EA201990621A1 - Кристаллические формы ингибитора лизилоксидаза-подобного белка 2 и способы получения - Google Patents

Кристаллические формы ингибитора лизилоксидаза-подобного белка 2 и способы получения

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Publication number
EA201990621A1
EA201990621A1 EA201990621A EA201990621A EA201990621A1 EA 201990621 A1 EA201990621 A1 EA 201990621A1 EA 201990621 A EA201990621 A EA 201990621A EA 201990621 A EA201990621 A EA 201990621A EA 201990621 A1 EA201990621 A1 EA 201990621A1
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EA
Eurasian Patent Office
Prior art keywords
methods
inhibitor
loxl2
protein
crystallic
Prior art date
Application number
EA201990621A
Other languages
English (en)
Inventor
Дэвид Лонерган
Кевин Росс Холм
Мартин У. Роуботтом
Original Assignee
Фармакеа, Инк.
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 Фармакеа, Инк. filed Critical Фармакеа, Инк.
Publication of EA201990621A1 publication Critical patent/EA201990621A1/ru

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/63Esters of sulfonic acids
    • C07C309/64Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to acyclic carbon atoms
    • C07C309/65Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to acyclic carbon atoms of a saturated carbon skeleton
    • C07C309/66Methanesulfonates
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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
    • C07D207/10Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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
    • C07D207/12Oxygen or sulfur atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Catalysts (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

В настоящем документе описаны кристаллические формы фармацевтически приемлемых солей ингибитора лизилоксидаза-подобного белка 2 (LOXL2) (3-(4-(аминометил)-6-(трифторметил)пиридин-2-илокси)фенил)((3R,4R)-3-фтор-4-гидроксипирролидин-1-ил)метанона. Также описаны способы получения ингибитора LOXL2, фармацевтические композиции и лекарственные средства, содержащие ингибитор LOXL2, и способы применения ингибитора LOXL2 при лечении состояний, заболеваний или расстройств, связанных с активностью LOXL2.
EA201990621A 2016-09-07 2017-09-06 Кристаллические формы ингибитора лизилоксидаза-подобного белка 2 и способы получения EA201990621A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201662384596P 2016-09-07 2016-09-07
PCT/US2017/050332 WO2018048943A1 (en) 2016-09-07 2017-09-06 Crystalline forms of a lysyl oxidase-like 2 inhibitor and methods of making

Publications (1)

Publication Number Publication Date
EA201990621A1 true EA201990621A1 (ru) 2019-09-30

Family

ID=61561660

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201990621A EA201990621A1 (ru) 2016-09-07 2017-09-06 Кристаллические формы ингибитора лизилоксидаза-подобного белка 2 и способы получения

Country Status (14)

Country Link
US (2) US10774069B2 (ru)
EP (1) EP3510023A4 (ru)
JP (1) JP7079772B2 (ru)
KR (1) KR102587178B1 (ru)
CN (1) CN109983006B (ru)
AU (1) AU2017324445A1 (ru)
BR (1) BR112019004517A2 (ru)
CA (1) CA3036064A1 (ru)
EA (1) EA201990621A1 (ru)
IL (1) IL265192A (ru)
MA (1) MA46204A (ru)
MX (1) MX2019002615A (ru)
SG (1) SG11201901999XA (ru)
WO (1) WO2018048943A1 (ru)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016144702A1 (en) * 2015-03-06 2016-09-15 Pharmakea, Inc. Lysyl oxidase-like 2 inhibitors and uses thereof
SG11201707246YA (en) 2015-03-06 2017-10-30 Pharmakea Inc Fluorinated lysyl oxidase-like 2 inhibitors and uses thereof
EP3414229B1 (en) * 2016-02-09 2021-06-16 Pharmakea, Inc. Quinolinone lysyl oxidase-like 2 inhibitors and uses thereof
KR102587178B1 (ko) 2016-09-07 2023-10-06 파마케아, 인크. 리실 옥시다아제-유사 2 억제제의 결정질 형태 및 제조 방법
EP3509594A4 (en) 2016-09-07 2020-05-06 Pharmakea, Inc. USE OF A LYSYLOXIDASE-LIKE 2 INHIBITOR

