IL232291A0 - Quinoline carboxamide and quinoline carbonitrile derivatives as negative allosteric modulators of mglur2, their compositions and use - Google Patents

Quinoline carboxamide and quinoline carbonitrile derivatives as negative allosteric modulators of mglur2, their compositions and use

Info

Publication number
IL232291A0
IL232291A0 IL232291A IL23229114A IL232291A0 IL 232291 A0 IL232291 A0 IL 232291A0 IL 232291 A IL232291 A IL 232291A IL 23229114 A IL23229114 A IL 23229114A IL 232291 A0 IL232291 A0 IL 232291A0
Authority
IL
Israel
Prior art keywords
quinoline
mglur2
compositions
allosteric modulators
negative allosteric
Prior art date
Application number
IL232291A
Other languages
English (en)
Hebrew (he)
Original Assignee
Merck Sharp & Dohme
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Merck Sharp & Dohme filed Critical Merck Sharp & Dohme
Publication of IL232291A0 publication Critical patent/IL232291A0/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—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
    • A61K31/47—Quinolines; Isoquinolines
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—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
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • 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
    • C07D401/04—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
    • 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
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • General Chemical & Material Sciences (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Anesthesiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Quinoline Compounds (AREA)
IL232291A 2011-11-03 2014-04-28 Quinoline carboxamide and quinoline carbonitrile derivatives as negative allosteric modulators of mglur2, their compositions and use IL232291A0 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161555227P 2011-11-03 2011-11-03
US201261672334P 2012-07-17 2012-07-17
PCT/US2012/062027 WO2013066736A1 (en) 2011-11-03 2012-10-26 QUINOLINE CARBOXAMIDE AND QUINOLINE CARBONITRILE DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE

Publications (1)

Publication Number Publication Date
IL232291A0 true IL232291A0 (en) 2014-06-30

Family

ID=48192643

Family Applications (1)

Application Number Title Priority Date Filing Date
IL232291A IL232291A0 (en) 2011-11-03 2014-04-28 Quinoline carboxamide and quinoline carbonitrile derivatives as negative allosteric modulators of mglur2, their compositions and use

Country Status (16)

Country Link
US (3) US9278960B2 (enExample)
EP (1) EP2775841B1 (enExample)
JP (2) JP5857136B2 (enExample)
KR (1) KR20140088887A (enExample)
CN (1) CN104010504B (enExample)
AR (1) AR088611A1 (enExample)
AU (2) AU2012332895B2 (enExample)
CA (1) CA2853923A1 (enExample)
CO (1) CO6950474A2 (enExample)
IL (1) IL232291A0 (enExample)
IN (1) IN2014CN03234A (enExample)
MX (1) MX344308B (enExample)
MY (1) MY167423A (enExample)
RU (1) RU2610262C2 (enExample)
TW (1) TWI605040B (enExample)
WO (1) WO2013066736A1 (enExample)

