AR076601A1 - Pirimidinas como agentes terapeuticos - Google Patents

Pirimidinas como agentes terapeuticos

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Publication number
AR076601A1
AR076601A1 ARP100101785A ARP100101785A AR076601A1 AR 076601 A1 AR076601 A1 AR 076601A1 AR P100101785 A ARP100101785 A AR P100101785A AR P100101785 A ARP100101785 A AR P100101785A AR 076601 A1 AR076601 A1 AR 076601A1
Authority
AR
Argentina
Prior art keywords
aromatic
nhc
unsubstituted
alkyl
independently
Prior art date
Application number
ARP100101785A
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English (en)
Original Assignee
Chlorion Pharma Inc
Univ Laval
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 Chlorion Pharma Inc, Univ Laval filed Critical Chlorion Pharma Inc
Publication of AR076601A1 publication Critical patent/AR076601A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed 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
    • A61K31/435—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
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic 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
    • A61K31/495—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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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]
    • 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
    • C07D239/38—One sulfur 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
    • C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • 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
    • C07D239/56—One oxygen atom and one sulfur atom
    • 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
    • C07D403/02—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 two hetero rings
    • C07D403/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Un compuesto de cualquiera de las Formulas ((1a-2)-(1a-21)), incluyendo otros tautomeros, estereoisomeros, estereoisomeros E/Z, profármacos, sales farmacéuticamente aceptables, y también caracteriza composiciones, métodos para tratar o prevenir dolor (por ej., dolor neuropático), inflamacion, o epilepsia y como anticonvulsivos. Reivindicacion 1: Un compuesto que tiene la siguiente estructura (1a) y sus tautomeros (1b), incluyendo otros tautomeros, estereoisomeros, estereoisomeros E/Z, profármacos y sus sales farmacéuticamente aceptables, donde Q1 es -O-, -S-, -SO-, -SO2-, -CH2-, -CH2CH2-, -CH=CH-, -OCH2-, -SCH2-, -SOCH2-, o -SO2CH2-; V es O, S, NH, o NZ, o amino ácido ligado a N-terminal, halogeno, o H cuando R1 está ausente; R1 está ausente, -H, alquilo C1-8, alquenillo C2-8, alquinilo C2-8, cicloalquilo C3-12, arilo C6-12, arilalquilo C7-14, -(CH2)nOZ, -C(O)Z, -C(O)OZ, -C(O)NHZ, -C(O)N(Z)2, -(CR1AR1B)r2OPO(OZ)2, -(CR2AR2B)r3PO(OZ)2, o aminoácido ligado a C-terminal; cada R1A, R1B, R2A y R2B es, de manera independiente, H o alquilo C1-5; cada Z es, de manera independiente, -H, alquilo C1-8, alqcicloalquilo C4-12, alqheterociclilo C3-9, donde el heterociclilo es de 3 a 9 miembros, cicloalquilo C3-12, arilo C6-12, arilalquilo C7-14, heterociclilo 3 a 9 miembros aromático o no aromático, alquenilo C2-8, o alquinilo C2-8, o dos Z, junto con el átomo(s) al cual cada uno está adherido, se juntan para formar un heterociclo de 3 a 7 miembros aromático o no aromático; cada n es 1 o 2; cada r2 es un numero entero entre 1-3; cada r3 es un numero entero entre 0-2; R2 y R3 son cada uno, de manera independiente, -H, -D, -OH, -halogeno, -CN, -NO2, -SH, -CF3, alquilo C1-8, alquenilo C2-8, alquinilo C2-8, cicloalquilo C3-12, arilo C6-12, arilalquilo C7-14, heterociclilo de 3 a 9 miembros aromático o no