AR036598A1 - Derivados de 4,5-dihidro-1h-pirazol que tienen potente actividad antagonista de cb1 - Google Patents

Derivados de 4,5-dihidro-1h-pirazol que tienen potente actividad antagonista de cb1

Info

Publication number
AR036598A1
AR036598A1 ARP020103508A ARP020103508A AR036598A1 AR 036598 A1 AR036598 A1 AR 036598A1 AR P020103508 A ARP020103508 A AR P020103508A AR P020103508 A ARP020103508 A AR P020103508A AR 036598 A1 AR036598 A1 AR 036598A1
Authority
AR
Argentina
Prior art keywords
group
alkyl
whose
amino
substituted
Prior art date
Application number
ARP020103508A
Other languages
English (en)
Inventor
Josephus H M Lange
Cornelis G Kruse
Jacobus Tipker
Stuivenberg Herman H Van
Arnoldus H J Herremans
Original Assignee
Solvay Pharm Bv
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 Solvay Pharm Bv filed Critical Solvay Pharm Bv
Publication of AR036598A1 publication Critical patent/AR036598A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/06—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • 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
    • A61P1/12—Antidiarrhoeals
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • A61P25/22—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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P3/08—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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • A61P9/10—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
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond

Landscapes

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

Abstract

Derivados de 4,5-dihidro-1H-pirazol que son potentes antagonistas de receptores (CB1) de cannabinoides con utilidad para el tratamiento de enfermedades conectadas con desórdenes del sistema cannabinoide. Los compuestos tienen la fórmula general (1) ó (2), en donde: R y R1 representan independientemente fenilo, tienilo o piridilo, cuyos grupos pueden estar sustituidos con 1, 2, ó 3 sustituyentes Y, que pueden ser iguales o diferentes, del grupo alquilo o alcoxi C1-3, hidroxi, halógeno, trifluorometilo, trifluorometiltio, trifluorometoxi, nitro, amino, mono- o dialquil C1-2-amino, mono o dialquil C1-2-amido, alquil C1-3-sulfonilo, dimetilsulfamido, alcoxi C1-3-carbonilo, carboxilo, trifluorometilsulfonilo, ciano, carbamoílo, sulfamoílo y acetilo, o R y/o R1 representa naftilo; R2 representa hidrógeno, hidroxi, alcoxi C1-3, acetiloxi o propioniloxi; R3 representa un átomo de hidrógeno o un grupo alquilo C1-8 ramificado o no ramificado o un grupo cicloalquilo C3-7 cuyo grupo alquilo o gtupo cicloalquilo puede estar sustituido con un grupo hidroxi; R4 representa un átomo de hidrógeno o un grupo molecular alquilo C1-8 ramificado o no ramificado, cicloalquilo C3-8, heteroalquilo C2-10, heterocicloalquilo C3-8 no aromático o heterocicloalquil-alquilo C4-10 no aromático cuyos grupos moleculares pueden contener uno o más heteroátomos del grupo (O, N, S), cuyos grupos moleculares pueden estar sustituidos con un grupo ceto, grupo trifluorometilo, grupo alquilo C1-3, hidroxi, amino, monoalquilamino, o grupo dialquilamino o un átomo de flúor, o R4 representa un grupo amino, hidroxi, fenoxi o benciloxi o R4 representa un grupo alcoxi C1-8, alquenilo C3-8, ramificados o no ramificados, cicloalquenilo C5-8 o cicloalquenilalquilo C6-9 cuyos grupos pueden contener un átomo de azufre, nitrógeno u oxígeno, un grupo ceto o un grupo -SO2- cuyos grupos alcoxi C1-8, alquenilo C3-8, cicloalquenilo C5-8 o cicloalquenilalquilo C6-9 pueden estar sustituidos con un grupo hidroxi, un grupo trifluorometilo, un grupo amino, un grupo monoalquilamino o un grupo dialquilamino o un átomo de flúor, o R4 representa un grupo fenilo, bencilo, piridilo, tienilo, piridilmetilo o fenetilo en donde los anillos