Nothing Special   »   [go: up one dir, main page]

AR050194A1 - Analogos de biaril piperazinil-piridina sustituidos - Google Patents

Analogos de biaril piperazinil-piridina sustituidos

Info

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
Application number
ARP050103213A
Other languages
English (en)
Original Assignee
Neurogen Corp
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Neurogen Corp filed Critical Neurogen Corp
Publication of AR050194A1 publication Critical patent/AR050194A1/es

Links

Classifications

    • 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
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • 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)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Diabetes (AREA)
  • Child & Adolescent Psychology (AREA)
  • Dermatology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (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.
ARP050103213A 2004-08-13 2005-08-02 Analogos de biaril piperazinil-piridina sustituidos AR050194A1 (es)

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)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1430033A4 (en) 2001-08-31 2004-12-15 Univ Northwestern PROTEIN KINASE ANTI-INFLAMMATORY AND INHIBITOR COMPOSITION AND METHOD OF USE
WO2005007648A2 (en) * 2003-07-16 2005-01-27 Neurogen Corporation Biaryl piperazinyl-pyridine analogues
MY145822A (en) * 2004-08-13 2012-04-30 Neurogen Corp Substituted biaryl piperazinyl-pyridine analogues
EP1812408B1 (en) 2004-11-02 2013-10-09 Northwestern University Pyridazine compounds, compositions and methods
WO2006050359A2 (en) 2004-11-02 2006-05-11 Northwestern University Pyridazine compounds and methods
CA2590299A1 (en) * 2004-12-13 2006-06-22 Neurogen Corporation Piperazinyl-pyridine analogues
JP2008528506A (ja) * 2005-01-19 2008-07-31 ニューロジェン・コーポレーション ヘテロアリール置換ピペラジニル−ピリジン類縁体
US8158627B2 (en) 2006-04-28 2012-04-17 Northwestern University Compositions and treatments using pyridazine compounds and cholinesterase inhibitors
AU2007243280A1 (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
EP2604598B1 (en) * 2007-04-27 2016-04-06 Purdue Pharma L.P. TRPV1 antagonists and uses thereof
US8343966B2 (en) * 2008-01-11 2013-01-01 Novartis Ag Organic compounds
CN103501610A (zh) * 2011-03-09 2014-01-08 西建阿维拉米斯研究公司 Pi3激酶抑制剂和其用途
ES2390326B1 (es) * 2011-04-05 2013-08-14 Universidad Miguel Hernández De Elche Antagonistas de trpv1 y sus usos.
EA025183B1 (ru) 2011-09-27 2016-11-30 Новартис Аг 3-пиримидин-4-ил-оксазолидин-2-оны в качестве ингибиторов мутантной 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
CN105263929B (zh) 2013-03-14 2018-08-28 诺华股份有限公司 作为突变idh抑制剂的3-嘧啶-4-基-噁唑烷-2-酮化合物
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

Family Cites Families (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS4921148B1 (es) * 1970-12-28 1974-05-30
US3775326A (en) 1972-04-17 1973-11-27 Addressograph Multigraph Pressure fixable electroscopic printing powder
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
KR930702312A (ko) 1990-08-31 1993-09-08 아만 히데아키 피리미딘 유도체 및 의약
RU2147233C1 (ru) 1994-08-08 2000-04-10 Ниппон Синяку Ко., Лтд. Лекарственные композиции и производные триазина
US5962453A (en) 1995-08-08 1999-10-05 Nippon Shinyaku Co. Ltd. Triazine derivative and medicine
AR038955A1 (es) 1996-12-05 2005-02-02 Amgen Inc Compuestos de pirimidinona y piridona sustituidos y metodos para su uso
DE69919707T2 (de) 1998-06-19 2005-09-01 Chiron Corp., Emeryville 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
OA11856A (en) 1999-04-01 2006-03-03 Pfizer Prod Inc Aminopyrimidines as sorbitol dehydrogenase inhibitors.
AU2001262150A1 (en) * 2000-03-23 2001-10-03 Mitsubishi Pharma Corporation 2-(nitrogen-heterocyclic)pyrimidone derivatives
EP1136483A1 (en) 2000-03-23 2001-09-26 Sanofi-Synthelabo 2-[Piperazinyl]pyrimidone derivatives
CA2414461A1 (en) 2000-06-29 2002-01-10 Abbott Laboratories Aryl phenylheterocyclyl sulfide derivatives and their use as cell adhesion-inhibiting anti-inflammatory and immune-suppressive agents
KR20030024799A (ko) * 2000-07-20 2003-03-26 뉴로젠 코포레이션 캡사이신 수용체 리간드
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
JP4049742B2 (ja) 2001-06-01 2008-02-20 エフ．ホフマン−ラ ロシュ アーゲー グルタミン酸受容体としてのピリミジン、トリアジン及びピラジン誘導体
AU2003245669A1 (en) 2002-06-21 2004-01-06 Cellular Genomics, Inc. Certain aromatic monocycles as kinase modulators
ES2412273T3 (es) * 2002-11-21 2013-07-10 Novartis Ag Inhibidores de 2-morfolín-4-pirimidinas como inhibidores de fosfotidilinositol (PI) 3-quinasa y su uso en el tratamiento del cáncer.
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
WO2005007648A2 (en) * 2003-07-16 2005-01-27 Neurogen Corporation Biaryl piperazinyl-pyridine analogues
AU2004259346A1 (en) 2003-07-22 2005-02-03 Neurogen Corporation Substituted pyridin-2-ylamine analogues
MY145822A (en) * 2004-08-13 2012-04-30 Neurogen Corp Substituted biaryl piperazinyl-pyridine analogues
CA2590299A1 (en) 2004-12-13 2006-06-22 Neurogen Corporation Piperazinyl-pyridine analogues
JP2008528506A (ja) 2005-01-19 2008-07-31 ニューロジェン・コーポレーション ヘテロアリール置換ピペラジニル−ピリジン類縁体
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

