ES2574014T3 - Derivado de piperidina novedoso - Google Patents

Derivado de piperidina novedoso Download PDF

Info

Publication number
ES2574014T3
ES2574014T3 ES06747135.9T ES06747135T ES2574014T3 ES 2574014 T3 ES2574014 T3 ES 2574014T3 ES 06747135 T ES06747135 T ES 06747135T ES 2574014 T3 ES2574014 T3 ES 2574014T3
Authority
ES
Spain
Prior art keywords
usp
inhibitors
compounds disclosed
srcard7799
mmol
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
ES06747135.9T
Other languages
English (en)
Inventor
Shiho Ishikawa
Nagaaki Sato
Tsuyoshi Nagase
Shigeru Tokita
Toshihiro Wada
Hidekazu Takahashi
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
MSD KK
Original Assignee
MSD KK
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
Application filed by MSD KK filed Critical MSD KK
Application granted granted Critical
Publication of ES2574014T3 publication Critical patent/ES2574014T3/es
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/20—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms
    • C07D211/22—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms by oxygen atoms
    • 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
    • A61K31/435—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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/16—Central respiratory analeptics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36—Opioid-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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 chain containing hetero atoms as chain links
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/20—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/10—Spiro-condensed systems

Landscapes

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

Abstract

El compuesto 4-(2-metoxipirimidin-5-il)-9-(4-{3-[(2R)-2-metilpirrolidin-1-il]propoxi}fenil)-1-oxa-4,9-diazaespiro- [5,5]undecan-3-ona, o una sal farmacéuticamente aceptable del mismo.

