The present invention generally relates to new compounds for therapeutic uses. In particular, the disclosed series compounds with immunomodulatory activities are useful for treatment of dysfunctions of the immune system and various cancers. Pharmaceutical composition matters and methods for treating a patient with an immune disease and/or a cancer by administering therapeutically effective amounts of such compound alone or together with other therapeutics are within the scope of this disclosure.

The present invention generally relates to new compounds for therapeutic uses. In particular, the disclosed series compounds with immunomodulatory activities are useful for treatment of dysfunctions of the immune system and various cancers. Pharmaceutical composition matters and methods for treating a patient with an immune disease and/or a cancer by administering therapeutically effective amounts of such compound alone or together with other therapeutics are within the scope of this disclosure.

The present invention relates to compounds of formula (I) and (II)

##STR00001##

and pharmaceutically acceptable salts thereof. The compounds of formula (I) or (II) possess utility as cytochrome P450 monooxygenase 11A1 (CYP11A1) inhibitors. The compounds are useful as medicaments in the treatment of steroid receptor, particularly androgen receptor, dependent diseases and conditions, such as prostate cancer.

A compound represented by formula:

##STR00001##

or its pharmaceutically acceptable salt, wherein L is NR.sup.2R.sup.3, SR.sup.7, SO.sub.2R.sup.8, substituted or unsubstituted alkyl, or substituted or unsubstituted alkenyl; R.sup.2 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, or the like; R.sup.3 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, or the like; R.sup.7 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, or the like; R.sup.8 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, or the like, provided that R.sup.8 is not unsubstituted methyl or trifluoromethyl; Y is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, or the like, provided that Y is not unsubstituted methyl or unsubstituted ethyl; Z is —CR.sup.6═, or —N═; R.sup.1 is hydrogen, or substituted or unsubstituted alkyl; R.sup.4, R.sup.5 and R.sup.6 are each independently hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, or the like.

A compound represented by formula:

##STR00001##

or its pharmaceutically acceptable salt, wherein L is NR.sup.2R.sup.3, SR.sup.7, SO.sub.2R.sup.8, substituted or unsubstituted alkyl, or substituted or unsubstituted alkenyl; R.sup.2 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, or the like; R.sup.3 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, or the like; R.sup.7 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, or the like; R.sup.8 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, or the like, provided that R.sup.8 is not unsubstituted methyl or trifluoromethyl; Y is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, or the like, provided that Y is not unsubstituted methyl or unsubstituted ethyl; Z is —CR.sup.6═, or —N═; R.sup.1 is hydrogen, or substituted or unsubstituted alkyl; R.sup.4, R.sup.5 and R.sup.6 are each independently hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, or the like.

A dry powder containing dry particles that contain a tiotropium salt, one or more amino acids, and acid content, and optionally, sodium chloride, and/or one or more additional therapeutic agents, wherein the molar ratio of acid to amino acid is from about 0.0005 to about 5, or 0.002 to about 1. In one aspect, the dry powder containing dry particles is suitable for administration to the respiratory tract. In one aspect, the dry powder containing dry particles is a respirable dry powder contains respirable dry particles that contain a tiotropium salt, one or more amino acids, acid content, sodium chloride, and optionally one or ore additional therapeutic agents, wherein the tiotropium salt is about 0.01% to about 0.5%, the leucine is about 5% to about 40%, the sodium chloride is about 50% to about 90%, the optional one or more additional therapeutic agents are up to about 30%, and the molar ratio of acid to amino acid is from about 0.002 to about 1, where all percentages are weight percentages on a dry basis and all the components of the respirable dry particles amount to 100%.

A dry powder containing dry particles that contain a tiotropium salt, one or more amino acids, and acid content, and optionally, sodium chloride, and/or one or more additional therapeutic agents, wherein the molar ratio of acid to amino acid is from about 0.0005 to about 5, or 0.002 to about 1. In one aspect, the dry powder containing dry particles is suitable for administration to the respiratory tract. In one aspect, the dry powder containing dry particles is a respirable dry powder contains respirable dry particles that contain a tiotropium salt, one or more amino acids, acid content, sodium chloride, and optionally one or ore additional therapeutic agents, wherein the tiotropium salt is about 0.01% to about 0.5%, the leucine is about 5% to about 40%, the sodium chloride is about 50% to about 90%, the optional one or more additional therapeutic agents are up to about 30%, and the molar ratio of acid to amino acid is from about 0.002 to about 1, where all percentages are weight percentages on a dry basis and all the components of the respirable dry particles amount to 100%.

