[go: up one dir, main page]

SG11201803757UA - N-[2-(1 -benzylpiperidin-4-yl)ethyl]-4-(pyrazin-2-yl)-piperazine-1 -carboxamide derivatives and related compounds as muscarinic receptor 4 (m4) antagonists for treating neurological diseases - Google Patents

N-[2-(1 -benzylpiperidin-4-yl)ethyl]-4-(pyrazin-2-yl)-piperazine-1 -carboxamide derivatives and related compounds as muscarinic receptor 4 (m4) antagonists for treating neurological diseases

Info

Publication number
SG11201803757UA
SG11201803757UA SG11201803757UA SG11201803757UA SG11201803757UA SG 11201803757U A SG11201803757U A SG 11201803757UA SG 11201803757U A SG11201803757U A SG 11201803757UA SG 11201803757U A SG11201803757U A SG 11201803757UA SG 11201803757U A SG11201803757U A SG 11201803757UA
Authority
SG
Singapore
Prior art keywords
international
benzylpiperidin
pyrazin
piperazine
diseases
Prior art date
Application number
SG11201803757UA
Inventor
Nicole Harriott
Nicholas Pagano
Original Assignee
Neurocrine Biosciences 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 Neurocrine Biosciences Inc filed Critical Neurocrine Biosciences Inc
Publication of SG11201803757UA publication Critical patent/SG11201803757UA/en

Links

Classifications

    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non 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
    • 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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/28—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/26—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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
    • C07D211/40—Oxygen 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
    • C07D401/14—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
    • C07D405/14—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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property -' Organization International Bureau (43) International Publication Date .... ..sr ,„„..) 11 May 2017(11.05.2017) WIPO I PCT (10) WO International 111111111111311111111111111111111111111111111111111111111111111111111111111111111111111111 2017/079641 Publication Al Number (51) International Patent Classification: AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, C07D 401/12 (2006.01) A61K 31/4545 (2006.01) BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, CO7D 211/26 (2006.01) A61P 25/28 (2006.01) DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, CO7D 211/40 (2006.01) A61P 25/16 (2006.01) HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KN, KP, KR, A61K 31/445 (2006.01) A61P 25/18 (2006.01) KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, (21) International Application Number: OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, PCT/US2016/060659 SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, (22) International Filing Date: TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, 4 November 2016 (04.11.2016) ZW. (25) Filing Language: English (8 4 ) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, (26) Publication Language: English GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, (30) Priority Data: TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, 62/252,179 6 November 2015 (06.11.2015) US TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, 62/275,708 6 January 2016 (06.01.2016) US 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, (71) Applicant: NEUROCRINE BIOSCIENCES, INC. SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, [US/US]; 12780 El Camino Real, San Diego, California GW, KM, ML, MR, NE, SN, TD, TG). 