Description

imagen1
imagen2
imagen3
imagen4
imagen5
imagen6
imagen7
imagen8
imagen9
imagen10
imagen11
imagen12
imagen13
imagen14
5
15
25
35
45
55
65
y otros compuestos desvelados en el documento USP 5.739.106; 16) CNTF (factores neurotróficos ciliares) tales como GI181771 (GlaxoSmith Kline), SR146131 (Sanofi Synthelabo), butabindida, PD170.292, PS149164 (Pfizer); 17) derivados de CNTF tales como axokina (Regeneron), y otros compuestos desvelados en los documentos WO 94/09134, WO 98/22128, WO 99/43813; 18) agonistas de GHS (receptor de secreción de la hormona de crecimiento) tales como NN703, hexarelina, MK0677, SM130686, CP424.391, L692.429, L163.255, y compuestos desvelados en los documentos USP 6.358.951, solicitud de patente de Estados Unidos Nº 2002/049196, nº 2002/022637, WO 01/56592, WO 02/32888; 19) agonistas de 5HT2c (receptor de serotonina 2c) tales como BVT933, DPCA37215, IK264, PNU22394, WAY161503, R1065, YM348, y otros compuestos desvelados en los documentos USP 3.914.250, WO 02/36596, WO 02/48124, WO 02/10169, WO 01/66548, WO 02/44152, WO 02/51844, WO 02/40456 y WO 02/40457; 20) agonistas de Mc3r (receptor de melanocortina 3); 21) agonistas del receptor Mc4r (receptor de melanocortina 4) tales como CHIR86036 (Chiron), ME10142, ME10145 (Melacure) y otros compuestos desvelados en los documentos WO99/64002, WO00/74679, WO01/991752, WO01/74844, WO01/70708, WO01/70337, WO01/91752, WO02/059095, WO02/059107, WO02/059108, WO02/059117, WO02/12166, WO02/11715, WO02/12178, WO02/15909, WO02/068387, WO02/068388, WO02/067869, WO03/007949 y WO03/009847; 22) inhibidores de la recaptación de monoaminas tales como sibutramina (Meridia®/Reductil®) y sus sales, y otros derivados desvelados en los documentos USP 4.746.680, USP 4.806.570, USP 5.436.272, solicitud de patente de Estados Unidos Nº 2002/0006964, WO 01/27068 y WO 01/62341; 23) inhibidores de la recaptación de serotonina tales como dexflenfuramina, fluoxetina y otros compuestos desvelados en los documentos USP 6.365.633, WO 01/27060 y WO 01/162341; 24) agonistas de GLP1 (peptido 1 similar a glucagón); 25) topiramato (Topimax®); 26) compuesto 57 de Phytopharm (por ejemplo, CP644.673); 27) inhibidores de ACC2 (acetil CoA carboxilasa2); 28) agonistas de β3 (receptor 3 de adrenalina) tales como AD9677/TAK677 (DaiNippon Pharmaceutical/Takeda Chemical), CL316.243, SB418790, BRL37344, L796568, BMS196085, BRL35135A, CGP12177A, BTA243, W427353, trecadrina, Zeneca D7114, SR59119A, y otros compuestos desvelados en los documentos USP 5.705.515, USP 5.451.677, WO 01/74782 y WO 02/32897; 29) inhibidores de DGAT1 (diacilglicerol aciltransferasa1); 30) inhibidores de DGAT2 (diacilglicerol aciltransferasa2); 31) inhibidores de FAS (ácido graso sintasa) tales como cerulenina, C75; 32) inhibidores de PDE (fosfodiesterasa) tales como teofilina, pentoxifilina, zaprinast, sildenafilo, amrinona, milrinona, cilastamida, rolipram y cilomilast; 33) agonistas de la hormona β del tiroides tales como KB2611 (KaroBio BMS), y otros compuestos desvelados en los documentos WO 02/15845, JPA 2000256190; 34) activadores 1, 2 o 3 de UCP (proteína de desacoplamiento) tales como ácido fitánico, ácido 4[(E)2(5,6,7,8tetrahidro5,5,8,8tetrametil2naftalenil1propenil]benzoico (TTNPB), ácido retinoico y otros compuestos desvelados en el documento WO 99/00123; 35) acilestrógenos tal como oleilestrona (desvelados en del MarGrasa, M. y col, Obesity Research, 9: 2029 (2001)), 36) antagonistas de glucocorticoides; 37) inhibidores de 11β HSD1 (11βhidroesteroide deshidrogenasa1) tales como BVT3498, BVT2733, y otros compuestos desvelados en los documentos WO 01/90091, WO 01/90090, WO 01/90092; 38) inhibidores de SCD1 (estearoilCoA desaturasa1); 39) inhibidores de DPIV (dipeptidil peptidasaIV) tales como isoleucina tiazolidina, valina pirrolidida, NVPDPP728, AF237, P93/01, TSL225, TMC2A/2B/2C, FE999011, P9310/K364, VIP0177, SDZ274444, y otros compuestos desvelados en los documentos WO03/004498, WO03/004496, EP1258476, WO02/083128, WO02/062764, WO03/000250, WO03/002530, WO03/002531, WO03/002553, WO03/002593, WO03/000180 y WO03/000181; 40) inhibidores de lipasa tales como tetrahidroliptatina (Orlisat/Xenical®), Triton WR1339, RHC80267, lipstatina, saponina del té, fosfato de dietilumbilferilo, FL386, WAY121898, BayN3176, valilactona, esteracina, ebelactona A, ebalactona B, RHC80267, y otros compuestos desvelados en los documentos WO 01/77094, USP 4.598.089, USP 4.452.813, USP 5.512.565, USP 5.391.571, USP 5.602.151, USP 4.405.644, USP 4.189.438, y USP 4.242.453; 41) inhibidores del transportador de ácidos grasos; 42) inhibidores del transportador de dicarboxilato; 43) inhibidores del transportador de glucosa; 44) inhibidores del transportador de fosfato; 45) antagonistas de melanocortina tales como melanotán II, y otros compuestos desvelados en los documentos WO 99/64002 y WO 00/746799; 46) antagonistas de la hormona concentradora de melanina; 47) antagonistas de galanina; 48) agonistas de CCK;
16
imagen15
Hz: hertzio
Ejemplo 1: (referencia)
5 Producción de 1'[4(3peridin1ilpropoxi)fenil]3Hespiro[2benzofuran1,4'piperidina]
Se mezclaron 3Hespiro[2benzofuran1,4'piperidina] (131 mg, 0,695 mmol), 1[3(4yodofenoxi)propil]piperidina (200 mg, 0,58 mmol) preparada en el Ejemplo de Referencia (2), tercbutóxido sódico (78 mg, 0,812 mmol), Pd2(dba)3 (5 mg, 0,0058 mmol), 9,9dimetil4,5bis(difenilfosfino)xanteno (7 mg, 0,0116 mmol) y se agitaron durante
10 una noche en 1,4dioxano en una atmósfera de nitrógeno a 60 ºC. La solución de reacción se filtró bajo succión a través de Celite, se diluyó con acetato de etilo, se lavó con agua y una solución salina saturada en este orden, y la capa orgánica se secó con sulfato sódico. El disolvente se retiró por evaporación a presión reducida, y el residuo resultante se purificó a través de cromatografía preparativa de capa fina (eluato: cloroformo/metanol = 10/1) para obtener el compuesto del título en forma de un sólido incoloro (60,5 mg, 26 %).
15 1H RMN (400 MHz, CDCl3) δ: 1,43 (2H, s a), 1,561,61 (4H, m), 1,87 (2H, d, J = 12,0 Hz), 1,921,99 (2H, m), 2,082,16 (2H, m), 2,392,48 (6H, m), 3,10 (2H, t, J = 12,4 Hz), 3,43 (2H, d, J = 11,2 Hz), 3,96 (2H, t, (J=6,4 Hz), 5,09 (2H, s), 6,83 (2H, d, J = 8,8 Hz), 6,96 (2H, d, J = 8,8 Hz), 7,137,15 (1H, m), 7,217,28 (3H, m)
Ejemplo 3: (referencia)
20 Producción de 4(4fluorofenil)9[4(3[(3S)3metilpiperidin1il]propoxi)fenil]1oxa4,9diazaespiro[5,5]undecan3ona
Se mezclaron 9(4{3[(3S)3metilpiperidin1il]propoxi}fenil)1oxa4,9diazaespiro[5,5]undecan3ona (100 mg,
25 0,25 mmol) obtenida en el Ejemplo de Referencia 121, 1bromo4fluorobenceno (52 mg, 0,25 mmol), fosfato potásico (110 mg, 0,50 mmol), yoduro de cobre (23 mg, 0,125 mmol), N,N'dimetildiaminoetano (22 mg, 0,25 mmol) en 1,4dioxano, y se agitaron durante una noche con calentamiento en un tubo cerrado herméticamente a 110 ºC. La solución de reacción se diluyó con acetato de etilo, se lavó con agua y una solución salina saturada en este orden, y la capa orgánica se secó con sulfato sódico. El disolvente se concentró a presión reducida, y el residuo se purificó a
30 través de HPLC preparativa de fase inversa (líquido A, TFA al 0,1 %/agua; líquido B, TFA al 0,1 %/acetonitrilo; A/B = 90/10 a 50/50; elución de gradiente de concentración lineal de 8 minutos; caudal, 40 ml/min) para recoger una fracción que contenía el producto pretendido. Después, el disolvente se concentró a presión reducida, y el residuo se neutralizó con una solución acuosa 2 N de hidróxido sódico añadida al mismo. Éste se extrajo mediante la adición de acetato de etilo al mismo, y la capa orgánica se lavó con una solución salina saturada y se secó con sulfato sódico.
35 El disolvente se retiró por evaporación a presión reducida para obtener el compuesto del título en forma de un sólido de color pardo pálido (83,7 mg, 68 %). 1H RMN (400 MHz, CDCl3) δ: 0,86 (3H, d, J = 6,3 Hz), 1,531,72 (6H, m), 1,821,90 (3H, m), 1,932,00 (2H, m), 2,13 (2H, d, J = 12,9 Hz), 2,462,50 (2H, m), 2,832,90 (2H, m), 3,07 (2H, t, J = 10,6 Hz), 3,27 (2H, d, J = 12,5 Hz), 3,60 (2H, s), 3,96 (2H, t, J = 6,3 Hz), 4,35 (2H, s), 6,84 (2H, d, J = 9,0 Hz), 6,92 (2H, d, J = 9,0 Hz), 7,11 (2H, t, J = 8,6
40 Hz), 7,267,28 (2H, m)
Ejemplo 38 (referencia):
Producción de 4fenil9[4(3piperidin1ilpropoxi)fenil]1oxa4,9diazaespiro[55]undecan3ona
45 El compuesto del título se obtuvo en forma de un sólido de color blanco, de acuerdo con el mismo método que en el Ejemplo 3 o de acuerdo con un método similar a éste pero usando 9[4(3piperidin1ilpropoxi)fenil]1oxa4,9diazaespiro[5,5]undecan3ona obtenida en el Ejemplo de Referencia 12, y bromobenceno en lugar de 1bromo4fluorobenceno.
50 1H RMN (400 MHz, CDCl3) δ: 1,43 (2H, m), 1,561,60 (4H, m), 1,841,99 (4H, m), 2,13 (2H, d, J = 13,2 Hz), 2,402,48 (6H, m), 3,053,10 (2H, m), 3,26 (2H, d, J = 12,4 Hz), 3,64 (2H, s), 3,96 (2H, t, J = 6,4 Hz), 4,36 (2H, s), 6,84 (2H, d, J = 9,2 Hz), 6,93 (2H, d, J = 9,2 Hz), 7,287,31 (3H, m), 7,417,45 (2H, m)
Ejemplo 381:
55 Producción de 4(2metoxipirimidin5il)9(4{3[(2R)2metilpirrolidin1il]propoxi}fenil)1oxa4,9diazaespiro[5,5]undecan3ona
El compuesto del título se obtuvo en forma de un sólido de color amarillo pálido, de acuerdo con el mismo método
60 que en el Ejemplo 3 o de acuerdo con un método similar a éste pero usando 9(4{3[(2R)2metilpirrolidin1il]propoxi}fenil)1oxa4,9diazaespiro[5,5]undecan3ona obtenida en el Ejemplo de Referencia 124, y 5yodo2metoxipirimidina en lugar de 1bromo4fluorobenceno. 1H RMN (400 MHz, CDCl3) δ: 1,10 (3H, d, J = 6,3 Hz), 1,381,48 (1H, m), 1,572,01 (7H, m), 2,092,23 (4H, m), 2,272,33 (1H, m), 2,943,01 (1H, m), 3,033,09 (2H, m), 3,163,21 (1H, m), 3,263,31 (2H, m), 3,63 (2H, s), 3,944,01 (2H,
65 m), 4,03 (3H, s), 4,37 (2H, s), 6,85 (2H, d, J = 9,3 Hz), 6,93 (2H, d, J = 9,3 Hz), 8,53 (2H, s)
18
imagen16
imagen17
imagen18
imagen19
imagen20

