AR058071A1 - Derivados de dihidropirazolo (3,4-e)(1,4)diazepina. procesos de obtencion y composiciones farmaceuticas. - Google Patents
Derivados de dihidropirazolo (3,4-e)(1,4)diazepina. procesos de obtencion y composiciones farmaceuticas.Info
- Publication number
- AR058071A1 AR058071A1 ARP060104273A ARP060104273A AR058071A1 AR 058071 A1 AR058071 A1 AR 058071A1 AR P060104273 A ARP060104273 A AR P060104273A AR P060104273 A ARP060104273 A AR P060104273A AR 058071 A1 AR058071 A1 AR 058071A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- optionally substituted
- alkoxy
- halogen
- heteroaryl
- Prior art date
Links
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 7
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 4
- 125000003118 aryl group Chemical group 0.000 abstract 4
- 229910052736 halogen Inorganic materials 0.000 abstract 4
- 150000002367 halogens Chemical class 0.000 abstract 4
- 125000001072 heteroaryl group Chemical group 0.000 abstract 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 4
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 abstract 1
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 abstract 1
- 125000001054 5 membered carbocyclic group Chemical group 0.000 abstract 1
- 125000004008 6 membered carbocyclic group Chemical group 0.000 abstract 1
- 101100296719 Caenorhabditis elegans pde-4 gene Proteins 0.000 abstract 1
- 150000001204 N-oxides Chemical class 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000004414 alkyl thio group Chemical group 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- -1 nitro, hydroxy Chemical group 0.000 abstract 1
- 125000005359 phenoxyalkyl group Chemical group 0.000 abstract 1
- 125000002071 phenylalkoxy group Chemical group 0.000 abstract 1
- 125000003884 phenylalkyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229920006395 saturated elastomer Chemical group 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
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- 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
-
- 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
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- 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
-
- 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
- A61P13/00—Drugs for disorders of the urinary system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological 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
-
- 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
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- 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
- A61P25/06—Antimigraine agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic 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
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Ophthalmology & Optometry (AREA)
- Urology & Nephrology (AREA)
- Rheumatology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Heart & Thoracic Surgery (AREA)
- Endocrinology (AREA)
- Transplantation (AREA)
- Diabetes (AREA)
- Cardiology (AREA)
- Dermatology (AREA)
- Gastroenterology & Hepatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Procesos para preparar dichos compuestos, el uso de dichos compuestos en el tratamiento de un estado de enfermedad mediado por PDE 4, y composiciones farmacéuticas que los contienen. Reivindicacion 1: Un compuesto caracterizado porque responde a la formula (1) donde R1 es un anillo carbocíclico o heterocíclico e 5 o 6 miembros, saturado o no saturado; cuando R1 es arilo o heteroarilo entonces dicho arilo o heteroarilo se sustituye opcionalmente como se muestra a continuacion; cuando R1 es un carbociclo no aromático o heterociclilo no aromático entonces dicho anillo esta opcionalmente sustituido con alquilo C1-6; R2 es alquilo C1-4, alcoxi C1-4 o alquiltio C1-4; R3 es H o alquilo C1-4; R4 es alquilo C1-6 (opcionalmente sustituido con CO2R26 o C(O)NR27R28), arilo opcionalmente sustituido o heteroarilo opcionalmente sustituido; R25 es H o fenilo opcionalmente