AR067156A1 - DERIVADOS DE TETRAHIDRO-2H-PIRIDO(4,3-B)INDOL-2-ILO, UN PROCESO PARA SU PREPARACION, UNA COMPOSICION FARMACEUTICA QUE LOS COMPRENDE Y SU USO EN LA FABRICACIoN DE UN MEDICAMENTO PARA EL TRATAMIENTO DE ENFERMEDADES MEDIADAS POR LA INHIBICION DE CATEPSINA K - Google Patents
DERIVADOS DE TETRAHIDRO-2H-PIRIDO(4,3-B)INDOL-2-ILO, UN PROCESO PARA SU PREPARACION, UNA COMPOSICION FARMACEUTICA QUE LOS COMPRENDE Y SU USO EN LA FABRICACIoN DE UN MEDICAMENTO PARA EL TRATAMIENTO DE ENFERMEDADES MEDIADAS POR LA INHIBICION DE CATEPSINA KInfo
- Publication number
- AR067156A1 AR067156A1 ARP080102722A ARP080102722A AR067156A1 AR 067156 A1 AR067156 A1 AR 067156A1 AR P080102722 A ARP080102722 A AR P080102722A AR P080102722 A ARP080102722 A AR P080102722A AR 067156 A1 AR067156 A1 AR 067156A1
- Authority
- AR
- Argentina
- Prior art keywords
- independently selected
- optionally substituted
- ring
- alkyl
- halogen
- Prior art date
Links
- 201000010099 disease Diseases 0.000 title abstract 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title abstract 3
- 238000000034 method Methods 0.000 title abstract 2
- 230000005764 inhibitory process Effects 0.000 title 1
- 238000004519 manufacturing process Methods 0.000 title 1
- 229940126601 medicinal product Drugs 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 10
- 150000001875 compounds Chemical class 0.000 abstract 8
- 229910052736 halogen Inorganic materials 0.000 abstract 7
- 150000002367 halogens Chemical class 0.000 abstract 7
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 6
- 229910052739 hydrogen Inorganic materials 0.000 abstract 6
- 125000002950 monocyclic group Chemical group 0.000 abstract 6
- 125000001424 substituent group Chemical group 0.000 abstract 6
- 239000001257 hydrogen Substances 0.000 abstract 5
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 5
- 229910052757 nitrogen Inorganic materials 0.000 abstract 5
- 229910052760 oxygen Inorganic materials 0.000 abstract 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 5
- 229910052717 sulfur Inorganic materials 0.000 abstract 5
- 125000004429 atom Chemical group 0.000 abstract 4
- 125000005842 heteroatom Chemical group 0.000 abstract 4
- 125000000623 heterocyclic group Chemical group 0.000 abstract 4
- 125000006413 ring segment Chemical group 0.000 abstract 4
- -1 OR3 Chemical group 0.000 abstract 3
- 125000004122 cyclic group Chemical group 0.000 abstract 3
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 3
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 3
- 229920006395 saturated elastomer Polymers 0.000 abstract 3
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 2
- 102000005927 Cysteine Proteases Human genes 0.000 abstract 2
- 108010005843 Cysteine Proteases Proteins 0.000 abstract 2
- 101100295738 Gallus gallus COR3 gene Proteins 0.000 abstract 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 125000001624 naphthyl group Chemical group 0.000 abstract 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 125000004434 sulfur atom Chemical group 0.000 abstract 2
- ABADUMLIAZCWJD-UHFFFAOYSA-N 1,3-dioxole Chemical group C1OC=CO1 ABADUMLIAZCWJD-UHFFFAOYSA-N 0.000 abstract 1
- 102000004171 Cathepsin K Human genes 0.000 abstract 1
- 108090000625 Cathepsin K Proteins 0.000 abstract 1
- 102000005600 Cathepsins Human genes 0.000 abstract 1
- 108010084457 Cathepsins Proteins 0.000 abstract 1
- 125000001931 aliphatic group Chemical group 0.000 abstract 1
- 229910052796 boron Inorganic materials 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 229910052731 fluorine Inorganic materials 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 229910052700 potassium Inorganic materials 0.000 abstract 1
