JP2014518543A5 - - Google Patents
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- Publication number
- JP2014518543A5 JP2014518543A5 JP2013555559A JP2013555559A JP2014518543A5 JP 2014518543 A5 JP2014518543 A5 JP 2014518543A5 JP 2013555559 A JP2013555559 A JP 2013555559A JP 2013555559 A JP2013555559 A JP 2013555559A JP 2014518543 A5 JP2014518543 A5 JP 2014518543A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- pharmaceutically acceptable
- alkyl
- acceptable salt
- optionally
- 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.)
- Granted
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- 150000003839 salts Chemical class 0.000 claims 14
- 150000001875 compounds Chemical class 0.000 claims 13
- 125000001424 substituent group Chemical group 0.000 claims 12
- 125000000217 alkyl group Chemical group 0.000 claims 11
- 125000000753 cycloalkyl group Chemical group 0.000 claims 10
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 239000001257 hydrogen Substances 0.000 claims 10
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 10
- 125000003710 aryl alkyl group Chemical group 0.000 claims 9
- 125000003118 aryl group Chemical group 0.000 claims 9
- 125000001072 heteroaryl group Chemical group 0.000 claims 9
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 9
- 125000003342 alkenyl group Chemical group 0.000 claims 7
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 7
- 125000005885 heterocycloalkylalkyl group Chemical group 0.000 claims 7
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 125000004429 atom Chemical group 0.000 claims 4
- 125000002619 bicyclic group Chemical group 0.000 claims 4
- -1 carbocycle Chemical group 0.000 claims 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 125000002950 monocyclic group Chemical group 0.000 claims 4
- 125000000169 tricyclic heterocycle group Chemical group 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 3
- 229910052736 halogen Inorganic materials 0.000 claims 3
- 150000002367 halogens Chemical class 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 3
- 102000000393 Ghrelin Receptors Human genes 0.000 claims 2
- 108010016122 Ghrelin Receptors Proteins 0.000 claims 2
- UFWIBTONFRDIAS-UHFFFAOYSA-N Naphthalene Chemical group C1=CC=CC2=CC=CC=C21 UFWIBTONFRDIAS-UHFFFAOYSA-N 0.000 claims 2
- 206010033799 Paralysis Diseases 0.000 claims 2
- 206010054048 Postoperative ileus Diseases 0.000 claims 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 2
- 125000001309 chloro group Chemical group Cl* 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 230000002496 gastric effect Effects 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
- WGIAKIIMCPKJQN-SFVWDYPZSA-N 3-[(1s)-1-(2,3-dichloro-4-methoxyphenyl)ethyl]-1-methyl-1-(1,3,3-trimethylpiperidin-4-yl)urea Chemical compound ClC1=C(Cl)C(OC)=CC=C1[C@H](C)NC(=O)N(C)C1C(C)(C)CN(C)CC1 WGIAKIIMCPKJQN-SFVWDYPZSA-N 0.000 claims 1
- 208000030507 AIDS Diseases 0.000 claims 1
- 208000000103 Anorexia Nervosa Diseases 0.000 claims 1
- 206010006895 Cachexia Diseases 0.000 claims 1
- 206010007559 Cardiac failure congestive Diseases 0.000 claims 1
- 206010010774 Constipation Diseases 0.000 claims 1
- 208000007882 Gastritis Diseases 0.000 claims 1
- 206010019280 Heart failures Diseases 0.000 claims 1
- 206010028813 Nausea Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000030053 Opioid-Induced Constipation Diseases 0.000 claims 1
- 208000002193 Pain Diseases 0.000 claims 1