aromáticos pueden estar sustituidos con 1, 2 ó 3 de los sustituyentes Y, en donde Y tiene el significado como indicado anteriormente, o R4 representa un grupo NR8R9 con la condición que R3 representa un átomo de hidrógeno o un grupo metilo y en donde R8 y R9 son iguales o diferentes y representan alquilo C1-4 o trifluoroalquilo C2-4 o R8 y R9, junto con el átomo de nitrógeno al cual ellos están unidos, forman un grupo molecular heterocíclico saturado o no saturado que tiene 4 a 8 átomos de anillo cuyo grupo molecular heterocíclico puede contener un átomo de oxígeno o de azufre o un grupo ceto o un grupo -SO2- o un átomo de nitrógeno adicional, cuyo grupo molecular heterocíclico saturado o no saturado puede estar sustituido con un grupo alquilo C1-4 ó R3 y R4, junto con el átomo de nitrógeno al cual ellos están unidos, forman un grupo molecular heterocíclico monocíclico o bicíclico, saturado o no saturado que tiene 4 a 10 átomos de anillo, cuyo grupo molecular heterocíclico puede contener uno o más átomos del grupo (O, N, S) o un grupo ceto o un grupo -SO2-, cuyo grupo molecular puede estar sustituido con un grupo alquilo C1-4, hidroxialquilo, fenilo, tienilo, piridilo, amino, monoalquilaminoalquilo, dialquilaminoalquilo, monoalquilamino, dialquilamino, aminoalquilo, azetidinilo, pirrolidinilo, piperidinilo o hexahidro-1H-azepinilo; R5 y R6 independientemente uno de otro representan un átomo de hidrógeno o un grupo alquilo o alquenilo C1-8 ramificado o no ramificado cuyos grupos pueden contener uno o más heteroátomos del grupo (O, N, S), un grupo ceto o un grupo -SO2- y cuyos grupos pueden estar sustituidos con un grupo hidroxi o amino, o R5 y R6 independientemente uno del otro representan un grupo cicloalquilo C3-8 o un grupo cicloalquenilo C3-8 cuyo grupo puede contener uno o más heteroátomos de anillo del grupo (O, N, S) o el grupo -SO2-, y cuyos grupos pueden estar sustituidos con un grupo hidroxi, alquilo C1-3, el grupo -SO2-, el grupo ceto, el grupo amino, el grupo monoalquil C1-3-amino o el grupo dialquil C1-3-amino, ó R5 representa un grupo naftilo o un grupo fenilo cuyo grupo fenilo puede estar sustituido con 1, 2 ó 3 sustituyentes Y en donde Y tiene el significado como el descripto anteriormente, con la condición que R6 representan un átomo de hidrógeno, o un grupo alquilo C1-5 ramificado o no ramificado cuyo grupo alquilo puede contener uno o más heteroátomos del grupo (O, N, S) o el grupo -SO2- y cuyo grupo alquilo puede estar sustituido con un grupo hidroxi, ceto o amino, o R5 y R6, junto con el átomo de nitrógeno al cual ellos están unidos, forman un grupo alquilo o alquenilo monocíclico, bicíclico o tricíclico el cual puede contener heteroátomos de anillo del grupo (O, N, S), el grupo ceto o el grupo SO2 y cuyo grupo alquilo o alquenilo monocíclico, bicíclico o tricíclico puede estar sustituido con un grupo hidroxi, un grupo alquilo C1-3, un grupo SO2, un grupo ceto, un grupo amino, un grupo monoalquil C1-3-amino, un grupo dialquil C1-3 amino, un grupo pirrolidinilo, un grupo piperidinilo, el cual grupo alquilo o alquenilo monocíclico, bicíclico o tricíclico puede contener un grupo fenilo condensado el cual grupo fenilo condensado puede estar sustituido con 1 ó 2 sustituyentes Y, en donde Y tiene el significado como se describió anteriormente; R7 representa un alquilo C1-3 ramificado o no ramificado, y tautómeros, estereoisómeros, prodrogas y sales de los mismos. Se describen métodos para la preparación de estos compuestos, y composiciones farmacéuticas que contienen uno o más de estos compuestos como un componente activo.
ARP020103508A 2001-09-21 2002-09-18 Derivados de 4,5-dihidro-1h-pirazol que tienen potente actividad antagonista de cb1 AR036598A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP01203849 2001-09-21

