WO2001058450A2 - Utilisation d'un antagoniste des recepteurs aux cannabinoides centraux pour la preparation de medicaments utiles pour faciliter l'arret de la consommation de tabac - Google Patents

Utilisation d'un antagoniste des recepteurs aux cannabinoides centraux pour la preparation de medicaments utiles pour faciliter l'arret de la consommation de tabac Download PDF

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Publication number
WO2001058450A2
WO2001058450A2 PCT/FR2001/000356 FR0100356W WO0158450A2 WO 2001058450 A2 WO2001058450 A2 WO 2001058450A2 FR 0100356 W FR0100356 W FR 0100356W WO 0158450 A2 WO0158450 A2 WO 0158450A2
Authority
WO
WIPO (PCT)
Prior art keywords
solvates
methylpyrazole
piperidino
dichlorophenyl
carboxamide
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.)
Ceased
Application number
PCT/FR2001/000356
Other languages
English (en)
French (fr)
Other versions
WO2001058450A3 (fr
Inventor
Jean Charles Blanchard
François MENARD
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.)
Sanofi Aventis France
Original Assignee
Sanofi Synthelabo SA
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
Priority to DE60109903T priority Critical patent/DE60109903T2/de
Priority to EEP200200439A priority patent/EE04836B1/xx
Priority to HU0300237A priority patent/HU225328B1/hu
Priority to PL358221A priority patent/PL201685B1/pl
Application filed by Sanofi Synthelabo SA filed Critical Sanofi Synthelabo SA
Priority to IL15071001A priority patent/IL150710A0/xx
Priority to AU35620/01A priority patent/AU781827B2/en
Priority to NZ519924A priority patent/NZ519924A/en
Priority to HK03103301.5A priority patent/HK1051140B/xx
Priority to JP2001557560A priority patent/JP2003522145A/ja
Priority to CA002397262A priority patent/CA2397262C/en
Priority to DK01907722T priority patent/DK1257275T3/da
Priority to EP01907722A priority patent/EP1257275B1/fr
Priority to AT01907722T priority patent/ATE292467T1/de
Priority to SI200130365T priority patent/SI1257275T1/xx
Priority to SK1129-2002A priority patent/SK284952B6/sk
Priority to US10/203,077 priority patent/US6930122B2/en
Priority to MXPA02007766A priority patent/MXPA02007766A/es
Priority to BR0108126-8A priority patent/BR0108126A/pt
Priority to UA2002075476A priority patent/UA72783C2/uk
Publication of WO2001058450A2 publication Critical patent/WO2001058450A2/fr
Publication of WO2001058450A3 publication Critical patent/WO2001058450A3/fr
Priority to IS6450A priority patent/IS6450A/is
Priority to BG106946A priority patent/BG65856B1/bg
Priority to NO20023765A priority patent/NO324521B1/no
Anticipated expiration legal-status Critical
Priority to US11/113,864 priority patent/US20050187253A1/en
Ceased legal-status Critical Current

