MX2018007143A - Formas de sales y polimorfos de (r)-1-(4-(6-(2-(4-(3,3-difluorocic lobutoxi)-6-metilpiridin-2-il)acetamido)piridazin-3-il)-2-fluorob util)-n-metil-1h-1,2,3-triazol-4-carboxamida. - Google Patents

Formas de sales y polimorfos de (r)-1-(4-(6-(2-(4-(3,3-difluorocic lobutoxi)-6-metilpiridin-2-il)acetamido)piridazin-3-il)-2-fluorob util)-n-metil-1h-1,2,3-triazol-4-carboxamida.

Info

Publication number
MX2018007143A
MX2018007143A MX2018007143A MX2018007143A MX2018007143A MX 2018007143 A MX2018007143 A MX 2018007143A MX 2018007143 A MX2018007143 A MX 2018007143A MX 2018007143 A MX2018007143 A MX 2018007143A MX 2018007143 A MX2018007143 A MX 2018007143A
Authority
MX
Mexico
Prior art keywords
pyridazin
methylpyridin
polymorphs
acetamido
carboxamide
Prior art date
Application number
MX2018007143A
Other languages
English (en)
Inventor
Le Kang
Jones Philip
J Soth Michael
b burke Jason
Liu Gang
Original Assignee
Univ Texas
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 Univ Texas filed Critical Univ Texas
Publication of MX2018007143A publication Critical patent/MX2018007143A/es

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
    • A61K31/495—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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Abstract

En el presente documento se da a conocer el compuesto (R)-1-(4-(6-(2-(4-(3,3-difluorociclobutoxi)-6-metilpiridin-2-il)a cetamido)piridazin-3-il)-2-fluorobutil)-N-metil-1H-1,2,3-triazol- 4-carboxamida, y formas de sales y polimorfos del mismo, que demuestran una exposición mejorada después de la dosificación oral. También se proporcionan métodos de inhibición de la actividad de GLS1 en un sujeto humano o animal.
MX2018007143A 2015-12-22 2016-12-21 Formas de sales y polimorfos de (r)-1-(4-(6-(2-(4-(3,3-difluorocic lobutoxi)-6-metilpiridin-2-il)acetamido)piridazin-3-il)-2-fluorob util)-n-metil-1h-1,2,3-triazol-4-carboxamida. MX2018007143A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201562271018P 2015-12-22 2015-12-22
PCT/US2016/068149 WO2017112831A1 (en) 2015-12-22 2016-12-21 Salt forms and polymorphs of (r)-1-(4-(6-(2-(4-(3,3-difluorocyclobutoxy)-6-methylpyridin-2-yl) acetamido) pyridazin-3-yl)-2-fluorobutyl)-n-methyl-1h-1,2,3-triazole-4-carboxamide

Publications (1)

Publication Number Publication Date
MX2018007143A true MX2018007143A (es) 2018-11-29

Family

ID=59065954

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2018007143A MX2018007143A (es) 2015-12-22 2016-12-21 Formas de sales y polimorfos de (r)-1-(4-(6-(2-(4-(3,3-difluorocic lobutoxi)-6-metilpiridin-2-il)acetamido)piridazin-3-il)-2-fluorob util)-n-metil-1h-1,2,3-triazol-4-carboxamida.

Country Status (14)

