PE20050772A1 - Piperidinilcarbonil-pirrolidinas como agonistas de melanocortina - Google Patents

Piperidinilcarbonil-pirrolidinas como agonistas de melanocortina

Info

Publication number
PE20050772A1
PE20050772A1 PE2005000122A PE2005000122A PE20050772A1 PE 20050772 A1 PE20050772 A1 PE 20050772A1 PE 2005000122 A PE2005000122 A PE 2005000122A PE 2005000122 A PE2005000122 A PE 2005000122A PE 20050772 A1 PE20050772 A1 PE 20050772A1
Authority
PE
Peru
Prior art keywords
alkyl
agonists
terc
difluorophenyl
pyrrolidin
Prior art date
Application number
PE2005000122A
Other languages
English (en)
Inventor
Andrew Antony Calabrese
David Sebastien Fradet
Mark Lansdell
David Hepworth
Original Assignee
Pfizer
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34864830&utm_source=***_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20050772(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority claimed from GB0412417A external-priority patent/GB0412417D0/en
Priority claimed from GB0425530A external-priority patent/GB0425530D0/en
Application filed by Pfizer filed Critical Pfizer
Publication of PE20050772A1 publication Critical patent/PE20050772A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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 containing two hetero rings
    • C07D401/06Heterocyclic 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 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10Drugs for genital or sexual disorders; Contraceptives for impotence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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 containing three or more hetero rings

Abstract

SE REFIERE A UN COMPUESTO DE FORMULA I DONDE R1 ES ALQUILO C1-C6, ALQUENILO C2-C6, ALQUINILO C2-C6, CICLOALQUILO C3-C8, CICLOALQUENILO C5-C8, ARILO, ENTRE OTROS; R2 ES H, OH, OCH3; R3 ES H, ALQUILO C1-C6, ALQUENILO C2-C6, ALQUINILO C2-C6, CICLOALQUILO C3-C8, ENTRE OTROS; R4 ES H, ALQUILO C1-C4, ALQUENILO C2-C4, ENTRE OTROS; R5 SON ALQUILO C1-C4, ALQUENILO C2-C4, ALQUINILO C2-C4, ENTRE OTROS; R4 Y R5 JUNTOS FORMAN UN ANILLO SATURADO O IINSATURADO DE 5 A 7 MIEMBROS. SON COMPUESTOS PREFERIDOS: (3R,4R,5S)-1-{[(3s,4R)-1-TERC-BUTIL-4-(2,4-DIFLUOROFENIL)PIRROLIDIN-3-IL]CARBONIL}-3,5-DIMETIL-4-FENILPIPERIDIN-4-OL CONOCIDO COMO [1-TERC-BUTIL-4-(2,4-DIFLUOROFENIL)-PIRROLIDIN-3-IL]-(4-HIDROXI-3,5-DIMETIL-4-FENIL-PIPERIDIN-1-IL)-METANONA Y SALES DE ACIDOS FARMACEUTICAMENTE ACPETABLES, HIDRATOS O SOLVATOS DEL MISMO. SE REFIERE TAMBIEN A UN PROCESO PARA LA PREPARACION Y UNA COMPOSICION FARMACEUTICA. LOS COMPUESTOS MENCIONADOS SON AGONISTAS SELECTIVOS DE MELANOCORTINA CR4 (MCR4) UTILES EN EL TRATAMIENTO DE DISFUNCION SEXUAL
PE2005000122A 2004-02-04 2005-02-02 Piperidinilcarbonil-pirrolidinas como agonistas de melanocortina PE20050772A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB0402492.3A GB0402492D0 (en) 2004-02-04 2004-02-04 Pharmaceutically active compounds
GB0412417A GB0412417D0 (en) 2004-06-03 2004-06-03 Pharmaceutically active compounds
GB0425530A GB0425530D0 (en) 2004-11-19 2004-11-19 Pharmaceutically active compounds

Publications (1)

Publication Number Publication Date
PE20050772A1 true PE20050772A1 (es) 2005-10-31

Family

ID=34864830

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2005000122A PE20050772A1 (es) 2004-02-04 2005-02-02 Piperidinilcarbonil-pirrolidinas como agonistas de melanocortina

Country Status (25)

