AR063680A1 - Derivados de pirazolo[1, 5-a]pirimidina, metodos e intermediario para su preparacion, composiciones farmaceuticas que los comprenden y su uso en la fabricacion de medicamentos para el tratamiento de enfermedades mediadas por la modulacion de mglur5. - Google Patents

Derivados de pirazolo[1, 5-a]pirimidina, metodos e intermediario para su preparacion, composiciones farmaceuticas que los comprenden y su uso en la fabricacion de medicamentos para el tratamiento de enfermedades mediadas por la modulacion de mglur5.

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Publication number
AR063680A1
AR063680A1 ARP070103437A ARP070103437A AR063680A1 AR 063680 A1 AR063680 A1 AR 063680A1 AR P070103437 A ARP070103437 A AR P070103437A AR P070103437 A ARP070103437 A AR P070103437A AR 063680 A1 AR063680 A1 AR 063680A1
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Argentina
Prior art keywords
alkylaminocarbonyl
alkylamino
alkyl
aryl
heterocyclyl
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ARP070103437A
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Merz Pharma Gmbh & Co Kgaa
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Publication of AR063680A1 publication Critical patent/AR063680A1/es

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Abstract

Estos compuestos son potentes moduladores de mGluR5 y son útiles, por ejemplo, para el tratamiento de diversos trastornos neurológicos. Reivindicación 1: Un compuesto de pirazolo-pirimidina de fórmula (1) donde Y1, Y2 e Y3 independientemente son CR10, CR11, CR10R11, NR12, S o O, donde al menos uno de Y1, Y2 e Y3 denota CR10; o Y1 e Y2 juntos denotan un grupo R10C=N; R10C=CR11; R10R11C-C(=O) o R12N-(C=O); o Y2 e Y3 juntos denotan un grupo R10C=N; R10C=CR11; R10R11C-C(=O) o R12N-(C=O); R1 representa cloro o bromo; R2 representa hidrógeno, alquilo C1-6, cicloalquiIo C3-7 o trifluorometilo; R3 representa hidrógeno, alquilo C1-6, cicloaIquilo C3-7 o trifluorometilo; o R2 y R3, junto con el átomo de carbono del anillo, representan un grupo carbonilo; R4 representa hidrógeno, alquilo C1-6, cicloalquilo C3-7 o trifluorometilo; R5 representa hidrógeno, alquilo C1-6, cicloalquilo C3-7 o trifluorometilo; o R4 y R5, junto con el átomo de carbono del anillo, representan un grupo carbonilo; R6 representa hidrógeno, alquilo C1-6, cicloalquilo C3-7 o trifluorometilo; R7 representa hidrógeno, alquilo C1-6, cicloalquilo C3-7 o trifluorometilo; R6 y R7, junto con el átomo de carbono del anillo, representan un grupo carbonilo; R2 o R3, junto con R6 o R7, pueden formar un radical bivalente del tipo CH2-CH2 o CH2-O; R10 y R11 independientemente representan hidrógeno, halógeno, amino, hidroxi, nitro, ciano, trifluorometilo, trifluorometoxi, arilo, alquilo C1-6, cicloalquilo C3- 7, alquenilo C2-6, alquinilo C2-6, alcoxi C1-6, cicloalquiloxi C3-7, alqueniloxi C2-6, alquiniloxi C2-6, heteroarilo, heterociclilo, ariloxi, heteroariloxi, heterocicliloxi, alquilamino C1-6, di-alquilamino