92130 (US). Declarations under Rule 4.17: (72) Inventors: HARRIOTT, Nicole; 11340 Squamish Road, as to applicant's entitlement to apply for and be granted a San Diego, California 92126 (US). PAGANO, Nicholas; patent (Rule 4.17 (ii)) 1512 La Playa Avenue, Apartment 312, San Diego, Cali- fornia 92109 (US). — as to the applicant's entitlement to claim the priority of the earlier application (Rule 4.17(iii)) (74) Agents: HERMANNS, Karl, R. et al.; Seed Intellectual Property Law Group LLP, Suite 5400, 701 Fifth Avenue, Published: Seattle, Washington 98104-7064 (US). — with international search report (Art 21(3)) (81) Designated States (unless otherwise indicated, for every _ 19(1)) with amended claims (Art kind AE, AG, AL, AM, of national protection available): Title: (54) N-[2-(1 -BENZYLPIPERIDIN-4-YL)ETHYL]-4-(PYRAZIN-2-YL)-PIPERAZINE-1 -CARBOXAMIDE DERIVATIVES AND RE- LATED COMPOUNDS AS MUSCARINIC RECEPTOR 4 (M4) ANTAGONISTS FOR TREATING NEUROLOGICAL DISEASES (R2)w (R3)x Il .4t A 11 i t 0 \ IN (57) : Provided herein are small molecule 0 ---- ter or pharmaceutically acceptable salt thereof, Methods for treating diseases/ disorders by antagonizing 1:::j ceptor 4 (M4), are also disclosed. Such diseases/disorders el Lewy Body Dementia and the cognitive deficits ea ) dyskinesias, dystonia, chorea, levodopa induced Preferred compounds are e.g. 1\112-(1-benzylpiperidin-4-yflethyl]-4- compounds wherein the pyrazine has been replaced N '- ''' .--r 'Th-] wherein dyskinesia, by compounds associated ) o,i A, B, are muscarinic cerebral e.g. pyridazine, (IR,Oy B L2 of the following C, L I , L 2, e.g. neurological with schizophrenia, palsy, receptors, pyrimidine, r-7\ C .Y R I , R R R R 2, progressive (pyrazin-2-y1)-piperazine-1-carboxamide formula diseases/disorders sh (I) (I): or a stereoisomer, tautomer, solvate, es - 3, 4, 5, w, x, y and z are as defined herein. including specifically antagonizing muscarinic re - such as e.g. Alzheimer's Disease, Parkinson's Disease, drug induced Parkinsonism, supranuclear palsy, and Huntington's disease. derivatives and related pyridine or phenyl.
SG11201803757UA 2015-11-06 2016-11-04 N-[2-(1 -benzylpiperidin-4-yl)ethyl]-4-(pyrazin-2-yl)-piperazine-1 -carboxamide derivatives and related compounds as muscarinic receptor 4 (m4) antagonists for treating neurological diseases SG11201803757UA (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562252179P 2015-11-06 2015-11-06
US201662275708P 2016-01-06 2016-01-06
PCT/US2016/060659 WO2017079641A1 (en) 2015-11-06 2016-11-04 N-[2-(1 -benzylpiperidin-4-yl)ethyl]-4-(pyrazin-2-yl)-piperazine-1 -carboxamide derivatives and related compounds as muscarinic receptor 4 (m4) antagonists for treating neurological diseases

