PE20140610A1 - Derivados de la piperidina 3-espirociclica como agonistas de receptores de la ghrelina - Google Patents
Derivados de la piperidina 3-espirociclica como agonistas de receptores de la ghrelinaInfo
- Publication number
- PE20140610A1 PE20140610A1 PE2013002562A PE2013002562A PE20140610A1 PE 20140610 A1 PE20140610 A1 PE 20140610A1 PE 2013002562 A PE2013002562 A PE 2013002562A PE 2013002562 A PE2013002562 A PE 2013002562A PE 20140610 A1 PE20140610 A1 PE 20140610A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- cycloalkyl
- oxo
- phenyl
- piperidine
- Prior art date
Links
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical class C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 title abstract 3
- 102000000393 Ghrelin Receptors Human genes 0.000 title abstract 2
- 108010016122 Ghrelin Receptors Proteins 0.000 title abstract 2
- 239000000556 agonist Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- -1 BENZYLOXY Chemical class 0.000 abstract 2
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical group [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 1
- 201000006549 dyspepsia Diseases 0.000 abstract 1
- 210000000936 intestine Anatomy 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 239000000018 receptor agonist Substances 0.000 abstract 1
- 229940044601 receptor agonist Drugs 0.000 abstract 1
- 208000011580 syndromic disease Diseases 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/10—Spiro-condensed systems
-
- 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
- A61K31/40—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
- A61K31/407—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 other heterocyclic ring systems, e.g. ketorolac, physostigmine
-
- 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
- A61K31/435—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
-
- 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
- A61K31/435—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
- A61K31/438—The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/10—Laxatives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/10—Spiro-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Nutrition Science (AREA)
- Hospice & Palliative Care (AREA)
- Otolaryngology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Hydrogenated Pyridines (AREA)
Abstract
SE REFIERE A COMPUESTOS DERIVADOS DE PIPERIDINA 3-ESPIROCICLICA DE FORMULA (I) DONDE X1 ES (CRx1H)n, NRx1 O N, EN DONDE Rx1 ES H O ALQUILO(C1-C6); n ES 0 O 1; X2 ES CH, N O C; m ES 1 O 2; p ES 0 O 1; Y ES NR1 U O, EN DONDE R1 ES H, ALQUILO(C1-C6), HALOALQUILO(C1-C6), CICLOALQUILO(C3-C6), ENTRE OTROS; R2a ES -A-FENILO, -A-HETEROARILO DE 5 A 6 MIEMBROS, -A-CICLOALQUILO(C5-C6), ENTRE OTROS, EN DONDE A ES UN ENLACE, ENTRE OTROS; R2b ES H O ALQUILO(C1-C4); R3 Y R4 SON CADA UNO H, ALQUILO(C1-C6), CICLOALQUILO(C3-C6), ENTRE OTROS; R6 Y R7 SON CADA UNO H, ALQUILO(C1-C6), HIDROXIALQUILO(C1-C6) O HALOALQUILO(C1-C6); R5 ES FENILO, HETEROARILO DE 5 A 6 MIEMBROS; CICLOALQUILO(C3-C6), ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 