US20120058986A1 - Di-azetidinyl diamide as monoacylglycerol lipase inhibitors - Google Patents

Di-azetidinyl diamide as monoacylglycerol lipase inhibitors Download PDF

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Publication number
US20120058986A1
US20120058986A1 US13/224,654 US201113224654A US2012058986A1 US 20120058986 A1 US20120058986 A1 US 20120058986A1 US 201113224654 A US201113224654 A US 201113224654A US 2012058986 A1 US2012058986 A1 US 2012058986A1
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United States
Prior art keywords
compound
phenyl
thiazol
benzothiophen
trifluoromethyl
Prior art date
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Abandoned
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US13/224,654
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English (en)
Inventor
Peter J. Connolly
Mark J. Macielag
Bin Zhu
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.)
Janssen Pharmaceutica NV
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Janssen Pharmaceutica NV
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Filing date
Publication date
Application filed by Janssen Pharmaceutica NV filed Critical Janssen Pharmaceutica NV
Priority to US13/224,654 priority Critical patent/US20120058986A1/en
Assigned to JANSSEN PHARMACEUTICA N.V. reassignment JANSSEN PHARMACEUTICA N.V. ASSIGNMENT OF ASSIGNORS INTEREST (SEE DOCUMENT FOR DETAILS). Assignors: ZHU, BIN, CONNOLLY, PETER J., MACIELAG, MARK J.
Publication of US20120058986A1 publication Critical patent/US20120058986A1/en
Priority to US13/798,699 priority patent/US8759533B2/en
Priority to US13/798,770 priority patent/US8759333B2/en
Abandoned legal-status Critical Current

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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • A—HUMAN NECESSITIES
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    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/4035—Isoindoles, e.g. phthalimide
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
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    • C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
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    • C07D403/14—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 three or more hetero rings
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    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
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  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Pulmonology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Immunology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
US13/224,654 2010-09-03 2011-09-02 Di-azetidinyl diamide as monoacylglycerol lipase inhibitors Abandoned US20120058986A1 (en)

Priority Applications (3)

Application Number Priority Date Filing Date Title
US13/224,654 US20120058986A1 (en) 2010-09-03 2011-09-02 Di-azetidinyl diamide as monoacylglycerol lipase inhibitors
US13/798,699 US8759533B2 (en) 2010-09-03 2013-03-13 Di-azetidinyl diamide as monoacylglcerol lipase inhibitors
US13/798,770 US8759333B2 (en) 2010-09-03 2013-03-13 Di-azetidinyl diamide as monoacylglycerol lipase inhibitors

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US37976410P 2010-09-03 2010-09-03
US13/224,654 US20120058986A1 (en) 2010-09-03 2011-09-02 Di-azetidinyl diamide as monoacylglycerol lipase inhibitors

Related Child Applications (2)

Application Number Title Priority Date Filing Date
US13/798,770 Division US8759333B2 (en) 2010-09-03 2013-03-13 Di-azetidinyl diamide as monoacylglycerol lipase inhibitors
US13/798,699 Division US8759533B2 (en) 2010-09-03 2013-03-13 Di-azetidinyl diamide as monoacylglcerol lipase inhibitors

Publications (1)

Publication Number Publication Date
US20120058986A1 true US20120058986A1 (en) 2012-03-08

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Application Number Title Priority Date Filing Date
US13/224,654 Abandoned US20120058986A1 (en) 2010-09-03 2011-09-02 Di-azetidinyl diamide as monoacylglycerol lipase inhibitors
US13/798,699 Active US8759533B2 (en) 2010-09-03 2013-03-13 Di-azetidinyl diamide as monoacylglcerol lipase inhibitors
US13/798,770 Active US8759333B2 (en) 2010-09-03 2013-03-13 Di-azetidinyl diamide as monoacylglycerol lipase inhibitors

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Application Number Title Priority Date Filing Date
US13/798,699 Active US8759533B2 (en) 2010-09-03 2013-03-13 Di-azetidinyl diamide as monoacylglcerol lipase inhibitors
US13/798,770 Active US8759333B2 (en) 2010-09-03 2013-03-13 Di-azetidinyl diamide as monoacylglycerol lipase inhibitors

Country Status (12)

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US (3) US20120058986A1 (fr)
EP (1) EP2611774B1 (fr)
JP (1) JP2013536852A (fr)
KR (1) KR20130101040A (fr)
CN (1) CN103068798A (fr)
AR (1) AR082891A1 (fr)
AU (1) AU2011296068B2 (fr)
BR (1) BR112013005141A2 (fr)
CA (1) CA2809991A1 (fr)
RU (1) RU2013114771A (fr)
TW (1) TW201305132A (fr)
WO (1) WO2012030907A1 (fr)

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8759333B2 (en) * 2010-09-03 2014-06-24 Janssen Pharmaceutica Nv Di-azetidinyl diamide as monoacylglycerol lipase inhibitors
WO2016046130A1 (fr) * 2014-09-22 2016-03-31 INSERM (Institut National de la Santé et de la Recherche Médicale) Procédés et compositions pharmaceutiques destinés au traitement de la fibrose
EP3279191A4 (fr) * 2015-03-30 2018-10-17 Takeda Pharmaceutical Company Limited Composé hétérocyclique
US10323026B2 (en) 2016-03-31 2019-06-18 Takeda Pharmaceutical Company Limited Heterocyclic compound
US11274101B2 (en) 2017-09-29 2022-03-15 Takeda Pharmaceutical Company Limited Heterocyclic compound

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* Cited by examiner, † Cited by third party
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US9227978B2 (en) 2013-03-15 2016-01-05 Araxes Pharma Llc Covalent inhibitors of Kras G12C
TWI659021B (zh) 2013-10-10 2019-05-11 亞瑞克西斯製藥公司 Ｋｒａｓ ｇ１２ｃ之抑制劑
EP3087067B1 (fr) 2013-12-26 2018-10-24 Takeda Pharmaceutical Company Limited Composés 4-(pipérazin-1-yl)-pyrrolidin-2-one comme inhibiteurs de la monoacylglycérol lipase (magl)
JO3556B1 (ar) 2014-09-18 2020-07-05 Araxes Pharma Llc علاجات مدمجة لمعالجة السرطان
WO2016049565A1 (fr) * 2014-09-25 2016-03-31 Araxes Pharma Llc Compositions et procédés pour inhiber la ras
US10011600B2 (en) 2014-09-25 2018-07-03 Araxes Pharma Llc Methods and compositions for inhibition of Ras
WO2016049524A1 (fr) 2014-09-25 2016-03-31 Araxes Pharma Llc Inhibiteurs de protéines mutantes kras g12c
TW201702232A (zh) 2015-04-10 2017-01-16 亞瑞克西斯製藥公司 經取代之喹唑啉化合物及其使用方法
US10428064B2 (en) 2015-04-15 2019-10-01 Araxes Pharma Llc Fused-tricyclic inhibitors of KRAS and methods of use thereof
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
US10858343B2 (en) 2015-09-28 2020-12-08 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
WO2017058807A1 (fr) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibiteurs de protéines kras portant la mutation g12c
US10730867B2 (en) 2015-09-28 2020-08-04 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
WO2017058768A1 (fr) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibiteurs de protéines kras portant la mutation g12c
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AR082891A1 (es) 2013-01-16
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TW201305132A (zh) 2013-02-01
US8759533B2 (en) 2014-06-24
US20130196968A1 (en) 2013-08-01
AU2011296068A1 (en) 2013-03-14
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