SG11201808220VA - Allosteric modulators of nicotinic acetylcholine receptors - Google Patents

Allosteric modulators of nicotinic acetylcholine receptors

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Publication number
SG11201808220VA
SG11201808220VA SG11201808220VA SG11201808220VA SG11201808220VA SG 11201808220V A SG11201808220V A SG 11201808220VA SG 11201808220V A SG11201808220V A SG 11201808220VA SG 11201808220V A SG11201808220V A SG 11201808220VA SG 11201808220V A SG11201808220V A SG 11201808220VA
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SG
Singapore
Prior art keywords
pike
pennsylvania
sumneytown
west point
international
Prior art date
Application number
SG11201808220VA
Inventor
Brendan Crowley
Brian Campbell
Joseph Duffy
Thomas Greshock
Deodial Guiadeen
Andrew John Harvey
Belinda Huff
Kenneth Leavitt
Vanessa Rada
John Sanders
William Shipe
Linda Suen
Ian Bell
Original Assignee
Merck Sharp & Dohme
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Application filed by Merck Sharp & Dohme filed Critical Merck Sharp & Dohme
Publication of SG11201808220VA publication Critical patent/SG11201808220VA/en

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    • C07D285/01—Five-membered rings
    • C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/12—1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4192—1,2,3-Triazoles
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/421—1,3-Oxazoles, e.g. pemoline, trimethadione
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4245—Oxadiazoles
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    • A61K31/425—Thiazoles
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/433—Thidiazoles
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    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
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    • C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
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    • C07D249/04—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
    • C07D249/06—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles with aryl radicals directly attached to ring atoms
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    • C07D271/10—1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles
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    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D277/26—Radicals substituted by sulfur atoms
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    • C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
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    • C07D495/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Control Of El Displays (AREA)
  • Steroid Compounds (AREA)
  • Pyridine Compounds (AREA)

Abstract

INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property -, Organization MD 1111101110101011111 HO 11111 011101111011110101111101111111011011# International Bureau ... ...j .......,./ (10) International Publication Number (43) International Publication Date WO 2017/165256 Al 28 September 2017 (28.09.2017) WIP0 I PCT (51) International Patent Classification: Ranley Grove, Paddington, New South Wales QLD4064 C07D 231/12 (2006.01) C07D 261/08 (2006.01) C07D 233/64 (2006.01) C07D 263/32 (2006.01) C07D 413/04 (2006.01) C07D 271/06 (2006.01) C07D 413/06 (2006.01) C07D 495/04 (2006.01) (AU). HUFF, Belinda, C. [AU/AU]; 85 Morphett Road, Camden Park, South Australia 5038 (AU). LEAVITT, Kenneth, J. [US/US]; 770 Sumneytown Pike, West Point, Pennsylvania 19486 (US). RADA, Vanessa, L. [US/US]; C07D 413/10 (2006.01) C07D 277/26 (2006.01) 770 Sumneytown Pike, West Point, Pennsylvania 19486 C07D 417/04 (2006.01) C07D 285/08 (2006.01) (US). SANDERS, John, M. [US/US]; 770 Sumneytown C07D 249/06 (2006.01) CO7D 285/12 (2006.01) Pike, West Point, Pennsylvania 19486 (US). SHIPE, Wil- CO7D 249/08 (2006.01) Ram, D. [US/US]; 770 Sumneytown Pike, West Point, (21) International Application Number: Pennsylvania 19486 (US). SUEN, Linda, M. [US/US]; PCT/US2017/023127 770 Sumneytown Pike, West Point, Pennsylvania 19486 (US). BELL, Ian, M. [US/US]; 770 Sumneytown Pike, (22) International Filing Date: West Point, Pennsylvania 19486 (US). 20 March 2017 (20.03.2017) (74) Common Representative: MERCK SHARP & DOHME (25) Filing Language: English CORP.; 126 East Lincoln Avenue, Rahway, New Jersey 07065-0907 (US). (26) Publication Language: English (81) Designated States (unless otherwise indicated, for every (30) Priority Data: kind of national protection available): AE, AG, AL, AM, 62/311,888 22 March 2016 (22.03.2016) US AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, 62/369,778 2 August 2016 (02.08.2016) US BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, (71) Applicant: MERCK SHARP & DOHME CORP. DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, [US/US]; 126 East Lincoln Avenue, Rahway, New Jersey HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KH, KN, 07065-0907 (US). KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, = Inventors; and NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, (72) (71) Applicants (for US only): CROWLEY, Brendan, M. RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, [US/US]; 770 Sumneytown Pike, West Point, Pennsylvania TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, 19486 (US). CAMPBELL, Brian, T. [US/US]; 770 Sum- ZA, ZM, ZW. neytown Pike, West Point, Pennsylvania 19486 (US). DUFFY, Joseph, L. [US/US]; 2000 Galloping Hill Road, (84) Designated States (unless otherwise indicated, for every Kenilworth, New Jersey 07033 (US). GRESHOCK, kind of regional protection available): ARIPO (BW, GH, Thomas, J. [US/US]; 770 Sumneytown Pike, West Point, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, Pennsylvania 19486 (US). GUIADEEN, Deodial, G. TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, [US/US]; 770 Sumneytown Pike, West Point, Pennsylvania TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, 19486 (US). HARVEY, Andrew John [AU/AU]; 4A/6 DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, [Continued on next page] Title: ALLOSTERIC MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS (54) R 3 R4 Y \ A ir) ei R 5 ir) X 0) 1-1 N 1-1 (57) : The present disclosure relates to compounds of formula (I) that are useful as modulators of ca nAChR, compositions N comprising such compounds, and the use of such compounds for preventing, treating, or ameliorating disease, particularly disorders of the central nervous system such as cognitive impairments in Alzheimer's disease, Parkinson's disease, and schizophrenia, as well 0 as for L-DOPA induced-dyskinesia and inflammation. WO 2017/165256 Al MIDEDIMOMOIDEIR010130HinillUMMOIMIE SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, as to the applicant's entitlement to claim the priority of GW, KM, ML, MR, NE, SN, TD, TG). the earlier application (Rule 4.17(iii)) Declarations under Rule 4.17: Published: — as to applicant's entitlement to apply for and be granted a patent (Rule 4.17(0 with international search report (Art. 21(3))
SG11201808220VA 2016-03-22 2017-03-20 Allosteric modulators of nicotinic acetylcholine receptors SG11201808220VA (en)

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