Publications (1)

Publication Number Publication Date
AR036598A1 true AR036598A1 (es) 2004-09-22

Family

ID=8181042

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP020103508A AR036598A1 (es) 2001-09-21 2002-09-18 Derivados de 4,5-dihidro-1h-pirazol que tienen potente actividad antagonista de cb1

Country Status (20)

Country Link
US (2) US6974810B2 (es)
EP (1) EP1429762A1 (es)
JP (1) JP4313672B2 (es)
KR (1) KR100950430B1 (es)
CN (2) CN1529595A (es)
AR (1) AR036598A1 (es)
AU (1) AU2002333853B2 (es)
BR (1) BR0208253A (es)
CA (1) CA2442245C (es)
HR (1) HRP20030913A2 (es)
HU (1) HUP0402113A3 (es)
IL (2) IL157704A0 (es)
MX (1) MXPA03009439A (es)
NO (1) NO20041170L (es)
NZ (1) NZ528280A (es)
PL (1) PL367814A1 (es)
RU (1) RU2286988C2 (es)
UA (1) UA77441C2 (es)
WO (1) WO2003026648A1 (es)
ZA (1) ZA200307218B (es)

Families Citing this family (88)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6974810B2 (en) * 2001-09-21 2005-12-13 Solvay Pharmaceuticals B.V. 4,5-Dihydro-1H-pyrazole derivatives having potent CB1-antagonistic activity
ATE486842T1 (de) 2002-03-12 2010-11-15 Merck Sharp & Dohme Substituierte amide
US7129239B2 (en) 2002-10-28 2006-10-31 Pfizer Inc. Purine compounds and uses thereof
US7247628B2 (en) 2002-12-12 2007-07-24 Pfizer, Inc. Cannabinoid receptor ligands and uses thereof
US7772188B2 (en) 2003-01-28 2010-08-10 Ironwood Pharmaceuticals, Inc. Methods and compositions for the treatment of gastrointestinal disorders
US7329658B2 (en) 2003-02-06 2008-02-12 Pfizer Inc Cannabinoid receptor ligands and uses thereof
US7176210B2 (en) 2003-02-10 2007-02-13 Pfizer Inc. Cannabinoid receptor ligands and uses thereof
US7145012B2 (en) 2003-04-23 2006-12-05 Pfizer Inc. Cannabinoid receptor ligands and uses thereof
US7268133B2 (en) 2003-04-23 2007-09-11 Pfizer, Inc. Patent Department Cannabinoid receptor ligands and uses thereof
US7141669B2 (en) 2003-04-23 2006-11-28 Pfizer Inc. Cannabiniod receptor ligands and uses thereof
US7232823B2 (en) 2003-06-09 2007-06-19 Pfizer, Inc. Cannabinoid receptor ligands and uses thereof
US20050239859A2 (en) * 2003-09-03 2005-10-27 Solvay Pharmaceuticals Gmbh Novel medical uses of 4,5-dihydro-1h-pyrazole derivatives having cb1- antagonistic activity
JP2007521322A (ja) * 2003-09-18 2007-08-02 メルク　エンド　カムパニー　インコーポレーテッド 置換スルホンアミド類
CA2543338A1 (en) * 2003-10-24 2005-05-06 Solvay Pharmaceuticals Gmbh Novel medical uses of compounds showing cb1-antagonistic activity and combination treatment involving said compounds
TW200528102A (en) * 2003-10-24 2005-09-01 Solvay Pharm Gmbh Novel medical combination treatment of obesity involving 4,5-dihydro-1h-pyrazole derivatives having cb1-antagonistic activity
US20050124660A1 (en) * 2003-10-27 2005-06-09 Jochen Antel Novel medical uses of compounds showing CB1-antagonistic activity and combination treatment involving said compounds
US20050143441A1 (en) * 2003-10-27 2005-06-30 Jochen Antel Novel medical combination treatment of obesity involving 4,5-dihydro-1H-pyrazole derivatives having CB1-antagonistic activity
TW200522944A (en) 2003-12-23 2005-07-16 Lilly Co Eli CB1 modulator compounds
ATE402697T1 (de) * 2004-01-30 2008-08-15 Solvay Pharm Bv 1,3,5-trisubstituierte 4,5-dihydro-1h-pyrazol- derivative mit cb1-antagonistischer aktivität
US20080125403A1 (en) 2004-04-02 2008-05-29 Merck & Co., Inc. Method of Treating Men with Metabolic and Anthropometric Disorders
TW200602314A (en) 2004-05-28 2006-01-16 Tanabe Seiyaku Co A novel pyrrolidine compound and a process for preparing the same
WO2006025069A2 (en) 2004-07-12 2006-03-09 Cadila Healthcare Limited Tricyclic pyrazole derivatives as cannabinoid receptor modulators
US20060025448A1 (en) 2004-07-22 2006-02-02 Cadila Healthcare Limited Hair growth stimulators
MX2007004889A (es) 2004-10-25 2007-09-11 Solvay Pharm Gmbh Composiciones farmaceuticas que comprenden antagonistas del receptor cannabinoide cb1 y activadores de canales de potasio para el tratamiento de la diabetes mellitus tipo i, la obesidad y trastornos relacionados.
WO2006060461A1 (en) 2004-12-03 2006-06-08 Schering Corporation Substituted piperazines as cb1 antagonists
