AR079076A1 - Compuestos heterociclicos antivirales - Google Patents

Compuestos heterociclicos antivirales

Info

Publication number
AR079076A1
AR079076A1 ARP100104279A ARP100104279A AR079076A1 AR 079076 A1 AR079076 A1 AR 079076A1 AR P100104279 A ARP100104279 A AR P100104279A AR P100104279 A ARP100104279 A AR P100104279A AR 079076 A1 AR079076 A1 AR 079076A1
Authority
AR
Argentina
Prior art keywords
alkyl
hydrogen
carbamoyl
alkoxy
haloalkyl
Prior art date
Application number
ARP100104279A
Other languages
English (en)
Inventor
Joshua Paul Gergely Taygerly
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR079076A1 publication Critical patent/AR079076A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic 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
    • C07D213/02—Heterocyclic 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
    • C07D213/04—Heterocyclic 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
    • C07D213/60—Heterocyclic 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
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • 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
    • A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic 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
    • C07D213/02—Heterocyclic 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
    • C07D213/04—Heterocyclic 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
    • C07D213/60—Heterocyclic 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
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • 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
    • C07D239/52—Two oxygen atoms
    • C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D253/00—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00
    • C07D253/02—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00 not condensed with other rings
    • C07D253/06—1,2,4-Triazines
    • C07D253/065—1,2,4-Triazines having three double bonds between ring members or between ring members and non-ring members
    • C07D253/07—1,2,4-Triazines having three 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Virology (AREA)
  • Engineering & Computer Science (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Son inhibidores de la polimerasa NS5B del virus de la hepatitis C. Se describen también composiciones y métodos para tratar una infeccion del HCV y para inhibir la replicacion del HCV. Reivindicacion 1: Un compuesto de la formula 1: en la que R1 es CH=CHAr, C=CAr, [C(R5)2]2Ar o naftilo, dicho naftilo está opcionalmente sustituido por [C(R5)2]0-3NRaRb; Ar es fenilo, piridinilo o piridazinilo, dicho Ar está opcionalmente sustituido con independencia de una a tres veces por sustituyentes elegidos entre el grupo formado por: (a) [C(R5)2]0-3NRaRb, (b) hidroxialquilo C1-10, en el que uno o dos átomos de carbono pueden reemplazarse opcionalmente por oxígeno con la condicion de que con el reemplazo no se forme un peroxido, (c) (alcoxi C1-3) -alquilo C1-6, (d) carboxilo, (e) X1[C(R5)2]1-6CO2R4, en el que X1 es O, NR5, o un enlace y R4 es hidrogeno o alquilo C1-6, (f) (alcoxi C1-6)-carbonilo, (g) halogeno, (h) [C(R5)2]0-3CN, (i) alquilo C1-6 y (j) haloalquilo C1-6 R2 es hidrogeno, alcoxi C1-6, halogeno o alquilo C1-6 R3 es un resto heteroarilo elegido entre el grupo formado por A-1, A-2, A-3 y A-4, dicho heteroarilo está opcionalmente sustituido por halogeno, alquilo C1-6, haloalquilo C1-3, alcoxi; R5 con independencia de cada aparicion es hidrogeno o alquilo C1-3; R7 se elige entre el grupo formado por: (a) halogeno, (b) alquilo C1-6 en el que uno o dos átomos de carbono pueden reemplazarse opcionalmente por oxígeno, con la condicion de que con el reemplazo no se forme un peroxido, (c) haloalquilo C1-3, (d) alcoxi C1-3, (e) hidroxialquilo C2-6 en el que uno o dos átomos de carbono pueden reemplazarse opcionalmente por oxígeno con la condicion de que con el reemplazo no se forme un peroxido ni un hemiacetal; (f) NR5[C(R5)2]-hidroxialquilo C2-6 (g) ciano-alquilo C1-3, (h) X2[C(R5)2]1-6CO2H, (i) [C(R5)2]1-6NRcRd, (j) X2-[C(R5)2]2-6NRcRd, en el que X2 es O o NR5 R8 es hidrogeno o CH2OR9, en el que R9 es valina, prolina o P(=O) (OH)2; R9 es hidrogeno o alquilo C1-6 Y es hidrogeno o hidroxilo; m es el numero cero o uno; Ra y Rb son (i) con independencia de cada aparicion: (a) hidrogeno, (b) alquilo C1-6, (c) SO2R6, en el que R6 es alquilo C1-6, haloalquilo C1-6, cicloalquilo C3-7, (cicloalquil C3-7) -alquilo C1-3, (alcoxi C1-6) -alquilo C1-6 o [C(R5)2]0-6NRcRd, (d) haloalquilo C1-3, (e) acilo C1-6, (f) carbamoílo, (g) (alquil C1-3)-carbamoílo o (h) (dialquil C1-3)-carbamoílo, (d) acilo C1-6, (e) carbamoílo, (f) (alquil C1-3)-carbamoílo o (g) (dialquil C1-3)-carbamoílo o (ii) Ra y Rb junto con el nitrogeno al que están unidos forman una amina cíclica opcionalmente sustituida; Rc y Rd son con independencia hidrogeno o alquilo C1-6 o Rc y Rd junto con el nitrogeno al que están unidos forman una amina cíclica opcionalmente sustituida.
ARP100104279A 2009-11-21 2010-11-19 Compuestos heterociclicos antivirales AR079076A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US26335009P 2009-11-21 2009-11-21

