AR050194A1 - Analogos de biaril piperazinil-piridina sustituidos - Google Patents
Analogos de biaril piperazinil-piridina sustituidosInfo
- Publication number
- AR050194A1 AR050194A1 ARP050103213A ARP050103213A AR050194A1 AR 050194 A1 AR050194 A1 AR 050194A1 AR P050103213 A ARP050103213 A AR P050103213A AR P050103213 A ARP050103213 A AR P050103213A AR 050194 A1 AR050194 A1 AR 050194A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- mono
- independently selected
- halogen
- amino
- Prior art date
Links
- 125000000217 alkyl group Chemical group 0.000 abstract 16
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 15
- 125000000623 heterocyclic group Chemical group 0.000 abstract 14
- 125000001424 substituent group Chemical group 0.000 abstract 11
- 229910052736 halogen Inorganic materials 0.000 abstract 10
- 150000002367 halogens Chemical class 0.000 abstract 10
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 abstract 8
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 7
- 229910052739 hydrogen Inorganic materials 0.000 abstract 7
- 239000001257 hydrogen Substances 0.000 abstract 7
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 6
- 125000001589 carboacyl group Chemical group 0.000 abstract 6
- 125000004043 oxo group Chemical group O=* 0.000 abstract 6
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 abstract 5
- 150000002431 hydrogen Chemical class 0.000 abstract 5
- -1 hydroxy, amino Chemical group 0.000 abstract 5
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 5
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 4
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 4
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 3
- 125000002837 carbocyclic group Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000003884 phenylalkyl group Chemical group 0.000 abstract 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 3
- 125000004400 (C1-C12) alkyl group Chemical group 0.000 abstract 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 2
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 abstract 2
- 125000006619 (C1-C6) dialkylamino group Chemical group 0.000 abstract 2
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 abstract 2
- 125000003342 alkenyl group Chemical group 0.000 abstract 2
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- 125000002947 alkylene group Chemical group 0.000 abstract 2
- 239000011230 binding agent Substances 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- 238000000034 method Methods 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 1
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 abstract 1
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 abstract 1
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 1
- 125000003161 (C1-C6) alkylene 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
- 125000006648 (C1-C8) haloalkyl group Chemical group 0.000 abstract 1
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 1
- 125000003341 7 membered heterocyclic group Chemical group 0.000 abstract 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 230000004913 activation Effects 0.000 abstract 1
- 125000004423 acyloxy group Chemical group 0.000 abstract 1
- 150000005215 alkyl ethers Chemical class 0.000 abstract 1
- 125000004414 alkyl thio group Chemical group 0.000 abstract 1
- 125000004103 aminoalkyl group Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 229910002091 carbon monoxide Inorganic materials 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 125000001841 imino group Chemical group [H]N=* 0.000 abstract 1
