Abrégé

The present invention relates to a compound of formula (3Z,5S)-5-(hydroxymethyl)-1-[(2′-methyl-1,1′-biphenyl-4-yl)carbonyl]pyrrolidin-3-one O-methl9243yloxime, and/or an active metabolite thereof having antagonist action at the oxytocin receptor and/or vasopressin V1a receptor, to processes for their preparation, pharmaceutical compositions containing them and their use.

Classes IPC  ?

• C07D 207/22 - Composés hétérocycliques contenant des cycles à cinq chaînons, non condensés avec d'autres cycles, ne comportant qu'un atome d'azote comme unique hétéro-atome du cycle avec uniquement des atomes d'hydrogène ou de carbone liés directement à l'atome d'azote du cycle comportant une liaison double entre chaînons cycliques ou entre chaînon cyclique et chaînon non cyclique avec des hétéro-atomes ou avec des atomes de carbone comportant trois liaisons à des hétéro-atomes, avec au plus une liaison à un halogène, p. ex. radicaux ester ou nitrile, liés directement aux atomes de carbone du cycle
• A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
• A61K 31/40 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil
• C07D 207/09 - Radicaux substitués par des atomes d'azote ne faisant pas partie d'un radical nitro

Abrégé

The present invention relates to solid oral formulations comprising a compound of formula (3Z,5S)-5-(hydroxymethyl)-1-[(2′-methyl-1,1′-biphenyl-4-yl)carbonyl]pyrrolidin-3-one-O-methyloxime, and/or an active metabolite thereof, and the use of said formulations in the treatment and/or prevention of preterm labor, premature birth, dysmenorrhea and embryo implantation failure due to uterine contractions. The present invention is furthermore related to processes for their preparation.

Classes IPC  ?

• A61K 31/40 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil
• A61K 31/401 - ProlineSes dérivés, p. ex. captopril
• A61K 9/20 - Pilules, pastilles ou comprimés
• A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
• A61K 47/40 - CyclodextrinesLeurs dérivés
• A61P 15/08 - Médicaments pour le traitement des troubles génitaux ou sexuelsContraceptifs pour les troubles gonadiques ou pour augmenter la fertilité, p. ex. inducteurs d'ovulation ou de spermatogénèse
• A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p. ex. composés antiphlogistiques et pour le cœur

Abrégé

The disclosure provides compositions and methods for determining the propensity of a subject (e.g., a female human subject) undergoing embryo transfer therapy to benefit from administration of an oxytocin receptor antagonist, as well as for treating such patients accordingly. Using the compositions and methods of the disclosure, a subject undergoing embryo transfer therapy may be selected for treatment with an oxytocin receptor antagonist on the basis of a pre-treatment gene signature. Additionally or alternatively, a subject that is undergoing embryo transfer therapy and that has been administered an oxytocin receptor antagonist may be monitored following treatment to determine whether the subject is responding to the oxytocin receptor antagonist or if subsequent dosing is desirable. Exemplary oxytocin receptor antagonists useful in conjunction with the compositions and methods of the disclosure include pyrrolidin-3-one oxime compounds, such as (3Z,5S)-5-(hydroxymethyl)-1-[(2′-methyl-1,1′-biphenyl-4-yl)carbonyl]pyrrolidin-3-one O-methyloxime, among others.

Classes IPC  ?

• C12Q 1/6883 - Produits d’acides nucléiques utilisés dans l’analyse d’acides nucléiques, p. ex. amorces ou sondes pour les maladies provoquées par des altérations du matériel génétique
• A61K 31/404 - Indoles, p. ex. pindolol
• A61K 31/4025 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil non condensés et contenant d'autres hétérocycles, p. ex. cromakalim
• A61K 31/5377 - 1,4-Oxazines, p. ex. morpholine non condensées et contenant d'autres hétérocycles, p. ex. timolol
• A61K 38/24 - Hormone folliculostimulante [FSH]Gonadotropines chorioniques, p. ex. HCGHormone lutéinisante [LH]Hormone thyréotrope [TSH]
• A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
• A61K 9/20 - Pilules, pastilles ou comprimés
• A61P 15/08 - Médicaments pour le traitement des troubles génitaux ou sexuelsContraceptifs pour les troubles gonadiques ou pour augmenter la fertilité, p. ex. inducteurs d'ovulation ou de spermatogénèse

Abrégé

The disclosure provides compositions and methods for the use of oxytocin antagonists, such as substituted pyrrolidin-3-one oxime derivatives of formula (I), among other compounds, in the treatment of subjects undergoing embryo transfer therapy. The compositions and methods of the disclosure can be used to dose subjects with oxytocin antagonists, including (3Z,5S)-5-(hydroxymethyl)-1-[(2′-methyl-1,1′-biphenyl-4-yl)carbonyl]pyrrolidin-3-one O-methyloxime, among others, so as to improve endometrial receptivity and reduce the likelihood of embryo implantation failure and miscarriage following, for example, in vitro fertilization (IVF) and intra cytoplasmic sperm injection (ICSI) embryo transfer procedures. The disclosure provides compositions and methods for the use of oxytocin antagonists, such as substituted pyrrolidin-3-one oxime derivatives of formula (I), among other compounds, in the treatment of subjects undergoing embryo transfer therapy. The compositions and methods of the disclosure can be used to dose subjects with oxytocin antagonists, including (3Z,5S)-5-(hydroxymethyl)-1-[(2′-methyl-1,1′-biphenyl-4-yl)carbonyl]pyrrolidin-3-one O-methyloxime, among others, so as to improve endometrial receptivity and reduce the likelihood of embryo implantation failure and miscarriage following, for example, in vitro fertilization (IVF) and intra cytoplasmic sperm injection (ICSI) embryo transfer procedures.

Classes IPC  ?

• A61K 31/40 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil
• A61K 38/24 - Hormone folliculostimulante [FSH]Gonadotropines chorioniques, p. ex. HCGHormone lutéinisante [LH]Hormone thyréotrope [TSH]
• A61P 15/06 - Agents antiabortifsTocolytiques

Abrégé

The disclosure provides compositions and methods for delaying the onset of delivery in a pregnant subject, such as a pregnant human subject, that is undergoing or at risk of undergoing preterm labor at a gestational age of from about 24 weeks to about 34 weeks. Using the compositions and methods described herein, such subjects may be administered atosiban in combination with a prostaglandin F2α (PGF2α) antagonist. Exemplary PGF2α receptor antagonists that may be used for the treatment or prevention of preterm labor as described herein include 1,3-thiazolidine-2-carboxamide compounds, such as (3S)-3-({[(2S)-3-(biphenyl-4-ylsulfonyl)-1,3-thiazolidin-2-yl]carbonyl}-amino)-3-(4-fluorophenyl)propyl L-valinate or a pharmaceutically acceptable salt thereof (e.g., (3S)-3-({[(2S)-3-(biphenyl-4-ylsulfonyl)-1,3-thiazolidin-2-yl]carbonyl}-amino)-3-(4-fluorophenyl)propyl L-valinate hydrochloride). The compositions and methods described herein provide various clinical benefits. Delivery at an early gestational age is a leading cause of perinatal mortality. By delaying labor in pregnant human patients at an early gestational age, the compositions and methods of the disclosure provide unborn infants with additional time to develop vital organs and tissue systems, thereby significantly improving the likelihood of survival following delivery. The compositions and methods described herein may be used to delay the onset of delivery by one or more hours, days, or weeks, for example, so as to enable pregnant subjects to reach a gestational age at which parturition is substantially safer.