US7923465B2 (en) 2005-06-02 2011-04-12 Glenmark Pharmaceuticals S.A. Cannabinoid receptor ligands, pharmaceutical compositions containing them, and process for their preparation
EP1902034B1 (en) 2005-06-02 2011-03-30 Glenmark Pharmaceuticals S.A. Novel cannabinoid receptor ligands, pharmaceutical compositions containing them, and process for their preparation
NZ564759A (en) 2005-06-30 2011-08-26 Prosidion Ltd GPCR agonists
EP1743890A1 (en) * 2005-07-15 2007-01-17 Laboratorios Del Dr. Esteve, S.A. 4,5-Dihydro-1H-pyrazole derivatives, their preparation and use as medicaments
CA2619480A1 (en) * 2005-08-17 2007-02-22 Solvay Pharmaceuticals Gmbh Method of using potassium channel inhibiting compounds
BRPI0706623A2 (pt) * 2006-01-18 2011-04-12 Schering Corp moduladores de receptor canabinóide
JP5561720B2 (ja) * 2006-05-05 2014-07-30 ジェンリン ディスカバリー 肥満及び糖尿病を含む心臓血管障害を治療するために有用なカンナビノイド受容体アンタゴニスト／インバ−スアゴニスト
US7964728B2 (en) 2006-07-06 2011-06-21 Solvay Pharmaceuticals B.V. Azaindole derivatives with a combination of partial nicotinic acetyl-choline receptor agonism and dopamine reuptake inhibition
TWI428334B (zh) * 2006-09-22 2014-03-01 Abbvie Bahamas Ltd 作為５-ｈｔ6拮抗劑之磺醯基吡唑及磺醯基吡唑啉的甲脒衍生物
US7923026B2 (en) 2006-10-20 2011-04-12 Solvay Pharmaceuticals B.V. Embedded micellar nanoparticles
AU2007312233B2 (en) * 2006-10-20 2012-09-20 Abbvie B.V. Micellar nanoparticles of chemical substances
AR064736A1 (es) 2007-01-04 2009-04-22 Prosidion Ltd Agonistas de gpcr
WO2008081208A1 (en) 2007-01-04 2008-07-10 Prosidion Limited Piperidine gpcr agonists
BRPI0806498A2 (pt) 2007-01-04 2014-04-22 Prosidion Ltd Agonistas gpcr piperidina
GB0700122D0 (en) 2007-01-04 2007-02-14 Prosidion Ltd GPCR agonists
CL2008000018A1 (es) 2007-01-04 2008-08-01 Prosidion Ltd Compuestos derivados de heterociclos de nitrogeno y oxigeno, agonistas de gpcr; composicion farmaceutica que comprende a dicho compuesto; y uso del compuesto para el tratamiento de la obesidad, diabetes, sindrome metabolico, hiperlipidemia, toleranci
US20100197564A1 (en) * 2007-04-19 2010-08-05 Schering Corporation Diaryl morpholines as cb1 modulators
US8969514B2 (en) 2007-06-04 2015-03-03 Synergy Pharmaceuticals, Inc. Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases
CN101318931B (zh) * 2007-06-04 2010-05-19 上海阳帆医药科技有限公司 二芳基取代吡唑衍生物、其制备方法和用途
MX2009013293A (es) 2007-06-04 2010-02-15 Synergy Pharmaceuticals Inc Agonistas de guanilato ciclasa útiles para el tratamiento de trastornos gastrointestinales, inflamación, cáncer y otros trastornos.
WO2008152086A2 (en) * 2007-06-15 2008-12-18 Solvay Pharmaceuticals B.V. 4,5-dihydro-(1h)-pyrazole derivatives as cannabinoid cb1 receptor modulators
US8410135B2 (en) * 2007-06-15 2013-04-02 Solvay Pharmaceuticals B.V. 4,5 dihydro-(1H)-pyrazole derivatives as cannabinoid CB1 receptor modulators
US20100286160A1 (en) * 2007-06-28 2010-11-11 Intervet Inc. Substituted piperazines as cb1 antagonists
EP2548874A3 (en) * 2007-06-28 2013-05-15 Intervet International B.V. Substituted piperazines as CB1 antagonists
EP2025674A1 (de) 2007-08-15 2009-02-18 sanofi-aventis Substituierte Tetrahydronaphthaline, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
GB0720390D0 (en) 2007-10-18 2007-11-28 Prosidion Ltd G-Protein coupled receptor agonists
GB0720389D0 (en) 2007-10-18 2008-11-12 Prosidion Ltd G-Protein Coupled Receptor Agonists
US7655685B2 (en) 2007-11-02 2010-02-02 Jenrin Discovery, Inc. Cannabinoid receptor antagonists/inverse agonists useful for treating metabolic disorders, including obesity and diabetes
JP5551604B2 (ja) 2007-11-30 2014-07-16 オールトランツ インコーポレイティド テトラヒドロカンナビノールのプロドラッグ、テトラヒドロカンナビノールのプロドラッグを含む組成物、及び同一のものを使用する方法
AR070898A1 (es) 2008-03-18 2010-05-12 Solvay Pharm Bv Derivados de arilsulfonil pirazolin carboxamidina como antagonistas de 5-ht6
EP2810951B1 (en) 2008-06-04 2017-03-15 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
AR071995A1 (es) * 2008-06-16 2010-07-28 Solvay Pharm Bv Derivados de 3,4-diaril-4,5-dihidro-1h-pirazol-1-carboxamidina sustituidos con fluor que tienen actividad antagonista cb1, procesos de preparacion y composiciones farmaceuticas que los contienen
CA2730603C (en) 2008-07-16 2019-09-24 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