Publications (1)

Publication Number Publication Date
AR079076A1 true AR079076A1 (es) 2011-12-21

Family

ID=43446565

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100104279A AR079076A1 (es) 2009-11-21 2010-11-19 Compuestos heterociclicos antivirales

Country Status (11)

Country Link
US (1) US8383824B2 (es)
EP (1) EP2501679A1 (es)
JP (1) JP2013511489A (es)
KR (1) KR20120085918A (es)
CN (1) CN102639504A (es)
AR (1) AR079076A1 (es)
BR (1) BR112012012085A2 (es)
CA (1) CA2778206A1 (es)
MX (1) MX2012005706A (es)
TW (1) TW201129362A (es)
WO (1) WO2011061243A1 (es)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE102014217907B4 (de) 2014-09-08 2018-12-20 Carl Zeiss Smt Gmbh Verfahren zum Herstellen einer Maske für den extrem ultra-violetten Wellenlängenbereich und Maske
US9765050B2 (en) 2014-12-30 2017-09-19 Novira Therapeutics, Inc. Pyridyl reverse sulfonamides for HBV treatment

Family Cites Families (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6221335B1 (en) * 1994-03-25 2001-04-24 Isotechnika, Inc. Method of using deuterated calcium channel blockers
US6440710B1 (en) * 1998-12-10 2002-08-27 The Scripps Research Institute Antibody-catalyzed deuteration, tritiation, dedeuteration or detritiation of carbonyl compounds
DK1104760T3 (da) * 1999-12-03 2003-06-30 Pfizer Prod Inc Sulfamoylheteroarylpyrazolforbindelser som anti-inflammatoriske/analgetiske midler
WO2001047833A1 (fr) 1999-12-24 2001-07-05 Asahi Glass Company, Limited Filtre au nitrure de silicium et procede de fabrication correspondant
JP2004509066A (ja) 2000-05-10 2004-03-25 スミスクライン・ビーチャム・コーポレイション 新規抗感染症薬
US6448281B1 (en) 2000-07-06 2002-09-10 Boehringer Ingelheim (Canada) Ltd. Viral polymerase inhibitors
AR036081A1 (es) 2001-06-07 2004-08-11 Smithkline Beecham Corp Compuesto de 1,2-dihidroquinolina, su uso para preparar una composicion farmaceutica, metodos para prepararlo y compuestos del acido 2-aminobenzoico n-alquilado de utilidad como intermediarios en dichos metodos
AR035543A1 (es) 2001-06-26 2004-06-16 Japan Tobacco Inc Agente terapeutico para la hepatitis c que comprende un compuesto de anillo condensado, compuesto de anillo condensado, composicion farmaceutica que lo comprende, compuestos de benzimidazol, tiazol y bifenilo utiles como intermediarios para producir dichos compuestos, uso del compuesto de anillo con
US6841566B2 (en) 2001-07-20 2005-01-11 Boehringer Ingelheim, Ltd. Viral polymerase inhibitors
US6899700B2 (en) 2001-08-29 2005-05-31 Kimberly-Clark Worldwide, Inc. Therapeutic agent delivery tampon