Classes IPC  ?

• A61K 31/426 - 1,3-Thiazoles
• A61K 31/401 - ProlineSes dérivés, p. ex. captopril
• A61K 38/095 - Oxytocines Vasopressines Peptides apparentés
• A61P 5/12 - Médicaments pour le traitement des troubles du système endocrinien des hormones de l'hypophyse postérieure, p. ex. ocytocine, ADH pour réduire, bloquer ou contrarier l'activité des hormones de l'hypophyse postérieure

Abrégé

The disclosure provides compositions and methods for determining the propensity of a subject (e.g., a female human subject) undergoing embryo transfer therapy to benefit from administration of an oxytocin receptor antagonist, as well as for treating such patients accordingly. Using the compositions and methods of the disclosure, a subject undergoing embryo transfer therapy may be selected for treatment with an oxytocin receptor antagonist on the basis of a pre-treatment gene signature. Additionally or alternatively, a subject that is undergoing embryo transfer therapy and that has been administered an oxytocin receptor antagonist may be monitored following treatment to determine whether the subject is responding to the oxytocin receptor antagonist or if subsequent dosing is desirable. Exemplary oxytocin receptor antagonists useful in conjunction with the compositions and methods of the disclosure include pyrrolidin-3-one oxime compounds, such as (3Z,5S)-5-(hydroxymethyl)-1-[(2'-methyl- 1,1'-biphenyl-4-yl)carbonyl]pyrrolidin-3-one O-methyloxime, among others.

Classes IPC  ?

• C12Q 1/6883 - Produits d’acides nucléiques utilisés dans l’analyse d’acides nucléiques, p. ex. amorces ou sondes pour les maladies provoquées par des altérations du matériel génétique
• A61K 38/24 - Hormone folliculostimulante [FSH]Gonadotropines chorioniques, p. ex. HCGHormone lutéinisante [LH]Hormone thyréotrope [TSH]

Abrégé

The disclosure provides compositions and methods for the use of oxytocin antagonists, such as substituted pyrrolidin-3-one oxime derivatives of formula (I), among other compounds, in the treatment of subjects undergoing embryo transfer therapy. The compositions and methods of the disclosure can be used to dose subjects with oxytocin antagonists, including (3Z,5S)-5-(hydroxymethyl)-l-[(2'- methyl-l,l'-biphenyl-4-yl)carbonyl]pyrrolidin-3-one O-methyloxime, among others, so as to improve endometrial receptivity and reduce the likelihood of embryo implantation failure and miscarriage following, for example, in vitro fertilization (IVF) and intra cytoplasmic sperm injection (ICSI) embryo transfer procedures. (Formula I)

Classes IPC  ?

• A61K 31/40 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil
• A61P 5/10 - Médicaments pour le traitement des troubles du système endocrinien des hormones de l'hypophyse postérieure, p. ex. ocytocine, ADH
• A61P 15/06 - Agents antiabortifsTocolytiques

Abrégé

The present invention relates to a compound of formula (3Z,5S)-5-(hydroxymethyl)-1-[(2′-methyl-1,1′-biphenyl-4-yl)carbonyl]pyrrolidin-3-one O-meth19243yloxime, and/or an active metabolite thereof having antagonist action at the oxytocin receptor and/or vasopressin V1a receptor, to processes for their preparation, pharmaceutical compositions containing them and their use.

Classes IPC  ?

• C07D 207/22 - Composés hétérocycliques contenant des cycles à cinq chaînons, non condensés avec d'autres cycles, ne comportant qu'un atome d'azote comme unique hétéro-atome du cycle avec uniquement des atomes d'hydrogène ou de carbone liés directement à l'atome d'azote du cycle comportant une liaison double entre chaînons cycliques ou entre chaînon cyclique et chaînon non cyclique avec des hétéro-atomes ou avec des atomes de carbone comportant trois liaisons à des hétéro-atomes, avec au plus une liaison à un halogène, p. ex. radicaux ester ou nitrile, liés directement aux atomes de carbone du cycle
• C07D 207/09 - Radicaux substitués par des atomes d'azote ne faisant pas partie d'un radical nitro
• A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
• A61K 31/40 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil

Abrégé

The present disclosure provides compositions and methods for treating estrogen-dependent disorders, such as disorders of the female reproductive system, including uterine fibroids and endometriosis, among others. Compounds described herein that may be used to treat such indications include gonadotropin-releasing hormone (GnRH) antagonists. Suitable GnRH antagonists useful in conjunction with the compositions and methods described herein include thieno[3,4d]pyrimidine derivatives, such as 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)4-methoxyphenyI]-2,4-dioxo-1,2,3,4- tetrahydrothieno [3,4d]pyrimidine-5-carboxylic acid and the choline salt thereof, among others. Using the compositions and methods described herein, GnRH antagonists may be periodically administered to a patient, such as one or more times per day, week, or month. Advantageously, using the dosing schedules of the present disclosure, the periodic administration the GnRH antagonist may be temporarily halted, allowing a patient to recover any lost bone mineral density, without an accompanying return in the patient's symptoms.

Classes IPC  ?

• A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
• A61K 31/565 - Composés contenant des systèmes cycliques du cyclopenta[a]hydrophénanthrèneLeurs dérivés, p. ex. stéroïdes non substitués en position 17 bêta par un atome de carbone, p. ex. œstrane, œstradiol
• A61K 31/57 - Composés contenant des systèmes cycliques du cyclopenta[a]hydrophénanthrèneLeurs dérivés, p. ex. stéroïdes substitués en position 17 bêta par une chaîne à deux atomes de carbone, p. ex. prégnane ou progestérone
• A61P 15/00 - Médicaments pour le traitement des troubles génitaux ou sexuelsContraceptifs

Abrégé

The present disclosure provides compositions and methods for treating estrogen-dependent disorders, such as disorders of the female reproductive system, including uterine fibroids and endometriosis, among others. Compounds described herein that may be used to treat such indications include gonadotropin-releasing hormone (GnRH) antagonists. Suitable GnRH antagonists useful in conjunction with the compositions and methods described herein include thieno[3,4d]pyrimidine derivatives, such as 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)4-methoxyphenyl]-2,4-dioxo-1,2,3,4- tetrahydrothieno [3,4d]pyrimidine-5-carboxylic acid and the choline salt thereof, among others. Using the compositions and methods described herein, GnRH antagonists may be periodically administered to a patient, such as one or more times per day, week, or month, over the course of an extended treatment period, such as a treatment period having a duration of multiple years. Advantageously, using the compositions and methods of the present disclosure, the GnRH antagonist may be administered to a patient over a lengthy treatment period without inducing adverse side effects, such as a loss in bone mineral density, which is otherwise known to be a risk associated with GnRH antagonism.