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/34—Tobacco-abuse

Definitions

  • the present invention relates to a new use of a central cannabinoid receptor antagonist called CB1 receptors. More specifically. the invention relates to the use of a CB 1 receptor antagonist for the preparation of medicaments useful for facilitating the cessation of tobacco consumption.
  • 4-methylpyrazole-3-carboxamide hereinafter called compound A, of formula: its pharmaceutically acceptable salts and their solvates, are described in European patent EP-656 354 and by M. Rinaldi-Carmona et al. (FEBS Lett, 1994, 350, 240-2424), as central CB receptor antagonists.
  • the compound A and its salts which are central cannabinoid receptor antagonists can be used for the treatment of appetite disorders, in particular as an appetite suppressant, and in the treatment of disorders linked to the use of psychotropic substances.
  • international application WO99 / 00119 discloses the use of central cannabinoid receptor antagonists to treat appetite disorders, that is to say to regulate the desires for consumption, in particular for the consumption of sugars, of carbohydrates. alcohol or drugs and more generally appetizing ingredients.
  • compound A its pharmaceutically acceptable salts and their solvates make it possible to facilitate the cessation of tobacco consumption, that they are useful in the treatment of nicotine dependence and / or in the treatment of nicotine withdrawal symptoms.
  • compound A of one of its pharmaceutically acceptable salts or solvates, makes it possible to observe in consumers of nicotine such as tobacco smokers, total or partial smoking abstinence early or delayed.
  • the symptoms of nicotine withdrawal are very significantly reduced or even eliminated, and weight gain following cessation of smoking is reduced or nonexistent.
  • the present invention relates to the use of N-piperidino-5- (4-chlorophenyl) - 1 - (2.4-dichlorophenyl) -4-methylpyrazole-3-carboxamide, of one of its pharmaceutically acceptable salts or one of their solvates for the preparation of medicaments useful in facilitating the cessation of tobacco consumption, in the treatment of nicotine dependence and / or in the treatment of symptoms of nicotine withdrawal.
  • compound A one of its pharmaceutically acceptable salts or one of their solvates, in combination with another active principle, for the preparation of medicaments useful for facilitating the cessation of tobacco consumption, in the treatment of nicotine dependence and / or in the treatment of symptoms of nicotine withdrawal.
  • compound A can be combined
  • MAOI monoamine oxidase inhibitor
  • any other active ingredient that has demonstrated effectiveness in facilitating the cessation of tobacco consumption for example an antidepressant such as bupropion, doxepine, nortriptyline or an anxiolytic such as buspirone, or even clonidine.
  • an antidepressant such as bupropion, doxepine, nortriptyline or an anxiolytic such as buspirone, or even clonidine.
  • compound A For its use as a medicament, compound A, one of its pharmaceutically acceptable salts or one of their solvates, alone or in combination with another active principle, must be formulated in pharmaceutical composition.
  • the present invention also relates to pharmaceutical compositions containing in combination N-piperidino-5- (4-chlorophenyl) -l- (2,4-dichlorophenyl) -4-methylpyrazole-3-carboxamide, one of its pharmaceutically salts acceptable or one of their solvates and another active principle, the other active principle being a compound useful for facilitating the cessation of tobacco consumption, and / or useful in the treatment of nicotine dependence and / or in the treatment of nicotine withdrawal symptoms.
  • Said other active principle being preferably chosen from:
  • a nicotinic agonist or a partial nicotinic agonist or else - a monoamine oxidase inhibitor (MAOI)
  • compositions of the present invention for oral, sublingual, subcutaneous, intramuscular, intravenous, transdermal, local or rectal administration, the active principle, alone or in combination with another active principle, can be administered in unit form administration, mixed with conventional pharmaceutical carriers, animals and humans.
  • Suitable unit dosage forms include oral forms such as tablets, capsules, pills, powders, granules, chewing gum and oral solutions or suspensions, sublingual and buccal forms of administration, aerosols, implants, local, transdermal, subcutaneous, intramuscular, intravenous, intranasal or intraocular administration forms and forms of rectal administration.
  • the active principle or the active principles are generally formulated in dosage units.
  • the dosage unit contains 0.5 to 300 mg, advantageously from 5 to 60 mg, preferably from 5 to 40 mg per dosage unit, for daily administrations, one or more times a day.
  • the appropriate dosage for each patient is determined by the doctor according to the mode of administration, the age, the weight and the response of said patient.
  • a solid composition is prepared in the form of tablets, it is possible to add to the active ingredient (s) micronized (s) or not a wetting agent such as sodium lauryl sulfate and the whole is mixed with a pharmaceutical vehicle such as silica, starch, lactose, magnesium stearate, talc or the like.
  • a pharmaceutical vehicle such as silica, starch, lactose, magnesium stearate, talc or the like.
