SG11201804936UA - Hydroxyalkylamine- and hydroxycycloalkylamine-substituted diamine-arylsulfonamide compounds with selective activity in voltage-gated sodium channels - Google Patents

Hydroxyalkylamine- and hydroxycycloalkylamine-substituted diamine-arylsulfonamide compounds with selective activity in voltage-gated sodium channels

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Publication number
SG11201804936UA
SG11201804936UA SG11201804936UA SG11201804936UA SG11201804936UA SG 11201804936U A SG11201804936U A SG 11201804936UA SG 11201804936U A SG11201804936U A SG 11201804936UA SG 11201804936U A SG11201804936U A SG 11201804936UA SG 11201804936U A SG11201804936U A SG 11201804936UA
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SG
Singapore
Prior art keywords
new jersey
international
pike
pennsylvania
compounds
Prior art date
Application number
SG11201804936UA
Inventor
Thomas Greshock
James Mulhearn
Junying Zheng
Ronald Kim
Ting Zhang
Anthony Roecker
Walter Won
Philippe Nantermet
Rajan Anand
Gang Zhou
Deping Wang
Liangqin Guo
Original Assignee
Merck Sharp & Dohme
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Application filed by Merck Sharp & Dohme filed Critical Merck Sharp & Dohme
Publication of SG11201804936UA publication Critical patent/SG11201804936UA/en

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    • 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
    • A61K31/41—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
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles
    • 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
    • A61K31/41—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
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • 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
    • A61K31/41—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
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/14—Antitussive agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • 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
    • 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
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • 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
    • C07D277/32—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 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
    • C07D277/38—Nitrogen atoms
    • C07D277/50—Nitrogen atoms bound to hetero atoms
    • C07D277/52—Nitrogen atoms bound to hetero atoms to sulfur atoms, e.g. sulfonamides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01—Five-membered rings
    • C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/08—1,2,4-Thiadiazoles; Hydrogenated 1,2,4-thiadiazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Abstract