Classes IPC  ?

• A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
• A61P 15/00 - Médicaments pour le traitement des troubles génitaux ou sexuelsContraceptifs
• A61K 31/00 - Préparations médicinales contenant des ingrédients actifs organiques
• A61P 5/24 - Médicaments pour le traitement des troubles du système endocrinien des hormones sexuelles

Abrégé

The present invention relates to solid oral formulations comprising a compound of formula (3Z,5S)-5-(hydroxymethyl)-1-[(2′-methyl-1,1′-biphenyl-4-yl)carbonyl]pyrrolidin-3-one O-methyloxime, and/or an active metabolite thereof, and the use of said formulations in the treatment and/or prevention of preterm labor, premature birth, dysmenorrhea and embryo implantation failure due to uterine contractions. The present invention is furthermore related to processes for their preparation.

Classes IPC  ?

• A61K 31/40 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil
• A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
• A61P 15/00 - Médicaments pour le traitement des troubles génitaux ou sexuelsContraceptifs
• A61K 31/401 - ProlineSes dérivés, p. ex. captopril
• A61K 9/20 - Pilules, pastilles ou comprimés
• A61K 47/40 - CyclodextrinesLeurs dérivés
• A61P 15/08 - Médicaments pour le traitement des troubles génitaux ou sexuelsContraceptifs pour les troubles gonadiques ou pour augmenter la fertilité, p. ex. inducteurs d'ovulation ou de spermatogénèse
• A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p. ex. composés antiphlogistiques et pour le cœur

Abrégé

The present disclosure provides compositions and methods for treating estrogen-dependent disorders, such as disorders of the female reproductive system, including uterine fibroids and endometriosis, among others. Compounds described herein that may be used to treat such indications include gonadotropin-releasing hormone (GnRH) antagonists. Suitable GnRH antagonists useful in conjunction with the compositions and methods described herein include thieno[3,4d]pyrimidine derivatives, such as 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)4-methoxypheny I]-2,4-dioxo-1,2,3,4-tetrahydrothieno [3,4d]pyrimidine-5-carboxylic acid and the choline salt thereof, among others. Using the compositions and methods described herein, GnRH antagonists may be periodically administered to a patient, such as one or more times per day, week, or month, in combination with periodic add-back therapy, thereby preventing bone mineral density loss that may otherwise accompany estrogen depletion effectuated by GnRH antagonist activity. Advantageously, using the dosing schedules of the present disclosure, the periodic administration the GnRH antagonist and add-back therapy may commence together, such as on the same day.

Classes IPC  ?

• A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
• A61K 31/565 - Composés contenant des systèmes cycliques du cyclopenta[a]hydrophénanthrèneLeurs dérivés, p. ex. stéroïdes non substitués en position 17 bêta par un atome de carbone, p. ex. œstrane, œstradiol
• A61K 31/57 - Composés contenant des systèmes cycliques du cyclopenta[a]hydrophénanthrèneLeurs dérivés, p. ex. stéroïdes substitués en position 17 bêta par une chaîne à deux atomes de carbone, p. ex. prégnane ou progestérone
• A61P 5/24 - Médicaments pour le traitement des troubles du système endocrinien des hormones sexuelles
• A61P 15/00 - Médicaments pour le traitement des troubles génitaux ou sexuelsContraceptifs
• A61P 15/12 - Médicaments pour le traitement des troubles génitaux ou sexuelsContraceptifs pour la ménopause

Abrégé

The present disclosure provides compositions and methods for treating endometrial growth disorders in a patient, such as a human patient, and particularly pre-menopausal female human patients. Exemplary disorders that may be treated using the compounds and therapeutic regimens described herein include adenomyosis and rectovaginal endometriosis. The compounds described herein that may be used to treat such indications include gonadotropin-releasing hormone (GnRH) antagonists. Suitable GnRH antagonists useful in conjunction with the compositions and methods described herein include thieno[3,4d]pyrimidine derivatives, such as 3-[2-fluoro-5-(2,3-difluoro-6- methoxybenzyloxy)4-methoxyphenyl]-2,4-dioxo-1,2,3,4- tetrahydrothieno [3,4d]pyrimidine-5- carboxylic acid and the choline salt thereof, among others.

Classes IPC  ?

• A61K 31/4184 - 1,3-Diazoles condensés avec des carbocycles, p. ex. benzimidazoles
• A61K 31/4439 - Pyridines non condenséesLeurs dérivés hydrogénés contenant d'autres systèmes hétérocycliques contenant un cycle à cinq chaînons avec l'azote comme hétéro-atome du cycle, p. ex. oméprazole
• A61K 31/513 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime ayant des groupes oxo liés directement à l'hétérocycle, p. ex. cytosine
• A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
• A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p. ex. composés antiphlogistiques et pour le cœur
• A61P 15/00 - Médicaments pour le traitement des troubles génitaux ou sexuelsContraceptifs
• A61P 15/02 - Médicaments pour le traitement des troubles génitaux ou sexuelsContraceptifs pour les pathologies du vagin

Produits et services

Medical preparations; pharmaceutical and veterinary products; sanitary preparations for medical use; pharmaceutical and biotechnological products for diagnosis, treatment and prevention of conditions in human and veterinary medicine.

Produits et services

Medical preparations; pharmaceutical and veterinary products; sanitary preparations for medical use; pharmaceutical and biotechnological products for diagnosis, treatment and prevention of conditions in human and veterinary medicine.

