Abstract

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.

IPC Classes  ?

• C07D 207/22 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
• C07D 207/09 - Radicals substituted by nitrogen atoms not forming part of a nitro radical

Abstract

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.

IPC Classes  ?

• A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
• A61K 31/401 - ProlineDerivatives thereof, e.g. captopril
• A61K 9/20 - Pills, lozenges or tablets
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 47/40 - CyclodextrinsDerivatives thereof
• A61P 15/08 - Drugs for genital or sexual disordersContraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

Abstract

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.

IPC Classes  ?

• C12Q 1/6883 - Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material
• A61K 31/404 - Indoles, e.g. pindolol
• A61K 31/4025 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61K 38/24 - Follicle-stimulating hormone [FSH]Chorionic gonadotropins, e.g. HCGLuteinising hormone [LH]Thyroid-stimulating hormone [TSH]
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 9/20 - Pills, lozenges or tablets
• A61P 15/08 - Drugs for genital or sexual disordersContraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis

Abstract

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.

IPC Classes  ?

• A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
• A61K 38/24 - Follicle-stimulating hormone [FSH]Chorionic gonadotropins, e.g. HCGLuteinising hormone [LH]Thyroid-stimulating hormone [TSH]
• A61P 15/06 - Antiabortive agentsLabour repressants

Abstract

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.

IPC Classes  ?

• A61K 31/426 - 1,3-Thiazoles
• A61K 31/401 - ProlineDerivatives thereof, e.g. captopril
• A61K 38/095 - OxytocinsVasopressinsRelated peptides
• A61P 5/12 - Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH for decreasing, blocking or antagonising the activity of the posterior pituitary hormones

Abstract

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.

IPC Classes  ?

• C12Q 1/6883 - Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material
• A61K 38/24 - Follicle-stimulating hormone [FSH]Chorionic gonadotropins, e.g. HCGLuteinising hormone [LH]Thyroid-stimulating hormone [TSH]

Abstract

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)

IPC Classes  ?

• A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
• A61P 5/10 - Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH
• A61P 15/06 - Antiabortive agentsLabour repressants

Abstract

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.

IPC Classes  ?

• C07D 207/22 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
• C07D 207/09 - Radicals substituted by nitrogen atoms not forming part of a nitro radical
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil

Abstract

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.

IPC Classes  ?

• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61K 31/565 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol
• A61K 31/57 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
• A61P 15/00 - Drugs for genital or sexual disordersContraceptives

Abstract

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.

IPC Classes  ?

• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61P 15/00 - Drugs for genital or sexual disordersContraceptives
• A61K 31/00 - Medicinal preparations containing organic active ingredients
• A61P 5/24 - Drugs for disorders of the endocrine system of the sex hormones

Abstract

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.

IPC Classes  ?

• A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61P 15/00 - Drugs for genital or sexual disordersContraceptives
• A61K 31/401 - ProlineDerivatives thereof, e.g. captopril
• A61K 9/20 - Pills, lozenges or tablets
• A61K 47/40 - CyclodextrinsDerivatives thereof
• A61P 15/08 - Drugs for genital or sexual disordersContraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

Abstract

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.

IPC Classes  ?

• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61K 31/565 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol
• A61K 31/57 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
• A61P 5/24 - Drugs for disorders of the endocrine system of the sex hormones
• A61P 15/00 - Drugs for genital or sexual disordersContraceptives
• A61P 15/12 - Drugs for genital or sexual disordersContraceptives for climacteric disorders

Abstract

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.

IPC Classes  ?

• A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
• A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
• A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61P 15/00 - Drugs for genital or sexual disordersContraceptives
• A61P 15/02 - Drugs for genital or sexual disordersContraceptives for disorders of the vagina

Goods & 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.

Goods & 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.

Goods & 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

Goods & 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

Goods & 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.

Goods & 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.

Abstract

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.

IPC Classes  ?

• A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
• A61K 35/54 - OvariesOvaOvulesEmbryosFoetal cellsGerm cells
• A61P 15/08 - Drugs for genital or sexual disordersContraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
• A61K 38/22 - Hormones
• A61K 31/57 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone

Goods & 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.

Goods & 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.

Goods & 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.

Goods & 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.

Goods & 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.

Goods & 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.

Abstract

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).

IPC Classes  ?

• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61P 15/00 - Drugs for genital or sexual disordersContraceptives

Abstract

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.

IPC Classes  ?

• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61P 15/00 - Drugs for genital or sexual disordersContraceptives

Goods & 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

Goods & 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.

Goods & 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.

Goods & 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

Goods & 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.

Goods & 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.

Goods & 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.

Goods & 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.

Goods & 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

Goods & 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

Goods & 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

Goods & 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

Abstract

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.

IPC Classes  ?

• A61K 31/401 - ProlineDerivatives thereof, e.g. captopril
• A61K 9/20 - Pills, lozenges or tablets
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 47/40 - CyclodextrinsDerivatives thereof
• A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
• A61P 15/08 - Drugs for genital or sexual disordersContraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis

Abstract

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.

IPC Classes  ?

• C07D 207/09 - Radicals substituted by nitrogen atoms not forming part of a nitro radical
• A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
• C07D 207/22 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
• A61K 9/00 - Medicinal preparations characterised by special physical form

Abstract

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.

IPC Classes  ?

• A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
• A61P 5/10 - Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH

Abstract

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.

IPC Classes  ?

• C07D 207/22 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms

Abstract

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.

IPC Classes  ?

• C07D 207/09 - Radicals substituted by nitrogen atoms not forming part of a nitro radical
• C07D 207/22 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil

Abstract

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.

IPC Classes  ?

• C07D 277/06 - Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61K 31/426 - 1,3-Thiazoles
• A61P 15/00 - Drugs for genital or sexual disordersContraceptives
• A61P 15/06 - Antiabortive agentsLabour repressants

Abstract

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.

IPC Classes  ?

• C07D 207/22 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms

Abstract

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.

IPC Classes  ?

• C07D 207/22 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
• A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
• A61P 5/10 - Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH

Abstract

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.

IPC Classes  ?

• A61K 9/20 - Pills, lozenges or tablets
• A61K 9/28 - DrageesCoated pills or tablets
• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate

Abstract

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.

IPC Classes  ?

• A61K 31/09 - Ethers or acetals having an ether linkage to aromatic ring nuclear carbon having two or more such linkages
• A61K 9/14 - Particulate form, e.g. powders
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 35/00 - Antineoplastic agents
• B82Y 5/00 - Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
• A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
• A61K 31/401 - ProlineDerivatives thereof, e.g. captopril
• A61K 9/20 - Pills, lozenges or tablets
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 47/40 - CyclodextrinsDerivatives thereof
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

Abstract

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.

IPC Classes  ?

• C07D 207/22 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
• A61K 31/4025 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
• A61P 5/10 - Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH

Abstract

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.

IPC Classes  ?

• C07D 207/22 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
• C07D 207/09 - Radicals substituted by nitrogen atoms not forming part of a nitro radical

Goods & 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.

Goods & 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 ]