ES2660249T3 - Compuestos de tipo triazolona y sus usos - Google Patents

Compuestos de tipo triazolona y sus usos Download PDF

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Publication number
ES2660249T3
ES2660249T3 ES13863783T ES13863783T ES2660249T3 ES 2660249 T3 ES2660249 T3 ES 2660249T3 ES 13863783 T ES13863783 T ES 13863783T ES 13863783 T ES13863783 T ES 13863783T ES 2660249 T3 ES2660249 T3 ES 2660249T3
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Prior art keywords
alkyl
cycloalkyl
halogen
heteroaromatic ring
heteroaryl
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ES13863783T
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English (en)
Inventor
Nicholas Simon Stock
Austin Chih-Yu Chen
Yalda Mostofi Bravo
Jason Duarte Jacintho
Jill Melissa Baccei
Brian Andrew Stearns
Ryan Christopher Clark
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Inception 2 Inc
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Inception 2 Inc
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C07D249/10—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles 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
    • C07D249/12—Oxygen or sulfur atoms
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4196—1,2,4-Triazoles
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D401/10—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 carbon chain containing aromatic 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
    • C07D403/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D403/10—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 carbon chain containing aromatic rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Communicable Diseases (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Virology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Un compuesto de fórmula I**Fórmula** o una sal farmacéuticamente aceptable de este donde: A1 es un anillo fenilo o un anillo heteroaromático de 6 miembros que tiene 1, 2 o 3 N en el anillo heteroaromático; A2 se selecciona entre A2a o A2b**Fórmula** donde A2a es un anillo fenilo o un anillo heteroaromático de 6 miembros que tiene 1, 2 o 3 N en el anillo heteroaromático, y A2b es un anillo heteroaromático de 5 miembros que tiene 1, 2 o 3 heteroátomos seleccionados de manera independiente entre O, S y N; X se selecciona a partir del grupo constituido por -(CH2)2-, -(CH2)3-, -(CH2)4-, y -(CH2)m-O-(CH2)n-, mono- o disustituido de manera opcional con halógeno, donde m y n son de manera independiente 0, 1, 2, 3 o 4, siempre que m+n sea 2, 3 o 4; Y es O; R1 y R2 se seleccionan cada uno de manera independiente a partir del grupo constituido por: (a) hidrógeno, (b) halógeno, (c) CN, (d) CF3, (e) -alquilo C1-6, (f) -(alquilo C1-6)-C(>=O)OH, (g) -O-(R7), (h) -S(>=O)oR7, (i) -N(R7)(R8), (j) -N(R7)-C(>=O)-(R8), (k) -N(R7)-C(>=O)-O-(R8), (l) -N(R7)S(>=O)2(R8), (m) -(cicloalquilo C3-6), (n) -C(>=O)(R7), (o) arilo, (p) heteroarilo, (q) -OC(>=O)N(R7)(R8), (r) -S(>=O)2N(R7)(R8), (s) -C(>=O)N(R7)(R8) y (t) -C(R7)(R8)OH, donde la porción alquilo de las opciones (e) y (f), y la porción cicloalquilo de la opción (m) están sustituidas de manera opcional con halógeno, y donde el arilo de la opción (o) y el heteroarilo de la opción (p) están mono- o disustituidos de manera opcional con sustituyentes seleccionados entre halógeno, nitro, alquilo C1-6, alcoxi C1-6, haloalquilo