Produits et services

Medical preparations for the prevention and treatment of reproductive and neuropsychiatric diseases and disorders; pharmaceutical and veterinary products for the prevention and treatment of reproductive and neuropsychiatric diseases and disorders; sanitary preparations for medical use; pharmaceutical and biotechnological products for the prevention and treatment of reproductive and neuropsychiatric diseases and disorders, for diagnosis, treatment and prevention of reproductive and neuropsychiatric diseases and disorders in humans and animals

Produits et services

Medical preparations for the prevention and treatment of reproductive and neuropsychiatric diseases and disorders; pharmaceutical and veterinary preparations for the prevention and treatment of reproductive and neuropsychiatric diseases and disorders; sanitary preparations for medical use; pharmaceutical and biotechnological products for the prevention and treatment of reproductive and neuropsychiatric diseases and disorders, for diagnosis, treatment and prevention of reproductive and neuropsychiatric diseases and disorders in humans and animals

Produits et services

(1) Medical preparations for the prevention and treatment of reproductive and neuropsychiatric diseases and disorders namely, seizures, attention deficit disorders, cognitive deficit disorders, palsies, migraine headaches, eating disorders, mood disorders, anxiety disorders, psychotic disorders, autism, social behavior disorders and psychosocial stress; pharmaceutical and veterinary preparations for the prevention and treatment of reproductive and neuropsychiatric diseases and disorders namely, seizures, attention deficit disorders, cognitive deficit disorders, palsies, migraine headaches, eating disorders, mood disorders, anxiety disorders, psychotic disorders, autism, social behavior disorders and psychosocial stress; pharmaceutical and biotechnological preparations for the prevention and treatment of reproductive and neuropsychiatric diseases and disorders namely, seizures, attention deficit disorders, cognitive deficit disorders, palsies, migraine headaches, eating disorders, mood disorders, anxiety disorders, psychotic disorders, autism, social behavior disorders and psychosocial stress, for diagnosis, prevention and treatment of reproductive and neuropsychiatric diseases and disorders namely, seizures, attention deficit disorders, cognitive deficit disorders, palsies, migraine headaches, eating disorders, mood disorders, anxiety disorders, psychotic disorders, autism, social behavior disorders and psychosocial stress in humans and animals.

Produits et services

(1) Medical preparations for the prevention and treatment of reproductive and neuropsychiatric diseases and disorders namely, seizures, attention deficit disorders, cognitive deficit disorders, palsies, migraine headaches, eating disorders, mood disorders, anxiety disorders, psychotic disorders, autism, social behavior disorders and psychosocial stress; pharmaceutical and veterinary preparations for the prevention and treatment of reproductive and neuropsychiatric diseases and disorders namely, seizures, attention deficit disorders, cognitive deficit disorders, palsies, migraine headaches, eating disorders, mood disorders, anxiety disorders, psychotic disorders, autism, social behavior disorders and psychosocial stress; pharmaceutical and biotechnological preparations for the prevention and treatment of reproductive and neuropsychiatric diseases and disorders namely, seizures, attention deficit disorders, cognitive deficit disorders, palsies, migraine headaches, eating disorders, mood disorders, anxiety disorders, psychotic disorders, autism, social behavior disorders and psychosocial stress, for diagnosis, prevention and treatment of reproductive and neuropsychiatric diseases and disorders namely, seizures, attention deficit disorders, cognitive deficit disorders, palsies, migraine headaches, eating disorders, mood disorders, anxiety disorders, psychotic disorders, autism, social behavior disorders and psychosocial stress in humans and animals.

Abrégé

The invention provides compositions and methods for the use of oxytocin antagonists, such as substituted pyrrolidin-3-one oxime derivatives, among other compounds, in the treatment of subjects undergoing embryo transfer therapy. The compositions and methods of the invention can be used to dose subjects with oxytocin antagonists, including (3Z,55)-5-(hydroxymethyl)-1-[(2′-methyl-1,1′-biphenyl-4-yl)carbonyl]pyrrolidin-3-one O-methyloxime, among others, so as to improve endometrial receptivity and reduce the likelihood of embryo implantation failure and miscarriage following, for example, in vitro fertilization (IVF) and intracytoplasmic sperm injection (ICSI) embryo transfer procedures.

Classes IPC  ?

• A61K 31/40 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil
• A61K 35/54 - OvairesOvules fécondésOvulesEmbryonsCellules fœtalesCellules germinales
• A61P 15/08 - Médicaments pour le traitement des troubles génitaux ou sexuelsContraceptifs pour les troubles gonadiques ou pour augmenter la fertilité, p. ex. inducteurs d'ovulation ou de spermatogénèse
• A61K 38/22 - Hormones
• A61K 31/57 - Composés contenant des systèmes cycliques du cyclopenta[a]hydrophénanthrèneLeurs dérivés, p. ex. stéroïdes substitués en position 17 bêta par une chaîne à deux atomes de carbone, p. ex. prégnane ou progestérone

Produits et services

Medical preparations; pharmaceutical and veterinary products; sanitary preparations for medical use; pharmaceutical and biotechnological products for diagnosis, treatment and prevention of conditions in human and veterinary medicine.

Produits et services

Medical preparations; pharmaceutical and veterinary products; sanitary preparations for medical use; pharmaceutical and biotechnological products for diagnosis, treatment and prevention of conditions in human and veterinary medicine.

Produits et services

Medical preparations; pharmaceutical and veterinary products; sanitary preparations for medical use; pharmaceutical and biotechnological products for diagnosis, treatment and prevention of conditions in human and veterinary medicine.

Produits et services

Medical preparations; pharmaceutical and veterinary products; sanitary preparations for medical use; pharmaceutical and biotechnological products for diagnosis, treatment and prevention of conditions in human and veterinary medicine.

Produits et services

Medical preparations; pharmaceutical and veterinary products; sanitary preparations for medical use; pharmaceutical and biotechnological products for diagnosis, treatment and prevention of conditions in human and veterinary medicine.

Produits et services

Medical preparations; pharmaceutical and veterinary products; sanitary preparations for medical use; pharmaceutical and biotechnological products for diagnosis, treatment and prevention of conditions in human and veterinary medicine.

Abrégé

The invention provides methods of treating endometriosis in a patient by administration of a gonadotropin-releasing hormone (GnRH) antagonist, for instance, according to dosing regimens predicated on the patient's level of anti-Müllerian hormone (AMH) or β17-estradiol (E2).

Classes IPC  ?

• A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
• A61P 15/00 - Médicaments pour le traitement des troubles génitaux ou sexuelsContraceptifs

Abrégé

The invention provides compositions and methods for reducing the volume of menstrual blood loss in a patient, such as a human patient, for instance, that has uterine fibroids, by administration of a gonadotropin-releasing hormone (GnRH) antagonist. Suitable GnRH antagonists useful in conjunction with the compositions and methods described herein include thieno[3,4d]pyrimidine derivatives, such as 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxypheny I]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4d]pyrimidine-5-carboxylic acid and the choline salt thereof.

Classes IPC  ?

