AR092742A1 - Piridinonas antifibroticas - Google Patents

Piridinonas antifibroticas

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Publication number
AR092742A1
AR092742A1 ARP130103530A ARP130103530A AR092742A1 AR 092742 A1 AR092742 A1 AR 092742A1 AR P130103530 A ARP130103530 A AR P130103530A AR P130103530 A ARP130103530 A AR P130103530A AR 092742 A1 AR092742 A1 AR 092742A1
Authority
AR
Argentina
Prior art keywords
optionally substituted
group
alkyl
aryl
alkynyl
Prior art date
Application number
ARP130103530A
Other languages
English (en)
Inventor
Buckman Brad
b nicholas John
Y Ramphal Johnnie
Emayan Kumaraswamy
D Seiwert Scott
Original Assignee
Intermune Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=50435378&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR092742(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Intermune Inc filed Critical Intermune Inc
Publication of AR092742A1 publication Critical patent/AR092742A1/es

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    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/4035—Isoindoles, e.g. phthalimide
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    • 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
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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    • 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
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    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
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    • C07D211/80—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D211/84—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two 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
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    • 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
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    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
    • C07D295/125—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
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    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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  • Biomedical Technology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
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  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
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  • Hydrogenated Pyridines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)

Abstract

Reivindicación 1: Un compuesto caracterizado porque tiene la estructura de fórmula (1) o una de sus sales farmacéuticamente aceptables, en el cual: R¹ se selecciona entre el grupo que comprende halógeno, -CN, -C(O)R⁸, -SO₂R¹⁶, alquilo C₁₋₆ opcionalmente sustituido por uno o más R⁴, alquenilo C₂₋₆ opcionalmente sustituido por uno o más R⁴, alquinilo C₂₋₆ opcionalmente sustituido por uno o más R⁴, arilo C₆₋₁₀ opcionalmente sustituido por uno o más R⁴, un heteroarilo de 5 - 10 miembros opcionalmente sustituido por uno o más R⁴, carbociclilo C₃₋₁₀ opcionalmente sustituido por uno o más R⁴, y heterociclilo de 3 - 10 miembros opcionalmente sustituido por uno o más R⁴; R² se selecciona entre el grupo que comprende halógeno, -CN, -OR⁵, -SR⁵, -NR⁶R⁷, y -C(O)R⁸; R³ se selecciona entre el grupo que comprende hidrógeno, -(CH₂)ₙ-(arilo C₆₋₁₀), -(CH₂)ₙ-(heteroarilo de 5 - 10 miembros), -(CH₂)ₙ-(carbociclilo C₃₋₁₀), y -(CH₂)ₙ-(heterociclilo de 3 - 10 miembros), cada uno opcionalmente sustituido por uno o más R⁹; cada R⁴ se selecciona independientemente entre el grupo que comprende halógeno, -CN, -OH, -C(O)R⁸, -SO₂R¹⁶, alquilo C₁₋₆ opcionalmente sustituido, alquenilo C₂₋₆ opcionalmente sustituido, alquinilo C₂₋₆ opcionalmente sustituido, alcoxi C₁₋₆ opcionalmente sustituido, arilo C₆₋₁₀ opcionalmente sustituido por uno o más R¹¹, aralquilo C₇₋₁₄ opcionalmente sustituido por uno o más R¹¹, heteroarilo de 5 - 10 miembros opcionalmente sustituido por uno o más R¹¹, o independientemente dos R⁴ geminales juntos son oxo; cada R⁵ se selecciona independientemente entre el grupo que comprende hidrógeno, alquilo C₁₋₆ opcionalmente sustituido, alquenilo C₂₋₆ opcionalmente sustituido, alquinilo C₂₋₆ opcionalmente sustituido, alcoxialquilo C₂₋₈ opcionalmente sustituido, arilo C₆₋₁₀ opcionalmente sustituido por uno o más R¹¹, aralquilo C₇₋₁₄ opcionalmente sustituido por uno o más R¹¹, y -(CH₂)ₙ-(heterociclilo de 3 - 10 miembros) opcionalmente sustituido por uno o más R¹⁰; R⁶ se selecciona entre el grupo que comprende hidrógeno, alquilo C₁₋₆ opcionalmente sustituido, alquenilo C₂₋₆ opcionalmente sustituido, alquinilo C₂₋₆ opcionalmente sustituido, arilo C₆₋₁₀ opcionalmente sustituido por uno o más R¹¹, aralquilo C₇₋₁₄ opcionalmente sustituido por uno o más R¹¹, y alquilo(heteroarilo de 5 - 10 miembros) opcionalmente sustituido por uno o más R¹¹, -C(O)R⁸, y -C(O)OR⁵; R⁷ se selecciona entre el grupo que comprende hidrógeno, alquilo C₁₋₆ opcionalmente sustituido, alquenilo C₂₋₆ opcionalmente sustituido, alquinilo C₂₋₆ opcionalmente sustituido, arilo C₆₋₁₀ opcionalmente sustituido por uno o más R¹¹, aralquilo C₇₋₁₄ opcionalmente sustituido por uno o más R¹¹, y alquilo-(heteroarilo de 5 - 10 miembros) opcionalmente sustituido por uno o más R¹¹, -C(O)R⁸, y -C(O)OR⁵; o R⁶ y R⁷ junto con el nitrógeno al que están unidos forman un heterociclilo de 3 - 10 miembros opcionalmente sustituido por uno o más R¹⁰; cada R⁸ se selecciona independientemente entre el grupo que comprende hidrógeno, alquilo C₁₋₆ opcionalmente sustituido, alquenilo C₂₋₆ opcionalmente sustituido, alquinilo C₂₋₆ opcionalmente sustituido, arilo C₆₋₁₀ opcionalmente sustituido por uno o más R¹¹, aralquilo C₇₋₁₄ opcionalmente sustituido por uno o más R¹¹, -NR¹²R¹³, y -OR⁵; cada R⁹ se selecciona independientemente entre el grupo que comprende hidroxi, halógeno, alquilo C₁₋₆ opcionalmente sustituido, alquenilo C₂₋₆ opcionalmente sustituido, alquinilo C₂₋₆ opcionalmente sustituido, alquiltio-C₁₋₆ opcionalmente sustituido, alcoxialquilo C₂₋₈ opcionalmente sustituido, carbociclilo C₃₋₁₀ opcionalmente sustituido, arilo C₆₋₁₀ opcionalmente sustituido, -OR⁵, -NR¹⁴R¹⁵, -C(O)R⁸, -SO₂R¹⁶, -CN, y -NO₂; cada R¹⁰ se selecciona independientemente entre el grupo que comprende alquilo C₁₋₆ opcionalmente sustituido, alquenilo C₂₋₆ opcionalmente sustituido, y alquinilo C₂₋₆ opcionalmente sustituido, o independientemente dos R¹⁰ geminales juntos son oxo; cada R¹¹ se selecciona independientemente entre el grupo que comprende halógeno, -CN, alquilo C₁₋₆ opcionalmente sustituido, alquenilo C₂₋₆ opcionalmente sustituido, alquinilo C₂₋₆ opcionalmente sustituido, -O-(CH₂)ₙ-alcoxi C₁₋₈, -C(O)R⁸, y alcoxi C₁₋₆ opcionalmente sustituido; cada R¹² se selecciona independientemente entre el grupo que comprende hidrógeno, alquilo C₁₋₆ opcionalmente sustituido, alquenilo C₂₋₆ opcionalmente sustituido, alquinilo C₂₋₆ opcionalmente sustituido, arilo C₆₋₁₀ opcionalmente sustituido por uno o más R¹¹, aralquilo C₇₋₁₄ opcionalmente sustituido por uno o más R¹¹; cada R¹³ se selecciona independientemente entre el grupo que comprende hidrógeno, alquilo C₁₋₆ opcionalmente sustituido, alquenilo C₂₋₆ opcionalmente sustituido, alquinilo C₂₋₆ opcionalmente sustituido, arilo C₆₋₁₀ opcionalmente sustituido por uno o más R¹¹, aralquilo C₇₋₁₄ opcionalmente sustituido por uno o más R¹¹; R¹⁴ se selecciona entre el grupo que comprende hidrógeno, alquilo C₁₋₆ opcionalmente sustituido, arilo C₆₋₁₀ opcionalmente sustituido, y -C(O)R⁸; R¹⁵ se selecciona entre el grupo que comprende hidrógeno, alquilo C₁₋₆ opcionalmente sustituido, arilo C₆₋₁₀ opcionalmente sustituido, y -C(O)R⁸; cada R¹⁶ se selecciona independientemente entre el grupo que comprende alquilo C₁₋₆ opcionalmente sustituido, alquenilo C₂₋₆ opcionalmente sustituido, alquinilo C₂₋₆ opcionalmente sustituido, arilo C₆₋₁₀ opcionalmente sustituido por uno o más R¹¹, aralquilo C₇₋₁₄ opcionalmente sustituido por uno o más R¹¹, -NR¹²R¹³, y -OR⁵; Z se selecciona entre oxígeno y azufre; cada n es, independientemente, un entero que oscila entre 0 y 4; y los enlaces representados por una línea continua y de guiones se seleccionan independientemente entre el grupo que comprende un enlace simple y un enlace doble, siempre que cuando R³ es H, entonces R¹ se selecciona entre arilo C₆₋₁₀ opcionalmente sustituido por uno o más R⁴, o heteroarilo de 5 - 10 miembros opcionalmente sustituido por uno o más R⁴; cuando R² es -NH-(2-fluoro-4-bromo-fenil) y R¹ es C(O)OH, entonces R³ no es fenilo-CH₂; cuando R² es metoxi, R¹ es 4-metoxifenilo, y Z es O, entonces R³ no es 2-fluoro-4-cloro-fenilo-(CH₂); cuando R³ es un fenilo; R² es OR⁵ o NR⁶R⁷; entonces R¹ no es triazolilo; cuando R³ es 4-metil fenilo, R² es morfolinilo, y Z es O; entonces R¹ no es metilo; y cuando R³ es 4-metil fenilo, R² es -N(CH₃)₂, Z es O; entonces R¹ no es metilo.
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Families Citing this family (64)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2007009796A (es) 2007-08-14 2009-02-25 Cell Therapy And Technology S Gel conteniendo pirfenidona.
CA2726588C (en) 2008-06-03 2019-04-16 Karl Kossen Compounds and methods for treating inflammatory and fibrotic disorders
MX346763B (es) 2012-03-28 2017-03-31 Cell Therapy And Tech S A De C V Composición tópica semisólida conteniendo pirfenidona y dialil óxido de disulfuro modificado (odd-m) para eliminar o prevenir el acné.
CN104364239B (zh) 2012-06-13 2017-08-25 霍夫曼-拉罗奇有限公司 二氮杂螺环烷烃和氮杂螺环烷烃
MX368615B (es) 2012-09-25 2019-10-09 Hoffmann La Roche Derivados bicíclicos como inhibidores de la autotaxina (atx) que son inhibidores de la producción de ácido lisofosfatídico (lpa) y el uso de los mismos.
