CN109983006B - 赖氨酰氧化酶样2抑制剂的结晶形式及其制备方法 - Google Patents

赖氨酰氧化酶样2抑制剂的结晶形式及其制备方法 Download PDF

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CN109983006B
CN109983006B CN201780068733.0A CN201780068733A CN109983006B CN 109983006 B CN109983006 B CN 109983006B CN 201780068733 A CN201780068733 A CN 201780068733A CN 109983006 B CN109983006 B CN 109983006B
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theta
pharmaceutically acceptable
acid
acceptable salt
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CN109983006A (zh
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戴维·罗纳根
凯文·罗斯·霍姆
马丁·W·罗伯特姆
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Pharmakea Inc
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    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non 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
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/63—Esters of sulfonic acids
    • C07C309/64—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to acyclic carbon atoms
    • C07C309/65—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to acyclic carbon atoms of a saturated carbon skeleton
    • C07C309/66—Methanesulfonates
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic 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
    • C07D207/04—Heterocyclic 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
    • C07D207/10—Heterocyclic 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
    • C07D207/12—Oxygen or sulfur atoms
    • 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

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  • 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)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Catalysts (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201780068733.0A 2016-09-07 2017-09-06 赖氨酰氧化酶样2抑制剂的结晶形式及其制备方法 Active CN109983006B (zh)

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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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CN109983006B true CN109983006B (zh) 2022-02-25

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US (2) US10774069B2 (https=)
EP (1) EP3510023B1 (https=)
JP (1) JP7079772B2 (https=)
KR (1) KR102587178B1 (https=)
CN (1) CN109983006B (https=)
AU (1) AU2017324445A1 (https=)
BR (1) BR112019004517A2 (https=)
CA (1) CA3036064A1 (https=)
EA (1) EA201990621A1 (https=)
IL (1) IL265192A (https=)
MA (1) MA46204A (https=)
MX (1) MX390964B (https=)
SG (1) SG11201901999XA (https=)
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Families Citing this family (7)

* 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
JP6697809B2 (ja) 2015-03-06 2020-05-27 ファーマケア，インク． フッ素化リシルオキシダーゼ様２阻害剤とその使用
ES2880766T3 (es) * 2016-02-09 2021-11-25 Pharmakea Inc Inhibidores de quinolinona lisil oxidasa similar al tipo 2 y usos de los mismos
KR102587178B1 (ko) 2016-09-07 2023-10-06 파마케아, 인크. 리실 옥시다아제-유사 2 억제제의 결정질 형태 및 제조 방법
KR102615565B1 (ko) 2016-09-07 2023-12-18 파마케아, 인크. 리실 옥시다제 유사 2 억제제의 용도
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 (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0110405A2 (en) * 1982-12-01 1984-06-13 RORER INTERNATIONAL (OVERSEAS) INC. (a Delaware corporation) Antiinflammatory/antiallergic compounds
EP1775347A2 (en) * 2005-10-14 2007-04-18 Procos S.p.A. A process for the enantiomeric resolution of 1-substituted 2-(aminomethyl)-pyrrolidines by amidation with lipases
CN103415515A (zh) * 2010-11-19 2013-11-27 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
CN104755501A (zh) * 2012-10-30 2015-07-01 吉联亚科学公司 与赖氨酰氧化酶样蛋白2(loxl2)相关的治疗和诊断方法
CN107592861A (zh) * 2015-03-06 2018-01-16 法玛克亚公司 氟化赖氨酰氧化酶样2抑制剂及其用途

Family Cites Families (54)

