A61K31/4422

Crush resistant delayed-release dosage forms

The invention relates to a dosage form comprising a physiologically effective amount of a physiologically active substance (A), a synthetic, semi-synthetic or natural polymer (C), optionally one or more physiologically acceptable auxiliary substances (B) and optionally a synthetic, semi-synthetic or natural wax (D), wherein the dosage form exhibits a resistance to crushing of at least 400 N and wherein under physiological conditions the release of the physiologically active substance (A) from the dosage form is at least partially delayed.

Crush resistant delayed-release dosage forms

The invention relates to a dosage form comprising a physiologically effective amount of a physiologically active substance (A), a synthetic, semi-synthetic or natural polymer (C), optionally one or more physiologically acceptable auxiliary substances (B) and optionally a synthetic, semi-synthetic or natural wax (D), wherein the dosage form exhibits a resistance to crushing of at least 400 N and wherein under physiological conditions the release of the physiologically active substance (A) from the dosage form is at least partially delayed.

TRIMEGESTONE (TMG) FOR TREATMENT OF PRETERM BIRTH
20200163976 · 2020-05-28 ·

As disclosed herein, novel compositions including steroid hormones, such as trimegestone (TMG) and progesterone (P4), provide treatments for term and preterm labor with significant effects on the delay of delivery. Delay and block of delivery occurs when both P4 and TMG are administered late in gestation in pregnant rat and guinea pig animal models. TMG exhibits remarkable drug efficacy, achieving the same inhibition as P4, but at much lower doses. These hereto unknown effects of TMG on the processes of cervical ripening and uterine contraction provide a novel approach for extending pregnancy term, including reducing a likelihood of preterm and/or term labor, along with improved methods of administration. Other diseases and/or conditions may be treated with TMG, such as dysmenorrhea or luteal insufficiency for sustaining pregnancy.

TRIMEGESTONE (TMG) FOR TREATMENT OF PRETERM BIRTH
20200163976 · 2020-05-28 ·

As disclosed herein, novel compositions including steroid hormones, such as trimegestone (TMG) and progesterone (P4), provide treatments for term and preterm labor with significant effects on the delay of delivery. Delay and block of delivery occurs when both P4 and TMG are administered late in gestation in pregnant rat and guinea pig animal models. TMG exhibits remarkable drug efficacy, achieving the same inhibition as P4, but at much lower doses. These hereto unknown effects of TMG on the processes of cervical ripening and uterine contraction provide a novel approach for extending pregnancy term, including reducing a likelihood of preterm and/or term labor, along with improved methods of administration. Other diseases and/or conditions may be treated with TMG, such as dysmenorrhea or luteal insufficiency for sustaining pregnancy.

TRIMEGESTONE (TMG) FOR TREATMENT OF PRETERM BIRTH
20200163976 · 2020-05-28 ·

As disclosed herein, novel compositions including steroid hormones, such as trimegestone (TMG) and progesterone (P4), provide treatments for term and preterm labor with significant effects on the delay of delivery. Delay and block of delivery occurs when both P4 and TMG are administered late in gestation in pregnant rat and guinea pig animal models. TMG exhibits remarkable drug efficacy, achieving the same inhibition as P4, but at much lower doses. These hereto unknown effects of TMG on the processes of cervical ripening and uterine contraction provide a novel approach for extending pregnancy term, including reducing a likelihood of preterm and/or term labor, along with improved methods of administration. Other diseases and/or conditions may be treated with TMG, such as dysmenorrhea or luteal insufficiency for sustaining pregnancy.

METHODS OF TREATMENT USING NIMODIPINE PARENTERAL FORMULATIONS

A method of treating a human patient suffering from subarachnoid hemorrhage (SAH), intra-cerebral hemorrhage, and traumatic brain injuries (TBI), and the like, comprising administering a nimodipine formulation suitable for parenteral injection, e.g., either via the subcutaneous or intramuscular route, is disclosed.