aromático, -OZ, -N(Z)2, -C(NH)N(Z)2, -O(CH2)nOZ, -C(O)Z, -OC(O)Z, -OC(O)OZ, -OC(O)N(Z)2, -C(O)N(Z)2, -C(O)OZ, -SZ, -SOZ, -S(O)2Z, -NHC(O)Z, -NHS(O)2Z, -NHC(NH)N(Z)2, -NZC(NH)N(Z)2, - NHC(NCN)N(Z)2, -NZC(NCN)N(Z)2, o -PO(OZ)2, o R2 y R3, junto con el átomo al cual cada uno está adherido, se juntan para formar un carbociclo o heterociclo de 5 o 6 miembros aromático o no aromático; A1 y A2 son cada uno, de manera independiente, -H, -D, -halogeno, alquilo C1-8, alquenilo C2-8, alquinilo C2-8, cicloalquilo C3-12, -arilo C6-12, o arilalquilo C7-14; A3 es un anillo heterocíclico aromático seleccionado entre el grupo integrado por los fragmentos A-1 a A-4; Q2, Q5 y Q6 son cada uno, de manera independiente, N, N+-O-, o C; Q3 y Q4 son cada uno, de manera independiente, N, N+-O-, C, O, o S, donde solamente uno de Q3 y Q4 puede ser O u S; donde Q2, Q3, Q4, Q5 y Q6 simultáneamente son C solo si R4 y R5, R5 y R6, R6 y R7, o R7 y R8, junto con los átomos al cual cada uno está adherido, se unen para formar un heterociclilo de 5 a 6 miembros aromático o no aromático; y R4, R5, R6, R7 y R8 son cada uno, de manera independiente, ausente, -H, -D, -OH, -O, -halogeno, -CN, -NO2, -SH, alquilo C1-8, alquenilo C2-8, alquinilo C2-8, cicloalquilo C3-12, arilo C6-12, arilalquilo C7-14, heterociclilo de 3 a 9 miembros aromático o no aromático, -OZ, -N(Z)2, -C(NH)N(Z)2, -O(CH2)nOZ, -C(O)Z, -OC(O)Z, -OC(O)OZ, -OC(O)N(Z)2, -C(O)N(Z)2, -C(O)OZ, -SZ, -SOZ, -S(O)2Z, -NHC(O)Z, -NHS(O)2Z, -NHC(NH)N(Z)2, -NZC(NH)N(Z)2, -NHC(NCN)N(Z)2, -NZC(NCN)N(Z)2, -PO(OZ)2, o R4 y R5, o R5 y R6, o R6 y R7, o R7 y R8, junto con los átomos al cual cada uno está adherido, se unen para formar un carbociclo o heterociclo de 5 a 6 miembros aromático o no aromático siempre y cuando el sistema anular resultante no esté sustituido o bencimidazol no sustituido, no sustituido benzotiazol, imidazo[1,2-a]piridina no sustituido, 5- o 6- cloro-imidazo[1,2-a]piridina, indol cuando R2 es C(O)OCH2CH3, quinolina no sustituido, quinolina 8-sustituida, quinoxalina no sustituido, 2- o 4-cloro-quinolina, 2-cloro-7-metil-quinolina o 2-piperidin-1-il-quinolina cuando R3 es NH2, o 4-hidroxi-1,3-quinazolina, donde cuando A3 es piridina-2-il no sustituido y A1, y A2 son cada uno -H, R3 no es -H, -OH, -NH2, -CF3, alquilo C1-3, fenilo, difluorobencil, -NHC(O)furan, -NHC(O)CH3, o -NHC(O)CH2CH3; donde cuando A3 es piridina-4-il no sustituido y A1 y A2 son cada uno -H, R3 no es -H, -OH, -NH2, -CH3, -CH2CH2CH3, o difluorobencil; donde cuando A3 es no sustituido, 6-cloro, o 2,6-dicloro piridina-3-il y A1 y A2 son cada uno -H, R3 no es -H, -OH, -NH2, -CF3, alquilo C1-3, fenilo, -C(O)OCH2CH3, o -NHC(O)CH3; donde cuando A3 es pirazol-1-il sustituido o no sustituido, R3 no es -OH; y donde A3 no es 4-NO2-imidazol-2-il.
ARP100101785A 2009-05-21 2010-05-21 Pirimidinas como agentes terapeuticos AR076601A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US18025309P 2009-05-21 2009-05-21
US28500309P 2009-12-09 2009-12-09
US28962809P 2009-12-23 2009-12-23

Publications (1)

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AR076601A1 true AR076601A1 (es) 2011-06-22

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US (2) US9040538B2 (es)
EP (1) EP2432776B1 (es)
AR (1) AR076601A1 (es)
CA (1) CA2762680C (es)
TW (1) TW201100411A (es)
WO (1) WO2010132999A1 (es)

Families Citing this family (44)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9040538B2 (en) 2009-05-21 2015-05-26 Universite Laval Pyrimidines as novel therapeutic agents
RS56080B1 (sr) 2010-01-15 2017-10-31 Inserm (Institut Nat De La Santé Et De La Rech Médicale) Inhibitori nkcc za lečenje autizma
MX351368B (es) 2010-05-26 2017-10-12 Sunovion Pharmaceuticals Inc Compuestos heteroarilo y metodos para utilizarlos.