C1-6, cicloalquilamino C3-7, di- cicloalquilamino C3-7, alquil C1-6-cicloalquilamino C3-7, alquenilamino C2-6, alquinilamino C2-6, di-alquenilamino C2-6, di-alquinilamino C2-6, alquil C1-6-alquenilamino C2-6, alquil C1-6-alquinilamino C2-6, alquenil C2-6-cicloalquilamino C3-7, alquinil C2-6-cicloalquilamino C3-7, alquenil C2-6-alquinilamino C2-6, arilamino, diarilamino, aril-alquilamino C1-6, aril-alquenilamino C2-6, aril-alquinilamino C2-6, aril-cicloalquilamino C3-7, heteroarilamino, diheteroarilamino, heteroaril- alquilamino C1-6, heteroaril-alquenilamino C2-6, heteroaril-alquinilamino C2-6, heteroaril-cicloalquilamino C3-7, heteroarilarilamino, heterociclilamino, diheterociclilamino, heterociclilalquilamino C1-6, heterociclil-alquenilamino C2-6, heterociclil-alquinilamino C2-6, heterociclil-cicloalquilamino C3-7, heterociclilarilamino, heterociclilheteroarilamino, acil, aciloxi, acilamino, alcoxicarbonilo C1-6, cicloalcoxicarbonilo C3-7, alqueniloxicarbonilo C2-6, alquiniloxicarbonilo C2-6, ariloxicarbonilo, heteroariloxicarbonilo, heterocicliloxicarbonilo, aminocarbonilo, alquilamino-carbonilo C1-6, di-alquilaminocarbonilo C1-6, cicloalquilaminocarbonilo C3-7, di-cicloalquilaminocarbonilo C3-7, aIquil C1-6-cicloalquilaminocarbonilo C3- 7, alquenil-aminocarbonilo C2-6, alquinil-aminocarbonilo C2-6, di-alquenilaminocarbonilo C2-6, di-alquinilaminocarbonilo C2-6, alquil C1-6-alquenilaminocarbonilo C2-6, aIquil C1-6-alquinil-aminocarbonilo C2-6, alquenil C2-6- cicloalquilaminocarbonilo C3-7, alquinil C2-6-cicloalquilaminocarbonilo C3-7, alqueniI C2-6-alquinilaminocarbonilo C2-6, arilaminocarbonilo, diarilaminocarbonilo, aril-alquilaminocarbonilo C1-6, aril-alquenilaminocarbonilo C2-6, aril- alquinilaminocarbonilo C2-6, aril- cicloalquilaminocarbonilo C3-7, heteroarilaminocarbonilo, diheteroarilaminocarbonilo, heteroaril-alquilaminocarbonilo C1-6, heteroaril-alquenilaminocarbonilo C2-6, heteroaril-alquinilaminocarbonilo C2-6, heteroaril- cicloalquilaminocarbonilo C3-7, heteroarilarilaminocarbonilo, heterociclilaminocarbonilo, diheterociclilamino-carbonilo, heterociclil-alquilaminocarbonilo C1-6, heterociclil-alquenilamino-carbonilo C2-6, heterociclil-alquinilaminocarbonilo C2-6, heterociclil- cicloalquilaminocarbonilo C3-7, heterociclilarilaminocarbonilo, heterociclilheteroarilamino-carbonilo, alquilsulfinilo C1-6, cicloalquilsulfinilo C3-7, alquenilsulfinilo C2-6, alquinilsulfinilo C2-6, arilsulfinilo, heteroarilsulfinilo, heterociclilsulfinilo, alquilsulfonilo C1-6, cicloalquilsulfonilo C3-7, alquenilsulfonilo C2-6, alquinilsulfonilo C2-6, arilsulfonilo, heteroarilsulfonilo, heterociclilsulfonilo, alquilsulfonilamino C1-6 o arilsulfonilamino; y R12 representa hidrógeno, alquilo C1-6, cicloalquilo C3-7, alquenilo C2-6, alquinilo C2-6, acilo, arilo, heteroarilo, heterociclilo, alquilamino-carbonilo C1-6, di-alquilamino-carbonilo C1-6, alquilsulfonilo C1-6, arilsulfonilo o heteroarilsulfonilo; e isómeros ópticos, sales, hidratos, solvatos