* 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
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
US7125880B1 (en) 1995-06-06 2006-10-24 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
US6995162B2 (en) 2001-01-12 2006-02-07 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
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
US7105682B2 (en) 2001-01-12 2006-09-12 Amgen Inc. Substituted amine 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
CN1791592B (zh) 2003-05-19 2012-07-04 Irm责任有限公司 免疫抑制剂化合物和组合物
WO2007016784A1 (en) 2005-08-11 2007-02-15 Merck Frosst Canada Ltd. Novel substituted 1,2,3-tπazolylmethyl-benzothiophene or -indole and their use as leukotπene biosynthesis inhibitors
JP2007519705A (ja) 2004-01-29 2007-07-19 ファイザー・プロダクツ・インク Ｃｎｓ障害を治療するための非定型抗精神病薬とアミノメチルピリジルオキシメチル／ベンゾイソオキサゾールアザビシクロ誘導体の組合せ
DE602005022572D1 (de) 2004-03-12 2010-09-09 Lilly Co Eli Antagonisten des opioidrezeptors
EP1735268B1 (en) 2004-03-15 2012-02-15 Eli Lilly And Company Opioid receptor antagonists
BRPI0510305A (pt) 2004-04-30 2007-10-02 Takeda Pharmaceutical composto ou um sal do mesmo, pródroga ou um sal da mesma, agente farmacêutico, método de produção do composto ou um sal do mesmo, inibidor de metaloproteinase de matriz ou um sal do mesmo ou uma pródroga do mesmo, método de inibir uma metaloproteinase de matriz, e, uso de um composto ou de um sal do mesmo ou de uma pródroga do mesmo
US7507748B2 (en) 2004-07-22 2009-03-24 Amgen Inc. Substituted aryl-amine derivatives and methods of use
BRPI0515143A (pt) 2004-09-10 2008-07-08 Pfizer Prod Inc usos de derivados azabicìclicos de piridiloximetila e benzisoxazol para a preparação de uma composição farmacêutica para o tratamento dos distúrbios de humor
WO2006027692A2 (en) 2004-09-10 2006-03-16 Pfizer Products Inc. Methods of treating cognitive disorders using pyridyloxymethyl and benzisoxazole azabicyclic derivatives
US20080004269A1 (en) 2004-11-04 2008-01-03 Yuelian Xu Pyrazolylmethy 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.
US7405302B2 (en) 2005-10-11 2008-07-29 Amira Pharmaceuticals, Inc. 5-lipoxygenase-activating protein (FLAP) inhibitors
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
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
CA2693310C (en) 2007-08-02 2018-11-27 Arresto Biosciences, Inc. Lox and loxl2 inhibitors, antibodies and uses thereof
WO2011017125A1 (en) 2009-07-28 2011-02-10 Anacor Pharmaceuticals, Inc. Trisubstituted boron-containing molecules
CN102711821A (zh) 2009-08-21 2012-10-03 吉联亚生物科技有限公司 治疗方法和组合物
US8680246B2 (en) 2010-02-04 2014-03-25 Gilead Biologics, Inc. Antibodies that bind to lysyl oxidase-like 2 (LOXL2)
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
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
RU2014120166A (ru) 2011-10-20 2015-11-27 ГЛЭКСОСМИТКЛАЙН ЭлЭлСи Замещенные бициклические аза-гетероциклы и их аналоги в качестве модуляторов сиртуина
IN2014MN01982A (https=) 2012-04-25 2015-07-10 Raqualia Pharma Inc
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
EP3129027A4 (en) 2014-02-14 2017-06-21 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
KR102615565B1 (ko) 2016-09-07 2023-12-18 파마케아, 인크. 리실 옥시다제 유사 2 억제제의 용도
KR102587178B1 (ko) 2016-09-07 2023-10-06 파마케아, 인크. 리실 옥시다아제-유사 2 억제제의 결정질 형태 및 제조 방법

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0110405A2 (en) * 1982-12-01 1984-06-13 RORER INTERNATIONAL (OVERSEAS) INC. (a Delaware corporation) Antiinflammatory/antiallergic compounds
EP1775347A2 (en) * 2005-10-14 2007-04-18 Procos S.p.A. A process for the enantiomeric resolution of 1-substituted 2-(aminomethyl)-pyrrolidines by amidation with lipases
CN103415515A (zh) * 2010-11-19 2013-11-27 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
CN104755501A (zh) * 2012-10-30 2015-07-01 吉联亚科学公司 与赖氨酰氧化酶样蛋白2(loxl2)相关的治疗和诊断方法
CN107592861A (zh) * 2015-03-06 2018-01-16 法玛克亚公司 氟化赖氨酰氧化酶样2抑制剂及其用途

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US20190202805A1 (en) 2019-07-04
WO2018048943A1 (en) 2018-03-15
EA201990621A1 (ru) 2019-09-30
US10774069B2 (en) 2020-09-15
CN109983006A (zh) 2019-07-05
KR102587178B1 (ko) 2023-10-06
MA46204A (fr) 2021-03-17
KR20190052040A (ko) 2019-05-15
JP2019532919A (ja) 2019-11-14
MX390964B (es) 2025-03-21
AU2017324445A1 (en) 2019-04-11
US11459309B2 (en) 2022-10-04
EP3510023A4 (en) 2020-03-18
BR112019004517A2 (pt) 2019-08-13
IL265192A (en) 2019-05-30
US20200361901A1 (en) 2020-11-19
SG11201901999XA (en) 2019-04-29
EP3510023A1 (en) 2019-07-17
EP3510023B1 (en) 2024-06-19
JP7079772B2 (ja) 2022-06-02
CA3036064A1 (en) 2018-03-15
MX2019002615A (es) 2019-10-15

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