Country Link
US (4) US10150753B2 (es)
EP (1) EP3394039A4 (es)
JP (1) JP6976248B2 (es)
KR (1) KR20180095677A (es)
CN (1) CN108602782B (es)
AU (1) AU2016378746B2 (es)
BR (1) BR112018012660B1 (es)
CA (1) CA3009355A1 (es)
IL (1) IL260178B2 (es)
MX (1) MX2018007143A (es)
RU (1) RU2018124266A (es)
SG (1) SG11201804664XA (es)
WO (1) WO2017112831A1 (es)
ZA (1) ZA201804843B (es)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR112016030730B1 (pt) 2014-07-03 2023-05-02 Board Of Regents, The University Of Texas System Composto
US10125128B2 (en) 2015-06-30 2018-11-13 Board Of Regents, The University Of Texas System GLS1 inhibitors for treating disease
AU2016378746B2 (en) 2015-12-22 2021-05-20 Board Of Regents, The University Of Texas System Salt forms and polymorphs of (R)-1-(4-(6-(2-(4-(3,3-difluorocyclobutoxy)-6-methylpyridin-2-yl) acetamido) pyridazin-3-yl)-2-fluorobutyl)-N-methyl-1H-1,2,3-triazole-4-carboxamide
EP3697764A4 (en) 2017-10-18 2021-07-21 Board Of Regents, The University Of Texas System GLUTAMINASE INHIBITOR THERAPY
CN116023375A (zh) * 2021-10-25 2023-04-28 成都苑东生物制药股份有限公司 一种杂环类衍生物、其制备方法及用途

Family Cites Families (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES498337A0 (es) 1980-01-07 1982-06-01 Nyegaard & Co As Un procedimiento para la preparacion de 5-halo-pirimidin-2- onas
EP0218753B1 (en) 1985-10-10 1989-08-09 Agfa-Gevaert N.V. Image-recieving element for the silver salt diffusion transfer reversal process
AU6979091A (en) 1989-12-22 1991-07-24 Upjohn Company, The Pyridinones useful as antiatherosclerotic agents
IL118325A0 (en) 1995-05-25 1996-10-31 Pont Merck And Pharmaceutical Integrin receptor antagonists and pharmaceutical compositions containing them
JP4422796B2 (ja) 1995-07-21 2010-02-24 タクティカル セラピューティクス インコーポレイテッド アミノイミダゾールカルボキサミドおよび５−アミノ、または置換アミノ１，２，３−トリアゾールの塩による癌の治療および阻止
WO1998043962A1 (en) 1997-03-28 1998-10-08 Du Pont Pharmaceuticals Company Heterocyclic integrin inhibitor prodrugs
JP2001524481A (ja) 1997-11-26 2001-12-04 デュポン ファーマシューティカルズ カンパニー αＶβ３アンタゴニストとしての１，３，４−チアジアゾール類および１，３，４−オキサジアゾール類
US6451828B1 (en) 2000-08-10 2002-09-17 Elan Pharmaceuticals, Inc. Selective inhibition of glutaminase by bis-thiadiazoles
SE0400208D0 (sv) 2004-02-02 2004-02-02 Astrazeneca Ab Chemical compounds
US7985548B2 (en) 2006-03-03 2011-07-26 The United States Of America As Represented By The Department Of Health And Human Services Materials and methods directed to asparagine synthetase and asparaginase therapies
US7638541B2 (en) 2006-12-28 2009-12-29 Metabolex Inc. 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine
US20100255117A1 (en) 2007-04-06 2010-10-07 The Johns Hopkins University Methods and compositions for the treatment of cancer
PT2247592E (pt) 2008-02-25 2011-11-03 Hoffmann La Roche Inibidores de pirrolpirazina-cinase
DK2300013T3 (en) 2008-05-21 2017-12-04 Ariad Pharma Inc PHOSPHORUS DERIVATIVES AS KINASE INHIBITORS
JP2011231015A (ja) 2008-08-29 2011-11-17 Taiho Yakuhin Kogyo Kk 含窒素複素環を有する新規ウラシル化合物又はその塩
NZ595280A (en) 2009-02-27 2013-11-29 Enanta Pharm Inc Hepatitis c virus inhibitors
US10532034B2 (en) 2009-03-25 2020-01-14 Cornell University Inhibition of glutaminase C
WO2011089995A1 (ja) 2010-01-21 2011-07-28 公立大学法人名古屋市立大学 ヒドロキサム酸誘導体及びそれを用いたｈｄａｃ８阻害剤
US20130109643A1 (en) 2010-05-10 2013-05-02 The Johns Hopkins University Metabolic inhibitor against tumors having an idh mutation
EP2782570B1 (en) 2011-11-21 2019-09-18 Calithera Biosciences Inc. Heterocyclic inhibitors of glutaminase
US8604016B2 (en) 2011-11-21 2013-12-10 Calithera Biosciences Inc. Heterocyclic inhibitors of glutaminase
PT2920168T (pt) 2012-11-16 2021-10-18 Calithera Biosciences Inc Inibidores heterocíclicos de glutaminase
WO2014081925A1 (en) 2012-11-21 2014-05-30 Agios Pharmaceuticals, Inc. Glutamase inhibitors and method of use
WO2014079011A1 (en) 2012-11-22 2014-05-30 Agios Pharmaceuticals, Inc. Heterocyclic compounds for inhibiting glutaminase and their methods of use
US9029531B2 (en) 2012-11-22 2015-05-12 Agios Pharmaceuticals, Inc. Compounds and their methods of use
KR20150091389A (ko) * 2012-12-03 2015-08-10 칼리테라 바이오사이언시즈 인코포레이티드 글루타미나제의 헤테로사이클릭 억제제에 의한 암 치료
EP2952096B1 (en) 2013-01-30 2018-04-04 Sumitomo Chemical Company, Limited Amide compound, an arthropod pest control agent and a method for controlling arthropod pest
TW201500356A (zh) 2013-04-12 2015-01-01 Lilly Co Eli 二氫吡啶并嘧啶化合物
EP3092236B1 (en) * 2014-01-06 2020-08-26 Rhizen Pharmaceuticals S.A. Novel glutaminase inhibitors
US20160058759A1 (en) 2014-07-03 2016-03-03 Board Of Regents, The University Of Texas System Glutaminase inhibitor therapy
US20160002248A1 (en) 2014-07-03 2016-01-07 Board Of Regents, The University Of Texas System Gls1 inhibitors for treating disease
WO2016004418A1 (en) 2014-07-03 2016-01-07 Board Of Regents, University Of Texas System Glutaminase inhibitor therapy
WO2016004417A1 (en) 2014-07-03 2016-01-07 Board Of Regents, University Of Texas System Gls1 inhibitors for treating disease
BR112016030730B1 (pt) 2014-07-03 2023-05-02 Board Of Regents, The University Of Texas System Composto
US10125128B2 (en) 2015-06-30 2018-11-13 Board Of Regents, The University Of Texas System GLS1 inhibitors for treating disease
AU2016378746B2 (en) 2015-12-22 2021-05-20 Board Of Regents, The University Of Texas System Salt forms and polymorphs of (R)-1-(4-(6-(2-(4-(3,3-difluorocyclobutoxy)-6-methylpyridin-2-yl) acetamido) pyridazin-3-yl)-2-fluorobutyl)-N-methyl-1H-1,2,3-triazole-4-carboxamide
EP3697764A4 (en) 2017-10-18 2021-07-21 Board Of Regents, The University Of Texas System GLUTAMINASE INHIBITOR THERAPY

Also Published As

Publication number Publication date
RU2018124266A (ru) 2020-01-23
US20210206745A1 (en) 2021-07-08
JP2019502663A (ja) 2019-01-31
IL260178B2 (en) 2023-05-01
WO2017112831A1 (en) 2017-06-29
US20190144425A1 (en) 2019-05-16
CN108602782B (zh) 2022-06-17
US10150753B2 (en) 2018-12-11
CN108602782A (zh) 2018-09-28
US20170174661A1 (en) 2017-06-22
BR112018012660B1 (pt) 2023-12-19
EP3394039A4 (en) 2019-06-12
EP3394039A1 (en) 2018-10-31
JP6976248B2 (ja) 2021-12-08
ZA201804843B (en) 2019-09-25
AU2016378746A1 (en) 2018-06-28
RU2018124266A3 (es) 2020-03-25
IL260178B1 (en) 2023-01-01
US11603365B2 (en) 2023-03-14
BR112018012660A2 (pt) 2018-12-04
AU2016378746B2 (en) 2021-05-20
SG11201804664XA (en) 2018-07-30
US10899740B2 (en) 2021-01-26
KR20180095677A (ko) 2018-08-27
CA3009355A1 (en) 2017-06-29
IL260178A (en) 2018-07-31
US20230250081A1 (en) 2023-08-10

Similar Documents

Publication Publication Date Title
MX2018007143A (es) Formas de sales y polimorfos de (r)-1-(4-(6-(2-(4-(3,3-difluorocic lobutoxi)-6-metilpiridin-2-il)acetamido)piridazin-3-il)-2-fluorob util)-n-metil-1h-1,2,3-triazol-4-carboxamida.
CL2017001566A1 (es) Derivados de azabiciclootano como agonistas de fxr para el uso en el tratamiento de enfermedades hepáticas y gastrointestinales.
CY1120941T1 (el) Παραγωγα φαινυλοτριαζολιου υποκατεστημενα με υδροξυαλκυλιο και χρησεις αυτων
MX2019002212A (es) Compuestos de amino-pirrolo-pirimidinona y metodos de uso de los mismos.
MX2018013983A (es) Inhibidores g12c de kras.
SG11202001062XA (en) Compounds, salts thereof and methods for treatment of diseases
IL246875A0 (en) 2-amino-3,5,5-trifluoro-3,4,5,6-tetrahydropyridines as bace1 inhibitors for the treatment of Alzheimer's disease
MX2017003664A (es) Indazoles sustituidos con benzilo como inhibidores de bub1.
TR201904658T4 (tr) Bisiklik füzyonla birleştirilmiş heteroaril veya aril bileşikleri ve bunların ırak4 inhibitörleri olarak kullanımları.
CY1123216T1 (el) Αναστολεις της gls1 για την αντιμετωπιση νοσων
ZA201904522B (en) Heterocyclic inhibitors of mct4
MX2018011813A (es) Medicina obtenida mediante la combinacion de agonista fxr y arb.
TW201625535A (en) Inhibitors of histone demethylases
TR201909353T4 (tr) Multipl skleroz tedavisi.
MX2021005891A (es) Sondas para la proyeccion de imagen de la proteina huntingtina.
CL2021000044A1 (es) Composiciones que comprenden 2-((1-(2(4-fluorofenil)-2-oxoetil) piperidin-4-il)metil)isoindolin-1-ona para tratar la esquizofrenia (divisional solicitud no. 1376-2017)
EA201600508A1 (ru) Гербицидная смесь, содержащая имазетапир и циклоксидим
PL3207928T3 (pl) Preparat złożony, zawierający nową pochodną kwasu 3-(4-(benzyloksy)fenylo)heks-4-ynowego oraz inny składnik czynny, przeznaczony do zapobiegania lub leczenia chorób metabolicznych
MX2017002702A (es) Sondas para la proyección de imagen de la proteína huntingtina.
MX2018002338A (es) Sondas para formar imagenes de proteina de huntingtina.
DK4000662T3 (da) Kunstigt lungesystem og anvendelsesfremgangsmåder, der ikke udføres på den levende menneske- eller dyrekrop
IL273974A (en) Amine-Disubstituted Heterocyclic Compounds as EHMT2 Inhibitors, Their Salts, and Method for Their Synthesis
PH12017502069A1 (en) Method for treating coffee rust, citrus black spot, citrus scab and banana black sigatoka diseases
SG11202007726RA (en) Pharmaceutical compound, salts thereof, formulations thereof, and methods of making and using same
EA201990313A1 (ru) Производное триазолопиразинона, пригодное в качестве ингибитора фдэ1 человека