AR074817A1 - Dihidropiridona-amidas como moduladores de p2x7 - Google Patents
Dihidropiridona-amidas como moduladores de p2x7Info
- Publication number
- AR074817A1 AR074817A1 ARP090105000A ARP090105000A AR074817A1 AR 074817 A1 AR074817 A1 AR 074817A1 AR P090105000 A ARP090105000 A AR P090105000A AR P090105000 A ARP090105000 A AR P090105000A AR 074817 A1 AR074817 A1 AR 074817A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- alkoxy
- aminocarbonyl
- hydroxyc
- optionally substituted
- Prior art date
Links
- 102100037602 P2X purinoceptor 7 Human genes 0.000 title abstract 2
- 101710189965 P2X purinoceptor 7 Proteins 0.000 title abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 12
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 8
- 125000003545 alkoxy group Chemical group 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 abstract 1
- 125000004738 (C1-C6) alkyl sulfinyl group Chemical group 0.000 abstract 1
- 125000004916 (C1-C6) alkylcarbonyl group Chemical group 0.000 abstract 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000005078 alkoxycarbonylalkyl group Chemical group 0.000 abstract 1
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 abstract 1
- 125000005093 alkyl carbonyl alkyl group Chemical group 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 125000006620 amino-(C1-C6) alkyl group Chemical group 0.000 abstract 1
- 125000005121 aminocarbonylalkoxy group Chemical group 0.000 abstract 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- ORTFAQDWJHRMNX-UHFFFAOYSA-N hydroxidooxidocarbon(.) Chemical group O[C]=O ORTFAQDWJHRMNX-UHFFFAOYSA-N 0.000 abstract 1
- 125000002757 morpholinyl group Chemical group 0.000 abstract 1
- 150000002825 nitriles Chemical group 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000003170 phenylsulfonyl group Chemical group C1(=CC=CC=C1)S(=O)(=O)* 0.000 abstract 1
- 125000004193 piperazinyl group Chemical group 0.000 abstract 1
- -1 piperidinyloxy Chemical group 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 125000003107 substituted aryl group Chemical group 0.000 abstract 1
Classifications
-
- 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
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- 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
- 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
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/80—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D211/84—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen directly attached to ring carbon atoms
- C07D211/90—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
-
- 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
- C07D401/10—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 carbon chain containing aromatic rings
-
- 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
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 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)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Rheumatology (AREA)
- Pulmonology (AREA)
- Immunology (AREA)
- Endocrinology (AREA)
- Pain & Pain Management (AREA)
- Emergency Medicine (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Se describen también métodos de obtención de los compuestos y de uso de los compuestos para el tratamiento de enfermedades asociadas con el receptor purinérgico de P2X7, así como composiciones farmacéuticas. Reivindicación 1: Un compuesto de la fórmula (1) o sales farmacéuticamente aceptables de los mismos, en la que: m es el número 0 o 1; n es el número 0 o 1; p es un número de 0 a 4; q es el número 0 o 1; R1 es hidrógeno; alquilo C1-6; hidroxi-alquilo C1-6; alcoxi C1-6-alquilo C1-6; hidroxi-alcoxi C1-6-alquilo C1-6 o aminocarbonil-alquilo C1-6; R2 es arilo opcionalmente sustituido; heteroarilo