EA200400615A1 - Производные амидов в качестве ингибиторов гликогенсинтаза-киназы 3-бета - Google Patents

Производные амидов в качестве ингибиторов гликогенсинтаза-киназы 3-бета

Info

Publication number
EA200400615A1
EA200400615A1 EA200400615A EA200400615A EA200400615A1 EA 200400615 A1 EA200400615 A1 EA 200400615A1 EA 200400615 A EA200400615 A EA 200400615A EA 200400615 A EA200400615 A EA 200400615A EA 200400615 A1 EA200400615 A1 EA 200400615A1
Authority
EA
Eurasian Patent Office
Prior art keywords
hydrogen
alkyl
optionally substituted
6alkyloxy
nrr
Prior art date
Application number
EA200400615A
Other languages
English (en)
Other versions
EA007578B1 (ru
Inventor
Эдди Жан Эдгар Фрейн
Петер Якобус Йоханнес Антониус Бейнстерс
Марк Виллемс
Вернер Констант Йохан Эмбрехтс
Жан Фернан Арман Лакрамп
Поль Адриан Ян Жанссен
Паулус Йоаннес Леви
Ян Херес
Марк Рене Де Жонж
Люсьен Мария Хенрикус Койманс
Фредерик Франс Дезире Дайер
Майкл Джозеф Кукла
Юго Альфонс Габриель Гертс
Рони Мария Нюйденс
Марк Юбер Меркен
Дональд Вилльям Лудовики
Original Assignee
Янссен Фармацевтика Н.В.
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 Янссен Фармацевтика Н.В. filed Critical Янссен Фармацевтика Н.В.
Publication of EA200400615A1 publication Critical patent/EA200400615A1/ru
Publication of EA007578B1 publication Critical patent/EA007578B1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/24—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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C07D213/82—Amides; Imides in position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Hematology (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Rheumatology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

Данное изобретение относится к соединению формулы (I'), его N-оксиду, фармацевтически приемлемой аддитивной соли, четвертичному амину и стереохимически изомерной форме, где кольцо A является 6-членным гетероциклом; Rозначает водород; арил; формил; Cалкилкарбонил; необязательно замещенный Cалкил; Cалкилоксикарбонил; необязательно замещенный Cалкилокси-Cалкилкарбонил; X означает прямую связь или линкерный атом или линкерную группу; Z означает O или S; Rозначает водород, Cалкил, Cалкенил, Cалкинил, карбоцикл или гетероцикл, причем каждая из указанных групп может быть необязательно замещена; Rозначает водород; гидрокси; галоген; необязательно замещенный Cалкил или Cалкенил или Cалкинил; Cалкилокси; Cалкилтио; Cалкилоксикарбонил; Cалкилкарбонилокси; карбоксил; циано; нитро; амино; моно- или ди(Cалкил)амино; полигалоген-Cалкил; полигалоген-Cалкилокси; полигалоген-Cалкилтио; R; R-Cалкил; R-O-; R-S-; R-C(=O)-; R-S(=O)-; R-S(=O)-; R-S(=O)-NH-; R-S(=O)-NH-; R-C(=O)-; -NHC(=O)H; -C(=O)NHNH; R-C(=O)-NH-; R-C(=O)-NH-; -C(=NH)R; -C(=NH)R; Rили R, каждый независимо, означает водород, R, -Y-NR-Y-NRR, -Y-NR-Y-R, -Y-NRR; при условии, что -X-Rи/или Rявляется другим, чем водород; их применению, содержащим их фармацевтическим композициям и способам их получения.Международная заявка была опубликована вместе с отчетом о международном поиске.
EA200400615A 2001-11-01 2002-10-29 Производные амидов в качестве ингибиторов гликогенсинтаза-киназы 3-бета EA007578B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP01204193 2001-11-01
PCT/EP2002/012067 WO2003037869A1 (en) 2001-11-01 2002-10-29 Amide derivatives as glycogen synthase kinase 3-beta inhibitors

Publications (2)

Publication Number Publication Date
EA200400615A1 true EA200400615A1 (ru) 2004-08-26
EA007578B1 EA007578B1 (ru) 2006-12-29

Family

ID=8181176

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200400615A EA007578B1 (ru) 2001-11-01 2002-10-29 Производные амидов в качестве ингибиторов гликогенсинтаза-киназы 3-бета

Country Status (21)