AR072539A1 (es) * 2008-08-01 2010-09-01 Solvay Pharm Bv Sintesis de derivados de 3,4-diaril -4,5-dihidro -(1h) - pirazol -1- carboxamida
EP2348857B1 (en) 2008-10-22 2016-02-24 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
JP5557845B2 (ja) 2008-10-31 2014-07-23 メルク・シャープ・アンド・ドーム・コーポレーション 糖尿病用剤として有用な新規環状ベンゾイミダゾール誘導体
WO2010079241A1 (es) 2009-01-12 2010-07-15 Fundacion Hospital Nacional De Paraplejicos Para La Investigacion Y La Integracion Uso de antagonistas y/o agonistas inversos de los receptores cb1 para la preparación de medicamentos que incrementen la excitabilidad de las motoneuronas
US8217038B2 (en) 2009-10-07 2012-07-10 Jenrin Discovery, Inc. Cannabinoid receptor antagonists/inverse agonists useful for treating metabolic disorders, including obesity and diabetes
AR079935A1 (es) 2010-01-29 2012-02-29 Abbott Healthcare Products Bv Sintesis de derivados de pirazolin carboxamidina sustituida
AU2011218830B2 (en) 2010-02-25 2014-07-24 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
US8933024B2 (en) 2010-06-18 2015-01-13 Sanofi Azolopyridin-3-one derivatives as inhibitors of lipases and phospholipases
US9616097B2 (en) 2010-09-15 2017-04-11 Synergy Pharmaceuticals, Inc. Formulations of guanylate cyclase C agonists and methods of use
EP2640381A4 (en) 2010-11-18 2014-05-21 Jenrin Discovery CANNABINOID RECEPTOR ANTAGONISTS / INVERSAGONISTS FOR THE TREATMENT OF METABOLISM DISEASES INCLUDING ADIPOSITAS AND DIABETES
MX348131B (es) 2011-02-25 2017-05-26 Merck Sharp & Dohme Novedosos derivados de azabencimidazol ciclico utiles como agentes antidiabeticos.
EP2683703B1 (de) 2011-03-08 2015-05-27 Sanofi Neue substituierte phenyl-oxathiazinderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung
WO2012120058A1 (de) 2011-03-08 2012-09-13 Sanofi Mit benzyl- oder heteromethylengruppen substituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung
US8809325B2 (en) 2011-03-08 2014-08-19 Sanofi Benzyl-oxathiazine derivatives substituted with adamantane and noradamantane, medicaments containing said compounds and use thereof
WO2013048989A2 (en) * 2011-09-30 2013-04-04 National Health Research Institutes Pyrazole compounds
US8680131B2 (en) 2012-07-25 2014-03-25 Jenrin Discovery, Inc. Cannabinoid receptor antagonists/inverse agonists useful for treating disease conditions, including metabolic disorders and cancers
WO2014022528A1 (en) 2012-08-02 2014-02-06 Merck Sharp & Dohme Corp. Antidiabetic tricyclic compounds
US11155521B2 (en) 2012-11-13 2021-10-26 The United States Of America As Represented By The Secretary, Department Of Health And Human Services Cannabinoid receptor mediating compounds
CA2889697C (en) 2012-11-13 2023-03-14 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Cannabinoid receptor mediating compounds
WO2014130608A1 (en) 2013-02-22 2014-08-28 Merck Sharp & Dohme Corp. Antidiabetic bicyclic compounds
WO2014139388A1 (en) 2013-03-14 2014-09-18 Merck Sharp & Dohme Corp. Novel indole derivatives useful as anti-diabetic agents
JP2016514671A (ja) 2013-03-15 2016-05-23 シナジー ファーマシューティカルズ インコーポレイテッド グアニル酸シクラーゼのアゴニストおよびその使用
JP2016514670A (ja) 2013-03-15 2016-05-23 シナジー ファーマシューティカルズ インコーポレイテッド 他の薬物と組み合わせたグアニル酸シクラーゼ受容体アゴニスト
EA201592263A1 (ru) 2013-06-05 2016-05-31 Синерджи Фармасьютикалз, Инк. Ультрачистые агонисты гуанилатциклазы c, способ их получения и использования
WO2015051496A1 (en) 2013-10-08 2015-04-16 Merck Sharp & Dohme Corp. Antidiabetic tricyclic compounds
CN106660968B (zh) * 2014-05-09 2020-02-07 美国政府(由卫生和人类服务部的部长所代表) 吡唑衍生物及其作为大麻素受体介体的用途
US11072602B2 (en) 2016-12-06 2021-07-27 Merck Sharp & Dohme Corp. Antidiabetic heterocyclic compounds
WO2022128050A1 (en) 2020-12-14 2022-06-23 Symrise Ag Medicament for fighting inflammation and pain
WO2022245627A1 (en) * 2021-05-17 2022-11-24 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services A facile and odor-free approach to convert sulfonyl urea derivatives to chalcogenide sulfonyl urea derivatives
EP4444701A1 (en) * 2021-12-10 2024-10-16 The United States of America, as represented by The Secretary, Department of Health and Human Services Cannabinoid receptor modulating compounds