Claims (1)

  1. imagen1
ES06747135.9T 2005-05-30 2006-05-29 Derivado de piperidina novedoso Active ES2574014T3 (es)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
JP2005157739 2005-05-30
JP2005157739 2005-05-30
JP2006115778 2006-04-19
JP2006115778 2006-04-19
PCT/JP2006/311155 WO2006129826A1 (ja) 2005-05-30 2006-05-29 新規ピペリジン誘導体

Publications (1)

Publication Number Publication Date
ES2574014T3 true ES2574014T3 (es) 2016-06-14

Family

ID=37481747

Family Applications (1)

Application Number Title Priority Date Filing Date
ES06747135.9T Active ES2574014T3 (es) 2005-05-30 2006-05-29 Derivado de piperidina novedoso

Country Status (13)

Country Link
US (1) US8138206B2 (es)
EP (1) EP1892241B1 (es)
JP (1) JP5154927B2 (es)
KR (1) KR101397913B1 (es)
AU (1) AU2006253312B2 (es)
BR (1) BRPI0610580B8 (es)
CA (1) CA2609388C (es)
ES (1) ES2574014T3 (es)
IL (1) IL187533A0 (es)
NO (1) NO20076614L (es)
NZ (1) NZ562766A (es)
RU (1) RU2417985C2 (es)
WO (1) WO2006129826A1 (es)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009037542A2 (en) 2007-09-20 2009-03-26 Glenmark Pharmaceuticals, S.A. Spirocyclic compounds as stearoyl coa desaturase inhibitors
KR20210141778A (ko) 2016-06-07 2021-11-23 자코바이오 파마슈티칼스 컴퍼니 리미티드 Shp2 억제제로서 유용한 신규한 헤테로환형 유도체
KR20220113545A (ko) 2017-03-23 2022-08-12 자코바이오 파마슈티칼스 컴퍼니 리미티드 Shp2 억제제로서 유용한 신규한 헤테로환형 유도체

