CA2200468A1 - Antagonistes de muscarine - Google Patents
Antagonistes de muscarineInfo
- Publication number
- CA2200468A1 CA2200468A1 CA002200468A CA2200468A CA2200468A1 CA 2200468 A1 CA2200468 A1 CA 2200468A1 CA 002200468 A CA002200468 A CA 002200468A CA 2200468 A CA2200468 A CA 2200468A CA 2200468 A1 CA2200468 A1 CA 2200468A1
- Authority
- CA
- Canada
- Prior art keywords
- piperidin
- dihydro
- benzimidazol
- pyrimidinecarbonyl
- ethyl
- Prior art date
- Legal status (The legal status 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 status listed.)
- Abandoned
Links
Classifications
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Ophthalmology & Optometry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Composés, 1,3-dihydro-1-{1-[pipéridine-4-yl]pipéridine-4-yl}-2H-benzimidazole-2-ones et 1,3 dihydro-1-{4-amino-1-cyclohexyl}-2H-benzimidazole-2-ones et dérivés desdites substances, leur préparation, procédé d'utilisation et compositions pharmaceutiques. Lesdits composés possèdent une activité antimuscarinique et sont utiles dans le traitement et/ou la prévention de la myopie.
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US08/329,757 US5574044A (en) | 1994-10-27 | 1994-10-27 | Muscarine antagonists |
US440,153 | 1995-05-12 | ||
US08/440,153 US5691323A (en) | 1995-05-12 | 1995-05-12 | Muscarine antagonists |
US329,757 | 1995-05-12 |
Publications (1)
Publication Number | Publication Date |
---|---|
CA2200468A1 true CA2200468A1 (fr) | 1996-05-09 |
Family
ID=26986957
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CA002200468A Abandoned CA2200468A1 (fr) | 1994-10-27 | 1995-10-24 | Antagonistes de muscarine |
Country Status (5)
Country | Link |
---|---|
EP (1) | EP0786997A4 (fr) |
JP (1) | JP2002515008A (fr) |
AU (1) | AU701127B2 (fr) |
CA (1) | CA2200468A1 (fr) |
WO (1) | WO1996013262A1 (fr) |
Families Citing this family (83)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
FR2751647B1 (fr) * | 1996-07-25 | 1998-09-11 | Synthelabo | Derives de benzimidazole, leurs preparations et leurs applications en therapeutique |
DE19643331A1 (de) * | 1996-10-21 | 1998-04-23 | Thomae Gmbh Dr K | 1-(4-Piperidinyl)-piperidinylene, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung |
JP4366532B2 (ja) * | 1997-05-30 | 2009-11-18 | 萬有製薬株式会社 | 2−オキソイミダゾール誘導体 |
AU2095099A (en) * | 1997-12-23 | 1999-07-12 | Alcon Laboratories, Inc. | Phthalimide-piperidine, -pyrrolidine and -azepine derivatives, their preparationand their use as muscarinic receptor (ant-)agonists |
BR9911590A (pt) | 1998-05-26 | 2001-02-13 | Warner Lambert Co | Pirimidinas bicìclicas e 3,4-diidropirimidinas bicìclicas como inibidores da proliferação celular |
US6828460B2 (en) | 1999-03-22 | 2004-12-07 | Pfizer Inc. | Resorcinol derivatives |
ATE275141T1 (de) * | 1999-10-13 | 2004-09-15 | Banyu Pharma Co Ltd | Substituierte imidazolin-derivate |
DE19952146A1 (de) * | 1999-10-29 | 2001-06-07 | Boehringer Ingelheim Pharma | Arylalkane, Arylalkene und Aryl-azaalkane, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung |
SE9904652D0 (sv) * | 1999-12-17 | 1999-12-17 | Astra Pharma Prod | Novel Compounds |
TWI258462B (en) | 1999-12-17 | 2006-07-21 | Astrazeneca Ab | Adamantane derivative compounds, process for preparing the same and pharmaceutical composition comprising the same |
