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

Info

Publication number
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
Authority
CN
China
Prior art keywords
compound
theta
pharmaceutically acceptable
acid
acceptable salt
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
CN201780068733.0A
Other languages
English (en)
Chinese (zh)
Other versions
CN109983006A (zh
Inventor
戴维·罗纳根
凯文·罗斯·霍姆
马丁·W·罗伯特姆
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Pharmakea Inc
Original Assignee
Pharmakea Inc
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 Pharmakea Inc filed Critical Pharmakea Inc
Publication of CN109983006A publication Critical patent/CN109983006A/zh
Application granted granted Critical
Publication of CN109983006B publication Critical patent/CN109983006B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • 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

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)
  • 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)
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)

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

Publications (2)

Publication Number Publication Date
CN109983006A CN109983006A (zh) 2019-07-05
CN109983006B true CN109983006B (zh) 2022-02-25

Family

ID=61561660

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201780068733.0A Active CN109983006B (zh) 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

Country Status (14)

Country Link
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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10766860B2 (en) * 2015-03-06 2020-09-08 Pharmakea, Inc. Lysyl oxidase-like 2 inhibitors and uses thereof
MX376835B (es) 2015-03-06 2025-03-07 Pharmakea Inc Inhibidores de lisil oxidasa tipo 2 fluorinados y usos de los mismos.
AU2017218889A1 (en) 2016-02-09 2018-08-30 Pharmakea, Inc. Quinolinone lysyl oxidase-like 2 inhibitors and uses thereof
SG11201901999XA (en) * 2016-09-07 2019-04-29 Pharmakea Inc Crystalline forms of a lysyl oxidase-like 2 inhibitor and methods of making
KR20230162996A (ko) 2016-09-07 2023-11-29 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
CA2397633A1 (en) 2000-01-18 2001-07-26 Pfizer Products Inc. Corticotropin releasing factor antagonists
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
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
US7102009B2 (en) 2001-01-12 2006-09-05 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
AU2004240649A1 (en) 2003-05-19 2004-12-02 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
US7378448B2 (en) 2004-03-15 2008-05-27 Eli Lilly And Company Diphenylether amide derivatives as 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
CA2580042A1 (en) 2004-09-10 2006-03-16 Pfizer Products Inc. Methods of treating cognitive disorders using pyridyloxymethyl and benzisoxazole azabicyclic derivatives
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
EP1807417A2 (en) 2004-11-04 2007-07-18 Neurogen Corporation Pyrazolylmethyl heteroaryl derivatives
DE102004056226A1 (de) 2004-11-22 2006-05-24 Burchardt, Elmar Reinhold, Dr.Dr. Neuartige Inhibitoren der Lysyloxidase
JP2008528628A (ja) 2005-01-31 2008-07-31 メルク エンド カムパニー インコーポレーテッド 抗糖尿病性二環式化合物
AR055041A1 (es) 2005-03-23 2007-08-01 Merck Frosst Canada Ltd Tiadiazoles y oxadiazoles como inhibidores de la sintesis de leucotrienos. composiciones farmaceuticas.
CA2618586A1 (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
US20070225285A1 (en) 2005-11-04 2007-09-27 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
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
JP2010501553A (ja) 2006-08-18 2010-01-21 アストラゼネカ アクチボラグ Ｍｃｈｒ１アンタゴニストとしてのチエノピリミジン−４−オン誘導体およびチエノピリダジン−７−オン誘導体
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
EP2458995A1 (en) 2009-07-28 2012-06-06 Anacor Pharmaceuticals, Inc. Trisubstituted boron-containing molecules
MX2012002271A (es) 2009-08-21 2012-07-20 Gilead Biologics Inc Metodos y composiciones terapeuticas.
BR112012019693A2 (pt) 2010-02-04 2017-06-20 Gilead Biologics Inc anticorpos que se ligam à lisil oxidase-like 2 (loxl2) e métodos de uso para eles.
WO2011109799A1 (en) 2010-03-05 2011-09-09 Karyopharm Therapeutics, Inc. Nuclear transport modulatiors and uses thereof
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
KR20140077963A (ko) 2011-10-20 2014-06-24 글락소스미스클라인 엘엘씨 시르투인 조절제로서의 치환된 비시클릭 아자-헤테로사이클 및 유사체
IN2014MN01982A (enExample) 2012-04-25 2015-07-10 Raqualia Pharma Inc
EP2937335A4 (en) 2012-12-18 2016-09-14 Ea Pharma Co Ltd HETEROCYCLIC AMID DERIVATIVE AND MEDICAMENT THEREWITH
AU2015298491A1 (en) 2014-02-14 2016-09-01 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
CA2975196A1 (en) 2015-02-15 2016-08-18 F. Hoffmann-La Roche Ag 1-(het)arylsulfonyl-(pyrrolidine or piperidine)-2-carboxamide derivatives and their use as trpa1 antagonists
US10766860B2 (en) 2015-03-06 2020-09-08 Pharmakea, Inc. Lysyl oxidase-like 2 inhibitors and uses thereof
SG11201901999XA (en) 2016-09-07 2019-04-29 Pharmakea Inc Crystalline forms of a lysyl oxidase-like 2 inhibitor and methods of making
KR20230162996A (ko) 2016-09-07 2023-11-29 파마케아, 인크. 리실 옥시다제 유사 2 억제제의 용도