y polimorfos farmacéuticamente aceptables de dicho compuesto. Reivindicación 29: Un proceso para la síntesis de un compuesto seleccionado entre aquellos de fórmula (1) donde: Y1, Y2 e Y3 independientemente son CR10, CR11, CR10R11, NR12, S o O, donde al menos uno de Y1, Y2 e Y3 denota CR10; o Y1 e Y2 juntos denotan un grupo R10C=N; R10C=CR11; R10R11C-C(=O) o R12N-(C=O); o Y2 e Y3 juntos denotan un grupo R10C=N; R10C=CR11; R10R11C-C(=O) o R12N-(C=O); R1 representa cloro o bromo; R2 representa hidrógeno, alquilo C1-6, cicloalquiIo C3-7 o trifluorometilo; R3 representa hidrógeno, alquilo C1-6, cicloaIquilo C3-7 o trifluorometilo; o R2 y R3, junto con el átomo de carbono del anillo, representan un grupo carbonilo; R4 representa hidrógeno, alquilo C1-6, cicloalquilo C3-7 o trifluorometilo; R5 representa hidrógeno, alquilo C1-6, cicloalquilo C3-7 o trifluorometilo; o R4 y R5, junto con el átomo de carbono del anillo, representan un grupo carbonilo; R6 representa hidrógeno, alquilo C1-6, cicloalquilo C3-7 o trifluorometilo; R7 representa hidrógeno, alquilo C1-6, cicloalquilo C3-7 o trifluorometilo; R6 y R7, junto con el átomo de carbono del anillo, representan un grupo carbonilo; R2 o R3, junto con R6 o R7, pueden formar un radical bivalente del tipo CH2-CH2 o CH2-O; R10 y R11 independientemente representan hidrógeno, halógeno, amino, hidroxi, nitro, ciano, trifluorometilo, trifluorometoxi, arilo, alquilo C1-6, cicloalquilo C3- 7, alquenilo C2-6, alquinilo C2-6, alcoxi C1-6, cicloalquiloxi C3-7, alqueniloxi C2-6, alquiniloxi C2-6, heteroarilo, heterociclilo, ariloxi, heteroariloxi, heterocicliloxi, alquilamino C1-6, di-alquilamino C1-6, cicloalquilamino C3-7, di- cicloalquilamino C3-7, alquil C1-6-cicloalquilamino C3-7, alquenilamino C2-6, alquinilamino C2-6, di-alquenilamino C2-6, di-alquinilamino C2-6, alquil C1-6-alquenilamino C2-6, alquil C1-6-alquinilamino C2-6, alquenil C2-6-cicloalquilamino C3-7, alquinil C2-6-cicloalquilamino C3-7, alquenil C2-6-alquinilamino C2-6, arilamino, diarilamino, aril-alquilamino C1-6, aril-alquenilamino C2-6, aril-alquinilamino C2-6, aril-cicloalquilamino C3-7, heteroarilamino, diheteroarilamino, heteroaril- alquilamino C1-6, heteroaril-alquenilamino C2-6, heteroaril-alquinilamino C2-6, heteroaril-cicloalquilamino C3-7, heteroarilarilamino, heterociclilamino, diheterociclilamino, heterociclilalquilamino C1-6, heterociclil-alquenilamino C2-6, heterociclil-alquinilamino C2-6, heterociclil-cicloalquilamino C3-7, heterociclilarilamino, heterociclilheteroarilamino, acil, aciloxi, acilamino, alcoxicarbonilo C1-6, cicloalcoxicarbonilo C3-7, alqueniloxicarbonilo C2-6, alquiniloxicarbonilo C2-6, ariloxicarbonilo, heteroariloxicarbonilo, heterocicliloxicarbonilo, aminocarbonilo, alquilamino-carbonilo C1-6, di-alquilaminocarbonilo C1-6, cicloalquilaminocarbonilo C3-7, di-cicloalquilaminocarbonilo C3-7, aIquil C1-6-cicloalquilaminocarbonilo C3- 7, alquenil-aminocarbonilo C2-6, alquinil-aminocarbonilo