AR048232A1 - Piperidinilcarbonil- pirrolidinas y su uso como agonistas de melanocortina cr4 - Google Patents

Piperidinilcarbonil- pirrolidinas y su uso como agonistas de melanocortina cr4

Info

Publication number
AR048232A1
AR048232A1 ARP050100409A ARP050100409A AR048232A1 AR 048232 A1 AR048232 A1 AR 048232A1 AR P050100409 A ARP050100409 A AR P050100409A AR P050100409 A ARP050100409 A AR P050100409A AR 048232 A1 AR048232 A1 AR 048232A1
Authority
AR
Argentina
Prior art keywords
groups
alkyl
cycloalkyl
halogen
och2cf3
Prior art date
Application number
ARP050100409A
Other languages
English (en)
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.)
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Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34864830&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR048232(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 AR048232A1 publication Critical patent/AR048232A1/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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Psychiatry (AREA)
  • Dermatology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Emergency Medicine (AREA)
  • Anesthesiology (AREA)
  • Addiction (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pregnancy & Childbirth (AREA)
  • Child & Adolescent Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Gastroenterology & Hepatology (AREA)

Abstract

Se refiere a su uso en medicina, a composiciones que los contienen, a procesos para su preparacion y a intermedios usados en tales procesos. Reivindicacion 1: Un compuesto de formula general (1), o una sal farmacéuticamente aceptable, hidrato, solvato, isomero o profármaco del mismo, en la que R1 se selecciona entre: grupos -alquilo C1-6, -alquenilo C2-6, -alquinilo C2-6, -cicloalquilo C3-8, -cicloalquenilo C5-8, -alquilC1-2-cicloalquiloC3-8, arilo, -alquilarilo C1-2, heterociclilo o grupos alquilC1-2-heterocíclicos; donde cada uno de los grupos R1 anteriores está opcionalmente sustituido con uno o más grupos seleccionados entre: alquilo C1-4, -(CH2)mcicloalquiloC3-5, halogeno, -(CH2)mOR6, -CN, -C(O)OR6, -(CH2)mNR7SO2R8, CF3, CH2CF3, OCF3 o OCH2CF3, donde m = 0, 1 o 2; R2 es H, OH o OCH3; R3 se selecciona entre: grupos H, -alquilo C1-6, -alquenilo C2-6, -alquinilo C2-6, -cicloalquilo C3-8, -cicloalquenilo C5-8, -alquilC1-2-cicloalquiloC3-8, arilo, -alquilarilo C1-2, heterociclilo o grupos -alquilC1-2-heterocíclicos; donde cada uno de los ultimos diez grupos R3 está opcionalmente sustituido con uno o más grupos seleccionados entre: -OH, -alquilo C1-4, -(CH2)ncicloalquiloC3-5, halogeno, -CN, -(CH2)nOR6 o - (CH2)nNR7R8, donde n = 0, 1 o 2; R4 se selecciona entre: -H, -alquilo C1-4, -alquenilo C2-4, -alquinilo C2-4, -(CH2)pcicloalquiloC3-5, -(CH2)pciclo-alqueniloC5, halogeno, -(CH2)pOR6, (CH2)pNR7R8, -CN, -C(O)R6, -C(O)OR6, -C(O)NR7R8, -(CH2)pNR7SO2R8, CF3, CH2CF3, OCF3 o OCH2CF3, donde p = 0, 1 o 2; R5 se selecciona entre: grupos -alquilo C1-4, -alquenilo C2-4, -alquinilo C2-4, -(CH2)pcicloalquiloC3-5, -(CH2)pciclo-alqueniloC5, halogeno, -(CH2)pOR6, (CH2)pNR7R8, -CN, -C(O)R6, -C(O)OR6, - C(O)NR7R8, -(CH2)pNR7SO2R8, CF3, CH2CF3, OCF3 o OCH2CF3, donde p = 0, 1 o 2; o R4 y R5 pueden formar conjuntamente u anillo saturado o insaturado de 5 a 7 miembros condensado; cada uno de R6, R7 y R8 se selecciona independientemente entre H, CH3 o CH2CH3; y donde los grupos heterocíclicos de R1 y R3 se seleccionan independientemente entre sistemas de anillo de 4 a 10 miembros que contienen hasta 4 heteroátomos seleccionados independientemente entre O, N o S.
ARP050100409A 2004-02-04 2005-02-03 Piperidinilcarbonil- pirrolidinas y su uso como agonistas de melanocortina cr4 AR048232A1 (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
AR048232A1 true AR048232A1 (es) 2006-04-12