EN N R (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (10) International Publication Number (43) International Publication Date WO 2017/106226 Al 22 June 2017 (22.06.2017) WIPO I PCT (51) International Patent Classification: CO7D 285/08 (2006.01) A61K 31/4196 (2006.01) CO7D 417/12 (2006.01) A61K 31/551 (2006.01) CO7D 277/52 (2006.01) A61P 29/00 (2006.01) A61K 31/4168 (2006.01) A61P 11/14 (2006.01) A61K 31/4178 (2006.01) (21) International Application Number: PCT/US2016/066445 (22) International Filing Date: 14 December 2016 (14.12.2016) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/269,327 18 December 2015 (18.12.2015) US 62/290,235 2 February 2016 (02.02.2016) US 62/420,956 11 November 2016 (11.11.2016) US (71) Applicant (for all designated States except US): MERCK SHARP & DOHME CORP. [US/US]; 126 East Lincoln Avenue, Rahway, New Jersey 07065-0907 (US). (72) Inventors; and (71) Applicants NZ, US only): GRESHOCK, Thomas, J. [US/US]; 770 Surrmeytown Pike, West Point, Pennsylvania 19486 (US). MULHEARN, James [US/US]; 770 Sum- neytown Pike, West Point, Pennsylvania 19486 (US). ZHENG, Junying [US/US]; 31 Newcomb Drive, New Providence, New Jersey 07074 (US). KIM, Ronald, M. [US/US]; 2000 Galloping Hill Road, Kenilworth, New Jer- sey 07033 (US). ZHANG, Ting [CN/US]; 126 East Lin- coln Avenue, Rahway, New Jersey 07065-0907 (US). ROECKER, Anthony, J. [US/US]; 770 Surrmeytown Pike, West Point, Pennsylvania 19486 (US). WON, Wal- ter [US/US]; 950 Closter Rock Road, Alpine, New Jersey 08820 (US). NANTERMET, Philippe [US/US]; 770 Surrmeytown Pike, West Point, Pennsylvania 19486 (US). ANAND, Rajan [KE/US]; 22 Rainier Road, Fanwood, New Jersey 07012 (US). ZHOU, Gang [CN/US]; 111 Timothy Place, Bridgewater, New Jersey 08807 (US). WANG, Deping [US/US]; 770 Surrmeytown Pike, West Point, Pennsylvania 19486 (US). GUO, Liangqin [US/US]; 2000 Galloping Hill Road, Kenilworth, New Jer- sey 07033 (US). (74) Common Representative: MERCK SHARP & DOHME CORP.; 126 East Lincoln Avenue, Rahway, New Jersey 07065-0907 (US). (81) Designated States (unless otherwise indicated, for every kind of national protection available): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (84) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, 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, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). Decl arations under Rule 4.17: as to applicant's entitlement to apply for and be granted a patent (Rule 4.1700) [Continued on next page] = (54) Title: HYDROXYALKYLAMINE- AND HYDROXYCYCLOALKYLAMINE-SUBSTITUTED DIAMINE-ARYLSULFON- - AMIDE COMPOUNDS WITH SELECTIVE ACTIVITY IN VOLTAGE-GATED SODIUM CHANNELS (A) (57) : Disclosed are compounds of Formula A, or a salt thereof: Formula (A) wherein R I , R 2 , and E are defined herein, which compounds have properties for inhibiting Na„ 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A or their salts, and methods of treating pain disorders, cough, and itch using the same. 1111111111111101110101011111010111110111010110111111011101111111111111111110111111 W O 20 17 / 106 226 Al WO 2017/106226 Al 1#1101M01101DEIROIDEOM0101101101011101111MOVOIMIE as to the applicant's entitlement to claim the priority of Published: the earlier application (Rule 4.17(iii)) — with international search report (Art. 21(3))
SG11201804936UA 2015-12-18 2016-12-14 Hydroxyalkylamine- and hydroxycycloalkylamine-substituted diamine-arylsulfonamide compounds with selective activity in voltage-gated sodium channels SG11201804936UA (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201562269327P 2015-12-18 2015-12-18
US201662290235P 2016-02-02 2016-02-02
US201662420956P 2016-11-11 2016-11-11
PCT/US2016/066445 WO2017106226A1 (en) 2015-12-18 2016-12-14 Hydroxyalkylamine- and hydroxycycloalkylamine-substituted diamine-arylsulfonamide compounds with selective activity in voltage-gated sodium channels

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SG11201804936UA true SG11201804936UA (en) 2018-07-30

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US (2) US10221167B2 (en)
EP (1) EP3390374B1 (en)
JP (1) JP6572392B2 (en)
KR (1) KR20180095598A (en)
CN (1) CN108699015A (en)
AR (1) AR106987A1 (en)
AU (1) AU2016370554B2 (en)
BR (1) BR112018012327A2 (en)
CA (1) CA3008611A1 (en)
CL (1) CL2018001640A1 (en)
CO (1) CO2018006137A2 (en)
CR (1) CR20180322A (en)
DO (1) DOP2018000150A (en)
EA (1) EA201891313A1 (en)
EC (1) ECSP18052850A (en)
HK (1) HK1255027A1 (en)
IL (1) IL260052A (en)
MX (1) MX2018007450A (en)
NI (1) NI201800067A (en)
PE (1) PE20181495A1 (en)
PH (1) PH12018501288A1 (en)
SG (1) SG11201804936UA (en)
SV (1) SV2018005708A (en)
TN (1) TN2018000195A1 (en)
TW (1) TW201726637A (en)
WO (1) WO2017106226A1 (en)
ZA (1) ZA201803591B (en)

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EA201891313A1 (en) 2018-11-30
US20190233406A1 (en) 2019-08-01
TW201726637A (en) 2017-08-01
PH12018501288A1 (en) 2019-01-28
CA3008611A1 (en) 2017-06-22
AU2016370554B2 (en) 2018-11-29
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CR20180322A (en) 2018-08-21
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