• A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
• A61P 15/00 - Médicaments pour le traitement des troubles génitaux ou sexuelsContraceptifs

Produits et services

Medical preparations for the prevention and treatment of reproductive and neuro-psychiatric diseases and disorders; pharmaceutical, and veterinary preparations for the prevention and treatment of reproductive and neuro-psychiatric diseases and disorders; sanitary preparations for medical use; pharmaceutical and biotechnological preparations for the prevention and treatment of reproductive and neuro-psychiatric diseases and disorders, for diagnosis, treatment and prevention of reproductive and neuro-psychiatric diseases and disorders in humans and animals

Produits et services

(1) Medical preparations for the prevention and treatment of reproductive and neuropsychiatric diseases and disorders namely, seizures, attention deficit disorders, cognitive deficit disorders, palsies, migraine headaches, eating disorders, mood disorders, anxiety disorders, psychotic disorders, autism, social behavior disorders and psychosocial stress; pharmaceutical and veterinary preparations for the prevention and treatment of reproductive and neuropsychiatric diseases and disorders namely, seizures, attention deficit disorders, cognitive deficit disorders, palsies, migraine headaches, eating disorders, mood disorders, anxiety disorders, psychotic disorders, autism, social behavior disorders and psychosocial stress; pharmaceutical and biotechnological preparations for the prevention and treatment of reproductive and neuropsychiatric diseases and disorders namely, seizures, attention deficit disorders, cognitive deficit disorders, palsies, migraine headaches, eating disorders, mood disorders, anxiety disorders, psychotic disorders, autism, social behavior disorders and psychosocial stress, for diagnosis, prevention and treatment of reproductive and neuropsychiatric diseases and disorders namely, seizures, attention deficit disorders, cognitive deficit disorders, palsies, migraine headaches, eating disorders, mood disorders, anxiety disorders, psychotic disorders, autism, social behavior disorders and psychosocial stress in humans and animals.

Produits et services

(1) Medical preparations for the prevention and treatment of reproductive and neuropsychiatric diseases and disorders namely, seizures, attention deficit disorders, cognitive deficit disorders, palsies, migraine headaches, eating disorders, mood disorders, anxiety disorders, psychotic disorders, autism, social behavior disorders and psychosocial stress; pharmaceutical and veterinary preparations for the prevention and treatment of reproductive and neuropsychiatric diseases and disorders namely, seizures, attention deficit disorders, cognitive deficit disorders, palsies, migraine headaches, eating disorders, mood disorders, anxiety disorders, psychotic disorders, autism, social behavior disorders and psychosocial stress; pharmaceutical and biotechnological preparations for the prevention and treatment of reproductive and neuropsychiatric diseases and disorders namely, seizures, attention deficit disorders, cognitive deficit disorders, palsies, migraine headaches, eating disorders, mood disorders, anxiety disorders, psychotic disorders, autism, social behavior disorders and psychosocial stress, for diagnosis, prevention and treatment of reproductive and neuropsychiatric diseases and disorders namely, seizures, attention deficit disorders, cognitive deficit disorders, palsies, migraine headaches, eating disorders, mood disorders, anxiety disorders, psychotic disorders, autism, social behavior disorders and psychosocial stress in humans and animals.

Produits et services

Medical preparations for the prevention and treatment of reproductive and neuro-psychiatric diseases and disorders; pharmaceutical, and veterinary preparations for the prevention and treatment of reproductive and neuro-psychiatric diseases and disorders; sanitary preparations for medical use; pharmaceutical and biotechnological preparations for the prevention and treatment of reproductive and neuro-psychiatric diseases and disorders, for diagnosis, treatment and prevention of reproductive and neuro-psychiatric diseases and disorders in humans and animals

Produits et services

(1) Medical preparations for the prevention and treatment of reproductive and neuropsychiatric diseases and disorders namely, seizures, attention deficit disorders, cognitive deficit disorders, palsies, migraine headaches, eating disorders, mood disorders, anxiety disorders, psychotic disorders, autism, social behavior disorders and psychosocial stress; pharmaceutical and veterinary preparations for the prevention and treatment of reproductive and neuropsychiatric diseases and disorders namely, seizures, attention deficit disorders, cognitive deficit disorders, palsies, migraine headaches, eating disorders, mood disorders, anxiety disorders, psychotic disorders, autism, social behavior disorders and psychosocial stress; pharmaceutical and biotechnological preparations for the prevention and treatment of reproductive and neuropsychiatric diseases and disorders namely, seizures, attention deficit disorders, cognitive deficit disorders, palsies, migraine headaches, eating disorders, mood disorders, anxiety disorders, psychotic disorders, autism, social behavior disorders and psychosocial stress, for diagnosis, prevention and treatment of reproductive and neuropsychiatric diseases and disorders namely, seizures, attention deficit disorders, cognitive deficit disorders, palsies, migraine headaches, eating disorders, mood disorders, anxiety disorders, psychotic disorders, autism, social behavior disorders and psychosocial stress in humans and animals.

Produits et services

(1) Medical preparations for the prevention and treatment of reproductive and neuropsychiatric diseases and disorders namely, seizures, attention deficit disorders, cognitive deficit disorders, palsies, migraine headaches, eating disorders, mood disorders, anxiety disorders, psychotic disorders, autism, social behavior disorders and psychosocial stress; pharmaceutical and veterinary preparations for the prevention and treatment of reproductive and neuropsychiatric diseases and disorders namely, seizures, attention deficit disorders, cognitive deficit disorders, palsies, migraine headaches, eating disorders, mood disorders, anxiety disorders, psychotic disorders, autism, social behavior disorders and psychosocial stress; pharmaceutical and biotechnological preparations for the prevention and treatment of reproductive and neuropsychiatric diseases and disorders namely, seizures, attention deficit disorders, cognitive deficit disorders, palsies, migraine headaches, eating disorders, mood disorders, anxiety disorders, psychotic disorders, autism, social behavior disorders and psychosocial stress, for diagnosis, prevention and treatment of reproductive and neuropsychiatric diseases and disorders namely, seizures, attention deficit disorders, cognitive deficit disorders, palsies, migraine headaches, eating disorders, mood disorders, anxiety disorders, psychotic disorders, autism, social behavior disorders and psychosocial stress in humans and animals.

Produits et services

(1) Medical preparations for the prevention and treatment of reproductive and neuropsychiatric diseases and disorders namely, seizures, attention deficit disorders, cognitive deficit disorders, palsies, migraine headaches, eating disorders, mood disorders, anxiety disorders, psychotic disorders, autism, social behavior disorders and psychosocial stress; pharmaceutical and veterinary preparations for the prevention and treatment of reproductive and neuropsychiatric diseases and disorders namely, seizures, attention deficit disorders, cognitive deficit disorders, palsies, migraine headaches, eating disorders, mood disorders, anxiety disorders, psychotic disorders, autism, social behavior disorders and psychosocial stress; pharmaceutical and biotechnological preparations for the prevention and treatment of reproductive and neuropsychiatric diseases and disorders namely, seizures, attention deficit disorders, cognitive deficit disorders, palsies, migraine headaches, eating disorders, mood disorders, anxiety disorders, psychotic disorders, autism, social behavior disorders and psychosocial stress, for diagnosis, prevention and treatment of reproductive and neuropsychiatric diseases and disorders namely, seizures, attention deficit disorders, cognitive deficit disorders, palsies, migraine headaches, eating disorders, mood disorders, anxiety disorders, psychotic disorders, autism, social behavior disorders and psychosocial stress in humans and animals.