Family

ID=34864830

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP050100409A AR048232A1 (es) 2004-02-04 2005-02-03 Piperidinilcarbonil- pirrolidinas y su uso como agonistas de melanocortina cr4

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 (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007015162A1 (en) * 2005-08-04 2007-02-08 Pfizer Limited Piperidinoyl-pyrrolidine and piperidinoyl-piperidine compounds
KR20080048502A (ko) * 2005-09-29 2008-06-02 머크 앤드 캄파니 인코포레이티드 멜라노코르틴-4 수용체 조절제로서의 아실화스피로피페리딘 유도체
US7652024B2 (en) * 2005-10-18 2010-01-26 Merck Sharp & Dohme Corp. Acylated spiropiperidine derivatives as melanocortin-4 receptor modulators
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
AP2008004602A0 (en) * 2006-02-23 2008-10-31 Pfizer Ltd Melanocortin type 4 receptor agonist piperidinoylpyrrolidines
AU2008284662B2 (en) 2007-08-07 2013-07-25 Takeda Pharmaceutical Company Limited Pyrrolidin-2 -one derivatives as androgen receptor modulator
UA99555C2 (en) 2008-11-12 2012-08-27 Элджи Лайф Саенсез Лтд. Melanocortin receptor agonists
US9044606B2 (en) 2010-01-22 2015-06-02 Ethicon Endo-Surgery, Inc. Methods and devices for activating brown adipose tissue using electrical energy
US8476227B2 (en) 2010-01-22 2013-07-02 Ethicon Endo-Surgery, Inc. Methods of activating a melanocortin-4 receptor pathway in obese subjects
MY193597A (en) * 2014-05-29 2022-10-19 Mitsubishi Tanabe Pharma Corp Novel pyrrolidine compound and application as melanocortin receptor agonist
US10080884B2 (en) 2014-12-29 2018-09-25 Ethicon Llc Methods and devices for activating brown adipose tissue using electrical energy
US10092738B2 (en) 2014-12-29 2018-10-09 Ethicon Llc Methods and devices for inhibiting nerves when activating brown adipose tissue
PE20180690A1 (es) 2015-04-27 2018-04-23 Intercept Pharmaceuticals Inc Composiciones de acido obeticolico y metodos de uso
PT3333165T (pt) * 2015-08-04 2019-10-29 Astellas Pharma Inc Derivado de piperazina
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
CA3217201A1 (en) * 2021-05-06 2022-11-10 Lg Chem, Ltd. Crystal form vii of melanocortin receptor agonist compound and method for preparing same
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
GEP20053710B (en) * 2001-02-28 2005-12-26 Merck & Co Inc Acylated Piperidine Derivatives as Melanocortin-4 Receptor Agonists
EP1372653B1 (en) * 2001-02-28 2006-10-04 Merck & Co., Inc. Acylated piperidine derivatives as melanocortin-4 receptor agonists

Also Published As

Publication number Publication date
AU2005213538A1 (en) 2005-08-25
JP4031814B2 (ja) 2008-01-09
CR8545A (es) 2007-09-03
GEP20084361B (en) 2008-04-29
CA2555800A1 (en) 2005-08-25
ATE511507T1 (de) 2011-06-15
ECSP066751A (es) 2006-11-16
MA28348A1 (fr) 2006-12-01
EA200601279A1 (ru) 2006-12-29
UY28737A1 (es) 2005-09-30
GB0402492D0 (en) 2004-03-10
ZA200606236B (en) 2008-04-30
NO20063944L (no) 2006-10-31
BRPI0507435A (pt) 2007-07-03
AP2006003699A0 (en) 2006-08-31
EP1716135B1 (en) 2011-06-01
PE20050772A1 (es) 2005-10-31
TWI300066B (en) 2008-08-21
TW200526625A (en) 2005-08-16
KR100830763B1 (ko) 2008-05-19
EP1716135A1 (en) 2006-11-02
WO2005077935A1 (en) 2005-08-25
NL1028193C2 (nl) 2006-04-20
PA8623101A1 (es) 2006-05-16
CA2555800C (en) 2010-06-15
JP2007534668A (ja) 2007-11-29
NL1028193A1 (nl) 2005-08-08
CN1930146A (zh) 2007-03-14
IL177004A0 (en) 2006-12-10
EA011159B1 (ru) 2009-02-27
KR20060127125A (ko) 2006-12-11

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