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20140088887A (ko) * 2011-11-03 2014-07-11 머크 샤프 앤드 돔 코포레이션 mGluR2-음성 알로스테릭 조절제로서의 퀴놀린 카르복스아미드 및 퀴놀린 카르보니트릴 유도체, 조성물, 및 그의 용도
JO3368B1 (ar) 2013-06-04 2019-03-13 Janssen Pharmaceutica Nv مركبات 6، 7- ثاني هيدرو بيرازولو [5،1-a] بيرازين- 4 (5 يد)- اون واستخدامها بصفة منظمات تفارغية سلبية لمستقبلات ميجلور 2
NZ724691A (en) 2014-03-24 2018-02-23 Guangdong Zhongsheng Pharmaceutical Co Ltd Quinoline derivatives as smo inhibitors
JOP20150177B1 (ar) 2014-08-01 2021-08-17 Janssen Pharmaceutica Nv مركبات 6 ، 7 ثاني هيدرو بيرازولو [ 1، 5 الفا ] بيرازين – 4 (5 يد) – اون واستخدامها كمنظمات الوسترية سلبية لمستقبلات ملجور 2
RU2696135C2 (ru) 2014-08-01 2019-07-31 Янссен Фармацевтика Нв 6,7-ДИГИДРОПИРАЗОЛО[1,5-α]ПИРАЗИН-4(5Н)-ОНОВЫЕ СОЕДИНЕНИЯ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ОТРИЦАТЕЛЬНЫХ АЛЛОСТЕРИЧЕСКИХ МОДУЛЯТОРОВ РЕЦЕПТОРОВ MGLUR2
JOP20150179B1 (ar) 2014-08-01 2021-08-17 Janssen Pharmaceutica Nv مركبات 6 ، 7 ثاني هيدرو بيرازولو [ 1، 5 الفا ] بيرازين – 4 (5 يد) – اون واستخدامها كمنظمات الوسترية سلبية لمستقبلات ملجور 2
JP6517340B2 (ja) 2014-08-01 2019-05-22 ヤンセン ファーマシューティカ エヌ．ベー． ６，７−ジヒドロピラゾロ［１，５−ａ］ピラジン−４（５Ｈ）−オン化合物およびＭＧＬＵＲ２受容体の負のアロステリック調節因子としてのそれらの使用
JO3601B1 (ar) 2014-08-01 2020-07-05 Janssen Pharmaceutica Nv مركبات 6 ، 7 ثاني هيدرو بيرازولو [ 1، 5 الفا ] بيرازين – 4 (5 يد) – اون واستخدامها كمنظمات الوسترية سلبية لمستقبلات ملجور 2
WO2016029454A1 (en) * 2014-08-29 2016-03-03 Merck Sharp & Dohme Corp. TETRAHYDRONAPHTHYRIDINE DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE
EP3000814A1 (en) 2014-09-26 2016-03-30 Domain Therapeutics Substituted pyrazoloquinazolinones and pyrroloquinazolinones as allosteric modulators of group II metabotropic glutamate receptors
JP6861154B2 (ja) 2014-12-03 2021-04-21 ヤンセン ファーマシューティカ エヌ．ベー． 放射標識されたｍＧｌｕＲ２ ＰＥＴリガンド
CN107001375B (zh) * 2014-12-03 2020-06-09 詹森药业有限公司 6,7-二氢吡唑并[1,5-a]吡嗪-4(5H)-酮化合物及其作为MGLUR2受体的负向别构调节剂的用途
WO2016149324A1 (en) * 2015-03-16 2016-09-22 Vanderbilt University Negative allosteric modulators of metabotropic glutamate receptor 2
CR20180109A (es) * 2015-07-20 2018-05-03 Genzyme Corp Inhibidores de receptor del factor estimulador de colonias 1 (csf-1r)
JP6916175B2 (ja) 2015-10-26 2021-08-11 バイエル・クロップサイエンス・アクチェンゲゼルシャフト 有害生物防除剤としての縮合二環式ヘテロ環誘導体
US11045562B2 (en) 2015-12-18 2021-06-29 Janssen Pharmaceutica Nv Radiolabelled mGluR2/3 PET ligands
HUE050665T2 (hu) 2015-12-18 2020-12-28 Janssen Pharmaceutica Nv Radiojelzett MGLUR2/3 PET ligandumok
MD3519416T2 (ro) * 2016-09-27 2021-09-30 Merck Sharp & Dohme Derivați croman, izocroman și dihidroizobenzofuran ca modulatori alosterici negativi ai mGluR2, compoziții și utilizarea lor
MY201041A (en) 2017-11-24 2024-01-31 Sumitomo Pharma Co Ltd Substituted pyrazolo[1,5-a]pyrazines as negative allosteric modulators of group ii metabotropic glutamate receptor
CN108689957B (zh) * 2018-07-23 2020-07-03 南京药石科技股份有限公司 一种2r/2s-三氟甲基吗啉及其盐酸盐的制备方法和应用
AU2019375983A1 (en) * 2018-11-09 2021-06-10 Vivace Therapeutics, Inc. Bicyclic compounds
HUE070525T2 (hu) 2019-04-16 2025-06-28 Vivace Therapeutics Inc Biciklusos vegyületek
EP3976027B1 (en) * 2019-05-30 2025-11-05 Merck Sharp & Dohme LLC Quinoline derivatives as factor xi activation inhibitors
JP7618597B2 (ja) 2019-07-01 2025-01-21 ユーシービー バイオファルマ エスアールエル Ｄ１ポジティブアロステリックモジュレーターとしての置換されたテトラヒドロイソキノリン誘導体
CN110256342B (zh) * 2019-07-16 2022-06-07 河南省科学院化学研究所有限公司 一种2-氰基喹啉衍生物的合成方法
EP4267573A1 (en) 2020-12-23 2023-11-01 Genzyme Corporation Deuterated colony stimulating factor-1 receptor (csf-1r) inhibitors
WO2024112853A1 (en) * 2022-11-24 2024-05-30 Exelixis, Inc. Compounds that inhibit pkmyt1
TW202519226A (zh) * 2023-11-08 2025-05-16 美商艾克塞里克斯公司 使用抑制ｐｋｍｙｔ１之化合物治療癌症之方法