  • the tablets can be coated with sucrose, various polymers or other suitable materials or else they can be treated in such a way that they have a prolonged or delayed activity and that they continuously release a predetermined quantity of active principle.
  • a preparation in capsules is obtained by mixing the active principle or the active principles with a diluent such as a glycol or a glycerol ester and by incorporating the mixture obtained in soft or hard capsules.
  • a preparation in the form of a syrup or elixir may contain the active principle or active principles together with a sweetener, preferably calorie-free, methylparaben and propylparaben as antiseptics, as well as a flavoring agent and an appropriate color.
  • the powders or granules dispersible in water can contain the active principle or the active principles in mixture with dispersing agents or wetting agents, or suspending agents, such as polyvinylpyrrolidone or polyvidone, as well as with sweeteners or flavor correctors.
  • Suppositories are used for rectal administration which are prepared with binders that melt at rectal temperature, for example cocoa butter or polyethylene glycols.
  • aqueous suspensions, isotonic saline solutions or sterile injectable solutions which contain pharmacologically compatible dispersing agents and / or solubilizing agents, for example propylene glycol or butylene glycol.
  • a cosolvent for example an alcohol such as ethanol or a glycol such as polyethylene glycol or propylene glycol, and a hydrophilic surfactant such as polysorbate 80 can be used.
  • the active principle can be dissolved by a triglyceride or a glycerol ester.
  • the active principle is in alcoholic solution.
  • the active principle or the active principles can also be formulated in the form of microcapsules or microspheres, optionally with one or more carriers or additives.
  • the active principle or the active principles can also be presented in the form of a complex with a cyclodextrin, for example ⁇ -, ⁇ - or ⁇ -cyclodextrin, 2-hydroxypropyl- ⁇ -cyclodextrin or methyl- ⁇ -cyclodextrin.
  • a sustained-release form useful in the case of chronic treatments, implants can be used. These can be prepared in the form of an oily suspension or in the form of a suspension of microspheres in an isotonic medium.
  • compound A is administered by the oral route, in a single dose per day.
  • compound A, one of its pharmaceutically acceptable salts or one of their solvates and the other associated active principle can be administered simultaneously, separately or spread over time to facilitate the cessation of tobacco consumption.
  • simultaneous use is understood to mean the administration of the compounds of the composition according to the invention included in one and the same pharmaceutical form.
  • separatate use is meant the administration, at the same time, of the two compounds of the composition according to the invention each included in a separate pharmaceutical form.
  • use spread over time is understood to mean the successive administration of the first compound of the composition according to the invention, included in a pharmaceutical form, then of the second compound of the composition according to the invention, included in a pharmaceutical form separate.
  • the period of time between the administration of the first compound of the composition according to the invention and the administration of the second compound of the same composition according to the invention does not exceed usually not 24 hours.
  • the pharmaceutical forms comprising either only one of the constituent compounds of the composition according to the invention or the combination of the two compounds, which can be used in the different types of uses described above, may for example be suitable for oral, nasal, parenteral or transdermal administration.
  • two distinct pharmaceutical forms can be intended for the same route of administration or for a different route of administration (oral and transdermal or oral and nasal or parenteral and transdermal etc).
  • the invention therefore also relates to a kit for facilitating the cessation of the consumption of tobacco containing the compound A and another active ingredient facilitating the cessation of the consumption of tobacco in which the said compound A and the said active ingredient are in separate compartments and in similar or different packaging, and are intended to be administered simultaneously, separately or spread over time.
  • Said active principle is preferably chosen from:
  • LMAO monoamine oxidase inhibitor
  • any other active ingredient that has demonstrated efficacy in facilitating cessation of tobacco consumption for example an antidepressant such as bupropion, doxepine, nortriptyline or an anxiolytic such as buspirone, or clonidine.
  • an antidepressant such as bupropion, doxepine, nortriptyline or an anxiolytic such as buspirone, or clonidine.
  • the invention also relates to a method for facilitating the cessation of tobacco consumption which consists in administering to a nicotine consumer a therapeutically effective amount of compound A, of one of its pharmaceutically acceptable salts or one of their solvates.
  • Compound A administered at a dose of 0.3 mg / kg and 1 mg / kg statistically significantly decreases the number of nicotine injections in rats who have learned to self-administer nicotine intravenously.
  • EXAMPLE 5 tablet dosed at 30 mg of compound A.
  • Purified water Q.S. For a tablet finished at 400 mg

