AU2012220531B2 - Asymmetric ureas and medical uses thereof - Google Patents

Asymmetric ureas and medical uses thereof Download PDF

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AU2012220531B2
AU2012220531B2 AU2012220531A AU2012220531A AU2012220531B2 AU 2012220531 B2 AU2012220531 B2 AU 2012220531B2 AU 2012220531 A AU2012220531 A AU 2012220531A AU 2012220531 A AU2012220531 A AU 2012220531A AU 2012220531 B2 AU2012220531 B2 AU 2012220531B2
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pharmaceutically acceptable
disease
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AU2012220531A1 (en
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Silvina Garcia Rubio
Claudio Giuliano
Zhigang Li
Claudio Pietra
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Helsinn Healthcare SA
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Helsinn Healthcare SA
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    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
    • C07D211/56—Nitrogen atoms
    • C07D211/58—Nitrogen atoms attached in position 4
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    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
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    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
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    • C—CHEMISTRY; METALLURGY
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    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
    • C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/92—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with a hetero atom directly attached to the ring nitrogen atom
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/92—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with a hetero atom directly attached to the ring nitrogen atom
    • C07D211/96—Sulfur atom
    • C—CHEMISTRY; METALLURGY
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    • 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
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    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Addiction (AREA)
  • Neurology (AREA)
  • Endocrinology (AREA)
  • Neurosurgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Emergency Medicine (AREA)
  • Psychiatry (AREA)
  • Child & Adolescent Psychology (AREA)
  • Nutrition Science (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Hydrogenated Pyridines (AREA)
AU2012220531A 2011-02-25 2012-02-23 Asymmetric ureas and medical uses thereof Active AU2012220531B2 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
PCT/CN2011/000298 WO2012113103A1 (en) 2011-02-25 2011-02-25 Asymmetric ureas and medical uses thereof
AUPCT/CN2011/000298 2011-02-25
US201161466070P 2011-03-22 2011-03-22
US61/466,070 2011-03-22
PCT/US2012/026315 WO2012116176A2 (en) 2011-02-25 2012-02-23 Asymmetric ureas and medical uses thereof

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AU2012220531A1 AU2012220531A1 (en) 2013-09-26
AU2012220531B2 true AU2012220531B2 (en) 2017-02-23

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KR (2) KR20140014186A (enExample)
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AP (1) AP3768A (enExample)
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Families Citing this family (17)

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Publication number Priority date Publication date Assignee Title
WO2012113103A1 (en) * 2011-02-25 2012-08-30 Helsinn Healthcare S.A. Asymmetric ureas and medical uses thereof
ES3066738T3 (en) 2012-12-21 2026-05-14 Aveo Pharmaceuticals Inc Anti-gdf15 antibodies
TWI690512B (zh) * 2014-03-07 2020-04-11 瑞士商赫爾辛保健股份有限公司 對位取代的不對稱脲及其醫療用途
JP6910800B2 (ja) 2014-06-20 2021-07-28 アベオ ファーマシューティカルズ, インコーポレイテッド Gdf15調節剤を用いたうっ血性心不全及びその他の心機能不全の治療
RU2686317C2 (ru) * 2015-04-24 2019-04-25 Федеральное государственное бюджетное научное учреждение "Научно-исследовательский институт фармакологии имени В.В. Закусова" Замещенные 1,2,5-триметил- и 2,2,6,6-тетраметил-4-аминопиперидины, обладающие антиишемическим действием
HUE061547T2 (hu) 2016-03-22 2023-07-28 Helsinn Healthcare Sa Aszimmetrikus benzolszulfonil-karbamid-származékok és gyógyászati alkalmazásuk
CN117986363A (zh) 2016-03-31 2024-05-07 恩格姆生物制药公司 结合蛋白及其使用方法
US11071738B2 (en) 2017-08-07 2021-07-27 Hiroshima University Therapeutic agent for fatty liver diseases and therapeutic agent for adiposity
WO2019040107A1 (en) 2017-08-21 2019-02-28 Acadia Pharmaceuticals Inc. COMPOUNDS, CORRESPONDING SALTS AND METHODS FOR THE TREATMENT OF DISEASES
US11440884B2 (en) 2017-08-21 2022-09-13 Acadia Pharmaceuticals Inc. Compounds, salts thereof and methods for treatment of diseases
AU2018385438B2 (en) 2017-12-11 2022-12-15 Helsinn Healthcare Sa Fumarate salt of (R)-3-(1-(2,3-dichloro-4-(pyrazin-2-yl)phenyl)-2,2,2-trifluoroethyl)-1-methyl-1-(1-methylpiperidin-4-yl) urea, methods of preparation, and uses thereof
EP3542799A1 (en) * 2018-03-22 2019-09-25 Helsinn Healthcare SA New centrally-active ghrelin agonist and medical uses thereof
IL305262A (en) 2021-03-10 2023-10-01 Jnana Therapeutics Inc Small molecule inhibitors of mammalian SLC6A19 function
ES3027259T3 (en) 2021-06-02 2025-06-13 Helsinn Healthcare Sa Piperidine urea derivatives for use as inotropic agents
US20240391928A1 (en) * 2021-09-22 2024-11-28 Duke University Compositions for the treatment of food and chemical addiction and methods of making and using same
US20260226036A1 (en) * 2023-01-25 2026-08-06 University Of North Texas Health Science Center Thiourea antioxcompounds with neuroprotective activity
WO2026119870A1 (en) 2024-12-03 2026-06-11 Anacardio Ab New dose regimen

Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5285174A (en) * 1976-01-05 1977-07-15 Yoshitomi Pharmaceut Ind Ltd Novel urea or thiourea derivatives
WO2001066521A1 (en) * 2000-03-06 2001-09-13 Acadia Pharmaceuticals, Inc. Azacyclic compounds for use in the treatment of serotonin related diseases
US20040006081A1 (en) * 2000-05-17 2004-01-08 Jeremy Burrows Pharmaceutically active piperidine derivatives, in particular as modulators of chemokine receptor activity
WO2005077914A1 (en) * 2004-02-10 2005-08-25 Janssen Pharmaceutica, N.V. PYRIDAZINONE UREAS AS ANTAGONISTS OF α4 INTEGRINS
WO2005112927A1 (en) * 2004-05-21 2005-12-01 Acadia Pharmaceuticals Inc. Selective serotonin receptor inverse agonists as therapeutics for disease
WO2006014136A1 (en) * 2004-08-02 2006-02-09 Astrazeneca Ab Piperidine derivatives as histamine h3 receptor ligands
US20070149512A1 (en) * 2005-12-09 2007-06-28 Solvay Pharmaceuticals Gmbh N-Sulfamoyl-piperidineamides for the treatment or inhibition of obesity and related conditions
WO2009039460A2 (en) * 2007-09-21 2009-03-26 Acadia Pharmaceuticals, Inc. Co-administration of pimavanserin with other agents
WO2011060397A1 (en) * 2009-11-16 2011-05-19 Schering Corporation Substituted amino heterocycles useful as hiv antagonists