Family Cites Families (59)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4229447A (en) 1979-06-04 1980-10-21 American Home Products Corporation Intraoral methods of using benzodiazepines
IE56702B1 (en) 1982-12-01 1991-11-06 Usv Pharma Corp Antiinflammatory antiallergic compounds
US4596795A (en) 1984-04-25 1986-06-24 The United States Of America As Represented By The Secretary, Dept. Of Health & Human Services Administration of sex hormones in the form of hydrophilic cyclodextrin derivatives
US4755386A (en) 1986-01-22 1988-07-05 Schering Corporation Buccal formulation
US5021456A (en) 1988-02-25 1991-06-04 Merrell Dow Pharmaceuticals Inc. Inhibitors of lysyl oxidase
US5739136A (en) 1989-10-17 1998-04-14 Ellinwood, Jr.; Everett H. Intraoral dosing method of administering medicaments
US5563143A (en) 1994-09-21 1996-10-08 Pfizer Inc. Catechol diether compounds as inhibitors of TNF release
US6956047B1 (en) 1995-06-06 2005-10-18 Pfizer Inc. Corticotropin releasing factor antagonists
US7067664B1 (en) 1995-06-06 2006-06-27 Pfizer Inc. Corticotropin releasing factor antagonists
US6632823B1 (en) 1997-12-22 2003-10-14 Merck & Co., Inc. Substituted pyridine compounds useful as modulators of acetylcholine receptors
HUP0204272A3 (en) 2000-01-18 2005-03-29 Pfizer Prod Inc Corticotropin releasing factor antagonists, pharmaceutical compositions containing them and their use
US20030134836A1 (en) 2001-01-12 2003-07-17 Amgen Inc. Substituted arylamine derivatives and methods of use
US20020147198A1 (en) 2001-01-12 2002-10-10 Guoqing Chen Substituted arylamine derivatives and methods of use
US6878714B2 (en) 2001-01-12 2005-04-12 Amgen Inc. Substituted alkylamine derivatives and methods of use
US7102009B2 (en) 2001-01-12 2006-09-05 Amgen Inc. Substituted amine derivatives and methods of use
US7105682B2 (en) 2001-01-12 2006-09-12 Amgen Inc. Substituted amine derivatives and methods of use
US6995162B2 (en) 2001-01-12 2006-02-07 Amgen Inc. Substituted alkylamine derivatives and methods of use
US7307088B2 (en) 2002-07-09 2007-12-11 Amgen Inc. Substituted anthranilic amide derivatives and methods of use
FI20030030A0 (fi) 2003-01-09 2003-01-09 Orion Corp Uusia yhdisteitä
EP1638551B1 (en) 2003-05-19 2011-12-21 Irm Llc Immunosuppressant compounds and compositions
BRPI0507250A (pt) 2004-01-29 2007-06-26 Pfizer Prod Inc combinações para tratar desordens do snc
US7381750B2 (en) 2004-03-12 2008-06-03 Eli Lilly And Company Amino-phenoxymethyl-benzamide opioid receptor antagonists
EP1735268B1 (en) 2004-03-15 2012-02-15 Eli Lilly And Company Opioid receptor antagonists
MXPA06012333A (es) 2004-04-30 2007-01-17 Takeda Pharmaceutical Compuesto de amida heterociclico y uso del mismo como un inhibidor mmp-13.
US7507748B2 (en) 2004-07-22 2009-03-24 Amgen Inc. Substituted aryl-amine derivatives and methods of use
MX2007002842A (es) 2004-09-10 2007-04-30 Pfizer Prod Inc Metodos de tratamiento de trastornos cognitivos que usan derivados azabiciclicos de piridiloximetilo y benzoisoxazol.
JP2008512440A (ja) 2004-09-10 2008-04-24 ファイザー・プロダクツ・インク ジアザビシクロ化合物含有ベンゾイソオキサゾールを用いる気分障害の治療方法
WO2006052546A2 (en) 2004-11-04 2006-05-18 Neurogen Corporation Pyrazolylmethyl heteroaryl derivatives
DE102004056226A1 (de) 2004-11-22 2006-05-24 Burchardt, Elmar Reinhold, Dr.Dr. Neuartige Inhibitoren der Lysyloxidase
CA2593858A1 (en) 2005-01-31 2006-08-10 Min Ge Antidiabetic bicyclic compounds
AR055041A1 (es) 2005-03-23 2007-08-01 Merck Frosst Canada Ltd Tiadiazoles y oxadiazoles como inhibidores de la sintesis de leucotrienos. composiciones farmaceuticas.
EP1915369A4 (en) 2005-08-11 2010-09-08 Merck Frosst Canada Ltd NEW SUBSTITUTED 1,2,3-TRIAZOLYLMETHYLBENZOTHIOPHENE OR ENDOLE AND THEIR USE AS INHIBITORS OF LEUKOTRIENBIOSYNTHESIS
US7405302B2 (en) 2005-10-11 2008-07-29 Amira Pharmaceuticals, Inc. 5-lipoxygenase-activating protein (FLAP) inhibitors
ITMI20051943A1 (it) * 2005-10-14 2007-04-15 Procos Spa Processo di risoluzione anantiomerica di 2-aminometil-pirrolidine 1-sostitute per ammidazione in presenza di lipasi
US20070219206A1 (en) 2005-11-04 2007-09-20 Amira Pharmaceuticals, Inc. 5-lipoxygenase-activating protein (flap) inhibitors
US7977359B2 (en) 2005-11-04 2011-07-12 Amira Pharmaceuticals, Inc. 5-lipdxygenase-activating protein (FLAP) inhibitors
US20070225285A1 (en) 2005-11-04 2007-09-27 Amira Pharmaceuticals, Inc. 5-lipoxygenase-activating protein (flap) inhibitors
JP2009523820A (ja) 2006-01-23 2009-06-25 アミラ ファーマシューティカルス,インコーポレーテッド 5−リポキシゲナーゼの三環系抑制剤
GB0614579D0 (en) 2006-07-21 2006-08-30 Black James Foundation Pyrimidine derivatives
EP2121703A4 (en) 2006-08-18 2011-12-28 Astrazeneca Ab THIENOPYRIMIDIN-4-ON- AND THIENOPYRIDAZIN-7-ONDERIVATES AS MCH-RL ANTAGONISTS
IL184627A0 (en) 2007-07-15 2008-12-29 Technion Res & Dev Foundation Agents for diagnosing and modulating metastasis and fibrosis as well as inflammation in a mammalian tissue
EP2537529B1 (en) 2007-08-02 2018-10-17 Gilead Biologics, Inc. Loxl2 inhibitory antibodies and uses thereof
MX2012001156A (es) 2009-07-28 2012-05-08 Anacor Pharmaceuticals Inc Moleculas que contienen boro trisustituidas.
JP2013502437A (ja) 2009-08-21 2013-01-24 ギリアド バイオロジクス,インク. 治療方法及び組成物
CN103370080A (zh) 2010-02-04 2013-10-23 吉联亚生物科技有限公司 结合赖氨酰氧化酶样2(loxl2)的抗体和其使用方法
CN103002742B (zh) 2010-03-05 2016-07-13 卡尔约药物治疗公司 核转运调节剂及其应用
WO2012068450A1 (en) 2010-11-19 2012-05-24 Incyte Corporation Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
TW201313721A (zh) 2011-08-18 2013-04-01 Incyte Corp 作為jak抑制劑之環己基氮雜環丁烷衍生物
AU2012325909B2 (en) 2011-10-20 2016-06-09 Glaxosmithkline Llc Substituted bicyclic aza-heterocycles and analogues as sirtuin modulators
RU2632899C2 (ru) 2012-04-25 2017-10-11 Раквалиа Фарма Инк. Амидопроизводные как блокаторы ttx-s
US20140120102A1 (en) * 2012-10-30 2014-05-01 Gilead Sciences, Inc. Therapeutic and diagnostic methods related to lysyl oxidase-like 2 (loxl2)
CN104854086B (zh) 2012-12-18 2017-06-27 Ea制药株式会社 杂环酰胺衍生物和含有其的药物
WO2016020732A1 (en) 2014-08-05 2016-02-11 The University Of British Columbia Modulators of caspase-6
US9051320B1 (en) 2014-08-18 2015-06-09 Pharmakea, Inc. Methods for the treatment of metabolic disorders by a selective small molecule autotaxin inhibitor
SG11201706451TA (en) 2015-02-15 2017-09-28 Hoffmann La Roche 1-(het)arylsulfonyl-(pyrrolidine or piperidine)-2-carboxamide derivatives and their use as trpa1 antagonists
WO2016144702A1 (en) 2015-03-06 2016-09-15 Pharmakea, Inc. Lysyl oxidase-like 2 inhibitors and uses thereof
SG11201707246YA (en) * 2015-03-06 2017-10-30 Pharmakea Inc Fluorinated lysyl oxidase-like 2 inhibitors and uses thereof
EP3509594A4 (en) 2016-09-07 2020-05-06 Pharmakea, Inc. USE OF A LYSYLOXIDASE-LIKE 2 INHIBITOR
KR102587178B1 (ko) 2016-09-07 2023-10-06 파마케아, 인크. 리실 옥시다아제-유사 2 억제제의 결정질 형태 및 제조 방법

Also Published As

Publication number Publication date
BR112019004517A2 (pt) 2019-08-13
EP3510023A1 (en) 2019-07-17
AU2017324445A1 (en) 2019-04-11
KR102587178B1 (ko) 2023-10-06
US20190202805A1 (en) 2019-07-04
CA3036064A1 (en) 2018-03-15
MA46204A (fr) 2021-03-17
EP3510023A4 (en) 2020-03-18
SG11201901999XA (en) 2019-04-29
IL265192A (en) 2019-05-30
CN109983006B (zh) 2022-02-25
US10774069B2 (en) 2020-09-15
JP2019532919A (ja) 2019-11-14
WO2018048943A1 (en) 2018-03-15
CN109983006A (zh) 2019-07-05
JP7079772B2 (ja) 2022-06-02
KR20190052040A (ko) 2019-05-15
US20200361901A1 (en) 2020-11-19
MX2019002615A (es) 2019-10-15
US11459309B2 (en) 2022-10-04

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