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  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Neurosurgery (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Addiction (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
PCT/FR2001/000356 2000-02-09 2001-02-07 Utilisation d'un antagoniste des recepteurs aux cannabinoides centraux pour la preparation de medicaments utiles pour faciliter l'arret de la consommation de tabac Ceased WO2001058450A2 (fr)

Priority Applications (23)

Application Number Priority Date Filing Date Title
EP01907722A EP1257275B1 (fr) 2000-02-09 2001-02-07 Utilisation d'un antagoniste des recepteurs aux cannabinoides centraux pour la preparation de medicaments utiles pour faciliter l'arret de la consommation de tabac
HU0300237A HU225328B1 (en) 2000-02-09 2001-02-07 Use of n-piperidino-5-(chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-pyrazole-3-carboxamide for preparing pharmaceutical compositions designed to facilitate smoking cessation
PL358221A PL201685B1 (pl) 2000-02-09 2001-02-07 Zastosowanie N-piperydyno-5-(4-chlorofenylo)-1-(2,4-dichlorofenylo)-4-metylopirazolo-3-karboksyamidu do wytwarzania leków
SI200130365T SI1257275T1 (en) 2000-02-09 2001-02-07 Use of central cannabinoid receptor antagonist for preparing medicines designed to facilitate smoking cessation
IL15071001A IL150710A0 (en) 2000-02-09 2001-02-07 Use of a central cannabinoid receptor antagonist for preparing medicines designed to facilitate smoking cessation
AU35620/01A AU781827B2 (en) 2000-02-09 2001-02-07 Use of central cannabinoid receptor antagonist for preparing medicines designed to facilitate smoking cessation
NZ519924A NZ519924A (en) 2000-02-09 2001-02-07 Use of central cannabinoid receptor antagonist for preparing medicines designed to facilitate smoking cessation
HK03103301.5A HK1051140B (en) 2000-02-09 2001-02-07 Use of central cannabinoid receptor antagonist for preparing medicines designed to facilitate smoking cessation
EEP200200439A EE04836B1 (et) 2000-02-09 2001-02-07 N-piperidino-5-(4-klorofenüül)-1-(2,4-diklorofenüül)-4-metüülpürasool-3-karboksamii di kasutamine ravimtoodete valmistamiseks, aitamaks loobuda tubakatarbimisest
CA002397262A CA2397262C (en) 2000-02-09 2001-02-07 Use of central cannabinoid receptor antagonist for preparing medicines designed to facilitate smoking cessation
DK01907722T DK1257275T3 (da) 2000-02-09 2001-02-07 Anvendelse af en antagonist til centrale cannabiboidreceptorer til fremstilling af lægemidler, der er nyttige for at göre det lettere at ophöre med brug af tobak
JP2001557560A JP2003522145A (ja) 2000-02-09 2001-02-07 セントラルカンナビノイドレセプター拮抗剤のタバコ消費を止める助けに有用である医薬品への使用
AT01907722T ATE292467T1 (de) 2000-02-09 2001-02-07 Verwendung eines zentralen cannabinoid-rezeptor- antagonisten für die herstelling von arzneimitteln zur erleichterung der aufgabe des tabakverbrauchs
DE60109903T DE60109903T2 (de) 2000-02-09 2001-02-07 Verwendung eines zentralen cannabinoid-rezeptor-antagonisten für die herstelling von arzneimitteln zur erleichterung der aufgabe des tabakverbrauchs
SK1129-2002A SK284952B6 (sk) 2000-02-09 2001-02-07 Použitie N-piperidino-5-(4-chlórfenyl)-1-(2,4-dichlórfenyl)-4- metylpyrazol-3-karboxamidu na prípravu liečebných prostriedkov, farmaceutická kompozícia a súprava s jeho obsahom
US10/203,077 US6930122B2 (en) 2000-02-09 2001-02-07 Use of central cannabinoid receptor antagonist for preparing medicines designed to facilitate smoking cessation
MXPA02007766A MXPA02007766A (es) 2000-02-09 2001-02-07 Utilizacion de un antagonista de los receptores a los canabinoides centrales para la preparacion de medicamentos utiles para facilitar la interrupcion del consumo de tabaco.
BR0108126-8A BR0108126A (pt) 2000-02-09 2001-02-07 Utilização de um antagonista dos receptores aos canabinóides centrais para o preparo de medicamentos úteis para facilitar a parada do consumo de tabaco
UA2002075476A UA72783C2 (en) 2000-02-09 2001-07-02 Agonist of central canabinoid receptors for preparation of drug disaccustoming smoking, combined pharmaceutical composition and kit
IS6450A IS6450A (is) 2000-02-09 2002-06-28 Notkun á miðju-kannabinóið-viðtaka mótlyfi til aðframleiða lyf sem eru hönnuð til að auðvelda að hætta að reykja
BG106946A BG65856B1 (bg) 2000-02-09 2002-07-23 Използване на антагонисти на централни канабиноидни рецептори за получаване на лекарствени средства за улесняване спирането на консумацията на тютюн
NO20023765A NO324521B1 (no) 2000-02-09 2002-08-08 Anvendelse av sentrale cannabinoidreseptor-antagonister for fremstilling av legemidler som er anvendbare for a fremme stans av tobakksforbruk, farmasoytisk preparat, og sett.
US11/113,864 US20050187253A1 (en) 2000-02-09 2005-04-25 Medicinal kit to quit tobacco consumption comprising central cannabinoid receptor antagonist