Publications (1)

Publication Number Publication Date
SG11201803757UA true SG11201803757UA (en) 2018-06-28

Family

ID=57349137

Family Applications (1)

Application Number Title Priority Date Filing Date
SG11201803757UA SG11201803757UA (en) 2015-11-06 2016-11-04 N-[2-(1 -benzylpiperidin-4-yl)ethyl]-4-(pyrazin-2-yl)-piperazine-1 -carboxamide derivatives and related compounds as muscarinic receptor 4 (m4) antagonists for treating neurological diseases

Country Status (22)

Country Link
US (2) US11033539B2 (en)
EP (1) EP3371164B1 (en)
JP (2) JP6917989B2 (en)
KR (1) KR20180073685A (en)
CN (1) CN108349936B (en)
AU (1) AU2016348524B2 (en)
BR (1) BR112018008630A2 (en)
CA (1) CA3001873A1 (en)
CL (1) CL2018001217A1 (en)
CO (1) CO2018004800A2 (en)
ES (1) ES2915266T3 (en)
HK (1) HK1253029A1 (en)
IL (1) IL258862B (en)
MA (1) MA43168A (en)
MX (1) MX386148B (en)
MY (1) MY194461A (en)
PE (1) PE20181010A1 (en)
PH (1) PH12018500940A1 (en)
SA (1) SA518391518B1 (en)
SG (1) SG11201803757UA (en)
TN (1) TN2018000130A1 (en)
WO (1) WO2017079641A1 (en)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2016348493B2 (en) 2015-11-06 2021-02-25 F. Hoffmann-La Roche Ag Indolin-2-one derivatives
SG11201803757UA (en) * 2015-11-06 2018-06-28 Neurocrine Biosciences Inc N-[2-(1 -benzylpiperidin-4-yl)ethyl]-4-(pyrazin-2-yl)-piperazine-1 -carboxamide derivatives and related compounds as muscarinic receptor 4 (m4) antagonists for treating neurological diseases
JP2020530451A (en) 2017-08-08 2020-10-22 ヴァンダービルト ユニバーシティー Antagonist of muscarinic acetylcholine receptor M4
JP2020537667A (en) 2017-10-17 2020-12-24 ヴァンダービルト ユニバーシティー Antagonist of muscarinic acetylcholine receptor M4
KR20250037575A (en) 2017-10-20 2025-03-17 반더빌트유니버시티 Antagonists of the muscarinic acetylcholine receptor m4
CA3081324A1 (en) 2017-10-31 2019-05-09 Vanderbilt University Antagonists of the muscarinic acetylcholine receptor m4
EP3732163A4 (en) 2017-12-20 2021-07-14 Vanderbilt University MUSCARINIAN ACETYLCHOLINE RECEPTOR ANTAGONISTS M4
IL276411B2 (en) 2018-02-02 2024-04-01 Univ Vanderbilt Antagonists of the muscarinic acetylcholine receptor m4
SMT202200134T1 (en) 2018-03-08 2022-05-12 Incyte Corp Aminopyrazine diol compounds as pi3k-y inhibitors
US11046658B2 (en) 2018-07-02 2021-06-29 Incyte Corporation Aminopyrazine derivatives as PI3K-γ inhibitors
WO2020048827A1 (en) 2018-09-03 2020-03-12 Bayer Aktiengesellschaft 1, 3, 9-triazaspiro[5.5] undecan-2-one compounds
WO2020048828A1 (en) 2018-09-03 2020-03-12 Bayer Pharma Aktiengesellschaft 5-heteroaryl-3,9-diazaspiro[5.5]undecane compounds
WO2020048826A1 (en) 2018-09-03 2020-03-12 Bayer Aktiengesellschaft 5-substituted 1-oxa-3,9-diazaspiro[5.5]undecan-2-one compounds
JP7460264B2 (en) * 2018-09-04 2024-04-02 コンティニューム・セラピューティクス・インコーポレイテッド Muscarinic acetylcholine M1 receptor antagonists
US11590134B2 (en) * 2019-06-17 2023-02-28 Deciphera Pharmaceuticals, Llc Aminopyrimidine amide autophagy inhibitors and methods of use thereof
CN114901652A (en) * 2019-09-17 2022-08-12 比亚尔R&D投资股份公司 Substituted saturated and unsaturated N-heterocyclic carboxamides and related compounds for the treatment of medical disorders
US11752149B2 (en) 2019-12-02 2023-09-12 Pipeline Therapeutics, Inc. Muscarinic acetylcholine M1 receptor antagonists
TW202134231A (en) 2019-12-06 2021-09-16 美商紐羅克里生物科學有限公司 Muscarinic receptor 4 antagonists and methods of use
CN111072551A (en) * 2019-12-30 2020-04-28 上海睿瓦科技有限公司 Method for preparing piperidine amine by catalytic hydrogenation one-step method
CA3166597A1 (en) * 2020-02-05 2021-08-12 Nicole Harriott Muscarinic receptor 4 antagonists and methods of use
WO2022156708A1 (en) * 2021-01-20 2022-07-28 Jacobio Pharmaceuticals Co., Ltd. Parp7 enzyme inhibitor
AU2022289728A1 (en) * 2021-06-11 2023-11-16 Neuronascent, Inc. Methods and compositions for lipid formulation of lipophilic small molecule therapies of the heterocyclic type
CR20240039A (en) * 2021-07-30 2024-03-21 Neurocrine Biosciences Inc MUSCARINIC RECEPTOR 4 ANTAGONISTS AND METHODS OF USE
CN120475969A (en) * 2022-11-16 2025-08-12 维恩韦疗法公司 TYK2 inhibitors

Family Cites Families (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0619814A1 (en) * 1991-12-31 1994-10-19 Fujisawa Pharmaceutical Co., Ltd. Oxadiazole derivatives having acetylcholinesterase-inhibitory and muscarinic agonist activity
GB9313201D0 (en) * 1993-06-25 1993-08-11 Fujisawa Pharmaceutical Co New heterocyclic compounds
US5700801A (en) * 1994-12-23 1997-12-23 Karl Thomae, Gmbh Piperazine derivatives, pharmaceutical compositions containing these compounds, their use and processes for preparing them
JP3786578B2 (en) * 1997-11-18 2006-06-14 帝人ファーマ株式会社 Cyclic amine derivatives and their use as pharmaceuticals
US7390830B1 (en) * 1999-05-18 2008-06-24 Teijin Limited Remedies or prophylactics for diseases in association with chemokines
WO2001021590A1 (en) * 1999-09-22 2001-03-29 Schering Corporation Muscarinic antagonists
WO2001042208A1 (en) * 1999-12-08 2001-06-14 Teijin Limited Cycloamine ccr5 receptor antagonists
US6362177B1 (en) * 2000-05-16 2002-03-26 Teijin Limited Cyclic amine derivatives and their use as drugs
JPWO2003062234A1 (en) 2002-01-23 2005-05-19 山之内製薬株式会社 Quinoxaline compounds
US8673924B2 (en) 2002-09-04 2014-03-18 Merck Sharp & Dohme Corp. Substituted pyrazolo[1,5-a]pyrimidines as cyclin dependent kinase inhibitors
US7645771B2 (en) * 2002-12-13 2010-01-12 Smithkline Beecham Corp. CCR5 antagonists as therapeutic agents
TW200536830A (en) 2004-02-06 2005-11-16 Chugai Pharmaceutical Co Ltd 1-(2H)-isoquinolone derivative
US20090012116A1 (en) * 2005-07-11 2009-01-08 Naresh Kumar Muscarinic Receptor Antagonists
KR20080087833A (en) * 2005-12-21 2008-10-01 쉐링 코포레이션 Phenoxypiperidine and its analogs useful as histamine H3 antagonists
WO2007130383A2 (en) * 2006-04-28 2007-11-15 Northwestern University Compositions and treatments using pyridazine compounds and secretases
EP1997805A1 (en) * 2007-06-01 2008-12-03 Commissariat à l'Energie Atomique Compounds with antiparasitic activity, applications thereof to the treatment of infectious diseases caused by apicomplexans
JP2013028538A (en) 2009-11-13 2013-02-07 Dainippon Sumitomo Pharma Co Ltd Novel amide derivative
BR112014012031A2 (en) 2011-11-25 2017-05-30 Nerviano Medical Sciences Srl 3-phenyl isoquinolin-1 (2h) -one derivatives as parp-1 inhibitors
WO2014074517A1 (en) * 2012-11-08 2014-05-15 Emory University Cellular compositions used to restore stem cell or progenitor cell function and methods related thereto
CN104812387A (en) * 2012-11-20 2015-07-29 霍夫曼-拉罗奇有限公司 Substituted 1,6-naphthyridines
KR20150132192A (en) 2013-03-18 2015-11-25 제노사이언스 파마 Quinolines derivatives as novel anticancer agents
EP2982666B1 (en) * 2013-04-04 2019-08-07 Takeda Pharmaceutical Company Limited Heterocyclic compound
JP6456392B2 (en) * 2013-09-11 2019-01-23 インスティチュート オブ キャンサー リサーチ：ロイヤル キャンサー ホスピタル 3-Aryl-5-substituted isoquinolin-1-one compounds and therapeutic uses thereof
CA2942687A1 (en) * 2014-03-20 2015-09-24 Samumed, Llc 5-substituted indazole-3-carboxamides and preparation and use thereof
SG11201803757UA (en) * 2015-11-06 2018-06-28 Neurocrine Biosciences Inc N-[2-(1 -benzylpiperidin-4-yl)ethyl]-4-(pyrazin-2-yl)-piperazine-1 -carboxamide derivatives and related compounds as muscarinic receptor 4 (m4) antagonists for treating neurological diseases

Also Published As

Publication number Publication date
MX2018005215A (en) 2018-08-01
TN2018000130A1 (en) 2019-10-04
EP3371164B1 (en) 2022-03-16
SA518391518B1 (en) 2021-06-13
IL258862A (en) 2018-06-28
JP2018531981A (en) 2018-11-01
MY194461A (en) 2022-11-30
CL2018001217A1 (en) 2018-08-03
US20210338653A1 (en) 2021-11-04
US20180325887A1 (en) 2018-11-15
AU2016348524A1 (en) 2018-05-17
AU2016348524B2 (en) 2021-01-28
WO2017079641A1 (en) 2017-05-11
IL258862B (en) 2021-02-28
JP2021050243A (en) 2021-04-01
KR20180073685A (en) 2018-07-02
HK1253029A1 (en) 2019-06-06
EP3371164A1 (en) 2018-09-12
CA3001873A1 (en) 2017-05-11
PE20181010A1 (en) 2018-06-26
JP6917989B2 (en) 2021-08-11
PH12018500940A1 (en) 2018-12-17
MX386148B (en) 2025-03-18
CN108349936A (en) 2018-07-31
MA43168A (en) 2018-09-12
CN108349936B (en) 2021-10-01
US11033539B2 (en) 2021-06-15
BR112018008630A2 (en) 2018-10-30
ES2915266T3 (en) 2022-06-21
CO2018004800A2 (en) 2018-10-31

Similar Documents

Publication Publication Date Title
SG11201803757UA (en) N-[2-(1 -benzylpiperidin-4-yl)ethyl]-4-(pyrazin-2-yl)-piperazine-1 -carboxamide derivatives and related compounds as muscarinic receptor 4 (m4) antagonists for treating neurological diseases
SG11201810683VA (en) Process for preparing n-(5-(3-(7-(3-fluorophenyl)-3h-imidazo[4,5-c]pyridin-2-yl)-1h-indazol-5-yl)pyridin-3-yl)-3-methylbutanamide
SG11201906427QA (en) Heterocyclic spiro compounds as magl inhibitors
SG11201805685PA (en) Substituted thiohydantoin derivatives as androgen receptor antagonists
SG11201907544VA (en) Jak inhibitors containing a 4-membered heterocyclic amide
SG11201805300QA (en) Heterocyclic compounds as immunomodulators
SG11201811712QA (en) 5,7-dihydro-pyrrolo-pyridine derivatives for treating neurological and neurodegenerative diseases
SG11201811414TA (en) Heterocyclic compounds as immunomodulators
SG11201804152RA (en) Heterocyclic compounds as immunomodulators
SG11201804170RA (en) Polycyclic tlr7/8 antagonists and use thereof in the treatment of immune disorders
SG11201907356SA (en) Piperidine-substituted mnk inhibitors and methods related thereto
SG11201908598PA (en) Compounds useful in the treatment or prevention of a prmt5-mediated disorder
SG11201810983PA (en) Novel heterocyclic derivatives useful as shp2 inhibitors
SG11201908633SA (en) Kappa opioid receptor antagonists and products and methods related thereto
SG11201809342YA (en) Pyrimidine compounds as jak kinase inhibitors
SG11201408186TA (en) Pyridinone and pyridazinone derivatives
SG11201808582RA (en) Pyrrolotriazine compounds as tam inhibitors
SG11201803920TA (en) Compounds and compositions useful for treating disorders related to ntrk
SG11201811470PA (en) Pyrazolopyrimidine derivatives as kinase inhibitor
SG11201804098TA (en) Purinones as ubiquitin-specific protease 1 inhibitors
SG11201902886SA (en) Cyclic peptide tyrosine tyrosine compounds as modulators of neuropeptide y receptors
SG11201903487SA (en) PROCESS FOR THE PREPARATION OF PYRAZOLO[1,5-a]PYRIMIDINES AND SALTS THEREOF
SG11201805380YA (en) Urea-based prostate specific membrane antigen (psma) inhibitors for imaging and therapy
SG11201810371XA (en) ANTI-N3pGlu AMYLOID BETA PEPTIDE ANTIBODIES AND USES THEREOF
SG11201808220VA (en) Allosteric modulators of nicotinic acetylcholine receptors