EP1598339B1 (fr) * | 2001-04-18 | 2009-06-24 | Euro-Celtique S.A. | Derivés de la 1-(4-amino-cyclohexyl)-1,3-dihydro-2h-benzimidazole-2-one et composés similaires pour l'utilisation comme analogues du nociceptin et ligandes du orl1 pour le traitement de la douleur |
WO2002085890A1 (fr) * | 2001-04-20 | 2002-10-31 | Banyu Pharmaceutical Co., Ltd. | Derives de benzimidazolone |
WO2004089942A2 (fr) * | 2001-10-02 | 2004-10-21 | Acadia Pharmaceuticals Inc. | Derives de benzimidazolidinone utilises en tant qu'agents muscariniques |
CN1561212A (zh) * | 2001-10-02 | 2005-01-05 | 阿卡蒂亚药品公司 | 作为毒蕈碱试剂的苯并咪唑啉酮衍生物 |
US6951849B2 (en) | 2001-10-02 | 2005-10-04 | Acadia Pharmaceuticals Inc. | Benzimidazolidinone derivatives as muscarinic agents |
AU2003223631B2 (en) * | 2002-04-18 | 2006-07-20 | Schering Corporation | 1-(4-Piperidinyl) benzimidazolones as histamine H3 antagonists |
US7279490B2 (en) | 2002-06-17 | 2007-10-09 | Merck & Co, Inc. | Ophthalmic compositions for treating ocular hypertension |
PA8577501A1 (es) | 2002-07-25 | 2004-02-07 | Warner Lambert Co | Inhibidores de quinasas |
JPWO2004069828A1 (ja) * | 2003-02-04 | 2006-05-25 | 三菱ウェルファーマ株式会社 | ピペリジン化合物およびその医薬用途 |
TWI396686B (zh) | 2004-05-21 | 2013-05-21 | Takeda Pharmaceutical | 環狀醯胺衍生物、以及其製品和用法 |
AR054816A1 (es) * | 2005-07-13 | 2007-07-18 | Banyu Pharma Co Ltd | Derivados de n-dihidroxialquil 2-oxo- imidazol sustituidos |
JP5209479B2 (ja) * | 2005-09-30 | 2013-06-12 | グラクソ グループ リミテッド | M1受容体にて活性を有するベンゾイミダゾロン類 |
JP5209481B2 (ja) * | 2005-09-30 | 2013-06-12 | グラクソ グループ リミテッド | M1受容体にて活性を有する化合物および医薬におけるそれらの使用 |
KR20130091791A (ko) * | 2005-09-30 | 2013-08-19 | 글락소 그룹 리미티드 | M1 수용체에서 활성을 갖는 화합물 및 그의 의약적 용도 |
GB0605784D0 (en) * | 2006-03-22 | 2006-05-03 | Glaxo Group Ltd | Compounds |
GB0605786D0 (en) * | 2006-03-22 | 2006-05-03 | Glaxo Group Ltd | Compounds |
GB0605785D0 (en) * | 2006-03-22 | 2006-05-03 | Glaxo Group Ltd | Compounds |
TW200815405A (en) * | 2006-06-09 | 2008-04-01 | Astrazeneca Ab | Novel compounds |
TW200813018A (en) | 2006-06-09 | 2008-03-16 | Astrazeneca Ab | Novel compounds |
CA2674076A1 (fr) * | 2006-12-26 | 2008-07-10 | Qlt Plug Delivery, Inc. | Implants a liberation de medicaments pour inhiber des defauts optiques |
GB0706173D0 (en) * | 2007-03-29 | 2007-05-09 | Glaxo Group Ltd | Compounds |
GB0706167D0 (en) * | 2007-03-29 | 2007-05-09 | Glaxo Group Ltd | Compounds |
GB0706189D0 (en) * | 2007-03-29 | 2007-05-09 | Glaxo Group Ltd | Compounds |
GB0706168D0 (en) * | 2007-03-29 | 2007-05-09 | Glaxo Group Ltd | Compounds |
GB0706190D0 (en) * | 2007-03-29 | 2007-05-09 | Glaxo Group Ltd | Compounds |
GB0706187D0 (en) * | 2007-03-29 | 2007-05-09 | Glaxo Group Ltd | Compounds |
GB0706165D0 (en) * | 2007-03-29 | 2007-05-09 | Glaxo Group Ltd | Compounds |
US8119661B2 (en) | 2007-09-11 | 2012-02-21 | Astrazeneca Ab | Piperidine derivatives and their use as muscarinic receptor modulators |
JP2010539218A (ja) * | 2007-09-20 | 2010-12-16 | グラクソ グループ リミテッド | M1受容体にて活性を有する化合物および医薬としてのそれらの使用 |
GB0718415D0 (en) | 2007-09-20 | 2007-10-31 | Glaxo Group Ltd | Compounds |
WO2009037294A1 (fr) * | 2007-09-20 | 2009-03-26 | Glaxo Group Limited | Composés présentant une activité au niveau du récepteur m1 et leurs utilisations en médecine |
WO2009124883A1 (fr) * | 2008-04-09 | 2009-10-15 | H. Lundbeck A/S | Nouveaux 1,3-dihydro-benzoimidazol-2-ones utilisés en tant qu’agonistes m1 |
