SG11201903209TA - Structures and mechanism for the design of highly potent glucocorticoids - Google Patents

Structures and mechanism for the design of highly potent glucocorticoids

Info

Publication number
SG11201903209TA
SG11201903209TA SG11201903209TA SG11201903209TA SG11201903209TA SG 11201903209T A SG11201903209T A SG 11201903209TA SG 11201903209T A SG11201903209T A SG 11201903209TA SG 11201903209T A SG11201903209T A SG 11201903209TA SG 11201903209T A SG11201903209T A SG 11201903209TA
Authority
SG
Singapore
Prior art keywords
ova
international
compounds
pct
grand rapids
Prior art date
Application number
SG11201903209TA
Inventor
Huaqiang Xu
Yuanzheng He
Original Assignee
Van Andel Res Institute
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 Van Andel Res Institute filed Critical Van Andel Res Institute
Publication of SG11201903209TA publication Critical patent/SG11201903209TA/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0036—Nitrogen-containing hetero ring
    • C07J71/0042—Nitrogen only
    • C07J71/0047—Nitrogen only at position 2(3)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
    • A61P5/44—Glucocorticosteroids; Drugs increasing or potentiating the activity of glucocorticosteroids
    • 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
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • 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
    • A61P17/10—Anti-acne agents

Abstract

INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property MD HIM 0 11101 010 11111 01 110 1 0 011101M 010 11111 HUHU° ill 011 Organization International Bureau (10) International Publication Number (43) International Publication Date .....0\"\" WO 2018/071736 Al 19 April 2018 (19.04.2018) WIP0 1 PCT (51) International Patent Classification: OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, A61M 37/00 (2006.01) A61P 37/06 (2006.01) SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, A61K 35/16 (2015.01) TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (21) International Application Number: (84) Designated States (unless otherwise indicated, for every PCT/US2017/056447 kind of regional protection available): ARIPO (BW, GH, (22) International Filing Date: GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, 13 October 2017 (13.10.2017) UG, TM), ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, (25) Filing Language: English EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, (26) Publication Language: English 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, (30) Priority Data: KM, ML, MR, NE, SN, TD, TG). 62/408,314 14 October 2016 (14.10.2016) US Published: (71) Applicant: VAN ANDEL RESEARCH INSTITUTE — [US/US]; 333 Bostwick Avenue NE, Grand Rapids, MI with international search report (Art. 21(3)) 49503 (US). — with amended claims (Art. 19(1)) (72) Inventors: XU, Huanqiang, Eric; 7145 Mooring Heights Court, S.E., Grand Rapids, MI 49546 (US). HE, Yuanzheng; 5337 Burton Court, S.E., Grand Rapids, MI 49525 (US). — = (74) Agent: SIEGEL, Douglas, H.; Honigman Miller Schwartz And Cohn LLP, 350 E. Michigan Ave., Suite 300, Kalama- = zoo, MI 49007 (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, = = _ (54) Title: STRUCTURES AND MECHANISM FOR THE DESIGN OF HIGHLY POTENT GLUCOCORTICOIDS — = = = 50 = P.Ill Saline — = ••••••••••OVA + DIVISO 46 ...111...OVA. cat.e4(0,62125m6606 — ...op...OVA + cam • (0.125mctikg) a ...411..OVA +care 4 (0.0625M914) \" • klY , • OVA 1-e:ram .• (0,615625n-4CM = ....OVA -1. FF 6,,,125tagikgt # 3 ..411....OVA +CM.> 4 (0.03125m~ ,....... OVA. FF (0,0625thvy46 e 1:4 20 • •At • OVA ../API, P. 00.7215625mg( kg) P.m...OVA + FF (0.125rng(kg) „ , t ....o. OVA + FF — (0.0625Ingl614—____1 ' 4 ....e I 10 ....o.' .. .....;111 0 a , . El 0.25 0,5 N 2 4 L 0 0.55 0.5 1 2 4 M Acetylcholine IN. (taci)tt SW) IN 11 IN 00 Figure 15 1-1 0 \" (57) : The present invention relates to novel glucocorticoid compounds. The invention also relates to methods of using these compounds, the synthesis of these compounds, and to compositions and formulations comprising the glucocorticoid compounds, and 0 uses thereof. P''
SG11201903209TA 2016-10-14 2017-10-13 Structures and mechanism for the design of highly potent glucocorticoids SG11201903209TA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201662408314P 2016-10-14 2016-10-14
PCT/US2017/056447 WO2018071736A1 (en) 2016-10-14 2017-10-13 Structures and mechanism for the design of highly potent glucocorticoids

Publications (1)

Publication Number Publication Date
SG11201903209TA true SG11201903209TA (en) 2019-05-30

Family

ID=61906432

Family Applications (1)

Application Number Title Priority Date Filing Date
SG11201903209TA SG11201903209TA (en) 2016-10-14 2017-10-13 Structures and mechanism for the design of highly potent glucocorticoids

Country Status (12)

Country Link
US (1) US10954265B2 (en)
EP (1) EP3525870B1 (en)
JP (2) JP7146750B2 (en)
KR (1) KR102497070B1 (en)
CN (1) CN110382033B (en)
ES (1) ES2945983T3 (en)
MA (1) MA46539A (en)
PH (1) PH12019500801A1 (en)
RU (1) RU2019111101A (en)
SG (1) SG11201903209TA (en)
WO (1) WO2018071736A1 (en)
ZA (1) ZA201902595B (en)

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK66202C (en) 1945-03-03 1948-01-12 Danske Securitas As Code switch for electrical alarm systems.
DK71662C (en) 1946-09-05 1950-11-06 Ingenioer Frank Broadbent Drying centrifuge.
US4049813A (en) 1976-07-15 1977-09-20 Sandoz, Inc. Substituted isoxazolo pyridinones
US5837698A (en) * 1996-05-02 1998-11-17 G. D. Searle & Co. Steroid nitrite and nitrate ester derivatives useful as anti-inflammatory drugs
WO2002102807A1 (en) 2001-06-14 2002-12-27 Banyu Pharmaceutical Co., Ltd. Novel isoxazolopyridone derivatives and use thereof
GB0119911D0 (en) 2001-08-15 2001-10-10 Novartis Ag Organic Compounds
BRPI0416591A (en) * 2003-11-13 2007-01-30 Combinatorx Inc methods and reagents for the treatment of inflammatory disorders
CN101300265A (en) * 2005-09-02 2008-11-05 尼科克斯公司 Nitrooxy derivatives of glucocorticoids
CN1813768A (en) * 2005-11-18 2006-08-09 成都力思特制药股份有限公司 Medicinal composition for treating respiratory system disease and its pharmaceutical use
KR20100087147A (en) 2007-10-04 2010-08-03 아스트라제네카 아베 Steroidal [3,2-c]pyrazole compounds, with glucocorticoid activity
EP2235037A1 (en) * 2007-12-20 2010-10-06 AstraZeneca AB Steroid derivatives acting as glucocorticosteroid receptor agonists
WO2010083218A1 (en) 2009-01-13 2010-07-22 Van Andel Research Institute Methods of using substituted isoxazolo pyridinones as dissociated glucocorticoids
UY32520A (en) 2009-04-03 2010-10-29 Astrazeneca Ab COMPOUNDS THAT HAVE AGONIST ACTIVITY OF THE GLUCOCORTICOESTEROID RECEPTOR
UY32523A (en) * 2009-04-03 2010-10-29 Astrazeneca Ab COMPOUNDS THAT HAVE AGONISTIC ACTIVITY OF THE GLUCOCORTICOSTEROID RECEPTOR
UY32525A (en) * 2009-04-03 2010-10-29 Astrazeneca Ab COMPOUNDS THAT HAVE AGONISTIC ACTIVITY OF THE GLUCOCORTICOSTEROID RECEPTOR
CA2764830A1 (en) * 2009-06-16 2010-12-23 Schering Corporation Novel [3,2-c] heteroaryl steroids as glucocorticoid receptor agonists, compositions and uses thereof
ES2751457T3 (en) 2013-09-25 2020-03-31 Van Andel Res Institute Highly potent glucocorticoids
TWI695831B (en) * 2014-09-13 2020-06-11 香港商南北兄弟藥業投資有限公司 Compounds as crth2 antagonist and uses thereof

Also Published As

Publication number Publication date
US10954265B2 (en) 2021-03-23
KR20190068577A (en) 2019-06-18
EP3525870B1 (en) 2023-05-10
JP2019532071A (en) 2019-11-07
US20190263853A1 (en) 2019-08-29
JP2022132464A (en) 2022-09-08
MA46539A (en) 2019-08-21
PH12019500801A1 (en) 2019-11-11
RU2019111101A3 (en) 2020-11-27
CN110382033A (en) 2019-10-25
WO2018071736A1 (en) 2018-04-19
CN110382033B (en) 2022-04-15
RU2019111101A (en) 2020-11-16
KR102497070B1 (en) 2023-02-06
ZA201902595B (en) 2021-04-28
EP3525870A1 (en) 2019-08-21
WO2018071736A9 (en) 2019-05-23
JP7146750B2 (en) 2022-10-04
ES2945983T3 (en) 2023-07-11
EP3525870A4 (en) 2020-04-29

Similar Documents

Publication Publication Date Title
SG11201809344QA (en) Process for synthesizing 2-hydroxy-6-((2-(1-isopropyl-1h-pyrazol-5-yl)-pyridin-3-yl)methoxy)benzaldehyde
SG11201807784SA (en) 3-desoxy derivative and pharmaceutical compositions thereof
SG11201810280YA (en) Spiro-lactam nmda receptor modulators and uses thereof
SG11201906883SA (en) Methods for the administration of certain vmat2 inhibitors
SG11201909963YA (en) Methods for treating dravet syndrome
SG11201810420YA (en) Antibodies to alpha-synuclein and uses thereof
SG11201408261UA (en) Syringe
SG11201909155VA (en) Ask1 inhibitor compounds and uses thereof
SG11201909960UA (en) Methods for improving memory and cognition and for treating memory and cognitive disorders
SG11201809499UA (en) Processes for preparing phosphorodiamidate morpholino oligomers
SG11201811442UA (en) Formulation of a peptide vaccine
SG11201900554YA (en) Spiro-lactam nmda modulators and methods of using same
SG11201900558RA (en) Spiro-lactam nmda receptor modulators and uses thereof
SG11201900551WA (en) Spiro-lactam nmda receptor modulators and uses thereof
SG11201900546UA (en) Spiro-lactam and bis-spiro-lactam nmda receptor modulators and uses thereof
SG11201407837WA (en) Beta-hairpin peptidomimetics
SG11201901558VA (en) Pth compounds with low peak-to-trough ratios
SG11201807593TA (en) Compositions and methods to program therapeutic cells using targeted nucleic acid nanocarriers
SG11201906436VA (en) Novel heterocyclic compound, its preparation method, and pharmaceutical composition comprising the same
SG11201811559WA (en) Cancer treatment combinations
SG11201408617PA (en) Bifluorodioxalane-amino-benzimidazole kinase inhibitors for the treatment of cancer, autoimmuneinflammation and cns disorders
SG11201805001UA (en) Method of treating influenza a
SG11201907356SA (en) Piperidine-substituted mnk inhibitors and methods related thereto
SG11201900633XA (en) Piperidine cxcr7 receptor modulators
SG11201901048VA (en) Pharmaceutical compositions and uses directed to lysosomal storage disorders