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
FR0001682A FR2804604B1 (fr) 2000-02-09 2000-02-09 Utilisation d'un antagoniste des recepteurs aux cannabinoides centraux pour la preparation de medicaments utiles pour faciliter l'arret de la consommation de tabac
FR00/01682 2000-02-09

Related Child Applications (1)

Application Number Title Priority Date Filing Date
US11/113,864 Continuation US20050187253A1 (en) 2000-02-09 2005-04-25 Medicinal kit to quit tobacco consumption comprising central cannabinoid receptor antagonist

Publications (2)

Publication Number Publication Date
WO2001058450A2 true WO2001058450A2 (fr) 2001-08-16
WO2001058450A3 WO2001058450A3 (fr) 2002-04-25

Family

ID=8846875

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/FR2001/000356 Ceased WO2001058450A2 (fr) 2000-02-09 2001-02-07 Utilisation d'un antagoniste des recepteurs aux cannabinoides centraux pour la preparation de medicaments utiles pour faciliter l'arret de la consommation de tabac

Country Status (32)

Country Link
US (2) US6930122B2 (https=)
EP (1) EP1257275B1 (https=)
JP (2) JP2003522145A (https=)
CN (1) CN1250220C (https=)
AR (1) AR028505A1 (https=)
AT (1) ATE292467T1 (https=)
AU (1) AU781827B2 (https=)
BG (2) BG110386A (https=)
BR (1) BR0108126A (https=)
CA (1) CA2397262C (https=)
CZ (1) CZ296685B6 (https=)
DE (1) DE60109903T2 (https=)
DK (1) DK1257275T3 (https=)
EE (1) EE04836B1 (https=)
ES (1) ES2240416T3 (https=)
FR (1) FR2804604B1 (https=)
HU (1) HU225328B1 (https=)
IL (1) IL150710A0 (https=)
IS (1) IS6450A (https=)
MX (1) MXPA02007766A (https=)
NO (1) NO324521B1 (https=)
NZ (1) NZ519924A (https=)
PL (1) PL201685B1 (https=)
PT (1) PT1257275E (https=)
RS (1) RS50404B (https=)
RU (1) RU2257207C2 (https=)
SI (1) SI1257275T1 (https=)
SK (1) SK284952B6 (https=)
TW (1) TWI243677B (https=)
UA (1) UA72783C2 (https=)
WO (1) WO2001058450A2 (https=)
ZA (1) ZA200205317B (https=)