Country Link
US (1) US7183288B2 (ru)
EP (1) EP1442019B8 (ru)
JP (1) JP2005507419A (ru)
KR (1) KR20050040814A (ru)
CN (1) CN1582277A (ru)
AT (1) ATE375331T1 (ru)
AU (1) AU2002363174B2 (ru)
BR (1) BR0213791A (ru)
CA (1) CA2463821A1 (ru)
DE (1) DE60222921T2 (ru)
DK (1) DK1442019T3 (ru)
EA (1) EA007578B1 (ru)
ES (1) ES2294190T3 (ru)
HU (1) HUP0402330A3 (ru)
IL (1) IL161661A0 (ru)
MX (1) MXPA04004177A (ru)
NO (1) NO327097B1 (ru)
NZ (1) NZ531855A (ru)
PL (1) PL368917A1 (ru)
PT (1) PT1442019E (ru)
WO (1) WO2003037869A1 (ru)

Families Citing this family (61)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4206382B2 (ja) 2002-11-19 2009-01-07 アキリオン ファーマシューティカルズ，インコーポレーテッド 置換されたアリールチオウレアおよび関連化合物；ウイルス複製のインヒビター
US7423147B2 (en) 2004-03-31 2008-09-09 Janssen Pharmaceutical, N.V. Pyridine compounds as histamine H3 modulators
EP1734963A4 (en) 2004-04-02 2008-06-18 Merck & Co Inc METHOD FOR TREATING PEOPLE WITH METABOLIC AND ANTHROPOMETRIC DISORDER
WO2006000589A1 (en) 2004-06-28 2006-01-05 Altana Pharma Ag 4,6-disubstituted pyrimidines and their use as protein kinase inhibitors
JP2009506069A (ja) 2005-08-26 2009-02-12 ブレインセルス，インコーポレイティド ムスカリン性受容体調節による神経発生
EP2258359A3 (en) 2005-08-26 2011-04-06 Braincells, Inc. Neurogenesis by muscarinic receptor modulation with sabcomelin
AU2006304787A1 (en) 2005-10-21 2007-04-26 Braincells, Inc. Modulation of neurogenesis by PDE inhibition
CA2625210A1 (en) 2005-10-31 2007-05-10 Braincells, Inc. Gaba receptor mediated modulation of neurogenesis
JP2009520811A (ja) * 2005-12-22 2009-05-28 クリスタルジェノミクス、インコーポレイテッド プロテインキナーゼ活性を阻害するアミノピリミジン誘導体、及びその製造方法並びにこれを有効成分として含む医薬組成物
US20100216734A1 (en) 2006-03-08 2010-08-26 Braincells, Inc. Modulation of neurogenesis by nootropic agents
US7678808B2 (en) 2006-05-09 2010-03-16 Braincells, Inc. 5 HT receptor mediated neurogenesis
AU2007249399A1 (en) 2006-05-09 2007-11-22 Braincells, Inc. Neurogenesis by modulating angiotensin
CA2653940C (en) 2006-05-30 2015-07-14 Janssen Pharmaceutica N.V. Substituted pyridyl amide compounds as modulators of the histamine h3 receptor
CA2647598A1 (en) * 2006-05-31 2007-12-06 Abbott Laboratories Compounds as cannabinoid receptor ligands and uses thereof
US8841334B2 (en) * 2006-05-31 2014-09-23 Abbvie Inc. Compounds as cannabinoid receptor ligands and uses thereof
EP2068872A1 (en) 2006-09-08 2009-06-17 Braincells, Inc. Combinations containing a 4-acylaminopyridine derivative
US20100184806A1 (en) 2006-09-19 2010-07-22 Braincells, Inc. Modulation of neurogenesis by ppar agents
CN101765594A (zh) 2007-03-28 2010-06-30 雅培制药有限公司 作为大麻素受体配体的1,3-噻唑-2(3h)-亚基化合物
US7872033B2 (en) * 2007-04-17 2011-01-18 Abbott Laboratories Compounds as cannabinoid receptor ligands
US8735434B2 (en) * 2007-05-18 2014-05-27 Abbvie Inc. Compounds as cannabinoid receptor ligands
US8969514B2 (en) 2007-06-04 2015-03-03 Synergy Pharmaceuticals, Inc. Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases
US9193713B2 (en) * 2007-10-12 2015-11-24 Abbvie Inc. Compounds as cannabinoid receptor ligands
CA2706328C (en) 2007-11-20 2016-04-19 Janssen Pharmaceutica N.V. Cycloalkyloxy- and heterocycloalkyloxypyridine compounds as modulators of the histamine h3 receptor
FR2931108B1 (fr) * 2008-05-15 2011-01-07 Peugeot Citroen Automobiles Sa Limiteur de vitesse a indicateur de vitesse limite a deplacement manuel, pour vehicule automobile
WO2010009319A2 (en) 2008-07-16 2010-01-21 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal, inflammation, cancer and other disorders
US8846730B2 (en) * 2008-09-08 2014-09-30 Abbvie Inc. Compounds as cannabinoid receptor ligands
US8188135B2 (en) * 2008-09-16 2012-05-29 Abbott Laboratories Compounds as cannabinoid receptor ligands
CA2741125A1 (en) 2008-10-22 2010-04-29 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
CN102271509A (zh) 2008-10-31 2011-12-07 默沙东公司 用于抗糖尿病药的新型环苯并咪唑衍生物
PA8854001A1 (es) * 2008-12-16 2010-07-27 Abbott Lab Compuestos novedosos como ligandos de receptores de canabinoides
WO2010099217A1 (en) 2009-02-25 2010-09-02 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
