JP2009521483A - ムスカリン受容体のモジュレーター - Google Patents

ムスカリン受容体のモジュレーター Download PDF

Info

Publication number
JP2009521483A
JP2009521483A JP2008547641A JP2008547641A JP2009521483A JP 2009521483 A JP2009521483 A JP 2009521483A JP 2008547641 A JP2008547641 A JP 2008547641A JP 2008547641 A JP2008547641 A JP 2008547641A JP 2009521483 A JP2009521483 A JP 2009521483A
Authority
JP
Japan
Prior art keywords
compound
optionally
group
optionally substituted
alkyl
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.)
Pending
Application number
JP2008547641A
Other languages
English (en)
Japanese (ja)
Other versions
JP2009521483A5 (https=
Inventor
ルイス・アール・メイキングズ
ミゲル・ガルシア−グスマン・ブランコ
デニス・ジェイ・ハーリー
イオアナ・ドルトゥ
ガブリエル・ラファイ
ダニエル・エム・バージェロン
彰子 中谷
アンドレアス・ペー・テルミン
アリーナ・シリナ
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Vertex Pharmaceuticals Inc
Original Assignee
Vertex Pharmaceuticals 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
Application filed by Vertex Pharmaceuticals Inc filed Critical Vertex Pharmaceuticals Inc
Publication of JP2009521483A publication Critical patent/JP2009521483A/ja
Publication of JP2009521483A5 publication Critical patent/JP2009521483A5/ja
Pending legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/438The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/468-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/498Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/501Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D221/00Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/20Spiro-condensed ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/10Spiro-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Emergency Medicine (AREA)
  • Immunology (AREA)
  • Psychology (AREA)
  • Psychiatry (AREA)
  • Pulmonology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Child & Adolescent Psychology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Dermatology (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2008547641A 2005-12-22 2006-12-22 ムスカリン受容体のモジュレーター Pending JP2009521483A (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US75318705P 2005-12-22 2005-12-22
PCT/US2006/049141 WO2007076070A2 (en) 2005-12-22 2006-12-22 Modulators of muscarinic receptors

Publications (2)

Publication Number Publication Date
JP2009521483A true JP2009521483A (ja) 2009-06-04
JP2009521483A5 JP2009521483A5 (https=) 2010-02-18

Family

ID=38138812

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2008547641A Pending JP2009521483A (ja) 2005-12-22 2006-12-22 ムスカリン受容体のモジュレーター

Country Status (12)

Country Link
US (1) US7858635B2 (https=)
EP (1) EP1973543A2 (https=)
JP (1) JP2009521483A (https=)
KR (1) KR20080087841A (https=)
CN (1) CN101374519A (https=)
AU (1) AU2006330866A1 (https=)
CA (1) CA2634456A1 (https=)
IL (1) IL192327A0 (https=)
NO (1) NO20083011L (https=)
RU (1) RU2008130094A (https=)
WO (1) WO2007076070A2 (https=)
ZA (1) ZA200806028B (https=)

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2009527569A (ja) * 2006-02-22 2009-07-30 バーテックス ファーマシューティカルズ インコーポレイテッド ムスカリン受容体の調節剤
JP2013535412A (ja) * 2010-07-09 2013-09-12 アブビー・ベー・ブイ S1pモジュレーターとしてのスピロ環状アミン誘導体
JP2017507997A (ja) * 2014-03-19 2017-03-23 ヘプタレス セラピューティクス リミテッドHeptares Therapeutics Limited ムスカリン受容体アゴニスト
JP2018021057A (ja) * 2012-09-18 2018-02-08 ヘプタレス セラピューティックス リミテッド ムスカリンm1受容体作動薬としての二環式アザ化合物
JP2018508562A (ja) * 2015-03-19 2018-03-29 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m1受容体及び/またはm4受容体のアゴニストとしてのスピロ環状化合物
JP2023509345A (ja) * 2019-12-23 2023-03-08 クリネティックス ファーマシューティカルズ,インク. スピロ環式ピペリジンメラノコルチンサブタイプ-2受容体(mc2r)アンタゴニストおよびその使用