CN102070553B (zh) * 2010-12-17 2013-08-07 西安瑞联近代电子材料有限责任公司 一种噻唑-4-甲醛的合成方法
BR112013028895A2 (pt) 2011-05-10 2016-08-09 Bayer Ip Gmbh (tio)carbonilamidinas bicíclicas
DE102012200354A1 (de) 2012-01-11 2013-07-11 Bayer Intellectual Property Gmbh Heteroaryl-substituierte Pyrazolopyridine und ihre Verwendung
JP6109161B2 (ja) 2011-07-06 2017-04-05 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングＢａｙｅｒ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ ＧｍｂＨ ヘテロアリール置換ピラゾロピリジン類およびその使用
DK2746265T3 (da) 2011-08-18 2016-02-01 Nippon Shinyaku Co Ltd Heterocyclisk derivat som mikrosomal prostaglandin-E-syntase-(mPGEs)-inhibitor
DE102012200349A1 (de) 2012-01-11 2013-07-11 Bayer Intellectual Property Gmbh Substituierte annellierte Pyrimidine und Triazine und ihre Verwendung
DE102012200360A1 (de) 2012-01-11 2013-07-11 Bayer Intellectual Property Gmbh Substituierte Triazine und ihre Verwendung
JP6140738B2 (ja) 2012-03-06 2017-05-31 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングＢａｙｅｒ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ ＧｍｂＨ 置換アザ二環およびその使用
EP2732815A1 (en) 2012-11-16 2014-05-21 Neurochlore Modulators of intracellular chloride concentration for treating fragile X syndrome
WO2014139983A1 (en) 2013-03-13 2014-09-18 H. Lundbeck A/S [1,2,4]triazolo[4,3-a]quinoxalines as dual pde2/pde10 inhibitors
KR20150140381A (ko) 2013-04-12 2015-12-15 바이엘 크롭사이언스 악티엔게젤샤프트 신규 트리아졸 유도체
MX2015014365A (es) 2013-04-12 2015-12-07 Bayer Cropscience Ag Derivados de triazol novedosos.
BR112015025331A2 (pt) 2013-04-12 2017-07-18 Bayer Cropscience Ag novos derivados de triazolintiona
BR112015027395A2 (pt) 2013-05-14 2017-08-29 Active Biotech Ab Composto, composição farmacêutica, e, método para tratar uma doença ou condição
UY35652A (es) 2013-07-10 2015-01-30 Bayer Pharma AG Bencil-1h-pirazolo[3,4-b]piridinas y su uso
CN104693114B (zh) * 2013-12-10 2019-08-16 四川海思科制药有限公司 一种贝曲西班的改进的制备方法
RU2537848C1 (ru) * 2013-12-10 2015-01-10 Федеральное государственное казенное учреждение "33 Центральный научно-исследовательский испытательный институт Министерства обороны Российской Федерации" Способ получения 2-хлор-5-гидроксиметилпиридина
CN106255414A (zh) * 2014-01-17 2016-12-21 瓦伦特生物科学公司 S‑苄硫尿嘧啶化合物以及增强植物根部生长的方法
WO2016025778A1 (en) 2014-08-15 2016-02-18 The Johns Hopkins University Compositions and methods for treating refractory seizures
DK3186242T3 (da) * 2014-08-29 2021-12-20 Tes Pharma S R L Alfa-amino-beta-carboxymuconsyre-semialdehyd-decarboxylasehæmmere
CN104478795A (zh) * 2014-11-24 2015-04-01 苏州乔纳森新材料科技有限公司 一种2-氯烟醛的制备方法
WO2016156294A1 (en) 2015-04-02 2016-10-06 Bayer Cropscience Aktiengesellschaft Triazol derivatives as fungicides
US10231453B2 (en) 2015-04-02 2019-03-19 Bayer Cropscience Aktiengesellschaft 5-substituted imidazole derivatives
CA3001974A1 (en) 2015-10-14 2017-04-20 Bristol-Myers Squibb Company 2,4-dihydroxy-nicotinamides as apj agonists
JP6948322B2 (ja) 2015-12-16 2021-10-13 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ Ａｐｊ受容体のａｐｊアゴニストとしてのヘテロアリールヒドロキシピリミジノン
AU2017238504B2 (en) 2016-03-24 2021-05-27 Bristol-Myers Squibb Company 6-hydroxy-4-oxo-1,4-dihydropyrimidine-5-carboxamides as APJ agonists
EP3484876A1 (en) 2016-07-14 2019-05-22 Pfizer Inc Novel pyrimidine carboxamides as inhibitors of vanin-1 enzyme