The present invention relates to N-acylimino compound of formula (I): ##STR00001##
wherein X is O or S, in particular O; Y is a single bond, O, S or NR.sup.5; Het is a 5 or 6 membered carbon-bound or nitrogen-bound heterocyclic ring, W.sup.1-W.sup.2-W.sup.3-W.sup.4 represents a carbon chain group connected to N and C═N, and thus forming a saturated, unsaturated, or partially unsaturated 5 or 6 membered nitrogen containing heterocycle, wherein W.sup.1, W.sup.2, W.sup.3 and W.sup.4 each individually represent CR.sup.vR.sup.w; R.sup.1, R.sup.2 may be hydrogen, halogen, etc.; R.sup.3 may be hydrogen, CN, C.sub.1-C.sub.6-alkyl, etc.; R.sup.4 may be of hydrogen, C.sub.1-C.sub.6-alkyl, C.sub.2-C.sub.6-alkenyl, C.sub.2-C.sub.6-alkinyl, C.sub.3-C.sub.8-cycloalkyl, Q-phenyl, Q′-O-phenyl, Q′-S-phenyl, where the phenyl ring is optionally substituted with one or more, e.g. 1, 2, 3, 4 or 5 identical or different substituents R.sup.10, and the moieties Q-Het.sup.#, Q′-O-Het.sup.# and Q′-S-Het.sup.# where Het# represents a heterocyclic radical and where Q and Q′ are C.sub.1-C.sub.6-alkandiyl, C.sub.2-C.sub.6-alkendiyl, or C.sub.2-C.sub.6-alkyndiyl, and where Q may also be a single bond; R.sup.3 and R.sup.4 together may also may also a bivalent radical, selected from the group consisting of C.sub.2-C.sub.5-alkandiyl, C.sub.2-C.sub.5-alkendiyl, Q″-C.sub.1-C.sub.4-alkandiyl and Q″-C.sub.2-C.sub.4-alkendiyl, where Q″ is O or S. The invention also relates to the use of the N-acylimino heterocyclic compounds, their stereoisomers, their tautomers and their salts, for combating invertebrate pests. Furthermore the invention relates also to methods of combating invertebrate pests, which comprises applying such compounds.

The present invention relates to N-acylimino compound of formula (I): ##STR00001##
wherein X is O or S, in particular O; Y is a single bond, O, S or NR.sup.5; Het is a 5 or 6 membered carbon-bound or nitrogen-bound heterocyclic ring, W.sup.1-W.sup.2-W.sup.3-W.sup.4 represents a carbon chain group connected to N and C═N, and thus forming a saturated, unsaturated, or partially unsaturated 5 or 6 membered nitrogen containing heterocycle, wherein W.sup.1, W.sup.2, W.sup.3 and W.sup.4 each individually represent CR.sup.vR.sup.w; R.sup.1, R.sup.2 may be hydrogen, halogen, etc.; R.sup.3 may be hydrogen, CN, C.sub.1-C.sub.6-alkyl, etc.; R.sup.4 may be of hydrogen, C.sub.1-C.sub.6-alkyl, C.sub.2-C.sub.6-alkenyl, C.sub.2-C.sub.6-alkinyl, C.sub.3-C.sub.8-cycloalkyl, Q-phenyl, Q′-O-phenyl, Q′-S-phenyl, where the phenyl ring is optionally substituted with one or more, e.g. 1, 2, 3, 4 or 5 identical or different substituents R.sup.10, and the moieties Q-Het.sup.#, Q′-O-Het.sup.# and Q′-S-Het.sup.# where Het# represents a heterocyclic radical and where Q and Q′ are C.sub.1-C.sub.6-alkandiyl, C.sub.2-C.sub.6-alkendiyl, or C.sub.2-C.sub.6-alkyndiyl, and where Q may also be a single bond; R.sup.3 and R.sup.4 together may also may also a bivalent radical, selected from the group consisting of C.sub.2-C.sub.5-alkandiyl, C.sub.2-C.sub.5-alkendiyl, Q″-C.sub.1-C.sub.4-alkandiyl and Q″-C.sub.2-C.sub.4-alkendiyl, where Q″ is O or S. The invention also relates to the use of the N-acylimino heterocyclic compounds, their stereoisomers, their tautomers and their salts, for combating invertebrate pests. Furthermore the invention relates also to methods of combating invertebrate pests, which comprises applying such compounds.

The present invention describes dibenzofuran derivatives substituted by electron-deficient heteroaryl groups, and electronic devices, especially organic electroluminescent devices, comprising these compounds as triplet matrix materials.