- 230000002441 reversible effect Effects 0.000 abstract 1
- 229910052721 tungsten Inorganic materials 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
-
- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
- C07D471/14—Ortho-condensed systems
-
- 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
-
- 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
-
- 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
- C07D491/12—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 three hetero rings
- C07D491/14—Ortho-condensed systems
- C07D491/147—Ortho-condensed systems the condensed system containing one ring with oxygen as ring hetero atom and two rings with nitrogen as ring hetero atom
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Physical Education & Sports Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pain & Pain Management (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Oncology (AREA)
- Biomedical Technology (AREA)
- Immunology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
Compuestos y composiciones para el tratamiento de enfermedades asociadas con la actividad de cisteina proteasa. Los compuestos son inhibidores reversibles de cisteina proteasa, incluyendo las catepsinas B, K, C, F, H, L, O, S, W y X. Las enfermedades asociadas con la Catepsina K son de particular interés. Reivindicacion 1: Un compuesto, caracterizado porque responde a la formula (1) en el cual: A es un anillo alifático de 5 a 7 miembros que contiene optativamente una ligadura doble y que comprende optativamente un átomo de oxígeno como un miembro del anillo y que se sustituye optativamente con hasta tres sustituyentes cada uno independientemente seleccionado entre halogeno, C1-2alquilo y C3-4carbociclilo; R es hidrogeno o C1-6 alquilo; R1 y R2 junto con el átomo de nitrogeno al cual están unidos forman un anillo heterocíclico saturado o parcialmente insaturado monocíclico de 5 a 7 miembros, en el cual el anillo comparte al menos un átomo con un segundo anillo monocíclico saturado, parcialmente insaturado o insaturado para formar un sistema de anillos bicíclico; sistema de anillos bicíclico el cual comparte al menos un átomo con un tercer anillo saturado, parcialmente insaturado o insaturado para formar un sistema de anillos tricíclico que comprende hasta 19 átomos del anillo, y donde el sistema de anillos tricíclico comprende optativamente hasta cinco heteroátomos cada uno independientemente seleccionado entre átomos de O, S o N, y está optativamente sustituido por hasta tres sustituyentes cada uno independientemente seleccionado entre fenilo, bencilo, naftilo, C1-6 alquilo, C2-6alquenilo, C2-6alquinilo, ciano, halogeno, COOR3, COR3, NO2, OR3, CONR4R5, NR4R5, C1-2alcansulfonilo, heteroarilo monocíclico que comprende hasta 7 átomos del anillo, y heteroarilo bicíclico que comprende hasta 12 átomos de carbono, y el sistema de anillos tricíclico está sustituido optativamente en átomos de carbono adyacentes por un grupo -O-C(R8)2-O-, donde cada R8 es hidrogeno o un átomo de halogeno de modo que forma un grupo 1,3-dioxol, y donde (i) fenilo, naftilo, C1-6 alquilo, C2-6alquenilo, C2-6alquinilo y bencilo se sustituyen optativamente además con hasta tres sustituyentes cada uno independientemente seleccionado entre halogeno, NR4R5, SO2R3, CONR4R5, ciano, OR3, SO2NR4R5, NSO2R3, NR4COR5, y C1-6 alquilo el mismo optativamente sustituido con hasta tres sustituyentes seleccionados independientemente entre halogeno, ciano, SO2R3, NR4R5, OR3, SO2NR4R5, NSO2R3, NR4COR5 y CONR4R5, y (ii) heteroarilo monocíclico o bicíclico se sustituyen optativamente además con hasta tres sustituyentes cada uno independientemente seleccionado entre