Country Link
EP (1) EP1716135B1 (es)
JP (1) JP4031814B2 (es)
KR (1) KR100830763B1 (es)
CN (1) CN1930146A (es)
AP (1) AP2006003699A0 (es)
AR (1) AR048232A1 (es)
AT (1) ATE511507T1 (es)
AU (1) AU2005213538A1 (es)
BR (1) BRPI0507435A (es)
CA (1) CA2555800C (es)
CR (1) CR8545A (es)
EA (1) EA011159B1 (es)
EC (1) ECSP066751A (es)
GB (1) GB0402492D0 (es)
GE (1) GEP20084361B (es)
IL (1) IL177004A0 (es)
MA (1) MA28348A1 (es)
NL (1) NL1028193C2 (es)
NO (1) NO20063944L (es)
PA (1) PA8623101A1 (es)
PE (1) PE20050772A1 (es)
TW (1) TWI300066B (es)
UY (1) UY28737A1 (es)
WO (1) WO2005077935A1 (es)
ZA (1) ZA200606236B (es)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1912968A1 (en) * 2005-08-04 2008-04-23 Pfizer Limited Piperidinoyl-pyrrolidine and piperidinoyl-piperidine compounds
WO2007041052A2 (en) * 2005-09-29 2007-04-12 Merck & Co., Inc. Acylated spiropiperidine derivatives as melanocortin-4 receptor modulators
WO2007047496A2 (en) * 2005-10-18 2007-04-26 Merck & Co., Inc. Acylated spiropiperidine derivatives as melanocortin-4 receptor modulators
AP2008004602A0 (en) * 2006-02-23 2008-10-31 Pfizer Ltd Melanocortin type 4 receptor agonist piperidinoylpyrrolidines
CN101426782B (zh) * 2006-02-23 2012-10-31 辉瑞股份有限公司 黑皮质素4型受体激动剂哌啶羰基吡咯烷
DK2176220T3 (da) 2007-08-07 2013-06-10 Takeda Pharmaceutical Pyrrolidin-2-on-derivater som androgenreceptormodulatorer.
UA99555C2 (en) 2008-11-12 2012-08-27 Элджи Лайф Саенсез Лтд. Melanocortin receptor agonists
US8476227B2 (en) 2010-01-22 2013-07-02 Ethicon Endo-Surgery, Inc. Methods of activating a melanocortin-4 receptor pathway in obese subjects
US9044606B2 (en) 2010-01-22 2015-06-02 Ethicon Endo-Surgery, Inc. Methods and devices for activating brown adipose tissue using electrical energy
WO2015182723A1 (ja) 2014-05-29 2015-12-03 田辺三菱製薬株式会社 新規ピロリジン化合物およびメラノコルチン受容体作動薬としての用途
US10092738B2 (en) 2014-12-29 2018-10-09 Ethicon Llc Methods and devices for inhibiting nerves when activating brown adipose tissue
US10080884B2 (en) 2014-12-29 2018-09-25 Ethicon Llc Methods and devices for activating brown adipose tissue using electrical energy
PE20180690A1 (es) 2015-04-27 2018-04-23 Intercept Pharmaceuticals Inc Composiciones de acido obeticolico y metodos de uso
EP3333165B1 (en) * 2015-08-04 2019-09-18 Astellas Pharma Inc. Piperazine derivative
CN112694436B (zh) * 2020-12-30 2022-07-08 济南周行医药科技有限公司 一种槟榔碱的合成方法
CN114211258B (zh) * 2021-11-04 2023-09-26 江阴市大久金属科技有限公司 高精密无缝钢管制备工艺

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE60219295T2 (de) * 2001-02-28 2008-01-03 Merck & Co., Inc. Acylierte piperidinderivate als melanocortin-4-rezeptoragonisten
DE60215132T2 (de) * 2001-02-28 2007-08-23 Merck & Co., Inc. Acylierte piperidin-derivate als melanocortin-4-rezeptor-agonisten

Also Published As

Publication number Publication date
CA2555800A1 (en) 2005-08-25
EA200601279A1 (ru) 2006-12-29
CN1930146A (zh) 2007-03-14
AU2005213538A1 (en) 2005-08-25
KR100830763B1 (ko) 2008-05-19
ZA200606236B (en) 2008-04-30
CA2555800C (en) 2010-06-15
TW200526625A (en) 2005-08-16
JP4031814B2 (ja) 2008-01-09
IL177004A0 (en) 2006-12-10
NO20063944L (no) 2006-10-31
BRPI0507435A (pt) 2007-07-03
UY28737A1 (es) 2005-09-30
GEP20084361B (en) 2008-04-29
GB0402492D0 (en) 2004-03-10
JP2007534668A (ja) 2007-11-29
NL1028193A1 (nl) 2005-08-08
NL1028193C2 (nl) 2006-04-20
AP2006003699A0 (en) 2006-08-31
WO2005077935A1 (en) 2005-08-25
MA28348A1 (fr) 2006-12-01
PA8623101A1 (es) 2006-05-16
CR8545A (es) 2007-09-03
EP1716135A1 (en) 2006-11-02
EP1716135B1 (en) 2011-06-01
ATE511507T1 (de) 2011-06-15
AR048232A1 (es) 2006-04-12
TWI300066B (en) 2008-08-21
ECSP066751A (es) 2006-11-16
KR20060127125A (ko) 2006-12-11
EA011159B1 (ru) 2009-02-27

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