US20090275574A1 (en) * | 2008-05-05 | 2009-11-05 | Astrazeneca Ab | Novel compounds-300 |
CN106831541B (zh) | 2011-11-18 | 2019-09-06 | 赫普泰雅治疗有限公司 | 毒蕈碱性m1受体激动剂 |
TW201348231A (zh) | 2012-02-29 | 2013-12-01 | Amgen Inc | 雜雙環化合物 |
JP6478923B2 (ja) | 2013-02-07 | 2019-03-06 | ヘプタレス セラピューティクス リミテッドHeptares Therapeutics Limited | ムスカリンm4受容体アゴニストとしてのピペリジン−1−イル及びアゼピン−1−イルカルボキシレート |
WO2014143659A1 (fr) | 2013-03-15 | 2014-09-18 | Araxes Pharma Llc | Inhibiteurs covalents irréversibles de la gtpase k-ras g12c |
US9227978B2 (en) | 2013-03-15 | 2016-01-05 | Araxes Pharma Llc | Covalent inhibitors of Kras G12C |
TWI659021B (zh) | 2013-10-10 | 2019-05-11 | 亞瑞克西斯製藥公司 | Kras g12c之抑制劑 |
WO2015138700A1 (fr) * | 2014-03-13 | 2015-09-17 | Bodor Laboratories, Inc. | Utilisation de zwitterions anticholinergiques sélectionnés |
JO3556B1 (ar) | 2014-09-18 | 2020-07-05 | Araxes Pharma Llc | علاجات مدمجة لمعالجة السرطان |
EP3197870B1 (fr) | 2014-09-25 | 2020-08-19 | Araxes Pharma LLC | Inhibiteurs de protéines mutantes kras g12c |
WO2016164675A1 (fr) | 2015-04-10 | 2016-10-13 | Araxes Pharma Llc | Composés quinazoline substitués et leurs procédés d'utilisation |
US10428064B2 (en) | 2015-04-15 | 2019-10-01 | Araxes Pharma Llc | Fused-tricyclic inhibitors of KRAS and methods of use thereof |
US10144724B2 (en) | 2015-07-22 | 2018-12-04 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use thereof |
GB201513743D0 (en) | 2015-08-03 | 2015-09-16 | Heptares Therapeutics Ltd | Muscarinic agonists |
WO2017058728A1 (fr) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibiteurs de protéines kras portant la mutation g12c |
WO2017058902A1 (fr) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibiteurs de protéines mutantes kras g12c |
EP3356359B1 (fr) | 2015-09-28 | 2021-10-20 | Araxes Pharma LLC | Inhibiteurs de protéines kras portant la mutation g12c |
US10647703B2 (en) | 2015-09-28 | 2020-05-12 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
US10975071B2 (en) | 2015-09-28 | 2021-04-13 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
WO2017058805A1 (fr) * | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibiteurs de protéines kras portant la mutation g12c |
US10875842B2 (en) | 2015-09-28 | 2020-12-29 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
JP7015059B2 (ja) | 2015-11-16 | 2022-02-15 | アラクセス ファーマ エルエルシー | 置換複素環式基を含む2-置換キナゾリン化合物およびその使用方法 |
US9988357B2 (en) | 2015-12-09 | 2018-06-05 | Araxes Pharma Llc | Methods for preparation of quinazoline derivatives |
US10646488B2 (en) | 2016-07-13 | 2020-05-12 | Araxes Pharma Llc | Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof |
WO2018064510A1 (fr) | 2016-09-29 | 2018-04-05 | Araxes Pharma Llc | Inhibiteurs de protéines mutantes kras g12c |
CN110312711A (zh) | 2016-10-07 | 2019-10-08 | 亚瑞克西斯制药公司 | 作为ras抑制剂的杂环化合物及其使用方法 |
GB201617454D0 (en) * | 2016-10-14 | 2016-11-30 | Heptares Therapeutics Limited | Pharmaceutical compounds |
US10259787B2 (en) | 2016-10-14 | 2019-04-16 | Heptares Therapeutics Limited | Substituted cyclohexanes as muscarinic M1 receptor and/or M4 receptor agonists |
US11274093B2 (en) | 2017-01-26 | 2022-03-15 | Araxes Pharma Llc | Fused bicyclic benzoheteroaromatic compounds and methods of use thereof |
