SG11201810280YA - Spiro-lactam nmda receptor modulators and uses thereof - Google Patents

Spiro-lactam nmda receptor modulators and uses thereof

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Publication number
SG11201810280YA
SG11201810280YA SG11201810280YA SG11201810280YA SG11201810280YA SG 11201810280Y A SG11201810280Y A SG 11201810280YA SG 11201810280Y A SG11201810280Y A SG 11201810280YA SG 11201810280Y A SG11201810280Y A SG 11201810280YA SG 11201810280Y A SG11201810280Y A SG 11201810280YA
Authority
SG
Singapore
Prior art keywords
international
pct
compounds
nmda receptor
spiro
Prior art date
Application number
SG11201810280YA
Inventor
M Amin Khan
Original Assignee
Aptinyx Inc
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Publication date
Application filed by Aptinyx Inc filed Critical Aptinyx Inc
Publication of SG11201810280YA publication Critical patent/SG11201810280YA/en

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    • 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
    • C07D487/10Spiro-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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02Muscle relaxants, e.g. for tetanus or cramps
    • 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
    • A61P25/08Antiepileptics; Anticonvulsants
    • 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
    • A61P25/18Antipsychotics, 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
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • 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
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/06Antiglaucoma agents or miotics
    • 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
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C07D471/12Heterocyclic 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 three hetero rings
    • C07D471/20Spiro-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K16/00Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies

Abstract

INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property 1111111111111011101111111111111111111111111111111111111111111111111111111111111111110111111 Organization 0 International Bureau (10) International Publication Number (43) International Publication Date .....0\"\"\" WO 2017/201283 Al 23 November 2017 (23.11.2017) WIPO I PCT (51) International Patent Classification: CO7D 487/10 (2006.01) A61P 25/00 (2006.01) A61K 31/407 (2006.01) (21) International Application Number: PCT/US2017/033323 (22) International Filing Date: 18 May 2017 (18.05.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/338,767 19 May 2016 (19.05.2016) US (71) Applicant: APTINYX INC. [US/US]; 1801 Maple Av- enue, Suite 4300, Evanston, IL 60201 (US). (72) Inventor: KHAN, M. Amin; 720 Oakton Street #3A, Evanston, IL 60202 (US). (74) Agent: BRODOWSKI, Michael et al.; Goodwin Procter LLP, 100 Northern Avenue, Boston, MA 02210 (US). 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, = (81) =_ _ 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. = Designated States (unless otherwise indicated, for every = (84) = = 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). = Published: — with international search report (Art. 21(3)) Il en (54) Title: SPIRO-LACTAM NMDA RECEPTOR MODULATORS AND USES THEREOF ot) ei o (57) : Disclosed are compounds having enhanced potency in the modulation of NMDA receptor 1-1 Rd R 2 0 NH 2 activity. Such compounds can be used in the treatment of conditions such as depression and related ei N disorders. Orally available formulations and other pharmaceutically acceptable delivery forms of the IN R i N OH compounds, including intravenous formulations, are also disclosed. 1-1 0 ei o -_/ ( 1 ) C
SG11201810280YA 2016-05-19 2017-05-18 Spiro-lactam nmda receptor modulators and uses thereof SG11201810280YA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201662338767P 2016-05-19 2016-05-19
PCT/US2017/033323 WO2017201283A1 (en) 2016-05-19 2017-05-18 Spiro-lactam nmda receptor modulators and uses thereof

Publications (1)

Publication Number Publication Date
SG11201810280YA true SG11201810280YA (en) 2018-12-28

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SG11201810280YA SG11201810280YA (en) 2016-05-19 2017-05-18 Spiro-lactam nmda receptor modulators and uses thereof

Country Status (18)

Country Link
US (2) US9932347B2 (en)
EP (1) EP3458458B1 (en)
JP (1) JP6823083B2 (en)
KR (1) KR102128675B1 (en)
CN (1) CN109415372B (en)
AU (1) AU2017267708B2 (en)
BR (1) BR112018073663A2 (en)
CA (1) CA3024606C (en)
CL (1) CL2018003265A1 (en)
CO (1) CO2018013747A2 (en)
EA (1) EA201892657A1 (en)
IL (1) IL263045B (en)
MX (1) MX2018014202A (en)
PE (1) PE20190174A1 (en)
PH (1) PH12018502438A1 (en)
SG (1) SG11201810280YA (en)
WO (1) WO2017201283A1 (en)
ZA (1) ZA201807731B (en)

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MX2018014202A (en) * 2016-05-19 2019-06-20 Aptinyx Inc Spiro-lactam nmda receptor modulators and uses thereof.
WO2017201285A1 (en) 2016-05-19 2017-11-23 Aptinyx Inc. Spiro-lactam nmda receptor modulators and uses thereof
KR102462288B1 (en) 2016-08-01 2022-11-01 앱티닉스 인크. Spiro-lactam and bis-spiro-lactam NMDA receptor modulators and uses thereof
KR102503590B1 (en) 2016-08-01 2023-02-24 앱티닉스 인크. Spiro-lactam NMDA receptor modulators and uses thereof
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