halogeno, NR4R5, SO2NR4R5, NSO2R3, NR4COR5, CONR4R5 , SO2R3, ciano, OR3, y fenilo el mismo optativamente sustituido con hasta tres grupos halogeno, SO2R3, o C1-6 alquilo el mismo optativamente sustituido con hasta tres sustituyentes seleccionados independientemente entre halogeno, ciano, SO2R3, SO2NR4R5, NSO2R3, NR4COR5, NR4R5, OR3, C3-7carbociclilo y CONR4R5; R3 se selecciona entre hidrogeno, C1-6 alquilo, C3-7carbociclilo, fenilo, heteroarilo monocíclico, un anillo heterocíclico saturado monocíclico de 4 a 7 miembros que comprende hasta tres heteroátomos cada uno independientemente seleccionado entre átomos de O, S o N, y donde C1-6 alquilo y fenilo y heteroarilo monocíclico cada uno puede sustituirse optativamente con hasta tres grupos seleccionados independientemente entre halogeno, ciano, CONR4R5, NR4R5, SO2NR4R5, NSO2R3 y SO2R3; R4 y R5 son independientemente hidrogeno, C1-6 alquilo, COR3, heteroarilo monocíclico que comprende hasta 7 átomos del anillo o heteroarilo biciclico que comprende hasta 12 átomos del anillo o junto con el nitrogeno al cual están unidos forman un anillo heterocíclico saturado monociclico de 5 a 7 miembros que comprende optativamente hasta tres heteroátomos adicionales cada uno independientemente seleccionado entre átomos de O, S o N y se sustituye optativamente con C1-6 alquilo optativamente sustituido con NR6R7; R6 y R7 son independientemente hidrogeno, C1-6 alquilo, o junto con el nitrogeno al cual están unidos forman un anillo heterocíclico saturado monocíclico de 5 a 7 miembros que comprende optativamente hasta tres heteroátomos adicionales cada uno independientemente seleccionado entre átomos de O, S o N; y sus sales aceptables para uso farmacéutico. Reivindicacion 5: Un proceso para la preparacion de un compuesto de la formula (1) como se define en la reivindicacion 1, caracterizado porque comprende: (a) tratar un compuesto de la formula (2): con un compuesto de la formula (3) donde R, R1 y R2 son como se define en cualquiera entre las reivindicaciones 1 a 5, o (b) tratar un compuesto de la formula (4): con un compuesto de la formula (5) donde R, R1 y R2 son como se define en cualquiera entre las reivindicaciones 1 a 5, y optativamente después de (a) o (b) formar una sal aceptable para uso farmacéutico.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US94617807P | 2007-06-26 | 2007-06-26 | |
| US4284008P | 2008-04-07 | 2008-04-07 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR067156A1 true AR067156A1 (es) | 2009-09-30 |
Family
ID=39761131
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP080102722A AR067156A1 (es) | 2007-06-26 | 2008-06-25 | DERIVADOS DE TETRAHIDRO-2H-PIRIDO(4,3-B)INDOL-2-ILO, UN PROCESO PARA SU PREPARACION, UNA COMPOSICION FARMACEUTICA QUE LOS COMPRENDE Y SU USO EN LA FABRICACIoN DE UN MEDICAMENTO PARA EL TRATAMIENTO DE ENFERMEDADES MEDIADAS POR LA INHIBICION DE CATEPSINA K |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US8008279B2 (es) |
| EP (1) | EP2170879B1 (es) |
| JP (1) | JP2010531344A (es) |
| KR (1) | KR20100039862A (es) |
| CN (1) | CN101687864A (es) |
| AR (1) | AR067156A1 (es) |
| AU (1) | AU2008269513B2 (es) |
| BR (1) | BRPI0813306A2 (es) |
| CA (1) | CA2689945A1 (es) |
| CL (1) | CL2008001899A1 (es) |
| CO (1) | CO6251264A2 (es) |
| EC (1) | ECSP109882A (es) |
| IL (1) | IL202519A0 (es) |
| NZ (1) | NZ581719A (es) |
| PE (1) | PE20090841A1 (es) |
| RU (1) | RU2470023C2 (es) |
| TW (1) | TW200911806A (es) |
| UY (1) | UY31180A1 (es) |
| WO (1) | WO2009001129A1 (es) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2523580T3 (es) | 2008-01-11 | 2014-11-27 | Albany Molecular Research, Inc. | Piridoindoles substituidos con (1-Azinona) |