C2-6, di-alquenilaminocarbonilo C2-6, di-alquinilaminocarbonilo C2-6, alquil C1-6-alquenilaminocarbonilo C2-6, aIquil C1-6-alquinil-aminocarbonilo C2-6, alquenil C2-6- cicloalquilaminocarbonilo C3-7, alquinil C2-6-cicloalquilaminocarbonilo C3-7, alqueniI C2-6-alquinilaminocarbonilo C2-6, arilaminocarbonilo, diarilaminocarbonilo, aril-alquilaminocarbonilo C1-6, aril-alquenilaminocarbonilo C2-6, aril- alquinilaminocarbonilo C2-6, aril- cicloalquilaminocarbonilo C3-7, heteroarilaminocarbonilo, diheteroarilaminocarbonilo, heteroaril-alquilaminocarbonilo C1-6, heteroaril-alquenilaminocarbonilo C2-6, heteroaril-alquinilaminocarbonilo C2-6, heteroaril- cicloalquilaminocarbonilo C3-7, heteroarilarilaminocarbonilo, heterociclilaminocarbonilo, diheterociclilamino-carbonilo, heterociclil-alquilaminocarbonilo C1-6, heterociclil-alquenilamino-carbonilo C2-6, heterociclil-alquinilaminocarbonilo C2-6, heterociclil- cicloalquilaminocarbonilo C3-7, heterociclilarilaminocarbonilo, heterociclilheteroarilamino-carbonilo, alquilsulfinilo C1-6, cicloalquilsulfinilo C3-7, alquenilsulfinilo C2-6, alquinilsulfinilo C2-6, arilsulfinilo, heteroarilsulfinilo, heterociclilsulfinilo, alquilsulfonilo C1-6, cicloalquilsulfonilo C3-7, alquenilsulfonilo C2-6, alquinilsulfonilo C2-6, arilsulfonilo, heteroarilsulfonilo, heterociclilsulfonilo, alquilsulfonilamino C1-6 o arilsulfonilamino; y R12 representa hidrógeno, alquilo C1-6, cicloalquilo C3-7, alquenilo C2-6, alquinilo C2-6, acilo, arilo, heteroarilo, heterociclilo, alquilamino-carbonilo C1-6, di-alquilamino-carbonilo C1-6, alquilsulfonilo C1-6, arilsulfonilo o heteroarilsulfonilo; e isómeros ópticos, sales, hidratos, solvatos y polimorfos farmacéuticamente aceptables de dicho compuesto, donde un compuesto de fórmula (2) se suspende en una mezcla de etanol y agua y se trata con ácido clorhídrico, seguido por la reacción con H2NNHCOOCH3, para proporcionar un compuesto de fórmula (3), el cual se hace reaccionar con un compuesto de fórmula (4) para proporcionar un compuesto de fórmula (5) el cual se hidroliza en condiciones ácidas para proporcionar un compuesto de fórmula (6) el cual se trata con una amina de fórmula (7) en presencia de un agente de condensación, para proporcionar un compuesto de fórmula (1), el cual se convierte, si así se desea, en una sal, hidrato, solvato o polimorfo farmacé
ARP070103437A 2006-08-04 2007-08-03 Derivados de pirazolo[1, 5-a]pirimidina, metodos e intermediario para su preparacion, composiciones farmaceuticas que los comprenden y su uso en la fabricacion de medicamentos para el tratamiento de enfermedades mediadas por la modulacion de mglur5. AR063680A1 (es)

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Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008056176A1 (en) * 2006-11-10 2008-05-15 Scottish Biomedical Limited Pyrazolopyrimidines as phosphodiesterase inhibitors
HK1136565A1 (en) * 2007-03-31 2010-07-02 Intervet Int Bv Processes for making zilpaterol and salts thereof