CA2787756C (en) 2010-01-22 2019-06-18 Acetylon Pharmaceuticals, Inc. Reverse amide compounds as protein deacetylase inhibitors and methods of use thereof
US8895596B2 (en) 2010-02-25 2014-11-25 Merck Sharp & Dohme Corp Cyclic benzimidazole derivatives useful as anti-diabetic agents
US20130156720A1 (en) 2010-08-27 2013-06-20 Ironwood Pharmaceuticals, Inc. Compositions and methods for treating or preventing metabolic syndrome and related diseases and disorders
US9616097B2 (en) 2010-09-15 2017-04-11 Synergy Pharmaceuticals, Inc. Formulations of guanylate cyclase C agonists and methods of use
WO2012060847A1 (en) 2010-11-07 2012-05-10 Targegen, Inc. Compositions and methods for treating myelofibrosis
PT2640709T (pt) 2010-11-16 2016-07-13 Acetylon Pharmaceuticals Inc Compostos de pirimidina hidroxiamida como inibidores de proteína desacetilase e métodos de utilização dos mesmos
EP2677869B1 (en) 2011-02-25 2017-11-08 Merck Sharp & Dohme Corp. Novel cyclic azabenzimidazole derivatives useful as anti-diabetic agents
CA2880901A1 (en) 2012-08-02 2014-02-06 Merck Sharp & Dohme Corp. Antidiabetic tricyclic compounds
CN103804362A (zh) * 2012-11-12 2014-05-21 韩文毅 一类治疗糖尿病的化合物及其用途
WO2014130608A1 (en) 2013-02-22 2014-08-28 Merck Sharp & Dohme Corp. Antidiabetic bicyclic compounds
EP2970119B1 (en) 2013-03-14 2021-11-03 Merck Sharp & Dohme Corp. Novel indole derivatives useful as anti-diabetic agents
JP6606491B2 (ja) 2013-06-05 2019-11-13 シナジー ファーマシューティカルズ インコーポレイテッド グアニル酸シクラーゼｃの超高純度アゴニスト、その作成および使用方法
EP3054952B1 (en) 2013-10-08 2022-10-26 Acetylon Pharmaceuticals, Inc. Combinations of histone deacetylase 6 inhibitors and the her2 inhibitor lapatinib for use in the treatment of breast cancer
WO2015051496A1 (en) 2013-10-08 2015-04-16 Merck Sharp & Dohme Corp. Antidiabetic tricyclic compounds
US9278963B2 (en) 2013-10-10 2016-03-08 Acetylon Pharmaceuticals, Inc. Pyrimidine hydroxy amide compounds as histone deacetylase inhibitors
EP3060217B1 (en) 2013-10-24 2022-06-08 Mayo Foundation for Medical Education and Research Treatment of polycystic diseases with an hdac6 inhibitor
CA2932411A1 (en) 2013-12-03 2015-06-11 Acetylon Pharmaceuticals, Inc. Combinations of histone deacetylase inhibitors and immunomodulatory drugs
US9464073B2 (en) 2014-02-26 2016-10-11 Acetylon Pharmaceuticals, Inc. Pyrimidine hydroxy amide compounds as HDAC6 selective inhibitors
EP3166603B1 (en) 2014-07-07 2020-02-12 Acetylon Pharmaceuticals, Inc. Treatment of leukemia with histone deacetylase inhibitors
CA2969790A1 (en) 2014-12-05 2016-06-09 University of Modena and Reggio Emilia Combinations of histone deacetylase inhibitors and bendamustine
US10272084B2 (en) 2015-06-01 2019-04-30 Regenacy Pharmaceuticals, Llc Histone deacetylase 6 selective inhibitors for the treatment of cisplatin-induced peripheral neuropathy
JP6873053B2 (ja) 2015-06-08 2021-05-19 アセチロン ファーマシューティカルズ インコーポレイテッドＡｃｅｔｙｌｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ，Ｉｎｃ． タンパク質脱アセチル化阻害剤の製造方法
JP6816036B2 (ja) 2015-06-08 2021-01-20 アセチロン ファーマシューティカルズ インコーポレイテッドＡｃｅｔｙｌｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ，Ｉｎｃ． ヒストン脱アセチル化阻害剤の結晶形態
JP2019515909A (ja) 2016-04-19 2019-06-13 アセチロン ファーマシューティカルズ インコーポレイテッドＡｃｅｔｙｌｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ，Ｉｎｃ． 慢性リンパ性白血病の治療を目的とするｈｄａｃ阻害剤単独またはｂｔｋ阻害剤との配合物
ES2929032T3 (es) 2016-08-08 2022-11-24 Acetylon Pharmaceuticals Inc Combinaciones farmacéuticas de inhibidores de histona desacetilasa 6 y anticuerpos inhibidores de CD20 y usos de los mismos
EP3551176A4 (en) 2016-12-06 2020-06-24 Merck Sharp & Dohme Corp. ANTIDIABETIC HETEROCYCLIC COMPOUNDS
WO2018118670A1 (en) 2016-12-20 2018-06-28 Merck Sharp & Dohme Corp. Antidiabetic spirochroman compounds
AU2020218366A1 (en) 2019-02-08 2021-09-16 Frequency Therapeutics, Inc. Valproic acid compounds and Wnt agonists for treating ear disorders
CN110128305A (zh) * 2019-05-10 2019-08-16 天津大学 二甲双胍-甲苯磺丁脲新盐型、其制备方法及医药用途
CN116813497B (zh) * 2023-08-31 2023-11-14 天津匠新致成科技有限公司 一种酰胺类化合物及其制备方法、药物组合物和应用