Produits et services

(1) Medical preparations for the prevention and treatment of reproductive and neuropsychiatric diseases and disorders namely, seizures, attention deficit disorders, cognitive deficit disorders, palsies, migraine headaches, eating disorders, mood disorders, anxiety disorders, psychotic disorders, autism, social behavior disorders and psychosocial stress; pharmaceutical and veterinary preparations for the prevention and treatment of reproductive and neuropsychiatric diseases and disorders namely, seizures, attention deficit disorders, cognitive deficit disorders, palsies, migraine headaches, eating disorders, mood disorders, anxiety disorders, psychotic disorders, autism, social behavior disorders and psychosocial stress; pharmaceutical and biotechnological preparations for the prevention and treatment of reproductive and neuropsychiatric diseases and disorders namely, seizures, attention deficit disorders, cognitive deficit disorders, palsies, migraine headaches, eating disorders, mood disorders, anxiety disorders, psychotic disorders, autism, social behavior disorders and psychosocial stress, for diagnosis, prevention and treatment of reproductive and neuropsychiatric diseases and disorders namely, seizures, attention deficit disorders, cognitive deficit disorders, palsies, migraine headaches, eating disorders, mood disorders, anxiety disorders, psychotic disorders, autism, social behavior disorders and psychosocial stress in humans and animals.

Produits et services

Medical preparations for the prevention and treatment of reproductive and neuro-psychiatric diseases and disorders; pharmaceutical, and veterinary preparations for the prevention and treatment of reproductive and neuro-psychiatric diseases and disorders; sanitary preparations for medical use; pharmaceutical and biotechnological preparations for the prevention and treatment of reproductive and neuro-psychiatric diseases and disorders, for diagnosis, treatment and prevention of reproductive and neuro-psychiatric diseases and disorders in humans and animals

Produits et services

Medical preparations for the prevention and treatment of reproductive and neuro-psychiatric diseases and disorders; pharmaceutical, and veterinary preparations for the prevention and treatment of reproductive and neuro-psychiatric diseases and disorders; sanitary preparations for medical use; pharmaceutical and biotechnological preparations for the prevention and treatment of reproductive and neuro-psychiatric diseases and disorders, for diagnosis, treatment and prevention of reproductive and neuro-psychiatric diseases and disorders in humans and animals

Produits et services

Medical preparations for the prevention and treatment of reproductive and neuro-psychiatric diseases and disorders; pharmaceutical, and veterinary preparations for the prevention and treatment of reproductive and neuro-psychiatric diseases and disorders; sanitary preparations for medical use; pharmaceutical and biotechnological preparations for the prevention and treatment of reproductive and neuro-psychiatric diseases and disorders, for diagnosis, treatment and prevention of reproductive and neuro-psychiatric diseases and disorders in humans and animals

Produits et services

Medical preparations for the prevention and treatment of reproductive and neuro-psychiatric diseases and disorders; pharmaceutical, and veterinary preparations for the prevention and treatment of reproductive and neuro-psychiatric diseases and disorders; sanitary preparations for medical use; pharmaceutical and biotechnological preparations for the prevention and treatment of reproductive and neuro-psychiatric diseases and disorders, for diagnosis, treatment and prevention of reproductive and neuro-psychiatric diseases and disorders in humans and animals

Abrégé

The present invention relates to solid oral formulations comprising a compound of formula (3Z,5S)-5-(hydroxymethyl)-1-[(2′-methyl-1,1′-biphenyl-4-yl)carbonyl]pyrrolidin-3-one-O-methyloxime, and/or an active metabolite thereof, and the use of said formulations in the treatment and/or prevention of preterm labor, premature birth, dysmenorrhea and embryo implantation failure due to uterine contractions. The present invention is furthermore related to processes for their preparation.

Classes IPC  ?

• A61K 31/401 - ProlineSes dérivés, p. ex. captopril
• A61K 9/20 - Pilules, pastilles ou comprimés
• A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p. ex. composés antiphlogistiques et pour le cœur
• A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
• A61K 47/40 - CyclodextrinesLeurs dérivés
• A61K 31/40 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil
• A61P 15/08 - Médicaments pour le traitement des troubles génitaux ou sexuelsContraceptifs pour les troubles gonadiques ou pour augmenter la fertilité, p. ex. inducteurs d'ovulation ou de spermatogénèse

Abrégé

The present invention relates to a compound of formula (3Z,5S)-5-(hydroxymethyl)-1-[(2′-methyl-1,1′-biphenyl-4-yl)carbonyl]pyrrolidin-3-one O-meth19243yloxime, and/or an active metabolite thereof having antagonist action at the oxytocin receptor and/or vasopressin V1a receptor, to processes for their preparation, pharmaceutical compositions containing them and their use.

Classes IPC  ?

• C07D 207/09 - Radicaux substitués par des atomes d'azote ne faisant pas partie d'un radical nitro
• A61K 31/40 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil
• C07D 207/22 - Composés hétérocycliques contenant des cycles à cinq chaînons, non condensés avec d'autres cycles, ne comportant qu'un atome d'azote comme unique hétéro-atome du cycle avec uniquement des atomes d'hydrogène ou de carbone liés directement à l'atome d'azote du cycle comportant une liaison double entre chaînons cycliques ou entre chaînon cyclique et chaînon non cyclique avec des hétéro-atomes ou avec des atomes de carbone comportant trois liaisons à des hétéro-atomes, avec au plus une liaison à un halogène, p. ex. radicaux ester ou nitrile, liés directement aux atomes de carbone du cycle
• A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier

Abrégé

The invention provides compositions and methods for the use of oxytocin antagonists, such as substituted pyrrolidin-3-one oxime derivatives, among other compounds, in the treatment of subjects undergoing embryo transfer therapy. The compositions and methods of the invention can be used to dose subjects with oxytocin antagonists, including (3Z,5S)-5-(hydroxymethyl)-1-[(2'-methyl-1,1'-biphenyl- 4-yl)carbonyl]pyrrolidin-3-one O-methyloxime, among others, so as to improve endometrial receptivity and reduce the likelihood of embryo implantation failure and miscarriage following, for example, in vitro fertilization (IVF) and intracytoplasmic sperm injection (ICSI) embryo transfer procedures.

Classes IPC  ?