EP2090576A1 (en) * 2008-02-01 2009-08-19 Merz Pharma GmbH & Co.KGaA 6-halo-pyrazolo[1,5-a]pyridines, a process for their preparation and their use as metabotropic glutamate receptor (mGluR) modulators
CN102131503A (zh) 2008-06-30 2011-07-20 诺瓦提斯公司 用于治疗帕金森病的包含mGluR调节剂的组合产品
JP2013512216A (ja) 2009-11-25 2013-04-11 メルツ・ファルマ・ゲゼルシヤフト・ミト・ベシュレンクテル・ハフツング・ウント・コンパニー・コマンデイトゲゼルシヤフト・アウフ・アクティーン 置換ピラゾロピリミジン類の結晶形
AU2011338339A1 (en) 2010-12-08 2013-06-27 Vanderbilt University Bicyclic pyrazole compounds as allosteric modulators of mGluR5 receptors
CA2830220A1 (en) * 2011-03-15 2012-09-20 Vanderbilt University Substituted imidazopyrimidin-5(6h)-ones as allosteric modulators of mglur5 receptors
US8865725B2 (en) 2011-03-15 2014-10-21 Vanderbilt University Substituted imidazopyrimidin-5(6H)-ones as allosteric modulators of MGLUR5 receptors
WO2012139876A1 (en) 2011-04-14 2012-10-18 Merz Pharma Gmbh & Co. Kgaa Enteric formulations of metabotropic glutamate receptor modulators
US8791108B2 (en) 2011-08-18 2014-07-29 Bristol-Myers Squibb Company Inhibitors of human immunodeficiency virus replication
WO2013087808A1 (en) 2011-12-15 2013-06-20 Merz Pharma Gmbh & Co. Kgaa Pharmaceutical composition comprising a pyrazolopyrimidme and cyclodextrin
WO2013087815A1 (en) 2011-12-15 2013-06-20 Merz Pharma Gmbh & Co. Kgaa Liquid pharmaceutical composition containing a pyrazolopyrimidine derivative and pharmaceutical uses thereof
US9006235B2 (en) 2012-03-06 2015-04-14 Bristol-Myers Squibb Company Inhibitors of human immunodeficiency virus replication
JP5898815B2 (ja) * 2012-03-29 2016-04-06 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 新規なピラゾロピリミジン
JO3407B1 (ar) 2012-05-31 2019-10-20 Eisai R&D Man Co Ltd مركبات رباعي هيدرو بيرازولو بيريميدين
JP2015529206A (ja) 2012-08-25 2015-10-05 ザ・ジョンズ・ホプキンス・ユニバーシティ Gapdhカスケードインヒビター化合物ならびに使用の方法および精神病を含むストレス誘導障害の処置
PE20151332A1 (es) 2013-02-19 2015-09-20 Pfizer Compuestos de azabencimidazol
WO2014164428A1 (en) 2013-03-13 2014-10-09 Bristol-Myers Squibb Company Inhibitors of human immunodeficiency virus replication
WO2014164467A1 (en) 2013-03-13 2014-10-09 Bristol-Myers Squibb Company Inhibitors of human immunodeficiency virus replication
US9540393B2 (en) 2013-03-14 2017-01-10 VIIV Healthcare UK (No.5) Limited Inhibitors of human immunodeficiency virus replication
EP3036219A4 (en) * 2013-06-04 2017-08-23 Temple University Of The Commonwealth System Of Higher Education Novel beta lactams as modulators of glutamate uptake and methods for use thereof
US10398142B2 (en) 2013-11-05 2019-09-03 Temple University Of The Commonwealth System Of Higher Education Polycationic amphiphiles as antimicrobial agents
US10136639B2 (en) 2013-11-05 2018-11-27 Villanova University Polycationic amphiphiles as antimicrobial agents
GB201320905D0 (en) 2013-11-27 2014-01-08 Takeda Pharmaceutical Therapeutic compounds
US9273067B2 (en) 2014-02-19 2016-03-01 Bristol-Myers Squibb Company Pyrazolopyrimidine macrocycles as inhibitors of human immunodeficiency virus replication