WO2003037262A2 (en) 2001-10-29 2003-05-08 Smithkline Beecham Corporation Novel anit-infectives
WO2003059356A2 (en) 2001-10-30 2003-07-24 Smithkline Beecham Corporation Novel anti-infectives
DE60305903T2 (de) * 2002-04-08 2007-03-08 Pfizer Inc. Tropanderivative als ccr5-modulatoren
WO2003099801A1 (en) 2002-05-24 2003-12-04 Smithkline Beecham Corporation Novel anti-infectives
EP1515978A1 (en) * 2002-06-20 2005-03-23 IC Vec Limited Sulfur-containing phospholipid derivatives
BR0315897A (pt) 2002-11-01 2008-05-13 Abbott Lab agentes antiinfecciosos
TW200413273A (en) * 2002-11-15 2004-08-01 Wako Pure Chem Ind Ltd Heavy hydrogenation method of heterocyclic rings
TWI332507B (en) 2002-11-19 2010-11-01 Hoffmann La Roche Antiviral nucleoside derivatives
AU2003300957A1 (en) 2002-12-11 2004-06-30 Smithkline Beecham Corporation Anti-infectives
WO2004052312A2 (en) 2002-12-11 2004-06-24 Smithkline Beecham Corporation Anti-infectives
WO2004058150A2 (en) 2002-12-17 2004-07-15 Smithkline Beecham Corporation Anti-infectives
WO2005019191A2 (en) 2003-08-25 2005-03-03 Abbott Laboratories 1, 1-dioxido-4h-1,2,4-benzothiadiazine derivate und verwandte verbindungen als inhibitoren der hcv polymerase zur behandlung von hepatitis c
BRPI0514591A (pt) 2004-08-23 2008-06-17 Hoffmann La Roche compostos antivirais heterocìclicos
BRPI0611388A2 (pt) 2005-05-04 2010-09-08 Hoffmann La Roche compostos antivirais heterocìclicos, uso dos mesmos e composição farmacêutica
CA2624179A1 (en) * 2005-10-06 2007-04-12 Auspex Pharmaceuticals, Inc. Deuterated inhibitors of gastric h+, k+-atpase with enhanced therapeutic properties
US7750168B2 (en) * 2006-02-10 2010-07-06 Sigma-Aldrich Co. Stabilized deuteroborane-tetrahydrofuran complex
BRPI0815811A2 (pt) * 2007-08-29 2015-02-18 Schering Corp Derivados de indol substituído e métodos de uso dos mesmos
PT2639226T (pt) * 2007-09-17 2016-12-09 Abbvie Bahamas Ltd Pirimidinas anti-infeciosas e suas utilizações
WO2009039127A1 (en) * 2007-09-17 2009-03-26 Abbott Laboratories Uracil or thymine derivative for treating hepatitis c
EP2548873A1 (en) * 2007-09-17 2013-01-23 Abbott Laboratories N-phenyl-dioxo-hydropyrimidines useful as hepatitis c virus (hcv) inhibitors
MX2010006397A (es) 2007-12-21 2010-07-05 Hoffmann La Roche Compuestos heterociclicos antivirales.
JP2011528686A (ja) * 2008-07-23 2011-11-24 エフ．ホフマン−ラ ロシュ アーゲー ヘテロ環式抗ウイルス性化合物
BRPI0924121A2 (pt) * 2008-12-22 2019-09-24 Hoffmann La Roche compostos antivirais heterocíclicos
MX2011010058A (es) * 2009-03-25 2011-10-11 Abbott Lab Compuestos antivirales y usos de los mismos.