• A61K 31/40 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil
• A61P 5/10 - Médicaments pour le traitement des troubles du système endocrinien des hormones de l'hypophyse postérieure, p. ex. ocytocine, ADH

Abrégé

Crystalline (3Z,S3)-5-(hydroxymethyl)-1-[(2′-methyl-1,1′-biphenyl-4-yl)carbonyl]pyrrolidin-3-one O-methyloxime is disclosed. A pharmaceutical composition containing the crystalline compound and methods for treating conditions related to the OT-R activity, such as preterm labor, and for increasing embryo implantation rate in a mammal undergoing embryo transfer, comprising administering the crystalline compound are also disclosed.

Classes IPC  ?

• C07D 207/22 - Composés hétérocycliques contenant des cycles à cinq chaînons, non condensés avec d'autres cycles, ne comportant qu'un atome d'azote comme unique hétéro-atome du cycle avec uniquement des atomes d'hydrogène ou de carbone liés directement à l'atome d'azote du cycle comportant une liaison double entre chaînons cycliques ou entre chaînon cyclique et chaînon non cyclique avec des hétéro-atomes ou avec des atomes de carbone comportant trois liaisons à des hétéro-atomes, avec au plus une liaison à un halogène, p. ex. radicaux ester ou nitrile, liés directement aux atomes de carbone du cycle

Abrégé

The present invention relates to a compound of formula (3Z,5S)-5-(hydroxymethyl)-1-[(2′-methyl-1,1′-biphenyl-4-yl)carbonyl]pyrrolidin-3-one O-meth19243yloxime, and/or an active metabolite thereof having antagonist action at the oxytocin receptor and/or vasopressin V1a receptor, to processes for their preparation, pharmaceutical compositions containing them and their use.

Classes IPC  ?

• C07D 207/09 - Radicaux substitués par des atomes d'azote ne faisant pas partie d'un radical nitro
• C07D 207/22 - Composés hétérocycliques contenant des cycles à cinq chaînons, non condensés avec d'autres cycles, ne comportant qu'un atome d'azote comme unique hétéro-atome du cycle avec uniquement des atomes d'hydrogène ou de carbone liés directement à l'atome d'azote du cycle comportant une liaison double entre chaînons cycliques ou entre chaînon cyclique et chaînon non cyclique avec des hétéro-atomes ou avec des atomes de carbone comportant trois liaisons à des hétéro-atomes, avec au plus une liaison à un halogène, p. ex. radicaux ester ou nitrile, liés directement aux atomes de carbone du cycle
• A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
• A61K 31/40 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil

Abrégé

The invention provides pharmaceutical compositions comprising a compound of formula (I) or (II) and an additional therapeutic agent Also provided is the HCI salt and crystalline form of the compound of formula (I). The compounds inhibit the prostaglandin F receptor (PGF2alpha) and thus useful in the treatment of disorders such as preterm labor at the early gestational stage.

Classes IPC  ?

• C07D 277/06 - Composés hétérocycliques contenant des cycles thiazole-1, 3 ou thiazole-1, 3 hydrogénés non condensés avec d'autres cycles ne comportant pas de liaison double entre chaînons cycliques ou entre chaînons cycliques et chaînons non cycliques avec des atomes de carbone comportant trois liaisons à des hétéro-atomes, avec au plus une liaison à un halogène, p. ex. radicaux ester ou nitrile, liés directement aux atomes de carbone du cycle
• A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p. ex. composés antiphlogistiques et pour le cœur
• A61K 31/426 - 1,3-Thiazoles
• A61P 15/00 - Médicaments pour le traitement des troubles génitaux ou sexuelsContraceptifs
• A61P 15/06 - Agents antiabortifsTocolytiques

Abrégé

Crystalline (3Z,5S)-5-(hydroxymethyl)-1-[(2′-methyl-1,1-biphenyl-4-yl)carbonyl]pyrrolidin-3-one O-methyloxime is disclosed. A pharmaceutical composition containing the crystalline compound and methods for treating conditions related to the OT-R activity, such as preterm labor, and tor increasing embryo implantation rate in a mammal undergoing embryo transfer, comprising administering the crystalline compound are also disclosed.

Classes IPC  ?

• C07D 207/22 - Composés hétérocycliques contenant des cycles à cinq chaînons, non condensés avec d'autres cycles, ne comportant qu'un atome d'azote comme unique hétéro-atome du cycle avec uniquement des atomes d'hydrogène ou de carbone liés directement à l'atome d'azote du cycle comportant une liaison double entre chaînons cycliques ou entre chaînon cyclique et chaînon non cyclique avec des hétéro-atomes ou avec des atomes de carbone comportant trois liaisons à des hétéro-atomes, avec au plus une liaison à un halogène, p. ex. radicaux ester ou nitrile, liés directement aux atomes de carbone du cycle

Abrégé

Crystalline (3Z,5S)-5-(hydroxymethyl)-1-[(2'-methyl-1,1'-biphenyl-4-yl)carbonyl]pyrrolidin-3-one O-methyloxime is disclosed. A pharmaceutical composition containing the crystalline compound and methods for treating conditions related to the OT-R activity, such as preterm labor, and for increasing embryo implantation rate in a mammal undergoing embryo transfer, comprising administering the crystalline compound are also disclosed.

Classes IPC  ?

• C07D 207/22 - Composés hétérocycliques contenant des cycles à cinq chaînons, non condensés avec d'autres cycles, ne comportant qu'un atome d'azote comme unique hétéro-atome du cycle avec uniquement des atomes d'hydrogène ou de carbone liés directement à l'atome d'azote du cycle comportant une liaison double entre chaînons cycliques ou entre chaînon cyclique et chaînon non cyclique avec des hétéro-atomes ou avec des atomes de carbone comportant trois liaisons à des hétéro-atomes, avec au plus une liaison à un halogène, p. ex. radicaux ester ou nitrile, liés directement aux atomes de carbone du cycle
• A61K 31/40 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil
• A61P 5/10 - Médicaments pour le traitement des troubles du système endocrinien des hormones de l'hypophyse postérieure, p. ex. ocytocine, ADH

Abrégé

The present invention relates to solid oral formulations comprising a compound of formula (3Z,5S)-5-(hydroxymethyl)-1-[(2'-methyl-1,1'-biphenyl-4-yl)carbonyl]pyrrolidin-3-one- O-methyloxime, and/or an active metabolite thereof, and the use of said formulations in the treatment and/or prevention of preterm labor, premature birth, dysmenorrhea and embryo implantation failure due to uterine contractions. The present invention is furthermore related to processes for their preparation.

Classes IPC  ?

• A61K 9/20 - Pilules, pastilles ou comprimés
• A61K 9/28 - DragéesPilules ou comprimés avec revêtements
• A61K 9/48 - Préparations en capsules, p. ex. de gélatine, de chocolat

Abrégé

The present invention relates to solid oral formulations comprising a compound of formula (3Z,5S)-5-(hydroxymethyl)-1-[(2′-methyl-1,1′-biphenyl-4-yl)carbonyl]pyrrolidin-3-one-O-methyloxime, and/or an active metabolite thereof, and the use of said formulations in the treatment and/or prevention of preterm labor, premature birth, dysmenorrhea and embryo implantation failure due to uterine contractions. The present invention is furthermore related to processes for their preparation.