AR092742A1 (es) 2012-10-02 2015-04-29 Intermune Inc Piridinonas antifibroticas
US9315464B1 (en) 2013-01-31 2016-04-19 Nant Holdings Ip, Llc Small molecule inhibitors of influenza A RNA-dependent RNA polymerase
AR095079A1 (es) 2013-03-12 2015-09-16 Hoffmann La Roche Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo
HUE036117T2 (hu) 2013-11-26 2018-06-28 Hoffmann La Roche Oktahidro-ciklobuta[1,2-C;3,4-C']dipirrol származékok, mint autotaxin inhibitorok
NZ722927A (en) 2014-01-10 2022-07-29 Avalyn Pharma Inc Aerosol pirfenidone and pyridone analog compounds and uses thereof
MA39792B1 (fr) 2014-03-26 2019-12-31 Hoffmann La Roche Composés bicycliques en tant qu'inhibiteurs de production d'autotaxine (atx) et d'acide lysophosphatidique (lpa)
CN106029667B (zh) 2014-03-26 2019-08-23 豪夫迈·罗氏有限公司 作为自分泌运动因子(atx)和溶血磷脂酸(lpa)生产抑制剂的稠合[1,4]二氮杂*化合物
KR102373700B1 (ko) * 2014-04-02 2022-03-11 인터뮨, 인크. 항섬유성 피리디논
CA2953177C (en) 2014-06-23 2019-07-23 Dr. Reddy's Laboratories Ltd. Substituted imidazo[1,2-a]pyridine compounds useful for the treatment of pain
MA40940A (fr) 2014-11-10 2017-09-19 Constellation Pharmaceuticals Inc Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines
MA40943A (fr) * 2014-11-10 2017-09-19 Constellation Pharmaceuticals Inc Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines
WO2016077375A1 (en) 2014-11-10 2016-05-19 Genentech, Inc. Bromodomain inhibitors and uses thereof
JP6709792B2 (ja) 2015-01-29 2020-06-17 ジェネンテック， インコーポレイテッド 治療用化合物およびその使用
MA41898A (fr) 2015-04-10 2018-02-13 Hoffmann La Roche Dérivés de quinazolinone bicyclique
WO2017024406A1 (en) 2015-08-11 2017-02-16 Neomed Institute N-substituted bicyclic lactams, their preparation and their use as pharmaceuticals
US10501438B2 (en) 2015-08-11 2019-12-10 Neomed Institute Aryl-substituted dihydroquinolinones, their preparation and their use as pharmaceuticals
EP3334719B1 (en) 2015-08-12 2021-09-15 Neomed Institute Substituted benzimidazoles, their preparation and their use as pharmaceuticals
CN105085383B (zh) * 2015-08-19 2017-09-01 四川大学 5‑甲基‑2(1h)吡啶酮衍生物及其制备方法和用途
UA123362C2 (uk) 2015-09-04 2021-03-24 Ф. Хоффманн-Ля Рош Аг Феноксиметильні похідні
CA2991615A1 (en) 2015-09-24 2017-03-30 F. Hoffmann-La Roche Ag Bicyclic compounds as atx inhibitors
WO2017050791A1 (en) 2015-09-24 2017-03-30 F. Hoffmann-La Roche Ag New bicyclic compounds as dual atx/ca inhibitors
AU2016328535A1 (en) 2015-09-24 2017-11-09 F. Hoffmann-La Roche Ag Bicyclic compounds as ATX inhibitors
CN107614505B (zh) 2015-09-24 2021-05-07 豪夫迈·罗氏有限公司 作为双重atx/ca抑制剂的新型二环化合物
WO2017066876A1 (en) 2015-10-21 2017-04-27 Neomed Institute Substituted imidazopyridines, their preparation and their use as pharmaceuticals
AU2016341259B2 (en) * 2015-10-22 2019-09-12 Selvita S.A. Pyridone derivatives and their use as kinase inhibitors
KR20180079328A (ko) * 2015-11-04 2018-07-10 이데미쓰 고산 가부시키가이샤 벤즈이미다졸 축합 헤테로아릴
CN105330598B (zh) * 2015-12-02 2017-11-14 新发药业有限公司 一种吡非尼酮的制备方法
US10519151B2 (en) 2016-01-28 2019-12-31 Neomed Institute Substituted [1,2,4]triazolo[4,3-A]pyridines, their preparation and their use as pharmaceuticals
CN105541715B (zh) * 2016-02-02 2019-04-09 浙江工业大学 多取代吡啶-1(2h)-酮衍生物及其合成方法与应用
CN105732497B (zh) * 2016-02-02 2019-02-01 浙江工业大学 2-芳基-4-甲基环并吡啶-1(2h)-酮类衍生物及其合成方法与应用
WO2017177974A1 (zh) * 2016-04-14 2017-10-19 南京明德新药研发股份有限公司 用于治疗纤维化和炎性疾病的含杂原子环丁烷取代基的吡啶酮衍生物
EP3693369A3 (en) 2016-04-15 2020-09-09 AbbVie Inc. Bromodomain inhibitors
WO2018019755A1 (en) 2016-07-26 2018-02-01 Basf Se Herbicidal pyridine compounds
WO2018019721A1 (en) 2016-07-26 2018-02-01 Basf Se Herbicidal pyridine compounds
CN116082225A (zh) * 2016-08-08 2023-05-09 北京康蒂尼药业股份有限公司 一种羟尼酮的制备方法
CN107698498A (zh) * 2016-08-08 2018-02-16 罗楹 一种羟尼酮的制备方法
GB201614934D0 (en) * 2016-09-02 2016-10-19 Glaxosmithkline Intellectual Property (No 2) Ltd Chemical compounds
TWI826361B (zh) * 2016-11-30 2023-12-21 美商基因科技公司 投與抗纖維化療法之方法
AU2018233079B9 (en) 2017-03-16 2021-07-22 F. Hoffmann-La Roche Ag Heterocyclic compounds useful as dual ATX/CA inhibitors
WO2018167113A1 (en) 2017-03-16 2018-09-20 F. Hoffmann-La Roche Ag New bicyclic compounds as atx inhibitors
JP2020516672A (ja) 2017-04-18 2020-06-11 セルジーン クオンティセル リサーチ，インク． 治療用化合物
CA3108048A1 (en) * 2017-07-31 2019-02-07 Washington University Pirfenidone derivatives for modulation of b lymphocyte activity and organ protection
MX366086B (es) 2017-08-15 2019-06-27 Cell Therapy And Tech S A De C V Composicion topica semisolida conteniendo un agente antimicrobiano y pirfenidona para el tratamiento de daños cronicos de la piel.
US10513515B2 (en) 2017-08-25 2019-12-24 Biotheryx, Inc. Ether compounds and uses thereof
EP3459939A1 (en) * 2017-09-26 2019-03-27 Pragma Therapeutics Novel heterocyclic compounds as modulators of mglur7
US11198686B2 (en) 2017-10-13 2021-12-14 Guangzhou Joyo Pharmatech Co., Ltd. Crystal form and salt form of pyridone compound and preparation method therefor
MX2020008076A (es) * 2018-02-02 2020-09-24 Genentech Inc Compuesto farmaceutico, sales del mismo, formulaciones del mismo y metodos para hacer y usar el mismo.
CA3106239A1 (en) 2018-07-27 2020-01-30 Biotheryx, Inc. Bifunctional compounds as cdk modulators
US11171132B2 (en) * 2019-10-03 2021-11-09 Globalfoundries U.S. Inc. Bi-directional breakdown silicon controlled rectifiers
US20230000846A1 (en) 2019-12-04 2023-01-05 Idorsia Pharmaceuticals Ltd Combination of an azetidine lpa1 receptor antagonist with pirfenidone and/or nintedanib for use in the treatment of fibrotic diseases
WO2021222150A2 (en) 2020-04-28 2021-11-04 Anwita Biosciences, Inc. Interleukin-2 polypeptides and fusion proteins thereof, and their pharmaceutical compositions and therapeutic applications
EP4186901A1 (en) * 2020-07-23 2023-05-31 Cytosinlab Therapeutics Co., Ltd. Compound having kinase inhibitory activity
CN114129517A (zh) * 2020-09-03 2022-03-04 苏州爱科百发生物医药技术有限公司 一种ak3287制剂及其制备方法和应用
EP4288430A1 (en) * 2021-02-02 2023-12-13 Liminal Biosciences Limited Gpr84 antagonists and uses thereof
WO2022242769A1 (zh) * 2021-05-20 2022-11-24 广州嘉越医药科技有限公司 一种含杂原子环丁烷取代基的吡啶酮衍生物的应用
CN113234013B (zh) * 2021-05-21 2022-05-24 杭州医学院 一种抑制胶原合成和沉积的化合物及其应用
WO2023107714A2 (en) * 2021-12-10 2023-06-15 Prothena Biosciences Limited Methods for treating neurological disorders
CN116332947A (zh) * 2021-12-24 2023-06-27 上海海和药物研究开发股份有限公司 具有mat2a抑制活性的嘧啶-2(1h)-酮并二环类化合物及其用途
CN116514803A (zh) * 2022-01-21 2023-08-01 上海赛岚生物科技有限公司 一种激酶抑制剂的盐晶型和自由碱晶型

Family Cites Families (558)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1070639B (de) 1959-12-10 Farbenfabriken Bayer Aktiengesellschaft, Levenkusen-Bayerwerk Verfahren zur Herstellung von Peptiderj
DE149666C (es)
CH312530A (de) 1952-06-20 1955-12-31 Ciba Geigy Verfahren zur Herstellung eines Pyridazons.
CH312531A (de) 1952-06-20 1955-12-31 Ciba Geigy Verfahren zur Herstellung eines Pyridazons.
GB788393A (en) 1953-04-30 1958-01-02 Ciba Ltd Process for the manufacture of pyridazone compounds
CH333366A (de) 1953-09-04 1958-10-15 Ciba Geigy Verfahren zur Herstellung neuer Pyridazone
DE1070639C2 (es) 1958-09-30 1964-04-16
US3014034A (en) 1959-01-22 1961-12-19 Ciba Pharm Prod Inc 1, 3-diaryl, 5-amino-pyridazinones
GB889317A (en) 1959-01-22 1962-02-14 Ciba Ltd New phenyl-diazines and a process for their manufacture
JPS422264Y1 (es) 1966-08-10 1967-02-10
US3622340A (en) 1968-08-12 1971-11-23 Eastman Kodak Co 4-thiouracil compounds as fog inhibitors
US3644375A (en) * 1968-10-18 1972-02-22 Toray Industries Lactam dicarboxylic acids and process for producing them
GB1237031A (en) * 1969-03-07 1971-06-30 Toray Industries Lactam dicarboxylic acids and a process for their production
UST866035I4 (en) 1969-05-05 1969-09-30 Defensive publication
FR2081572B1 (es) * 1970-03-12 1973-04-06 Rhone Poulenc Sa
BE787523A (fr) 1971-08-13 1973-02-12 Chem Pharmac Fabrik Dr Hermann Medicament a base de pyridone-2
DE2143744A1 (de) 1971-09-01 1973-03-08 Hoechst Ag 3,4-dihydro-2h-isochinolin-1-one und verfahren zu ihrer herstellung
US3839346A (en) 1972-12-18 1974-10-01 Affiliated Med Res N-substituted pyridone and general method for preparing pyridones
CA1049411A (en) 1972-12-18 1979-02-27 Affiliated Medical Research N-substituted pyridone and general method for preparing pyridones
ES421598A1 (es) 1972-12-18 1977-01-01 Affiliated Med Res Un procedimiento para la sintesis de piridonas.
US4052509A (en) 1972-12-18 1977-10-04 Affiliated Medical Research, Inc. Method for reducing serum uric acid levels
US4042699A (en) 1972-12-18 1977-08-16 Affiliated Medical Research, Inc. Method for reducing serum glucose levels
AT333774B (de) 1974-09-24 1976-12-10 Chemie Linz Ag Verfahren zur herstellung von 3-phenylpyridazonen
JPS51128438A (en) 1975-04-26 1976-11-09 Yamanouchi Pharmaceut Co Ltd An antibacterial drug against fish diseases
DE2557342A1 (de) 1975-12-19 1977-06-30 Hoechst Ag Basisch substituierte indolderivate und verfahren zu ihrer herstellung
US4258052A (en) 1976-08-17 1981-03-24 Yu Ruey J Treatment of psoriasis with nicotinamide analogues
DE2707268A1 (de) 1977-02-19 1978-08-31 Hoechst Ag Indol-3-carbaldehyd-oxime und verfahren zu ihrer herstellung
GB1596887A (en) 1977-07-15 1981-09-03 Rohm & Haas 2-pyridone derivatives and their use as plant growth regulators
JPS557201A (en) 1978-05-23 1980-01-19 Shionogi & Co Ltd Derivative of tetrahydrothiopyrano(2,3-b)indole
GB2042562B (en) 1979-02-05 1983-05-11 Sandoz Ltd Stabilising polymers
DD149666A1 (de) 1979-06-27 1981-07-22 Karl Gewald Verfahren zur herstellung von 6-amino-und 6-hydroxy-1-aryl-5-cyan-2(1h)-pyridinonen und-thionen
JPS5721388A (en) 1980-07-11 1982-02-04 Nippon Nohyaku Co Ltd Condensed pyrazole derivative
JPS5777671A (en) 1980-10-31 1982-05-15 Yasumitsu Tamura Preparation of hydroxyindoles ( or 1,4-dihydroisoquinolones) and their intermediate
US4404203A (en) 1981-05-14 1983-09-13 Warner-Lambert Company Substituted 6-phenyl-3(2H)-pyridazinones useful as cardiotonic agents
US4397854A (en) 1981-05-14 1983-08-09 Warner-Lambert Company Substituted 6-phenyl-3(2H)-pyridazinones useful as cardiotonic agents
US4476307A (en) 1982-09-20 1984-10-09 Pfizer Inc. Heteroylidene indolone compounds
US4473696A (en) 1982-10-07 1984-09-25 Ici Americas Inc. Synthesis of 2-substituted-5-methyl-pyridines
US4645839A (en) 1982-12-17 1987-02-24 Ici Americas Inc. Sulphur dehydrogenation process to yield 5-methyl-2-pyridone
US4650804A (en) 1984-03-30 1987-03-17 Fujisawa Pharmaceutical Co., Ltd. Quinolizinone compounds and pharmaceutical composition comprising the same, useful as anti-ulcerative and anti-allergic agents
US4576942A (en) 1984-07-12 1986-03-18 Usv Pharmaceutical Corp. Anti-allergic and anti-inflammatory bi- and tri- cyclo-1,4-thiazine derivatives, composition, and method of use therefor
DK175432B1 (da) * 1984-10-30 2004-10-18 Otsuka Pharma Co Ltd Middel til forögelse af anticancervirkningen af anticancerforbindelser
DE3588036T2 (de) * 1984-10-30 1995-11-16 Otsuka Pharma Co Ltd 5-Fluoruracilderivate.
