AU2017361257B2 - Crystalline forms of a MAGL inhibitor - Google Patents

Crystalline forms of a MAGL inhibitor Download PDF

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Publication number
AU2017361257B2
AU2017361257B2 AU2017361257A AU2017361257A AU2017361257B2 AU 2017361257 B2 AU2017361257 B2 AU 2017361257B2 AU 2017361257 A AU2017361257 A AU 2017361257A AU 2017361257 A AU2017361257 A AU 2017361257A AU 2017361257 B2 AU2017361257 B2 AU 2017361257B2
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AU
Australia
Prior art keywords
compound
theta
crystalline
hexafluoropropan
pyrrolidin
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.)
Ceased
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AU2017361257A
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English (en)
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AU2017361257A1 (en
Inventor
Channing Rodney Beals
Jacqueline Lorayne BLANKMAN
Cheryl A. Grice
Kurt G. GRIMM
Todd K. Jones
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H Lundbeck AS
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H Lundbeck AS
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Publication of AU2017361257A1 publication Critical patent/AU2017361257A1/en
Assigned to LUNDBECK LA JOLLA RESEARCH CENTER, INC. reassignment LUNDBECK LA JOLLA RESEARCH CENTER, INC. Request for Assignment Assignors: ABIDE THERAPEUTICS, INC.
Assigned to H. LUNDBECK A/S. reassignment H. LUNDBECK A/S. Request for Assignment Assignors: LUNDBECK LA JOLLA RESEARCH CENTER, INC.
Application granted granted Critical
Publication of AU2017361257B2 publication Critical patent/AU2017361257B2/en
Ceased legal-status Critical Current
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/20—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof
    • C07D295/205—Radicals derived from carbonic acid
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
    • C07C57/02—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
    • C07C57/13—Dicarboxylic acids
    • C07C57/15—Fumaric acid
    • 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Neurology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Rheumatology (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
AU2017361257A 2016-11-16 2017-11-15 Crystalline forms of a MAGL inhibitor Ceased AU2017361257B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662423126P 2016-11-16 2016-11-16
US62/423,126 2016-11-16
PCT/US2017/061875 WO2018093953A1 (en) 2016-11-16 2017-11-15 Crystalline forms of a magl inhibitor

Publications (2)

Publication Number Publication Date
AU2017361257A1 AU2017361257A1 (en) 2019-05-30
AU2017361257B2 true AU2017361257B2 (en) 2022-02-10

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
AU2017361257A Ceased AU2017361257B2 (en) 2016-11-16 2017-11-15 Crystalline forms of a MAGL inhibitor

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US (2) US11142517B2 (enExample)
EP (2) EP3541807B1 (enExample)
JP (2) JP7042548B2 (enExample)
KR (1) KR102508739B1 (enExample)
CN (2) CN110291083B (enExample)
AU (1) AU2017361257B2 (enExample)
BR (1) BR112019010003A2 (enExample)
CA (1) CA3043610A1 (enExample)
CL (1) CL2019001340A1 (enExample)
CO (1) CO2019005045A2 (enExample)
CR (1) CR20190242A (enExample)
CY (1) CY1124870T1 (enExample)
DK (1) DK3541807T3 (enExample)
DO (1) DOP2019000120A (enExample)
EA (1) EA201991086A1 (enExample)
EC (1) ECSP19035171A (enExample)
ES (2) ES2900016T3 (enExample)
GE (1) GEP20237559B (enExample)
HR (2) HRP20231697T1 (enExample)
HU (2) HUE064559T2 (enExample)
IL (1) IL266548A (enExample)
JO (1) JOP20190109B1 (enExample)
LT (1) LT3541807T (enExample)
MA (2) MA58133B1 (enExample)
MX (2) MX389459B (enExample)
MY (1) MY199386A (enExample)
NI (1) NI201900053A (enExample)
PE (1) PE20191239A1 (enExample)
PH (1) PH12019501068A1 (enExample)
PL (2) PL3964503T3 (enExample)
PT (1) PT3541807T (enExample)
RS (2) RS65016B1 (enExample)
SI (1) SI3541807T1 (enExample)
SM (2) SMT202300494T1 (enExample)
TN (1) TN2019000151A1 (enExample)
UA (1) UA124585C2 (enExample)
WO (1) WO2018093953A1 (enExample)
ZA (1) ZA201903093B (enExample)