- 201000010769 Prader-Willi syndrome Diseases 0.000 claims 1
- 208000001647 Renal Insufficiency Diseases 0.000 claims 1
- 206010047700 Vomiting Diseases 0.000 claims 1
- 230000032683 aging Effects 0.000 claims 1
- 125000001246 bromo group Chemical group Br* 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000002837 carbocyclic group Chemical group 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 201000006549 dyspepsia Diseases 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 208000021302 gastroesophageal reflux disease Diseases 0.000 claims 1
- 230000005176 gastrointestinal motility Effects 0.000 claims 1
- 125000004438 haloalkoxy group Chemical group 0.000 claims 1
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 1
- 201000006370 kidney failure Diseases 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 230000008693 nausea Effects 0.000 claims 1
- 230000036407 pain Effects 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 238000006467 substitution reaction Methods 0.000 claims 1
- 230000008673 vomiting Effects 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNPCT/CN2011/00298 | 2011-02-25 | ||
| PCT/CN2011/000298 WO2012113103A1 (en) | 2011-02-25 | 2011-02-25 | Asymmetric ureas and medical uses thereof |
| 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 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014518543A JP2014518543A (ja) | 2014-07-31 |
| JP2014518543A5 true JP2014518543A5 (enExample) | 2015-03-19 |
| JP6077468B2 JP6077468B2 (ja) | 2017-02-08 |
Family
ID=46719417
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013555559A Active JP6077468B2 (ja) | 2011-02-25 | 2012-02-23 | 不斉尿素及びその医学的用途 |
Country Status (41)
Families Citing this family (14)
| 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 |
| CA2896076C (en) | 2012-12-21 | 2022-12-06 | Aveo Pharmaceuticals, Inc. | Anti-gdf15 antibodies |
| TWI703130B (zh) | 2014-03-07 | 2020-09-01 | 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 |
| 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 |
| CA3017048C (en) | 2016-03-22 | 2023-11-07 | Helsinn Healthcare Sa | Benzenesulfonyl-asymmetric ureas and medical uses thereof |
| EP3679930A4 (en) * | 2017-08-07 | 2021-11-17 | Hiroshima University | THERAPEUTIC FOR FATTY LIVER DISEASES AND THERAPEUTIC FOR OBESITY |
| EP3672960A2 (en) | 2017-08-21 | 2020-07-01 | Acadia Pharmaceuticals Inc. | Compounds, salts thereof and their use for the treatment of diseases |
| MX2020001757A (es) | 2017-08-21 | 2020-09-07 | Acadia Pharm Inc | Compuestos, sales de los mismos y metodos para el tratamiento de enfermedades. |
| IL275153B2 (en) | 2017-12-11 | 2024-12-01 | Helsinn Healthcare Sa | Fumarate salts 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 for their preparation and use |
| EP3542799A1 (en) | 2018-03-22 | 2019-09-25 | Helsinn Healthcare SA | New centrally-active ghrelin agonist and medical uses thereof |
| US20240208923A1 (en) | 2021-03-10 | 2024-06-27 | Jnana Therapeutics Inc. | Small molecule inhibitors of mammalian slc6a19 function |
| FI4346820T3 (fi) | 2021-06-02 | 2025-07-03 | Helsinn Healthcare Sa | Inotrooppisina aineina käytettävät piperidiiniureajohdannaiset |
| WO2023048762A1 (en) * | 2021-09-22 | 2023-03-30 | Duke University | Compositions for the treatment of food and chemical addiction and methods of making and using same |
| WO2024158862A1 (en) * | 2023-01-25 | 2024-08-02 | University Of North Texas Health Science Center | Thiourea antioxcompounds with neuroprotective activity |