Also Published As

Publication number Publication date
CN102639504A (zh) 2012-08-15
US20110123489A1 (en) 2011-05-26
JP2013511489A (ja) 2013-04-04
WO2011061243A1 (en) 2011-05-26
CA2778206A1 (en) 2011-05-26
EP2501679A1 (en) 2012-09-26
KR20120085918A (ko) 2012-08-01
TW201129362A (en) 2011-09-01
MX2012005706A (es) 2012-06-12
US8383824B2 (en) 2013-02-26
BR112012012085A2 (pt) 2016-05-17

Similar Documents

Publication Publication Date Title
AR078397A1 (es) Compuestos heterociclicos antivirales
RS54288B1 (en) SUBSTITUTED TRIAZOLOPYRIDINES AND THEIR USE AS TTK INHIBITORS
EA200970493A1 (ru) Макроциклические ингибиторы вируса гепатита с
ES2640911T3 (es) Cicloalquilnitrilpirazolcarboxamidas como inhibidores de la quinasa Janus
AR076579A1 (es) Espironucleosidos uracilicos oxetanicos, composiciones farmaceuticas que los contienen y uso de los mismos como inhibidores del virus de la hepatitis c (vhc).
CO6251247A2 (es) Imidazoquinolinas con propiedades inmuno-moduladoras
BR112012015951A2 (pt) 4 azido-nucleosídeos como compostos anti-hcv
AR079634A1 (es) Inhibidores del virus de la hepatitis c
ECSP088518A (es) Nucleósidos antivirales
AR092390A1 (es) Nucleosidos ramificados en 2 para el tratamiento de infecciones virales
AR059621A1 (es) Acidos 4- fenil- tiazol-5- carboxilicos y amidas de acidos 4- fenil- tiazol5 carboxilicos como inhibidores de la plk1
AR084976A1 (es) Compuestos de bifenileno sustituidos y metodos de uso de los mismos para el tratamiento de enfermedades virales
AR073136A1 (es) Compuestos de pirrol
CO6260076A2 (es) Derivados de uracilo o timina para el tratamiento de la hepatitis c
AR074504A1 (es) Nucleotidos uracil ciclopropilicos
AR062827A1 (es) Inhibidores virales policiclicos, una composicion farmaceutica que los comprende y su uso en la preparacion de medicamentos para el tratamiento de una infeccion viral mediada porl el virus de la hepatitis c
EA201600241A1 (ru) Замещенные (2r,3r,5r)-3-гидрокси-(5-пиримидин-1-ил)тетрагидрофуран-2-илметил арил фосфорамидаты
AR080596A1 (es) Compuestos alquilamido y composiciones farmaceuticas
AR069804A1 (es) Agonistas del receptor glucocorticoide c20- c21 sustituido
AR062258A1 (es) Compuestos heterociclicos condensados de tieno-pirrol, composiciones farmaceuticas que los contienen y usos para el tratamiento de infecciones por hcv
AR082889A1 (es) Compuestos y composiciones para la inhibicion de nampt
AR086290A1 (es) Inhibidores del virus de la hepatitis c
ES2630079T3 (es) Moduladores de la ruta del complemento y usos de los mismos
EA200971080A1 (ru) Кристаллическое соединение пиридазина
AR082619A1 (es) Inhibidores del virus de la hepatitis c

Legal Events

Date Code Title Description
FB Suspension of granting procedure