C1-6, cicloalquilo C3-6, cicloalcoxi C3-6, -NH(alquilo C1-6), -NH(cicloalquilo C3-6), -N(alquilo C1-6)2, -N(cicloalquilo C3-6)2, -S(>=O)o(alquilo C1-6), - S(>=O)o(cicloalquilo C3-6) y CN; R3 se selecciona a partir del grupo constituido por: (a) hidrógeno, (b) halógeno, (c) CN, (d) CF3, (e) -alquilo C1-6, (f) -(alquilo C1-6)-C(>=O)OH, (g) -O-(R7), (h) -S(>=O)oR7 (i) -N(R7)(R8), (j) -N(R7)-C(>=O)-(R8), (k) -N(R7)-C(>=O)-O-(R8), (l) -N(R7)S(>=O)2(R8), (m) -(cicloalquilo C3-6), (n) -C(>=O)(R7), (o) arilo, (p) heteroarilo, (q) -OC(>=O)N(R7)(R8), (r) -S(>=O)2N(R7)(R8), (s) -C(>=O)N(R7)(R8), (t) -C(R7)(R8)OH, (u) -NHC(>=O)-N(R7)(R8), (v) -(cicloalquil C3-6)-COOH, (w) heterociclo y (x) -(alquil C1-6)C(>=O)-N(R7)(R8), donde la porción alquilo de las opciones (e), (f) y (x), y la porción cicloalquilo de las opciones (m) y (v) están sustituidas de manera opcional con halógeno o hidroxilo, y
ES13863783T 2012-12-20 2013-12-10 Compuestos de tipo triazolona y sus usos Active ES2660249T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261739906P 2012-12-20 2012-12-20
PCT/US2013/074197 WO2014099503A1 (en) 2012-12-20 2013-12-10 Triazolone compounds and uses thereof

Publications (1)

Publication Number Publication Date
ES2660249T3 true ES2660249T3 (es) 2018-03-21

Family

ID=50979036

Family Applications (1)

Application Number Title Priority Date Filing Date
ES13863783T Active ES2660249T3 (es) 2012-12-20 2013-12-10 Compuestos de tipo triazolona y sus usos

Country Status (18)

Country Link
US (4) US9676754B2 (es)
EP (1) EP2935228B9 (es)
JP (1) JP6404230B2 (es)
KR (1) KR102300675B1 (es)
CN (1) CN104918922B (es)
AU (1) AU2013363398B2 (es)
BR (1) BR112015013350B1 (es)
CA (1) CA2894281C (es)
DK (1) DK2935228T3 (es)
EA (1) EA027986B9 (es)
ES (1) ES2660249T3 (es)
HK (1) HK1212680A1 (es)
IL (1) IL239372B (es)
MX (1) MX2015007433A (es)
NO (1) NO3003327T3 (es)
PE (1) PE20151521A1 (es)
SG (1) SG11201504622PA (es)
WO (1) WO2014099503A1 (es)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR112015013350B1 (pt) 2012-12-20 2022-04-05 Tempest Therapeutics, Inc Composto ou sal farmaceuticamente aceitável do mesmo, composição farmacêutica e respectivos usos
KR20160048988A (ko) * 2013-09-06 2016-05-04 인셉션 2 인코퍼레이티드 트라이아졸론 화합물 및 이의 용도
WO2022052982A1 (zh) * 2020-09-14 2022-03-17 昭明泽康（北京）生物医药科技有限公司 PPARα（过氧化物酶体增殖物激活受体α）配体在制备药物中的应用
WO2024102620A2 (en) * 2022-11-09 2024-05-16 Tempest Therapeutics, Inc. Triazolone compounds and uses thereof

Family Cites Families (139)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE160447C (es)
FI76795C (fi) 1979-09-04 1988-12-12 Bristol Myers Co Foerfarande foer framstaellning av nya, terapeutiskt anvaendbara 3,4-disubstituerade 1,2,5-tiadiazol-1-oxider och -1,1-dioxider samt nya mellanprodukter.
US4487773A (en) 1981-03-16 1984-12-11 Mead Johnson & Company 1,2,4-Triazol-3-one antidepressants
IN158869B (es) 1981-03-18 1987-02-07 Ici Plc
DD160447A1 (de) 1981-03-26 1983-08-03 Johannes Dost Herbizide mittel, die 1,2,4-triazolinone-(5) enthalten
EP0067508B1 (en) 1981-05-18 1985-10-30 Imperial Chemical Industries Plc Amidine derivatives
DE3238590A1 (de) 1982-10-19 1984-04-19 VEB Fahlberg-List Chemische und pharmazeutische Fabriken, DDR 3013 Magdeburg Herbizide mittel, die 1,2,4-triazolinone-(5) enthalten
NL8204109A (nl) 1982-10-25 1984-05-16 Fahlberg List Veb Herbicide middelen, die 1.2.4-triazolinon-(5)-verbindingen bevatten.