opcionalmente sustituido; cicloalquilo C3-6 o alquilo C1-6; y R3 es H; alquilo C1-6; alquilcarbonilalquilo; o alcoxicarbonilalquilo; R4 y R5 con independencia entre sí son: H; o alquilo C1-6; R6 es con independencia: halógeno; alquilo C1-6; alcoxi C1-6; halo-alquilo C1-6, halo-alcoxi C1-6, alquil C1-6-sulfonilo; alquil C1-6-sulfanilo; alquil C1-6-sulfinilo; fenilsulfonilo, cuya porción fenilo está opcionalmente sustituida por alquilo C1-6, nitrilo; hidroxi; alquil C1-6-carbonilo, aminocarbonilo, alcoxi C1-6-carbonilo; alcoxi C1-6-carbonil-alcoxi C1-6, hidroxicarbonilo; hidroxicarbonil-alcoxi C1-6; alquil C1-6-aminocarbonil-alcoxi C1-6, alcoxi C1-6-alcoxi C1-6; hidroxi-alcoxi C1-6, alquil C1-6-amino-alcoxi C1-6, alquil C1-6-sulfonil-alcoxi C1-6, hidroxi-alquilo C1-6, cicloalquil C3-6-alcoxi C1-6, amino; amino-alquilo C1-6, alquenilo C1-6, alquinilo C1-6; morfolinilo; morfolinil-alquilo C1-6, piperazinilo; piperidiniloxi; aminocarbonil-alcoxi C1-6; alcoxi C1-6-amino-alquilo C1-6, hidroxi-alquil C1-6-amino-alquilo C1-6, alcoxi C1-6-carbonilamino-alquilo C1-6, alquil C1-6-carbonilamino-alquilo C1-6; alquil C1-6-aminocarbonilo; alcoxi C1-6-carbonil-alquilo C1-6, alquil C1-6-aminocarbonil-alquilo C1-6, alquil C1-6-amino-alquilo C1-6, hidroxicarbonil-alquilo C1-6, hidroxi-alcoxi C1-6-alquilo C1-6 o nitro; o dos sustituyentes adyacentes pueden formar un alquileno C1-2-dioxi o halo-alquileno C1-2-dioxi; y A es un anillo heteroarilo de cinco o seis eslabones, que esta opcionalmente sustituido.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US20346208P | 2008-12-23 | 2008-12-23 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR074817A1 true AR074817A1 (es) | 2011-02-16 |
Family
ID=41800777
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP090105000A AR074817A1 (es) | 2008-12-23 | 2009-12-21 | Dihidropiridona-amidas como moduladores de p2x7 |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US8163929B2 (es) |
| EP (1) | EP2382202A1 (es) |
| JP (1) | JP5405592B2 (es) |
| KR (1) | KR101370185B1 (es) |
| CN (1) | CN102264722B (es) |
| AR (1) | AR074817A1 (es) |
| AU (1) | AU2009331669B2 (es) |
| BR (1) | BRPI0924059A2 (es) |
| CA (1) | CA2745952A1 (es) |
| IL (1) | IL213346A (es) |
| MX (1) | MX2011006843A (es) |
| SG (1) | SG172385A1 (es) |
| TW (1) | TW201028392A (es) |
| WO (1) | WO2010072607A1 (es) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011072012A2 (en) * | 2009-12-08 | 2011-06-16 | Vanderbilt University | Improved methods and compositions for vein harvest and autografting |
| NZ710270A (en) | 2013-01-31 | 2020-09-25 | Vertex Pharma | Pyridone amides as modulators of sodium channels |
| EP3640241B1 (en) * | 2013-10-18 | 2022-09-28 | Celgene Quanticel Research, Inc. | Bromodomain inhibitors |
| AR098436A1 (es) * | 2013-11-19 | 2016-05-26 | Actelion Pharmaceuticals Ltd | Compuestos tricíclicos de piperidina |
| DK3080134T3 (en) | 2013-12-13 | 2018-10-22 | Vertex Pharma | PRODRUGS OF PYRIDONAMIDS USED AS MODULATORS OF SODIUM CHANNELS |
| WO2015099107A1 (ja) | 2013-12-26 | 2015-07-02 | 塩野義製薬株式会社 | 含窒素6員環誘導体およびそれらを含有する医薬組成物 |
| CN104926801B (zh) * | 2014-03-22 | 2019-06-04 | 浙江大学 | 取代氮杂环类衍生物、含其的药物组合物及其在抗肿瘤中的应用 |
| MX391647B (es) | 2015-04-24 | 2025-03-21 | Shionogi & Co | Derivados heterociclicos de seis miembros y composicion farmaceutica que los comprende. |
| WO2018074390A1 (ja) | 2016-10-17 | 2018-04-26 | 塩野義製薬株式会社 | 二環性含窒素複素環誘導体およびそれらを含有する医薬組成物 |
| EP3625214B1 (en) | 2017-05-16 | 2022-07-06 | Vertex Pharmaceuticals Incorporated | Deuterated pyridone amides and prodrugs thereof as modulators of sodium channels |
| US20190343817A1 (en) | 2018-02-12 | 2019-11-14 | Vertex Pharmaceuticals Incorporated | Method of treating pain |
| AU2020397059A1 (en) | 2019-12-06 | 2022-07-21 | Vertex Pharmaceuticals Incorporated | Substituted tetrahydrofurans as modulators of sodium channels |