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL158178B (nl) * 1974-07-12 1978-10-16 Philips Nv Werkwijze ter bereiding van insekticide preparaten die een pyrazolinederivaat bevatten, aldus verkregen gevormde preparaten, en werkwijze ter bereiding van pyrazolinederivaten met insekticide werking.
JPH03173887A (ja) * 1989-03-27 1991-07-29 Nissan Chem Ind Ltd スルタムスルホンアミド及び除草剤
FR2692575B1 (fr) * 1992-06-23 1995-06-30 Sanofi Elf Nouveaux derives du pyrazole, procede pour leur preparation et compositions pharmaceutiques les contenant.
FR2713225B1 (fr) * 1993-12-02 1996-03-01 Sanofi Sa N-pipéridino-3-pyrazolecarboxamide substitué.
FR2789079B3 (fr) * 1999-02-01 2001-03-02 Sanofi Synthelabo Derive d'acide pyrazolecarboxylique, sa preparation, les compositions pharmaceutiques en contenant
JP2004500401A (ja) 2000-03-23 2004-01-08 ソルベイ・フアーマシユーチカルズ・ベー・ブイ Ｃｂ１−拮抗活性を有する４，５−ジヒドロ−１ｈ−ピラゾール誘導体
US6974810B2 (en) * 2001-09-21 2005-12-13 Solvay Pharmaceuticals B.V. 4,5-Dihydro-1H-pyrazole derivatives having potent CB1-antagonistic activity
US20050143441A1 (en) * 2003-10-27 2005-06-30 Jochen Antel Novel medical combination treatment of obesity involving 4,5-dihydro-1H-pyrazole derivatives having CB1-antagonistic activity
US20050124660A1 (en) * 2003-10-27 2005-06-09 Jochen Antel Novel medical uses of compounds showing CB1-antagonistic activity and combination treatment involving said compounds