2-AMINO-N-[(R)-1-BENCILOXIMETIL-2-(2-METIL-1-OXO-4-FENIL-2,7-DIAZA-ESPIRO[4.5]DEC-7-IL)-2-OXO-ETIL]-2-METIL-PROPIONAMIDA; 2-AMINO-N-((2R)-3-(BENCILOXI)-1-(4-(4-FLUOROFENIL)-2-METIL-1-OXO-2,7-DIAZAESPIRO[4.5]DECAN-7-IL)-1-OXOPROPAN-2-IL)-2-METILPROPANAMIDA; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON AGONISTAS DE RECEPTORES DE LA GHRELINA SIENDO UTILES EN EL TRATAMIENTO DE GASTROPARESIA, DISPEPSIA FUNCIONAL, SINDROME DEL INTESTINO CORTO
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161490848P | 2011-05-27 | 2011-05-27 | |
| US201161560960P | 2011-11-17 | 2011-11-17 | |
| US201261642116P | 2012-05-03 | 2012-05-03 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20140610A1 true PE20140610A1 (es) | 2014-05-31 |
Family
ID=46317469
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2013002562A PE20140610A1 (es) | 2011-05-27 | 2012-05-25 | Derivados de la piperidina 3-espirociclica como agonistas de receptores de la ghrelina |
Country Status (22)
| Country | Link |
|---|---|
| US (2) | US8546416B2 (es) |
| EP (1) | EP2714690A1 (es) |
| JP (1) | JP2014515369A (es) |
| KR (1) | KR20140023399A (es) |
| CN (1) | CN103562206A (es) |
| AP (1) | AP2013007234A0 (es) |
| AR (1) | AR086554A1 (es) |
| AU (1) | AU2012264305A1 (es) |
| BR (1) | BR112013030391A2 (es) |
| CA (1) | CA2835916A1 (es) |
| CL (1) | CL2013003211A1 (es) |
| CO (1) | CO6811856A2 (es) |
| CR (1) | CR20130625A (es) |
| EA (1) | EA201391797A1 (es) |
| IL (1) | IL229320A0 (es) |
| MX (1) | MX355072B (es) |
| PE (1) | PE20140610A1 (es) |
| PH (1) | PH12013502204A1 (es) |
| SG (1) | SG194616A1 (es) |
| TW (1) | TW201302749A (es) |
| UY (1) | UY34094A (es) |
| WO (1) | WO2012164473A1 (es) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2867043A1 (en) * | 2012-05-03 | 2013-11-07 | Novartis Ag | L-malate salt of 2,7-diaza-spiro[4.5]dec-7-yle derivatives and crystalline forms thereof as ghrelin receptor agonists |
| CN104768544B (zh) * | 2012-08-09 | 2017-06-16 | 迪纳米斯治疗公司 | 包括葡甲胺或其盐的组合物在制备减少或预防甘油三酯水平增加的药物中的应用 |
| WO2015154023A1 (en) | 2014-04-04 | 2015-10-08 | X-Rx Discovery, Inc. | Substituted spirocydic inhibitors of autotaxin |
| WO2016067638A1 (en) * | 2014-10-31 | 2016-05-06 | Raqualia Pharma Inc. | Tetrahydropyrazolopyridine derivatives as ghrelin receptor agonists |
| CA3062880A1 (en) * | 2017-05-12 | 2018-11-15 | Millennium Pharmaceuticals, Inc. | Treatment of gastroparesis with triazaspiro[4.5]decanone |
| CN111175387B (zh) * | 2018-11-13 | 2022-06-07 | 成都康弘药业集团股份有限公司 | 一种米那普仑异构体的检测方法 |
| CN113125583B (zh) * | 2019-12-30 | 2022-06-21 | 成都百裕制药股份有限公司 | 一种注射用泮托拉唑钠中基因毒性杂质含量的检测方法 |
| WO2022109363A1 (en) * | 2020-11-23 | 2022-05-27 | Enanta Pharmaceuticals, Inc. | Novel spiropyrrolidine derived antiviral agents |
| CN116806150A (zh) * | 2021-01-05 | 2023-09-26 | 载度思生命科学有限公司 | 新的自分泌运动因子抑制剂 |
| US12398147B2 (en) | 2021-05-11 | 2025-08-26 | Enanta Pharmaceuticals, Inc. | Macrocyclic spiropyrrolidine derived antiviral agents |
| US12479854B2 (en) | 2021-07-29 | 2025-11-25 | Enanta Pharmaceuticals, Inc. | Spiropyrrolidine derived antiviral agents |
