PE20130318A1 - Nuevos procesos - Google Patents

Nuevos procesos

Info

Publication number
PE20130318A1
PE20130318A1 PE2012002160A PE2012002160A PE20130318A1 PE 20130318 A1 PE20130318 A1 PE 20130318A1 PE 2012002160 A PE2012002160 A PE 2012002160A PE 2012002160 A PE2012002160 A PE 2012002160A PE 20130318 A1 PE20130318 A1 PE 20130318A1
Authority
PE
Peru
Prior art keywords
alkyl
compound
treating
phenyl
het
Prior art date
Application number
PE2012002160A
Other languages
English (en)
Inventor
Kevin Stuart Cardwell
Claire Frances Crawford
Suzanne Helen Davies
Charles Edward Wade
Original Assignee
Glaxo Group Ltd
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=44992024&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20130318(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Glaxo Group Ltd filed Critical Glaxo Group Ltd
Publication of PE20130318A1 publication Critical patent/PE20130318A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • 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
    • A61P9/10—Drugs 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C227/00—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C227/04—Formation of amino groups in compounds containing carboxyl groups
    • C07C227/06—Formation of amino groups in compounds containing carboxyl groups by addition or substitution reactions, without increasing the number of carbon atoms in the carbon skeleton of the acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C227/00—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C227/04—Formation of amino groups in compounds containing carboxyl groups
    • C07C227/06—Formation of amino groups in compounds containing carboxyl groups by addition or substitution reactions, without increasing the number of carbon atoms in the carbon skeleton of the acid
    • C07C227/08—Formation of amino groups in compounds containing carboxyl groups by addition or substitution reactions, without increasing the number of carbon atoms in the carbon skeleton of the acid by reaction of ammonia or amines with acids containing functional groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C229/04—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C229/06—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton
    • C07C229/10—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings
    • C07C229/16—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings to carbon atoms of hydrocarbon radicals substituted by amino or carboxyl groups, e.g. ethylenediamine-tetra-acetic acid, iminodiacetic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/46—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino or carboxyl groups bound to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
    • C07C229/48—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino or carboxyl groups bound to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups and carboxyl groups bound to carbon atoms of the same non-condensed ring

Abstract

SE REFIERE A UN PROCESO PARA LA OBTENCION DEL COMPUESTO DE FORMULA (I) DONDE: R1 ES FENILO CON UNO O MAS GRUPOS F; R2 ES ALQUILO C1-C3 OPCIONALMENTE SUSTITUIDO, HET-ALQUILO C0-C2, ENTRE OTROS; R3 ES FENILO; R4 ES FENILO OPCIONALMENTE SUSTITUIDO CON ALQUILO C1-C6 O DE MONO A PERFLUORO-ALQUILO C1-C4; Ra Y Rb FORMAN JUNTO A LOS ATOMOS DE CARBONO A LOS QUE ESTAN UNIDOS UN ANILLO DE CICLOPENTILO; HET ES UN ANILLO HETEROCICLICO C5-C7 CON UN ATOMO DE N OPCIONALMENTE SUSTITUIDO CON ALQUILO C1-C6. DICHO PROCESO COMPRENDE: (i) TRATAR UN 2-OXOCICLOPENTANOCARBOXILATO DE ALQUILO C1-C4 CON UNA SAL DE METAL ALCALINO DE GLICINA PARA OBTENER UN COMPUESTO; (ii) CICLAR EL COMPUESTO OBTENIDO; (iii) TRATAR EL NUEVO COMPUESTO RESULTANTE DE (ii) CON UN REACTIVO DE TIOALQUILACION PARA FORMAR UN ACIDO (TIO-4-OXO-4,5,6,7-TETRAHIDRO-1H-CICLOPENTA[d]PIRIMIDIN-1-IL)ACETICO; (iv) TRATAR UN ALDEHIDO CON UNA AMINA EN PRESENCIA DE UNA CATALIZADOR DE METALES PESADOS E HIDROGENO PARA LA FORMACION DE LA AMINA SECUNDARIA ; (v) TRATAR EL COMPUESTO OBTENIDO EN (iii) CON LA AMIDA SECUNDARIA PARA LA OBTENCION DEL COMPUESTO (I). DICHO PROCESO PARA LA OBTENCION DE COMPUESTOS DE PIRIMIDINONA PRESENTA UN MAYOR RENDIMIENTO DEL COMPUESTO (I) QUE ES UTIL EN EL TRATAMIENTO DE ATEROESCLEROSIS.
PE2012002160A 2010-05-17 2011-05-17 Nuevos procesos PE20130318A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US34522410P 2010-05-17 2010-05-17