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0551831A1 (de) * 1992-01-15 1993-07-21 Hoechst Schering AgrEvo GmbH Verfahren zur Herstellung substituierter 2-Cyanopyridine
US5552437A (en) 1994-10-27 1996-09-03 Merck Frosst Canada, Inc. Bisarylcarbinol derivatives as inhibitors of leukotriene biosynthesis
US5576338A (en) * 1995-02-15 1996-11-19 Merck Frosst Canada, Inc. Bis (biaryl) compounds as inhibitors of leukotriene biosynthesis
GB9524137D0 (en) 1995-11-24 1996-01-24 Smithkline Beecham Spa Novel compounds
JPH115772A (ja) * 1997-04-25 1999-01-12 Takeda Chem Ind Ltd アミド誘導体、その製造法および用途
EP0975621A1 (en) * 1997-04-25 2000-02-02 Takeda Chemical Industries, Ltd. Cell differentiation inducing amide derivatives, their production and use
DK1224175T3 (da) * 1999-10-15 2004-07-12 Hoffmann La Roche Benzodiazepinderivater som metabotropiske glutamatreceptorantagonister
TWI328009B (en) * 2003-05-21 2010-08-01 Glaxo Group Ltd Quinoline derivatives as phosphodiesterase inhibitors
CA2532036A1 (en) * 2003-07-11 2005-02-03 Merck & Co., Inc. Methods for identifying cell surface receptor protein modulators
US7692017B2 (en) 2003-09-23 2010-04-06 Merck Sharp & Dohme Corp. Quinoline potassium channel inhibitors
JP2008518913A (ja) * 2004-10-28 2008-06-05 メルク エンド カムパニー インコーポレーテッド 代謝調節型グルタミン酸受容体のピリミジン及びキノリン増強因子
AU2006299671A1 (en) * 2005-10-05 2007-04-12 Merck Frosst Canada Ltd Substituted quinolines as inhibitors of leukotriene biosynthesis
AR065093A1 (es) * 2007-02-05 2009-05-13 Merck Frosst Canada Ltd Compuestos farmacéuticos inhibidores de la biosintesis de leucotrienos
WO2008155588A1 (en) * 2007-06-18 2008-12-24 Richter Gedeon Nyrt. Sulfonyl-quinoline derivatives
WO2011153553A2 (en) 2010-06-04 2011-12-08 The Regents Of The University Of California Methods and compositions for kinase inhibition
CN102603628B (zh) 2010-12-22 2016-08-17 香港理工大学 作为抗癌试剂的喹啉衍生物
KR20140088887A (ko) * 2011-11-03 2014-07-11 머크 샤프 앤드 돔 코포레이션 mGluR2-음성 알로스테릭 조절제로서의 퀴놀린 카르복스아미드 및 퀴놀린 카르보니트릴 유도체, 조성물, 및 그의 용도