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2290731A1 (en) * 1999-11-26 2001-05-26 D. Jed Harrison Apparatus and method for trapping bead based reagents within microfluidic analysis system
JP2003294742A (ja) 2002-03-29 2003-10-15 Inst Of Physical & Chemical Res ハイブリダイゼーション用基板及びその使用方法
US7786141B2 (en) * 2004-08-19 2010-08-31 Vertex Pharmaceuticals Incorporated Dihydrospiroindene modulators of muscarinic receptors
WO2008121066A1 (en) * 2007-03-30 2008-10-09 Astrazeneca Ab Novel tricyclic spiropiperidines or spiropyrrolidines and their use as modulators of chemokine receptors
TW201322983A (zh) * 2007-08-31 2013-06-16 Purdue Pharma Lp 經取代之喹□啉型哌啶化合物及其用途
HRP20120968T1 (hr) * 2008-02-06 2013-01-31 Astrazeneca Ab Spojevi
CA2794153C (en) 2010-03-25 2018-01-02 Glaxosmithkline Llc Substituted indoline derivatives as perk inhibitors
AU2012338581B2 (en) 2011-11-18 2016-12-08 Nxera Pharma Uk Limited Muscarinic M1 receptor agonists
GB2519470A (en) * 2013-09-18 2015-04-22 Heptares Therapeutics Ltd Bicyclic aza compounds as muscarinic M1 receptor agonists
KR102352388B1 (ko) 2014-02-06 2022-01-17 헵테얼즈 테라퓨틱스 리미티드 무스카린성 m1 수용체 및/또는 m4 수용체 작용제로서 바이사이클릭 아자 화합물
US10118890B2 (en) 2014-10-10 2018-11-06 The Research Foundation For The State University Of New York Trifluoromethoxylation of arenes via intramolecular trifluoromethoxy group migration
US9745253B2 (en) 2015-03-13 2017-08-29 Forma Therapeutics, Inc. Alpha-cinnamide compounds and compositions as HDAC8 inhibitors
GB201513743D0 (en) 2015-08-03 2015-09-16 Heptares Therapeutics Ltd Muscarinic agonists
AR105911A1 (es) 2015-09-03 2017-11-22 Forma Therapeutics Inc Inhibidores de hdac8 bicíclicos fusionados [6,6]
GB201519352D0 (en) 2015-11-02 2015-12-16 Heptares Therapeutics Ltd Pharmaceutical compounds
WO2017107089A1 (en) 2015-12-23 2017-06-29 Merck Sharp & Dohme Corp. 3- (1h-pyrazol-4-yl) pyridineallosteric modulators of the m4 muscarinic acetylcholine receptor
US10329289B2 (en) 2015-12-23 2019-06-25 Merck Sharp & Dohme Corp. 6,7-dihydro-5H-pyrrolo[3,4-B]pyridin-5-one allosteric modulators of the M4 muscarinic acetylcholine receptor
GB201617454D0 (en) 2016-10-14 2016-11-30 Heptares Therapeutics Limited Pharmaceutical compounds
WO2018112842A1 (en) 2016-12-22 2018-06-28 Merck Sharp & Dohme Corp. 6,6-fused heteroaryl piperidine ether allosteric modulators of m4 muscarinic acetylcholine receptor
WO2018112843A1 (en) 2016-12-22 2018-06-28 Merck Sharp & Dohme Corp. Heteroaryl piperidine ether allosteric modulators of the m4 muscarinic acetylcholine receptor
WO2018112840A1 (en) 2016-12-22 2018-06-28 Merck Sharp & Dohme Corp. 6, 5-fused heteroaryl piperidine ether allosteric modulators of the m4 muscarinic acetylcholine receptor
WO2019000236A1 (en) 2017-06-27 2019-01-03 Merck Sharp & Dohme Corp. ALLOSTERIC MODULATORS OF 3- (1H-PYRAZOL-4-YL) PYRIDINE FROM THE M4 ACETYLCHOLINE MUSCARINIC RECEPTOR
WO2019000238A1 (en) 2017-06-27 2019-01-03 Merck Sharp & Dohme Corp. 5- (PYRIDIN-3-YL) OXAZOLE ALLOSTERIC MODULATORS OF M4 ACETYLCHOLINE MUSCARINIC RECEPTOR
WO2019000237A1 (en) 2017-06-27 2019-01-03 Merck Sharp & Dohme Corp. ALLOSTERIC MODULATORS OF 3- (1H-PYRAZOL-4-YL) PYRIDINE FROM THE M4 ACETYLCHOLINE MUSCARINIC RECEPTOR
GB201810239D0 (en) 2018-06-22 2018-08-08 Heptares Therapeutics Ltd Pharmaceutical compounds
GB201810245D0 (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
GB201819961D0 (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
EP4077307B1 (en) 2019-12-18 2025-03-12 Crinetics Pharmaceuticals, Inc. Gem-disubstituted piperidine melanocortin subtype-2 receptor (mc2r) antagonists and uses thereof
AU2021275233A1 (en) * 2020-05-22 2022-12-08 Vanderbilt University Competitive and noncompetitive inhibitors of the muscarinic acetylcholine receptor M5
WO2022032073A2 (en) * 2020-08-07 2022-02-10 Casma Therapeutics, Inc. Trpml modulators

