AR086554A1 - 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
- AR086554A1 AR086554A1 ARP120101842A ARP120101842A AR086554A1 AR 086554 A1 AR086554 A1 AR 086554A1 AR P120101842 A ARP120101842 A AR P120101842A AR P120101842 A ARP120101842 A AR P120101842A AR 086554 A1 AR086554 A1 AR 086554A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- cra1ra2
- membered
- hydrogen
- independently selected
- Prior art date
Links
Classifications
-
- 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
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- 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)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (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
Procedimientos para la preparación de tales derivados, composiciones farmacéuticas que comprenden tales derivados, tales derivados como un medicamento, tales derivados para el tratamiento de un trastorno o una enfermedad mediada por el receptor de la ghrelina.Reivindicación 1: Un compuesto de la fórmula (1), en donde - - - - - es un enlace sencillo o un enlace doble; X1 es (CRx1H)n y X2 es (CH); ó X1 es (CRx1H)n y X2 es N; ó X1 es NRx1 y X2 es (CH); ó X1 es NRx1 y X2 es N; ó X1 es N y X2 es C; en donde el enlace entre X1 y X2 es un enlace doble si X1 es N y X2 es C; n es 0 ó 1; Rx1 se selecciona a partir de hidrógeno y alquilo C1-6; m es 1 y p es 0; ó m es 1 y p es 1;ó m es 2 y p es 1; Y es NR1 u O; R1 se selecciona a partir de hidrógeno, alquilo C1-6, -alquil C1-4C(O)NR1aR1b, -alquil C1-4C(O)O-alquilo C1-4, -alquil C1-4C(O)O-haloalquilo C1-4, haloalquilo C1-6, cicloalquilo C3-6, -alquil C1-4-heteroarilo de 5 - 6 miembros, hidroxialquilo C1-6, alcoxilo C1-6 y alcoxi C1-4-alquilo C1-4; en donde el heteroarilo de 5 - 6 miembros es sustituido o no sustituido por 1 a 3 sustituyentes independientemente seleccionados a partir de halógeno y alquilo C1-6; R1a y R1b son independientemente seleccionados a partir de hidrógeno, alquilo C1-6 y haloalquilo C1-6; ó R1a y R1b junto con el nitrógeno al cual se fijan forman un anillo heterocíclico de 4 - 6 miembros que contiene 0, 1 ó 2 heteroátomos adicionales seleccionados a partir de oxígeno, nitrógeno y azufre; R2a se selecciona a partir de (i) -A-fenilo; (ii) -A-heteroarilo de 5 - 6 miembros; (iii) -A-heterociclilo de 4 - 6 miembros; (iv) -A-cicloalquilo C5-6; (v) -D-sistema de anillo bicíclico condensado de 8 - 10 miembros; en donde el fenilo, heteroarilo de 5 - 6 miembros, heterociclilo de 4 - 6 miembros, cicloalquilo C5-6 y sistema de anillo bicíclico condensado de 8 - 10 miembros son sustituidos o no sustituidos por 1 a 3 sustituyentes independientemente seleccionados a partir de halógeno, hidroxilo, alquilo C1-6, alcoxilo C1-6 y haloalquilo C1-6; A se selecciona a partir de un enlace, -(CRA1RA2), -(CRA1RA2)(CRA1RA2), -(CRA1RA2)-O-, -O-(CRA1RA2), -(CRA1RA2)-S-, -(CRA1RA2)-S(O)-, -(CRA1RA2)-S(O)2-, -S-(CRA1RA2)-, -S(O)-(CRA1RA2)-, -S(O)2-(CRA1RA2)-, -NRA3-(CRA1RA2), -(CRA1RA2)-NRA3- y -(CRA1)=(CRA1)-; D es un enlace, -O- ó -(CRD1RD2)-; RA1, RA2 y RA3 son independientemente seleccionados a partir de hidrógeno, alquilo C1-6 y halógeno; RD1 y RD2 son independientemente seleccionados a partir de hidrógeno, alquilo C1-6 y halógeno; R2b es hidrógeno ó alquilo C1-4; R3 y R4 son independientemente seleccionados a partir de hidrógeno, alquilo C1-6 y cicloalquilo C3-6; ó R3 y R4 junto con el nitrógeno al cual se fijan forman un anillo heterocíclico de 4 - 6 miembros que contiene 0, 1 ó 2 heteroátomos adicionales seleccionados a partir de oxígeno, nitrógeno y azufre; tal anillo heterocíclico de 4 - 6 miembros es sustituido o no sustituido por 1 ó 2 sustituyentes de halógeno; R6 y R7 son independientemente seleccionados a partir de hidrógeno, alquilo C1-6, hidroxialquilo C1-6 y haloalquilo C1-6; R5 se selecciona a partir de fenilo, un heteroarilo de 5 - 6 miembros, cicloalquilo C3-6 y heterociclilo de 4 - 6 miembros; tal fenilo, heteroarilo de 5 - 6 miembros, cicloalquilo C3-6 y heterociclilo de 4 - 6 miembros es sustituido o no sustituido por 1 a 3 sustituyentes independientemente seleccionados a partir de halógeno, alquilo C1-6, alcoxilo C1-6 y haloalquilo C1-6; o una sal farmacéuticamente aceptable de los mismos.