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1198551A (en) * 1968-01-22 1970-07-15 Union Pharma Scient Appl New Nicotinuric Acid Derivatives
DE2334266A1 (de) * 1972-07-07 1974-01-31 Hisamitsu Pharmaceutical Co Pyrido eckige klammer auf 2,3-d eckige klammer zu pyrimidin-2,4 (1h, 3h)-dione
JPS5069096A (ru) * 1973-10-25 1975-06-09
US5264437A (en) * 1992-03-20 1993-11-23 Syntex (U.S.A.) Inc. Optionally substituted pyrido[2,3-d]pyridine-2,4(1H,3H)-diones and pyrido[2,]pyrimidine-2(1H,3H)-ones
GB9523675D0 (en) * 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
NO311614B1 (no) 1996-10-01 2001-12-17 Janssen Pharmaceutica Nv Substituerte diamino-1,3,5-triazinderivater
US6022884A (en) * 1997-11-07 2000-02-08 Amgen Inc. Substituted pyridine compounds and methods of use
AU1507199A (en) * 1997-12-15 1999-07-05 Yamanouchi Pharmaceutical Co., Ltd. Novel pyrimidine-5-carboxamide derivatives
KR100699514B1 (ko) 1998-03-27 2007-03-26 얀센 파마슈티카 엔.브이. Ｈｉｖ를 억제하는 피리미딘 유도체
JP4533534B2 (ja) * 1998-06-19 2010-09-01 ノバルティス バクシンズ アンド ダイアグノスティックス，インコーポレーテッド グリコーゲンシンターゼキナーゼ３のインヒビター
KR100658489B1 (ko) 1998-11-10 2006-12-18 얀센 파마슈티카 엔.브이. Ｈｉｖ 복제를 억제하는 피리미딘
PT1169038E (pt) 1999-04-15 2012-10-26 Bristol Myers Squibb Co Inibidores cíclicos da proteína tirosina cinase

