Abstract: Provided is a compound having a cholinergic muscarinic M1 receptor positive allosteric modulator activity, and useful as a prophylactic or therapeutic drug for Alzheimer's disease, schizophrenia, pain, sleep disorder and the like. The present invention relates to a compound represented by the formula wherein ring A is a 4- to 7-membered ring optionally having substituent(s); L is —O—, —S—, —SO— or —SO2—; R1 is a C1-6 alkyl group optionally having substituent(s) (provided that when L is —O—, R1 is not a C1-6 alkyl group optionally substituted by halogen atom(s)), or a cyclic group optionally having substituent(s); X1 is —CRa? or —N?; X2 is —CRb? or —N?; X3 is —CRc= or —N?; Ra, Rb and Rc are each a C1-6 alkyl group, C2-6 alkenyl group, C1-6 alkoxy group, C3-6 cycloalkyl group, C3-6 cycloalkoxy group or C6-14 aryl group, each of which optionally having substituent(s), H or halogen, or a salt thereof.

Abstract: This invention is directed to photoluminescent compounds based on rhodamine dyes with red-shifted absorption and emission maxima and uses thereof for photoluminescence based devices.

Abstract: The present invention is directed to 3-ester-4-substituted compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 3-ester-4-substituted compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.

Abstract: Compounds of formula (I), defined herein, are both phosphodiesterase 4 (PDE4) enzyme inhibitors and muscarinic M3 receptor antagonists and are useful for the prevention and/or treatment of a disease of the respiratory tract.

Abstract: The present invention relates to a method for the synthesis of 7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin (i.e. iriniotecan), comprising: (a) preparing 10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptotecin; and (b) selectively ethylating the compound of step (a) at the 7-position, thus resulting in the preparation of 7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin. The present invention is further directed to the use of 10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin (i.e. 7-des-ethyl-irinotecan) as intermediate in a method for the synthesis of irinotecan as described.

Abstract: The present invention is directed to [1,2,4]triazolo[4,3-a]pyridine and [1,2,4]triazolo[4,3-a]pyrazine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer.

Abstract: Trientine prodrugs, pharmaceutical compositions comprising the trientine prodrugs, and methods of using trientine prodrugs and pharmaceutical compositions thereof for treating Wilson's disease.

Abstract: Provided is a compound having a cholinergic muscarinic M1 receptor positive allosteric modulator activity, and useful as a prophylactic or therapeutic drug for Alzheimer's disease, schizophrenia, pain, sleep disorder and the like. The present invention relates to a compound represented by the formula wherein ring A is a 4- to 7-membered ring optionally having substituent(s); L is —O—, —S—, —SO— or —SO2—; R1 is a C1-6 alkyl group optionally having substituent(s) (provided that when L is —O—, R1 is not a C1-6 alkyl group optionally substituted by halogen atom(s)), or a cyclic group optionally having substituent(s); X1 is —CRa? or —N?; X2 is —CRb? or —N?; X3 is —CRc= or —N?; Ra, Rb and Rc are each a C1-6 alkyl group, C2-6 alkenyl group, C1-6 alkoxy group, C3-6 cycloalkyl group, C3-6 cycloalkoxy group or C6-14 aryl group, each of which optionally having substituent(s), H or halogen, or a salt thereof.

Abstract: A compound of formula (Ie?): wherein Ar?, R1, R4e and Y are as defined herein and a method of controlling pests using the compound.

Abstract: The present invention relates to novel crystal forms of 4-(6-ethoxy-1-methoxy-thioxanthene-9-ylidene)-1-methyl piperidine salts and 4-(6-ethoxy-1-hydroxy-thioxanthene-9-ylidene)-1-methyl piperidine salts; especially to novel crystal forms of 4-(6-ethoxy-1-methoxy-thioxanthene-9-ylidene)-1-methyl piperidine hydrochloride and 4-(6-ethoxy-1-hydroxy-thioxanthene-9-ylidene)-1-methyl piperidine hydrochloride as well as to the use of these salts for preventing or treating migraine or pulmonary hypertension.

Abstract: 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.

Abstract: A borate compound for use as photoinduced chemical bleaching reagent is disclosed having improved bleaching performance under certain conditions, compared to neutral borates. The compounds are comprised of Formula I; R1R2R3R4BXa?? I where each R1, R2, and R3 and R4 is, independently, an alkyl, alkylaryl, or arylalkyl, with the proviso that at least one of R1, R2, and R3 and R4 is an alkyl group and at least two of R1, R2, R3 and R4 group is positively charged; X is an anion; and a equals 1, 2, or 3.

Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, W, A and B are as described herein, compositions including the compounds and methods of using the compounds.

Abstract: Provided herein are solid forms comprising {[5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl]amino}acetic acid, compositions comprising the solid forms, methods of making the solid forms and methods of their use for the treatment of various diseases and/or disorders.

Abstract: The present invention relates to amide derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.

Abstract: The present invention relates to compounds of general formula I wherein R1, R2, R3 and R4 are as defined herein which may be used for the treatment of schizophrenia, obsessive-compulsive personality disorder, major depression, bipolar disorders, anxiety disorders, normal aging, epilepsy, retinal degeneration, traumatic brain injury, spinal cord injury, post-traumatic stress disorder, panic disorder, Parkinson's disease, dementia, Alzheimer's disease, cognitive impairment, chemotherapy-induced cognitive dysfunction (“chemobrain”), Down syndrome, autism spectrum disorders, hearing loss, tinnitus, spinocerebellar ataxia, amyotrophic lateral sclerosis, multiple sclerosis, Huntington's disease, stroke, and disturbances due to radiation therapy, chronic stress, optic neuropathy or macular degeneration, or abuse of neuro-active drugs, selected from alcohol, opiates, methamphetamine, phencyclidine and cocaine.

Abstract: The subject of the present invention are water-soluble derivatives of camptothecin, their synthesis and use. These compounds exhibit preferable biological properties for use in anti-neoplasm therapy.

Abstract: Provided herein are modified amino acids comprising an azido group, polypeptides, antibodies and conjugates comprising the modified amino acids, and methods of producing the polypeptides, antibodies and conjugates comprising the modified amino acids. The polypeptides, antibodies and conjugates are useful in methods of treatment and prevention, methods of detection and methods of diagnosis.

Abstract: Compounds and compositions are provided that inhibit histone deacylase activity and which expand renal progenitor cell populations and improve kidney function in a damaged kidney. Methods of use of the compounds and compositions are provided.

Abstract: Provided herein are processes useful for the preparation of 2-carboxamide cycloamino urea derivatives of formula (X), and useful intermediates therefore, at internal temperatures such as less than about ?5° C. to about ?15° C. and using solvents such as tetrahydrofuran, bases such as amines, and the like.