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 |
---|---|
AR086554A1 true AR086554A1 (es) | 2014-01-08 |
Family
ID=46317469
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP120101842A AR086554A1 (es) | 2011-05-27 | 2012-05-24 | Derivados de la piperidina 3-espirociclica como agonistas de receptores de la ghrelina |
Country Status (21)
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) |
SG (1) | SG194616A1 (es) |
TW (1) | TW201302749A (es) |
UY (1) | UY34094A (es) |
WO (1) | WO2012164473A1 (es) |
Families Citing this family (8)
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AU2013255458A1 (en) * | 2012-05-03 | 2014-10-09 | Novartis Ag | L-malate salt of 2, 7 - diaza - spiro [4.5 ] dec- 7 - yle derivatives and crystalline forms thereof as ghrelin receptor agonists |
EP3378472A1 (en) * | 2012-08-09 | 2018-09-26 | Dynamis Therapeutics, Inc. | Combinations of meglumine |
KR20160133004A (ko) | 2014-04-04 | 2016-11-21 | 엑스-알엑스, 인크. | 오토탁신의 치환된 스피로시클릭 억제제 |
TW201625613A (zh) | 2014-10-31 | 2016-07-16 | 拉夸里亞創藥股份有限公司 | 作為生長激素釋放肽受體激動劑之四氫吡唑並吡啶衍生物 |
JP2020519639A (ja) * | 2017-05-12 | 2020-07-02 | ミレニアム ファーマシューティカルズ, インコーポレイテッドMillennium Pharmaceuticals, Inc. | トリアザスピロ[4.5]デカノンによる胃不全麻痺の処置 |
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 |
US11993600B2 (en) * | 2021-12-08 | 2024-05-28 | Enanta Pharmaceuticals, Inc. | Saturated spirocyclics as antiviral agents |
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2012
- 2012-05-24 AR ARP120101842A patent/AR086554A1/es unknown
- 2012-05-24 UY UY0001034094A patent/UY34094A/es not_active Application Discontinuation
- 2012-05-24 US US13/479,596 patent/US8546416B2/en active Active
- 2012-05-25 JP JP2014512000A patent/JP2014515369A/ja active Pending
- 2012-05-25 AU AU2012264305A patent/AU2012264305A1/en not_active Abandoned
- 2012-05-25 KR KR1020137034118A patent/KR20140023399A/ko not_active Application Discontinuation
- 2012-05-25 TW TW101118859A patent/TW201302749A/zh unknown
- 2012-05-25 CA CA2835916A patent/CA2835916A1/en not_active Abandoned
- 2012-05-25 BR BR112013030391A patent/BR112013030391A2/pt not_active Application Discontinuation
- 2012-05-25 PE PE2013002562A patent/PE20140610A1/es not_active Application Discontinuation
- 2012-05-25 AP AP2013007234A patent/AP2013007234A0/xx unknown
- 2012-05-25 WO PCT/IB2012/052649 patent/WO2012164473A1/en active Application Filing
- 2012-05-25 MX MX2013013950A patent/MX355072B/es active IP Right Grant
- 2012-05-25 EP EP12727947.9A patent/EP2714690A1/en not_active Withdrawn
- 2012-05-25 SG SG2013079082A patent/SG194616A1/en unknown
- 2012-05-25 EA EA201391797A patent/EA201391797A1/ru unknown
- 2012-05-25 CN CN201280025862.9A patent/CN103562206A/zh active Pending
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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
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Also Published As
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JP2014515369A (ja) | 2014-06-30 |
IL229320A0 (en) | 2014-01-30 |
US20120302540A1 (en) | 2012-11-29 |
KR20140023399A (ko) | 2014-02-26 |
CN103562206A (zh) | 2014-02-05 |
UY34094A (es) | 2013-01-03 |
MX355072B (es) | 2018-04-04 |
WO2012164473A1 (en) | 2012-12-06 |
CL2013003211A1 (es) | 2014-07-04 |
SG194616A1 (en) | 2013-12-30 |
EP2714690A1 (en) | 2014-04-09 |
AP2013007234A0 (en) | 2013-11-30 |
AU2012264305A1 (en) | 2013-11-21 |
CA2835916A1 (en) | 2012-12-06 |
US8546416B2 (en) | 2013-10-01 |
PE20140610A1 (es) | 2014-05-31 |
CR20130625A (es) | 2014-02-04 |
US20130331369A1 (en) | 2013-12-12 |
EA201391797A1 (ru) | 2014-04-30 |
BR112013030391A2 (pt) | 2016-12-13 |
CO6811856A2 (es) | 2013-12-16 |
MX2013013950A (es) | 2014-01-23 |
TW201302749A (zh) | 2013-01-16 |
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