AR064312A1 - Procedimientos para la preparacion de 3-(4-(2,4-difluorobenciloxi)-3-bromo-6-metil-2-oxopiridin-1(2h)-il)-n,4-dimetilbenzamida - Google Patents

Procedimientos para la preparacion de 3-(4-(2,4-difluorobenciloxi)-3-bromo-6-metil-2-oxopiridin-1(2h)-il)-n,4-dimetilbenzamida

Info

Publication number
AR064312A1
AR064312A1 ARP070105576A ARP070105576A AR064312A1 AR 064312 A1 AR064312 A1 AR 064312A1 AR P070105576 A ARP070105576 A AR P070105576A AR P070105576 A ARP070105576 A AR P070105576A AR 064312 A1 AR064312 A1 AR 064312A1
Authority
AR
Argentina
Prior art keywords
compound
formula
contacting
alkyl
produce
Prior art date
Application number
ARP070105576A
Other languages
English (en)
Inventor
G Klemm
R Vanderroest
B Chekal
M Mao
Embse R Vonder
R Geurnik
G Yalamanchili
R Valdyanathan
D Dukeshereer
Original Assignee
Pfizer Prod Inc
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 Pfizer Prod Inc filed Critical Pfizer Prod Inc
Publication of AR064312A1 publication Critical patent/AR064312A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/62Oxygen or sulfur atoms
    • C07D213/63One oxygen atom
    • C07D213/64One oxygen atom attached in position 2 or 6
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • A61K31/165Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/166Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4412Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/06Antiglaucoma agents or miotics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07Optical isomers

Abstract

Procedimientos para la preparacion de compuestos de la formula 1 en la que R2, R3, R4, R5, XI, X2, X3, X4, X5, X6 son como se definen en la memoria descriptiva. Reivindicacion 1: Un procedimiento caracterizado porque es para la preparacion de un compuesto de la formula 1, que comprende las etapas: a) poner en contacto un compuesto de la formula 5, con un reactivo de halogenacion en presencia de al menos un disolvente para producir un compuesto de la formula 4, b) poner en contacto un compuesto de la formula 4 con una hidrolasa en presencia de una solucion tampon para producir un compuesto de la formula 10, c) poner en contacto un compuesto de la formula 10 con un reactivo activante en presencia de al menos un disolvente y después poner en contacto la mezcla resultante con una amina para producir un compuesto de la formula 9; y d) poner en contacto un compuesto de la formula 9 con un haluro de bencilo sustituido en presencia de una base y al menos un disolvente para producir un compuesto de la formula 1; en el X1, X2, X3, X4, X5 y X6 son independientemente H, halo, o un alquilo C1-6; R1 es un alquilo C 1-6 o arilo; R2 es H, halo, o un alquilo C1-6; R3 es halo, o un alquilo C1-6; y R4 es H o un alquilo C1-6; R5 es H, un alquilo C1-6 o arilo; o R4, R5, y el nitrogeno al que están unidos forman un anillo morfolinilo, tiomorfolinilo, piperidinilo, pirrolidinilo, o piperazinilo que está opcionalmente sustituido con 1 o 2 grupos que son independientemente alquilo C1-4, alcoxi C1-4, hidroxi,.hidroxi-alquiIo C1-4,dihidroxi-alquilo C1-4, o halogeno. Reivindicacion 20: Un procedimiento para la preparacion de un compuesto de la formula 1 caracterizado porque tiene la siguiente estructura: que comprende las etapas: a) poner en contacto un compuesto de la formula 5 con 1,3-dibromo-5,5-dimetilhidantoína en presencia de acetonitrilo para producir un compuesto de la formula 4; b) poner en contacto un compuesto de la formula 4 con proteasa de Bacillus sp. En presencia de una solucion tampon de fosfato de potasio para producir un compuesto de la formula 10; c) poner en contacto un compuesto de la formula 10 con 1,1'-carbonildiimidazol en presencia de dimetilformamida y después se pone en contacto la mezcla resultante con NH2CH3 en tetrahidrofurano para producir un compuesto de la formula 9; y d) poner en contacto un compuesto de la formula 9 con un compuesto que tiene la estructura (1) en presencia de carbonato de potasio y N- metilpirrolidinona.
ARP070105576A 2006-12-13 2007-12-12 Procedimientos para la preparacion de 3-(4-(2,4-difluorobenciloxi)-3-bromo-6-metil-2-oxopiridin-1(2h)-il)-n,4-dimetilbenzamida AR064312A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US86974806P 2006-12-13 2006-12-13

Publications (1)

Publication Number Publication Date
AR064312A1 true AR064312A1 (es) 2009-03-25

Family

ID=39365911

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP070105576A AR064312A1 (es) 2006-12-13 2007-12-12 Procedimientos para la preparacion de 3-(4-(2,4-difluorobenciloxi)-3-bromo-6-metil-2-oxopiridin-1(2h)-il)-n,4-dimetilbenzamida

Country Status (17)

