PE20161414A1 - UREAS ASIMETRICAS p-SUSTITUIDAS Y USOS MEDICOS DE LAS MISMAS - Google Patents
UREAS ASIMETRICAS p-SUSTITUIDAS Y USOS MEDICOS DE LAS MISMASInfo
- Publication number
- PE20161414A1 PE20161414A1 PE2016001557A PE2016001557A PE20161414A1 PE 20161414 A1 PE20161414 A1 PE 20161414A1 PE 2016001557 A PE2016001557 A PE 2016001557A PE 2016001557 A PE2016001557 A PE 2016001557A PE 20161414 A1 PE20161414 A1 PE 20161414A1
- Authority
- PE
- Peru
- Prior art keywords
- halo
- alkyl
- medical uses
- ureas
- substituted asymmetric
- Prior art date
Links
- 150000003672 ureas Chemical class 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 3
- -1 1- (2,3-DICHLORO-4-CYCLOPROPYLPHENYL) ETHYL Chemical class 0.000 abstract 2
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 abstract 2
- 239000004202 carbamide Substances 0.000 abstract 2
- 102000000393 Ghrelin Receptors Human genes 0.000 abstract 1
- 108010016122 Ghrelin Receptors Proteins 0.000 abstract 1
- 206010022489 Insulin Resistance Diseases 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 abstract 1
Classifications
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/17—Amides, e.g. hydroxamic acids having the group >N—C(O)—N< or >N—C(S)—N<, e.g. urea, thiourea, carmustine
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- 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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4453—Non condensed piperidines, e.g. piperocaine only substituted in position 1, e.g. propipocaine, diperodon
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- 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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
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- C07F7/0803—Compounds with Si-C or Si-Si linkages
- C07F7/081—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te
- C07F7/0812—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te comprising a heterocyclic ring
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Abstract
SE REFIERE A COMPUESTOS DERIVADOS DE UREAS DE FORMULA (I) DONDE X ES CH O N; Z ES O, ENTRE OTROS; R1 ES H, ALQUILO C1-C6, ENTRE OTROS; R2 ES H O ALQUILO C1-C6; R3 Y R4 SON CADA UNO H, CN, HALO, ENTRE OTROS; R5 ES HALO, CN, CHO, ENTRE OTROS; R6 ESTA AUSENTE O ES H; R7 ES H, CN O HALO; R8 ES H O ALQUILO C1-C6; r ES 1 O 2; s ES DE 0 A 4; n ES DE 0 A 3. SON COMPUESTOS PREFERIDOS: 3-(1-(2,3-DICLORO-4-CICLOPROPILFENIL)ETIL)-1-METIL-1-(1-METILPIPERIDIN-4-IL)UREA; 3-(1-(2,3-DICLORO-4-(DIFLUOROMETIL)FENIL)ETIL)-1-HIDROXI-1-(1-METILPIPERIDIN-4-IL)UREA; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON MODULADORES DEL RECEPTOR DE GHRELINA SIENDO UTILES EN EL TRATAMIENTO DE DIABETES, RESISTENCIA A LA INSULINA
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JP (2) | JP2017507116A (es) |
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CN (2) | CN106170485B (es) |
AP (1) | AP2016009415A0 (es) |
AR (1) | AR099690A1 (es) |
AU (1) | AU2015227011B2 (es) |
BR (1) | BR112016020556B1 (es) |
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CL (1) | CL2016002267A1 (es) |
CR (1) | CR20160458A (es) |
DK (1) | DK3114118T3 (es) |
DO (1) | DOP2016000161A (es) |
EA (1) | EA032847B1 (es) |
ES (1) | ES2820511T3 (es) |
GE (1) | GEP20186908B (es) |
HK (1) | HK1231464A1 (es) |
HR (1) | HRP20201661T1 (es) |
HU (1) | HUE050688T2 (es) |
IL (1) | IL246844B (es) |
MD (1) | MD4780C1 (es) |
MX (1) | MX2016011535A (es) |
MY (1) | MY187441A (es) |
NI (1) | NI201600091A (es) |
PE (1) | PE20161414A1 (es) |
PH (1) | PH12016501483B1 (es) |
PT (1) | PT3114118T (es) |
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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 |
EP3724176B1 (en) | 2017-12-11 | 2022-01-26 | 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 |
EP4186893A1 (en) * | 2020-07-22 | 2023-05-31 | Geneora Pharma (Shijiazhuang) Co., Ltd. | 5-ht2a receptor inhibitor or inverse agonist, preparation method therefor, and application thereof |
CA3221574A1 (en) | 2021-06-02 | 2022-12-08 | Helsinn Healthcare Sa | Piperidine urea derivatives for use as inotropic agents |
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DK171732B1 (da) * | 1996-05-01 | 1997-04-21 | Georg Fischer Disa As | Indretning af støbeindløbssystem med efterfødningsreservoir i en indløbskanal til efterfødning af støbegods samt fremgangsmåde til udformning af støbeindløbssystem |
US6399619B1 (en) * | 1999-04-06 | 2002-06-04 | Merck & Co., Inc. | Pyrrolidine modulators of chemokine receptor activity |
SE0103818D0 (sv) * | 2001-11-15 | 2001-11-15 | Astrazeneca Ab | Chemical compounds |
CA2512639C (en) * | 2003-01-16 | 2012-10-30 | Acadia Pharmaceuticals Inc. | Selective serotonin 2a/2c receptor inverse agonists as therapeutics for neurodegenerative diseases |
SE0401971D0 (sv) * | 2004-08-02 | 2004-08-02 | Astrazeneca Ab | Piperidne derivatives |
MX2009009754A (es) * | 2007-03-13 | 2009-09-24 | Arete Therapeutics Inc | Compuestos de 4-piperidinilurea como inhibidores de epoxido hidrolasa soluble. |
US20090082342A1 (en) * | 2007-09-21 | 2009-03-26 | Acadia Pharmaceuticals, Inc. | N-substituted piperidine derivatives as serotonin receptor agents |
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 |
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 |
CN103086925B (zh) * | 2011-11-04 | 2016-07-06 | 浙江海正药业股份有限公司 | 具有抗癌活性的苯甲酰脲衍生物及其制备方法和用途 |
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 |
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