- 238000000338 in vitro Methods 0.000 abstract 1
- 238000001727 in vivo Methods 0.000 abstract 1
- 244000144972 livestock Species 0.000 abstract 1
- 230000004807 localization Effects 0.000 abstract 1
- 230000001575 pathological effect Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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- 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
- C07D405/14—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 three or more hetero rings
-
- 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
-
- 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
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/08—Bronchodilators
-
- 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
- A61P11/14—Antitussive agents
-
- 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
- A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
-
- 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
- A61P13/10—Drugs for disorders of the urinary system of the bladder
-
- 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
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- 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
- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
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- 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]
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- 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
- A61P3/04—Anorexiants; Antiobesity agents
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/42—One nitrogen atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/48—Two nitrogen atoms
-
- 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
- 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
- C07D401/14—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 three or more hetero rings
-
- 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
- C07D403/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
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- 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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pulmonology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Urology & Nephrology (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Obesity (AREA)
- Child & Adolescent Psychology (AREA)
- Hematology (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Dermatology (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Tales compuestos son ligantes que pueden utilizarse para modular la actividad de un receptor específico in vivo o in vitro, y que son particularmente utiles en el tratamiento de cuadros asociados con la activacion patologica de los receptores en seres humanos, animales domésticos y ganado. También se proporcionan las composiciones farmacéuticas y los métodos para usar dichos compuestos en el tratamiento de esos desordenes, así como métodos para usar dichos ligantes para estudios de localizacion de receptores. Reivindicacion 1: Un compuesto de la formula (1), o una sal farmacéuticamente aceptables del mismo, en donde: Ar2 es fenilo o un heterociclo aromático de 6 miembros, cada uno de los cuales está sustituido con desde 0 a 4 sustituyentes independientemente elegidos de R2; X, Y y Z son independientemente CRx o N, de tal modo que por lo menos uno de X, Y y Z es N; D, K, J y F son independientemente N, CH o carbono sustituido con un sustituyente representado por R1 o R10; Rx es elegido independientemente en cada caso entre hidrogeno, halogeno, alquilo C1-4, amino, ciano y mono- o