Family Cites Families (178)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US340683A (en) 1886-04-27 Method of making split bolts
US3914250A (en) 1974-08-01 1975-10-21 American Home Prod 1,4-Diazepino{8 6,5,4-jk{9 carbazoles
JPS608117B2 (ja) 1977-02-08 1985-02-28 財団法人微生物化学研究会 新生理活性物質エステラスチンおよびその製造法
DE2928485A1 (de) 1979-07-14 1981-01-29 Bayer Ag Verwendung von harnstoffderivaten als arzneimittel bei der behandlung von fettstoffwechselstoerungen
ZA821577B (en) 1981-04-06 1983-03-30 Boots Co Plc Therapeutic agents
US4452813A (en) 1981-05-22 1984-06-05 Taiho Pharmaceutical Company Limited Sulfonate derivatives, process for preparing same and antilipemic compositions containing the derivative
EP0090972B1 (en) 1982-03-17 1990-05-30 Asahi Kasei Kogyo Kabushiki Kaisha Indazole derivatives
CA1247547A (en) 1983-06-22 1988-12-28 Paul Hadvary Leucine derivatives
IE61928B1 (en) 1988-11-29 1994-11-30 Boots Co Plc Treatment of obesity
US5391571A (en) 1989-11-15 1995-02-21 American Home Products Corporation Cholesterol ester hydrolase inhibitors
US5081122A (en) 1990-03-05 1992-01-14 Sterling Drug Inc. Antiglaucoma compositions containing 4-arylcarbonyl-1-(4-morpholinyl)-lower-alkyl)-1H-indoles and method of use thereof
US5112820A (en) 1990-03-05 1992-05-12 Sterling Drug Inc. Anti-glaucoma compositions containing 2- and 3-aminomethyl-6-arylcarbonyl- or 6-phenylthio-2,3-dihydropyrrolo-(1,2,3-de)-1,4-benzoxazines and method of use thereof
US4973587A (en) 1990-03-08 1990-11-27 Sterling Drug Inc. 3-arylcarbonyl-1-aminoalkyl-1H-indole-containing antiglaucoma method
US5013837A (en) 1990-03-08 1991-05-07 Sterling Drug Inc. 3-Arylcarbonyl-1H-indole-containing compounds
FR2692575B1 (fr) 1992-06-23 1995-06-30 Sanofi Elf Nouveaux derives du pyrazole, procede pour leur preparation et compositions pharmaceutiques les contenant.
US5349056A (en) 1992-10-09 1994-09-20 Regeneron Pharmaceuticals Modified ciliary neurotrophic factors
US6472178B1 (en) 1998-02-27 2002-10-29 Regeneron Pharmaceuticals, Inc. Nucleic acids encoding a modified ciliary neurotrophic factor and method of making thereof
US5451677A (en) 1993-02-09 1995-09-19 Merck & Co., Inc. Substituted phenyl sulfonamides as selective β 3 agonists for the treatment of diabetes and obesity
US5292736A (en) 1993-02-26 1994-03-08 Sterling Winthrop Inc. Morpholinoalkylindenes as antiglaucoma agents
FR2714057B1 (fr) 1993-12-17 1996-03-08 Sanofi Elf Nouveaux dérivés du 3-pyrazolecarboxamide, procédé pour leur préparation et compositions pharmaceutiques les contenant.
US5705515A (en) 1994-04-26 1998-01-06 Merck & Co., Inc. Substituted sulfonamides as selective β-3 agonists for the treatment of diabetes and obesity
PL321136A1 (en) 1994-11-07 1997-11-24 Pfizer Some substituted derivatives of bencylamine as a new class of specific ligands of neuropeptide y1
US5552522A (en) 1995-01-31 1996-09-03 Eli Lilly And Company Anti-obesity proteins
US5552523A (en) 1995-01-31 1996-09-03 Eli Lilly And Company Anti-obesity proteins
AU4766196A (en) 1995-01-31 1996-08-21 Eli Lilly And Company Anti-obesity proteins
US5554727A (en) 1995-01-31 1996-09-10 Eli Lilly And Company Anti-obesity proteins
US5552524A (en) 1995-01-31 1996-09-03 Eli Lilly And Company Anti-obesity proteins
US5605886A (en) 1995-01-31 1997-02-25 Eli Lilly And Company Anti-obesity proteins
AU4766096A (en) 1995-01-31 1996-08-21 Eli Lilly And Company Anti-obesity proteins
US5559208A (en) 1995-01-31 1996-09-24 Eli Lilly And Company Anti-obesity proteins
US5521283A (en) 1995-01-31 1996-05-28 Eli Lilly And Company Anti-obesity proteins
US5532237A (en) 1995-02-15 1996-07-02 Merck Frosst Canada, Inc. Indole derivatives with affinity for the cannabinoid receptor
US5831115A (en) 1995-04-21 1998-11-03 Abbott Laboratories Inhibitors of squalene synthase and protein farnesyltransferase
US20020006964A1 (en) 1995-05-16 2002-01-17 Young James W. Methods of using and compositions comprising (+) sibutramine optionally in combination with other pharmacologically active compounds
US5739106A (en) 1995-06-07 1998-04-14 Rink; Timothy J. Appetite regulating compositions
FR2741621B1 (fr) 1995-11-23 1998-02-13 Sanofi Sa Nouveaux derives de pyrazole, procede pour leur preparation et compositions pharmaceutiques en contenant
WO1997019682A1 (en) 1995-12-01 1997-06-05 Synaptic Pharmaceutical Corporation Aryl sulfonamide and sulfamide derivatives and uses thereof
WO1997020821A1 (en) 1995-12-01 1997-06-12 Novartis Ag Heteroaryl derivatives
AU7692896A (en) 1995-12-01 1997-06-27 Novartis Ag Quinazolin-2,4-diazirines as NPY receptor antagonist
WO1997020823A2 (en) 1995-12-01 1997-06-12 Novartis Ag 2-amino quinazoline derivatives as npy receptor antagonists
AU7626496A (en) 1995-12-01 1997-06-27 Ciba-Geigy Ag Heteroaryl compounds
TW432073B (en) 1995-12-28 2001-05-01 Pfizer Pyrazolopyridine compounds
AU1618697A (en) 1996-02-06 1997-08-28 Japan Tobacco Inc. Novel compounds and pharmaceutical use thereof
IT1288388B1 (it) 1996-11-19 1998-09-22 Angeletti P Ist Richerche Bio Uso di sostanze che attivano il recettore del cntf ( fattore neurotrofico ciliare) per la preparazione di farmaci per la terapia
AU7738198A (en) 1996-12-15 1998-07-15 Banyu Pharmaceutical Co., Ltd. Aminopyrazole derivatives
WO1998031227A1 (en) 1997-01-21 1998-07-23 Smithkline Beecham Corporation Novel cannabinoid receptor modulators