JPS6256187A (ja) 1985-09-05 1987-03-11 Ricoh Co Ltd 感熱記録材料
US5173489A (en) 1986-04-10 1992-12-22 The Dupont Merck Pharmaceutical Co. α,α-disubstituted aromatics and heteroaromatics as cognition enhancers
US4760083A (en) 1986-04-10 1988-07-26 E. I. Dupont De Nemours & Company 3,3-disubstituted indolines
GB8621217D0 (en) 1986-09-03 1986-10-08 Ici Plc Chemical compounds
DE3805746C2 (de) 1987-03-05 2003-04-10 Clariant Finance Bvi Ltd 1:2-Chromkomplexfarbstoffe
JPS63290821A (ja) 1987-05-25 1988-11-28 Otsuka Pharmaceut Co Ltd 抗不整脈剤
DK641487A (da) 1987-12-07 1989-06-08 Gluetech Aps Fremgangsmaade til modificering af polymeroverflader
DE3807295A1 (de) 1988-03-05 1989-09-14 Basf Ag Neue n-heteroaryl-tetrahydrophthalimidverbindungen
JP2614081B2 (ja) 1988-05-27 1997-05-28 大塚化学株式会社 光学活性β−ラクタム誘導体の製造法
JPH022264A (ja) 1988-06-14 1990-01-08 Canon Inc メツセージ通信システム
US5167941A (en) 1988-11-29 1992-12-01 The Dow Chemical Company Quaternary polyamines as sulfite oxidation inhibitors in amine scrubbing of SO2
US5019365A (en) 1988-11-29 1991-05-28 The Dow Chemical Company Quaternary polyamines as sulfite oxidation inhibitors
GB8901836D0 (en) 1989-01-27 1989-03-15 Sobio Lab Compounds
US5047554A (en) 1989-04-18 1991-09-10 Pfizer Inc. 3-substituted-2-oxindole derivatives
US5077142A (en) 1989-04-20 1991-12-31 Ricoh Company, Ltd. Electroluminescent devices
WO1991000863A1 (en) 1989-07-07 1991-01-24 Pfizer Inc. Heteroaryl piperazine antipsychotic agents
JPH0343744A (ja) 1989-07-12 1991-02-25 Hitachi Chem Co Ltd 電子写真感光体
US5716632A (en) 1989-11-22 1998-02-10 Margolin; Solomon B. Compositions and methods for reparation and prevention of fibrotic lesions
US5518729A (en) 1989-11-22 1996-05-21 Margolin; Solomon B. Compositions and methods for reparation and prevention of fibrotic lesions
US5310562A (en) 1989-11-22 1994-05-10 Margolin Solomon B Composition and method for reparation and prevention of fibrotic lesions
CA2078126A1 (en) 1990-03-27 1991-09-28 Jerry Leroy Adams 5-lipoxygenase inhibitors
JPH0444235A (ja) 1990-06-08 1992-02-14 New Japan Radio Co Ltd 高速バイポーラトランジスタの製造方法
JPH0449567A (ja) 1990-06-19 1992-02-18 Matsushita Electric Ind Co Ltd 磁気記録再生装置
EP0478195B1 (en) 1990-09-21 1999-05-26 Rohm And Haas Company Dihydropyridazinones and pyridazinones as fungicides
JPH04223457A (ja) 1990-12-26 1992-08-13 Konica Corp ハロゲン化銀写真感光材料
WO1992013451A1 (en) 1991-02-11 1992-08-20 Schering Agrochemicals Limited Imidazole pesticides
US5491148A (en) * 1991-04-26 1996-02-13 Syntex (U.S.A.) Inc. Isoquinolinone and dihydroisoquinolinone 5-HT3 receptor antagonists
WO1992020642A1 (en) 1991-05-10 1992-11-26 Rhone-Poulenc Rorer International (Holdings) Inc. Bis mono-and bicyclic aryl and heteroaryl compounds which inhibit egf and/or pdgf receptor tyrosine kinase
EP0586523A4 (en) 1991-05-15 1995-11-29 Univ Yale Determination of prodrugs metabolizable by the liver and therapeutic use thereof
JPH0519023A (ja) 1991-07-11 1993-01-26 Hitachi Ltd 集積回路装置
EP0531578B1 (en) 1991-09-10 1995-12-20 Agfa-Gevaert N.V. Thermally transferable fluorescent compounds
DK0548680T3 (da) 1991-12-26 1998-09-23 Mitsubishi Chem Corp Beta-oxo-beta-benzenpropanthioamidderivater
US5241065A (en) 1992-02-25 1993-08-31 Schering Corporation 2,3,4,5-tetrahydro-1h-3-benzazepines having anti-psychotic activity
JPH07507772A (ja) 1992-04-16 1995-08-31 ザ・デュポン・メルク・ファーマシュウティカル・カンパニー 認識欠損治療用の置換された窒素含有スピロ化合物
WO1993023404A1 (en) 1992-05-19 1993-11-25 Immunopharmaceutics, Inc. Compounds that modulate endothelin activity
DE4237656A1 (de) 1992-06-13 1993-12-16 Merck Patent Gmbh Benzimidazolderivate
US5459269A (en) * 1992-06-18 1995-10-17 North Carolina State University 14-halo-camptothecins
US5457099A (en) 1992-07-02 1995-10-10 Sawai Pharmaceutical Co., Ltd. Carbostyril derivatives and antiallergic agent
CA2099743A1 (en) 1992-07-02 1994-01-03 Akihiko Ishida Pyridazinone derivatives and processes for preparing the same
US5877278A (en) 1992-09-24 1999-03-02 Chiron Corporation Synthesis of N-substituted oligomers
US5356904A (en) 1992-10-07 1994-10-18 Merck & Co., Inc. Carbostyril oxytocin receptor antagonists
DE4242451A1 (de) 1992-12-16 1994-06-23 Basf Ag Verfahren zur Herstellung von 5-Ringheterocyclen
WO1994017059A1 (en) 1993-01-29 1994-08-04 Nippon Soda Co., Ltd. Heterocyclic derivative
JPH06256187A (ja) 1993-03-02 1994-09-13 Fujisawa Pharmaceut Co Ltd キノリジノン化合物またはその塩を含有する鎮咳・去痰剤
BR9406461A (pt) 1993-05-07 1996-01-30 Solomon Begelfor Margolin Composições e métodos para a reparação e prevenção de les~es fibróticas
JP3507124B2 (ja) 1993-05-26 2004-03-15 塩野義製薬株式会社 ベンジリデン誘導体の製造法
DE4423934A1 (de) 1993-09-02 1995-03-09 Basf Ag 3(2H)-Pyridazinon-Derivate, Verfahren zu ihrer Herstellung und Verwendung
RU2146674C1 (ru) 1993-10-15 2000-03-20 Такеда Кемикал Индастриз, Лтд. Производные триазина, способы их получения, антипротозойная композиция, добавка в пищу животных, способ ингибирования протозои у животных
JPH07128793A (ja) 1993-11-05 1995-05-19 Konica Corp 染料の固体微粒子分散物および該分散物を含有するハロゲン化銀写真感光材料
EP0677519A4 (en) 1993-11-10 1996-04-03 Japan Tobacco Inc CHROMAN DERIVATIVE AND THERAPEUTIC USE THEREOF.
DE69430006T2 (de) 1993-12-15 2002-11-28 Smithkline Beecham Corp Verbindungen und verfahren
JPH07233072A (ja) 1993-12-28 1995-09-05 Tanabe Seiyaku Co Ltd 医薬組成物
HUT76280A (en) 1993-12-29 1997-07-28 Fujisawa Pharmaceutical Co Pyrazolopyridine derivatives, pharmaceutical compositions containing them, process for proiducing them and their use
JP3781200B2 (ja) 1994-04-27 2006-05-31 コニカミノルタホールディングス株式会社 ハロゲン化銀写真感光材料の処理方法
JP3261641B2 (ja) 1994-04-28 2002-03-04 コニカ株式会社 ハロゲン化銀写真感光材料の処理方法
US5466697A (en) 1994-07-13 1995-11-14 Syntex (U.S.A.) Inc. 8-phenyl-1,6-naphthyridin-5-ones
JP2794392B2 (ja) 1994-07-22 1998-09-03 大同テック株式会社 高圧ガス容器の保守装置
JPH08134371A (ja) 1994-11-02 1996-05-28 Konica Corp 固体微粒子分散物及びハロゲン化銀写真感光材料及び画像形成方法
EP0717143A1 (de) 1994-12-16 1996-06-19 Lignozym GmbH Mehrkomponentensystem zum Verändern, Abbau oder Bleichen von Lignin, ligninhaltigen Materialien oder ähnlichen Stoffen sowie Verfahren zu seiner Anwendung
US6323201B1 (en) 1994-12-29 2001-11-27 The Regents Of The University Of California Compounds for inhibition of ceramide-mediated signal transduction
US6090822A (en) 1995-03-03 2000-07-18 Margolin; Solomon B. Treatment of cytokine growth factor caused disorders
BR9607541A (pt) 1995-03-03 1997-12-23 Solomon Begelfor Margolin Tratamento de doenças que tem por causa o fator de crescimento da citoquina
US6114353A (en) 1995-03-03 2000-09-05 Margolin; Solomon B. Compositions and method for treatment of lymphomas, leukemias, and leiomyomas
US5869428A (en) 1995-03-13 1999-02-09 Ishihara Sangyo Kaisha Ltd. Pyridonesulfonylurea compounds, process for their production and herbicides containing them
US5635494A (en) 1995-04-21 1997-06-03 Rohm And Haas Company Dihydropyridazinones and pyridazinones and their use as fungicides and insecticides
WO1996033994A1 (fr) 1995-04-28 1996-10-31 Nippon Soda Co., Ltd. Derives amino-substitues, leur procede de preparation et herbicide
DE19520613A1 (de) 1995-06-06 1996-12-12 Bayer Ag Phenylpyridazinone
JPH0933072A (ja) 1995-07-18 1997-02-07 Hitachi Ltd 蓄熱水槽及びマルチ氷蓄熱ユニット
AU6514296A (en) 1995-07-31 1997-02-26 Novo Nordisk A/S Heterocyclic compounds, their preparation and use
AU6514196A (en) 1995-07-31 1997-02-26 Novo Nordisk A/S Heterocyclic compounds, their preparation and use
AR003978A1 (es) 1995-08-25 1998-09-30 Rohm & Haas Composiciones de acidos grasos y piridazinonas que tienen efectos fungitoxicos sinergicos y metodos para controlar hongos.
