RU2009105764A - Макроциклические соединения, применимые в качестве ингибиторов васе - Google Patents
Макроциклические соединения, применимые в качестве ингибиторов васе Download PDFInfo
- Publication number
- RU2009105764A RU2009105764A RU2009105764/04A RU2009105764A RU2009105764A RU 2009105764 A RU2009105764 A RU 2009105764A RU 2009105764/04 A RU2009105764/04 A RU 2009105764/04A RU 2009105764 A RU2009105764 A RU 2009105764A RU 2009105764 A RU2009105764 A RU 2009105764A
- Authority
- RU
- Russia
- Prior art keywords
- alkyl
- group
- cycloalkyl
- dioxo
- heteroaryl
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- 150000002678 macrocyclic compounds Chemical class 0.000 title 1
- -1 aryl (C1-C4) alkyl Chemical group 0.000 claims abstract 59
- 150000001875 compounds Chemical class 0.000 claims abstract 16
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 claims abstract 14
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims abstract 13
- 125000001072 heteroaryl group Chemical group 0.000 claims abstract 13
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract 13
- 239000001257 hydrogen Substances 0.000 claims abstract 13
- 125000003118 aryl group Chemical group 0.000 claims abstract 12
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims abstract 8
- 125000004432 carbon atom Chemical group C* 0.000 claims abstract 7
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims abstract 6
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims abstract 5
- 125000001424 substituent group Chemical group 0.000 claims abstract 5
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims abstract 4
- 229910052736 halogen Inorganic materials 0.000 claims abstract 4
- 125000004043 oxo group Chemical group O=* 0.000 claims abstract 4
- 125000004768 (C1-C4) alkylsulfinyl group Chemical group 0.000 claims abstract 3
- 125000004769 (C1-C4) alkylsulfonyl group Chemical group 0.000 claims abstract 3
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims abstract 3
- 125000000217 alkyl group Chemical group 0.000 claims abstract 3
- 125000004414 alkyl thio group Chemical group 0.000 claims abstract 3
- 125000004093 cyano group Chemical group *C#N 0.000 claims abstract 3
- 125000005842 heteroatom Chemical group 0.000 claims abstract 3
- 229910052799 carbon Inorganic materials 0.000 claims abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 claims abstract 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims abstract 2
- 239000002253 acid Substances 0.000 claims 10
- 150000003839 salts Chemical class 0.000 claims 10
- 238000004519 manufacturing process Methods 0.000 claims 5
- 102000013455 Amyloid beta-Peptides Human genes 0.000 claims 4
- 108010090849 Amyloid beta-Peptides Proteins 0.000 claims 4
- 208000012902 Nervous system disease Diseases 0.000 claims 4
- 208000025966 Neurological disease Diseases 0.000 claims 4
- 238000004220 aggregation Methods 0.000 claims 4
- 230000002776 aggregation Effects 0.000 claims 4
- 230000000926 neurological effect Effects 0.000 claims 4
- 208000019553 vascular disease Diseases 0.000 claims 4
- 125000002947 alkylene group Chemical group 0.000 claims 3
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 150000002367 halogens Chemical group 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- 239000001301 oxygen Substances 0.000 claims 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 2
- 125000005194 alkoxycarbonyloxy group Chemical group 0.000 claims 2
- 125000005196 alkyl carbonyloxy group Chemical group 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 1
- ZOKXTWBITQBERF-UHFFFAOYSA-N Molybdenum Chemical compound [Mo] ZOKXTWBITQBERF-UHFFFAOYSA-N 0.000 claims 1
- KJTLSVCANCCWHF-UHFFFAOYSA-N Ruthenium Chemical compound [Ru] KJTLSVCANCCWHF-UHFFFAOYSA-N 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 239000008186 active pharmaceutical agent Substances 0.000 claims 1
- 125000005529 alkyleneoxy group Chemical group 0.000 claims 1
- 150000001721 carbon Chemical group 0.000 claims 1
- 239000011203 carbon fibre reinforced carbon Substances 0.000 claims 1
- 239000003054 catalyst Substances 0.000 claims 1
- 238000006243 chemical reaction Methods 0.000 claims 1
- 238000003776 cleavage reaction Methods 0.000 claims 1
- 125000002993 cycloalkylene group Chemical group 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229940088679 drug related substance Drugs 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 239000011737 fluorine Substances 0.000 claims 1
- 238000007306 functionalization reaction Methods 0.000 claims 1
- 238000005649 metathesis reaction Methods 0.000 claims 1
- 229910052750 molybdenum Inorganic materials 0.000 claims 1
- 239000011733 molybdenum Substances 0.000 claims 1
- 230000003647 oxidation Effects 0.000 claims 1
- 238000007254 oxidation reaction Methods 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000008024 pharmaceutical diluent Substances 0.000 claims 1
- 239000002243 precursor Substances 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
- 238000011084 recovery Methods 0.000 claims 1
- 238000007363 ring formation reaction Methods 0.000 claims 1
- 125000006413 ring segment Chemical group 0.000 claims 1