Family Cites Families (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU7545894A (en) 1993-09-02 1995-03-22 Yamanouchi Pharmaceutical Co., Ltd. Carbamate derivative and medicine containing the same
AU3785597A (en) 1996-08-14 1998-03-06 Takeda Chemical Industries Ltd. Cyclic urea compounds, their production and use as herbicides
US6399619B1 (en) 1999-04-06 2002-06-04 Merck & Co., Inc. Pyrrolidine modulators of chemokine receptor activity
US20030022891A1 (en) * 2000-12-01 2003-01-30 Anandan Palani MCH antagonists and their use in the treatment of obesity
US20040110952A1 (en) 2001-03-01 2004-06-10 Jeremy Burrows N-4-piperidinyl compounds as ccr5 modulators
GB0107228D0 (en) 2001-03-22 2001-05-16 Astrazeneca Ab Chemical compounds
US6673829B2 (en) * 2001-09-14 2004-01-06 Novo Nordisk A/S Aminoazetidine,-pyrrolidine and -piperidine derivatives
SE0103818D0 (sv) 2001-11-15 2001-11-15 Astrazeneca Ab Chemical compounds
SE0200919D0 (sv) 2002-03-25 2002-03-25 Astrazeneca Ab Chemical compounds
US7414057B2 (en) * 2002-09-11 2008-08-19 Merck & Co., Inc. Piperazine urea derivatives as melanocortin-4 receptor agonists
AU2003284402A1 (en) 2002-11-15 2004-06-15 Yamanouchi Pharmaceutical Co., Ltd. Antagonist to melanin-concentrating hormone receptor
EP1640361B9 (en) * 2003-06-30 2015-11-04 Sumitomo Chemical Company, Limited Asymmetric urea compounds and process for producing asymmetric compounds by asymmetric conjugate addition reaction using the same as catalyst
US7115767B2 (en) * 2003-07-18 2006-10-03 Abbott Laboratories Tetraline derivatives as ghrelin receptor modulators
GB0412865D0 (en) 2004-06-09 2004-07-14 Glaxo Group Ltd Chemical compounds
SE0401657D0 (sv) 2004-06-24 2004-06-24 Astrazeneca Ab Chemical compounds
EP1784390A2 (en) * 2004-08-13 2007-05-16 Amgen Inc. Substituted benzofused heterocycles
CA2575764A1 (en) * 2004-10-27 2006-05-11 Neurogen Corporation Diaryl ureas as cb1 antagonists
AR051802A1 (es) 2004-12-21 2007-02-07 Astrazeneca Ab Heterociclos antagonistas de mchr1
US7829589B2 (en) 2005-06-10 2010-11-09 Elixir Pharmaceuticals, Inc. Sulfonamide compounds and uses thereof
EP1931633A2 (en) * 2005-09-05 2008-06-18 Ranbaxy Laboratories Limited Derivatives of 3-azabicyclo[3.1.0]hexane as dipeptidyl peptidase-iv inhibitors
EA200801243A1 (ru) * 2005-11-01 2008-10-30 Транстек Фарма Фармацевтическое применение замещенных амидов
US20090253673A1 (en) 2006-07-12 2009-10-08 Min Ge Substituted Pyrazoles as Ghrelin Receptor Antagonists
JP2008042298A (ja) 2006-08-02 2008-02-21 Olympus Corp 固体撮像装置
GB0701992D0 (en) 2007-02-02 2007-03-14 7Tm Pharma As Grehlin Receptor Modulators
US20080280886A1 (en) * 2007-05-08 2008-11-13 Auspex Pharmaceuticals, Inc. Substituted ureas
GB0710863D0 (en) 2007-06-06 2007-07-18 Glaxo Group Ltd Novel compounds
GB0710865D0 (en) 2007-06-06 2007-07-18 Glaxo Group Ltd Novel compounds
WO2009020960A1 (en) 2007-08-06 2009-02-12 The Regents Of The University Of California Preparation of novel 1,3-substituted ureas as inhibitors of soluble epoxide hydrolase
UA100527C2 (en) 2007-10-10 2013-01-10 Астразенека Аб Benzothiazoles as ghrelin receptor modulators
WO2009092293A1 (en) 2008-01-18 2009-07-30 Shanghai Targetdrug Co., Ltd. Pyrollidine-based compounds
WO2009089659A1 (en) 2008-01-18 2009-07-23 Shanghai Targetdrug Co., Ltd. Pyrollidine-based compounds
USRE49686E1 (en) * 2008-09-19 2023-10-10 Takeda Pharmaceutical Company Limited Nitrogen-containing heterocyclic compound and use of same
WO2010111353A1 (en) * 2009-03-25 2010-09-30 Acadia Pharmaceuticals, Inc. N-substituted piperidine derivatives as serotonin receptor agents
WO2012113103A1 (en) * 2011-02-25 2012-08-30 Helsinn Healthcare S.A. Asymmetric ureas and medical uses thereof

Patent Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5285174A (en) * 1976-01-05 1977-07-15 Yoshitomi Pharmaceut Ind Ltd Novel urea or thiourea derivatives
WO2001066521A1 (en) * 2000-03-06 2001-09-13 Acadia Pharmaceuticals, Inc. Azacyclic compounds for use in the treatment of serotonin related diseases
US20040006081A1 (en) * 2000-05-17 2004-01-08 Jeremy Burrows Pharmaceutically active piperidine derivatives, in particular as modulators of chemokine receptor activity
WO2005077914A1 (en) * 2004-02-10 2005-08-25 Janssen Pharmaceutica, N.V. PYRIDAZINONE UREAS AS ANTAGONISTS OF α4 INTEGRINS
WO2005112927A1 (en) * 2004-05-21 2005-12-01 Acadia Pharmaceuticals Inc. Selective serotonin receptor inverse agonists as therapeutics for disease
WO2006014136A1 (en) * 2004-08-02 2006-02-09 Astrazeneca Ab Piperidine derivatives as histamine h3 receptor ligands
US20070149512A1 (en) * 2005-12-09 2007-06-28 Solvay Pharmaceuticals Gmbh N-Sulfamoyl-piperidineamides for the treatment or inhibition of obesity and related conditions
WO2009039460A2 (en) * 2007-09-21 2009-03-26 Acadia Pharmaceuticals, Inc. Co-administration of pimavanserin with other agents
WO2011060397A1 (en) * 2009-11-16 2011-05-19 Schering Corporation Substituted amino heterocycles useful as hiv antagonists

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
BURROWS, J. N. et al., Bioorganic & Medicinal Chemistry Letters, 2005, Vol. 15, Pages 25-28 *

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