di-(alquilC1-4)amino; R1 representa desde 0 a 3 sustituyentes elegidos independientemente entre: a) halogeno, ciano y nitro; b) grupos de la formula -Q-M-Ry; y c) grupos que se toman en forma conjunta con R10 para formar un anillo heterocíclico o carbocíclico de 5 a 7 miembros fusionados que está sustituido con desde 0 a 4 sustituyentes elegidos independientemente entre halogeno, ciano, nitro y grupos de la formula -Q-M-Ry; R10 representa un sustituyente elegido entre: a) grupos de la formula -Q-M-Ry; y b) grupos que se toman en forma conjunta con un R1 para formar un anillo heterocíclico o carbocíclico de 5 a 7 miembros opcionalmente sustituidos, fusionados; de tal modo que R10 no es hidroxi, amino ni un grupo no sustituido elegido entre: alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alcoxi C1-6, alquilC2-6éter, alcanoilo C2-6, alcanona C3-6, haloalquilo C1-6, haloalcoxi C1-6, mono- o di-(alquil C1-6)amino, alquilC1-6-sulfonilo, mono- o di-(alquil C1-6)aminosulfonilo o mono- o di-(alquil C1-6)aminocarbonilo; cada Q es independientemente elegido entre alquileno C0-4; cada M está independientemente ausente o seleccionado entre 0, C(=O), OC(=O), C(=O)O, O-C(=O)O, S(O)m, N(Rz), C(=O)N(Rz), C(=NH)N(Rz), N(Rz)C(=O), N(Rz)C(=NH), N(Rz)S(O)m, S(O)mN(Rz) y N[S(O)mN(Rz)]S(O)m; en donde m es independientemente seleccionado en cada caso entre 0, 1 y 2; y Rz es independientemente seleccionado en cada caso entre hidrogeno, alquilo C1-8 y grupos que se toman junto con Ry para formar un heterociclo de 4 a 7 miembros opcionalmente sustituido; y cada Ry es independientemente hidrogeno, haloalquilo C1-8, alquilo C1-8, carbocicloC3-8alquiloC0-4, heterociclo de 4 a 7 miembros)alquiloC0-4, o se toma en forma conjunta con Rz para formar un heterociclo de 4 a 7 miembros en donde cada alquilo, carbociclo y heterociclo está sustituido con desde 0 a 4 sustituyentes independientemente seleccionados entre hidroxi, halogeno, amino, ciano, nitro, oxo, -COOH, aminocarbonilo, aminosulfonilo, alquilo C1-6, cicloalquilo C3-7, alquiloC2-6éter, alcanoilo C1-6, alquilC1-6-sulfonilo, alcoxi C1-8, alquiltio C1-8, mono- y di-(alquil C1-6)aminocarbonilo, mono- y di-(alquil C1-6)aminosulfonilo, mono- y di(alquil C1-6)amino y fenilo; de tal modo que Ry no es hidrogeno si Q es alquilo C0 y si M está ausente; cada R2 es: a) independientemente elegido entre i) hidroxi, amino, ciano, halogeno, -COOH, aminosulfonilo, nitro y aminocarbonilo; y ii) alquilo C1-6, cicloalquilC3-8alquiloC0-4, haloalquilo C1-6, alcoxi C1-6, alquiltio C1-6, alquilC2-6éter, alcanoilo C2-6, alcoxiC1-6-carbonilo, alcanoiloxi C2-6, alcanona C3- 6, mono- y di-(alquil C1-6)aminoalquilC0-6, (heterociclo de 4 a 7 miembros)alquiloC0-4, alquilC1-6-sulfonilo, mono- y di-(alquil C1-6)aminosulfonilo, y mono- y di-(alquil C1-6)aminocarbonilo, cada uno de los cuales está sustituido con desde 0 a 4 sustituyentes independientemente elegidos entre halogeno, hidroxi, ciano, amino, aminocarbonilo, aminosulfonilo, -COOH y oxo; o b) tomado junto con un R2 adyacente para formar un grupo heterocíclico o carbocíclico de 5 a 13 miembros fusionados que está sustituido con desde 0 a 3 sustituyentes independientemente elegidos entre halogeno, oxo y alquilo C1-6; R3 está seleccionado entre: i) hidrogeno y halogeno; ii) alquilo C1-6, cicloalquilC3-8alquiloC0-2, haloalquilo C1-6 y fenialquilo C0-2; y iii) grupos de la formula (2), en donde: L es alquileno C0-6 o alquileno C1-6 que está tomado junto con R5, R6 o R7 para formar un heterociclo de 4 a 7 miembros; W es O, CO, S, SO o SO2; R5 y R6 están: a) independientemente