ATE287402T1 - Nanomolare, non-peptidische inhibitoren von cathepsin d - Google Patents
Nanomolare, non-peptidische inhibitoren von cathepsin dInfo
- Publication number
- ATE287402T1 ATE287402T1 AT98904934T AT98904934T ATE287402T1 AT E287402 T1 ATE287402 T1 AT E287402T1 AT 98904934 T AT98904934 T AT 98904934T AT 98904934 T AT98904934 T AT 98904934T AT E287402 T1 ATE287402 T1 AT E287402T1
- Authority
- AT
- Austria
- Prior art keywords
- cathepsin
- nanomolar
- peptidic inhibitors
- peptidic
- inhibitors
- Prior art date
Links
- 102000005600 Cathepsins Human genes 0.000 title 1
- 108010084457 Cathepsins Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 102000003908 Cathepsin D Human genes 0.000 abstract 2
- 108090000258 Cathepsin D Proteins 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 238000001514 detection method Methods 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 238000002372 labelling Methods 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 108090000765 processed proteins & peptides Proteins 0.000 abstract 1
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)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (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)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Plural Heterocyclic Compounds (AREA)
- Peptides Or Proteins (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)
- Indole Compounds (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US3690397P | 1997-02-04 | 1997-02-04 | |
| PCT/US1998/002199 WO1998033795A1 (en) | 1997-02-04 | 1998-02-03 | Nanomolar, non-peptide inhibitors of cathepsin d |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ATE287402T1 true ATE287402T1 (de) | 2005-02-15 |
Family
ID=21891303
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AT98904934T ATE287402T1 (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 (31)
| 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 |
| US20010041964A1 (en) * | 1998-09-14 | 2001-11-15 | George M. Grass | Pharmacokinetic-based drug design tool and method |
| JP2002539260A (ja) * | 1999-03-24 | 2002-11-19 | ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア | アスパルチルプロテアーゼインヒビターを使用して神経変性障害を処置する方法 |
| AU2756801A (en) * | 2000-01-03 | 2001-07-16 | Trustees Of Princeton University, The | High efficiency mapping of molecular variations to functional properties |
| DE60124080T2 (de) | 2000-03-23 | 2007-03-01 | Elan Pharmaceuticals, Inc., San Francisco | Verbindungen und verfahren zur behandlung der alzheimerschen 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 |
| EP1666452A2 (de) | 2000-06-30 | 2006-06-07 | 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 |
| JP2004502664A (ja) * | 2000-06-30 | 2004-01-29 | イーラン ファーマスーティカルズ、インコーポレイテッド | アルツハイマー病処置用化合物 |
| EP1586556A3 (de) * | 2000-06-30 | 2005-12-21 | Elan Pharmaceuticals, Inc. | Verbindungen zur Behandlung der Alzheimerischen Krankheit |
| 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 |
| MXPA03011046A (es) * | 2001-06-01 | 2004-06-25 | Elan Pharm Inc | Hidroxialquilaminas. |
| BR0210721A (pt) | 2001-06-27 | 2004-07-20 | Elan Pharm Inc | Composto, sal ou éster farmaceuticamente aceitável, método para fabricar um composto, e, método para tratar um paciente que tem, ou para evitar que o paciente adquira uma doença ou condição |
| EP1432674A2 (de) | 2001-10-04 | 2004-06-30 | Elan Pharmaceuticals, Inc. | Hydroxypropylamine |
| AU2002359376B2 (en) | 2001-11-08 | 2008-01-10 | Elan Pharmaceuticals, Inc. | N, N'-substituted-1,3-diamino-2-hydroxypropane derivatives |
| BR0214295A (pt) | 2001-11-19 | 2004-11-09 | Elan Pharm Inc | Composto, método para tratar um paciente que tem ou prevenir um paciente de adquirir uma doença ou condição, e, método para produzir um composto |
| WO2004058686A1 (en) | 2002-04-30 | 2004-07-15 | Elan Pharmaceuticals, Inc. | Hydroxypropyl amides for the treatment of alzheimer’s disease |
| US7101880B2 (en) * | 2002-06-24 | 2006-09-05 | Schering Aktiengesellschaft | 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 |
| US20060264415A1 (en) * | 2005-04-01 | 2006-11-23 | Methylgene Inc. | Inhibitors of histone deacetylase |
| AU2012216230B2 (en) | 2011-02-08 | 2017-05-25 | Merck Patent Gmbh | Amino statin derivatives for the treatement of arthrosis |
| US9624264B2 (en) | 2012-07-24 | 2017-04-18 | Merck Patent Gmbh | Hydroxystatin derivatives for the treatment of arthrosis |
| WO2014084430A1 (ko) * | 2012-11-30 | 2014-06-05 | 경상대학교 산학협력단 | 병용 항암요법 |
| JP6321685B2 (ja) | 2013-02-25 | 2018-05-09 | 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 | ２−アミノ−３，４−ジヒドロ−キナゾリン誘導体、およびそのカテプシンｄ阻害剤としての使用 |
| CA2920420C (en) | 2013-08-06 | 2021-11-23 | Merck Patent Gmbh | Intraarticular administration of pepstatin in the case of arthrosis |
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 |
| ATE196759T1 (de) * | 1990-11-19 | 2000-10-15 | Monsanto Co | Inhibitoren retroviraler proteasen |
-
1998
- 1998-02-03 EP EP98904934A patent/EP0958293B1/de not_active Expired - Lifetime
- 1998-02-03 WO PCT/US1998/002199 patent/WO1998033795A1/en not_active Ceased
- 1998-02-03 JP JP53323698A patent/JP2001510474A/ja not_active Ceased
- 1998-02-03 CA CA002280096A patent/CA2280096A1/en not_active Abandoned
- 1998-02-03 AT AT98904934T patent/ATE287402T1/de not_active IP Right Cessation
- 1998-02-03 DE DE69828682T patent/DE69828682T2/de not_active Expired - Lifetime
- 1998-02-03 AU AU62686/98A patent/AU749281B2/en not_active Ceased
- 1998-02-03 US US09/018,226 patent/US6150416A/en not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| DE69828682D1 (de) | 2005-02-24 |
| EP0958293A1 (de) | 1999-11-24 |
| WO1998033795A1 (en) | 1998-08-06 |
| CA2280096A1 (en) | 1998-08-06 |
| US6150416A (en) | 2000-11-21 |
| JP2001510474A (ja) | 2001-07-31 |
| EP0958293B1 (de) | 2005-01-19 |
| AU749281B2 (en) | 2002-06-20 |
| AU6268698A (en) | 1998-08-25 |
| DE69828682T2 (de) | 2006-04-06 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| RER | Ceased as to paragraph 5 lit. 3 law introducing patent treaties |