JP2001511147A (ja) 1997-02-04 2001-08-07 ザ・ボード・オブ・トラステイーズ・オブ・ザ・ユニバーシテイ・オブ・アーカンソー 殺菌・殺カビ性のカルボキサミド類
PT966436E (pt) 1997-02-21 2003-03-31 Bayer Ag Arilsulfonamidas e analogos e sua aplicacao para o tratamento de doencas neurodegenerativas
WO1998041519A1 (en) 1997-03-18 1998-09-24 Smithkline Beecham Corporation Novel cannabinoid receptor agonists
FR2761266B1 (fr) 1997-03-28 1999-07-02 Sanofi Sa Composition pharmaceutique formee par granulation humide pour l'administration orale d'un derive du n-piperidino-3- pyrazolecarboxamide, de ses sels et de leurs solvates
FR2761265B1 (fr) 1997-03-28 1999-07-02 Sanofi Sa Composition pharmaceutique pour l'administration orale d'un derive du n-piperidino-3-pyrazolecarboxamide, de ses sels et de leurs solvates
JP4228398B2 (ja) 1997-04-23 2009-02-25 萬有製薬株式会社 神経ペプチドｙ受容体拮抗剤
US6001836A (en) 1997-05-28 1999-12-14 Bristol-Myers Squibb Company Dihydropyridine NPY antagonists: cyanoguanidine derivatives
SE9702457D0 (sv) 1997-06-26 1997-06-26 Pharmacia & Upjohn Ab Screening
WO1999002499A1 (fr) 1997-07-11 1999-01-21 Japan Tobacco Inc. Composes quinoline et utilisations de ceux-ci en medecine
EP1068207A1 (en) 1998-04-02 2001-01-17 Neurogen Corporation AMINOALKYL SUBSTITUTED 9H-PYRIDINO 2,3-b]INDOLE AND 9H-PYRIMIDINO 4,5-b]INDOLE DERIVATIVES
ATE269846T1 (de) 1998-04-29 2004-07-15 Ortho Mcneil Pharm Inc N-substituierte aminotetraline als neuropeptid y y5 rezeptor-liganden und ihre anwendung zur behandlung von fettleibigkeit und anderen erkrankungen
US6329395B1 (en) 1998-06-08 2001-12-11 Schering Corporation Neuropeptide Y5 receptor antagonists
CA2334551A1 (en) 1998-06-11 1999-12-16 Merck & Co., Inc. Spiropiperidine derivatives as melanocortin receptor agonists
HN1998000027A (es) 1998-08-19 1999-06-02 Bayer Ip Gmbh Arilsulfonamidas y analagos
DE19837627A1 (de) 1998-08-19 2000-02-24 Bayer Ag Neue Aminosäureester von Arylsulfonamiden und Analoga
US6358951B1 (en) 1998-08-21 2002-03-19 Pfizer Inc. Growth hormone secretagogues
US6337332B1 (en) 1998-09-17 2002-01-08 Pfizer Inc. Neuropeptide Y receptor antagonists
US7417038B1 (en) 1998-10-15 2008-08-26 Imperial Innovations Limited Methods of treating cachexia
ES2255330T3 (es) 1998-11-10 2006-06-16 MERCK & CO., INC. Espiroindolinas como antagonistas del receptor y5.
ES2161594B1 (es) 1998-12-17 2003-04-01 Servier Lab Nuevos derivados de la hidrazida, su procedimiento de preparacion y las composiciones farmaceuticas que los contienen.
US6344481B1 (en) 1999-03-01 2002-02-05 Pfizer Inc. Thyromimetic antiobesity agents
IL145240A (en) 1999-03-19 2007-02-11 Abbott Gmbh & Co Kg Compound and its use in the treatment of eating disorders
FR2792314B1 (fr) 1999-04-15 2001-06-01 Adir Nouveaux composes aminotriazoles, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
EP1816127A1 (en) 1999-04-22 2007-08-08 H. Lundbeck A/S Triazine derivatives for use as selective npy (y5) antagonists
EP1177172A1 (en) 1999-05-05 2002-02-06 Ortho-McNeil Pharmaceutical, Inc. 3a,4,5,9b-TETRAHYDRO-1H-BENZ e]INDOL-2-YL AMINE-DERIVED NEUROPEPTIDE Y RECEPTORS LIGANDS USEFUL IN THE TREATMENT OF OBESITY AND OTHER DISORDERS
EP1177188B1 (en) 1999-05-12 2005-10-12 Ortho-McNeil Pharmaceutical, Inc. Pyrazole carboxamides useful for the treatment of obesity and other disorders
AU766191B2 (en) 1999-06-04 2003-10-09 Merck & Co., Inc. Substituted piperidines as melanocortin-4 receptor agonists
EP1194421B1 (en) 1999-06-30 2005-10-12 H. Lundbeck A/S Selective npy (y5) antagonists
WO2001007409A1 (en) 1999-07-23 2001-02-01 Astrazeneca Uk Limited Carbazole derivatives and their use as neuropeptide y5 receptor ligands
CA2380032A1 (en) 1999-07-28 2001-02-08 Ortho-Mcneil Pharmaceutical, Inc. Amine and amide derivatives as ligands for the neuropeptide y y5 receptor useful in the treatment of obesity and other disorders
TWI279402B (en) 1999-08-20 2007-04-21 Banyu Pharma Co Ltd Spiro compounds having NPY antagonistic activities and agents containing the same
US6506762B1 (en) 1999-09-30 2003-01-14 Neurogen Corporation Certain alkylene diamine-substituted heterocycles
CN1377355A (zh) 1999-09-30 2002-10-30 纽罗杰有限公司 氨基取代的吡唑并[1,5－a]－1,5－嘧啶和吡唑并[1,5－a]－1,3,5－三嗪
IL148905A0 (en) 1999-09-30 2002-09-12 Neurogen Corp Pfizer Inc Certain alkylene diamine-substituted pyrazolo{1,5,-a}-1,5-pyrimidines and pyrazolo{1,5,-a}-1,3,5-triazines
GEP20043160B (en) 1999-10-13 2004-01-26 Pfizer Products Inc Us Biaryl Ether Derivatives, Pharmaceutical Compositions Containing Them and Their Use as Monoamine Reuptake Inhibitors
DE19949319A1 (de) 1999-10-13 2001-06-13 Ruetgers Vft Ag Verfahren zur Herstellung von Arylalkylethern
ES2243337T3 (es) 1999-12-16 2005-12-01 Schering Corporation Imidazoles sustituidos antagonistas del receptor y5 del neuropeptido y.
WO2001056592A1 (en) 2000-02-01 2001-08-09 Novo Nordisk A/S Use of compounds for the regulation of food intake
AU2001234958A1 (en) 2000-02-11 2001-08-20 Bristol-Myers Squibb Company Cannabinoid receptor modulators, their processes of preparation, and use of cannabinoid receptor modulators for treating respiratory and non-respiratory diseases
JP2001226269A (ja) 2000-02-18 2001-08-21 Takeda Chem Ind Ltd メラニン凝集ホルモン拮抗剤
ES2236178T3 (es) 2000-02-22 2005-07-16 Banyu Pharmaceutical Co., Ltd. Nuevos compuestos de imidazolina.
GB0004003D0 (en) 2000-02-22 2000-04-12 Knoll Ag Therapeutic agents