elegidos entre hidrogeno, alquilo C1-12, alquenilo C2-12, cicloalquilC3-8alquiloC0-4, alcanoilo C2-6, alquilC1-6-sulfonilo, fenilalquilo C0-6, (heterociclo de 4 a 7 miembros)alquiloC0-6 y grupos que están unidos a L para formar un heterociclo de 4 a 7 miembros; o b) unidos para formar un heterociclo de 4 a 12 miembros; y R7 es hidrogeno, alquilo C1-12, alquenilo C2-12, cicloalquilC3-8alquiloC1-4, alcanoilo C2-6, fenilalquilo C0-6, (heterociclo de 4 a 7 miembros)alquilo C0-6 o un grupo que está unido a L para formar un heterociclo de 4 a7 miembros; en donde cada uno de ii) y iii) está opcionalmente sustituido con desde 0 a 4 sustituyentes independientemente elegidos entre: a) halogeno, hidroxi, amino, ciano, nitro, -COOH, aminosulfonilo, aminocarbonilo y oxo; y b) alquilo C1-6, cicloalquilC3-8alquiloC0-2, haloalquilo C1-6, alcoxi C1-6, alcanoilo C1-6, alcoxiC1-6-carbonilo, alcanoilC2-6-amino, mono- y di-(alquilC1-6)aminoalquiloC0-4, alquilC1-6sulfonilo, mono- y di-(alquil C1-6)aminosulfonilo, mono- y di- (alquilC1-6)aminocarbonilalquiloC0-4, fenilalquilo C0-4 y (heterociclo de 4 a 7 miembros)alquiloC0-4, cada uno de los cuales está sustituido con desde 0 a 4 sustituyentes secundarios independientemente elegidos entre halogeno, hidroxi, ciano, oxo, imino, alquilo C1-4, alcoxi C1-4 y haloalquilo C1-4; y R4 representa desde 0 a 2 sustituyentes elegidos independientemente entre alquilo C1-3, haloalquilo C1-3 y oxo.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US60172104P | 2004-08-13 | 2004-08-13 | |
| US64179605P | 2005-01-05 | 2005-01-05 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR050194A1 true AR050194A1 (es) | 2006-10-04 |
Family
ID=36000525
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP050103213A AR050194A1 (es) | 2004-08-13 | 2005-08-02 | Analogos de biaril piperazinil-piridina sustituidos |
Country Status (24)
| Country | Link |
|---|---|
| US (2) | US7662830B2 (es) |
| EP (1) | EP1786800B1 (es) |
| JP (1) | JP4955554B2 (es) |
| KR (1) | KR20070046924A (es) |
| CN (1) | CN101014587B (es) |
| AR (1) | AR050194A1 (es) |
| BR (1) | BRPI0514319A (es) |
| CA (1) | CA2577301C (es) |
| CR (1) | CR8992A (es) |
| EC (1) | ECSP077318A (es) |
| HN (1) | HN2007006799A (es) |
| IL (1) | IL181040A0 (es) |
| MA (1) | MA28857B1 (es) |
| MX (1) | MX2007001696A (es) |
| MY (1) | MY145822A (es) |
| NI (1) | NI200700040A (es) |
| NO (1) | NO20071243L (es) |
| NZ (1) | NZ553388A (es) |
| PE (1) | PE20060620A1 (es) |
| RU (1) | RU2413726C2 (es) |
| SG (1) | SG157399A1 (es) |
| TW (1) | TW200605889A (es) |
| WO (1) | WO2006026135A2 (es) |
| ZA (1) | ZA200701530B (es) |
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| US20030176437A1 (en) | 2001-08-31 | 2003-09-18 | D.M. Watterson | Anti-inflammatory and protein kinase inhibitor compositions and related methods for downregulation of detrimental cellular responses and inhibition of cell death |
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| MY145822A (en) * | 2004-08-13 | 2012-04-30 | Neurogen Corp | Substituted biaryl piperazinyl-pyridine analogues |
| EP1812007B1 (en) | 2004-11-02 | 2011-09-07 | Northwestern University | Pyridazine compounds and methods |
| WO2006050389A2 (en) | 2004-11-02 | 2006-05-11 | Northwestern University | Pyridazine compounds, compositions and methods |
| AU2005317176A1 (en) * | 2004-12-13 | 2006-06-22 | Neurogen Corporation | Piperazinyl-pyridine analogues |
| WO2006078992A2 (en) * | 2005-01-19 | 2006-07-27 | Neurogen Corporation | Heteroaryl substituted piperazinyl-pyridine analogues |