EP3512338A1 (en) 2016-09-13 2019-07-24 Bayer CropScience Aktiengesellschaft Active compound combinations comprising a 5-substituted imidazole derivative
EP3519408A1 (en) 2016-09-29 2019-08-07 Bayer CropScience Aktiengesellschaft 1 -[2-(1 -chlorocyclopropyl)-2-hydroxy-3-(3-phenyl-1,2-oxazol-5-yl)propyl]-1h-imidazole-5-carbonitrile derivatives and related compounds as fungicides for crop protection
BR112019006450A2 (pt) 2016-09-29 2019-06-25 Bayer Cropscience Ag novos derivados de imidazolilmetila substituídos na posição 5
CN109890795A (zh) 2016-09-29 2019-06-14 拜耳作物科学股份公司 新的5-取代的咪唑衍生物
CN106946772B (zh) * 2016-11-02 2019-08-06 河南省商业科学研究所有限责任公司 一种2,2’-联吡啶-4,4’-甲酸甲酯的合成方法
RU2762833C2 (ru) * 2017-03-17 2021-12-23 Мейдзи Сейка Фарма Ко., Лтд. Средство для борьбы с болезнями растений
RU2733723C1 (ru) 2017-03-24 2020-10-06 Ст Фарм Ко., Лтд. Новое пирролопиридиновое соединение, способ его получения и его применение
HUE059057T2 (hu) * 2017-05-04 2022-10-28 Bayer Cropscience Ag 2-{[2-(feniloximetil)piridin-5-il]oxi}-etánamin-származékok és rokon vegyületek mint peszticidek, például növényvédelemre
CN107286083A (zh) * 2017-06-16 2017-10-24 康化（上海）新药研发有限公司 一种2‑氯‑6‑溴‑3‑吡啶甲醛的合成方法
WO2019092086A1 (en) 2017-11-13 2019-05-16 Bayer Aktiengesellschaft Tetrazolylpropyl derivatives and their use as fungicides
US10300100B1 (en) 2018-09-27 2019-05-28 King Saud University Extract of Vicia faba beans
JP2022550297A (ja) 2019-09-25 2022-12-01 ファイザー・インク Ｓｔｉｎｇ（インターフェロン遺伝子刺激因子）のヘテロ多環式モジュレーター
US11964978B2 (en) 2021-03-18 2024-04-23 Pfizer Inc. Modulators of STING (stimulator of interferon genes)
WO2023196614A1 (en) * 2022-04-08 2023-10-12 Axonis Therapeutics, Inc. Methods and compounds for treating neurological disorders

Family Cites Families (38)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3369514D1 (en) 1983-05-05 1987-03-05 Heumann Ludwig & Co Gmbh Pyrimidinethioalkyl pyridine derivatives, process for their preparation and medicines containing these compounds
HU203736B (en) 1989-04-06 1991-09-30 Gyogyszerkutato Intezet Process for producing new thiouracil-derivatives and pharmaceutical compositions containing them
US5472967A (en) * 1991-02-20 1995-12-05 Synthelabo 4-pyrimidinone derivatives their preparation and their application in therapy
JPH06206805A (ja) * 1992-02-17 1994-07-26 Hisamitsu Pharmaceut Co Inc チロシナーゼ阻害剤及びそれを用いた皮膚外用剤
US5464854A (en) 1993-11-11 1995-11-07 Depadova; Anathony S. Method of modifying ovarian hormone-regulated AT1 receptor activity as treatment of incapacitating symptom(s) of P.M.S.
KR100354309B1 (ko) 1993-11-12 2003-01-06 파마시아 앤드 업존 캄파니 피리미딘-티오알킬및알킬에테르화합물
GB9420557D0 (en) 1994-10-12 1994-11-30 Zeneca Ltd Aromatic compounds
UA56992C2 (uk) 1995-05-08 2003-06-16 Фармація Енд Апджон Компані <font face="Symbol">a</font>-ПІРИМІДИНТІОАЛКІЛЗАМІЩЕНІ ТА <font face="Symbol">a</font>-ПІРИМІДИНОКСОАЛКІЛЗАМІЩЕНІ СПОЛУКИ
PL334194A1 (en) 1996-12-20 2000-02-14 Byk Gulden Lomberg Chem Fab Imidazopyridazines
AR023071A1 (es) 1998-12-23 2002-09-04 Syngenta Participations Ag Compuestos de piridincetona, compuestos intermediarios, composicion herbicida e inhibidora del crecimiento de plantas, metodo para controlar la vegetacion indeseada, metodo para inhibir el crecimiento de las plantas, y uso de la composicion para controlar el crecimiento indeseado de plantas.