METHODS OF TREATMENT USING NIMODIPINE PARENTERAL FORMULATIONS

A method of treating a human patient suffering from subarachnoid hemorrhage (SAH), intra-cerebral hemorrhage, and traumatic brain injuries (TBI), and the like, comprising administering a nimodipine formulation suitable for parenteral injection, e.g., either via the subcutaneous or intramuscular route, is disclosed.

1,4-dihydropyridine derivatives with HSP modulating activity

The invention provides 1,4-dihydropyridine derivatives of formula (I) wherein R.sup.1 is optionally substituted C.sub.6-24aryl group or 5 to 6 membered heteroaryl group comprising 1 to 3 nitrogen atoms or other heteroatoms like oxygen and sulphur, and combinations thereof; R.sup.2 and R.sup.3 are independently hydrogen or C.sub.1-6alkyl group; R.sup.4 and R.sup.5 are independently hydrogen, C.sub.1-6alkyl group optionally substituted with amino, mono- or di(C.sub.1-6alkyl)amino, or with 5 to 24 membered optionally fused heterocyclic ring attached by nitrogen and optionally comprising additional 1 to 3 N, O, S heteroatoms and optionally substituted with C.sub.1-6alkyl group or C.sub.1-6 alkoxy group; R.sup.6 is C.sub.1-6alkyl, C.sub.3-7cycloalkyl, C.sub.3-7cycloalkylC.sub.1-6alkyl or arylC.sub.1-6alkyl group; and stereoisomers including enantiomers, diastereomers, racemic mixtures, mixture of enantiomers and combination thereof, as well as polymorphs, pharmaceutically acceptable salts, solvates, esters and prodrugs thereof for use in the therapeutic or prophylactic treatment of a disorder mediated by heat shock proteins. ##STR00001##

1,4-dihydropyridine derivatives with HSP modulating activity

The invention provides 1,4-dihydropyridine derivatives of formula (I) wherein R.sup.1 is optionally substituted C.sub.6-24aryl group or 5 to 6 membered heteroaryl group comprising 1 to 3 nitrogen atoms or other heteroatoms like oxygen and sulphur, and combinations thereof; R.sup.2 and R.sup.3 are independently hydrogen or C.sub.1-6alkyl group; R.sup.4 and R.sup.5 are independently hydrogen, C.sub.1-6alkyl group optionally substituted with amino, mono- or di(C.sub.1-6alkyl)amino, or with 5 to 24 membered optionally fused heterocyclic ring attached by nitrogen and optionally comprising additional 1 to 3 N, O, S heteroatoms and optionally substituted with C.sub.1-6alkyl group or C.sub.1-6 alkoxy group; R.sup.6 is C.sub.1-6alkyl, C.sub.3-7cycloalkyl, C.sub.3-7cycloalkylC.sub.1-6alkyl or arylC.sub.1-6alkyl group; and stereoisomers including enantiomers, diastereomers, racemic mixtures, mixture of enantiomers and combination thereof, as well as polymorphs, pharmaceutically acceptable salts, solvates, esters and prodrugs thereof for use in the therapeutic or prophylactic treatment of a disorder mediated by heat shock proteins. ##STR00001##

ALPHA-AMINO ESTERS OF HYDROXYPROPYLTHIAZOLIDINE CARBOXAMIDE DERIVATIVE AND SALT FORM, CRYSTAL POLYMORPH THEREOF

The invention provides -amino esters of a hydroxypropylthiazolidine carboxamide derivative, (2S)-3-([1,1-biphenyl]-4-ylsulfonyl)-N-[(1S)-3-hydroxy-1-phenylpropyl]-1,3-thiazolidine-2-carboxamide, as well as salts and crystal polymorphs thereof, that can be used to inhibit prostaglandin F receptor. The invention further encompasses methods of treating disorders such as preterm labor at the early gestational stage by the administration of these substances to a patient in need of treatment.