EA201170480A1 - PROTEAS INHIBITORS - Google Patents
PROTEAS INHIBITORSInfo
- Publication number
- EA201170480A1 EA201170480A1 EA201170480A EA201170480A EA201170480A1 EA 201170480 A1 EA201170480 A1 EA 201170480A1 EA 201170480 A EA201170480 A EA 201170480A EA 201170480 A EA201170480 A EA 201170480A EA 201170480 A1 EA201170480 A1 EA 201170480A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- 6alkyl
- fluorine
- methyl
- cycloalkyl
- optionally substituted
- Prior art date
Links
- 241000208465 Proteaceae Species 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 235000019419 proteases Nutrition 0.000 title 1
- 229910052731 fluorine Inorganic materials 0.000 abstract 3
- 239000011737 fluorine Substances 0.000 abstract 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 3
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 102000004171 Cathepsin K Human genes 0.000 abstract 1
- 108090000625 Cathepsin K Proteins 0.000 abstract 1
- 206010027452 Metastases to bone Diseases 0.000 abstract 1
- 150000001204 N-oxides Chemical class 0.000 abstract 1
- 208000001132 Osteoporosis Diseases 0.000 abstract 1
- 230000004913 activation Effects 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 150000002221 fluorine Chemical class 0.000 abstract 1
- 125000001153 fluoro group Chemical group F* 0.000 abstract 1
- 230000001771 impaired effect Effects 0.000 abstract 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 1
- 201000008482 osteoarthritis Diseases 0.000 abstract 1
- 206010039073 rheumatoid arthritis Diseases 0.000 abstract 1
- 125000006413 ring segment Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 abstract 1
- 125000000335 thiazolyl group Chemical group 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
Classifications
-
- 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
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
- A61P3/14—Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pain & Pain Management (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Immunology (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Соединение формулы II, в котором Rпредставляет собой C-Салкил или С-Сциклоалкил, любой из которых является необязательно замещенным одним или двумя метилами и/или фтором, трифторметилом или метокси, когда Rпредставляет собой С-Сциклоалкил, он альтернативно может быть гемзамещенным фтором; Rпредставляет собой метил или фтор; m принимает значения 0, 1 или 2; Е является связью или тиазолилом, необязательно замещенным метилом или фтором; Aпредставляет собой СН или N; Aпредставляет собой CRRили NR, при условии, что по крайней мере один из Aи Асодержит N; n принимает значения 0 или 1, так что кольцо, содержащее Aи А,представляет собой насыщенный азотсодержащий цикл из 5 или 6 кольцевых атомов; Rпредставляет собой Н, С-Салкил, C-Сгалогеналкил, С-Салкил-О-С-Салкил; или когда Aявляется С, Rможет также представлять С-Салкокси или F; Rявляется Н, С-Салкилом или F; или его фармацевтически приемлемые соль, N-оксид или гидрат, применяющиеся при лечении расстройств, отличающихся нарушенной экспрессией или активацией катепсина K, таких как остеопороз, остеоартрит, ревматоидный артрит или метастазы в кости.A compound of formula II in which R 1 is C 1-6 alkyl or C 1-6 cycloalkyl, any of which is optionally substituted with one or two methyl and / or fluorine, trifluoromethyl or methoxy, when R 1 is C 1-6 cycloalkyl, it can alternatively be gemisubstituted fluorine; R 1 is methyl or fluoro; m is 0, 1 or 2; E is a bond or thiazolyl optionally substituted with methyl or fluorine; A represents CH or N; A is CRR or NR, provided that at least one of A and A contains N; n takes the values 0 or 1, so that the ring containing A and A represents a saturated nitrogen-containing ring of 5 or 6 ring atoms; R is H, C-C1-6alkyl, C-Haloalkyl, C-C1-6alkyl-O-C-C1-6alkyl; or when A is C, R may also represent C-Salkoxy or F; R is H, C-C1-6alkyl or F; or a pharmaceutically acceptable salt, N-oxide or hydrate thereof, used in the treatment of disorders characterized by impaired expression or activation of cathepsin K, such as osteoporosis, osteoarthritis, rheumatoid arthritis or bone metastases.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0817425.2A GB0817425D0 (en) | 2008-09-24 | 2008-09-24 | Protease inhibitors |
| PCT/EP2009/062407 WO2010034789A1 (en) | 2008-09-24 | 2009-09-24 | Protease inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| EA201170480A1 true EA201170480A1 (en) | 2011-12-30 |
Family
ID=39952075
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201170480A EA201170480A1 (en) | 2008-09-24 | 2009-09-24 | PROTEAS INHIBITORS |
Country Status (10)
| Country | Link |
|---|---|
| EP (1) | EP2350089A1 (en) |
| JP (1) | JP2012503626A (en) |
| KR (1) | KR20110059657A (en) |
| CN (1) | CN102224155A (en) |
| AU (1) | AU2009295899A1 (en) |
| BR (1) | BRPI0919073A2 (en) |
| CA (1) | CA2738025A1 (en) |
| EA (1) | EA201170480A1 (en) |
| GB (1) | GB0817425D0 (en) |
| WO (1) | WO2010034789A1 (en) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201314503D0 (en) * | 2013-08-13 | 2013-09-25 | Medivir Ab | Cysteine protease inhibitor salt |
| US20220193048A1 (en) | 2019-04-05 | 2022-06-23 | Universite De Bretagne Occidentale | Protease-activated receptor-2 inhibitors for the treatment of sensory neuropathy induced by a marine neurotoxic poisoning |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0003111D0 (en) * | 2000-02-10 | 2000-03-29 | Novartis Ag | Organic compounds |
| SE0400022D0 (en) * | 2004-01-08 | 2004-01-08 | Medivir Ab | New compounds |
| GB0614052D0 (en) * | 2006-07-14 | 2006-08-23 | Amura Therapeutics Ltd | Compounds |
-
2008
- 2008-09-24 GB GBGB0817425.2A patent/GB0817425D0/en not_active Ceased
-
2009
- 2009-09-24 EA EA201170480A patent/EA201170480A1/en unknown
- 2009-09-24 CA CA2738025A patent/CA2738025A1/en not_active Abandoned
- 2009-09-24 BR BRPI0919073A patent/BRPI0919073A2/en not_active Application Discontinuation
- 2009-09-24 KR KR1020117009282A patent/KR20110059657A/en not_active Application Discontinuation
- 2009-09-24 WO PCT/EP2009/062407 patent/WO2010034789A1/en active Application Filing
- 2009-09-24 CN CN2009801480408A patent/CN102224155A/en active Pending
- 2009-09-24 JP JP2011528327A patent/JP2012503626A/en active Pending
- 2009-09-24 AU AU2009295899A patent/AU2009295899A1/en not_active Abandoned
- 2009-09-24 EP EP09783392A patent/EP2350089A1/en not_active Withdrawn
Also Published As
| Publication number | Publication date |
|---|---|
| JP2012503626A (en) | 2012-02-09 |
| AU2009295899A1 (en) | 2010-04-01 |
| CN102224155A (en) | 2011-10-19 |
| KR20110059657A (en) | 2011-06-02 |
| GB0817425D0 (en) | 2008-10-29 |
| WO2010034789A1 (en) | 2010-04-01 |
| BRPI0919073A2 (en) | 2016-03-15 |
| EP2350089A1 (en) | 2011-08-03 |
| CA2738025A1 (en) | 2010-04-01 |
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