US6531478B2 (en) 2000-02-24 2003-03-11 Cheryl P. Kordik Amino pyrazole derivatives useful for the treatment of obesity and other disorders
FR2805810B1 (fr) 2000-03-03 2002-04-26 Aventis Pharma Sa Compositions pharmaceutiques contenant des derives de 3- amino-azetidine, les nouveaux derives et leur preparation
FR2805817B1 (fr) 2000-03-03 2002-04-26 Aventis Pharma Sa Compositions pharmaceutiques contenant des derives d'azetidine, les nouveaux derives d'azetidine et leur preparation
FR2805818B1 (fr) 2000-03-03 2002-04-26 Aventis Pharma Sa Derives d'azetidine, leur preparation et les compositions pharmaceutiques les contenant
EP1132389A1 (en) 2000-03-06 2001-09-12 Vernalis Research Limited New aza-indolyl derivatives for the treatment of obesity
MXPA02008797A (es) 2000-03-14 2005-09-08 Actelion Pharmaceuticals Ltd Derivados de 1,2,3,4-tetrahidroisoquinolina.
AU4928101A (en) 2000-03-23 2001-10-03 Merck & Co Inc Spiropiperidine derivatives as melanocortin receptor agonists
US6458790B2 (en) 2000-03-23 2002-10-01 Merck & Co., Inc. Substituted piperidines as melanocortin receptor agonists
US6600015B2 (en) 2000-04-04 2003-07-29 Hoffmann-La Roche Inc. Selective linear peptides with melanocortin-4 receptor (MC4-R) agonist activity
ATE479429T1 (de) 2000-04-28 2010-09-15 Takeda Pharmaceutical Antagonisten des melanin-konzentrierenden hormons
GB0010757D0 (en) 2000-05-05 2000-06-28 Astrazeneca Ab Chemical compounds
GB0011013D0 (en) 2000-05-09 2000-06-28 Astrazeneca Ab Chemical compounds
US6444675B2 (en) 2000-05-10 2002-09-03 Bristol-Myers Squibb Company 4-alkyl and 4-cycloalkyl derivatives of dihydropyridine NPY antagonists
WO2001085173A1 (en) 2000-05-10 2001-11-15 Bristol-Myers Squibb Company Alkylamine derivatives of dihydropyridine npy antagonists
US6432960B2 (en) 2000-05-10 2002-08-13 Bristol-Myers Squibb Company Squarate derivatives of dihydropyridine NPY antagonists
ATE310728T1 (de) 2000-05-11 2005-12-15 Bristol Myers Squibb Co Tetrahydroisochinolin-analoga als wachstumshormon-sekretagoga
WO2001087834A1 (fr) 2000-05-16 2001-11-22 Takeda Chemical Industries, Ltd. Antagoniste de l'hormone de concentration de la melanine
AUPQ761100A0 (en) 2000-05-18 2000-06-08 Australian Rural Group Limited Lipophilic medicament
US6391881B2 (en) 2000-05-19 2002-05-21 Bristol-Myers Squibb Company Thiourea derivatives of dihydropyridine NPY antagonists
SE0001899D0 (sv) 2000-05-22 2000-05-22 Pharmacia & Upjohn Ab New compounds
AU6497701A (en) 2000-05-30 2001-12-11 Merck & Co Inc Melanocortin receptor agonists
EP2301930B1 (en) 2000-06-15 2016-01-06 Merck Sharp & Dohme Corp. Derivatives of hexahydrobenzofuranone useful for the treatment of (inter alia) auto-immune or inflammatory disorders
PT1289955E (pt) 2000-06-16 2005-08-31 Smithkline Beecham Plc Piperidinas para utilizacao como antagonistas dos receptores da orexina
AU783403B2 (en) 2000-07-05 2005-10-20 H. Lundbeck A/S Selective melanin concentrating hormone-1 (MCH1) receptor antagonists and uses thereof
JP2004516239A (ja) 2000-07-06 2004-06-03 ニューロジェン コーポレイション メラニン凝集ホルモン受容体リガンド
GB0019357D0 (en) 2000-08-07 2000-09-27 Melacure Therapeutics Ab Novel phenyl guanidines
CN1443198A (zh) 2000-07-24 2003-09-17 阿达纳生物科学有限公司 Ghrelin拮抗剂
AU8395501A (en) 2000-07-31 2002-02-13 Hoffmann La Roche Piperazine derivatives
US6768024B1 (en) 2000-08-04 2004-07-27 Lion Bioscience Ag Triamine derivative melanocortin receptor ligands and methods of using same
GB0019359D0 (en) 2000-08-07 2000-09-27 Melacure Therapeutics Ab Novel guanidines
CN1468227A (zh) 2000-08-08 2004-01-14 ����-������ҩƷ��˾ 非咪唑芳氧基烷基胺
WO2002015845A2 (en) 2000-08-21 2002-02-28 Merck & Co., Inc. Anti-hypercholesterolemic drug combination
WO2002015905A1 (en) 2000-08-21 2002-02-28 Gliatech, Inc. The use of histamine h3 receptor inverse agonists for the control of appetite and treatment of obesity
CA2419310A1 (en) 2000-08-23 2002-02-28 Merck & Co., Inc. Substituted piperidines as melanocortin receptor agonists
US6900226B2 (en) 2000-09-06 2005-05-31 Hoffman-La Roche Inc. Neuropeptide Y antagonists
MXPA03002263A (es) 2000-09-14 2003-06-24 Schering Corp Antagonistas de receptor de neuropeptido y y5 de urea sustituidos.
CN1469871A (zh) 2000-10-13 2004-01-21 作为生长激素促分泌素的取代的二肽
CA2422698C (en) 2000-10-16 2009-12-15 F. Hoffmann-La Roche Ag Indoline derivatives and their use as 5-ht2 receptor ligands
CA2423792A1 (en) 2000-10-20 2002-04-25 Pfizer Products Inc. Alpha-aryl ethanolamines and their use as beta-3 adrenergic receptor agonists
AU2002227170A1 (en) 2000-11-03 2002-05-15 Wyeth Cycloalkyl(b)(1,4)diazepino(6,7,1-hi)indoles and derivatives
CA2428905A1 (en) 2000-11-20 2002-05-23 Biovitrum Ab PIPERAZINYLPYRAZINE COMPOUNDS FOR USE AS ANTAGONISTS OF THE SEROTONIN 5-HT2 RECEPTOR
JP4387103B2 (ja) 2000-11-20 2009-12-16 ビオヴィトルム・アクチボラゲット（プブリクト） セロトニン５ｈｔ−２レセプターのアゴニストまたはアンタゴニストとしてのピペラジニルピラジン化合物
US6566367B2 (en) 2000-12-12 2003-05-20 Pfizer Inc. Spiro[isobenzofuran-1,4′-piperidin]-3-ones and 3H-spiroisobenzofuran-1,4′-piperidines
GB0030710D0 (en) 2000-12-15 2001-01-31 Hoffmann La Roche Piperazine derivatives
CA2432809C (en) 2000-12-21 2010-11-30 Schering Corporation Heteroaryl urea neuropeptide y y5 receptor antagonists
KR20040011447A (ko) 2000-12-22 2004-02-05 쉐링 코포레이션 피페리딘 ｍｃｈ 길항제 및 비만 치료에 있어서의 이의 용도