US5962478A (en) 1995-09-19 1999-10-05 Margolin; Solomon B. Inhibition of tumor necrosis factor α
ATE360419T1 (de) 1995-09-19 2007-05-15 Solomon B Margolin Verwendung von n-substituierten pyridonen als tumornekrose-faktor alpha hemmer
DE19535501A1 (de) 1995-09-25 1997-03-27 Bayer Ag Pyridonmethidazofarbstoffe
JPH0995165A (ja) 1995-09-29 1997-04-08 Tachi S Co Ltd シートの前後チルト機構
JPH0995166A (ja) 1995-10-02 1997-04-08 Tatsuya Mikami 乗物用座席
JPH09249567A (ja) 1996-01-12 1997-09-22 Otsuka Pharmaceut Co Ltd 医薬組成物
JPH09204932A (ja) 1996-01-25 1997-08-05 Fujitsu Ltd リチウム二次電池用電解液及びリチウム二次電池
IT1286545B1 (it) 1996-02-09 1998-07-15 Antonio Guarna Derivati benzo(c) chinolizinici,loro preparazione ed uso come inibitori delle 5-alfa-riduttasi
JPH09244235A (ja) 1996-03-14 1997-09-19 Toshiba Corp アルカリ現像用レジスト
GB9607503D0 (en) 1996-04-11 1996-06-12 Merck Frosst Canada Inc Bisaryl cyclobutenes derivatives as cyclooxygenase inhibitors
JP2000510444A (ja) 1996-03-29 2000-08-15 メルク フロスト カナダ アンド カンパニー シクロオキシゲナーゼ抑制剤としてのビスアリールシクロブテン誘導体
JPH09319023A (ja) 1996-05-27 1997-12-12 Fuji Photo Film Co Ltd 感熱記録材料
AU708883B2 (en) 1996-06-10 1999-08-12 Merck & Co., Inc. Substituted imidazoles having cytokine inhibitory activity
US6294504B1 (en) 1996-09-26 2001-09-25 Syngenta Crop Protection, Inc. Herbicidal composition
CA2216512A1 (en) 1996-10-11 1998-04-11 Rohm And Haas Company Dihydropyridazinones and pyridazinones their use as fungicides and insecticides
US5977134A (en) 1996-12-05 1999-11-02 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
DE19754348A1 (de) 1996-12-11 1998-06-18 Ciba Geigy Ag Neue Herbizide
EP0951285A1 (en) 1996-12-30 1999-10-27 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5855654A (en) 1997-01-30 1999-01-05 Rohm And Haas Company Pyridazinones as marine antifouling agents
US6117973A (en) 1997-02-24 2000-09-12 Georgia Tech Research Corp. PNA monomers with electron donor or acceptor
DE19708928A1 (de) 1997-03-05 1998-09-10 Bayer Ag Substituierte aromatische Aminoverbindungen
DE19821263A1 (de) 1997-05-12 1998-11-19 Call Krimhild Enzymatisches Bleichsystem mit enzymwirkungsverstärkenden Verbindungen zur Behandlung von Textilien
WO1998051772A1 (de) 1997-05-12 1998-11-19 Call, Krimhild Enzymatisches bleichsystem mit neuen enzymwirkungsverstärkenden verbindungen
JP3043744U (ja) 1997-05-26 1997-11-28 株式会社新和 バッグ
DE19726241A1 (de) 1997-06-20 1998-12-24 Call Krimhild Erweitertes enzymatisches Multikomponentensystem zur Behandlung von Abwässern, zur Herstellung von Holzverbundstoffen, zum Deinken von Altpapier, Colour stripping von Altpapier, zum Einsatz als Oxidationssystem bei der organischen Synthese und zum Einsatz bei der Kohleverflüssigung
DE19729061A1 (de) 1997-07-08 1999-01-14 Agfa Gevaert Ag Farbfotografisches Aufzeichnungsmaterial
SE9702651D0 (sv) 1997-07-09 1997-07-09 Astra Pharma Prod Novel compounds
DE19731784A1 (de) 1997-07-24 1999-02-04 Bayer Ag Substituierte N-Aryl-N-thioxocarbonyl-sulfonamide
SE9702794D0 (sv) 1997-07-24 1997-07-24 Astra Pharma Prod New compounds
JPH1149755A (ja) 1997-07-30 1999-02-23 Nippon Kayaku Co Ltd 新規含窒素ヘテロ環誘導体およびそれを有効成分とする殺虫殺ダニ組成物
ITFI970193A1 (it) 1997-08-01 1999-02-01 Applied Research Systems Uso di derivati benzo(c) chinolizinici come regolatori della crescita delle piante e composizioni ad uso agricolo che contengono tali
CA2299300C (en) 1997-08-22 2007-04-17 Abbott Laboratories Arylpyridazinones as prostaglandin endoperoxide h synthase bisoynthesis inhibitors
US6307047B1 (en) 1997-08-22 2001-10-23 Abbott Laboratories Prostaglandin endoperoxide H synthase biosynthesis inhibitors
JP2002511887A (ja) 1997-08-22 2002-04-16 アボツト・ラボラトリーズ プロスタグランジンエンドペルオキシドｈシンターゼ生合成阻害薬
DE69823843T2 (de) 1997-09-09 2005-05-12 Bristol-Myers Squibb Pharma Co. Benzimidazolinone, benzoxazolinone, benzopiperazinone, indanone und deren derivate als faktor xa inhibitoren
CN1680274A (zh) 1997-10-27 2005-10-12 Isk美国有限公司 取代的苯化合物、它们的制备方法和含它们的除草剂和脱叶剂组合物
ATE213242T1 (de) 1997-11-21 2002-02-15 Astrazeneca Uk Ltd Neue verbindungen, welche antagonisten sind für p2-purinorezeptor 7-transmembran (tm) g-protein gekoppelte rezeptoren
EP1042293B9 (en) 1997-12-19 2008-09-03 Amgen Inc. Substituted pyridine and pyridazine compounds and their pharmaceutical use
US6174901B1 (en) 1998-12-18 2001-01-16 Amgen Inc. Substituted pyridine and pyridazine compounds and methods of use
JPH11180952A (ja) 1997-12-19 1999-07-06 Maruho Co Ltd ２−オキシインドール誘導体
DE19803667A1 (de) 1998-01-30 1999-08-05 Max Planck Gesellschaft Verfahren zur Herstellung von 5-Alkoxy (bzw. 5-Aroxy) -2,3-dihydrofuran-2-onen
AU2108099A (en) * 1998-01-30 1999-08-16 Procept, Inc. Immunosuppressive agents
FR2774986A1 (fr) 1998-02-16 1999-08-20 Rhodia Chimie Sa Utilisation de pyrone(s) ou equivalent pour masquer des isocyanates, procede de masquage, isocyanates ainsi masques, composition en contenant, procede de revetement utilisant ces compositions, revetement aini obtenu
ATE266405T1 (de) 1998-03-17 2004-05-15 Solomon B Margolin Topische antiseptische zusammenstellungen und methoden
NZ505921A (en) 1998-03-31 2003-08-29 Warner Lambert Co 1-[5-(2,6-Dimethylpiperidino)pentyl] substituted quinolone serine protease inhibitors and their use for treating thrombin related disorders
BR9909548A (pt) 1998-04-09 2000-12-12 Bayer Ag Fenilpiridazinonas substituìdas
US6509354B1 (en) 1998-04-27 2003-01-21 Kumiai Chemical Industry Co., Ltd. 3-arylphenyl sulfide derivative and insecticide and miticide
JP2002513004A (ja) 1998-04-27 2002-05-08 サーントル ナスィヨナル ドゥ ラ ルシェルシュ スイヤンティフィック ３−（アミノ−またはアミノアルキル）ピリジノン誘導体およびｈｉｖ関連疾患治療におけるその用途
DE69933671T2 (de) 1998-06-01 2007-02-01 Astellas Pharma Inc. Adenosin a1 antagonisten gegen männliche sterilität
FR2779429B1 (fr) 1998-06-03 2000-07-13 Synthelabo Derives d'oxindole, leurs preparations et leurs applications en therapeutique
DE19826671A1 (de) 1998-06-16 1999-12-23 Hoechst Schering Agrevo Gmbh 1,3-Oxazolin- und 1,3-Thiazolin-Derivate, Verfahren zu ihrer Herstellung und ihre Verwendung als Schädlingsbekämpfungsmittel
US6492395B1 (en) 1998-09-18 2002-12-10 Mepha Ag Topical formulation of alkyl-, phenyl-pyridone
WO2000025789A1 (en) 1998-10-29 2000-05-11 Merck & Co., Inc. A method of treating endometriosis
JP3043744B1 (ja) 1999-03-17 2000-05-22 日本ピラー工業株式会社 単結晶ＳｉＣの育成方法
US6586447B1 (en) 1999-04-01 2003-07-01 Pfizer Inc 3,3-disubstituted-oxindole derivatives useful as anticancer agents
DE19918725A1 (de) 1999-04-24 2000-10-26 Bayer Ag Substituierte N-Cyano-sulfonsäureanilide
KR100767199B1 (ko) 1999-05-07 2007-10-17 엔싸이시브 파마슈티칼즈 인코퍼레이티드 인테그린이 이의 수용체에 결합하는 것을 억제하는프로판산 유도체
US6972296B2 (en) * 1999-05-07 2005-12-06 Encysive Pharmaceuticals Inc. Carboxylic acid derivatives that inhibit the binding of integrins to their receptors
US6723711B2 (en) 1999-05-07 2004-04-20 Texas Biotechnology Corporation Propanoic acid derivatives that inhibit the binding of integrins to their receptors
US6534535B1 (en) 1999-08-12 2003-03-18 Millennium Pharmaceuticals, Inc. Inhibitors of factor Xa
FR2797629B1 (fr) 1999-08-19 2001-09-21 Rhodia Chimie Sa Utilisation de pyrone(s) ou equivalent pour masquer des isocyanates, procede de masquage, isocyanates ainsi masques, composition en contenant, procede de revetement utilisant ces compositions, revetement ainsi obtenu
AT408223B (de) 1999-12-27 2001-09-25 Dsm Fine Chem Austria Gmbh Verfahren zur herstellung von oxindolen
MXPA02007036A (es) 2000-01-20 2002-12-13 Eisai Co Ltd Compuesto de piperidina novedoso y composicion farmaceutica del mismo.
AU2001234705A1 (en) 2000-02-01 2001-08-14 Cor Therapeutics, Inc. Indalone and benzimidazolone inhibitors of factor xa
EP1255741A2 (en) 2000-02-01 2002-11-13 Cor Therapeutics, Inc. 2- 1H]-QUINOLONE AND 2- 1H]-QUINOXALONE INHIBITORS OF FACTOR Xa
US6906063B2 (en) 2000-02-04 2005-06-14 Portola Pharmaceuticals, Inc. Platelet ADP receptor inhibitors
WO2001057037A1 (en) 2000-02-04 2001-08-09 Cor Therapeutics, Inc. Platelet adp receptor inhibitors
GB0002740D0 (en) 2000-02-07 2000-03-29 Novartis Ag Organic compounds
WO2001058448A1 (fr) 2000-02-09 2001-08-16 Shionogi & Co., Ltd. Inhibiteur d'apoptose
KR20020081334A (ko) 2000-02-21 2002-10-26 시마르 인코포레이티드 간질 치료를 위한 조성물과 방법
DE60125026T2 (de) 2000-03-23 2007-06-28 Takeda Pharmaceutical Co. Ltd. Fluorisochinolinderivate, verfahren zu ihrer herstellung und ihre anwendung
AU2001249397A1 (en) 2000-03-24 2001-10-08 Cor Therapeutics, Inc. Oxindole inhibitors of factor xa
DE10024938A1 (de) 2000-05-19 2001-11-22 Bayer Ag Substituierte Iminoazine
WO2001092188A1 (fr) 2000-05-29 2001-12-06 Shionogi & Co., Ltd. Procede de marquage au tritium
ES2320973T3 (es) 2000-06-12 2009-06-01 EISAI R&D MANAGEMENT CO., LTD. Compuestos de 1,2-dihidropiridina, procedimiento para su preparacion y uso de los mismos.
DE10034803A1 (de) 2000-07-18 2002-01-31 Bayer Ag Substituierte Sulfonsäureanilide
WO2002014282A1 (fr) 2000-08-11 2002-02-21 Eisai Co., Ltd. Composes 2-aminopyridine et leur utilisation comme medicaments
US20020049211A1 (en) 2000-09-06 2002-04-25 Sobolov-Jaynes Susan Beth Combination treatment for depression and anxiety
HU228961B1 (en) 2000-09-18 2013-07-29 Eisai R & D Man Co Triazinones and their use as active ingredients of pharmaceutical compositions
ATE319706T1 (de) 2000-09-19 2006-03-15 Centre Nat Rech Scient Pyridinon und pyridinethion-derivate mit hiv- hemmenden eigenschaften
CN1120151C (zh) 2000-10-24 2003-09-03 大连化学工业股份有限公司 制备内酰胺的方法
EP1337150A4 (en) 2000-10-27 2007-09-26 Dow Agrosciences Llc SUBSTITUTED 4,5-DIHYDRO-1,2,4-TRIAZIN-6-ONE, 1,2,4-TRIAZIN-6-ONE AND THEIR USE AS FUNGICIDES AND INSECTICIDES
US6670380B2 (en) 2000-11-20 2003-12-30 Bristol-Myers Squibb Co. Pyridone inhibitors of fatty acid binding protein and method
YU52403A (sh) 2000-12-26 2006-03-03 Dr.Reddy's Research Foundation Heterociklična jedinjenja koja imaju antibakterijsko dejstvo, postupak za njihovo dobijanje i farmaceutske smeše koje ih sadrže
US7160912B2 (en) 2000-12-26 2007-01-09 Dr.Reddy's Laboratories Ltd. Heterocyclic compounds having antibacterial activity: process for their preparation and pharmaceutical compositions containing them
CA2433158C (en) 2000-12-28 2011-05-10 Shionogi & Co., Ltd. Pyridone derivatives having a binding activity to the cannabinoid type 2 receptor
US7867516B2 (en) 2001-01-29 2011-01-11 Shionogi & Co., Ltd. Medicinal preparation containing 5-methyl-1-phenyl-2-(1h)-pyridone as active ingredient
WO2002062816A1 (en) * 2001-02-07 2002-08-15 Celltech R & D Limited Non-natural nucleotides and dinucleotides
DE10108995A1 (de) 2001-02-23 2002-09-05 Abbott Gmbh & Co Kg Substituierte Pyrimidinon-Derivate als Liganden von Integrinrezeptoren
WO2002085858A1 (fr) 2001-04-20 2002-10-31 Asahi Glass Company, Limited Procede de production d'un derive de piperidine purifie
CA2444531A1 (en) 2001-05-08 2002-11-14 Kudos Pharmaceuticals Limited Isoquinolinone derivatives as parp inhibitors
AU2002316180A1 (en) 2001-06-01 2002-12-16 The Regents Of The University Of California Inhibitors of cell proliferation, angiogenesis, fertility, and muscle contraction
JP2002371078A (ja) 2001-06-12 2002-12-26 Sankyo Co Ltd キノリン誘導体及びキノロン誘導体
JP4180254B2 (ja) 2001-06-29 2008-11-12 独立行政法人科学技術振興機構 窒素含有６員環の製造方法
JP2003021901A (ja) 2001-07-05 2003-01-24 Fuji Photo Film Co Ltd 感光性平版印刷版の光重合方法
KR100898888B1 (ko) 2001-08-06 2009-05-21 시오노기세이야쿠가부시키가이샤 5-메틸-1-페닐-2(1ｈ)피리디논의 제조 방법
WO2003035650A1 (fr) 2001-09-25 2003-05-01 Takeda Chemical Industries, Ltd. Inhibiteur d'entree
GB0124848D0 (en) 2001-10-16 2001-12-05 Celltech R&D Ltd Chemical compounds
TWI301834B (en) 2001-10-22 2008-10-11 Eisai R&D Man Co Ltd Pyrimidone compound and pharmaceutical composition including the same
TWI330183B (es) 2001-10-22 2010-09-11 Eisai R&D Man Co Ltd
CN1257901C (zh) 2001-11-08 2006-05-31 中国科学院上海药物研究所 一类四氢喹啉酮哌啶类化合物及其制备方法和用途
US7030141B2 (en) * 2001-11-29 2006-04-18 Christopher Franklin Bigge Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade
GB0129260D0 (en) 2001-12-06 2002-01-23 Eisai London Res Lab Ltd Pharmaceutical compositions and their uses
GB0129391D0 (en) 2001-12-07 2002-01-30 Syngenta Participations Ag Microbiocidal n-phenyl-n-[4-(4-pyridyl)-2-pyrimidin-2-yl]-amine derivatives
JP2005170790A (ja) 2002-01-09 2005-06-30 Ajinomoto Co Inc Ｎ−アルキルスルフォニル置換アミド誘導体
EP1470112A1 (en) 2002-01-18 2004-10-27 Pharmacia Corporation Substituted pyridazinones as inhibitors of p38
DE60330126D1 (de) 2002-02-14 2009-12-31 Pharmacia Corp Substituierte pyridinone als modulatoren für p38 map kinase
JP2003238611A (ja) 2002-02-18 2003-08-27 Japan Polyolefins Co Ltd オレフィン類重合用触媒成分、オレフィン類重合用触媒及びポリオレフィン類の製造方法
JPWO2003070277A1 (ja) 2002-02-19 2005-06-09 塩野義製薬株式会社 抗掻痒剤
JP2003261535A (ja) 2002-03-08 2003-09-19 Mitsubishi Chemicals Corp ２−ヒドロキシ−５−メチルピリジンの製造方法
JP2005526068A (ja) 2002-03-14 2005-09-02 バイエル・ヘルスケア・アクチェンゲゼルシャフト 抗炎症剤としての単環式アロイルピリジノン類
WO2003082265A2 (en) 2002-04-02 2003-10-09 Fujisawa Pharmaceutical Co Pharmaceutical composition for treating or preventing virus infectious diseases
GB0210127D0 (en) 2002-05-02 2002-06-12 Merck Sharp & Dohme Therapeutic agents
WO2003097062A1 (en) 2002-05-13 2003-11-27 Merck & Co., Inc. Phenyl substituted imidazopyridines and phenyl substituted benzimidazoles
JP2004043458A (ja) 2002-05-22 2004-02-12 Kyorin Pharmaceut Co Ltd ４−アリール−５−ヒドロキシイソキノリン誘導体およびその製造法
CN1218942C (zh) 2002-06-11 2005-09-14 中南大学湘雅医学院 抗纤维化吡啶酮化合物及其生产工艺方法
CA2488635C (en) 2002-06-12 2012-10-23 Abbott Laboratories Antagonists of melanin concentrating hormone receptor
US20040006135A1 (en) 2002-06-19 2004-01-08 Pfizer Inc. Combination treatment for depression and anxiety
GB0214268D0 (en) 2002-06-20 2002-07-31 Celltech R&D Ltd Chemical compounds
GB0215293D0 (en) 2002-07-03 2002-08-14 Rega Foundation Viral inhibitors
WO2004006906A2 (en) 2002-07-15 2004-01-22 Combinatorx, Incorporated Methods for the treatment of neoplasms
CA2492342C (en) 2002-07-22 2011-03-22 Orchid Chemicals & Pharmaceuticals Ltd. Novel bio-active pyrimidine derivatives
KR20050030636A (ko) * 2002-07-24 2005-03-30 교린 세이야꾸 가부시키 가이샤 4-(치환된 아릴)-5-하이드록시이소퀴놀리논 유도체
GB0218630D0 (en) 2002-08-10 2002-09-18 Tanabe Seiyaku Co Novel compounds
BR0313459A (pt) 2002-08-13 2005-06-21 Warner Lambert Co Derivados monocìclicos como inibidores de metaloproteinases de matriz
JP2006502152A (ja) 2002-08-28 2006-01-19 インターミューン インコーポレイテッド 線維性疾患治療用の併用療法
WO2004024694A1 (ja) 2002-09-10 2004-03-25 Kyorin Pharmaceutical Co., Ltd. ４-置換アリール-５-ヒドロキシイソキノリノン誘導体
WO2004024078A2 (en) 2002-09-11 2004-03-25 Merck & Co., Inc. Dihydroxypyridopyrazine-1,6-dione compounds useful as hiv integrase inhibitors
CH696420A5 (de) 2002-09-13 2007-06-15 Mepha Ag Neue stabile Zubereitungen von Alkyl-, Phenyl-Pyridonen für topische Anwendung.