GB2359081A (en) * 2000-02-11 2001-08-15 Astrazeneca Uk Ltd Pharmaceutically active thiazolopyrimidines
GT200100103A (es) 2000-06-09 2002-02-21 Nuevos herbicidas
CA2443697A1 (en) 2001-04-13 2002-10-24 Pier F. Cirillo 1,4-disubstituted benzo-fused compounds
CA2445003A1 (en) 2001-05-16 2002-11-21 Boehringer Ingelheim Pharmaceuticals, Inc. Diarylurea derivatives useful as anti-inflammatory agents
US7138404B2 (en) * 2001-05-23 2006-11-21 Hoffmann-La Roche Inc. 4-aminopyrimidine derivatives
JP4424983B2 (ja) 2001-06-05 2010-03-03 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド １，４−ジ置換ベンゾ−縮合シクロアルキルウレア化合物
US6921762B2 (en) 2001-11-16 2005-07-26 Amgen Inc. Substituted indolizine-like compounds and methods of use
JP2003206230A (ja) 2002-01-10 2003-07-22 Yamanouchi Pharmaceut Co Ltd シアノヘテロ環誘導体又はその塩
CA2494824A1 (en) 2002-08-08 2004-02-19 Boehringer Ingelheim Pharmaceuticals, Inc. Fluorinated phenyl-naphthalenyl-urea compounds as inhibitors of cytokines involved in inflammatory processes
PT1601653E (pt) 2003-03-07 2009-04-27 Syngenta Participations Ag Processo para a produção de ésteres de ácido nicotínico substituído
US7078419B2 (en) 2003-03-10 2006-07-18 Boehringer Ingelheim Pharmaceuticals, Inc. Cytokine inhibitors
US20050124637A1 (en) * 2003-08-15 2005-06-09 Irm Llc Compounds and compositions as inhibitors of receptor tyrosine kinase activity
JP4534452B2 (ja) * 2003-09-04 2010-09-01 株式会社クレハ ３−メチルイソチアゾール−５−メタノール誘導体、その製造法および農園芸用病害防除剤
EP1664000A1 (en) * 2003-09-12 2006-06-07 Arpida A/S Isoxazoles as peptide deformylase inhibitors
CN102796081B (zh) 2004-08-28 2015-04-22 阿斯利康(瑞典)有限公司 作为趋化因子受体调节剂的嘧啶磺酰胺衍生物
EP1789413A1 (en) 2004-09-13 2007-05-30 Amgen Inc. Vanilloid receptor ligands and their use in treatments
WO2006040558A1 (en) * 2004-10-15 2006-04-20 Astrazeneca Ab Substituted adenines and the use thereof
AU2005310979A1 (en) 2004-11-16 2006-06-08 Bellus Health (International) Limited Compounds for the treatment of CNS and amyloid associated diseases
CA2600067A1 (en) 2005-03-04 2006-09-14 Alsgen, Inc. Treatment of amyotrophic lateral sclerosis with pyrimethamine and analogues 6
US20070135437A1 (en) 2005-03-04 2007-06-14 Alsgen, Inc. Modulation of neurodegenerative diseases
AR053347A1 (es) 2005-04-06 2007-05-02 Astrazeneca Ab Derivados de [1,3]tiazolo[4,5-d]pirimidin-2(3h)-ona 5,7-sustituidos
UA90707C2 (en) 2005-04-06 2010-05-25 Астразенека Аб Novel 5-substituted 7-amino-[1,3]thiazolo[4,5-d]pyrimidine derivatives
US8686045B2 (en) 2005-06-08 2014-04-01 The University Of North Carolina At Chapel Hill Methods of facilitating neural cell survival using non-peptide and peptide BDNF neurotrophin mimetics
TW200806675A (en) 2006-01-30 2008-02-01 Array Biopharma Inc Heterobicyclic thiophene compounds and methods of use
PT2562162E (pt) * 2008-01-22 2015-10-21 Dow Agrosciences Llc Derivados de n-ciano-4-amino-5-fluoro-pirimidina como fungicidas
JP5290406B2 (ja) 2008-09-04 2013-09-18 田辺三菱製薬株式会社 三置換ピリミジン化合物及びそのｐｄｅ１０阻害薬としての使用
WO2010030027A1 (en) * 2008-09-10 2010-03-18 Mitsubishi Tanabe Pharma Corporation Aromatic nitrogen-containing 6-membered ring compounds and their use
US9040538B2 (en) 2009-05-21 2015-05-26 Universite Laval Pyrimidines as novel therapeutic agents

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