- 229910052707 ruthenium Inorganic materials 0.000 claims 1
- 230000007017 scission Effects 0.000 claims 1
- WFKWXMTUELFFGS-UHFFFAOYSA-N tungsten Chemical compound [W] WFKWXMTUELFFGS-UHFFFAOYSA-N 0.000 claims 1
- 229910052721 tungsten Inorganic materials 0.000 claims 1
- 239000010937 tungsten Substances 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
-
- 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
-
- 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
- A61P35/00—Antineoplastic agents
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D245/00—Heterocyclic compounds containing rings of more than seven members having two nitrogen atoms as the only ring hetero atoms
- C07D245/02—Heterocyclic compounds containing rings of more than seven members having two nitrogen atoms as the only ring hetero atoms not condensed with other rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D273/00—Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00
- C07D273/02—Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00 having two nitrogen atoms and only one oxygen atom
-
- 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
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP06117583 | 2006-07-20 | ||
| EP06117583.2 | 2006-07-20 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2009105764A true RU2009105764A (ru) | 2010-08-27 |
Family
ID=37451237
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2009105764/04A RU2009105764A (ru) | 2006-07-20 | 2007-07-19 | Макроциклические соединения, применимые в качестве ингибиторов васе |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20090170878A1 (enExample) |
| EP (1) | EP2046760A1 (enExample) |
| JP (1) | JP2009544597A (enExample) |
| KR (1) | KR20090041387A (enExample) |
| CN (1) | CN101484431A (enExample) |
| AU (1) | AU2007275132A1 (enExample) |
| BR (1) | BRPI0715437A2 (enExample) |
| CA (1) | CA2656869A1 (enExample) |
| MX (1) | MX2009000768A (enExample) |
| RU (1) | RU2009105764A (enExample) |
| WO (1) | WO2008009734A1 (enExample) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0325830D0 (en) * | 2003-11-05 | 2003-12-10 | Novartis Ag | Organic compounds |
| US7763609B2 (en) | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| BRPI0606636A2 (pt) * | 2005-01-13 | 2009-07-07 | Novartis Ag | compostos macrocìclicos úteis como inibidores de bace |
| GB0500683D0 (en) * | 2005-01-13 | 2005-02-23 | Novartis Ag | Organic compounds |
| GB0526614D0 (en) | 2005-12-30 | 2006-02-08 | Novartis Ag | Organic compounds |
| CA2657280A1 (en) * | 2006-07-20 | 2008-01-24 | Novartis Ag | Macrocyclic compounds useful as bace inhibitors |
| EP3653609B1 (en) | 2013-02-12 | 2024-04-03 | Buck Institute for Research on Aging | Hydantoins that modulate bace-mediated app processing |
| US11834515B2 (en) | 2017-10-11 | 2023-12-05 | Cornell University | Macrocyclic compounds as proteasome inhibitors |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1395257A1 (en) * | 2001-06-12 | 2004-03-10 | Elan Pharmaceuticals, Inc. | Macrocycles useful in the treatment of alzheimer's disease |
| JP2004534064A (ja) * | 2001-06-12 | 2004-11-11 | 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 | アルツハイマー病の治療に有用な大環状分子 |
| GB0325830D0 (en) * | 2003-11-05 | 2003-12-10 | Novartis Ag | Organic compounds |
| CA2575340A1 (en) * | 2004-07-28 | 2006-02-09 | Schering Corporation | Macrocyclic beta-secretase inhibitors |
| BRPI0606636A2 (pt) * | 2005-01-13 | 2009-07-07 | Novartis Ag | compostos macrocìclicos úteis como inibidores de bace |
| GB0500683D0 (en) * | 2005-01-13 | 2005-02-23 | Novartis Ag | Organic compounds |
| GB0526614D0 (en) * | 2005-12-30 | 2006-02-08 | Novartis Ag | Organic compounds |
| CA2657280A1 (en) * | 2006-07-20 | 2008-01-24 | Novartis Ag | Macrocyclic compounds useful as bace inhibitors |
-
2007
- 2007-07-19 KR KR1020097001068A patent/KR20090041387A/ko not_active Withdrawn
- 2007-07-19 WO PCT/EP2007/057492 patent/WO2008009734A1/en not_active Ceased
- 2007-07-19 BR BRPI0715437-2A patent/BRPI0715437A2/pt not_active Application Discontinuation
- 2007-07-19 JP JP2009519989A patent/JP2009544597A/ja not_active Withdrawn
- 2007-07-19 MX MX2009000768A patent/MX2009000768A/es unknown
- 2007-07-19 US US12/374,469 patent/US20090170878A1/en not_active Abandoned
- 2007-07-19 RU RU2009105764/04A patent/RU2009105764A/ru not_active Application Discontinuation
- 2007-07-19 AU AU2007275132A patent/AU2007275132A1/en not_active Abandoned
- 2007-07-19 CN CNA2007800255206A patent/CN101484431A/zh active Pending
- 2007-07-19 EP EP07819907A patent/EP2046760A1/en not_active Withdrawn
- 2007-07-19 CA CA002656869A patent/CA2656869A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| CN101484431A (zh) | 2009-07-15 |
| WO2008009734A1 (en) | 2008-01-24 |
| MX2009000768A (es) | 2009-01-28 |
| US20090170878A1 (en) | 2009-07-02 |
| BRPI0715437A2 (pt) | 2013-04-16 |
| CA2656869A1 (en) | 2008-01-24 |
| AU2007275132A1 (en) | 2008-01-24 |
| JP2009544597A (ja) | 2009-12-17 |
| KR20090041387A (ko) | 2009-04-28 |
| EP2046760A1 (en) | 2009-04-15 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA93 | Acknowledgement of application withdrawn (no request for examination) |
Effective date: 20110315 |