BE894856A (fr) 1982-10-28 1983-02-14 Fahlberg List Veb Compositions herbicides a base d'un derive de la 1,2,4-triazolinone-(5)
FR2535168B1 (fr) 1982-10-29 1985-08-09 Fahlberg List Veb Agents herbicides a base de 1, 2, 4-triazolinone 5
JPS60215675A (ja) 1984-04-09 1985-10-29 Nippon Nohyaku Co Ltd オキサジアゾリノン誘導体及びトリアゾリノン誘導体並びにその製造方法並びに昆虫成長制御剤
JP2542880B2 (ja) 1986-12-19 1996-10-09 メレルダウファーマスーティカルズ インコーポレーテッド ５−アリ―ル−３ｈ−１，２，４，−トリアゾ―ル−３−オン類の抗痙攣剤としての用途
DE3934081A1 (de) 1989-10-12 1991-04-18 Bayer Ag Sulfonylaminocarbonyltriazolinone
DE69132735T2 (de) 1990-09-06 2002-05-29 Pfizer Inc., New York Anti-muscarin bronchodilatoren
JP2772875B2 (ja) 1991-05-14 1998-07-09 富士写真フイルム株式会社 ハロゲン化銀カラー写真感光材料の処理方法及び写真用漂白定着組成物
PT612314E (pt) 1991-10-30 2000-06-30 Astra Ab Derivados de etilamina 2-heterociclicos e seu uso como produtos farmaceuticos
EP0636130A1 (en) 1992-04-15 1995-02-01 Merck Sharp & Dohme Ltd. Azacyclic compounds
DE4224929A1 (de) 1992-07-28 1994-02-03 Bayer Ag Heterocyclyltriazolinone
US5284957A (en) 1992-09-03 1994-02-08 Eli Lilly And Company Excitatory amino acid receptor antagonists
IT1256387B (it) 1992-11-13 1995-12-04 Acraf Procedimento per preparare triazoloni
US5783593A (en) 1993-11-04 1998-07-21 Abbott Laboratories Inhibitors of squalene synthetase and protein farnesyltransferase
DE4343595A1 (de) 1993-12-21 1995-06-22 Bayer Ag Verfahren zur Herstellung von Sulfonylaminocarbonyltriazolinonen
US5550118A (en) 1994-01-31 1996-08-27 Eli Lilly And Company Polyhydronorharman synthase inhibitors
DE4404848A1 (de) 1994-02-16 1995-08-17 Hoechst Ag Substituierte Cyclohexanolester, ihre Verwendung zur Behandlung von Krankheiten und pharmazeutische Präparate
US5464788A (en) 1994-03-24 1995-11-07 Merck & Co., Inc. Tocolytic oxytocin receptor antagonists
GB9418545D0 (en) 1994-09-15 1994-11-02 Merck Sharp & Dohme Therapeutic agents
JPH08157473A (ja) 1994-10-06 1996-06-18 Nissan Chem Ind Ltd ピラゾール系チアゾリジン類
US5641796A (en) 1994-11-01 1997-06-24 Eli Lilly And Company Oral hypoglycemic agents
IN183333B (es) 1995-03-15 1999-11-20 Indian Drugs & Pharma
IL118325A0 (en) 1995-05-25 1996-10-31 Pont Merck And Pharmaceutical Integrin receptor antagonists and pharmaceutical compositions containing them
DE19521162A1 (de) 1995-06-09 1996-12-12 Bayer Ag N-Aryl-1,2,4-triazolin-5-one
GB9513121D0 (en) 1995-06-28 1995-08-30 Merck Sharp & Dohme Therapeutic agents
GB9513117D0 (en) 1995-06-28 1995-08-30 Merck Sharp & Dohme Therapeutic agents
EP0784053A1 (de) 1996-01-15 1997-07-16 Degussa Aktiengesellschaft Verfahren zur Herstellung von Triazolinonherbiziden
DE19601189A1 (de) 1996-01-15 1997-07-17 Degussa Verfahren zur Herstellung von 1,2,4-Triazolin-3(2H)-onen
JP2000511883A (ja) 1996-04-19 2000-09-12 ノボ ノルディスク アクティーゼルスカブ ホスホチロシン認識ユニットを有する分子のモジュレーター
TW467902B (en) 1996-07-31 2001-12-11 Bristol Myers Squibb Co Diphenyl heterocycles as potassium channel modulators
CA2266773A1 (en) 1996-10-07 1998-04-16 Merck Sharp & Dohme Limited Use of a nk-1 receptor antagonist and an antidepressant and/or an anti-anxiety agent