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EP1266657A1 (en) * 2001-06-14 2002-12-18 USV Limited Cyclodextrin stabilized pharmaceutical compositions of bupropion hydrochloride
US6825209B2 (en) 2002-04-15 2004-11-30 Research Triangle Institute Compounds having unique CB1 receptor binding selectivity and methods for their production and use
WO2004098580A3 (en) * 2003-05-09 2005-01-06 Pfizer Prod Inc A pharmaceutical composition for the prevention and treatment of nicotine addiction in a mammal
WO2004098641A3 (en) * 2003-05-09 2005-01-20 Pfizer Prod Inc A pharmaceutical composition for the treatment of obesity or to facilitate or promote weight loss
US6972295B2 (en) 2002-03-12 2005-12-06 Merck & Co., Inc. Substituted amides
EP1623741A2 (en) 2004-07-22 2006-02-08 Cadila Healthcare Ltd. Cannabinoid receptor ligands for hair growth modulation
US7091216B2 (en) 2002-08-02 2006-08-15 Merck & Co., Inc. Substituted furo[2,3-b]pyridine derivatives
US7129239B2 (en) 2002-10-28 2006-10-31 Pfizer Inc. Purine compounds and uses thereof
US7145012B2 (en) 2003-04-23 2006-12-05 Pfizer Inc. Cannabinoid receptor ligands and uses thereof
US7176210B2 (en) 2003-02-10 2007-02-13 Pfizer Inc. Cannabinoid receptor ligands and uses thereof
US7247628B2 (en) 2002-12-12 2007-07-24 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
US7271266B2 (en) 2002-03-28 2007-09-18 Merck & Co., Inc. Substituted 2,3-diphenyl pyridines
US7329658B2 (en) 2003-02-06 2008-02-12 Pfizer Inc Cannabinoid receptor ligands and uses thereof
US7348456B2 (en) 2002-12-19 2008-03-25 Merck & Co., Inc. Substituted amides
US7351729B2 (en) 2002-03-08 2008-04-01 Signal Pharmaceuticals, Llc JNK inhibitors for use in combination therapy for treating or managing proliferative disorders and cancers
WO2008046905A1 (en) * 2006-10-20 2008-04-24 Solvay Pharmaceuticals B.V. Micellar nanoparticles of chemical substances
US7405221B2 (en) 2002-09-27 2008-07-29 Merck & Co., Inc. Substituted pyrimidines
US7423067B2 (en) 2002-03-26 2008-09-09 Merck & Co., Inc. Diphenyl cyclopentyl amides as cannabinoid-1 receptor inverse agonists
EP2095814A1 (de) * 2008-02-26 2009-09-02 Wolfgang J. Kox Medikamentengestützter Nikotinentzug
US7667053B2 (en) 2002-04-12 2010-02-23 Merck & Co., Inc. Bicyclic amides
EP2343302A1 (en) 2004-07-12 2011-07-13 Cadila Healthcare Limited Tricyclic pyrazole derivatives as cannabinoid receptor modulators

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FR2804604B1 (fr) * 2000-02-09 2005-05-27 Sanofi Synthelabo Utilisation d'un antagoniste des recepteurs aux cannabinoides centraux pour la preparation de medicaments utiles pour faciliter l'arret de la consommation de tabac
US8129253B2 (en) 2001-08-13 2012-03-06 Finisar Corporation Providing current control over wafer borne semiconductor devices using trenches
US7169942B2 (en) * 2003-05-20 2007-01-30 University Of Tennessee Research Foundation Cannabinoid derivatives, methods of making, and use thereof
US7232823B2 (en) 2003-06-09 2007-06-19 Pfizer, Inc. Cannabinoid receptor ligands and uses thereof
WO2005044785A1 (en) * 2003-10-30 2005-05-19 Merck & Co., Inc. Aralkyl amines as cannabinoid receptor modulators
CN101115726A (zh) 2004-12-03 2008-01-30 先灵公司 作为cb1拮抗剂的取代哌嗪
AR059021A1 (es) * 2006-01-18 2008-03-05 Schering Corp Moduladores de receptores cannabinoides
WO2007121687A1 (en) * 2006-04-26 2007-11-01 Institute Of Pharmacology And Toxicology Academy Of Military Medical Sciences P.L.A. China 4-methyl-1h-diaryl pyrazole derivatives and their uses as medicament
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