JP6713982B2 (ja) * 2014-07-24 2020-06-24 ファイザー・インク ピラゾロピリミジン化合物
KR102061952B1 (ko) 2014-08-06 2020-01-02 화이자 인코포레이티드 이미다조피리다진 화합물
KR102482200B1 (ko) 2016-01-27 2022-12-27 우니페르지타에트 취리히 가려움증 치료를 위한 gabaa 수용체 조절인자의 용도

Family Cites Families (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL7305644A (es) 1972-04-20 1973-10-23
GB1383409A (en) * 1972-09-09 1974-02-12 Pfizer Ltd Derivatives of 2-amino- and 4-amino-quinazoline and pharmaceutical compositions containing them
US3988339A (en) * 1974-02-08 1976-10-26 Smithkline Corporation Pharmaceutical compositions and methods of inhibiting phenylethanolamine N-methyltransferase
US3974283A (en) * 1974-03-18 1976-08-10 Sandoz, Inc. N-substituted-4-T-butyl-1-pyridinethiocarboxamides and their use for treatment of inflammation or pain
NZ190915A (en) * 1978-07-31 1984-07-31 Hoffmann La Roche Oxadiazolotriazine derivatives and pharmaceutical compositions
DE2856393C2 (de) 1978-12-27 1983-04-28 Merz + Co GmbH & Co, 6000 Frankfurt Arzneimittel zur Behandlung von Morbus Parkinson
SU768177A1 (ru) * 1979-04-23 1985-08-07 МГУ им.М.В.Ломоносова Способ получени ( @ )-(-) или ( @ )-(+)-1=метил-1,2,3,4-тетрагидроизохинолина
ZA803591B (en) * 1979-07-09 1981-06-24 American Cyanamid Co Substituted pyrazolo(1,5-a)pyrimidines
US4340597A (en) * 1981-04-13 1982-07-20 Schering Corporation 1-Substituted-4-aryl-1,2,5,6-tetrahydro and hexahydropyridines
DE3308554A1 (de) * 1983-03-10 1984-09-13 Hoechst Ag, 6230 Frankfurt 1-/1,3-dioxolan-2-ylmethyl)-azole, ihre salze, verfahren zu ihrer herstellung und ihre verwendung
WO1989005643A1 (en) * 1987-12-18 1989-06-29 Pfizer Inc. Heterocyclic-substituted quinoline-carboxylic acids
ATE94384T1 (de) 1989-04-14 1993-10-15 Merz & Co Gmbh & Co Verwendung von adamantan-derivaten zur praevention und behandlung der cerebralen ischaemie.
US6177443B1 (en) 1997-03-07 2001-01-23 Novo Nordisk A/S 4,5,6,7-tetrahydro-thieno[3, 2-C]pyridine derivatives, their preparation and use
TW593225B (en) 1997-06-30 2004-06-21 Merz Pharma Gmbh & Co Kgaa 1-amino-alkylcyclohexane NMDA receptor antagonists
US6071966A (en) 1997-06-30 2000-06-06 Merz + Co. Gmbh & Co. 1-amino-alkylcyclohexane NMDA receptor antagonists
DE19732589A1 (de) * 1997-07-29 1999-02-04 Huels Chemische Werke Ag Verfahren zur Herstellung von 1,2,3,6-tetrahydro-2,2,6,6-tetramethylpyridin
FR2769313B1 (fr) 1997-10-06 2000-04-21 Sanofi Sa Derives d'esters hydroxyacetiques, leur procede de preparation et leur utilisation comme intermediaires de synthese
JP2001524468A (ja) 1997-11-21 2001-12-04 エヌピーエス ファーマシューティカルズ インコーポレーテッド 中枢神経系疾患を治療するための代謝調節型グルタミン酸受容体アンタゴニスト
CN1129578C (zh) * 1997-12-25 2003-12-03 明治制果株式会社 四氢苯并吲哚衍生物
CN1261098C (zh) 1998-08-28 2006-06-28 西奥斯股份有限公司 p38-α激酶的抑制剂
US20020049223A1 (en) 1999-11-05 2002-04-25 Elmore Steven W. Quinoline and naphthyridine carboxylic acid antibacterials
MXPA02006474A (es) * 1999-12-28 2002-11-29 Eisai Co Ltd Compuestos heterociclicos que contienen sulfonamida.