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US10899737B2 (en) 2016-09-19 2021-01-26 Lundbeck La Jolla Research Center, Inc. Piperazine carbamates and methods of making and using same
JOP20190107A1 (ar) 2016-11-16 2019-05-09 Lundbeck La Jolla Research Center Inc مثبطات أحادي أسيل جليسرول ليباز (magl)
JOP20190108B1 (ar) 2016-11-16 2023-09-17 H Lundbeck As تركيبات صيدلانية
HUE064559T2 (hu) 2016-11-16 2024-03-28 H Lundbeck As MAGL inhibitor kristályos formája
RS64006B1 (sr) 2017-05-23 2023-03-31 H Lundbeck As Pirazol magl inhibitori
US10927105B1 (en) 2017-05-23 2021-02-23 Lundbeck La Jolla Research Center, Inc. Pyrazole MAGL inhibitors
ES2952332T3 (es) 2017-08-29 2023-10-30 H Lundbeck As Compuestos espirocíclicos y sus métodos de preparación y uso
KR20210010475A (ko) 2018-05-15 2021-01-27 룬드벡 라 졸라 리서치 센터 인코포레이티드 Magl 저해제
KR20210033504A (ko) * 2018-07-19 2021-03-26 화이자 인코포레이티드 Magl 억제제로서 헤테로환형 스피로 화합물
HUE067912T2 (hu) 2018-08-13 2024-11-28 Hoffmann La Roche Új heterociklusos vegyületek, mint monoacil-glicerin-lipáz inhibitorok
WO2020154683A1 (en) * 2019-01-25 2020-07-30 Lundbeck La Jolla Research Center, Inc. Methods of treating disease with magl inhibitors
CN114761382A (zh) * 2019-11-15 2022-07-15 H.隆德贝克有限公司 Magl抑制剂的晶型
KR20230004622A (ko) * 2020-04-21 2023-01-06 하. 룬드벡 아크티에셀스카브 모노아실글리세롤 리파제 억제제의 합성
WO2023092079A1 (en) * 2021-11-19 2023-05-25 Bryant Cynthia W Use of cannabinoid compounds to treat gastrointestinal disorders
US20250084065A1 (en) 2021-12-29 2025-03-13 Psy Therapeutics, Inc. Inhibiting monoacylglycerol lipase (magl)
CN119137114A (zh) 2022-05-04 2024-12-13 H.隆德贝克有限公司 作为单酰基甘油脂肪酶抑制剂的(s)-1-(哒嗪-3-基氨基甲酰基)-6-氮杂螺[2.5]辛烷-6-甲酸1,1,1,3,3,3-六氟丙-2-酯的结晶形式
CN117665187B (zh) * 2023-11-23 2024-08-16 宁波大红鹰药业股份有限公司 一种舒林酸中间体杂质的测定方法

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Also Published As

Publication number Publication date
EP3964503A1 (en) 2022-03-09
PT3541807T (pt) 2021-12-09
ZA201903093B (en) 2020-11-25
US11993588B2 (en) 2024-05-28
HRP20211863T1 (hr) 2022-03-04
EP3541807A1 (en) 2019-09-25
TN2019000151A1 (en) 2020-10-05
WO2018093953A1 (en) 2018-05-24
CY1124870T1 (el) 2022-11-25
NZ753241A (en) 2021-06-25
RS62665B1 (sr) 2021-12-31
BR112019010003A2 (pt) 2019-08-20
MX2022000249A (es) 2022-02-03
PE20191239A1 (es) 2019-09-16
HUE056973T2 (hu) 2022-04-28
JP2019537596A (ja) 2019-12-26
CR20190242A (es) 2019-07-09
EA201991086A1 (ru) 2019-11-29
MA58133B1 (fr) 2024-02-29
MX2019005767A (es) 2019-12-05
SI3541807T1 (sl) 2022-01-31
CL2019001340A1 (es) 2019-10-04
HRP20231697T1 (hr) 2024-03-15
AU2017361257A1 (en) 2019-05-30
NI201900053A (es) 2019-10-30
CN110291083A (zh) 2019-09-27
SMT202300494T1 (it) 2024-01-10
LT3541807T (lt) 2021-12-27
KR20190077561A (ko) 2019-07-03
ECSP19035171A (es) 2019-05-31
EP3541807B1 (en) 2021-09-29
RS65016B1 (sr) 2024-01-31
JOP20190109A1 (ar) 2019-05-09
ES2966939T3 (es) 2024-04-25
PH12019501068A1 (en) 2019-08-19
IL266548A (en) 2019-07-31
JP7042548B2 (ja) 2022-03-28
US20220235037A1 (en) 2022-07-28
DK3541807T3 (da) 2021-12-06
CA3043610A1 (en) 2018-05-24
HUE064559T2 (hu) 2024-03-28
JP7350117B2 (ja) 2023-09-25
RU2019116689A3 (enExample) 2021-02-26
CN110291083B (zh) 2022-06-17
UA124585C2 (uk) 2021-10-13
US11142517B2 (en) 2021-10-12
MY199386A (en) 2023-10-25
EP3964503C0 (en) 2023-11-08
GEP20237559B (en) 2023-10-25
US20200190063A1 (en) 2020-06-18
MA46866A (fr) 2021-06-02
PL3541807T3 (pl) 2022-01-17
MX389459B (es) 2025-03-20
MA46866B1 (fr) 2021-11-30
EP3541807A4 (en) 2020-04-22
JP2022084717A (ja) 2022-06-07
CO2019005045A2 (es) 2019-05-31
SMT202100675T1 (it) 2022-01-10
EP3964503B1 (en) 2023-11-08
RU2019116689A (ru) 2020-12-17
ES2900016T3 (es) 2022-03-15
CN115093382A (zh) 2022-09-23
JOP20190109B1 (ar) 2022-09-15
PL3964503T3 (pl) 2024-04-02
DOP2019000120A (es) 2019-09-30
KR102508739B1 (ko) 2023-03-09

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