C07D405/00

Processes and intermediates for the preparations of isomer free prostaglandis

Novel processes for the preparation of a compound of Formula I-2 substantially free of the 5,6-trans isomer: ##STR00001##
wherein ##STR00002##
R.sub.2, R.sub.3 and R.sub.4 are as defined in the specification are provided. Novel intermediates for the preparations of isomer free Prostaglandins and derivatives thereof are also provided.

COMPOUND

This invention relates to compounds, as defined in the specification, useful in the treatment of mycoses, compositions containing them and their use in therapy.

Compounds as tyrosine kinase modulators
09725433 · 2017-08-08 · ·

The present invention is directed to novel compounds of Formula I. The compounds of the present invention are potent tyrosine kinase modulators, and are suitable for the treatment and prevention of diseases and conditions related to abnormal activities of tyrosine kinase receptors. ##STR00001##

Compounds as tyrosine kinase modulators
09725433 · 2017-08-08 · ·

The present invention is directed to novel compounds of Formula I. The compounds of the present invention are potent tyrosine kinase modulators, and are suitable for the treatment and prevention of diseases and conditions related to abnormal activities of tyrosine kinase receptors. ##STR00001##

Urethanes, ureas, amidines and related inhibitors of factor Xa

The invention relates to a new class of compounds, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions that are effective as selective inhibitors of factor Xa, both in the isolated state and in a complex with other proteins. The compounds of the invention can be used for treating and preventing diseases, such as acute coronary syndrome, myocardial infarction, unstable angina, refractory angina, thromboses caused by post-thrombolytic therapy or coronary angioplasty, acute ischemia mediated cerebrovascular syndrome, embolic stroke, thrombotic stroke, and other diseases in humans and other mammals associated with blood coagulation problems.

Trisubstituted bicyclic heterocyclic compounds with kinase activities and uses thereof

Trisubstituted bicyclic heterocyclic compounds (e.g., chromenones and quinolines) and pharmaceutical compositions,that modulate kinase activity, including PI3 kinase activity, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.

Tackifier compounds and methods of using the same

The present invention relates to tackifier compounds and methods of using the same. In various embodiments, the present invention provides a tackifier compound including independently substituted or unsubstituted fused rings A and B each independently chosen from (C.sub.5-C.sub.10)cycloalkyl and (C.sub.2-C.sub.10)heterocyclyl. Fused ring A is substituted with (R.sup.1).sub.1-8 and fused ring B is substituted with (OC(O)RC(O)R.sup.2).sub.1-8. At each occurrence R is independently chosen from (C.sub.2-C.sub.10)alkanylene, (C.sub.2-C.sub.10)alkenylene, (C.sub.2-C.sub.10)alkynylene, C.sub.5-C.sub.20(arylene), and (C.sub.1-C.sub.20)heteroarylene, wherein R is unsubstituted or substituted. At each occurrence R.sup.1 is independently selected from OH, OR.sup.3, and OC(O)RC(O)R.sup.2. At each occurrence R.sup.2 is independently chosen from OH, OR.sup.3, NH.sub.2, NHR.sup.3, and NR.sup.3.sub.2. At each occurrence R.sup.3 is independently chosen from (C.sub.1-C.sub.10)alkanyl, (C.sub.2-C.sub.10)alkenyl, (C.sub.2-C.sub.10)alkynyl, C.sub.5-C.sub.20(aryl), and (C.sub.1-C.sub.20)heteroaryl, wherein R.sup.3 is unsubstituted or substituted.

AMINOPYRIMIDINE/PYRAZINE DERIVATIVES AS CTPS1 INHIBITORS
20250066324 · 2025-02-27 ·

Compounds of formula (I), and related aspects.

##STR00001##

Compounds as diacylglycerol acyltransferase inhibitors
09624174 · 2017-04-18 · ·

Compounds of Formula (I) are inhibitors of acyl coenzyme A: diacylglycerol acyltransferase 1 (DGAT-1), useful in the treatment of obesity, obesity related disorders, genetic (Type 1, Type 5 hyperlipidemia) and acquired forms of hypertriglyceridemia or hyperlipoproteinemia-related disorders, caused by but not limited to lipodystrophy, hypothyroidism, medications (beta blockers, thiazides, estrogen, glucocorticoids, transplant) and other factors (pregnancy, alcohol intake), hyperlipoproteinemia, chylomicronemia, dyslipidemia, non-alcoholic steatohepatitis, diabetes, insulin resistance, metabolic syndrome, cardiovascular outcomes, angina, excess hair growth (including syndromes associated with hirsutism), nephrotic syndrome, fibrosis such as mycocardial, renal and liver fibrosis, hepatitis C virus infection and acne or other skin disorders. ##STR00001##

Substituted 2-azabicycles and their use as orexin receptor modulators

The present invention is directed to compounds of Formula I: wherein X is N or CR1; Y is N or CR2; R1 is H, alkoxy, halo, triazolyl, pyrimidinyl, oxazolyl, isoxazole, oxadiazolyl, or pyrazolyl; R2 is H, alkyl, alkoxy, or halo; Z is NH or O; R3 is H, alkyl, alkoxy, halo, or triazolyl; R4 is H or alkyl; or R3 and R4, together with the atoms to which they are attached, form a 6-membered aryl ring or a 5- or 6-membered heteroaryl ring; R5 is pyridyl, pyrazinyl, or pyrimidinyl, wherein the pyridyl, pyrazinyl, or pyrimidinyl is optionally substituted with halo or alkyl; and n is 1 or 2. Methods of making the compounds of Formula I are also described. The invention also relates to pharmaceutical compositions comprising compounds of Formula I. Methods of using the compounds of the invention are also within the scope of the invention.