WO1998018496A2 (en) 1996-10-28 1998-05-07 Nycomed Imaging As Contrast agents
US6214834B1 (en) 1997-03-28 2001-04-10 Dupont Pharmaceuticals Company Integrin inhibitor prodrugs
AU8242598A (en) 1997-07-18 1999-02-10 Nippon Kayaku Kabushiki Kaisha Aromatic ketone derivatives and uses thereof
EP1049693A1 (en) 1997-11-26 2000-11-08 Du Pont Pharmaceuticals Company 1,3,4-THIADIAZOLES AND 1,3,4-OXADIAZOLES AS $g(a) v?$g(b) 3? ANTAGONISTS
WO1999062880A1 (en) 1998-06-03 1999-12-09 Gpi Nil Holdings, Inc. N-linked sulfonamides of n-heterocyclic carboxylic acids or carboxylic acid isosteres
US6331537B1 (en) 1998-06-03 2001-12-18 Gpi Nil Holdings, Inc. Carboxylic acids and carboxylic acid isosteres of N-heterocyclic compounds
WO1999062888A1 (en) 1998-06-03 1999-12-09 Gpi Nil Holdings, Inc. Aza-heterocyclic compounds used to treat neurological disorders and hair loss
US6339101B1 (en) 1998-08-14 2002-01-15 Gpi Nil Holdings, Inc. N-linked sulfonamides of N-heterocyclic carboxylic acids or isosteres for vision and memory disorders
CA2336152A1 (en) 1998-08-14 2000-02-24 Gpi Nil Holdings, Inc. Ureas and carbamates of n-heterocyclic carboxylic acids and isosteres for vision and memory disorders
US7265150B1 (en) 1998-08-14 2007-09-04 Gpi Nil Holdings Inc. Carboxylic acids and carboxylic acid isosteres of N-heterocyclic compounds for vision and memory disorders
SE9802937D0 (sv) * 1998-09-01 1998-09-01 Astra Pharma Prod Novel compounds
AU1345600A (en) 1998-11-12 2000-06-05 Merck & Co., Inc. Pyrimidinedione derivatives useful as alpha 1a adrenoceptor antagonists
FR2793791B1 (fr) 1999-05-19 2002-01-25 Univ Paris 7 Denis Diderot Nouveaux composes inhibiteurs specifiques de phospholipases a2
US6455525B1 (en) 1999-11-04 2002-09-24 Cephalon, Inc. Heterocyclic substituted pyrazolones
DE19955662B4 (de) 1999-11-19 2011-03-31 Arysta LifeScience North America, Herbizide auf Basis von Carbamoyltriazolinon
EP1110958A1 (en) 1999-12-20 2001-06-27 Ucb, S.A. Alpha-arylethylpiperazine derivatives as neurokinin antagonists
AU6594401A (en) 2000-05-24 2001-12-03 Bayer Aktiengesellschaft 6-heterocyclyl-3-oxo-3,4-dihydro-quinoxalines
US6465456B2 (en) 2000-06-29 2002-10-15 Bristol-Myers Squibb Company Isoxazolinone antibacterial agents
JO2654B1 (en) 2000-09-04 2012-06-17 شركة جانسين فارماسوتيكا ان. في Multiple aryl caroxa amides are useful as lipid - lowering agents
US6576644B2 (en) 2000-09-06 2003-06-10 Bristol-Myers Squibb Co. Quinoline inhibitors of cGMP phosphodiesterase
UA82048C2 (uk) * 2000-11-10 2008-03-11 Эли Лилли Энд Компани Агоністи альфа-рецепторів, активованих проліфератором пероксисом
US7196095B2 (en) 2001-06-25 2007-03-27 Merck & Co., Inc. (Pyrimidinyl) (phenyl) substituted fused heteroaryl p38 inhibiting and PKG kinase inhibiting compounds
DE60222698T2 (de) 2001-12-18 2008-06-19 Merck & Co., Inc. Heteroarylsubstituierte triazolmodulatoren des metabotropen glutamatarezeptors 5
ES2311711T3 (es) 2002-02-07 2009-02-16 The Curators Of The University Of Missouri Compuestos de 4-(3-hidroxifenil) o 4-(3-alcoxifenil)-1,2,4-triazol activos como receptores de opioides.