Classes IPC  ?

• A61K 31/09 - Éthers ou acétals ayant une liaison éther à un carbone cyclique d'un noyau aromatique ayant plusieurs liaisons éther
• A61K 9/14 - Préparations médicinales caractérisées par un aspect particulier à l'état particulaire, p. ex. poudres
• A61P 29/00 - Agents analgésiques, antipyrétiques ou anti-inflammatoires non centraux, p. ex. agents antirhumatismauxMédicaments anti-inflammatoires non stéroïdiens [AINS]
• A61P 35/00 - Agents anticancéreux
• B82Y 5/00 - Nanobiotechnologie ou nanomédecine, p. ex. génie protéique ou administration de médicaments
• A61K 31/40 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil
• A61K 31/401 - ProlineSes dérivés, p. ex. captopril
• A61K 9/20 - Pilules, pastilles ou comprimés
• A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
• A61K 47/40 - CyclodextrinesLeurs dérivés
• A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p. ex. composés antiphlogistiques et pour le cœur

Abrégé

The present invention relates to a compound of formula (3Z,5S)-5-(hydroxymethyl)-1- [(2'-methyl-1,1'-biphenyl-4-yl)carbonyl]pyrrolidin-3-one O-meth19243yloxime, and/or an active metabolite thereof having antagonist action at the oxytocin receptor and/or vasopressin V1a receptor, to processes for their preparation, pharmaceutical compositions containing them and their use.

Classes IPC  ?

• C07D 207/22 - Composés hétérocycliques contenant des cycles à cinq chaînons, non condensés avec d'autres cycles, ne comportant qu'un atome d'azote comme unique hétéro-atome du cycle avec uniquement des atomes d'hydrogène ou de carbone liés directement à l'atome d'azote du cycle comportant une liaison double entre chaînons cycliques ou entre chaînon cyclique et chaînon non cyclique avec des hétéro-atomes ou avec des atomes de carbone comportant trois liaisons à des hétéro-atomes, avec au plus une liaison à un halogène, p. ex. radicaux ester ou nitrile, liés directement aux atomes de carbone du cycle
• A61K 31/4025 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil non condensés et contenant d'autres hétérocycles, p. ex. cromakalim
• A61P 5/10 - Médicaments pour le traitement des troubles du système endocrinien des hormones de l'hypophyse postérieure, p. ex. ocytocine, ADH

Abrégé

The present invention relates to a compound of formula (3Z,5S)-5-(hydroxymethyl)-1-[(2′-methyl-1,1′-biphenyl-4-yl)carbonyl]pyrrolidin-3-one O-methy19243-yloxime, and/or an active metabolite thereof having antagonist action at the oxytocin receptor and/or vasopressin V1a receptor, to processes for their preparation, pharmaceutical compositions containing them and their use.

Classes IPC  ?

• C07D 207/22 - Composés hétérocycliques contenant des cycles à cinq chaînons, non condensés avec d'autres cycles, ne comportant qu'un atome d'azote comme unique hétéro-atome du cycle avec uniquement des atomes d'hydrogène ou de carbone liés directement à l'atome d'azote du cycle comportant une liaison double entre chaînons cycliques ou entre chaînon cyclique et chaînon non cyclique avec des hétéro-atomes ou avec des atomes de carbone comportant trois liaisons à des hétéro-atomes, avec au plus une liaison à un halogène, p. ex. radicaux ester ou nitrile, liés directement aux atomes de carbone du cycle
• C07D 207/09 - Radicaux substitués par des atomes d'azote ne faisant pas partie d'un radical nitro

Produits et services

Medical, pharmaceutical, veterinary and sanitary products; pharmaceutical and biotechnological products for diagnosis, treatment and prevention of conditions in human and veterinary medicine. Advertising; business management; business administration; office functions; promotion, retail sale of pharmaceutical and biotechnological products for diagnosis, treatment and prevention of conditions in human and veterinary medicine; assistance to customers in the marketing of new products; wholesaling of pharmaceutical and biotechnological products for diagnosis, treatment and prevention of conditions in human and veterinary medicine. Scientific and technological services and research and design relating thereto; industrial analysis and research services; research, development, consulting, information, assistance, analyses, clinical trials related to the design and development of pharmaceutical and biotechnological products for diagnosis, treatment and prevention of conditions in human and veterinary medicine. Acquisition and/or granting of licenses for intellectual property rights relating to the goods in class 5; consulting relating to services to be performed for others in the form of actions in relation to regulatory records and legal authorizations for marketing of pharmaceutical and biotechnological products for diagnosis, treatment and prevention of conditions in human and veterinary medicine before authorities and public administrations, particularly for medication approval.

Produits et services

Medical [, ] * and * pharmaceutical, [ and veterinary ] preparations for the prevention and treatment of reproductive [ and neuro-psychiatric ] diseases and disorders; [ sanitary preparations for the prevention and treatment of reproductive and neuro-psychiatric diseases and disorders; ] pharmaceutical and biotechnological preparations for the prevention and treatment of reproductive [ and neuro-psychiatric ] diseases and disorders, for diagnosis, treatment and prevention of medical conditions in humans [ and animals ] ; none of these products being for ophthalmic use [ Advertising; business management; business administration; office functions; promotion and retail store services featuring pharmaceutical and biotechnological products for diagnosis, treatment and prevention of medical conditions in humans and animals; assistance to customers in the marketing of new products; wholesale store services featuring pharmaceutical and biotechnological products for diagnosis, treatment and prevention of medical conditions in humans and animals; none of these services being performed in relation to ophthalmic use ] Scientific and technological services, namely, in the field of reproductive [ and neuro-psychiatry ] medicine and research and design relating thereto; industrial analysis and research services in the field of reproductive [ and neuro-psychiatry ] medicine; research, development, scientific consulting, providing scientific information, scientific research assistance, scientific analyses, and conducting clinical trials all related to the design and development of pharmaceutical and biotechnological products for diagnosis, treatment and prevention of medical conditions in humans [ and animals ] ; none of these services being performed in relation to ophthalmic use [ Licensing of intellectual property in the field of medical, pharmaceutical, veterinary and sanitary products, and pharmaceutical and biotechnological products for diagnosis, treatment and prevention of medical conditions in humans and animals; legal consulting and regulatory compliance consulting relating to regulatory records and legal authorizations for marketing of pharmaceutical and biotechnological products for diagnosis, treatment and prevention of medical conditions in humans and animals before authorities and public administrations, particularly for medication approval; none of these services being performed in relation to ophthalmic use ]