Family Cites Families (43)
| 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 |
| WO1995006635A1 (en) | 1993-09-02 | 1995-03-09 | 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 |
| EP1263729B1 (en) * | 2000-03-06 | 2006-12-20 | Acadia Pharmaceuticals Inc. | Azacyclic compounds for use in the treatment of serotonin related diseases |
| GB0011838D0 (en) * | 2000-05-17 | 2000-07-05 | Astrazeneca Ab | Chemical compounds |
| US20030022891A1 (en) * | 2000-12-01 | 2003-01-30 | Anandan Palani | MCH antagonists and their use in the treatment of obesity |
| EP1368314A1 (en) | 2001-03-01 | 2003-12-10 | AstraZeneca AB | 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 |
| WO2004024720A1 (en) * | 2002-09-11 | 2004-03-25 | Merck & Co., Inc. | Piperazine urea derivatives as melanocortin-4 receptor agonists |
| JPWO2004046110A1 (ja) | 2002-11-15 | 2006-03-16 | アステラス製薬株式会社 | メラニン凝集ホルモン受容体拮抗剤 |
| JP4384635B2 (ja) * | 2003-06-30 | 2009-12-16 | 住友化学株式会社 | 不斉尿素化合物およびこれを触媒として用いる不斉共役付加反応による不斉化合物の製造方法 |
| US7115767B2 (en) * | 2003-07-18 | 2006-10-03 | Abbott Laboratories | Tetraline derivatives as ghrelin receptor modulators |
| DE602005002251D1 (de) * | 2004-02-10 | 2007-10-11 | Janssen Pharmaceutica Nv | Pyridazinonharnstoffe als antagonisten von a4-integrinen |
| US20050261278A1 (en) * | 2004-05-21 | 2005-11-24 | Weiner David M | Selective serotonin receptor inverse agonists as therapeutics for disease |
| 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 |
| SE0401971D0 (sv) * | 2004-08-02 | 2004-08-02 | Astrazeneca Ab | Piperidne derivatives |
| CA2577060A1 (en) * | 2004-08-13 | 2006-02-23 | Amgen Inc. | Substituted benzofused heterocycles |
| US20090239841A1 (en) * | 2004-10-27 | 2009-09-24 | Hutchison Alan J | Diaryl Ureas as CB1 Antagonists |
| EP1831194A4 (en) | 2004-12-21 | 2009-12-02 | Astrazeneca Ab | HETEROCYCLIC ANTAGONISTS OF MCHr1 AND THERAPEUTIC APPLICATIONS THEREOF |
| US7829589B2 (en) | 2005-06-10 | 2010-11-09 | Elixir Pharmaceuticals, Inc. | Sulfonamide compounds and uses thereof |
| WO2007029086A2 (en) * | 2005-09-05 | 2007-03-15 | Ranbaxy Laboratories Limited | Derivatives of 3-azabicyclo[3.1.0]hexane as dipeptidyl peptidase-iv inhibitors |
| KR20080076916A (ko) * | 2005-11-01 | 2008-08-20 | 트랜스테크 파르마, 인크. | 치환된 아미드의 약학적 사용 |
| AR058277A1 (es) * | 2005-12-09 | 2008-01-30 | Solvay Pharm Gmbh | N- sulfamoil - piperidin - amidas, composiciones farmaceuticas que las comprenden y procedimiento para su preparacion |
| AU2007273057A1 (en) | 2006-07-12 | 2008-01-17 | Merck Sharp & Dohme Corp. | 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 |
| GB0710865D0 (en) | 2007-06-06 | 2007-07-18 | Glaxo Group Ltd | Novel compounds |
| GB0710863D0 (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 |
| JP2010540454A (ja) * | 2007-09-21 | 2010-12-24 | アカディア ファーマシューティカルズ，インコーポレーテッド | ピマバンセリンと他の薬剤との併用投与 |
| UA100527C2 (en) * | 2007-10-10 | 2013-01-10 | Астразенека Аб | Benzothiazoles as ghrelin receptor modulators |
| WO2009089659A1 (en) | 2008-01-18 | 2009-07-23 | Shanghai Targetdrug Co., Ltd. | Pyrollidine-based compounds |
| WO2009092293A1 (en) | 2008-01-18 | 2009-07-30 | Shanghai Targetdrug Co., Ltd. | Pyrollidine-based compounds |
| JP5580741B2 (ja) * | 2008-09-19 | 2014-08-27 | 武田薬品工業株式会社 | 含窒素複素環化合物およびその用途 |
| WO2010111353A1 (en) * | 2009-03-25 | 2010-09-30 | Acadia Pharmaceuticals, Inc. | N-substituted piperidine derivatives as serotonin receptor agents |