US6995144B2 (en) 2002-03-14 2006-02-07 Eisai Co., Ltd. Nitrogen containing heterocyclic compounds and medicines containing the same
US20050256003A1 (en) 2002-06-14 2005-11-17 Christoph Luthy Novel herbicides
EP1558581A4 (en) * 2002-10-07 2007-07-25 Bristol Myers Squibb Co DERIVATIVES OF TRIAZOLONE AND TRIAZOLETHIONE
MXPA05003830A (es) 2002-10-11 2005-06-23 Cytokinetics Inc Compuestos, composiciones y metodos.
AU2003300031A1 (en) 2002-10-11 2004-05-04 Cytokinetics, Inc. Compounds, compositions, and methods
TW200423930A (en) 2003-02-18 2004-11-16 Hoffmann La Roche Non-nucleoside reverse transcriptase inhibitors
CA2521396A1 (en) 2003-04-04 2004-10-21 Merck & Co., Inc. Di-aryl substituted triazole modulators of metabotropic glutamate receptor-5
DK1615647T3 (da) 2003-04-11 2010-04-06 High Point Pharmaceuticals Llc Farmaceutisk anvendelse af kondenserede 1,2,4-triazoler
UA89035C2 (ru) 2003-12-03 2009-12-25 Лео Фарма А/С Эфиры гидроксамовых кислот и их фармацевтическое применение
US7605171B2 (en) 2003-12-17 2009-10-20 Merck & Co., Inc. (3,4-disubstituted)propanoic carboxylates as S1P (Edg) receptor agonists
WO2005077345A1 (en) 2004-02-03 2005-08-25 Astrazeneca Ab Compounds for the treatment of gastro-esophageal reflux disease
WO2005077178A2 (en) 2004-02-16 2005-08-25 Syngenta Participations Ag Herbicidal composition
RU2006127575A (ru) 2004-02-18 2008-03-27 Астразенека Аб (Se) Соединение триазола и их применение в качестве антагонистов метаботропного рецептора глутамата
SE0400850D0 (sv) 2004-03-30 2004-03-31 Astrazeneca Ab Novel Compounds
EP1773790B1 (en) * 2004-07-27 2012-08-15 F.Hoffmann-La Roche Ag Benzyltriazolone compounds as non-nucleoside reverse transcriptase inhibitors
CN1315810C (zh) 2004-08-30 2007-05-16 北京理工大学 哌嗪桥联他克林双体衍生物及其合成方法
GT200500284A (es) 2004-10-15 2006-03-27 Aventis Pharma Inc Pirimidinas como antagonistas del receptor de prostaglandina d2
CA2583681A1 (en) 2004-10-22 2006-05-04 Merck & Co., Inc. 2-(aryl)azacyclylmethyl carboxylates, sulfonates, phosphonates, phosphinates and heterocycles as s1p receptor agonists
WO2006068199A1 (ja) 2004-12-22 2006-06-29 Mochida Pharmaceutical Co., Ltd. 代謝的に安定な３－オキシ－１，２，４－トリアゾール誘導体
ES2345997T3 (es) 2005-01-14 2010-10-07 Janssen Pharmaceutica Nv Pirazolopiramidinas como inhibidores de las quinasas del ciclo celular.