WO2002051232A2 (en) 2000-12-27 2002-07-04 Actelion Pharmaceuticals Ltd. Novel benzazepines and related heterocyclic derivatives
CA2432085C (en) 2000-12-27 2009-02-24 F. Hoffmann-La Roche Ag Indole derivatives and their use as 5-ht2b and 5-ht2c receptor ligands
CA2433025A1 (en) 2001-01-23 2002-08-01 Chaoyu Xie Substituted piperidines/piperazines as melanocortin receptor agonists
US7291619B2 (en) 2001-01-23 2007-11-06 Eli Lilly And Company Melanocortin receptor agonists
JP2004524297A (ja) 2001-01-23 2004-08-12 イーライ・リリー・アンド・カンパニー メラノコルチン受容体アゴニスト
US7034039B2 (en) 2001-02-02 2006-04-25 Takeda Pharmaceutical Company Limited Fused heterocyclic compounds
AU2002255597B8 (en) 2001-02-28 2006-10-26 Merck Sharp & Dohme Corp. Acylated piperidine derivatives as melanocortin-4 receptor agonists
DE60232238D1 (de) 2001-02-28 2009-06-18 Merck & Co Inc Acylierte piperidinderivate als melanocortin-4-rezeptoragonisten
EP1383501B1 (en) 2001-02-28 2007-04-04 Merck & Co., Inc. Acylated piperidine derivatives as melanocortin-4 receptor agonists
US6900329B2 (en) 2001-03-21 2005-05-31 Schering Corporation MCH antagonists and their use in the treatment of obesity
CA2441235C (en) 2001-03-21 2011-05-24 Pharmacopeia, Inc. Aryl and biaryl compounds having mch modulatory activity
AR033046A1 (es) 2001-03-22 2003-12-03 Solvay Pharm Bv Derivados de 4,5-dihidro-1h-pirazol que tienen actividad antagonista de cb1, composicion farmaceutica y metodos de preparacion
WO2001074782A1 (en) 2001-03-29 2001-10-11 Molecular Design International, Inc. β3-ADRENORECEPTOR AGONISTS, AGONIST COMPOSITIONS AND METHODS OF MAKING AND USING THE SAME
US6573287B2 (en) 2001-04-12 2003-06-03 Bristo-Myers Squibb Company 2,1-oxazoline and 1,2-pyrazoline-based inhibitors of dipeptidyl peptidase IV and method
CA2443672C (en) 2001-04-12 2011-03-29 Pharmacopeia, Inc. Aryl and biaryl piperidines used as mch antagonists
FR2824825B1 (fr) 2001-05-15 2005-05-06 Servier Lab Nouveaux derives d'alpha-amino-acides, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
MXPA03010565A (es) 2001-05-21 2004-03-02 Hoffmann La Roche Derivados de quinolina como ligandos para receptor del neuropeptido y.
CA2448080A1 (en) 2001-05-22 2002-11-28 Neurogen Corporation Melanin concentrating hormone receptor ligands: substituted 1-benzyl-4-aryl piperazine analogues
CA2450579A1 (en) 2001-06-20 2003-01-03 Merck & Co., Inc. Dipeptidyl peptidase inhibitors for the treatment of diabetes
EP1406622B1 (en) 2001-06-20 2006-02-22 Merck & Co., Inc. Dipeptidyl peptidase inhibitors for the treatment of diabetes
GB0115517D0 (en) 2001-06-25 2001-08-15 Ferring Bv Novel antidiabetic agents
EP1399433B1 (en) 2001-06-27 2007-08-22 Smithkline Beecham Corporation Fluoropyrrolidines as dipeptidyl peptidase inhibitors
ES2296962T3 (es) 2001-06-27 2008-05-01 Smithkline Beecham Corporation Pirrolidinas como inhibidores de dipeptidil peptidasa.
KR20040015298A (ko) 2001-06-27 2004-02-18 스미스클라인 비참 코포레이션 디펩티딜 펩티다제 억제제로서의 플루오로피롤리딘
CN1471538A (zh) 2001-06-27 2004-01-28 前体生物药物股份有限公司 用于竞争性调节二肽基肽酶iv催化的肽结构
DE60225556D1 (de) 2001-07-03 2008-04-24 Novo Nordisk As Dpp-iv-inhibierende purin-derivative zur behandlung von diabetes
IL159697A0 (en) 2001-07-05 2004-06-20 Synaptic Pharma Corp Substituted anilinic piperidines as mch selective antagonists
UA74912C2 (en) 2001-07-06 2006-02-15 Merck & Co Inc Beta-aminotetrahydroimidazo-(1,2-a)-pyrazines and tetratriazolo-(4,3-a)-pyrazines as inhibitors of dipeptylpeptidase for the treatment or prevention of diabetes
ITMI20011483A1 (it) 2001-07-11 2003-01-11 Res & Innovation Soc Coop A R Uso di composti come antagonisti funzionali ai recettori centrali deicannabinoidi
CA2453609C (en) 2001-07-18 2010-05-04 Merck & Co., Inc. Bridged piperidine derivatives as melanocortin receptor agonists
AU2002319627A1 (en) 2001-07-20 2003-03-03 Merck And Co., Inc. Substituted imidazoles as cannabinoid receptor modulators
US6977264B2 (en) 2001-07-25 2005-12-20 Amgen Inc. Substituted piperidines and methods of use
US6915444B2 (en) 2001-09-12 2005-07-05 Rockwell Automation Technologies, Inc. Network independent safety protocol for industrial controller using data manipulation techniques
CA2487957A1 (en) 2002-05-31 2003-12-11 Chowdary Nannapaneni Venkaiah An improved process for the preparation of 4-(n, n-disubstitutedamino) butyraldehyde acetals
GB0224084D0 (en) * 2002-10-16 2002-11-27 Glaxo Group Ltd Novel compounds
US20060019964A1 (en) 2002-10-16 2006-01-26 Ancliff Ranchael A Compounds
EP1554260A1 (en) 2002-10-22 2005-07-20 Glaxo Group Limited Aryloxyalkylamine derivatives as h3 receptor ligands
CA2504272A1 (en) * 2002-10-23 2004-05-06 Janssen Pharmaceutica, N.V. Phenylpiperidines and phenylpyrrolidines as histamine h3 receptor modulators
GB0308333D0 (en) 2003-04-10 2003-05-14 Glaxo Group Ltd Novel compounds
US7595316B2 (en) 2003-06-27 2009-09-29 Banyu Pharmaceutical Co., Ltd. Heteroaryloxy nitrogenous saturated heterocyclic derivative
CN1902177A (zh) * 2003-09-22 2007-01-24 万有制药株式会社 新哌啶衍生物
EP1717230B1 (en) 2004-02-13 2014-08-06 Msd K.K. Fused-ring 4-oxopyrimidine derivative
WO2006002341A2 (en) 2004-06-23 2006-01-05 Virginia Tech Intellectual Properties, Inc. Methods for purification of trimetallic nitride endohedral metallofullerenes and related fullerene derivatives
US7973174B2 (en) 2005-10-18 2011-07-05 Invista North America S.A.R.L. Process of making 3-aminopentanenitrile