sustituido; los anillos arilo, heteroarilo y fenilo mencionados se sustituyen opcionalmente en forma independiente con: halogeno, ciano, nitro, hidroxi, S(O)qR5, OC(O)NR6R7, NR8R9, NR10C(O)R11, NR12C(O)NR13R14, S(O)2NR15R16, NR17S(O)2R18, C(O)NR19R20, C(O)R21, CO2R22, NR23CO2R24, alquilo C1-6, haloalquilo C1-6 alcoxi C1-6-alquilo C1-6, alcoxi C1-6, haloalcoxi C1-6, alcoxi C1-6-alcoxi C1-6, alquiltio C1-6, O(CH2)nO, fenilalquilo C1-6, fenoxialquilo C1-6 o fenilalcoxi C1-6; los anillos fenilo de los ultimos tres sustituyentes se sustituyen opcionalmente con halogeno, alquilo C1-4, alcoxi C1-4, CF3 o OCF3; n es 1, 2 o 3; q es 0, 1 o 2; R6 y R7, R13 y R14, R15 y R16, o R19 y R20 se pueden unir para formar, con e N al cual están unidos, un anillo de 5 o 6 miembros; R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, R19, R20, R21, R22, R23, R24 y R26 son, en forma independiente, alquilo C1-6, (opcionalmente sustituido con halogeno, hidroxi o alcoxi C1-6) o fenilo (él mismo opcionalmente sustituido con halogeno, alquilo C1-4, alcoxi C1-4, CF3 o OCF3); R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R19, R20, R21, R22, R23 y R26 pueden también ser H; R27 es H o alquilo C1-6; R28 es H o alquilo C1-6 (opcionalmente sustituido con NH2, NH(alquilo C1-6) o N(alquil C1-6)2); o un N-oxido de los mismos; o una sal aceptable para uso farmacéutico de los mismos.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| SE0502176 | 2005-10-03 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR058071A1 true AR058071A1 (es) | 2008-01-23 |
Family
ID=37906399
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP060104273A AR058071A1 (es) | 2005-10-03 | 2006-09-28 | Derivados de dihidropirazolo (3,4-e)(1,4)diazepina. procesos de obtencion y composiciones farmaceuticas. |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US20090054413A1 (es) |
| EP (1) | EP1931672A1 (es) |
| JP (1) | JP2009510159A (es) |
| AR (1) | AR058071A1 (es) |
| TW (1) | TW200745106A (es) |
| UY (1) | UY29821A1 (es) |
| WO (1) | WO2007040435A1 (es) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2754922C (en) * | 2009-03-12 | 2016-10-18 | Cumberland Pharmaceuticals Inc. | Administration of intravenous ibuprofen |
| SG176571A1 (en) * | 2009-05-19 | 2012-01-30 | Vivia Biotech Sl | Methods for providing personalized medicine tests ex vivo for hematological neoplasms |
| US8871810B2 (en) | 2009-07-15 | 2014-10-28 | Cumberland Pharmaceuticals Inc. | Treating critically ill patients with intravenous ibuprofen |
| US9072661B2 (en) | 2012-03-16 | 2015-07-07 | Cumberland Pharmaceuticals Inc. | Injectable ibuprofen formulation |
| US9072710B2 (en) | 2012-03-16 | 2015-07-07 | Cumberland Pharmaceuticals Inc. | Injectable ibuprofen formulation |
| RU2768746C2 (ru) * | 2016-12-12 | 2022-03-24 | Юнион Терапьютикс А/С | Замещенные пиразолоазепин-4-оны и их применение в качестве ингибиторов фосфодиэстеразы |
| RU2762279C2 (ru) * | 2016-12-12 | 2021-12-17 | Юнион Терапьютикс А/С | Замещенные пиразолоазепин-4-оны и их применение в качестве ингибиторов фосфодиэстеразы |
| EP3551634B1 (en) * | 2016-12-12 | 2021-03-31 | Leo Pharma A/S | Substituted pyrazoloazepin-8-ones and their use as phosphodiesterase inhibitors |
| TWI812739B (zh) * | 2018-06-21 | 2023-08-21 | 景凱生物科技股份有限公司 | Nadph氧化酶抑制劑、含其的醫藥組合物、及其應用 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EA200200240A1 (ru) * | 1999-10-11 | 2002-10-31 | Пфайзер Инк. | 5-(2-ЗАМЕЩЕННЫЕ-5-ГЕТЕРОЦИКЛИЛСУЛЬФОНИЛПИРИД-3-ИЛ)-ДИГИДРОПИРАЗОЛО[4,3-d]ПИРИМИДИН-7-ОНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ ФОСФОДИЭСТЕРАЗЫ |
| FR2803299B1 (fr) * | 2000-01-05 | 2004-09-17 | Warner Lambert Co | NOUVELLES PYRAZOLO [4,3-e] DIAZEPINES SUBSTITUEES, COMPOSITIONS PHARMACEUTIQUES LES CONTENANT, UTILISATION A TITRE DE MEDICAMENT ET PROCEDES POUR LEUR PREPARATION |
| KR100358083B1 (ko) * | 2000-02-17 | 2002-10-25 | 에스케이케미칼주식회사 | 피롤로피리미디논 유도체와 이의 제조방법, 그리고 이의용도 |
| GB0113344D0 (en) * | 2001-06-01 | 2001-07-25 | Bayer Ag | Novel heterocycles 3 |