WO2006078698A1 (en) 2005-01-19 2006-07-27 Cengent Therapeutics, Inc. 2-imidazolone and 2-imidazolidinone heterocyclic inhibitors of tyrosine phosphatases
AR052888A1 (es) 2005-01-28 2007-04-11 Lilly Co Eli Uso del agonista alfa de ppar para preparar una formulacion farmaceutica, paquete y dosis unitaria de dicha formulacion
AU2006235706B2 (en) 2005-04-12 2012-03-08 Vicore Pharma Ab New tricyclic angiotensin II agonists
JPWO2006118219A1 (ja) 2005-04-28 2008-12-18 株式会社デンソー モータ及びその制御装置
DE102005025992A1 (de) 2005-06-07 2007-01-11 Lanxess Deutschland Gmbh Verfahren zur Herstellung von substituierten Azolen
US20070032488A1 (en) 2005-08-05 2007-02-08 Genelabs Technologies, Inc. 6-Membered aryl and heteroaryl derivatives for treating viruses
EP1953148B1 (en) 2005-10-28 2012-02-29 Takeda Pharmaceutical Company Limited Heterocyclic amide compound and use thereof
CA2630884A1 (en) 2005-11-30 2007-06-07 Vertex Pharmaceuticals Incorporated Inhibitors of c-met and uses thereof
DE102006003444A1 (de) 2006-01-25 2007-07-26 Lanxess Deutschland Gmbh Verfahren zur Herstellung von iodierten Azolen
GB2435829A (en) 2006-03-09 2007-09-12 Del Dr Esteve S A Spain Lab Pyrimidinyl-2-piperazine compounds for use in disorders related to food intake
GB2435828A (en) 2006-03-09 2007-09-12 Del Dr Esteve S A Spain Lab Use of substituted phenyl-piperazine compounds for treatment of food related disorders
GB2435827A (en) 2006-03-09 2007-09-12 Del Dr Esteve S A Spain Lab Use of substituted piperazine compounds for the treatment of food related disorders
US7674811B2 (en) 2006-03-14 2010-03-09 Ranbaxy Laboratories Limited 5-lipoxygenase inhibitors
NZ571271A (en) 2006-03-23 2011-10-28 Biota Europe Ltd The use of benzamide or pyridinamide derivatives as antibacterial agents
US7816522B2 (en) 2006-03-24 2010-10-19 Eisai Co., Ltd. Triazolone derivatives
DE102006023337A1 (de) * 2006-05-18 2007-11-22 Merck Patent Gmbh Triazolderivate II
AU2007267847B2 (en) 2006-05-25 2012-04-12 Synta Pharmaceuticals Corp. Triazole compounds that modulate Hsp90 activity
DE102006032164A1 (de) 2006-07-12 2008-01-24 Bayer Cropscience Ag Substituierte Furyl-sulfonylamino(thio)carbonyl-triazolin(thi)one
US7994321B2 (en) 2006-08-08 2011-08-09 Hoffmann-La Roche Inc. Substituted thieno[3,2-C]pyridine-7-carboxylic acid derivatives
PE20110341A1 (es) 2006-08-15 2011-06-21 Novartis Ag COMPUESTOS HETEROCICLICOS QUE MODULAN LA ACTIVIDAD DE LA ESTEROIL-CoA-DESATURASA
WO2008103574A2 (en) 2007-02-23 2008-08-28 Eli Lilly And Company Peroxisome proliferator activated receptor modulators
WO2008119662A1 (en) 2007-03-29 2008-10-09 F. Hoffmann-La Roche Ag Non-nucleoside reverse transcriptase inhibitors
WO2008128335A1 (en) 2007-04-20 2008-10-30 Merck Frosst Canada Ltd. Novel heteroaromatic compounds as inhibitors of stearoyl-coenzyme a delta-9 desaturase
EP2433496A1 (en) 2007-05-08 2012-03-28 Burnham Institute for Medical Research Tissue non-specific alkaline phosphatase inhibitors and uses thereof for treating vascular calcification
JP5457344B2 (ja) 2007-07-17 2014-04-02 アセア バイオサイエンシズ インコーポレイテッド 複素環式化合物および抗がん剤としての使用
CN101754962B (zh) 2007-07-19 2013-12-25 赛马拜制药公司 作为rup3或gpr119受体的激动剂治疗糖尿病和代谢性病症的n-氮杂环状经取代吡咯、吡唑、咪唑、***和四唑衍生物
EP2183227B1 (en) 2007-08-07 2014-09-24 Prosarix Limited 1,2,4-triazole derivatives as serotonergic modulators