GB0110338D0 (en) 2001-04-27 2001-06-20 Sb Pharmco Inc Novel processes
GB0118752D0 (en) * 2001-08-01 2001-09-26 Pfizer Ltd Process for the production of quinazolines
EP1506196B1 (en) * 2001-11-01 2012-01-18 Icagen, Inc. Pyrazolopyrimidines as sodium channel inhibitors
WO2003091256A1 (fr) 2002-04-23 2003-11-06 Shionogi & Co., Ltd. Derive de pyrazolo[1,5-a]pyrimidine et inhibiteur de la nad(p)h oxydase contenant ledit derive
CA2487211C (en) 2002-06-04 2010-09-14 Neogenesis Pharmaceuticals, Inc. Pyrazolo(1,5a) pyrimidine compounds as antiviral agents
CA2495179A1 (en) * 2002-08-09 2004-02-19 Astrazeneca Ab Compounds having an activity at metabotropic glutamate receptors
ES2423800T3 (es) 2003-03-28 2013-09-24 Novartis Vaccines And Diagnostics, Inc. Uso de compuestos orgánicos para la inmunopotenciación
WO2004089471A2 (en) * 2003-04-11 2004-10-21 Novo Nordisk A/S NEW PYRAZOLO[1,5-a] PYRIMIDINES DERIVATIVES AND PHARMACEUTICAL USE THEREOF
WO2004089416A2 (en) 2003-04-11 2004-10-21 Novo Nordisk A/S Combination of an 11beta-hydroxysteroid dehydrogenase type 1 inhibitor and an antihypertensive agent
WO2004089415A2 (en) 2003-04-11 2004-10-21 Novo Nordisk A/S COMBINATIONS OF AN 11β-HYDROXYSTEROID DEHYDROGENASE TYPE 1 INHIBITOR AND A GLUCOCORTICOID RECEPTOR AGONIST
US8197819B2 (en) 2004-06-08 2012-06-12 Novartis Vaccines And Diagnostics, Inc. Env polypeptide complexes and methods of use
ATE390424T1 (de) 2004-08-02 2008-04-15 Sanol Arznei Schwarz Gmbh Carboxamide des indolizins und seiner aza- und diazaderivate
US20090048285A1 (en) 2005-01-19 2009-02-19 Benjamin Pelcman Pyrrolopyridines Useful in the Treatment of Inflammation

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AU2007280428B2 (en) 2012-04-12
HRP20110128T1 (hr) 2011-03-31
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JP2009545569A (ja) 2009-12-24
IL196008A0 (en) 2009-09-01
RU2009107686A (ru) 2010-09-10
TWI399376B (zh) 2013-06-21
WO2008015271A1 (en) 2008-02-07
JP2010500288A (ja) 2010-01-07
US20110212956A1 (en) 2011-09-01
PL2054416T3 (pl) 2011-05-31
PT2054416E (pt) 2011-04-06
US7947689B2 (en) 2011-05-24
DE602007011773D1 (de) 2011-02-17
US20080032998A1 (en) 2008-02-07
RU2009107688A (ru) 2010-09-10
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US20080039458A1 (en) 2008-02-14
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