SG11201907844TA - Novel spiro and cyclic bis-benzylidine proteasome inhibitor for the treatment of cancer, diabetes and neurological disorders - Google Patents

Novel spiro and cyclic bis-benzylidine proteasome inhibitor for the treatment of cancer, diabetes and neurological disorders

Info

Publication number
SG11201907844TA
SG11201907844TA SG11201907844TA SG11201907844TA SG11201907844TA SG 11201907844T A SG11201907844T A SG 11201907844TA SG 11201907844T A SG11201907844T A SG 11201907844TA SG 11201907844T A SG11201907844T A SG 11201907844TA SG 11201907844T A SG11201907844T A SG 11201907844TA
Authority
SG
Singapore
Prior art keywords
international
benzylidine
diabetes
treatment
proteasome
Prior art date
Application number
SG11201907844TA
Inventor
Yung-Nien Chang
Original Assignee
Up Therapeutics 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 Up Therapeutics Inc filed Critical Up Therapeutics Inc
Publication of SG11201907844TA publication Critical patent/SG11201907844TA/en

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Classifications

    • 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
    • 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
    • A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • 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
    • A61K31/40—Heterocyclic 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
    • 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
    • A61K31/40—Heterocyclic 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
    • A61K31/403—Heterocyclic 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 carbocyclic rings, e.g. carbazole
    • 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
    • A61K31/438—The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
    • 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
    • A61K31/439—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 the ring forming part of a bridged ring system, e.g. quinuclidine
    • 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
    • A61K31/45—Non condensed piperidines, e.g. piperocaine having oxo groups directly attached to the heterocyclic ring, e.g. cycloheximide
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/12—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/54—Spiro-condensed
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/20—Spiro-condensed ring systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 02 August 2018 (02.08.2018) WIP0 I PCT ill 1111u°111110111sOHolo olomoiloimonlmo oimIE (10) International Publication Number WO 2018/140907 Al (51) International Patent Classification: A61K 31/439 (2006.01) CO7D 211/74 (2006.01) A61K 31/45 (2006.01) (21) International Application Number: PCT/US2018/015826 (22) International Filing Date: 30 January 2018 (30.01.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/451,920 30 January 2017 (30.01.2017) US (71) Applicant: UP THERAPEUTICS INC. [US/US]; 6811 Old Waterloo Road, Suite 916, Elkridge, MD 21075 (US). (72) Inventor: CHANG, Yung-Nien; c/o Up Therapeutics Inc., 6811 Old Waterloo Road, Suite 916, Elkridge, MD 21075 (US). (74) Agent: MCGOWAN, Malcolm K. et al.; Cermak Naka- jima & McGowan LLP, 127 S. Peyton Street, Suite 200, Alexandria, VA 22314 (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, JO, 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). Published: 11 with international search report (Art. 21(3)) N CZ CZ 1-1 (54) Title: NOVEL SPIRO AND CYCLIC BIS-BENZYLIDINE PROTEASOME INHIBITOR FOR THE TREATMENT OF CAN- CER, DIABETES AND NEUROLOGICAL DISORDERS 1-1 0 (57) : Described herein are spiro and cyclic bis-benzylidine proteasome inhibitors, which inhibit the proteasome function \" through either ubiquitin receptor ADRM1/RPN13 or proteasome DUB enzymes (USP14, UCH37 and RPN11), and which can be used 0 for the treatment of cancers/diabetes/neurological disorders.
SG11201907844TA 2017-01-30 2018-01-30 Novel spiro and cyclic bis-benzylidine proteasome inhibitor for the treatment of cancer, diabetes and neurological disorders SG11201907844TA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201762451920P 2017-01-30 2017-01-30
PCT/US2018/015826 WO2018140907A1 (en) 2017-01-30 2018-01-30 Novel spiro and cyclic bis-benzylidine proteasome inhibitor for the treatment of cancer, diabetes and neurological disorders

Publications (1)

Publication Number Publication Date
SG11201907844TA true SG11201907844TA (en) 2019-09-27

Family

ID=62979028

Family Applications (1)

Application Number Title Priority Date Filing Date
SG11201907844TA SG11201907844TA (en) 2017-01-30 2018-01-30 Novel spiro and cyclic bis-benzylidine proteasome inhibitor for the treatment of cancer, diabetes and neurological disorders

Country Status (9)

Country Link
US (1) US10947199B2 (en)
EP (1) EP3573616A4 (en)
JP (2) JP2020506230A (en)
KR (1) KR102636859B1 (en)
CN (1) CN110831595A (en)
AU (1) AU2018212994B2 (en)
CA (1) CA3061703A1 (en)
SG (1) SG11201907844TA (en)
WO (1) WO2018140907A1 (en)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2021030867A1 (en) * 2019-08-19 2021-02-25 Baker Heart and Diabetes Institute Method of modulating adiposity
WO2021072212A1 (en) * 2019-10-11 2021-04-15 Mayo Foundation For Medical Education And Research Proteasome inhibitors
EP4153173A4 (en) * 2020-05-18 2024-06-26 Univ Johns Hopkins Anti-cancer spirocyclic-guanidine compounds and uses thereof
KR102576102B1 (en) * 2021-10-22 2023-09-11 한국생명공학연구원 Probe for detecting uch37 and uses thereof

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2632786T3 (en) * 2011-09-16 2017-09-15 Vivolux Ab Proteasome desubiquitination inhibitor test
US20130079370A1 (en) * 2011-09-23 2013-03-28 Vivolux Ab Method for the Inhibition of Deubiquitinating Activity
DK2780326T3 (en) * 2011-10-19 2019-03-04 Vivolux Ab PROCEDURE FOR INHIBITING DEUBIQUITINATION ACTIVITY
WO2014182744A1 (en) * 2013-05-08 2014-11-13 The Johns Hopkins University Novel bis-benzylidine piperidone proteasome inhibitor with anticancer activity
CN106674112A (en) * 2016-12-15 2017-05-17 苏州汉德创宏生化科技有限公司 Synthetic methods of 7-azaspiro[3,5]-nonane-2-ol and hydrochloride compound thereof

Also Published As

Publication number Publication date
EP3573616A4 (en) 2021-02-17
WO2018140907A1 (en) 2018-08-02
CA3061703A1 (en) 2018-08-02
CN110831595A (en) 2020-02-21
KR20190123270A (en) 2019-10-31
KR102636859B1 (en) 2024-02-14
AU2018212994A1 (en) 2019-09-19
JP2023033425A (en) 2023-03-10
EP3573616A1 (en) 2019-12-04
US20190365726A1 (en) 2019-12-05
AU2018212994B2 (en) 2022-03-24
US10947199B2 (en) 2021-03-16
JP2020506230A (en) 2020-02-27

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SG11201907844TA (en) Novel spiro and cyclic bis-benzylidine proteasome inhibitor for the treatment of cancer, diabetes and neurological disorders