EP1400243A1 (en) 2002-09-19 2004-03-24 Tanabe Seiyaku Co., Ltd. Calcium-activated K channel activator
GB0222743D0 (en) 2002-10-01 2002-11-06 Celltech R&D Ltd Chemical compounds
WO2004031145A2 (en) 2002-10-02 2004-04-15 Bristol-Myers Squibb Company Lactam-containing diaminoalkyl, beta-aminoacids, alpha-aminoacids and derivatives thereof as factor xa inhibitors
WO2004035563A1 (en) * 2002-10-17 2004-04-29 Syngenta Participations Ag 3-heterocyclylpyridine derivatives useful as herbicides
WO2004037159A2 (en) 2002-10-23 2004-05-06 Obetherapy Biotechnology Compounds, compositions and methods for modulating fat metabolism
US6930117B2 (en) 2002-11-09 2005-08-16 The Procter & Gamble Company N-alkyl-4-methyleneamino-3-hydroxy-2-pyridones
PE20040844A1 (es) 2002-11-26 2004-12-30 Novartis Ag Acidos fenilaceticos y derivados como inhibidores de la cox-2
JP4542743B2 (ja) 2002-12-26 2010-09-15 Ｋｄｌ株式会社 ピリドン誘導体の溶液状医薬組成物
US7144911B2 (en) 2002-12-31 2006-12-05 Deciphera Pharmaceuticals Llc Anti-inflammatory medicaments
US7202257B2 (en) 2003-12-24 2007-04-10 Deciphera Pharmaceuticals, Llc Anti-inflammatory medicaments
US20040142950A1 (en) 2003-01-17 2004-07-22 Bunker Amy Mae Amide and ester matrix metalloproteinase inhibitors
US7618974B2 (en) 2003-01-31 2009-11-17 Vertex Pharmaceuticals Incorporated Gyrase inhibitors and uses thereof
US7569591B2 (en) 2003-01-31 2009-08-04 Vertex Pharmaceuticals Incorporated Gyrase inhibitors and uses thereof
US7582641B2 (en) 2003-01-31 2009-09-01 Vertex Pharmaceuticals Incorporated Gyrase inhibitors and uses thereof
AR042956A1 (es) 2003-01-31 2005-07-13 Vertex Pharma Inhibidores de girasa y usos de los mismos
US20040157738A1 (en) 2003-02-12 2004-08-12 Ishihara Sangyo Kaisha, Ltd. Novel oxygen containing fused cyclic derivatives and herbicidal, desiccant and defoliate compositions containing them
CL2004000234A1 (es) 2003-02-12 2005-04-15 Biogen Idec Inc Compuestos derivados 3-(piridin-2-il)-4-heteroaril-pirazol sustituidos, antagonistas de aik5 y/o aik4; composicion farmaceutica y uso del compuesto en el tratamiento de desordenes fibroticos como esclerodermia, lupus nefritico, cicatrizacion de herid
PL378111A1 (pl) 2003-02-14 2006-03-06 Smithkline Beecham Corporation Nowe związki
US7012088B2 (en) 2003-02-24 2006-03-14 Pharmacia & Upjohn Company Indolone oxazolidinones and derivatives thereof
EP1603563A4 (en) 2003-02-28 2007-08-22 Morgan Lee R RESONANCE MODULATOR FOR DIAGNOSIS AND THERAPY
EP1599171A2 (en) 2003-02-28 2005-11-30 Intermune, Inc. Combination therapy for treating alphavirus infection and liver fibrosis
JP2004269469A (ja) 2003-03-12 2004-09-30 Yamanouchi Pharmaceut Co Ltd ピリミジン誘導体又はその塩
WO2004089914A1 (de) 2003-04-08 2004-10-21 Basf Aktiengesellschaft Benzolsulfonamid-derivate als herbizide oder desikkante/defoliante verbindungen
JP4089491B2 (ja) 2003-04-14 2008-05-28 コニカミノルタホールディングス株式会社 重合開始剤、重合組成物、ラジカル発生方法、平版印刷版材料および平版印刷版の作製方法
US20070032457A1 (en) 2003-05-16 2007-02-08 Blatt Lawrence M Combination therapy for cancer treatment
US20070092488A1 (en) 2003-05-16 2007-04-26 Intermune Inc. Methods of treating idiopathic pulmonary fibrosis
WO2004105684A2 (en) 2003-05-16 2004-12-09 Intermune, Inc. Combination therapy for proliferative disorders
JP2004359641A (ja) 2003-06-06 2004-12-24 Ono Pharmaceut Co Ltd Ｃｃｒ５活性化剤
WO2005000227A2 (en) 2003-06-06 2005-01-06 Intermune, Inc. Methods of treating tnf-mediated disorders
AU2004249495A1 (en) 2003-06-20 2004-12-29 Ucb Pharma S.A. Thienopyridone derivatives as kinase inhibitors
AU2004249498B2 (en) 2003-06-20 2009-11-19 Ucb Pharma S.A. Thienopyridone derivatives as kinase inhibitors
JP2005013152A (ja) 2003-06-27 2005-01-20 Asahi Kasei Corp 細胞分化抑制剤及びこれを用いた細胞培養方法、培養液、培養された細胞
WO2005000818A1 (en) 2003-06-27 2005-01-06 Warner-Lambert Company Llc 5-substituted-4-`(substituted phenyl)!amino!-2-pyridone deviatives for use as mek inhibitors
US20050153941A1 (en) 2003-06-27 2005-07-14 Tomoyuki Miyabayashi Cell differntiation inhibiting agent, cell culture method using the same, culture medium, and cultured cell line
EP2236131A3 (en) 2003-07-01 2011-03-02 President and Fellows of Harvard College Sirt1 modulators for manipulating cell/organism lifespan/stress response
US20060025337A1 (en) 2003-07-01 2006-02-02 President And Fellows Of Harvard College Sirtuin related therapeutics and diagnostics for neurodegenerative diseases
WO2005007632A1 (en) 2003-07-18 2005-01-27 Pharmacia Corporation Substituted pyridazinones as inhibitors of p38
RU2355687C2 (ru) 2003-08-01 2009-05-20 Дженелэбс Текнолоджиз, Инк Бициклические производные имидазола в качестве средства против вирусов семейства flaviviridae
NL1026826C2 (nl) 2003-08-13 2007-01-04 Pharmacia Corp Gesubstitueerde pyridinonen.
JP2007504238A (ja) 2003-09-04 2007-03-01 アベンティス・ファーマスーティカルズ・インコーポレイテツド ポリ（ａｄｐ−リボース）ポリメラーゼ（ｐａｒｐ）の阻害剤としての置換インドール
US20050065144A1 (en) 2003-09-08 2005-03-24 Syrrx, Inc. Dipeptidyl peptidase inhibitors
SE0302486D0 (sv) 2003-09-18 2003-09-18 Astrazeneca Ab Novel compounds
SE0302487D0 (sv) 2003-09-18 2003-09-18 Astrazeneca Ab Novel compounds
DE10345648A1 (de) 2003-10-01 2005-04-21 Studiengesellschaft Kohle Mbh Verfahren zur Herstellung von TMC-69-6H und verwandten Pyridonderivaten und deren Verwendung als Phosphatase-Inhibitoren
WO2005039598A1 (en) 2003-10-24 2005-05-06 Intermune, Inc. Method of treating alcoholic liver disease
US7407973B2 (en) 2003-10-24 2008-08-05 Intermune, Inc. Use of pirfenidone in therapeutic regimens
JP4170198B2 (ja) 2003-11-14 2008-10-22 一丸ファルコス株式会社 化粧料組成物
AU2003284808B2 (en) 2003-11-14 2009-01-22 Catalyst Biosciences, Inc. The derivatives of pyridone and the use of them
EP1689387B1 (en) 2003-11-19 2011-09-14 Array Biopharma, Inc. Bicyclic inhibitors of mek and methods of synthesis thereof
US7732616B2 (en) 2003-11-19 2010-06-08 Array Biopharma Inc. Dihydropyridine and dihydropyridazine derivatives as inhibitors of MEK and methods of use thereof
US7517994B2 (en) 2003-11-19 2009-04-14 Array Biopharma Inc. Heterocyclic inhibitors of MEK and methods of use thereof
JPWO2005051949A1 (ja) * 2003-11-26 2007-06-21 住友製薬株式会社 新規縮合イミダゾール誘導体
DE10358004A1 (de) 2003-12-11 2005-07-14 Abbott Gmbh & Co. Kg Ketolactam-Verbindungen und ihre Verwendung
US20070191336A1 (en) 2003-12-24 2007-08-16 Flynn Daniel L Anti-inflammatory medicaments
JP4859672B2 (ja) 2004-01-29 2012-01-25 ファイザー株式会社 ５−ｈｔ４受容体作動活性を有する１−イソプロピル−２−オキソ−１，２−ジヒドロピリジン−３−カルボキサミド誘導体
GB0402812D0 (en) 2004-02-09 2004-03-10 Tanabe Seiyaku Co Novel compounds
JP2005255675A (ja) 2004-02-09 2005-09-22 Tanabe Seiyaku Co Ltd 医薬組成物
WO2005090294A2 (en) 2004-02-20 2005-09-29 Japan Science And Technology Agency PROCESS OF MAKING α-AMINOOXYKETONE/α-AMINOOXYALDEHYDE AND α-HYDROXYKETONE/α-HYDROXYALDEHYDE COMPOUNDS AND A PROCESS OF MAKING REACTION PRODUCTS FROM CYCLIC α,ß-UNSATURATED KETONE SUBSTRATES AND NITROSO SUBSTRATES
EP1741703A4 (en) 2004-03-05 2009-11-25 Banyu Pharma Co Ltd PYRIDONE DERIVATIVE
PE20060285A1 (es) 2004-03-30 2006-05-08 Aventis Pharma Inc Piridonas sustituidas como inhibidores de pol(adp-ribosa)-polimerasa (parp)
EP2522670A1 (en) 2004-04-07 2012-11-14 Takeda Pharmaceutical Company Limited Heterocyclic CRF receptor antagonists
NZ551027A (en) 2004-04-08 2011-01-28 Targegen Inc Benzotriazine inhibitors of kinases
MY143245A (en) 2004-04-28 2011-04-15 Mitsubishi Tanabe Pharma Corp 4- 2-(cycloalkylamino)pyrimidin-4-yl-(phenyl)-imidazolin-2-one derivatives as p38 map-kinase inhibitors for the treatment of inflammatory diseases
JPWO2005105743A1 (ja) 2004-04-28 2008-03-13 小野薬品工業株式会社 含窒素複素環化合物およびその医薬用途
DE102004028973A1 (de) * 2004-06-16 2006-01-05 Sanofi-Aventis Deutschland Gmbh Substituierte Tetrahydro-2H-isochinolin-1-on-Derivate, Verfahren zu ihrer Herstellung und ihre Verwendung als Medikament
CA2565437A1 (en) 2004-06-18 2006-01-05 Millennium Pharmaceuticals, Inc. Factor xa inhibitors
US7696352B2 (en) 2004-06-18 2010-04-13 Millennium Pharmaceuticals, Inc. Factor Xa inhibitors
MY148809A (en) 2004-07-06 2013-05-31 Eisai R&D Man Co Ltd Crystals of 1,2-dihydropyridine compound and their production process
WO2006011024A2 (en) 2004-07-19 2006-02-02 Glenmark Pharmaceuticals Ltd. New tricyclic compounds useful for the treatment of inflammatory and allergic disorders: process for their preparation and pharmaceutical compositions containing them
US20090054358A1 (en) 2004-07-19 2009-02-26 The John Hopkins University Flt3 inhibitors for immune suppression
BRPI0514094A (pt) 2004-08-02 2008-05-27 Osi Pharm Inc composto, composição, e, método de tratamento de distúrbio hiperproliferativo
AU2005280167A1 (en) 2004-08-31 2006-03-09 Biogen Idec Ma Inc. Pyrimidinylpyrazoles as TGF-beta inhibitors
GB0420722D0 (en) 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
US7694674B2 (en) * 2004-09-21 2010-04-13 Carleton Life Support Systems, Inc. Oxygen generator with storage and conservation modes