Publications (1)

Publication Number Publication Date
PE20130318A1 true PE20130318A1 (es) 2013-04-11

Family

ID=44992024

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2012002160A PE20130318A1 (es) 2010-05-17 2011-05-17 Nuevos procesos

Country Status (24)

Country Link
US (2) US9447052B2 (es)
EP (1) EP2571857B1 (es)
JP (1) JP6027529B2 (es)
KR (1) KR20130089157A (es)
CN (2) CN103003249B (es)
AR (1) AR081399A1 (es)
AU (1) AU2011256270B2 (es)
BR (1) BR112012030532A2 (es)
CA (1) CA2799520C (es)
CL (1) CL2012003206A1 (es)
CO (1) CO6630197A2 (es)
CR (1) CR20120630A (es)
DO (1) DOP2012000289A (es)
EA (1) EA026569B1 (es)
IL (1) IL223068A0 (es)
MA (1) MA34301B1 (es)
MX (1) MX2012013387A (es)
NZ (1) NZ603672A (es)
PE (1) PE20130318A1 (es)
SG (1) SG185559A1 (es)
TW (1) TW201209043A (es)
UY (1) UY33388A (es)
WO (1) WO2011146494A1 (es)
ZA (1) ZA201208631B (es)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW201209043A (en) * 2010-05-17 2012-03-01 Glaxo Group Ltd Novel processes
WO2015087239A1 (en) 2013-12-11 2015-06-18 Ranbaxy Laboratories Limited Processes for the preparation of darapladib and its intermediates
WO2015092687A2 (en) 2013-12-17 2015-06-25 Ranbaxy Laboratories Limited Process for the purification of darapladib
WO2019063634A1 (en) 2017-09-26 2019-04-04 INSERM (Institut National de la Santé et de la Recherche Médicale) DARAPLADIB RADIOMARQUÉ, ITS ANALOGUES AND THEIR USE AS IMAGING COMPOUNDS
US10866963B2 (en) * 2017-12-28 2020-12-15 Dropbox, Inc. File system authentication

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1143516B (de) 1961-04-27 1963-02-14 Bayer Ag Verfahren zur Herstellung von Peptiden
US4277465A (en) 1978-08-26 1981-07-07 Kyoto Yakuhin Kogyo Kabushiki Kaisha Adjuvant for promoting absorption of therapeutically active substances through the digestive tract
US4235776A (en) * 1979-03-15 1980-11-25 Eli Lilly And Company Tetrahydro-2H-benzo[c]pyrroles
DE2941597A1 (de) * 1979-10-13 1981-04-23 Basf Ag, 6700 Ludwigshafen Piperidinderivate von 4,5-dialkyl-3-hydroxy-pyrrol-2-carbonsaeureestern, ihre herstellung und diese enthaltende pharmazeutische zubereitungen
US4619941A (en) * 1984-11-19 1986-10-28 American Cyanamid Company N-[(1H-imidazol-1-yl)alkyl]-1H-indolecarboxamides useful as thromboxane synthetase inhibitors and antihypertensive agents
JP2001522844A (ja) * 1997-11-06 2001-11-20 スミスクライン・ビーチャム・パブリック・リミテッド・カンパニー ピリミジノン化合物およびそれを含有する医薬組成物
US6750228B1 (en) 1997-11-14 2004-06-15 Pharmacia Corporation Aromatic sulfone hydroxamic acid metalloprotease inhibitor
AU1520300A (en) 1998-11-05 2000-05-29 Biocryst Pharmaceuticals, Inc. New cyclopentane and cyclopentene compounds and use for detecting influenza virus
BR0010220A (pt) * 1999-05-01 2002-05-14 Smithkline Beecham Plc Compostos de pirimidinona
WO2001060805A1 (en) * 2000-02-16 2001-08-23 Smithkline Beecham P.L.C. Pyrimidine-4-one derivatives as ldl-pla2 inhibitors
GB0119795D0 (en) * 2001-08-14 2001-10-03 Smithkline Beecham Plc Novel process
TW201209043A (en) * 2010-05-17 2012-03-01 Glaxo Group Ltd Novel processes