| WO2023107417A1 (en) | 2021-12-08 | 2023-06-15 | Enanta Pharmaceuticals, Inc. | Heterocyclic antiviral agents |
| US11993600B2 (en) * | 2021-12-08 | 2024-05-28 | Enanta Pharmaceuticals, Inc. | Saturated spirocyclics as antiviral agents |
| WO2023196307A1 (en) | 2022-04-05 | 2023-10-12 | Enanta Pharmaceuticals, Inc. | Novel spiropyrrolidine derived antiviral agents |
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2012
- 2012-05-24 US US13/479,596 patent/US8546416B2/en active Active
- 2012-05-24 AR ARP120101842A patent/AR086554A1/es unknown
- 2012-05-24 UY UY0001034094A patent/UY34094A/es not_active Application Discontinuation
- 2012-05-25 SG SG2013079082A patent/SG194616A1/en unknown
- 2012-05-25 CA CA2835916A patent/CA2835916A1/en not_active Abandoned
- 2012-05-25 PE PE2013002562A patent/PE20140610A1/es not_active Application Discontinuation
- 2012-05-25 EA EA201391797A patent/EA201391797A1/ru unknown
- 2012-05-25 PH PH1/2013/502204A patent/PH12013502204A1/en unknown
- 2012-05-25 WO PCT/IB2012/052649 patent/WO2012164473A1/en not_active Ceased
- 2012-05-25 AP AP2013007234A patent/AP2013007234A0/xx unknown
- 2012-05-25 MX MX2013013950A patent/MX355072B/es active IP Right Grant
- 2012-05-25 TW TW101118859A patent/TW201302749A/zh unknown
- 2012-05-25 CN CN201280025862.9A patent/CN103562206A/zh active Pending
- 2012-05-25 JP JP2014512000A patent/JP2014515369A/ja active Pending
- 2012-05-25 BR BR112013030391A patent/BR112013030391A2/pt not_active Application Discontinuation
- 2012-05-25 KR KR1020137034118A patent/KR20140023399A/ko not_active Ceased
- 2012-05-25 EP EP12727947.9A patent/EP2714690A1/en not_active Withdrawn
- 2012-05-25 AU AU2012264305A patent/AU2012264305A1/en not_active Abandoned
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2013
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- 2013-11-07 IL IL229320A patent/IL229320A0/en unknown
- 2013-11-08 CL CL2013003211A patent/CL2013003211A1/es unknown
- 2013-11-20 CO CO13273132A patent/CO6811856A2/es active IP Right Grant
- 2013-11-27 CR CR20130625A patent/CR20130625A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| AP2013007234A0 (en) | 2013-11-30 |
| PH12013502204A1 (en) | 2017-10-25 |
| UY34094A (es) | 2013-01-03 |
| CN103562206A (zh) | 2014-02-05 |
| SG194616A1 (en) | 2013-12-30 |
| US20130331369A1 (en) | 2013-12-12 |
| AR086554A1 (es) | 2014-01-08 |
| EP2714690A1 (en) | 2014-04-09 |
| CR20130625A (es) | 2014-02-04 |
| EA201391797A1 (ru) | 2014-04-30 |
| MX355072B (es) | 2018-04-04 |
| BR112013030391A2 (pt) | 2016-12-13 |
| WO2012164473A1 (en) | 2012-12-06 |
| US8546416B2 (en) | 2013-10-01 |
| CL2013003211A1 (es) | 2014-07-04 |
| KR20140023399A (ko) | 2014-02-26 |
| IL229320A0 (en) | 2014-01-30 |
| MX2013013950A (es) | 2014-01-23 |
| JP2014515369A (ja) | 2014-06-30 |
| CO6811856A2 (es) | 2013-12-16 |
| TW201302749A (zh) | 2013-01-16 |
| CA2835916A1 (en) | 2012-12-06 |
| US20120302540A1 (en) | 2012-11-29 |
| AU2012264305A1 (en) | 2013-11-21 |
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