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

Also Published As

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

Similar Documents

Publication Publication Date Title
US11459309B2 (en) Crystalline forms of a lysyl oxidase-like 2 inhibitor and methods of making
US20200316041A1 (en) Formulations of an lsd1 inhibitor
US20250115603A1 (en) Crystalline forms of a kras inhibitor
JP7042548B2 (ja) Ｍａｇｌ阻害剤の結晶形態
TWI259081B (en) Treatment of acute myeloid leukemia with indolinone compounds
AU2019394974B2 (en) Crystalline forms of a compound for treating or preventing gout or hyperuricemia
AU2016344627B2 (en) Pyrimidine compositions, ultra-pure compositions and salts thereof, methods of making the same, and methods of using the same for treating histamine H4 receptor (H4) mediated diseases and conditions
CN116478165A (zh) 一种化合物的晶型、其制备和用途
TW200528109A (en) Method of treatment of atherosclerosis
CN102421775A (zh) 抑制Raf激酶的吡咯并[2，3-b]吡啶衍生物
EP2820019B1 (en) Novel crystalline form of sitagliptin sulfate
CN108473442A (zh) 包含赖氨酸特异性脱甲基酶-1的抑制剂的组合物
TW201305143A (zh) 光學活性吡唑基胺基喹唑啉及其醫藥組合物及使用方法
KR20240021239A (ko) Cdk 키나아제 억제제로 사용되는 화합물 및 이의 용도
MX2008008529A (es) Inhibidores de amida hidrolasa de acido graso.
CN102812000A (zh) Dp2拮抗剂及其用途
US12466835B1 (en) Solid forms of macrocyclic compounds, salts and formulations thereof, and methods of preparing and using the same
CN114222747A (zh) Pim激酶抑制剂组合物及其用途
EA041082B1 (ru) Кристаллические формы ингибитора лизилоксидаза-подобного белка 2 и способы получения
WO2021184958A1 (zh) 血管生成抑制剂、其制备方法和应用
WO2024040241A1 (en) Pharmaceutical formulations, processes for preparation, and methods of use
KR20210124976A (ko) 볼리난세린의 중수소화 형태 및 유도체
HK40089264A (en) Compound used as cdk7 kinase inhibitor and use thereof
CN103270030B (zh) 吡唑基氨基喹唑啉的氢溴酸盐
HK40032224A (en) Crystalline forms of compounds for preventing or treating sensory hair cell death

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
GR01 Patent grant
GR01 Patent grant