Country Link
US (1) US7906536B2 (es)
EP (1) EP2102161B1 (es)
JP (1) JP2008231090A (es)
KR (1) KR20090090379A (es)
CN (1) CN101611006A (es)
AR (1) AR064312A1 (es)
AT (1) ATE556055T1 (es)
AU (1) AU2007331199A1 (es)
BR (1) BRPI0720757A2 (es)
CA (1) CA2672256C (es)
IL (1) IL199239A0 (es)
MX (1) MX2009006266A (es)
NZ (1) NZ577639A (es)
RU (1) RU2411236C1 (es)
TW (1) TW200837057A (es)
WO (1) WO2008072079A2 (es)
ZA (1) ZA200903981B (es)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP5679159B2 (ja) * 2010-07-05 2015-03-04 信越化学工業株式会社 希土類金属抽出剤の合成方法、及び希土類金属の溶媒抽出用有機相
WO2014181213A1 (en) 2013-05-10 2014-11-13 Pfizer Inc. Crystalline form of (sa)-(-)-3-(3-bromo-4-((2,4-difluorobenzyl)oxy)-6-methyl-2-oxopyridin-1 (2h)-yl)-n,4-dimethylbenzamide
CA3128468A1 (en) 2017-10-05 2019-04-11 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce dux4 and downstream gene expression for the treatment of fshd
US10342786B2 (en) 2017-10-05 2019-07-09 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD
IL298694A (en) * 2019-10-18 2023-02-01 Fmc Corp Method for preparing 5-bromo-2-(3-chloro-pyridin-2-yl)-2H-pyrallose-3-carboxylic acid

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP3286645B2 (ja) * 1993-03-26 2002-05-27 メルシャン株式会社 光学活性1,4−ジヒドロピリジン誘導体およびその製造方法
GEP20063937B (en) * 2002-02-14 2006-10-10 Pharmacia Corp Substituted pyridinones as modulators of p38 map kinase
NL1026826C2 (nl) * 2003-08-13 2007-01-04 Pharmacia Corp Gesubstitueerde pyridinonen.
RU2007106863A (ru) * 2004-08-26 2008-08-27 Пфайзер Инк. (US) Энантиоселективное биопреобразование для получения промежуточных соединений ингибитора белка тирозинкиназы
JP2009526039A (ja) * 2006-02-10 2009-07-16 ファイザー・プロダクツ・インク ピリジノンピラゾール尿素およびピリミジノンピラゾール尿素誘導体

Also Published As

Publication number Publication date
MX2009006266A (es) 2009-06-22
KR20090090379A (ko) 2009-08-25
BRPI0720757A2 (pt) 2014-01-14
EP2102161A2 (en) 2009-09-23
TW200837057A (en) 2008-09-16
WO2008072079A3 (en) 2008-08-07
RU2411236C1 (ru) 2011-02-10
NZ577639A (en) 2012-01-12
CA2672256A1 (en) 2008-06-19
CN101611006A (zh) 2009-12-23
EP2102161B1 (en) 2012-05-02
ZA200903981B (en) 2010-08-25
JP2008231090A (ja) 2008-10-02
US7906536B2 (en) 2011-03-15
ATE556055T1 (de) 2012-05-15
CA2672256C (en) 2011-08-30
US20080177077A1 (en) 2008-07-24
WO2008072079A2 (en) 2008-06-19
IL199239A0 (en) 2010-03-28
AU2007331199A1 (en) 2008-06-19

Similar Documents

Publication Publication Date Title
AR064312A1 (es) Procedimientos para la preparacion de 3-(4-(2,4-difluorobenciloxi)-3-bromo-6-metil-2-oxopiridin-1(2h)-il)-n,4-dimetilbenzamida
ATE543807T1 (de) Verstärker von glutamat-rezeptoren
CO2021002382A2 (es) Nuevos compuestos heterocíclicos como inhibidores de la monoacilglicerol lipasa
BRPI0612888A8 (pt) anilino-piridinotriazinas cíclicas
PE20091623A1 (es) DERIVADOS DE 1H-PIRAZOLO[3,4-b]PIRIDINA COMO INHIBIDORES DE RAF QUINASA
RS50918B (sr) Novi estri fluorenkarbonske kiseline, postupak za njihovo pripremanje, kao i njihova upotreba kao lekova
ECSP045255A (es) Cumarinas utiles como biomarcadores
PE20070007A1 (es) Metodos para sintetizar derivados de 6-alquilaminoquinolina
DE602005013923D1 (de) Derivate von piperidinylalkylcarbamaten, herstellungsverfahren davon und verwendung derselben als faah-enzym-inhibitoren
DZ3493A1 (fr) N-(2-arylethyl)benzylamines comme antagonistes du recepteur 5-ht6
PE20120814A1 (es) Compuestos y composiciones como inhibidores de la proteina cinasa
SE0202465D0 (sv) New compounds
EA200970605A1 (ru) Ингибиторы mapk/erk-киназ
AR072016A1 (es) Derivados de isoxazol que funcionan como potenciadores de los receptores de glutamato
PE20050077A1 (es) Derivados de 4-pirrolidino-fenil-bencil-eter
PE20081174A1 (es) Inhibidores de metaloproteasas derivados de heterociclos
AR072431A1 (es) Procedimiento mejorado para la preparacion de 2-trifluormetil-5-(1-substituido)alquilpiridina
ATE441645T1 (de) Neue antibiotische derivate
CL2022000551A1 (es) Compuestos de 4,4a,5,7,8,8a-hexapirido[4,3-b][1,4]oxazin-3-ona como inhibidores de magl
EA200500528A1 (ru) Пиперазинил- и диазапанилбензамиды и бензтиоамиды
CY1111432T1 (el) Τετραϋδροκινολινες για χρηση ως διαμορφωτες της μιτοτικης κινητικης πρωτεϊνης eg5
PE20021003A1 (es) Fenil-heterociclil-eteres como inhibidores selectivos de la recaptacion de serotonina (ssri)
ATE517623T1 (de) Verwendung von methylphenidat-derivaten
CY1107193T1 (el) Παραγωγα πιπεραζινης και η χρηση τους ως αναστολεων της επανασυλληψης της σεροτονινης ή ως ανταγωνιστων της νευροκινινης
DE602005017122D1 (de) Derivate von heteroarylalkylcarbamaten, verfahren zu deren herstellung und deren verwendung als faah-enzyminhibitoren

Legal Events

Date Code Title Description
FB Suspension of granting procedure