Also Published As

Publication number Publication date
WO2011146494A1 (en) 2011-11-24
AU2011256270B2 (en) 2015-11-26
AU2011256270A1 (en) 2012-12-20
MX2012013387A (es) 2012-12-10
US9725420B2 (en) 2017-08-08
KR20130089157A (ko) 2013-08-09
US20130060028A1 (en) 2013-03-07
CA2799520A1 (en) 2011-11-24
EP2571857B1 (en) 2017-08-23
NZ603672A (en) 2015-01-30
EA201291235A1 (ru) 2013-04-30
ZA201208631B (en) 2013-09-25
UY33388A (es) 2011-12-01
CA2799520C (en) 2016-09-13
CR20120630A (es) 2013-02-15
MA34301B1 (fr) 2013-06-01
EP2571857A1 (en) 2013-03-27
EP2571857A4 (en) 2013-11-20
TW201209043A (en) 2012-03-01
CN103003249A (zh) 2013-03-27
IL223068A0 (en) 2013-02-03
CL2012003206A1 (es) 2013-01-25
US20160347720A1 (en) 2016-12-01
EA026569B1 (ru) 2017-04-28
DOP2012000289A (es) 2013-04-15
JP2013530948A (ja) 2013-08-01
SG185559A1 (en) 2012-12-28
CN105837520A (zh) 2016-08-10
AR081399A1 (es) 2012-08-29
JP6027529B2 (ja) 2016-11-16
CN103003249B (zh) 2016-04-27
US9447052B2 (en) 2016-09-20
BR112012030532A2 (pt) 2015-09-29
CO6630197A2 (es) 2013-03-01

Similar Documents

Publication Publication Date Title
PE20130318A1 (es) Nuevos procesos
AR061924A1 (es) Proceso para elaborar 2- amino -5 - halobenzamidas 3- sustituidas
PE20121440A1 (es) Derivados de oxazina y su uso como inhibidores de bace para el tratamiento de trastornos neurologicos
MY182568A (en) Quaternary ammonium compounds and their use as fuel or lubricant additives
SG195289A1 (en) Process for preparing heterocyclic compounds including trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide and salts thereof
PH12016502334B1 (en) Method for producing fused heterocyclic compound
AR084706A1 (es) Derivados sustituidos de imidazoquinolinas como inhibidores de quinasa y proceso para su preparacion
PE20181288A1 (es) Derivados de dihidroimidazopirazinona usados en el tratamiento del cancer
ES2570756T3 (es) Derivados pirimidinilpirrolopiridinona sustituidos, proceso para su preparación y su uso como inhibidores de cinasa
PE20141041A1 (es) Compuestos, metodos y formulaciones parasiticidas
PE20110672A1 (es) 4-fenil-1-h-pirazoles insecticidas
PE20142282A1 (es) Nuevos derivados de aril-quinolina
PE20091407A1 (es) Antagonistas de aminoalquilbifenilo n,n-disubstituidos de receptores de prostaglandina d2
AR087148A1 (es) Imidazopiridazinas
AR061806A1 (es) Derivados de alquilpiridazina como inhibidores de 11b-hsd1 (t2d)
MX2014006992A (es) Disales de acido malonico y metodo para preparar dihaluros de malonilo.
PE20150021A1 (es) 5-amino[1,4]tiazinas como inhibidores de bace1
BR112014004210B1 (pt) processo para a preparação de derivados de diamida do ácido antranílico substituídos com tetrazole por reação de benzoxazinonas com aminas
PE20140984A1 (es) 5 -(fenil / piridinil-etinilo)-2-piridina / 2-pirimidina carboxamidas como moduladores de mglur5
NZ702935A (en) Process for making hydroxylated cyclopentylpyrimidine compounds
CY1117087T1 (el) Διαδικασια για την παρασκευη εστερων (5-φθορο-2-μεθυλο-3-κινολιν-2-υλμεθυλ-ινδoλ-1-υλ)- οξικου οξεος
AR093977A1 (es) Proceso para la preparacion de 4-amino-5-fluoro-3-cloro-6-picolinatos (sustituidos)
CO6331471A2 (es) Derivados de piridina o su sal, plaguicida que contiene este y proceso para su produccion
AR088358A1 (es) Proceso de obtencion de acidos isoxazolil-metoxi-nicotinicos
CO6460700A2 (es) Compuesto de pirazol

Legal Events

Date Code Title Description
FD Application declared void or lapsed