| JP5666036B2 (ja) * | 2008-01-25 | 2015-02-04 | メディベイション テクノロジーズ， インコーポレイテッド | 新規２，３，４，５−テトラヒドロ−１Ｈ−ピリド［４，３−ｂ］インドール化合物およびその使用方法 |
| RU2544856C2 (ru) | 2008-01-25 | 2015-03-20 | Сергей Олегович Бачурин | НОВЫЕ ПРОИЗВОДНЫЕ 2,3,4,5-ТЕТРАГИДРО-1-ПИРИДО[4,3-b]ИНДОЛА И СПОСОБЫ ИХ ПРИМЕНЕНИЯ |
| CN102227431A (zh) | 2008-09-29 | 2011-10-26 | 雅培制药有限公司 | 吲哚和二氢吲哚衍生物及其应用方法 |
| US9625475B2 (en) | 2008-09-29 | 2017-04-18 | Abbvie Inc. | Indole and indoline derivatives and methods of use thereof |
| CA2745085C (en) * | 2008-12-18 | 2018-03-06 | Merck Patent Gmbh | Tricyclic azaindoles |
| US7893099B2 (en) * | 2009-06-11 | 2011-02-22 | Hoffman-La Roche Inc. | Cyclopentane derivatives |
| US8629158B2 (en) * | 2009-07-01 | 2014-01-14 | Albany Molecular Research, Inc. | Azabicycloalkane-indole and azabicycloalkane-pyrrolo-pyridine MCH-1 antagonists, methods of making, and use thereof |
| US9073925B2 (en) * | 2009-07-01 | 2015-07-07 | Albany Molecular Research, Inc. | Azinone-substituted azabicycloalkane-indole and azabicycloalkane-pyrrolo-pyridine MCH-1 antagonists, methods of making, and use thereof |
| EP2448585B1 (en) * | 2009-07-01 | 2014-01-01 | Albany Molecular Research, Inc. | Azinone-substituted azepino[b]indole and pyrido-pyrrolo-azepine mch-1 antagonists, methods of making, and use thereof |
| WO2011003012A1 (en) * | 2009-07-01 | 2011-01-06 | Albany Molecular Research, Inc. | Azinone-substituted azapolycycle mch-1 antagonists, methods of making, and use thereof |
| HRP20140213T1 (hr) * | 2009-10-21 | 2014-04-11 | Boehringer Ingelheim International Gmbh | Spojevi indazola i pirazolopiridina kao antagonisti ccr1-receptora |
| JP5542214B2 (ja) | 2009-10-27 | 2014-07-09 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Ｃｃｒ１受容体アンタゴニストとしての複素環化合物 |
| US8778959B2 (en) | 2009-12-17 | 2014-07-15 | Abbvie Inc. | AZA-bridged ring-fused indoles and indolines |
| ES2512241T3 (es) | 2009-12-17 | 2014-10-23 | Abbvie Inc. | Indoles e indolinas de anillos condensados con amina cabeza de puente útiles para tratar trastornos neurodegenerativos y neuropsiquiátricos |
| JP5793182B2 (ja) | 2010-04-30 | 2015-10-14 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Ｃｃｒ１受容体アンタゴニストとしてのアザインダゾールアミド化合物 |
| WO2012088124A2 (en) | 2010-12-21 | 2012-06-28 | Albany Molecular Research, Inc. | Tetrahydro-azacarboline mch-1 antagonists, methods of making, and uses thereof |
| US8697700B2 (en) | 2010-12-21 | 2014-04-15 | Albany Molecular Research, Inc. | Piperazinone-substituted tetrahydro-carboline MCH-1 antagonists, methods of making, and uses thereof |
| JP2014505738A (ja) | 2011-02-18 | 2014-03-06 | メディベイション テクノロジーズ， インコーポレイテッド | 高血圧を処置するための化合物および方法 |
| JP6068505B2 (ja) * | 2012-01-11 | 2017-01-25 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | プロテアーゼ阻害剤としてのマクロ環式アミド |
| CN103086923B (zh) * | 2013-01-21 | 2014-04-23 | 吉林大学 | 肼腈类组织蛋白酶k抑制剂及其在治疗骨质疏松症方面的应用 |
| EP3055314B1 (en) * | 2013-10-08 | 2018-09-12 | Merck Sharp & Dohme Corp. | Cathepsin cysteine protease inhibitors |
| WO2016027285A2 (en) * | 2014-08-22 | 2016-02-25 | Alkem Laboratories Ltd. | Bicyclic heteroaryl amides as cathepsin cysteine protease inhibitors |
| CN105837479B (zh) * | 2016-04-05 | 2017-10-27 | 吉林大学 | 肼腈类组织蛋白酶k抑制剂及其在制备治疗骨关节炎药物中的应用 |
| WO2018183654A1 (en) * | 2017-03-29 | 2018-10-04 | Minerva Biotechnologies Corporation | Agents for differentiating stem cells and treating cancer |
| US20250145576A1 (en) * | 2022-01-21 | 2025-05-08 | Shandong New Time Pharmaceutical Co., Ltd. | Cathepsin k inhibitor, and preparation method therefor and use thereof |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2264937T3 (es) * | 1999-07-30 | 2007-02-01 | Boehringer Ingelheim Pharmaceuticals Inc. | Nuevos compuestos derivados de succinato, utiles como inhibidores de cisteina-proteasa. |