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999032489A1 (en) * 1997-12-23 1999-07-01 Alcon Laboratories, Inc. Muscarinic agents and use thereof to treat glaucoma, myopia and various other conditions
WO2000051608A1 (en) * 1999-03-02 2000-09-08 Merck & Co., Inc. 3-thienyl and 3-furanyl pyrrolidine modulators of chemokine receptor activity
JP2001526178A (ja) * 1997-08-28 2001-12-18 メルク エンド カムパニー インコーポレーテッド ピロリジン系およびピペリジン系ケモカイン受容体活性調節剤
WO2003014083A1 (en) * 2001-08-07 2003-02-20 Banyu Pharmaceutical Co., Ltd. Spiro compounds
WO2004004714A1 (en) * 2002-07-03 2004-01-15 H. Lundbeck A/S Spirocyclic piperidines as mch1 antagonists and uses thereof
WO2004089307A2 (en) * 2003-04-04 2004-10-21 Merck & Co. Inc. Acylated spiropiperidine derivatives as melanocortin-4 receptor agonists
WO2006023852A2 (en) * 2004-08-19 2006-03-02 Vertex Pharmaceuticals, Incorporated Modulators of muscarinic receptors

Family Cites Families (79)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3666764A (en) * 1970-08-26 1972-05-30 Mead Johnson & Co Spiroindenylpiperidines
US3654287A (en) * 1970-08-26 1972-04-04 Mead Johnson & Co Spiroindanylpiperidines
DK145949C (da) 1973-09-28 1983-09-26 Ciba Geigy Ag Analogifremgangsmaade til fremstilling af i 3-stillingen substituerede rifamycin s-forbindelser eller sv-forbindelser eller syreadditionssalte eller kvaternaere ammoniumsalte deraf
US3962259A (en) * 1973-12-12 1976-06-08 American Hoechst Corporation 1,3-Dihydrospiro[isobenzofuran]s and derivatives thereof
US3959475A (en) * 1973-12-12 1976-05-25 American Hoechst Corporation Substituted 1,3-dihydrospiro(isobenzofuran)s
JPS54109983A (en) * 1978-02-13 1979-08-29 Sumitomo Chem Co Ltd Novel spiroamine derivative and its preparation
GB1575800A (en) 1978-05-16 1980-10-01 Sumitomo Chemical Co Spiro amines their production and compositions containing them
US4349549A (en) 1981-05-18 1982-09-14 Syntex (U.S.A.) Inc. Anti-hypertensive 1-substituted spiro(piperidine-oxobenzoxazine)s
JPS5815979A (ja) 1981-07-11 1983-01-29 Kyowa Hakko Kogyo Co Ltd 新規なピペリジン誘導体およびその製造法
JPS5959685A (ja) 1982-09-28 1984-04-05 Kyowa Hakko Kogyo Co Ltd 新規なピペリジン誘導体
US4558049A (en) * 1982-11-24 1985-12-10 Farmitalia Carlo Erba S.P.A. Antipsycotic benzoxazines
GB2131021B (en) 1982-11-24 1985-12-18 Erba Farmitalia Antipsychotic benzoxazines
SE445649B (sv) 1983-06-08 1986-07-07 Jorgen Hermansson Anvendning av en fast berare med immobiliserad orosomucoid for separation, forfarande for framstellning av separationsmaterial, separationsanordning samt separationsmaterial
GB8917069D0 (en) 1989-07-26 1989-09-13 Merck Sharp & Dohme Therapeutic agents
US5091387A (en) * 1990-03-02 1992-02-25 Merck & Co., Inc. Spirocyclic oxytocin antagonists
EP0444945A3 (en) 1990-03-02 1992-05-13 Merck & Co. Inc. Use of spirocyclic compounds as oxytocin antagonists
EP0445974A3 (en) * 1990-03-05 1992-04-29 Merck Sharp & Dohme Ltd. Spirocyclic antipsychotic agents
IL99957A0 (en) 1990-11-13 1992-08-18 Merck & Co Inc Piperidinylcamphorsulfonyl oxytocin antagonists and pharmaceutical compositions containing them
NZ243065A (en) 1991-06-13 1995-07-26 Lundbeck & Co As H Piperidine derivatives and pharmaceutical compositions
DE69223573D1 (de) 1991-09-16 1998-01-29 Merck & Co Inc Hydantoin und Succinimid-substituierte Spiroindanylcamphorsulfonyl als Oxytocin-Antagonisten
DK78692D0 (da) * 1992-06-12 1992-06-12 Lundbeck & Co As H Dimere piperidin- og piperazinderivater
NZ258412A (en) 1992-12-11 1997-01-29 Merck & Co Inc Spiro-fused piperidine derivatives and pharmaceutical compositions
US5536716A (en) 1992-12-11 1996-07-16 Merck & Co., Inc. Spiro piperidines and homologs which promote release of growth hormone
WO1994022846A1 (en) 1993-03-30 1994-10-13 Pfizer Inc. Compounds enhancing antitumor activity of other cytotoxic agents
US5817679A (en) * 1993-04-01 1998-10-06 University Of Virginia 7-Azabicyclo 2.2.1!-heptane and -heptene derivatives as cholinergic receptor ligands
US5457207A (en) 1993-10-05 1995-10-10 Regents Of The University Of Minnesota Spirovesamicols
HUT75224A (en) 1993-10-19 1997-04-28 Merck & Co Inc Combination of bisphosphonates and growth hormone secretagogues
AU687953B2 (en) 1993-11-16 1998-03-05 Merck & Co., Inc. Piperidinylcamphorsulfonyl oxytocin antagonists
AU2223495A (en) 1994-04-15 1995-11-10 Yamanouchi Pharmaceutical Co., Ltd. Spiro compound and medicinal composition thereof
US5789402A (en) * 1995-01-17 1998-08-04 Eli Lilly Company Compounds having effects on serotonin-related systems
US5627196A (en) * 1995-01-17 1997-05-06 Eli Lilly And Company Compounds having effects on serotonin-related systems
US5614523A (en) * 1995-01-17 1997-03-25 Eli Lilly And Company Compounds having effects on serotonin-related systems
US5576321A (en) * 1995-01-17 1996-11-19 Eli Lilly And Company Compounds having effects on serotonin-related systems
US5741789A (en) * 1995-01-17 1998-04-21 Eli Lilly And Company Compounds having effects on serotonin-related systems
US6130217A (en) * 1995-09-20 2000-10-10 Pfizer Inc Compounds enhancing antitumor activity of other cytotoxic agents
GB2308064A (en) 1995-10-31 1997-06-18 Merck & Co Inc Treatment of congestive heart failure with a growth hormone secretagogue
GB9601724D0 (en) * 1996-01-29 1996-03-27 Merck Sharp & Dohme Therapeutic agents
AU711884B2 (en) 1996-05-07 1999-10-21 Merck & Co., Inc. Enhancement of sleep with a growth hormone secretagogue
WO1997041878A1 (en) 1996-05-07 1997-11-13 Merck & Co., Inc. Treatment of mood disorders with a growth hormone secretagogue
BR9812118A (pt) 1997-07-31 2000-07-18 Elan Pharm Inc Compostos do tipo 4-amino-fenilalanina que inibem adesão de leucócito mediada por vla-4
US6013652A (en) * 1997-12-04 2000-01-11 Merck & Co., Inc. Spiro-substituted azacycles as neurokinin antagonists
GB9810886D0 (en) * 1998-05-13 1998-07-22 Lilly Industries Ltd Pharmaceutical compounds
AU742425B2 (en) 1998-06-11 2002-01-03 Merck & Co., Inc. Spiropiperidine derivatives as melanocortin receptor agonists
ID29137A (id) 1998-07-27 2001-08-02 Schering Corp Ligan-ligan afinitas tinggi untuk reseptor nosiseptin orl-1
BR9912406A (pt) 1998-07-28 2001-04-24 Smithkline Beecham Corp Compostos de anilida substituida e métodos
CA2338804A1 (en) 1998-07-28 2000-02-10 Smithkline Beecham Corporation Propenamides as ccr5 modulators
EP1142587A1 (en) 1998-12-24 2001-10-10 Meiji Seika Kaisha Ltd. Remedies for pain
ITMI991452A1 (it) 1999-07-01 2001-01-01 Mediolanum Farmaceutici Srl Antagonisti selettivi per i recettori m2 con struttura 5h-dibenzo b,fazepinica
US6803372B2 (en) * 1999-08-20 2004-10-12 Banyu Pharmaceutical Co., Ltd. Spiro compounds
TWI279402B (en) * 1999-08-20 2007-04-21 Banyu Pharma Co Ltd Spiro compounds having NPY antagonistic activities and agents containing the same
GB2355264A (en) 1999-09-30 2001-04-18 Merck & Co Inc Spirohydantoin derivatives useful as alpha 1a adrenoceptor antagonists
WO2001022919A2 (en) 1999-09-30 2001-04-05 Merck & Co., Inc. Spiro[bicyclic -azacycloalkyl and -cycloalkyl] derivatives and uses thereof
GB2355456A (en) * 1999-09-30 2001-04-25 Merck & Co Inc Novel arylhydantoin derivatives useful as alpha 1a adrenoceptor antagonists
AU7952800A (en) 1999-10-22 2001-04-30 Sankyo Company Limited 2-alkoxybenzene derivatives
JP2001278886A (ja) 2000-03-28 2001-10-10 Dai Ichi Seiyaku Co Ltd ベンゾオキサジン誘導体及びこれを含有する医薬
US6720324B2 (en) * 2000-07-05 2004-04-13 Synaptic Pharmaceutical Corporation Selective melanin concentrating hormone-1 (MCH1) receptor antagonists and uses thereof
BR0116113A (pt) * 2000-12-12 2004-08-03 Neurogen Corp Espiro[isobenzofuran-1,4'-piperidin]-3-onas e 3h-espiroisoben-zofuran-1,4'-piperidinas
PT1385514E (pt) * 2001-04-18 2009-02-04 Euro Celtique Sa Compostos espiroindeno e espiroindano
JP2002316987A (ja) 2001-04-20 2002-10-31 Sankyo Co Ltd 2−アルコキシベンゼン誘導体を含有する医薬
AU2002363236A1 (en) * 2001-10-30 2003-05-12 Millennium Pharmaceuticals, Inc. Compounds, pharmaceutical compositions and methods of use therefor
WO2003064425A1 (en) * 2002-01-28 2003-08-07 Pfizer Japan Inc. N-substituted spiropiperidine compounds as ligands for orl-1 receptor
US7220862B2 (en) * 2002-06-05 2007-05-22 Bristol-Myers Squibb Company Calcitonin gene related peptide receptor antagonists
GB0213715D0 (en) * 2002-06-14 2002-07-24 Syngenta Ltd Chemical compounds
US7105526B2 (en) * 2002-06-28 2006-09-12 Banyu Pharmaceuticals Co., Ltd. Benzimidazole derivatives
KR101025633B1 (ko) * 2002-09-19 2011-03-30 일라이 릴리 앤드 캄파니 오피오이드 수용체 안타고니스트로서의 디아릴 에테르
US7045527B2 (en) * 2002-09-24 2006-05-16 Amgen Inc. Piperidine derivatives
DE60328035D1 (de) * 2002-11-29 2009-07-30 Banyu Pharma Co Ltd Neue azolderivate
US7247628B2 (en) * 2002-12-12 2007-07-24 Pfizer, Inc. Cannabinoid receptor ligands and uses thereof
WO2004082682A1 (en) * 2003-03-18 2004-09-30 Merck & Co. Inc. Amino cyclobutylamide modulators of chemokine receptor activity
CN1297557C (zh) 2003-04-10 2007-01-31 上海药明康德新药开发有限公司 螺环类模板化合物的制备
WO2005016913A1 (en) * 2003-08-19 2005-02-24 Pfizer Japan, Inc. Tetrahydroisoquinoline or isochroman compounds as orl-1 receptor ligands for the treatment of pain and cns disorders
US20070254903A1 (en) * 2003-12-23 2007-11-01 Arena Pharmaceuticals, Inc. Novel Spiroindoline or Spiroisoquinoline Compounds, Methods of Use and Compositions Thereof
KR100863854B1 (ko) * 2004-02-10 2008-10-15 에프. 호프만-라 로슈 아게 케모카인 ccr5 수용체 조절제
TW200533398A (en) * 2004-03-29 2005-10-16 Bristol Myers Squibb Co Novel therapeutic agents for the treatment of migraine
CA2561801A1 (en) * 2004-04-02 2005-10-20 Elixir Pharmaceuticals, Inc. Sulfonamides and uses thereof
US7279471B2 (en) * 2004-04-15 2007-10-09 Boehringer Ingelheim International Gmbh Selected CGRP-antagonists, process for preparing them and their use as pharmaceutical compositions
AU2005249494A1 (en) * 2004-05-28 2005-12-15 Vertex Pharmaceuticals Incorporated Modulators of muscarinic receptors
US7786141B2 (en) * 2004-08-19 2010-08-31 Vertex Pharmaceuticals Incorporated Dihydrospiroindene modulators of muscarinic receptors
US7351706B2 (en) * 2006-01-05 2008-04-01 Hoffmann-La Roche Inc. Indol-3-yl-carbonyl-spiro-piperidine derivatives

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2001526178A (ja) * 1997-08-28 2001-12-18 メルク エンド カムパニー インコーポレーテッド ピロリジン系およびピペリジン系ケモカイン受容体活性調節剤
WO1999032489A1 (en) * 1997-12-23 1999-07-01 Alcon Laboratories, Inc. Muscarinic agents and use thereof to treat glaucoma, myopia and various other conditions
WO2000051608A1 (en) * 1999-03-02 2000-09-08 Merck & Co., Inc. 3-thienyl and 3-furanyl pyrrolidine modulators of chemokine receptor activity
WO2003014083A1 (en) * 2001-08-07 2003-02-20 Banyu Pharmaceutical Co., Ltd. Spiro compounds
WO2004004714A1 (en) * 2002-07-03 2004-01-15 H. Lundbeck A/S Spirocyclic piperidines as mch1 antagonists and uses thereof
WO2004089307A2 (en) * 2003-04-04 2004-10-21 Merck & Co. Inc. Acylated spiropiperidine derivatives as melanocortin-4 receptor agonists
WO2006023852A2 (en) * 2004-08-19 2006-03-02 Vertex Pharmaceuticals, Incorporated Modulators of muscarinic receptors

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
JPN6012042032; Bioorg. Med. Chem. Lett. 11, 2001, 3099-3102 *

Cited By (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2009527569A (ja) * 2006-02-22 2009-07-30 バーテックス ファーマシューティカルズ インコーポレイテッド ムスカリン受容体の調節剤
JP2013535412A (ja) * 2010-07-09 2013-09-12 アブビー・ベー・ブイ S1pモジュレーターとしてのスピロ環状アミン誘導体
JP2018021057A (ja) * 2012-09-18 2018-02-08 ヘプタレス セラピューティックス リミテッド ムスカリンm1受容体作動薬としての二環式アザ化合物
JP2017507997A (ja) * 2014-03-19 2017-03-23 ヘプタレス セラピューティクス リミテッドHeptares Therapeutics Limited ムスカリン受容体アゴニスト
JP2019112443A (ja) * 2014-03-19 2019-07-11 ヘプタレス セラピューティクス リミテッドHeptares Therapeutics Limited ムスカリン受容体アゴニスト
JP2020079291A (ja) * 2014-03-19 2020-05-28 ヘプタレス セラピューティクス リミテッドHeptares Therapeutics Limited ムスカリン受容体アゴニスト
JP2018508562A (ja) * 2015-03-19 2018-03-29 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m1受容体及び/またはm4受容体のアゴニストとしてのスピロ環状化合物
JP2023509345A (ja) * 2019-12-23 2023-03-08 クリネティックス ファーマシューティカルズ,インク. スピロ環式ピペリジンメラノコルチンサブタイプ-2受容体(mc2r)アンタゴニストおよびその使用
JP7651574B2 (ja) 2019-12-23 2025-03-26 クリネティックス ファーマシューティカルズ,インク. スピロ環式ピペリジンメラノコルチンサブタイプ-2受容体(mc2r)アンタゴニストおよびその使用
JP2025100541A (ja) * 2019-12-23 2025-07-03 クリネティックス ファーマシューティカルズ,インク. スピロ環式ピペリジンメラノコルチンサブタイプ-2受容体(mc2r)アンタゴニストおよびその使用

Also Published As

Publication number Publication date
ZA200806028B (en) 2009-04-29
KR20080087841A (ko) 2008-10-01
IL192327A0 (en) 2009-08-03
CN101374519A (zh) 2009-02-25
CA2634456A1 (en) 2007-07-05
US20080015179A1 (en) 2008-01-17
RU2008130094A (ru) 2010-01-27
WO2007076070A3 (en) 2007-10-25
WO2007076070A2 (en) 2007-07-05
EP1973543A2 (en) 2008-10-01
US7858635B2 (en) 2010-12-28
AU2006330866A1 (en) 2007-07-05
NO20083011L (no) 2008-09-19

Similar Documents

Publication Publication Date Title
US7858635B2 (en) Spiro compounds as modulators of muscarinic receptors
US8258148B2 (en) Spiroindoline modulators of muscarinic receptors
US20100311746A1 (en) Modulators of muscarinic receptors
JP2009527569A (ja) ムスカリン受容体の調節剤
JP2008521821A (ja) ムスカリン受容体のモジュレーター
TW202214233A (zh) 可做為tlr9抑制劑之經取代雜芳基化合物
EP1817036B1 (en) Modulators of muscarinic receptors
JP2009542670A (ja) ムスカリン受容体の調節剤
HK1129306A (en) Modulators of muscarinic receptors
HK1119558A (en) Modulators of muscarinic receptors
CN101479266A (zh) 作为毒蕈碱受体调节剂的螺稠合哌啶

Legal Events

Date Code Title Description
A524 Written submission of copy of amendment under article 19 pct

Free format text: JAPANESE INTERMEDIATE CODE: A524

Effective date: 20091222

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20091222

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20120814

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20130212