatin bei arthrose |
Family Cites Families (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4604402A (en) * | 1984-03-30 | 1986-08-05 | E. R. Squibb & Sons, Inc. | Hydroxy substituted ureido amino and imino acids |
DK0735019T3 (da) * | 1990-11-19 | 2000-10-23 | Monsanto Co | Retrovirale proteaseinhibitorer |
-
1998
- 1998-02-03 AU AU62686/98A patent/AU749281B2/en not_active Ceased
- 1998-02-03 EP EP98904934A patent/EP0958293B1/de not_active Expired - Lifetime
- 1998-02-03 AT AT98904934T patent/ATE287402T1/de not_active IP Right Cessation
- 1998-02-03 US US09/018,226 patent/US6150416A/en not_active Expired - Lifetime
- 1998-02-03 CA CA002280096A patent/CA2280096A1/en not_active Abandoned
- 1998-02-03 WO PCT/US1998/002199 patent/WO1998033795A1/en active IP Right Grant
- 1998-02-03 JP JP53323698A patent/JP2001510474A/ja not_active Ceased
- 1998-02-03 DE DE69828682T patent/DE69828682T2/de not_active Expired - Lifetime
Also Published As
Publication number | Publication date |
---|---|
WO1998033795A1 (en) | 1998-08-06 |
ATE287402T1 (de) | 2005-02-15 |
CA2280096A1 (en) | 1998-08-06 |
AU749281B2 (en) | 2002-06-20 |
AU6268698A (en) | 1998-08-25 |
JP2001510474A (ja) | 2001-07-31 |
DE69828682T2 (de) | 2006-04-06 |
EP0958293B1 (de) | 2005-01-19 |
US6150416A (en) | 2000-11-21 |
EP0958293A1 (de) | 1999-11-24 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
8364 | No opposition during term of opposition |