DK1809622T3 (da) 2004-09-22 2010-11-08 Janssen Pharmaceutica Nv Inhibitorer af interaktionen mellem MDM2 og P53
US20060069260A1 (en) 2004-09-28 2006-03-30 Huiping Zhang Preparation of N-aryl pyridones
JP4223457B2 (ja) 2004-10-06 2009-02-12 本田技研工業株式会社 車両の電動ステアリング装置
WO2006038734A1 (en) 2004-10-08 2006-04-13 Astellas Pharma Inc. Pyridazinone derivatives cytokines inhibitors
NZ554493A (en) 2004-10-12 2009-09-25 Decode Genetics Ehf Aryl sulfonamide peri-substituted bicyclics for occlusive artery disease
TWI360539B (en) 2004-10-28 2012-03-21 Shionogi & Co 3-carbamoyl-2-pyridone derivatives
JP4973191B2 (ja) 2004-11-10 2012-07-11 小野薬品工業株式会社 含窒素複素環化合物およびその医薬用途
WO2006055918A2 (en) 2004-11-19 2006-05-26 Pharmacopeia Drug Discovery, Inc. One-dimensional qsar models
JP2006142666A (ja) 2004-11-19 2006-06-08 Mitsubishi Chemicals Corp 光学記録媒体用色素
CA2587853A1 (en) 2004-11-23 2006-06-01 Wyeth Gonadotropin releasing hormone receptor antagonists
AU2005308956A1 (en) 2004-11-24 2006-06-01 Merck Serono Sa Novel 4-arylamino pyridone derivatives as MEK inhibitors for the treatment of hyperproliferative disorders
RU2412936C2 (ru) 2004-11-24 2011-02-27 Вертекс Фармасьютикалз Инкорпорейтед Производные 3-[2-(3-ациламино-2-оксо-2н-пиридин-1-ил)-ацетиламино]-4-оксо-пентановой кислоты и их применение в качестве ингибиторов каспазы
EP1833480A2 (en) 2004-11-30 2007-09-19 Artesian Therapeutics, Inc. Cardiotonic compounds with inhibitory activity against beta-adrenergic receptors and phosphodiesterase
CA2588867A1 (en) 2004-12-01 2006-06-08 Banyu Pharmaceutical Co., Ltd. Substituted pyridone derivative
KR20070100743A (ko) 2004-12-17 2007-10-11 애나디스 파마슈티칼스, 인코포레이티드 피리다지논 화합물
ATE479662T1 (de) 2004-12-23 2010-09-15 Hui Yao Pyrimidinonverbindungen, ihre herstellung und ihre verwendung
WO2006072037A1 (en) * 2004-12-29 2006-07-06 E. I. Du Pont De Nemours And Company Dihydronepetalactams and n-substituted derivatives thereof
CN101090890A (zh) * 2004-12-29 2007-12-19 纳幕尔杜邦公司 二氢荆芥内酰胺及其n－取代衍生物
US20060148842A1 (en) * 2004-12-29 2006-07-06 Scialdone Mark A Nepetalactams and N-substituted derivatives thereof
CN101090889A (zh) * 2004-12-29 2007-12-19 纳幕尔杜邦公司 荆芥内酰胺及其n－取代衍生物
US20060276393A1 (en) 2005-01-13 2006-12-07 Sirtris Pharmaceuticals, Inc. Novel compositions for preventing and treating neurodegenerative and blood coagulation disorders
AU2006206274A1 (en) 2005-01-20 2006-07-27 Sirtris Pharmaceuticals, Inc. Use of sirtuin-activating compounds for treating flushing and drug induced weight gain
JPWO2006082872A1 (ja) * 2005-02-04 2008-06-26 エーザイ・アール・アンド・ディー・マネジメント株式会社 １−（ピペリジン−４−イル）−１ｈ−インドール誘導体
US7534796B2 (en) 2005-02-18 2009-05-19 Wyeth Imidazo[4,5-b]pyridine antagonists of gonadotropin releasing hormone receptor
US7582634B2 (en) 2005-02-18 2009-09-01 Wyeth 7-substituted imidazo[4,5-c]pyridine antagonists of gonadotropin releasing hormone receptor
CN1676518B (zh) 2005-03-17 2010-05-12 南开大学 4-取代苯基哒嗪类化合物及除草活性
AU2006232517A1 (en) 2005-04-04 2006-10-12 Eisai R&D Management Co., Ltd. Dihydropyridine compounds and compositions for headaches
AU2006234627C1 (en) 2005-04-08 2009-11-26 Eisai R & D Management Co., Ltd. Therapeutic agent for dyskinesia
CN1846699A (zh) 2005-04-13 2006-10-18 中南大学湘雅医院 1－(取代苯基)－5－甲基－2－(1h) 吡啶酮(i)化合物用于制备抗除肾间质纤维化外其他器官纤维化或组织纤维化药物的应用
JO2787B1 (en) 2005-04-27 2014-03-15 امجين إنك, Alternative amide derivatives and methods of use
EP1877376A1 (de) 2005-04-28 2008-01-16 Boehringer Ingelheim International GmbH Neue verbindungen zur behandlung von entzündlichen erkrankungen
RS53599B1 (en) 2005-05-10 2015-02-27 Intermune, Inc. PIRIDON DERIVATIVES FOR STRESS MODULATION OF ACTIVATED PROTEIN KINASE SYSTEMS
GB0511190D0 (en) 2005-06-01 2005-07-06 Sterix Ltd Use
AU2006255009B2 (en) 2005-06-07 2011-10-27 Pharmacopeia L.L.C. Azinone and diazinone V3 inhibitors for depression and stress disorders
RU2007147959A (ru) 2005-06-08 2009-07-20 Новартис АГ (CH) Органические соединения
CA2611401C (en) 2005-06-10 2014-02-11 Merck Patent Gesellschaft Mit Beschraenkter Haftung Oxindoles as kinase inhibitors
WO2006138418A2 (en) 2005-06-14 2006-12-28 President And Fellows Of Harvard College Improvement of cognitive performance with sirtuin activators
CA2608821A1 (en) 2005-06-15 2006-12-28 Shibo Jiang Anti-viral compositions comprising heterocyclic substituted phenyl furans and related compounds
CA2613141A1 (en) 2005-07-07 2007-01-18 Sirtris Pharmaceuticals, Inc. Methods and related compositions for treating or preventing obesity, insulin resistance disorders, and mitochondrial-associated disorders
WO2007006591A2 (fr) 2005-07-13 2007-01-18 Bayer Cropscience Sa Dihalogenation d'hydroxipyridones n,o-disubstituees et leurs utilisations
JP2007063268A (ja) 2005-08-05 2007-03-15 Tanabe Seiyaku Co Ltd 医薬組成物
JP2007056213A (ja) 2005-08-26 2007-03-08 Fujifilm Corp 焼結含油軸受油用組成物、並びにそれを用いた軸受け装置及び摺動部材
TW200745034A (en) 2005-09-01 2007-12-16 Astellas Pharma Inc New compounds
NZ591443A (en) 2005-09-22 2013-04-26 Intermune Inc Granule formation of pirfenidone and pharmaceutically acceptable excipients
WO2007037543A1 (ja) 2005-09-29 2007-04-05 Banyu Pharmaceutical Co., Ltd. ビアリールアミド誘導体
RU2008112691A (ru) 2005-10-03 2009-10-10 Оно Фармасьютикал Ко., Лтд. (Jp) Азотсодержащее гетероциклическое соединение и его фармацевтическое применение
WO2007044796A2 (en) 2005-10-11 2007-04-19 Nps Pharmaceuticals, Inc. Pyridazinone compounds as calcilytics
US8101625B2 (en) 2005-10-21 2012-01-24 Exelixis, Inc. Pyrimidinones as Casein Kinase II (CK2) modulators
JP2007145819A (ja) 2005-10-28 2007-06-14 Tanabe Seiyaku Co Ltd 医薬組成物
WO2007053610A2 (en) 2005-11-01 2007-05-10 The Regents Of The University Of California Methods of treating atrial fibrillation wtih pirfenidone
DE602006017741D1 (de) 2005-11-18 2010-12-02 Hoffmann La Roche Azaindol-2-carboxamid-derivate
EP1953147A1 (en) * 2005-11-21 2008-08-06 Japan Tobacco, Inc. Heterocyclic compound and medicinal application thereof
CA2630752A1 (en) 2005-11-23 2007-05-31 Intermune, Inc. Method of modulating stress-activated protein kinase system
NZ568666A (en) 2005-11-30 2011-09-30 Vertex Pharma [1,2,4]Triazolo[3,4-b][1,3,4]thiadiazole derivative as inhibitors of c-Met
JPWO2007072868A1 (ja) 2005-12-21 2009-06-04 エーザイ・アール・アンド・ディー・マネジメント株式会社 １，２−ジヒドロピリジン化合物の結晶（ｉｖ型）
JPWO2007072869A1 (ja) 2005-12-21 2009-06-04 エーザイ・アール・アンド・ディー・マネジメント株式会社 １，２−ジヒドロピリジン化合物の非晶質体
WO2007076104A1 (en) 2005-12-23 2007-07-05 Amgen Inc. Vanilloid receptor ligands and their use in treatments
JP2009523170A (ja) * 2006-01-11 2009-06-18 メルク エンド カムパニー インコーポレーテッド 縮合トリアゾールタキキニン受容体アンダニスト
UY30117A1 (es) 2006-01-31 2007-06-29 Tanabe Seiyaku Co Compuesto amina trisustituido
EP1982978B1 (en) 2006-02-02 2014-08-27 Kumiai Chemical Industry Co., Ltd. Pyridone derivative and herbicide
TW200803855A (en) 2006-02-24 2008-01-16 Kalypsys Inc Quinolones useful as inducible nitric oxide synthase inhibitors
US7728031B2 (en) 2006-02-24 2010-06-01 Abbott Laboratories Octahydro-pyrrolo[3,4-b]pyrrole derivatives
US8034822B2 (en) 2006-03-08 2011-10-11 Takeda San Diego, Inc. Glucokinase activators
WO2007108968A2 (en) 2006-03-13 2007-09-27 Merck & Co., Inc. Ophthalmic compositions for treating ocular hypertension
CN100396669C (zh) 2006-03-15 2008-06-25 浙江省医学科学院 一种抗纤维化药物吡非尼酮的制备方法
AU2007228784B2 (en) 2006-03-22 2012-03-08 Janssen Pharmaceutica N.V. Cyclic-alkylaminederivatives as inhibitors of the interaction between MDM2 and p53
WO2007117559A2 (en) 2006-04-05 2007-10-18 Vitae Pharmaceuticals, Inc. Renin inhibitors
WO2007117482A2 (en) 2006-04-05 2007-10-18 Vitae Pharmaceuticals, Inc. Renin inhibitors
CN101460634A (zh) 2006-04-13 2009-06-17 康乃尔研究基金会有限公司 用于靶向c-rel的方法和组合物
WO2007127475A2 (en) 2006-04-28 2007-11-08 Northwestern University Pyridazines for demyelinating diseases and neuropathic pain
US8158627B2 (en) 2006-04-28 2012-04-17 Northwestern University Compositions and treatments using pyridazine compounds and cholinesterase inhibitors
HUE033281T2 (en) 2006-05-04 2017-11-28 Chroma Therapeutics Ltd p38 mitogen-activated protein (MAP) kinase inhibitors
JP5227311B2 (ja) 2006-05-05 2013-07-03 ミレニアム ファーマシューティカルズ， インコーポレイテッド 第Ｘａ因子阻害剤
WO2007139150A1 (ja) 2006-05-30 2007-12-06 The University Of Tokushima ＴＮＦα阻害物質を含有してなる抗インフルエンザウイルス剤
AU2007257959A1 (en) 2006-06-09 2007-12-21 Kemia, Inc. Therapy using cytokine inhibitors
CN101484167B (zh) 2006-06-15 2012-07-04 上海睿星基因技术有限公司 吡啶酮类衍生物预防和治疗放射性肺损伤的用途
GB0612428D0 (en) 2006-06-22 2006-08-02 Prolysis Ltd Antibacterial agents
GB0724349D0 (en) 2007-12-13 2008-01-30 Prolysis Ltd Antibacterial agents
EP2037905B1 (en) 2006-06-23 2013-05-01 Radius Health, Inc. Treatment of vasomotor symptoms with selective estrogen receptor modulators
MX2009000661A (es) 2006-07-19 2009-03-27 Univ Georgia Res Found Piridinon-diceto-acidos: inhibidores de replicacion de vih en terapia de combinacion.