| WO2007127474A2 (en) | 2006-04-28 | 2007-11-08 | Northwestern University | Compositions and treatments using pyridazine compounds and cholinesterase inhibitors |
| WO2007127375A2 (en) * | 2006-04-28 | 2007-11-08 | Northwestern University | Formulations containing pyridazine compounds for treating neuroinflammatory diseases |
| US20080153845A1 (en) * | 2006-10-27 | 2008-06-26 | Redpoint Bio Corporation | Trpv1 antagonists and uses thereof |
| TWI362930B (en) * | 2007-04-27 | 2012-05-01 | Purdue Pharma Lp | Trpv1 antagonists and uses thereof |
| US8343966B2 (en) * | 2008-01-11 | 2013-01-01 | Novartis Ag | Organic compounds |
| AU2012225382B2 (en) * | 2011-03-09 | 2016-10-27 | Celgene Avilomics Research, Inc. | PI3 kinase inhibitors and uses thereof |
| ES2390326B1 (es) * | 2011-04-05 | 2013-08-14 | Universidad Miguel Hernández De Elche | Antagonistas de trpv1 y sus usos. |
| GEP20166432B (en) | 2011-09-27 | 2016-02-10 | Novartis Ag | 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant idh |
| JP6129199B2 (ja) * | 2011-12-02 | 2017-05-17 | 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 | ピペリジン誘導体、その医薬組成物及び使用 |
| UY34632A (es) | 2012-02-24 | 2013-05-31 | Novartis Ag | Compuestos de oxazolidin- 2- ona y usos de los mismos |
| US9296733B2 (en) | 2012-11-12 | 2016-03-29 | Novartis Ag | Oxazolidin-2-one-pyrimidine derivative and use thereof for the treatment of conditions, diseases and disorders dependent upon PI3 kinases |
| WO2014141104A1 (en) | 2013-03-14 | 2014-09-18 | Novartis Ag | 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant idh |
| EA027732B1 (ru) | 2013-07-30 | 2017-08-31 | Янссен Сайенсиз Айрлэнд Юси | Замещенные аналоги пиридина-пиперазинила в качестве противовирусных соединений против rsv |
| CN115060832B (zh) * | 2022-08-18 | 2022-11-29 | 上海奥科达生物医药科技有限公司 | 奥卡西平口服混悬液中奥卡西平及防腐剂含量检测方法 |
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| FR2262512A1 (en) | 1974-03-01 | 1975-09-26 | Synthelabo | 2,4,6-Tri-substd. -1,3,5-triazines - with analgesic and psychotropic activity |
| DE2643753A1 (de) | 1976-09-29 | 1978-04-06 | Thomae Gmbh Dr K | Neue 1h-pyrazolo eckige klammer auf 3,4-b eckige klammer zu pyridine |
| FI70411C (fi) * | 1980-12-29 | 1986-09-19 | Pfizer | Foerfarande foer framstaellning av nya antihypertensiva 4-amino-6,7-dimetoxi-2-piperazinokinazolin derivat |
| DE3609596A1 (de) * | 1986-03-21 | 1987-10-01 | Hoechst Ag | 2-azolylmethyl-2-aryl-1,3-dioxolane und deren salze, verfahren zu ihrer herstellung, sie enthaltende mittel und ihre verwendung |
| GB9012311D0 (en) | 1990-06-01 | 1990-07-18 | Wellcome Found | Pharmacologically active cns compounds |
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| AU703263B2 (en) | 1994-08-08 | 1999-03-25 | Nippon Shinyaku Co. Ltd. | Triazine derivative and medicine |
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| JP2002514195A (ja) | 1996-12-05 | 2002-05-14 | アムジエン・インコーポレーテツド | 置換ピリミジン化合物およびそれの使用 |
| ATE274510T1 (de) | 1998-06-19 | 2004-09-15 | Chiron Corp | Glycogen synthase kinase 3 inhibitoren |
| DE19836697A1 (de) | 1998-08-13 | 2000-02-17 | Hoechst Marion Roussel De Gmbh | Substituierte 4-Amino-2-aryl-pyrimidine, ihre Herstellung, ihre Verwendung und sie enthaltende pharmazeutische Präparate |
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| EP1136483A1 (en) | 2000-03-23 | 2001-09-26 | Sanofi-Synthelabo | 2-[Piperazinyl]pyrimidone derivatives |
| AU2001262150A1 (en) | 2000-03-23 | 2001-10-03 | Mitsubishi Pharma Corporation | 2-(nitrogen-heterocyclic)pyrimidone derivatives |