Also Published As

Publication number Publication date
EP1442019B8 (en) 2013-10-30
EP1442019B1 (en) 2007-10-10
ATE375331T1 (de) 2007-10-15
MXPA04004177A (es) 2004-09-06
CA2463821A1 (en) 2003-05-08
IL161661A0 (en) 2004-09-27
WO2003037869A1 (en) 2003-05-08
NO327097B1 (no) 2009-04-20
HUP0402330A3 (en) 2010-03-29
PT1442019E (pt) 2007-12-11
DE60222921D1 (de) 2007-11-22
EA007578B1 (ru) 2006-12-29
EP1442019A1 (en) 2004-08-04
DE60222921T2 (de) 2008-08-07
NO20041891L (no) 2004-05-07
CN1582277A (zh) 2005-02-16
PL368917A1 (en) 2005-04-04
HUP0402330A2 (hu) 2005-02-28
BR0213791A (pt) 2004-12-07
JP2005507419A (ja) 2005-03-17
ES2294190T3 (es) 2008-04-01
AU2002363174B2 (en) 2008-09-25
US7183288B2 (en) 2007-02-27
NZ531855A (en) 2005-12-23
KR20050040814A (ko) 2005-05-03
DK1442019T3 (da) 2008-01-14
US20050176713A1 (en) 2005-08-11

Similar Documents

Publication Publication Date Title
EA200400615A1 (ru) Производные амидов в качестве ингибиторов гликогенсинтаза-киназы 3-бета
EA200400616A1 (ru) ПРОИЗВОДНЫЕ АМИНОБЕНЗАМИДОВ В КАЧЕСТВЕ ИНГИБИТОРОВ ГЛИКОГЕНСИНТАЗА-КИНАЗЫ 3β
EA200400617A1 (ru) Гетероариламины в качестве ингибиторов гликогенсинтаза-киназы 3-бета (ингибиторов gsk3)
PE20011166A1 (es) Piridinas, pirimidinas, purinonas, pirrolopirimidinonas y pirrolopiridinonas como antagonistas del factor liberador de corticotropina
HUP0201646A2 (hu) Új alfa-aminosav vegyületek, eljárás ezek előállítására, és ezeket tartalmazó gyógyászati készítmények
BRPI0211909B8 (pt) compostos derivados de pirimidina que inibem o hiv, processos para as suas preparações e respectiva composição farmacêutica
AR035695A1 (es) Compuestos inhibidores de metaloproteinasa, composicion farmaceutica, metodo de tratamiento, y uso de estos compuestos para la preparacion de medicamentos
AR054214A1 (es) Compuestos derivados de 1, 1 - dioxotiadiazina, composiciones farmaceuticas que los contienen y su uso en el tratamiento de la infeccion por el virus de la hepatitis c.
CY1110979T1 (el) Παραγωγα κιναζολινης ως αναστολεις αγγειογενεσης και ενδιαμεσες ενωσεις αυτων
PE20040155A1 (es) Derivados aminoinazoles, procedimiento de preparacion e intermedios de este procedimiento a titulo de medicamentos y composiciones farmaceuticas que los contienen
CY1106522T1 (el) Ετepοκυκλικη ενωση και αντικαρκινικο μεσο που πepιεχει την ιδια ως δραστικο συστατικο
EA200602060A1 (ru) Производные пирролидин-2-она и пиперидин-2-она, используемые в качестве ингибиторов 11-бета-гидроксистероид-дегидрогеназы
AR065927A1 (es) Derivados de 5,6-dihidro-1h-piridin-2-ona
AR053784A1 (es) Compuestos y derivados tetrazolicos de dibencil amina. composiciones farmaceuticas.
UY29312A1 (es) Piperazin-1-carboxamidas n,4,sustituidas y sus derivados, composiciones que los contienen, procedimientos de preparación y aplicaciones
ATE135701T1 (de) Imidazolderivate, starke und selektive angiotensin-ii-rezeptor-antagonisten
EA200000400A1 (ru) Галогензамещенные тетрациклические производные тетрагидрофурана
ATE307812T1 (de) Imidazopyridinverbindungen als 5-ht4- rezeptormodulatoren
DE60214401D1 (de) Hetero-bicyclische crf antagonisten
HUP0401588A2 (hu) Rákellenes és proliferáció elleni hatású indeno[1,2-c]pirazol-4-on-származékok és ezeket tartalmazó gyógyszerkészítmények
EA200400896A1 (ru) Терапевтические акридоновые и акридиновые соединения
MA33103B1 (fr) Derives de 6-(6-substitue-triazolopyridazine-sulfanyl) 5-fluoro-benzothiazoles et 5-fluoro-benzimidazoles : preparation, application comme medicaments et utilisation comme inhibiteurs de met
AR021137A1 (es) Derivados de triazina 2,4-disustituida, uso de los mismos para preparar medicamentos, composiciones farmacéuticas que los comprenden, procedimiento para prepararlas, y procedimiento para preparar dichos derivados.
ES2183500T3 (es) Nuevos compuestos y composiciones farmaceuticas que los contienen.
EA200100677A1 (ru) Производные 6-азаурацила, ингибирующие il-5

Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): RU