Also Published As

Publication number Publication date
US20140309227A1 (en) 2014-10-16
NZ624596A (en) 2016-10-28
EP2775841B1 (en) 2017-09-13
MY167423A (en) 2018-08-27
RU2610262C2 (ru) 2017-02-08
AU2012332895A1 (en) 2014-05-15
AU2016200998B2 (en) 2017-04-06
TW201321357A (zh) 2013-06-01
JP5857136B2 (ja) 2016-02-10
US20160158217A1 (en) 2016-06-09
MX344308B (es) 2016-12-13
CA2853923A1 (en) 2013-05-10
CN104010504B (zh) 2016-04-06
EP2775841A4 (en) 2015-05-06
RU2014122335A (ru) 2015-12-10
MX2014005415A (es) 2014-07-11
AU2016200998A1 (en) 2016-03-03
US9278960B2 (en) 2016-03-08
JP2016094447A (ja) 2016-05-26
KR20140088887A (ko) 2014-07-11
US9636337B2 (en) 2017-05-02
CN104010504A (zh) 2014-08-27
EP2775841A1 (en) 2014-09-17
US20160159744A1 (en) 2016-06-09
IN2014CN03234A (enExample) 2015-07-03
JP2015501783A (ja) 2015-01-19
US9663506B2 (en) 2017-05-30
AU2012332895B2 (en) 2015-12-17
AR088611A1 (es) 2014-06-25
TWI605040B (zh) 2017-11-11
CO6950474A2 (es) 2014-05-20
JP6114809B2 (ja) 2017-04-12
WO2013066736A1 (en) 2013-05-10

Similar Documents

Publication Publication Date Title
IL232291A0 (en) Quinoline carboxamide and quinoline carbonitrile derivatives as negative allosteric modulators of mglur2, their compositions and use
SMT201700340T1 (it) Modulatori di enzimi modificanti metile, composizioni e loro utilizzo
IL238958B (en) Glutaminase inhibitors, preparations containing them and their uses
ZA201401117B (en) Kynurenine-3-monooxygenase inhibitors,pharmaceutical compositions,and methods of use thereof
IL253911A0 (en) Inhibitors of kynurenine-3-monooxygenase, pharmaceutical compositions, and methods of their use
IL238959A0 (en) Glutamase inhibitors, preparations containing them and their uses
PT2665486T (pt) Composições para modular a atividade das citocinas gama-c
IL234884A0 (en) Inhibitors of kynurenine-3-monooxygenase pharmaceutical compositions, and methods of their use
IL230705A0 (en) Certain inhibitors of kynurenine-3-monooxygenase pharmaceutical compositions, and methods of their use
IL238825A0 (en) The history of heterocyclics, their preparation and pharmaceutical preparations containing them
IL230763A (en) Amide pyrazole is conserved by heterocyclic and their pharmaceutical preparations
IL256646B (en) History of azaquinazoline carboxamides and pharmaceutical preparations containing them
IL231444A (en) Aniline derivatives, their preparation and their medical application
IL233602A0 (en) History of benzamide, their preparation and pharmaceutical preparations containing them
ZA201308268B (en) Herbicidal composition comprising pinoxaden and fluroxypyrester, and methods of use thereof
ZA201306905B (en) Novel octahydrothienoquinonline derivative,pharmaceutical composition comprising derivative, and use of these
IL228705A (en) Derivatives of Reliable Phenoxy-Ethyl, Pharmaceutical Preparations Containing and Using Them
IL233199B (en) History of heterocyclic carboxamides, their preparation and pharmaceutical preparations containing them
IL233682A0 (en) Modified phenylazole derivatives, preparations containing them and their uses
ZA201504323B (en) 3-aminocyclopentane carboxamide derivatives
ZA201105042B (en) Benzothiophene carboxamide compounds, composition and applications thereof
ZA201500952B (en) Indole carboxamide derivatives and uses thereof
AU2012901658A0 (en) Compositions and methods of use