| WO2001049288A1 (en) * | 2000-01-06 | 2001-07-12 | Merck Frosst Canada & Co. | Novel compounds and compositions as protease inhibitors |
| WO2001068645A2 (en) | 2000-03-15 | 2001-09-20 | Axys Pharmaceuticals, Inc. | N-cyanomethylcarboxamides and their use as protease inhibitors |
| ATE409482T1 (de) * | 2001-03-02 | 2008-10-15 | Merck Frosst Canada Ltd | Cathepsincystein-proteasehemmer |
| RU2278863C2 (ru) * | 2001-08-10 | 2006-06-27 | Орто-Макнейл Фармасьютикал, Инк. | Замещенные пиразолы, фармацевтическая композиция и способ ингибирования активности катепсина s |
| DE60219068T2 (de) * | 2001-12-04 | 2007-12-13 | F. Hoffmann-La Roche Ag | Substituierte 2-amino-cykloalkankarboxamide und ihre verwendung als cysteinprotease-inhibitoren |
| SE0201977D0 (sv) * | 2002-06-24 | 2002-06-24 | Astrazeneca Ab | Novel compounds |
| SE0203712D0 (sv) | 2002-12-13 | 2002-12-13 | Astrazeneca Ab | Novel compounds |
| ES2364046T3 (es) | 2002-12-19 | 2011-08-23 | Bristol-Myers Squibb Company | Gamma-carbolinas tricíclicas sustituidas utilizadas como agonistas y antagonistas de los receptores de la serotonina. |
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2008
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- 2008-06-24 CN CN200880021955A patent/CN101687864A/zh active Pending
- 2008-06-24 CA CA2689945A patent/CA2689945A1/en not_active Abandoned
- 2008-06-24 KR KR1020107001848A patent/KR20100039862A/ko not_active Withdrawn
- 2008-06-24 NZ NZ581719A patent/NZ581719A/en not_active IP Right Cessation
- 2008-06-24 JP JP2010514135A patent/JP2010531344A/ja active Pending
- 2008-06-24 RU RU2010101279/04A patent/RU2470023C2/ru not_active IP Right Cessation
- 2008-06-24 EP EP08776161A patent/EP2170879B1/en active Active
- 2008-06-24 BR BRPI0813306A patent/BRPI0813306A2/pt not_active IP Right Cessation
- 2008-06-24 WO PCT/GB2008/050486 patent/WO2009001129A1/en not_active Ceased
- 2008-06-25 TW TW097123686A patent/TW200911806A/zh unknown
- 2008-06-25 AR ARP080102722A patent/AR067156A1/es not_active Application Discontinuation
- 2008-06-25 US US12/145,855 patent/US8008279B2/en not_active Expired - Fee Related
- 2008-06-25 UY UY31180A patent/UY31180A1/es not_active Application Discontinuation
- 2008-06-26 CL CL2008001899A patent/CL2008001899A1/es unknown
- 2008-06-26 PE PE2008001087A patent/PE20090841A1/es not_active Application Discontinuation
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2009
- 2009-12-03 IL IL202519A patent/IL202519A0/en unknown
- 2009-12-22 CO CO09146663A patent/CO6251264A2/es not_active Application Discontinuation
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2010
- 2010-01-15 EC EC2010009882A patent/ECSP109882A/es unknown
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| Publication number | Publication date |
|---|---|
| JP2010531344A (ja) | 2010-09-24 |
| ECSP109882A (es) | 2010-02-26 |
| UY31180A1 (es) | 2009-01-30 |
| KR20100039862A (ko) | 2010-04-16 |
| WO2009001129A1 (en) | 2008-12-31 |
| AU2008269513B2 (en) | 2011-06-16 |
| CO6251264A2 (es) | 2011-02-21 |
| CA2689945A1 (en) | 2008-12-31 |
| TW200911806A (en) | 2009-03-16 |
| BRPI0813306A2 (pt) | 2017-05-16 |
| CN101687864A (zh) | 2010-03-31 |
| RU2010101279A (ru) | 2011-08-10 |
| NZ581719A (en) | 2011-08-26 |
| CL2008001899A1 (es) | 2009-07-17 |
| EP2170879A1 (en) | 2010-04-07 |
| AU2008269513A1 (en) | 2008-12-31 |
| WO2009001129A9 (en) | 2010-02-04 |
| PE20090841A1 (es) | 2009-08-02 |
| RU2470023C2 (ru) | 2012-12-20 |
| US20090012077A1 (en) | 2009-01-08 |
| IL202519A0 (en) | 2010-06-30 |
| EP2170879B1 (en) | 2013-01-16 |
| US8008279B2 (en) | 2011-08-30 |
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