Also Published As

Publication number Publication date
WO2003026648A1 (en) 2003-04-03
UA77441C2 (en) 2006-12-15
IL157704A (en) 2008-07-08
AU2002333853B2 (en) 2006-07-13
KR100950430B1 (ko) 2010-04-02
NO20041170L (no) 2004-06-21
JP4313672B2 (ja) 2009-08-12
US7608718B2 (en) 2009-10-27
KR20040035845A (ko) 2004-04-29
PL367814A1 (en) 2005-03-07
HUP0402113A2 (hu) 2005-01-28
CN1529595A (zh) 2004-09-15
US6974810B2 (en) 2005-12-13
HUP0402113A3 (en) 2012-05-29
NZ528280A (en) 2005-11-25
MXPA03009439A (es) 2004-02-12
US20070259884A1 (en) 2007-11-08
RU2286988C2 (ru) 2006-11-10
BR0208253A (pt) 2004-04-13
JP2005503428A (ja) 2005-02-03
CA2442245A1 (en) 2003-04-03
CN101195604A (zh) 2008-06-11
ZA200307218B (en) 2005-03-16
HRP20030913A2 (en) 2004-06-30
US20040106800A1 (en) 2004-06-03
RU2003130268A (ru) 2005-01-27
EP1429762A1 (en) 2004-06-23
IL157704A0 (en) 2004-03-28
CA2442245C (en) 2010-03-30

