The invention relates to novel compounds that have S1P receptor modulating activity. Further, the invention relates to a pharmaceutical comprising at least one compound of the invention for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression, for example, autoimmune response. A further aspect of the invention relates to the use of a pharmaceutical comprising at least one compound of the invention for the manufacture of a medicament for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression such as autoimmune response.

The present application relates to a novel and efficient process for preparing novel substituted 5-fluoro-1H-pyrazolopyridines of the formula (VI)

##STR00001##

which are suitable as an intermediate for production of medicaments and for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders. More particularly, the 5-fluoro-1H-pyrazolopyridines of the formula (VI) are suitable for preparation of the compound of the formula (I)

##STR00002##

which serves for production of medicaments, for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders.

The present application relates to a novel and efficient process for preparing novel substituted 5-fluoro-1H-pyrazolopyridines of the formula (VI)

##STR00001##

which are suitable as an intermediate for production of medicaments and for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders. More particularly, the 5-fluoro-1H-pyrazolopyridines of the formula (VI) are suitable for preparation of the compound of the formula (I)

##STR00002##

which serves for production of medicaments, for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders.

The present invention relates to a medicament for treating or preventing a disease related to orexin receptor, especially orexin type 2 receptor, comprising a new compound having a urea structure or a pharmaceutically acceptable salt thereof as an active ingredient. In more detail, the present invention relates to a medicament for treating or preventing narcolepsy, idiopathic hypersomnia, hypersomnia, sleep apnea syndrome, etc.

Compositions for treating a condition associated with activity of a muscarinic receptor (e.g., one or more of M.sub.1, M.sub.2, M.sub.3, M.sub.4, M.sub.5) and for anesthetizing a subject include a bitopic muscarinic antagonist or agonist. A bitopic muscarinic antagonist named JB-D4 was discovered. Additional bitopic muscarinic antagonists discovered and described herein include BK-23, HD-42, HD153, HD-185, KH-5, JM-31 and JM-32. These bitopic ligands and their structural analogs, as well as bitopic muscarinic agonists, may be used as neuromuscular blocking agents (e.g., for use in compositions for anesthetizing a subject) and for the treatment of central nervous system disorders (e.g., Parkinson's disease, Schizophrenia, etc.), Overactive Bladder Syndrome, Chronic Obstructive Pulmonary Disease, asthma, and many other diseases associated with the activation or inhibition of M.sub.1-M.sub.5 acetylcholine receptors.

Compositions for treating a condition associated with activity of a muscarinic receptor (e.g., one or more of M.sub.1, M.sub.2, M.sub.3, M.sub.4, M.sub.5) and for anesthetizing a subject include a bitopic muscarinic antagonist or agonist. A bitopic muscarinic antagonist named JB-D4 was discovered. Additional bitopic muscarinic antagonists discovered and described herein include BK-23, HD-42, HD153, HD-185, KH-5, JM-31 and JM-32. These bitopic ligands and their structural analogs, as well as bitopic muscarinic agonists, may be used as neuromuscular blocking agents (e.g., for use in compositions for anesthetizing a subject) and for the treatment of central nervous system disorders (e.g., Parkinson's disease, Schizophrenia, etc.), Overactive Bladder Syndrome, Chronic Obstructive Pulmonary Disease, asthma, and many other diseases associated with the activation or inhibition of M.sub.1-M.sub.5 acetylcholine receptors.

The present invention is directed to a composition comprising the following compound: ##STR00001## The compound is associated with activity of a muscarinic receptor (e.g. one or more M.sub.1, M.sub.2, M.sub.3, M.sub.4 and M.sub.5.

The present application relates to a novel and efficient process for preparing novel substituted 5-fluoro-1H-pyrazolopyridines of the formula (VI) ##STR00001##
which are suitable as an intermediate for production of medicaments and for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders. More particularly, the 5-fluoro-1H-pyrazolopyridines of the formula (VI) are suitable for preparation of the compound of the formula (I) ##STR00002##
which serves for production of medicaments, for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders.

The present application relates to a novel and efficient process for preparing novel substituted 5-fluoro-1H-pyrazolopyridines of the formula (VI) ##STR00001##
which are suitable as an intermediate for production of medicaments and for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders. More particularly, the 5-fluoro-1H-pyrazolopyridines of the formula (VI) are suitable for preparation of the compound of the formula (I) ##STR00002##
which serves for production of medicaments, for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders.

The coupling of aryl, heteroaryl, and vinyl halides with ,-difluoroketones or silyl ethers or siylenol ethers of ,-difluoroketones and ,-difluoroamides and esters are described. Further derivatization of the coupling products (such as ketone cleavage and Baeyer-Villiger oxidation) is also described.