CA2658462C (en) 2006-07-20 2011-09-27 Amgen Inc. Substituted pyridone compounds and methods of use
DK2069312T3 (da) 2006-07-25 2013-02-04 Cephalon Inc Pyridazinonderivater
JP4747985B2 (ja) 2006-08-02 2011-08-17 コニカミノルタオプト株式会社 光学フィルム、それを用いた偏光板及び液晶表示装置
CN101506174B (zh) 2006-08-02 2012-05-02 株式会社Lg生命科学 基于哒嗪酮骨架的半胱天冬蛋白酶抑制剂
JP5073746B2 (ja) 2006-08-25 2012-11-14 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 Ｍｃｈ拮抗作用を有する新規ピリドン誘導体及びこの化合物を含む薬物
CN100516126C (zh) 2006-09-06 2009-07-22 北京理工大学 一种离子液体
PE20080839A1 (es) 2006-09-11 2008-08-23 Cgi Pharmaceuticals Inc Determinadas amidas sustituidas, metodo de elaboracion y metodo de uso de las mismas
JP2008076948A (ja) 2006-09-25 2008-04-03 Konica Minolta Medical & Graphic Inc 感光性平版印刷版材料
WO2008051416A2 (en) * 2006-10-19 2008-05-02 Synta Pharmaceuticals Corp. Compounds that inhibit the activity of hsp90 for treating infections
SI2089364T1 (sl) 2006-11-08 2013-10-30 Bristol-Myers Squibb Company Spojine piridinona
KR20080045538A (ko) 2006-11-20 2008-05-23 에스케이케미칼주식회사 피리딘 화합물을 포함하는 염증 및 면역질환 치료용 약제조성물
CN1962642A (zh) 2006-11-21 2007-05-16 南开大学 具有除草活性的三氟甲基苯基哒嗪类衍生物及制备方法
GB0624105D0 (en) 2006-12-01 2007-01-10 Sterix Ltd Use
EP2102208B1 (en) 2006-12-05 2014-04-23 Janssen Pharmaceutica NV Novel substituted diaza spiro pyridinone derivatives for use in mch-1 mediated diseases
JP5278318B2 (ja) 2006-12-14 2013-09-04 アステラス製薬株式会社 Ｃｒｔｈ２拮抗剤および抗アレルギー剤として有用な多環酸化合物
EA015559B1 (ru) 2006-12-14 2011-08-30 Эли Лилли Энд Компани ПРОИЗВОДНЫЕ 5-[4-(АЗЕТИДИН-3-ИЛОКСИ)ФЕНИЛ]-2-ФЕНИЛ-5H-ТИАЗОЛО[5,4-c]ПИРИДИН-4-ОНА И ИХ ИСПОЛЬЗОВАНИЕ В КАЧЕСТВЕ РЕЦЕПТОРОВ MCH
EP2091947A2 (en) 2006-12-20 2009-08-26 Takeda San Diego, Inc. Glucokinase activators
EP2518063B1 (en) 2006-12-21 2017-02-01 Sloan-Kettering Institute For Cancer Research Pyridazinones and furan-containing compounds
US7795249B2 (en) 2006-12-22 2010-09-14 Millennium Pharmaceuticals, Inc. Certain pyrazoline derivatives with kinase inhibitory activity
MX2009005825A (es) * 2006-12-27 2009-06-16 Sanofi Aventis Derivados de isoquinolina e isoquinolinona sustituidos en calidad de inhibidores de rho-quinasa.
MX2009007831A (es) * 2007-01-22 2010-01-15 Gtx Inc Agentes de union de receptor nuclear.
US9623021B2 (en) * 2007-01-22 2017-04-18 Gtx, Inc. Nuclear receptor binding agents
CN101235030A (zh) 2007-01-30 2008-08-06 中南大学 1-取代-5-三氟甲基-2-(1h)吡啶酮化合物、制备方法及其用途
US8314087B2 (en) 2007-02-16 2012-11-20 Amgen Inc. Nitrogen-containing heterocyclyl ketones and methods of use
DE102007007751A1 (de) 2007-02-16 2008-08-21 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue substituierte Arylsulfonylglycine, deren Herstellung und deren Verwendung als Arzneimittel
WO2008106202A1 (en) 2007-02-27 2008-09-04 Housey Gerard M Theramutein modulators
JP5134834B2 (ja) 2007-03-01 2013-01-30 東ソー株式会社 ５，５−二置換−３−ピロリン−２−オン誘導体の製造方法
TW200900065A (en) 2007-03-07 2009-01-01 Janssen Pharmaceutica Nv 3-cyano-4-(4-pyridinyloxy-phenyl)-pyridin-2-one derivatives
GB0722769D0 (en) 2007-11-21 2008-01-02 Biolipox Ab New compounds
US8586619B2 (en) 2007-03-12 2013-11-19 Vm Therapeutics Llc Agents of calcium ion channel modulators
KR20100049500A (ko) 2007-03-15 2010-05-12 쉐링 코포레이션 글루칸 신타제 억제제로서 유용한 피리다지논 유도체
CN101674833A (zh) 2007-03-20 2010-03-17 柯瑞斯公司 含有锌结合半族的Raf激酶抑制剂
EP2171478A4 (en) 2007-03-30 2013-01-30 Univ California IN VIVO IMAGING METHOD FOR SULPHOTRANSFERASES
US8283351B2 (en) 2007-04-02 2012-10-09 Institute For Oneworld Health Cyclic and acyclic hydrazine derivatives compositions including them and uses thereof
UA101611C2 (ru) 2007-04-03 2013-04-25 Аррей Байофарма Инк. СОЕДИНЕНИЯ ИМИДАЗО[1,2-а]ПИРИДИНА КАК ИНГИБИТОРЫ ТИРОЗИНКИНАЗЫ РЕЦЕПТОРОВ
WO2008124575A1 (en) 2007-04-05 2008-10-16 Smithkline Beecham Corporation Renin inhibitors
WO2008124582A1 (en) 2007-04-05 2008-10-16 Smithkline Beecham Corporation Renin inhibitors
CL2008000973A1 (es) 2007-04-05 2009-01-02 Astrazeneca Ab Compuestos derivados de 1-oxo-isoquinolina; procedimiento de preparación; composición farmacéutica; y su uso en el tratamiento de enfermedades pulmonares obstructvas crónicas (epoc) y asma.
US20100129933A1 (en) 2007-04-26 2010-05-27 Forschungszentrum Karlsruhe Gmbh Method for detecting the binding between mdm2 and the proteasome
TW200904421A (en) 2007-05-03 2009-02-01 Astellas Pharma Inc New compounds
AU2008251504B2 (en) 2007-05-09 2013-07-18 Vertex Pharmaceuticals Incorporated Modulators of CFTR
US8178091B2 (en) 2007-05-21 2012-05-15 University Of Washington Compositions and methods for the treatment of respiratory disorders
MX2007006349A (es) 2007-05-29 2009-02-18 Cell Therapy And Technology S Nuevo proceso de sintesis para la obtencion de 5-metil-1-fenil-2-(ih)-piridona, composicion y uso de la misma.
WO2008147169A2 (es) 2007-05-29 2008-12-04 Cell Therapy Technology, S.A. De C.V. Microemolsion conteniendo pirfenidona
US9603848B2 (en) 2007-06-08 2017-03-28 Senomyx, Inc. Modulation of chemosensory receptors and ligands associated therewith
US7928111B2 (en) 2007-06-08 2011-04-19 Senomyx, Inc. Compounds including substituted thienopyrimidinone derivatives as ligands for modulating chemosensory receptors
KR101583737B1 (ko) 2007-06-20 2016-01-11 오스펙스 파마슈티칼스, 인코포레이티드 섬유증 저해제로서의 치환된 ｎ-아릴 피리디논
DE102007028406A1 (de) 2007-06-20 2008-12-24 Bayer Healthcare Ag Substituierte Oxazolidinone und ihre Verwendung
CA2690087A1 (en) 2007-07-13 2009-01-22 Takahisa Hanada Ampa receptor antagonists and zonisamide for neuropathic pain
CA2690110A1 (en) 2007-07-13 2009-01-22 Eisai R&D Management Co., Ltd. Ampa receptor antagonists for neuropathic pain
EP2164488A1 (en) 2007-07-13 2010-03-24 Eisai R&D Management Co., Ltd. Ampa receptor antagonists and aldose reductase inhibitors for neuropathic pain
EA016595B1 (ru) 2007-07-17 2012-06-29 Бристол-Маерс Сквибб Компани Способ модулирования рецептора gpr119, сопряженного с g-белком, и используемые при этом соединения
DE102007035333A1 (de) 2007-07-27 2009-01-29 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue substituierte Arylsulfonylglycine, deren Herstellung und deren Verwendung als Arzneimittel
US8741803B2 (en) 2007-08-10 2014-06-03 Kumiai Chemical Industry Co., Ltd. Pesticidal composition and method for controlling pest
MX2007009796A (es) 2007-08-14 2009-02-25 Cell Therapy And Technology S Gel conteniendo pirfenidona.
CN101371833A (zh) 2007-08-23 2009-02-25 中南大学 1-芳基-2(1h)-吡啶酮类化合物在制备治疗皮肤瘙痒药物中的应用
WO2009029625A1 (en) 2007-08-27 2009-03-05 Kalypsys, Inc. 4- [heterocyclyl-methyl] -8-fluoro-quinolin-2-ones useful as nitric oxide synthase inhibitors
WO2009035598A1 (en) 2007-09-10 2009-03-19 Concert Pharmaceuticals, Inc. Deuterated pirfenidone
AU2008297877C1 (en) 2007-09-14 2013-11-07 Addex Pharma S.A. 1,3-disubstituted-4-phenyl-1 H-pyridin-2-ones
WO2009039773A1 (fr) 2007-09-19 2009-04-02 Central South University Nouvelle utilisation thérapeutique d'une aryl-2(1h)-pyridone substituée en position 1
CN101121697A (zh) * 2007-09-20 2008-02-13 东北师范大学 一种多取代吡啶-2(1h)-酮类化合物的合成方法
WO2009054544A1 (en) 2007-10-26 2009-04-30 Eisai R & D Management Co., Ltd. Ampa receptor antagonists for parkinson's disease and movement disorders
WO2009054543A1 (en) 2007-10-26 2009-04-30 Eisai R & D Management Co., Ltd. Ampa receptor antagonists and zonisamide for parkinson's disease and movement disorders
EP2203429A1 (en) 2007-10-31 2010-07-07 Nissan Chemical Industries, Ltd. Pyridazinone derivatives and use thereof as p2x7 receptor inhibitors
WO2009060835A1 (ja) 2007-11-05 2009-05-14 Kyoto University 新規ユビキリン結合性小分子
JP2011504481A (ja) 2007-11-22 2011-02-10 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 有機化合物
CN101932325B (zh) 2007-11-30 2014-05-28 新联基因公司 Ido抑制剂
WO2009076529A1 (en) 2007-12-11 2009-06-18 Research Development Foundation Small molecules for neuronal differentiation of embryonic stem cells
JP2011507800A (ja) 2007-12-26 2011-03-10 エーザイ・アール・アンド・ディー・マネジメント株式会社 癲癇、精神障害、または感覚器官の障害のためのａｍｐａ受容体アンタゴニスト
WO2009082038A2 (en) 2007-12-26 2009-07-02 Eisai R & D Management Co., Ltd. Ampa receptor antagonists and zonisamide for epilepsy
CN101977905B (zh) 2008-01-23 2014-07-02 百时美施贵宝公司 4-吡啶酮化合物及其对于癌症的用途
UA100877C2 (ru) 2008-01-30 2013-02-11 Сефалон, Інк. Замещенные спироциклические производные пиперидина как лиганды рецепторов гистамина-3 (h3)
US8372863B2 (en) 2008-02-25 2013-02-12 Merck Sharp & Dohme Corp. Tetrahydro-1H-pyrrolo fused pyridones
WO2009111785A2 (en) 2008-03-07 2009-09-11 Solanan, Inc. Treatment of sepsis with 5-ethyl-1-phenyl-2(1h)-pyridone and novel methods for synthesis
US8349864B2 (en) 2008-03-25 2013-01-08 New Mexico Technical Research Foundation Pyrano [3,2-C] pyridones and related heterocyclic compounds as pharmaceutical agents for treating disorders responsive to apoptosis, antiproliferation or vascular disruption, and the use thereof
WO2009146034A2 (en) 2008-03-31 2009-12-03 Takeda Pharmaceutical Company Limited Mapk/erk kinase inhibitors and methods of use thereof
WO2009124119A2 (en) 2008-04-01 2009-10-08 The Trustes of Columbia University in the City of New York Phosphodiesterase inhibitors and uses thereof
WO2009124553A2 (en) 2008-04-09 2009-10-15 Neurokey A/S Use of hypothermia inducing drugs
MY152042A (en) 2008-05-05 2014-08-15 Actelion Pharmaceuticals Ltd 3,4- substituted piperidine derivatives as renin inhibitors
WO2009142732A2 (en) 2008-05-20 2009-11-26 Cephalon, Inc. Substituted pyridazinone derivatives as histamine-3 (h3) receptor ligands
CA2726588C (en) 2008-06-03 2019-04-16 Karl Kossen Compounds and methods for treating inflammatory and fibrotic disorders
MX2011000175A (es) 2008-06-25 2011-06-27 Envivo Pharmaceuticals Inc Compuestos heterociclicos 1,2-di-substituidos.