EP2215065B1 (en) 2007-10-19 2012-07-11 Boehringer Ingelheim International GmbH Ccr10 antagonists
CN101896465A (zh) 2007-12-10 2010-11-24 7Tm制药联合股份有限公司 ***素受体调节剂
US20090281089A1 (en) 2008-04-11 2009-11-12 Genentech, Inc. Pyridyl inhibitors of hedgehog signalling
EP2913326B1 (en) 2008-05-14 2020-07-15 The Scripps Research Institute Novel modulators of sphingosine phosphate receptors
WO2009153496A2 (fr) 2008-05-26 2009-12-23 Genfit Composés agonistes ppar, préparation et utilisations
GB0810902D0 (en) 2008-06-13 2008-07-23 Astex Therapeutics Ltd New compounds
US7943796B2 (en) * 2008-07-31 2011-05-17 Chevron Oronise Company LLC Lubricating oil additive and lubricating oil composition containing same
CN101643451B (zh) 2008-08-07 2013-03-06 浙江海正药业股份有限公司 过氧化物酶增殖物激活受体亚型δ类激动剂化合物及其制备方法
JP2011231015A (ja) 2008-08-29 2011-11-17 Taiho Yakuhin Kogyo Kk 含窒素複素環を有する新規ウラシル化合物又はその塩
JP2012506386A (ja) 2008-10-21 2012-03-15 メタボレックス， インコーポレイテッド アリールｇｐｒ１２０受容体アゴニストおよびその使用
KR101220182B1 (ko) 2009-02-25 2013-01-11 에스케이바이오팜 주식회사 치환된 아졸 유도체 화합물, 이를 포함하는 약제학적 조성물 및 이를 이용한 파킨슨씨 병 치료방법
JP2012528842A (ja) 2009-06-05 2012-11-15 オスロ ユニヴァーシティー ホスピタル エイチエフ Ｗｔｎ経路阻害薬としてのアゾール誘導体
US20100331397A1 (en) 2009-06-24 2010-12-30 Alios Biopharma, Inc. 2-5a analogs and their methods of use
DE102009028929A1 (de) 2009-08-27 2011-07-07 Bayer Schering Pharma Aktiengesellschaft, 13353 Heterocyclisch-substituierte 2-Acetamido-5-Aryl-1,2,4-triazolone und deren Verwendung
WO2011058478A1 (en) 2009-11-16 2011-05-19 Pfizer Inc. Substituted triazolopyrimidines as pde8 inhibitors
WO2011082400A2 (en) 2010-01-04 2011-07-07 President And Fellows Of Harvard College Modulators of immunoinhibitory receptor pd-1, and methods of use thereof
KR101169359B1 (ko) 2010-01-29 2012-07-30 주식회사 레고켐 바이오사이언스 사이클릭 아미드라존 기를 가지는 신규한 옥사졸리디논 유도체 및 이를 함유하는 의약 조성물
EA201290822A1 (ru) 2010-02-22 2013-03-29 ГЛЭКСОСМИТКЛАЙН ЭлЭлСи Триазолоны в качестве ингибиторов синтазы жирных кислот
JP6026284B2 (ja) 2010-03-03 2016-11-16 プロビオドルグ エージー グルタミニルシクラーゼの阻害剤
EP2560966B1 (en) 2010-03-30 2021-01-06 Verseon International Corporation Multisubstituted aromatic compounds as inhibitors of thrombin
EP2371823A1 (de) 2010-04-01 2011-10-05 Bayer CropScience AG Cyclopropyl-substituierte Phenylsulfonylamino(thio)carbonyltriazolinone, ihre Herstellung und Verwendung als Herbizide und Pflanzenwachstumsregulatoren
US8097634B2 (en) 2010-04-15 2012-01-17 Hoffmann-La Roche Inc. Azacyclic derivatives
SG187757A1 (en) 2010-08-10 2013-03-28 Rempex Pharmaceuticals Inc Cyclic boronic acid ester derivatives and therapeutic uses thereof
US20130158063A1 (en) 2010-08-24 2013-06-20 Georgetown University Compounds, Compositions and Methods Related to PPAR Antagonists
JP2014508097A (ja) 2010-09-17 2014-04-03 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッド 脂肪酸合成酵素阻害剤
JP5847533B2 (ja) 2010-10-19 2016-01-27 田辺三菱製薬株式会社 新規甲状腺ホルモンβ受容体作動薬
WO2012058531A2 (en) 2010-10-29 2012-05-03 North Carolina State University Modulation of response regulators by imidazole derivatives
US9505728B2 (en) 2012-03-09 2016-11-29 Inception 2, Inc. Triazolone compounds and uses thereof
BR112015013350B1 (pt) 2012-12-20 2022-04-05 Tempest Therapeutics, Inc Composto ou sal farmaceuticamente aceitável do mesmo, composição farmacêutica e respectivos usos
KR20160048988A (ko) 2013-09-06 2016-05-04 인셉션 2 인코퍼레이티드 트라이아졸론 화합물 및 이의 용도

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