| AU2001268718B2 (en) * | 2000-06-29 | 2006-01-05 | Abbott Laboratories | Aryl phenylheterocyclyl sulfide derivatives and their use as cell adhesion-inhibiting anti-inflammatory and immune-suppressive agents |
| JP2004525071A (ja) | 2000-07-20 | 2004-08-19 | ニューロジェン コーポレイション | カプサイシン受容体リガンド |
| US6710058B2 (en) | 2000-11-06 | 2004-03-23 | Bristol-Myers Squibb Pharma Company | Monocyclic or bicyclic carbocycles and heterocycles as factor Xa inhibitors |
| EP1247809A3 (en) | 2001-03-30 | 2003-12-17 | Pfizer Products Inc. | Triazine compounds useful as sorbitol dehydrogenase inhibitors |
| WO2002098864A1 (en) | 2001-06-01 | 2002-12-12 | F. Hoffmann-La Roche Ag | Pyrimidine, triazine and pyrazine derivatives as glutamate receptors |
| AU2003245669A1 (en) | 2002-06-21 | 2004-01-06 | Cellular Genomics, Inc. | Certain aromatic monocycles as kinase modulators |
| EP2316831B1 (en) | 2002-11-21 | 2013-03-06 | Novartis AG | 2-(morpholin-4-yl)pyrimidines as phosphotidylinositol (PI) 3-kinase inhibitors and their use in the treatment of cancer |
| CN1820001A (zh) | 2003-07-10 | 2006-08-16 | 神经能质公司 | 经取代的杂环二芳基胺类似物 |
| EP1644358A2 (en) | 2003-07-16 | 2006-04-12 | Neurogen Corporation | Biaryl piperazinyl-pyridine analogues |
| CN1826328A (zh) | 2003-07-22 | 2006-08-30 | 神经能质公司 | 经取代的吡啶－2－基胺类似物 |
| MY145822A (en) * | 2004-08-13 | 2012-04-30 | Neurogen Corp | Substituted biaryl piperazinyl-pyridine analogues |
| AU2005317176A1 (en) | 2004-12-13 | 2006-06-22 | Neurogen Corporation | Piperazinyl-pyridine analogues |
| WO2006078992A2 (en) | 2005-01-19 | 2006-07-27 | Neurogen Corporation | Heteroaryl substituted piperazinyl-pyridine analogues |
| US8258143B2 (en) * | 2006-06-28 | 2012-09-04 | Duquesne University Of The Holy Ghost | Methods of using substituted pyrrolo[2,3-d]pyrimidines for targeting tumor cells and treating cancer |
-
2005
- 2005-06-22 MY MYPI20052848A patent/MY145822A/en unknown
- 2005-07-01 TW TW094122269A patent/TW200605889A/zh unknown
- 2005-08-02 AR ARP050103213A patent/AR050194A1/es unknown
- 2005-08-11 PE PE2005000929A patent/PE20060620A1/es not_active Application Discontinuation
- 2005-08-13 BR BRPI0514319-5A patent/BRPI0514319A/pt not_active IP Right Cessation
- 2005-08-13 KR KR1020077005831A patent/KR20070046924A/ko not_active Ceased
- 2005-08-13 CN CN2005800275501A patent/CN101014587B/zh not_active Expired - Fee Related
- 2005-08-13 JP JP2007525874A patent/JP4955554B2/ja not_active Expired - Fee Related
- 2005-08-13 NZ NZ553388A patent/NZ553388A/en unknown
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- 2005-08-13 US US11/204,202 patent/US7662830B2/en active Active
- 2005-08-13 ZA ZA200701530A patent/ZA200701530B/xx unknown
- 2005-08-13 EP EP05810146.0A patent/EP1786800B1/en not_active Expired - Lifetime
- 2005-08-13 MX MX2007001696A patent/MX2007001696A/es not_active Application Discontinuation
- 2005-08-13 SG SG200907610-0A patent/SG157399A1/en unknown
- 2005-08-13 WO PCT/US2005/028969 patent/WO2006026135A2/en not_active Ceased
- 2005-08-13 RU RU2007106042/04A patent/RU2413726C2/ru not_active IP Right Cessation
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2007
- 2007-01-29 IL IL181040A patent/IL181040A0/en unknown
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- 2007-03-07 NO NO20071243A patent/NO20071243L/no not_active Application Discontinuation
- 2007-03-13 CR CR8992A patent/CR8992A/es not_active Application Discontinuation
- 2007-03-13 MA MA29749A patent/MA28857B1/fr unknown
- 2007-03-13 EC EC2007007318A patent/ECSP077318A/es unknown
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2010
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