| WO2011060397A1 (en) * | 2009-11-16 | 2011-05-19 | Schering Corporation | Substituted amino heterocycles useful as hiv antagonists |
| WO2012113103A1 (en) * | 2011-02-25 | 2012-08-30 | Helsinn Healthcare S.A. | Asymmetric ureas and medical uses thereof |
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2011
- 2011-02-25 WO PCT/CN2011/000298 patent/WO2012113103A1/en not_active Ceased
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2012
- 2012-02-23 MX MX2013006974A patent/MX347587B/es active IP Right Grant
- 2012-02-23 WO PCT/US2012/026315 patent/WO2012116176A2/en not_active Ceased
- 2012-02-23 PL PL12749383T patent/PL2678017T3/pl unknown
- 2012-02-23 LT LTEP12749383.1T patent/LT2678017T/lt unknown
- 2012-02-23 AU AU2012220531A patent/AU2012220531B2/en active Active
- 2012-02-23 GE GEAP201213239A patent/GEP20156319B/en unknown
- 2012-02-23 DK DK12749383.1T patent/DK2678017T3/en active
- 2012-02-23 BR BR112013021566-6A patent/BR112013021566B1/pt active IP Right Grant
- 2012-02-23 PE PE2013001934A patent/PE20141000A1/es active IP Right Grant
- 2012-02-23 SM SM20170407T patent/SMT201700407T1/it unknown
- 2012-02-23 MY MYPI2013003013A patent/MY164354A/en unknown
- 2012-02-23 AP AP2013007123A patent/AP3768A/en active
- 2012-02-23 EA EA201300946A patent/EA027374B1/ru unknown
- 2012-02-23 MA MA36252A patent/MA34968B1/fr unknown
- 2012-02-23 PT PT127493831T patent/PT2678017T/pt unknown
- 2012-02-23 EP EP12749383.1A patent/EP2678017B1/en active Active
- 2012-02-23 ME MEP-2017-123A patent/ME02845B/me unknown
- 2012-02-23 KR KR1020137025184A patent/KR20140014186A/ko not_active Withdrawn
- 2012-02-23 SG SG2013056775A patent/SG192138A1/en unknown
- 2012-02-23 PH PH1/2013/501757A patent/PH12013501757A1/en unknown
- 2012-02-23 CN CN201280008805.XA patent/CN103874492B/zh active Active
- 2012-02-23 JP JP2013555559A patent/JP6077468B2/ja active Active
- 2012-02-23 HR HRP20170997TT patent/HRP20170997T1/hr unknown
- 2012-02-23 SI SI201230981A patent/SI2678017T1/sl unknown
- 2012-02-23 ES ES12749383.1T patent/ES2628386T3/es active Active
- 2012-02-23 KR KR1020187017910A patent/KR101907573B1/ko active Active
- 2012-02-23 CN CN201611088800.9A patent/CN106995403B/zh active Active
- 2012-02-23 HU HUE12749383A patent/HUE035039T2/en unknown
- 2012-02-23 RS RS20170546A patent/RS56033B1/sr unknown
- 2012-02-23 CA CA2820767A patent/CA2820767C/en active Active
- 2012-02-23 UA UAA201311289A patent/UA113510C2/uk unknown
- 2012-02-24 TW TW101106171A patent/TWI579273B/zh active
- 2012-02-24 AR ARP120100611A patent/AR085398A1/es active IP Right Grant
- 2012-02-24 US US13/404,165 patent/US8658797B2/en active Active
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2013
- 2013-08-13 IL IL227941A patent/IL227941A/en active IP Right Grant
- 2013-08-15 NI NI201300070A patent/NI201300070A/es unknown
- 2013-08-16 TN TNP2013000346A patent/TN2013000346A1/fr unknown
- 2013-08-21 CL CL2013002412A patent/CL2013002412A1/es unknown
- 2013-08-23 DO DO2013000195A patent/DOP2013000195A/es unknown
- 2013-09-19 ZA ZA2013/07071A patent/ZA201307071B/en unknown
- 2013-09-24 EC EC2013012893A patent/ECSP13012893A/es unknown
- 2013-09-24 CO CO13226995A patent/CO6771450A2/es unknown
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2014
- 2014-01-08 US US14/150,360 patent/US9751836B2/en active Active
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2017
- 2017-06-19 CY CY20171100635T patent/CY1118947T1/el unknown
- 2017-07-30 US US15/663,761 patent/US10407390B2/en active Active