Also Published As

Publication number Publication date
EP1786800A2 (en) 2007-05-23
ZA200701530B (en) 2008-11-26
EP1786800B1 (en) 2017-01-04
WO2006026135A2 (en) 2006-03-09
US8334382B2 (en) 2012-12-18
EP1786800A4 (en) 2009-05-06
MA28857B1 (fr) 2007-09-03
NZ553388A (en) 2011-01-28
CR8992A (es) 2007-08-14
JP4955554B2 (ja) 2012-06-20
US20060122394A1 (en) 2006-06-08
MY145822A (en) 2012-04-30
CA2577301C (en) 2014-05-27
US20110003813A1 (en) 2011-01-06
NO20071243L (no) 2007-04-27
ECSP077318A (es) 2007-04-26
RU2413726C2 (ru) 2011-03-10
SG157399A1 (en) 2009-12-29
JP2008509932A (ja) 2008-04-03
NI200700040A (es) 2008-04-01
TW200605889A (en) 2006-02-16
KR20070046924A (ko) 2007-05-03
MX2007001696A (es) 2007-04-23
US7662830B2 (en) 2010-02-16
BRPI0514319A (pt) 2008-06-10
AU2005280366A1 (en) 2006-03-09
IL181040A0 (en) 2007-07-04
HN2007006799A (es) 2010-11-03
CA2577301A1 (en) 2006-03-09
RU2007106042A (ru) 2008-09-20
CN101014587B (zh) 2013-12-18
PE20060620A1 (es) 2006-08-11
WO2006026135A3 (en) 2006-06-15
CN101014587A (zh) 2007-08-08

Similar Documents

Publication Publication Date Title
AR050194A1 (es) Analogos de biaril piperazinil-piridina sustituidos
AR053712A1 (es) Heteroarilos sustituidos, antagonistas de cb1 (receptor 1 canabinoide)
CO5700774A2 (es) Derivados de triazol como inhibidores de 11-beta-hidroxiesteroide deshidrogenasa-1
AR063311A1 (es) Compuestos organicos
AR054130A1 (es) Procedimiento para la preparacion de 1-alquil-3-feniluracilos
CO5601012A2 (es) Compuestos que modulan la actividad de ppar
PE20090509A1 (es) El uso de derivados de benzamida para el tratamiento de transtornos del snc
AR023060A1 (es) Uso de un compuesto que es un derivado de 2-ureido-1,3-tiazol, nuevos derivados de 2-ureido-1,3-tiazol, procedimientos para prepararlos y composicionesfarmaceuticas que los comprenden
AR038341A1 (es) Compuestos que son agonistas de receptores alfa-1 preferentemente agonistas de receptores alfa-1a/l
AR063335A1 (es) Derivados de 4- (2- amino-1- hidroxietil) fenol como agonistas del receptor beta 2 adrenergico
AR073406A1 (es) Aminodihidrotiazinas fusionadas con tetrahidropiranos,inhibidoras de bace1 y de la produccion de abeta amiloide, composiciones farmaceuticas que las contienen y usos de las mismas para el tratamiento de enfermedades neurodegenerativas,tales como alzheimer.
AR066169A1 (es) Derivados de benzo-imidazoles, utiles para trastornos asociados con la actividad de dgat
AR054799A1 (es) Derivados de oxindol
AR073530A1 (es) Inhibidores de janus quinasas para el tratamiento de ojo seco y otras enfermedades relacionadas con los ojos. inserto oftalmico
AR044519A1 (es) Derivados de piridin-tiazol amina y de pirimidin-tiazol amina
AR043014A1 (es) Amino-1,3,5-triazinas n-sustituidas con radicales biciclicos quirales, procedimiento para su preparacion, composiciones de las mismas, y su uso como herbicidas y reguladores del crecimiento de las plantas
AR033379A1 (es) Compuestos de difenilurea, procedimiento para su preparacion y composiciones farmaceuticas que los contienen
AR052568A1 (es) Derivados de pirazolo -pirimidina como antagonstas de mglur2
AR054783A1 (es) Derivados de pirrolo-quinolinas moduladores selectivos de receptores de androgeno
AR030243A1 (es) Carboxamidas heterociclicas, composiciones farmaceuticas, uso de las mismas para la manufactura de un medicamento antiviral y metodo in vitro para inhibir el adn polimerasa viral
AR040333A1 (es) Uso de derivados de ciclotiocarbamatos en el tratamiento de condiciones relacionadas con hormonas
AR060268A1 (es) Tiazolil - dihidro - indazoles
CO6351734A2 (es) Compuestos de amida utiles en terapia
AR060267A1 (es) Tiazolil- dihidro -ciclopentapirazoles
AR065583A1 (es) Compuestos macrociclicos y composicion farmaceutica

Legal Events

Date Code Title Description
FB Suspension of granting procedure