| CN117794920A (zh) | 2021-06-04 | 2024-03-29 | 沃泰克斯药物股份有限公司 | N-(羟烷基(杂)芳基)四氢呋喃甲酰胺作为钠通道调节剂 |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5399566A (en) * | 1990-06-19 | 1995-03-21 | Meiji Seika Kabushiki Kaisha | Pyridine derivatives having angiotensin II antagonism |
| CZ403592A3 (en) | 1992-02-20 | 1993-12-15 | Hoechst Ag | Arylcarbonylaminoalkyldihydrooxopyridines, process of their preparation and their use |
| DE4206045A1 (de) | 1992-02-27 | 1993-09-02 | Bayer Ag | Sulfonylbenzyl substituierte pyridone |
| DE4215587A1 (de) | 1992-05-12 | 1993-11-18 | Bayer Ag | Sulfonylbenzyl-substituierte Benzo- und Pyridopyridone |
| BR9907300A (pt) | 1998-01-27 | 2000-10-24 | Aventis Pharm Prod Inc | Inibidores do fator xa oxoaza-heterociclila substituìdos |
| DE10010430A1 (de) * | 2000-03-03 | 2001-09-06 | Bayer Ag | Substituierte 5-Ethyl-dihydropyridazinone und ihre Verwendung |
| HU229553B1 (en) | 2000-06-12 | 2014-01-28 | Eisai R & D Man Co | 1,2-dihydropyridine compound, process for preparation of the same and use thereof |
| GB0129260D0 (en) | 2001-12-06 | 2002-01-23 | Eisai London Res Lab Ltd | Pharmaceutical compositions and their uses |
| JP2005170790A (ja) | 2002-01-09 | 2005-06-30 | Ajinomoto Co Inc | N−アルキルスルフォニル置換アミド誘導体 |
| US7592357B2 (en) * | 2004-02-20 | 2009-09-22 | Smithkline Beecham Corporation | Compounds |
| FR2878528B1 (fr) | 2004-11-29 | 2008-05-16 | Aventis Pharma Sa | 2-alcoxy-3,4,5-trihydroxy-alkylamides, leur preparation, compositions les contenant et utilisation |
| HRP20110524T1 (hr) | 2005-04-04 | 2011-08-31 | Eisai R&D Management Co. | Spojevi dihidropiridina za neurodegenerativne bolesti i demenciju |
| EP1875912A4 (en) | 2005-04-08 | 2008-06-04 | Eisai R&D Man Co Ltd | MEANS OF TREATING UNWILLING MOVEMENTS |
| WO2007035428A1 (en) | 2005-09-15 | 2007-03-29 | Bristol-Myers Squibb Company | Met kinase inhibitors |
-
2009
- 2009-12-14 CN CN200980152119.8A patent/CN102264722B/zh not_active Expired - Fee Related
- 2009-12-14 EP EP20090775183 patent/EP2382202A1/en not_active Withdrawn
- 2009-12-14 MX MX2011006843A patent/MX2011006843A/es active IP Right Grant
- 2009-12-14 JP JP2011542764A patent/JP5405592B2/ja not_active Expired - Fee Related
- 2009-12-14 KR KR1020117014474A patent/KR101370185B1/ko not_active Expired - Fee Related
- 2009-12-14 WO PCT/EP2009/067060 patent/WO2010072607A1/en not_active Ceased
- 2009-12-14 SG SG2011046679A patent/SG172385A1/en unknown
- 2009-12-14 BR BRPI0924059-4A patent/BRPI0924059A2/pt not_active IP Right Cessation
- 2009-12-14 AU AU2009331669A patent/AU2009331669B2/en not_active Ceased
- 2009-12-14 CA CA2745952A patent/CA2745952A1/en not_active Abandoned
- 2009-12-15 US US12/637,940 patent/US8163929B2/en not_active Expired - Fee Related
- 2009-12-21 AR ARP090105000A patent/AR074817A1/es unknown
- 2009-12-22 TW TW098144253A patent/TW201028392A/zh unknown
-
2011
- 2011-06-02 IL IL213346A patent/IL213346A/en not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| CN102264722A (zh) | 2011-11-30 |
| CN102264722B (zh) | 2014-04-02 |
| IL213346A0 (en) | 2011-07-31 |
| AU2009331669B2 (en) | 2015-10-15 |
| EP2382202A1 (en) | 2011-11-02 |
| KR20110086868A (ko) | 2011-08-01 |
| SG172385A1 (en) | 2011-08-29 |
| CA2745952A1 (en) | 2010-07-01 |
| AU2009331669A1 (en) | 2011-06-23 |
| IL213346A (en) | 2015-08-31 |
| MX2011006843A (es) | 2011-08-04 |
| AU2009331669A8 (en) | 2011-07-07 |
| BRPI0924059A2 (pt) | 2015-07-07 |
| TW201028392A (en) | 2010-08-01 |
| JP2012513437A (ja) | 2012-06-14 |
| WO2010072607A1 (en) | 2010-07-01 |
| JP5405592B2 (ja) | 2014-02-05 |
| US8163929B2 (en) | 2012-04-24 |
| US20100160384A1 (en) | 2010-06-24 |
| KR101370185B1 (ko) | 2014-03-05 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |