KR102587178B1 - 리실 옥시다아제-유사 2 억제제의 결정질 형태 및 제조 방법 - Google Patents

리실 옥시다아제-유사 2 억제제의 결정질 형태 및 제조 방법 Download PDF

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KR102587178B1
KR102587178B1 KR1020197009870A KR20197009870A KR102587178B1 KR 102587178 B1 KR102587178 B1 KR 102587178B1 KR 1020197009870 A KR1020197009870 A KR 1020197009870A KR 20197009870 A KR20197009870 A KR 20197009870A KR 102587178 B1 KR102587178 B1 KR 102587178B1
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KR20190052040A (ko
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데이비드 로너간
케빈 로스 홀름
마틴 더블유. 로버텀
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파마케아, 인크.
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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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Catalysts (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
KR1020197009870A 2016-09-07 2017-09-06 리실 옥시다아제-유사 2 억제제의 결정질 형태 및 제조 방법 Active KR102587178B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662384596P 2016-09-07 2016-09-07
US62/384,596 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

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KR20190052040A KR20190052040A (ko) 2019-05-15
KR102587178B1 true KR102587178B1 (ko) 2023-10-06

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US (2) US10774069B2 (enExample)
EP (1) EP3510023B1 (enExample)
JP (1) JP7079772B2 (enExample)
KR (1) KR102587178B1 (enExample)
CN (1) CN109983006B (enExample)
AU (1) AU2017324445A1 (enExample)
BR (1) BR112019004517A2 (enExample)
CA (1) CA3036064A1 (enExample)
EA (1) EA201990621A1 (enExample)
IL (1) IL265192A (enExample)
MA (1) MA46204A (enExample)
MX (1) MX390964B (enExample)
SG (1) SG11201901999XA (enExample)
WO (1) WO2018048943A1 (enExample)

Families Citing this family (7)

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Publication number Priority date Publication date Assignee Title
EP3795568A1 (en) 2015-03-06 2021-03-24 Pharmakea, Inc. Fluorinated lysyl oxidase-like 2 inhibitors and uses thereof
JP6800872B2 (ja) * 2015-03-06 2020-12-16 ファーマケア,インク. リシルオキシダーゼ様2阻害剤とその使用
CA3013917A1 (en) 2016-02-09 2017-08-17 Pharmakea, Inc. Quinolinone lysyl oxidase-like 2 inhibitors and uses thereof
JP7097874B2 (ja) 2016-09-07 2022-07-08 ファーマケア,インク. リシルオキシダーゼ様2阻害剤の使用
AU2017324445A1 (en) 2016-09-07 2019-04-11 Pharmakea, Inc. Crystalline forms of a lysyl oxidase-like 2 inhibitor and methods of making
GB201716871D0 (en) 2017-10-13 2017-11-29 Inst Of Cancer Research: Royal Cancer Hospital Compounds
CN114487139B (zh) * 2020-10-27 2025-01-14 鲁南制药集团股份有限公司 一种盐酸西替利嗪有关物质的检测方法

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20140120102A1 (en) 2012-10-30 2014-05-01 Gilead Sciences, Inc. Therapeutic and diagnostic methods related to lysyl oxidase-like 2 (loxl2)

Family Cites Families (58)

* 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
HRP20020599A2 (en) 2000-01-18 2004-08-31 Pfizer Prod Inc Corticotropin releasing factor antagonists
US7105682B2 (en) 2001-01-12 2006-09-12 Amgen Inc. Substituted amine 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
US6995162B2 (en) 2001-01-12 2006-02-07 Amgen Inc. Substituted alkylamine derivatives and methods of 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
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
ATE537825T1 (de) 2003-05-19 2012-01-15 Irm Llc Immunosuppressive verbindungen und zusammensetzungen
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
ATE545413T1 (de) 2004-03-15 2012-03-15 Lilly Co Eli Antagonisten des opioidrezeptors
CA2564085C (en) 2004-04-30 2013-04-02 Takeda Pharmaceutical Company Limited Heterocyclic amide compound and use thereof as an mmp-13 inhibitor
US7507748B2 (en) 2004-07-22 2009-03-24 Amgen Inc. Substituted aryl-amine derivatives and methods of use
WO2006027691A2 (en) 2004-09-10 2006-03-16 Pfizer Products Inc. Methods of treating mood disorders using benzisoxazole containing diazabicyclic compounds
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.
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
AU2006210954A1 (en) 2005-01-31 2006-08-10 Merck & Co., Inc. 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.
AU2006279211A1 (en) 2005-08-11 2007-02-15 Merck Frosst Canada Ltd Novel substituted 1,2,3-triazolylmethyl-benzothiophene or -indole and their use as leukotriene biosynthesis inhibitors
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
US20070225285A1 (en) 2005-11-04 2007-09-27 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
US20070219206A1 (en) 2005-11-04 2007-09-20 Amira Pharmaceuticals, Inc. 5-lipoxygenase-activating protein (flap) inhibitors
CA2636043A1 (en) 2006-01-23 2007-08-02 Amira Pharmaceuticals, Inc. Tricyclic inhibitors of 5-lipoxygenase
GB0614579D0 (en) 2006-07-21 2006-08-30 Black James Foundation Pyrimidine derivatives
WO2008020799A1 (en) 2006-08-18 2008-02-21 Astrazeneca Ab Thienopyrimidin-4-one and thienopyridazin-7-one derivatives 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
CN110372795A (zh) 2007-08-02 2019-10-25 吉利德生物制剂公司 Lox和loxl2抑制剂及其应用
JP2013500974A (ja) 2009-07-28 2013-01-10 アナコール ファーマシューティカルズ,インコーポレイテッド 三置換ホウ素含有分子
AU2010284001A1 (en) 2009-08-21 2012-03-22 Gilead Biologics, Inc. Therapeutic methods and compositions
RU2015108348A (ru) 2010-02-04 2015-07-20 Джилид Байолоджикс, Инк. Антитела, связывающиеся с лизилоксидазоподобным ферментом-2 (loxl2), и способы их применения
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
CN103415515B (zh) 2010-11-19 2015-08-26 因塞特公司 作为jak抑制剂的环丁基取代的吡咯并吡啶和吡咯并嘧啶衍生物
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
WO2013059587A1 (en) 2011-10-20 2013-04-25 Sirtris Pharmaceuticals, Inc. Substituted bicyclic aza-heterocycles and analogues as sirtuin modulators
US9701658B2 (en) 2012-04-25 2017-07-11 Raqualia Pharma Inc. Amide derivatives as TTX-S blockers
WO2014098098A1 (ja) 2012-12-18 2014-06-26 味の素株式会社 複素環アミド誘導体及びそれを含有する医薬
CA2939655A1 (en) 2014-02-14 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
CN107922392B (zh) 2015-02-15 2020-07-21 豪夫迈·罗氏有限公司 1-(杂)芳基磺酰基-(吡咯烷或哌啶)-2-甲酰胺衍生物及其用途
JP6800872B2 (ja) 2015-03-06 2020-12-16 ファーマケア,インク. リシルオキシダーゼ様2阻害剤とその使用
EP3795568A1 (en) * 2015-03-06 2021-03-24 Pharmakea, Inc. Fluorinated lysyl oxidase-like 2 inhibitors and uses thereof
JP7097874B2 (ja) 2016-09-07 2022-07-08 ファーマケア,インク. リシルオキシダーゼ様2阻害剤の使用
AU2017324445A1 (en) * 2016-09-07 2019-04-11 Pharmakea, Inc. Crystalline forms of a lysyl oxidase-like 2 inhibitor and methods of making

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20140120102A1 (en) 2012-10-30 2014-05-01 Gilead Sciences, Inc. Therapeutic and diagnostic methods related to lysyl oxidase-like 2 (loxl2)

Also Published As

Publication number Publication date
IL265192A (en) 2019-05-30
CN109983006A (zh) 2019-07-05
JP7079772B2 (ja) 2022-06-02
MX390964B (es) 2025-03-21
EP3510023A4 (en) 2020-03-18
SG11201901999XA (en) 2019-04-29
CN109983006B (zh) 2022-02-25
EA201990621A1 (ru) 2019-09-30
WO2018048943A1 (en) 2018-03-15
AU2017324445A1 (en) 2019-04-11
MA46204A (fr) 2021-03-17
JP2019532919A (ja) 2019-11-14
US11459309B2 (en) 2022-10-04
CA3036064A1 (en) 2018-03-15
EP3510023A1 (en) 2019-07-17
US20190202805A1 (en) 2019-07-04
KR20190052040A (ko) 2019-05-15
US20200361901A1 (en) 2020-11-19
US10774069B2 (en) 2020-09-15
BR112019004517A2 (pt) 2019-08-13
MX2019002615A (es) 2019-10-15
EP3510023B1 (en) 2024-06-19

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