Also Published As

Publication number Publication date
IL187533A0 (en) 2008-03-20
BRPI0610580B1 (pt) 2020-09-15
BRPI0610580B8 (pt) 2021-05-25
NZ562766A (en) 2011-03-31
AU2006253312A1 (en) 2006-12-07
EP1892241B1 (en) 2016-03-30
KR20080013986A (ko) 2008-02-13
CA2609388A1 (en) 2006-12-07
RU2007144492A (ru) 2009-06-10
BRPI0610580A8 (pt) 2018-03-13
NO20076614L (no) 2008-02-27
CA2609388C (en) 2013-08-06
US20090137576A1 (en) 2009-05-28
JP5154927B2 (ja) 2013-02-27
EP1892241A4 (en) 2010-01-20
JPWO2006129826A1 (ja) 2009-01-08
WO2006129826A1 (ja) 2006-12-07
KR101397913B1 (ko) 2014-05-26
EP1892241A1 (en) 2008-02-27
US8138206B2 (en) 2012-03-20
RU2417985C2 (ru) 2011-05-10
BRPI0610580A2 (pt) 2010-11-09
AU2006253312B2 (en) 2011-08-18

Similar Documents

Publication Publication Date Title
KR101318127B1 (ko) 아자 치환된 스피로 유도체
US7732456B2 (en) Pyridone derivative
CN101056861B (zh) 氨基甲酰基取代螺衍生物
US20110071129A1 (en) Spirodiamine-diaryl ketoxime derivative
US10519115B2 (en) Antidiabetic tricyclic compounds
US10676458B2 (en) Antidiabetic bicyclic compounds
US10968232B2 (en) Antidiabetic spirochroman compounds
ES2574014T3 (es) Derivado de piperidina novedoso
EP1939194A1 (en) Bicyclic aromatic substituted pyridone derivative
WO2007024004A1 (ja) フェニルピリドン誘導体
US7485647B2 (en) 2-aminoquinoline derivatives
KR20220102669A (ko) 인간 인테그린 α4β7의 억제
AU2005310467A1 (en) Substituted pyridone derivative
US20160280626A1 (en) Antidiabetic bicyclic compounds
US20230102081A1 (en) Compound as cyclin-dependent kinase 9 inhibitor and use thereof
KR20230154194A (ko) 신장 섬유증의 치료를 위한 HIPK2의 옥사디아졸릴 디하이드로피라노[2,3-b]피리딘 억제제
CN105814068A (zh) 一种取代的氨基磷酸酯类衍生物、其制备方法及其应用
JP6570034B2 (ja) 新規なグルタミン酸誘導体およびその用途
WO2010147234A1 (en) Diarylamide-spirodiamine derivative
US20220096492A1 (en) Pharmaceutical compounds and therapeutic methods
ES2448217T3 (es) Moléculas policétidas como agentes anticancerosos
MX2008006063A (es) Derivados de espiro aza-sustituidos