| BR0207215A (pt) * | 2001-12-13 | 2004-02-10 | Daiichi Suntory Pharma Co Ltd | Derivados de pirazolopiriminona tendo ação de inibição de pde7 |
-
2006
- 2006-09-28 AR ARP060104273A patent/AR058071A1/es not_active Application Discontinuation
- 2006-09-28 TW TW095135979A patent/TW200745106A/zh unknown
- 2006-09-29 UY UY29821A patent/UY29821A1/es not_active Application Discontinuation
- 2006-10-02 JP JP2008534481A patent/JP2009510159A/ja active Pending
- 2006-10-02 US US12/088,552 patent/US20090054413A1/en not_active Abandoned
- 2006-10-02 EP EP06799711A patent/EP1931672A1/en not_active Withdrawn
- 2006-10-02 WO PCT/SE2006/001111 patent/WO2007040435A1/en not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| US20090054413A1 (en) | 2009-02-26 |
| TW200745106A (en) | 2007-12-16 |
| UY29821A1 (es) | 2007-05-31 |
| JP2009510159A (ja) | 2009-03-12 |
| WO2007040435A1 (en) | 2007-04-12 |
| EP1931672A1 (en) | 2008-06-18 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR056536A1 (es) | Compuestos de 2-amino-5- [4-(difluormetoxi)fenil]-5-fenilimidazolona como inhibidores de la beta secretasa (bace) | |
| AR114064A2 (es) | Compuestos insecticidas basados en derivados de isoxazolina | |
| AR088029A1 (es) | Compuestos de pirimidina sustituidos, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento del dolor, accidentes cerebrovasculares, epilepsia y otras enfermedades del sistema nervioso central | |
| AR047538A1 (es) | Piridazinonas como antagonistas de las integrinas alfa4 | |
| ES2531256T3 (es) | Amidas fungicidas | |
| AR067945A1 (es) | Pirimidinas biciclicas fusionadas | |
| AR066492A1 (es) | Derivados de imidazoquinolina, proceso para su preparacion, composiciones farmaceuticas que los contienen y usos para el tratamiento de enfermedades virales, bacterianas, alergicas y distintos tipos de canceres. | |
| PE20130306A1 (es) | Morfolinopirimidinas y su uso en terapia | |
| AR072952A1 (es) | Compuestos de 2-imino-3-metilpirrolopirimidinona fenilo-sustituida como inhibidores de bace-1, composiciones y su uso | |
| AR054799A1 (es) | Derivados de oxindol | |
| AR074648A1 (es) | Derivados de isoxazolina que poseen un anillo de cuatro miembros como grupo terminal, intermediarios de sintesis, composiciones biocidas que los contienen y metodos para combatir y controlar dichas plagas | |
| PE20121506A1 (es) | Compuestos triazolopiridinas como inhibidores de c-met | |
| AR060046A1 (es) | Derivados de 2, 4-dioxo-1, 4-dihidropirido[2, 3 -d]pirimidina, un proceso para prepararlos e intermediario para su sintesis, una composicion farmaceutica que los comprende y su uso en la fabricacion de un medicamento para el tratamiento de enfermedades mediadas por pde4 | |
| AR065811A1 (es) | Derivados de 2-amino-4h-imidazol-4-ona,composiciones farmaceuticas que los contienen y usos para el tratamiento de la enfermedad de alzheimer y otros trastornos neurodegenerativos. | |
| AR052458A1 (es) | Amino-imidazolonas para la inhibicion de beta-secretasa | |
| AR068115A1 (es) | Derivado del acido pirazolcarboxilico metodo de produccion del mismo y fungicida | |
| PE20141042A1 (es) | Nuevos derivados biciclicos de dihidroquinolina-2-ona | |
| AR058010A1 (es) | Derivados biciclicos como inhibidores de p38 y composicion farmaceutica en base al compuesto | |
| AR059338A1 (es) | N-fenilbenzotriazolilo como inhibidores de c-kit | |
| AR041250A1 (es) | Derivados de sulfonamida como inhibidores de enzimas convertidoras de tnf-alfa | |
| PE20070218A1 (es) | COMPUESTOS DE CICLOALQUILO AMINO-HIDANTOINA Y USO DE ESTOS PARA LA MODULACION DE ß-SECRETASA | |
| EA200702497A1 (ru) | Замещенные арилпиразолы для применения против паразитов | |
| AR072047A1 (es) | Compuestos heterociclicos utiles para inhibir la adn girasa | |
| AR069813A1 (es) | Derivados de 2- amino-pirimidina, una composicion farmaceutica, un metodo de preparacion del compuesto y uso del mismo para preparar un medicamento | |
| AR079550A1 (es) | Derivados de pirazol |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |