ES2575154T3 - Moduladores alostéricos positivos del receptor M1 de quinolina amida - Google Patents

Moduladores alostéricos positivos del receptor M1 de quinolina amida Download PDF

Info

Publication number
ES2575154T3
ES2575154T3 ES10841821.1T ES10841821T ES2575154T3 ES 2575154 T3 ES2575154 T3 ES 2575154T3 ES 10841821 T ES10841821 T ES 10841821T ES 2575154 T3 ES2575154 T3 ES 2575154T3
Authority
ES
Spain
Prior art keywords
alkyl
group
halogen
ring
ring atoms
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.)
Active
Application number
ES10841821.1T
Other languages
English (en)
Inventor
Scott D. Kuduk
Kelly-Ann Schlegel
Zhi-Qiang Yang
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.)
Merck Sharp and Dohme LLC
Original Assignee
Merck Sharp and Dohme LLC
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 and Dohme LLC filed Critical Merck Sharp and Dohme LLC
Application granted granted Critical
Publication of ES2575154T3 publication Critical patent/ES2575154T3/es
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/58—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems with hetero atoms directly attached to the ring nitrogen atom
    • C07D215/60—N-oxides
    • 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
    • A61K31/4704—2-Quinolinones, e.g. carbostyril
    • 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
    • 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
    • A61P25/28—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
    • 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
    • C07D401/02—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
    • C07D401/10—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 aromatic rings
    • 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
    • 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
    • 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
    • C07D405/14—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 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
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • 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
    • C07D413/10—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 aromatic rings
    • 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
    • C07D417/10—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 aromatic 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
    • C07D417/14—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

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)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Anesthesiology (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Quinoline Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Un compuesto de formula (I):**Fórmula** en la que X1 se selecciona entre el grupo que consiste en (1) N, y (2) NO; X2-X3 se seleccionan entre el grupo que consiste en (1) -CH2-CH2-, (2) -O-CH2-, (3) -CH2-O-, o (4) -CH2-; X4, X5, X6 y X7 se seleccionan cada uno entre el grupo que consiste en (1) N, (2) N→ O, (3) CH, (4) O con la condicion de que uno de X4, X5, X6 y X7 puede estar ausente, formando de ese modo un anillo de cinco miembros; R1 se selecciona entre el grupo que consiste en (1) hidrogeno, (2) halogeno, (3) -alquilo C1-6, (4) -alquinilo C2-6, (4) fenilo, (5) >=O, (6) >=CH2, (7) hidroxilo, en donde los grupos alquilo, alquinilo o fenilo de R1 estan opcionalmente sustituidos con uno o mas (a) hidroxilo, o (b) halogeno; R2A y R2B se seleccionan independientemente entre el grupo que consiste en (1) hidrogeno, (2) hidroxilo, y (3) halogeno, o R2A y R2B forman juntos >=O; R3 esta opcionalmente presente en uno o mas de los atomos de carbono del anillo y se selecciona independientemente entre el grupo que consiste en (1) halogeno, (2) -O-alquilo C1-6, (3) -S-alquilo C1-6, o (4) un grupo heteroarilo, que es un grupo ciclico aromatico, que tiene de cinco a doce atomos de anillo, dichos atomos de anillo se seleccionan entre C, O, N, N → O o S, al menos uno de los cuales es O, N, N → O o S, en donde el heteroarilo esta opcionalmente sustituido con alquilo C1-6; R4 esta opcionalmente presente en uno o mas de los atomos de anillo y se selecciona entre el grupo que consiste en (1) hidroxilo, (2) halogeno, (3) -alquilo C1-6, (4) -O-alquilo C1-6, (5) -S-alquilo C1-6, (6) -cicloalquilo C3-8, (7) -arilo C6-10, (8) -CN, (9) un grupo heteroarilo, que es un grupo ciclico aromatico, que tiene de cinco a doce atomos de anillo, dichos atomos de anillo se seleccionan entre C, O, N, NO o S, al menos uno de los cuales es O, N, N → O o S, (10) -O-heterociclilo, (11) -NRARB, en donde RA y RB se seleccionan entre el grupo que consiste en (a) hidrogeno, o (b) -alquilo C1-6, o RA y RB se unen junto con el nitrogeno al que estan unidos para formar un anillo carbociclico de 4 a 6 40 miembros, en el que uno o dos de los atomos de carbono de anillo estan opcionalmente reemplazados por un nitrogeno, un oxigeno o un azufre, y el anillo esta opcionalmente sustituido con uno o mas (a) halogeno, (b) hidroxilo, (c) alquilo C1-6, (d) -O-alquilo C1-6, (e) -C(>=O)-(O)n -alquilo C1-6; en donde n es 0-1; y el grupo alquilo, cicloalquilo, arilo o heteroarilo de R4 esta opcionalmente sustituido con uno o mas (a) halogeno, (b) hidroxi, (c) -O-alquilo C1-6, (d) -alquilo C1-6, (e) -S-alquilo C1-6, o (f) un grupo heteroarilo, que es un grupo ciclico aromatico, que tiene de cinco a doce atomos de anillo, dichos atomos de anillo se seleccionan entre C, O, N, N → O o S, al menos uno de los cuales es O, N, N → O o S, en donde los restos alquilo, arilo o heteroarilo estan opcionalmente sustituidos con uno o mas (i) halogeno, (ii) hidroxi, (iii) -O-alquilo C1-6, o (iv) -alquilo C1-6; o dos grupos R4 se unen conjuntamente para formar un grupo heteroarilo de anillo condensado de tres o cuatro atomos, dichos atomos de anillo se seleccionan entre C, O, N, N → O o S, al menos uno de los cuales es O, N, N → O o S, o una sal farmaceuticamente aceptable del mismo.

Description

imagen1
imagen2
imagen3
imagen4
imagen5
imagen6
imagen7
imagen8
imagen9
imagen10
imagen11
imagen12
imagen13
imagen14
imagen15
imagen16
imagen17
imagen18
imagen19
imagen20
imagen21
imagen22
imagen23
imagen24
imagen25
imagen26
imagen27
imagen28
imagen29
imagen30
imagen31
imagen32
imagen33
imagen34
imagen35
imagen36
imagen37
imagen38
imagen39
imagen40
imagen41
imagen42
imagen43
imagen44
imagen45
imagen46
imagen47
imagen48
imagen49
imagen50
imagen51
imagen52
imagen53
imagen54
imagen55
imagen56
imagen57
imagen58
imagen59
imagen60
imagen61
imagen62
imagen63
imagen64
imagen65
imagen66
imagen67
imagen68
imagen69
imagen70
imagen71
imagen72
imagen73
imagen74
imagen75
imagen76
imagen77
imagen78
imagen79
imagen80
imagen81
imagen82
imagen83
imagen84
imagen85
imagen86
imagen87
imagen88
imagen89
imagen90
imagen91
imagen92
imagen93
imagen94
imagen95
imagen96
imagen97
imagen98
imagen99
imagen100
imagen101
imagen102
imagen103
imagen104
imagen105
imagen106
imagen107
imagen108
imagen109
imagen110
imagen111
imagen112
imagen113

Claims (1)

  1. imagen1
    imagen2
    imagen3
    imagen4
    imagen5
    imagen6
    imagen7
    imagen8
ES10841821.1T 2009-12-17 2010-12-13 Moduladores alostéricos positivos del receptor M1 de quinolina amida Active ES2575154T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US287535P 2001-04-30
US28753509P 2009-12-17 2009-12-17
PCT/US2010/060007 WO2011084368A1 (en) 2009-12-17 2010-12-13 Quinoline amide m1 receptor positive allosteric modulators

Publications (1)

Publication Number Publication Date
ES2575154T3 true ES2575154T3 (es) 2016-06-24

Family

ID=44305688

Family Applications (1)

Application Number Title Priority Date Filing Date
ES10841821.1T Active ES2575154T3 (es) 2009-12-17 2010-12-13 Moduladores alostéricos positivos del receptor M1 de quinolina amida

Country Status (41)

Country Link
US (2) US9199939B2 (es)
EP (1) EP2512243B1 (es)
JP (1) JP5651708B2 (es)
KR (1) KR101494059B1 (es)
CN (1) CN102651970B (es)
AR (1) AR079510A1 (es)
AU (1) AU2010340142B2 (es)
BR (1) BR112012014180A2 (es)
CA (1) CA2782347C (es)
CL (1) CL2012001605A1 (es)
CO (1) CO6551729A2 (es)
CR (1) CR20120327A (es)
CY (1) CY1117726T1 (es)
DK (1) DK2512243T3 (es)
DO (1) DOP2012000167A (es)
EA (1) EA022494B1 (es)
EC (1) ECSP12011983A (es)
ES (1) ES2575154T3 (es)
GE (1) GEP201606506B (es)
GT (1) GT201200201A (es)
HK (1) HK1170122A1 (es)
HN (1) HN2012001265A (es)
HR (1) HRP20160574T1 (es)
HU (1) HUE029734T2 (es)
IL (1) IL220130A0 (es)
MA (1) MA33920B1 (es)
ME (1) ME02421B (es)
MX (1) MX336774B (es)
NI (1) NI201200107A (es)
NZ (1) NZ600674A (es)
PE (1) PE20121613A1 (es)
PL (1) PL2512243T3 (es)
PT (1) PT2512243E (es)
RS (1) RS54798B1 (es)
SG (1) SG181719A1 (es)
SI (1) SI2512243T1 (es)
TN (1) TN2012000231A1 (es)
TW (1) TWI412525B (es)
UA (1) UA106406C2 (es)
WO (1) WO2011084368A1 (es)
ZA (1) ZA201204313B (es)

Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10164139A1 (de) 2001-12-27 2003-07-10 Bayer Ag 2-Heteroarylcarbonsäureamide
US9101612B2 (en) * 2010-02-11 2015-08-11 Northwestern University Secondary structure stabilized NMDA receptor modulators and uses thereof
CN103221411B (zh) 2010-05-17 2016-05-11 富瑞姆制药公司 (R)-7-氯-N-(奎宁环-3-基)苯并[b]噻吩-2-甲酰胺盐酸盐单水合物的晶型
US8815902B2 (en) 2010-06-15 2014-08-26 Merck Sharp & Dohme Corp. Tetrahydroquinoline amide M1 receptor positive allosteric modulators
EP2709621B1 (en) * 2011-05-17 2016-11-02 Merck Sharp & Dohme Corp. N-linked quinolineamide m1 receptor positive allosteric modulators
WO2013129622A1 (ja) 2012-03-02 2013-09-06 武田薬品工業株式会社 複素環化合物およびその用途
AU2013259871A1 (en) 2012-05-08 2014-11-20 Forum Pharmaceuticals Inc. Methods of maintaining, treating or improving cognitive function
WO2014077401A1 (ja) 2012-11-19 2014-05-22 武田薬品工業株式会社 含窒素複素環化合物
TW201512197A (zh) * 2013-08-30 2015-04-01 Hoffmann La Roche 吡咯并吡啶或吡唑并吡啶衍生物
CA2918925A1 (en) * 2013-09-27 2015-04-02 F. Hoffmann-La Roche Ag Indol and indazol derivatives
GB201317363D0 (en) 2013-10-01 2013-11-13 Eisai Ltd Novel compounds
CA2930961A1 (en) * 2014-01-22 2015-07-30 F. Hoffmann-La Roche Ag Fluoro-naphthyl derivatives
JP6571077B2 (ja) * 2014-06-13 2019-09-04 武田薬品工業株式会社 含窒素複素環化合物
WO2016009297A1 (en) 2014-07-18 2016-01-21 Pfizer Inc. Pyridine derivatives as muscarinic m1 receptor positive allosteric modulators
JP6908536B2 (ja) 2015-06-09 2021-07-28 バイエル・ファルマ・アクティエンゲゼルシャフト ムスカリンｍ２受容体の正のアロステリックモジュレーター
DK3347349T3 (da) * 2015-09-10 2019-10-28 Suven Life Sciences Ltd Fluorindolderivater som muskarin m1-receptor-positive allosteriske modulatorer
WO2017099969A1 (en) * 2015-12-10 2017-06-15 Merck Sharp & Dohme Corp. Tetrahydroquinoxaline m1 receptor positive allosteric modulators
US11111251B2 (en) * 2016-02-16 2021-09-07 Vanderbilt University Positive allosteric modulators of the muscarinic acetylcholine receptor M1
WO2017151449A1 (en) * 2016-03-04 2017-09-08 Merck Sharp & Dohme Corp. M1 receptor positive allosteric modulator compounds and methods of use thereof
WO2018011017A1 (de) 2016-07-11 2018-01-18 Bayer Pharma Aktiengesellschaft 7-substituierte 1-pyridyl-naphthyridin-3-carbonsäureamide und ihre verwendung
CN109952302B (zh) 2016-09-02 2020-11-24 苏文生命科学有限公司 毒蕈碱m1受体正向别构调节剂
JOP20190045A1 (ar) 2016-09-14 2019-03-14 Bayer Ag مركبات أميد حمض 1- أريل-نفثيريدين-3-كربوكسيليك مستبدلة في الموضع 7 واستخدامها.
WO2018063552A1 (en) 2016-09-30 2018-04-05 Vanderbilt University Positive allosteric modulators of the muscarinic acetylcholine receptor m1
EA035599B1 (ru) * 2017-04-13 2020-07-14 Сувен Лайф Сайенсиз Лимитед Позитивные аллостерические модуляторы мускариновых m1-рецепторов
BR112019026096A2 (pt) * 2017-06-20 2020-07-07 Takeda Pharmaceutical Company Limited composto, medicamento, métodos para modulação alostérica positiva do receptor muscarínico colinérgico m1 e para a profilaxia ou o tratamento de constipação, e, uso do composto
LT3643718T (lt) * 2017-06-20 2023-10-25 Takeda Pharmaceutical Company Limited Heterociklinis junginys ir jo kaip teigiamo alosterinio cholinerginio muskarino m1 receptoriaus moduliatoriaus naudojimas
JP7110338B2 (ja) * 2017-10-27 2022-08-01 スヴェン・ライフ・サイエンシーズ・リミテッド ムスカリンｍ１受容体陽性アロステリックモジュレーターである多環式アミド類
WO2020067457A1 (ja) 2018-09-28 2020-04-02 武田薬品工業株式会社 縮合環化合物
EP3858828A4 (en) 2018-09-28 2022-07-06 Takeda Pharmaceutical Company Limited HETEROCYCLIC COMPOUND
AU2019362468B2 (en) 2018-10-17 2022-04-21 Suven Life Sciences Limited Pyrrolo-pyridazine derivatives as muscarinic M1 receptor positive allosteric modulators
WO2023114224A1 (en) 2021-12-13 2023-06-22 Sage Therapeutics, Inc. Combination of muscarinic receptor positive modulators and nmda positive allosteric modulators

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL135495A (en) 1995-09-28 2002-12-01 Hoechst Ag Intermediate compounds for the preparation of quinoline-converted amines - 2 - carboxylic acid
AU2001280176A1 (en) 2000-08-29 2002-03-13 Yamanouchi Pharmaceutical Co..Ltd. Novel ester or amide derivatives
EP1596867A4 (en) 2003-02-19 2006-03-22 Merck & Co Inc TREATMENT OF PSYCHOSIS WITH ECTOPIC ACTIVATOR OF M1 MUSCARINIC RECEPTOR
MXPA05009722A (es) 2003-03-10 2006-03-09 Schering Corp Inhibidores heterociclicos de cinasa: metodos de uso y sintesis.
SE0302139D0 (sv) * 2003-07-28 2003-07-28 Astrazeneca Ab Novel compounds
CA2551171C (en) 2003-12-23 2012-07-10 Bio-Medisinsk Innovasjon As Modulators of peripheral 5-ht receptors
EP1725240A4 (en) * 2004-03-17 2009-03-25 Glaxo Group Ltd ANTAGONISTS OF THE ACETYLCHOLINE MUSCARINIC RECEPTOR
WO2007100366A2 (en) * 2005-12-05 2007-09-07 Merck & Co., Inc. Quinolone m1 receptor positive allosteric modulators
CN101321733A (zh) * 2005-12-05 2008-12-10 默克公司 喹诺酮m1受体阳性变构调节剂
US8106073B2 (en) 2007-11-30 2012-01-31 Astrazeneca Ab Quinoline derivatives 057
WO2009117283A2 (en) * 2008-03-21 2009-09-24 Merck & Co., Inc. Quinolizidinone m1 receptor positive allosteric modulators
EA019098B1 (ru) 2008-11-20 2014-01-30 Мерк Шарп Энд Домэ Корп. Арилметилбензохиназолиноны в качестве позитивных аллостерических модуляторов рецептора м1
WO2010096338A1 (en) 2009-02-23 2010-08-26 Merck Sharp & Dohme Corp. PYRAZOLO [4,3-c] CINNOLIN-3-ONE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS
US8293744B2 (en) 2009-04-20 2012-10-23 Merck Sharp & Dohme Corp. Heterocyclic fused cinnoline M1 receptor positive allosteric modulators
RS54051B1 (en) 2009-08-31 2015-10-30 Merc Sharp & Dohme Corp. PIRANIL ARYL METHYL BENZOHINAZOLINONE AS POSITIVE M1 RECEPTOR MODULATORS
US8895580B2 (en) 2009-10-21 2014-11-25 Merck Sharp & Dohme Corp. Quinolinone-pyrazolone M1 receptor positive allosteric modulators
US8754220B2 (en) 2009-11-20 2014-06-17 Merck Sharp & Dohme Corp. Quinolizidinone carboxamide M1 receptor positive allosteric modulators
EP2512245B1 (en) 2009-12-14 2014-07-23 Merck Sharp & Dohme Corp. Pyridoquinazolinone m1 receptor positive allosteric modulators
US8383638B2 (en) 2009-12-21 2013-02-26 Merck Sharp & Dohme Aminobenzoquinazolinone M1 receptor positive allosteric modulators
WO2011149801A1 (en) 2010-05-28 2011-12-01 Merck Sharp & Dohme Corp. Naphthalene carboxamide m1 receptor positive allosteric modulators
US8815902B2 (en) 2010-06-15 2014-08-26 Merck Sharp & Dohme Corp. Tetrahydroquinoline amide M1 receptor positive allosteric modulators
EP2582241B1 (en) 2010-06-15 2016-04-06 Merck Sharp & Dohme Corp. Heterocyclic fused phenanthrolinone m1 receptor positive allosteric modulators
EP2709621B1 (en) 2011-05-17 2016-11-02 Merck Sharp & Dohme Corp. N-linked quinolineamide m1 receptor positive allosteric modulators

Also Published As

Publication number Publication date
EP2512243A1 (en) 2012-10-24
CO6551729A2 (es) 2012-10-31
TW201130824A (en) 2011-09-16
UA106406C2 (ru) 2014-08-26
EP2512243B1 (en) 2016-04-06
HUE029734T2 (en) 2017-03-28
TN2012000231A1 (en) 2013-12-12
US20160075656A1 (en) 2016-03-17
ME02421B (me) 2016-09-20
TWI412525B (zh) 2013-10-21
NZ600674A (en) 2013-05-31
EA022494B1 (ru) 2016-01-29
RS54798B1 (sr) 2016-10-31
PL2512243T3 (pl) 2016-09-30
CN102651970B (zh) 2014-11-12
PT2512243E (pt) 2016-06-08
HN2012001265A (es) 2015-09-07
HRP20160574T1 (hr) 2016-06-17
BR112012014180A2 (pt) 2015-09-15
CL2012001605A1 (es) 2012-10-05
IL220130A0 (en) 2012-07-31
PE20121613A1 (es) 2012-12-02
MX2012007013A (es) 2012-07-03
ECSP12011983A (es) 2012-07-31
AR079510A1 (es) 2012-02-01
AU2010340142B2 (en) 2014-05-08
CA2782347C (en) 2014-09-23
HK1170122A1 (zh) 2013-02-22
SG181719A1 (en) 2012-07-30
KR101494059B1 (ko) 2015-02-16
MX336774B (es) 2016-01-28
NI201200107A (es) 2012-10-30
US20120252808A1 (en) 2012-10-04
DK2512243T3 (en) 2016-07-25
SI2512243T1 (sl) 2016-07-29
KR20120084324A (ko) 2012-07-27
US9199939B2 (en) 2015-12-01
WO2011084368A1 (en) 2011-07-14
CR20120327A (es) 2012-07-30
JP5651708B2 (ja) 2015-01-14
JP2013514358A (ja) 2013-04-25
CN102651970A (zh) 2012-08-29
MA33920B1 (fr) 2013-01-02
GEP201606506B (en) 2016-07-11
DOP2012000167A (es) 2012-12-31
GT201200201A (es) 2015-05-20
AU2010340142A1 (en) 2012-06-14
ZA201204313B (en) 2016-01-27
CY1117726T1 (el) 2017-05-17
EA201290519A1 (ru) 2013-01-30
CA2782347A1 (en) 2011-07-14
EP2512243A4 (en) 2013-05-29

Similar Documents

Publication Publication Date Title
ES2575154T3 (es) Moduladores alostéricos positivos del receptor M1 de quinolina amida
ES2481409T3 (es) Compuestos 2,5,6,7-tetrahidro-[1,4]oxazepin-3-ilamina o 2,3,6,7-tetrahidro-[1,4]oxazepin-5-ilamina
PE20200008A1 (es) Isoquinolinas como inhibidores de hpk1
ES2525481T3 (es) Derivados espirocíclicos de ácido tetrónico
AR096371A1 (es) 2-fenilimidazo[1,2-a]pirimidinas
AR052568A1 (es) Derivados de pirazolo -pirimidina como antagonstas de mglur2
CY1119049T1 (el) Υποκατεστημενα πυρρολιδινο-2-καρβοξαμιδια
CR9959A (es) Derivados de pirazol
CO6251264A2 (es) Derivados de 1-ciano ciclopropilo como inhibidores de la captesina k
ECSP10010356A (es) Derivados de carboxamidas n-azabicíclicas, su preparación y su aplicación en terapéutica
AR089774A1 (es) Derivados de indolizina, su procedimiento de preparacion y las composiciones farmaceuticas que los contienen
AR096640A1 (es) Derivados de indolin-2-ona o pirrolo-piridin / pirimidin-2-ona
ES2531009T3 (es) Análogos sustituidos de dicetopiperazina para su uso como agentes para la administración de fármacos
ES2552462T3 (es) Nuevo compuesto de un mimético de giro inverso y un procedimiento de producción y uso del mismo
AR061603A1 (es) Derivados de etenilcarboxamidas microbicidas
ES2222336T3 (es) Inhibidores de girasas y sus usos.
AR053092A1 (es) Compuestos derivados de acido fenoxiacetico y compuestos intermediarios de sintesis
AR078674A1 (es) Derivados de pirazolo[3, 4-d]pirimidina, un intermediario para su sintesis, una composicion farmaceutica que los comprende y su uso en el tratamiento de enfermedades mediadas por la inhibicion de las pi3-quinasas
AR094225A1 (es) Peptidos como agonistas de oxitocina
EA201070871A1 (ru) Бициклические производные азабициклических карбоксамидов, их получение и их применение в терапии
ECSP12012161A (es) Compuestos en calidad de antagonistas de Bradiquinina-b1
AR065932A1 (es) Derivados de imidazolidinacarboxamida como inhibidores de lipasas y fosfolipasas
ECSP14013221A (es) Fenil-3-aza-biciclo [3.1.0] hex-3-il-metanonas y su uso como medicamento.
AR076850A1 (es) Derivados sustituidos de indazol y aza-indazol como moduladores de la gamma secretasa.
CU23761B7 (es) Nuevos derivados de diosmetina, su procedimiento de preparación y las composiciones farmacéuticas que los contienen