EP3573971A1 (fr) | 2017-01-26 | 2019-12-04 | Araxes Pharma LLC | Dérivés de 1-(3-(6-(3-hydroxynaphtalen-1-yl)benzofuran-2-yl)azétidin-1yl)prop-2-en-1-one et composés similaires utilisés en tant que modulateurs de kras g12c pour le traitement du cancer |
EP3573967A1 (fr) | 2017-01-26 | 2019-12-04 | Araxes Pharma LLC | Composés hétéro-hétéro-bicycliques fusionnés et leurs procédés d'utilisation |
EP3573970A1 (fr) | 2017-01-26 | 2019-12-04 | Araxes Pharma LLC | Dérivés de 1-(6-(3-hydroxynaphtalen-1-yl)quinazolin-2-yl)azétidin-1-yl)prop-2-en-1-one et composés similaires utilisés en tant qu'inhibiteurs de kras g12c pour le traitement du cancer |
US11358959B2 (en) | 2017-01-26 | 2022-06-14 | Araxes Pharma Llc | Benzothiophene and benzothiazole compounds and methods of use thereof |
TW201838629A (zh) * | 2017-03-23 | 2018-11-01 | 新加坡商新加坡保健集團私人有限公司 | 用於預防近視、治療近視及/或預防近視增長之包含蕪地銨作爲活性成分的藥劑 |
CN110505876A (zh) * | 2017-03-23 | 2019-11-26 | 新加坡保健服务集团 | 包含噻托铵作为活性成分的用于预防近视、治疗近视、及/或预防近视进展的药剂 |
WO2018218069A1 (fr) | 2017-05-25 | 2018-11-29 | Araxes Pharma Llc | Dérivés de quinazoline utilisés en tant que modulateurs de kras, hras ou nras mutants |
EP3630746A1 (fr) | 2017-05-25 | 2020-04-08 | Araxes Pharma LLC | Composés et leurs procédés d'utilisation pour le traitement du cancer |
JP2020521742A (ja) | 2017-05-25 | 2020-07-27 | アラクセス ファーマ エルエルシー | Krasの共有結合性阻害剤 |
GB201810239D0 (en) | 2018-06-22 | 2018-08-08 | Heptares Therapeutics Ltd | Pharmaceutical compounds |
GB201819960D0 (en) | 2018-12-07 | 2019-01-23 | Heptares Therapeutics Ltd | Pharmaceutical compounds |
GB202020191D0 (en) | 2020-12-18 | 2021-02-03 | Heptares Therapeutics Ltd | Pharmaceutical compounds |
Family Cites Families (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4066772A (en) * | 1975-07-21 | 1978-01-03 | Janssen Pharmaceutica N.V. | 1,3-Dihydro-1-[3-(1-piperidinyl)propyl]-2H-benzimidazol-2-ones and related compounds |
US4329353A (en) * | 1980-10-22 | 1982-05-11 | Janssen Pharmaceutica, N.V. | 1-(4-Aryl-cyclohexyl)piperidine derivatives, method of use thereof and pharmaceutical compositions thereof |
CA1336490C (fr) * | 1988-06-03 | 1995-08-01 | Paul Michael Iuvone | Traitement pharmacologique de la croissance anormale de l'oeil |
US5128327A (en) * | 1991-03-25 | 1992-07-07 | Merck & Co., Inc. | Angiotensin II antagonists incorporating a nitrogen containing six membered ring heterocycle |
US5322847A (en) * | 1992-11-05 | 1994-06-21 | Pfizer Inc. | Azabenzimidazoles in the treatment of asthma, arthritis and related diseases |
-
1995
- 1995-10-24 JP JP51469196A patent/JP2002515008A/ja active Pending
- 1995-10-24 WO PCT/US1995/013710 patent/WO1996013262A1/fr not_active Application Discontinuation
- 1995-10-24 EP EP95937615A patent/EP0786997A4/fr not_active Withdrawn
- 1995-10-24 CA CA002200468A patent/CA2200468A1/fr not_active Abandoned
- 1995-10-24 AU AU39674/95A patent/AU701127B2/en not_active Ceased
Also Published As
Publication number | Publication date |
---|---|
WO1996013262A1 (fr) | 1996-05-09 |
EP0786997A1 (fr) | 1997-08-06 |
AU3967495A (en) | 1996-05-23 |
AU701127B2 (en) | 1999-01-21 |
EP0786997A4 (fr) | 1998-03-11 |
JP2002515008A (ja) | 2002-05-21 |
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Legal Events
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EEER | Examination request | ||
FZDE | Dead |