WO2009158315A1 (en) 2008-06-25 2009-12-30 Smithkline Beecham Corporation Prolyl hydroxylase inhibitors
EA201100049A1 (ru) 2008-06-27 2011-08-30 Новартис Аг Органические соединения
CA2730511C (en) 2008-07-11 2013-06-11 Robert Epple 4-phenoxymethylpiperidines as modulators of gpr119 activity
TW201006821A (en) 2008-07-16 2010-02-16 Bristol Myers Squibb Co Pyridone and pyridazone analogues as GPR119 modulators
EP2318388A2 (en) 2008-07-23 2011-05-11 Schering Corporation Tricyclic spirocycle derivatives and methods of use thereof
BRPI0917394A2 (pt) 2008-08-18 2019-09-24 Univ Yale moduladores de mif
JP2012500850A (ja) 2008-08-25 2012-01-12 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー プロリルヒドロキシラーゼ阻害剤
CA2736970A1 (en) 2008-09-12 2010-03-18 Biolipox Ab Pyrimidinone derivatives for use as medicaments
CN102256966B (zh) 2008-10-17 2016-02-10 白头生物医学研究所 可溶性mTOR复合物和其调节剂
US8703962B2 (en) 2008-10-24 2014-04-22 Purdue Pharma L.P. Monocyclic compounds and their use as TRPV1 ligands
US20110288134A1 (en) 2008-10-29 2011-11-24 Pacific Therapeutics Ltd. Composition and method for treating fibrosis
US7635707B1 (en) 2008-11-10 2009-12-22 Intermune, Inc. Pirfenidone treatment for patients with atypical liver function
US20110313004A1 (en) 2008-12-04 2011-12-22 Concert Pharmaceuticals, Inc. Deuterated pyridinones
MX2011006108A (es) 2008-12-08 2011-11-18 Vm Pharma Llc Composiciones de inhibidores de los receptores tirosina quinasa.
CA2747279A1 (en) 2008-12-10 2010-06-17 Merck Canada Inc. 3,4 - substituted piperidine derivatives as renin inhibitors
ES2641765T3 (es) 2008-12-11 2017-11-13 Shionogi & Co., Ltd. Síntesis de inhibidores de integrasa de VIH carbamoilpiridona y productos intermedios
JP2012513481A (ja) 2008-12-23 2012-06-14 プレジデント アンド フェロウズ オブ ハーバード カレッジ ネクロトーシスの小分子阻害剤
CN102405210B (zh) 2009-01-07 2015-04-22 汉高美国知识产权有限责任公司 过氧化氢配合物和它们在厌氧粘合剂的固化体系中的用途
MX2011007854A (es) 2009-01-26 2011-08-15 Univ California Metodos para tratar infartos agudos al miocardio y trastornos relacionados.
CA2750051A1 (en) * 2009-02-02 2010-08-05 Merck Sharp & Dohme Corp. Inhibitors of akt activity
HUE027478T2 (en) 2009-02-05 2016-09-28 Takeda Pharmaceuticals Co Pyridazinone Compounds
US8563583B2 (en) 2009-03-09 2013-10-22 Bristol-Myers Squibb Company Pyridone analogs useful as melanin concentrating hormone receptor-1 antagonists
EP2406233B1 (en) 2009-03-09 2013-11-13 Bristol-Myers Squibb Company Aza pyridone analogs useful as melanin concentrating hormone receptor-1 antagonists
WO2010107816A2 (en) 2009-03-16 2010-09-23 Promega Corporation Nucleic acid binding dyes and uses therefor
ES2543608T3 (es) 2009-03-27 2015-08-20 Ardea Biosciences, Inc. Dihidropiridin sulfonamidas y dihidropiridin sulfamidas como inhibidores de MEK
EP2601840B1 (en) 2009-04-20 2017-02-01 Marrone Bio Innovations, Inc. Chemical and biological agents for the control of molluscs
AU2010241742A1 (en) 2009-04-27 2011-11-17 Elan Pharmaceuticals, Inc. Pyridinone antagonists of alpha-4 integrins
JP2012131708A (ja) 2009-04-28 2012-07-12 Nissan Chem Ind Ltd ４位置換ピリダジノン化合物及びｐ２ｘ７受容体阻害剤
SG175877A1 (en) 2009-05-04 2011-12-29 Plexxikon Inc Compounds and methods for inhibition of renin, and indications therefor
WO2010132864A1 (en) 2009-05-15 2010-11-18 Intermune, Inc. Methods of treating hiv patients with anti-fibrotics
WO2010135470A1 (en) 2009-05-19 2010-11-25 Intermune, Inc. Pifenidone derivatives for treating bronchial asthma
CN102149683B (zh) 2009-05-25 2013-10-02 中南大学 1-（取代苄基）-5-三氟甲基-2-（1h）吡啶酮化合物及其盐，其制备方法及其用途
US8426407B2 (en) 2009-05-25 2013-04-23 Central South University Preparation of 1-(substituted aryl)-5-trifluoromethyl-2-(1H)pyridone compounds and salts thereof and their applications
US20100305326A1 (en) 2009-06-02 2010-12-02 Marquette University Chemical Fragment Screening and Assembly Utilizing Common Chemistry for NMR Probe Introduction and Fragment Linkage
JP2012528869A (ja) 2009-06-03 2012-11-15 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー メラニン凝集ホルモン受容体１アンタゴニストとしてのビス−ピリジルピリドン類
US20120077795A1 (en) 2009-06-03 2012-03-29 Glaxsmithkline Llc Bis-pyridylpyridones as melanin-concentrating hormone receptor 1 antagonists
TWI434833B (zh) 2009-06-03 2014-04-21 Intermune Inc 用於合成吡非尼酮（ｐｉｒｆｅｎｉｄｏｎｅ）的改良方法
EP2437599A4 (en) 2009-06-03 2012-10-31 Glaxosmithkline Llc BIS-PYRIDYLPYRIDONE AS MELANIN CONCENTRATION HORMONE RECEPTOR-1 ANTAGONISTS
US20120071459A1 (en) 2009-06-03 2012-03-22 Glaxosmithkline Llc Bis-pyridylpyridones as melanin-concentrating hormone receptor 1 antagonists
WO2011055270A1 (en) * 2009-11-04 2011-05-12 Wyeth Llc Indole based receptor crth2 antagonists
US8084475B2 (en) 2009-12-04 2011-12-27 Intermune, Inc. Pirfenidone therapy and inducers of cytochrome P450
TW201143768A (en) 2009-12-15 2011-12-16 Lundbeck & Co As H Pyridone derivatives as NK3 antagonists
US20120225896A1 (en) 2009-12-22 2012-09-06 Kowa Company, Ltd. Novel 2-pyridone derivative and pharmaceutical product containing same
JP2013523822A (ja) * 2010-04-08 2013-06-17 ブリストル−マイヤーズ スクイブ カンパニー Ｇｐｒ１１９修飾因子としてのピリミジニルピペリジニルオキシピリジノ類似体
CA2812043A1 (en) 2010-04-23 2011-10-27 Kineta, Inc. Pyrimidinedione anti-viral compounds
AU2011273931B2 (en) * 2010-06-28 2015-04-23 Merck Patent Gmbh 2,4- diaryl - substituted [1,8] naphthyridines as kinase inhibitors for use against cancer
KR20120011357A (ko) * 2010-07-23 2012-02-08 현대약품 주식회사 치환된 피리디논 유도체 및 이의 제조방법
US9212130B2 (en) * 2010-08-10 2015-12-15 Shionogi & Co., Ltd. Heterocyclic derivative and pharmaceutical composition comprising the same
EP2627648A1 (en) 2010-09-16 2013-08-21 Novartis AG 17aHYDROXYLASE/C17,20-LYASE INHIBITORS
CN102432598A (zh) * 2010-09-29 2012-05-02 江苏恒瑞医药股份有限公司 三环化合物、其制备方法及其在医药上的应用
CN102020651B (zh) 2010-11-02 2012-07-18 北京赛林泰医药技术有限公司 6-芳基氨基吡啶酮甲酰胺mek抑制剂
US8643700B2 (en) * 2010-11-17 2014-02-04 Dell Products L.P. 3D content adjustment system
EP2649050A4 (en) 2010-12-06 2014-04-23 Glaxo Group Ltd LINKS
CN102558147B (zh) * 2010-12-23 2014-09-17 江苏先声药物研究有限公司 化合物、制备方法及应用
KR101925971B1 (ko) 2011-01-28 2018-12-06 에스케이바이오팜 주식회사 피리돈 유도체 및 이를 포함하는 약학적 조성물
KR101928505B1 (ko) 2011-01-28 2018-12-12 에스케이바이오팜 주식회사 피리돈 유도체 및 이를 포함하는 약학적 조성물
AU2012212269B2 (en) 2011-01-31 2016-05-19 Avalyn Pharma Inc. Aerosol pirfenidone and pyridone analog compounds and uses thereof
US10105356B2 (en) 2011-01-31 2018-10-23 Avalyn Pharma Inc. Aerosol pirfenidone and pyridone analog compounds and uses thereof
WO2012107831A1 (en) 2011-02-11 2012-08-16 Signa S.A. De C.V. Method of making a pyridone compound, 5-ethyl-1-phenyl-2-(1h)-pyridone, and intermediates thereof
FI20115234A0 (fi) * 2011-03-08 2011-03-08 Biotie Therapies Corp Uusia pyridatsinoni- ja pyridoniyhdisteitä
CN103561741A (zh) 2011-03-08 2014-02-05 奥斯拜客斯制药有限公司 取代的n-芳基吡啶酮
KR20140022048A (ko) 2011-05-25 2014-02-21 인터뮨, 인크. 선택된 환자에서의 피르페니돈 및 항-섬유성 치료제
CN103582728A (zh) * 2011-05-27 2014-02-12 简森丹麦有限公司 一种用于进送衣物的方法和进送器
CN102816175B (zh) 2011-06-09 2015-12-16 上海汇伦生命科技有限公司 一种杂环并吡啶酮类化合物,其中间体、制备方法和用途
WO2012175514A1 (en) 2011-06-21 2012-12-27 Bayer Intellectual Property Gmbh Pyridinone derivatives and pharmaceutical compositions thereof
JP2014520776A (ja) * 2011-07-04 2014-08-25 バイエル・インテレクチユアル・プロパテイー・ゲー・エム・ベー・ハー 植物における非生物的ストレスに対する活性薬剤としての置換されているイソキノリノン類、イソキノリンジオン類、イソキノリントリオン類およびジヒドロイソキノリノン類または各場合でのそれらの塩の使用
MX2011007675A (es) 2011-07-19 2012-07-11 Cell Therapy And Technology S A De C V Procedimiento para la fabricacion de una composicion farmaceutica en forma de tabletas de liberacion prolongada conteniendo pirfenidona y su aplicacion en la regresion de la insuficiencia renal cronica, contractura capsular mamaria y fibrosis hepatica humanas.
WO2013018685A1 (ja) 2011-07-29 2013-02-07 東レ株式会社 ラクタム誘導体及びその医薬用途
CN102276616B (zh) 2011-08-04 2013-09-04 中国科学院长春应用化学研究所 一种呋喃[3,2-c]吡啶-4(5H)-酮类化合物合成方法
CN104023725B (zh) 2011-08-16 2019-04-26 卡迪欧拉有限公司 控释制剂
US20130116241A1 (en) * 2011-11-09 2013-05-09 Abbvie Inc. Novel inhibitor compounds of phosphodiesterase type 10a
JP6382108B2 (ja) * 2011-11-30 2018-08-29 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ 新規二環式ジヒドロイソキノリン−１−オン誘導体
JP6068515B2 (ja) 2012-03-01 2017-01-25 アレイ バイオファーマ、インコーポレイテッド セリン／トレオニンキナーゼ阻害剤
WO2013142390A1 (en) 2012-03-21 2013-09-26 Gtx, Inc. Aldo-keto reductase subfamily 1c3 (akr1c3) inhibitors
AU2013292950C1 (en) 2012-07-18 2016-01-21 Sunshine Lake Pharma Co., Ltd. Nitrogenous heterocyclic derivatives and their application in drugs
JP6501264B2 (ja) 2012-07-24 2019-04-17 アヴァリン ファーマ インク． エアロゾルのピルフェニドン及びピリドンのアナログの化合物、及び、その使用
US20140094456A1 (en) 2012-10-02 2014-04-03 Intermune, Inc. Anti-fibrotic pyridinones
AR092742A1 (es) 2012-10-02 2015-04-29 Intermune Inc Piridinonas antifibroticas
UA111305C2 (uk) * 2012-12-21 2016-04-11 Пфайзер Інк. Конденсовані лактами арилу та гетероарилу
JP6256187B2 (ja) 2014-05-14 2018-01-10 株式会社デンソー 判定帰還型等化器

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