Similar Documents

Publication Publication Date Title
AR036596A1 (es) Derivados de 4,5-dihidro-1h-pirazol que tienen actividad antagonista de cb1
AR039127A1 (es) Compuesto de quinolina, procedimiento para su preparacion, composicion farmaceutica que lo comprende y uso del mismo para la fabricacion de un medicamento
EA200600892A1 (ru) Новые хинолиновые производные
AR036597A1 (es) Derivados de 1h-imidazol que tienen actividad agonista de cb1, agonista parcial de cb1 o antagonista de cb1
ES2137998T3 (es) Nuevos derivados de aminoacidos, procedimiento para su preparacion y composiciones farmaceuticas que contienen estos compuestos.
AR039673A1 (es) Derivados de heteroarilamida benzocondensada de tienopiridinas utiles como agentes terapeuticos, composiciones farmaceuticas que incluyen a los mismos y metodos para su aplicacion
AR065937A2 (es) Compuesto derivado indazol, composicion farmaceutica que lo comprende y su uso en la fabricacion de medicamentos para modular la actividad de proteina quinasa
AR036659A1 (es) Compuestos derivados de fenil-piperazina, fenil-piperidina y fenil-tetrahidropiridina como inhibidores de la reabsorcion de la serotonina, una composicion farmaceutica y utilizacion de los mismos para la preparacion de medicamentos
BR0307409A (pt) Compostos de hidrazida de ácido 2-furanocarboxìlico, composições farmacêuticas contendo os mesmos e uso dos mesmos para preparação de um agente preventivo ou terapêutico
ATE496620T1 (de) 1h-benzo(f)indazol-5-yl-derivate als selektive glucocorticoid-rezeptor-modulatoren
ECSP014097A (es) Derivados de tiofeno utiles como agentes anticancerosos
AR033379A1 (es) Compuestos de difenilurea, procedimiento para su preparacion y composiciones farmaceuticas que los contienen
AR086357A1 (es) Derivados de indazol sustituidos activos como inhibidores de quinasas
EA200500814A1 (ru) Производные пирролопиримидина
AR037534A1 (es) Derivado de adamantano, su uso en la fabricacion de un medicamento para usar en terapia, composicion farmaceutica, proceso para la preparacion de dicho compuesto y dicha composicion y compuestos intermediarios
DE60041763D1 (de) Inhibitoren von c-jun n-terminal kinasen (jnk)
AR058287A1 (es) Derivados de isoquinolina y composicion farmaceutica
BRPI0414514A (pt) uso de um composto, composto, e, composições farmacêuticas
EA200970704A1 (ru) ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ, СОДЕРЖАЩИЕ АНТАГОНИСТЫ NK1 РЕЦЕПТОРА И БЛОКАТОРЫ Na КАНАЛОВ
ATE469157T1 (de) Tetrahydrofuroä3,4-düdioxolverbindungen und zusammensetzungen und verfahren zur inhibierung der trombozytenaggregation
ATE277897T1 (de) Aminobenzophenone als inhibitoren von il-1beta und tnf-alpha
AR041882A1 (es) Compuestos de imidazopiridina, un procedimiento para su preparacion y composiciones farmaceuticas que los contienen
EA200100090A2 (ru) Новые пиперидин-4-сульфонамидные производные, способ их получения и содержащие их фармацевтические композиции
AR056883A1 (es) Derivados de 7-azaindol-2 carboxamida, un proceso para la preparacion de los mismos, composiciones farmaceuticas que los contienen y su uso en la fabricacion de un medicamento para el tratamiento de enfermedades asociadas con la modulacion de receptores de h3
DE602004023926D1 (de) Selektive spirocyclische glucocorticoid-rezeptor-modulatoren

Legal Events

Date Code Title Description
FB Suspension of granting procedure