Provided are compounds of Formula (I′) or (II′), or pharmaceutically acceptable salts thereof, and methods for their use and production.

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Provided are compounds of Formula (I′) or (II′), or pharmaceutically acceptable salts thereof, and methods for their use and production.

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The problem to be solved by the present invention is to provide a compound suitable for a pharmaceutical composition, specifically an agent for treating nocturia.

The inventors have assumed that inhibition of nocturnal activity of placental leucine aminopeptidase (P-LAP), i.e. aminopeptidase that cleaves AVP, would maintain and/or increase an endogenous AVP level to enhance the antidiuretic effect, which would contribute to a decreased number of nocturnal voids, and have extensively studied compounds which inhibit P-LAP. As a result, the inventors have found that (2R)-3-amino-2-(pyridylmethyl)-2-hydroxy-propanoic acid derivatives have excellent P-LAP inhibitory activity. The inventors have evaluated antidiuretic effects in water-loaded rats and have found that the compounds increase endogenous AVP levels by inhibiting P-LAP and consequently reduce urine production. The present invention therefore provides compounds expected to be used as an agent for treating nocturia based on P-LAP inhibition.

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 ##STR00001##
wherein ring A is a 4- to 7-membered ring optionally having substituent(s); L is —O—, —S—, —SO— or —SO.sub.2—; R.sup.1 is a C.sub.1-6 alkyl group optionally having substituent(s) (provided that when L is —O—, R.sup.1 is not a C.sub.1-6 alkyl group optionally substituted by halogen atom(s)), or a cyclic group optionally having substituent(s); X.sub.1 is —CRa═ or —N═; X.sub.2 is —CRb═ or —N═; X.sub.3 is —CRc= or —N═; Ra, Rb and Rc are each a C.sub.1-6 alkyl group, C.sub.2-6 alkenyl group, C.sub.1-6 alkoxy group, C.sub.3-6 cycloalkyl group, C.sub.3-6 cycloalkoxy group or C.sub.6-14 aryl group, each of which optionally having substituent(s), H or halogen, or a salt thereof.

Provided are a compound of Formula I or Formula IA, a composition comprising a compound of Formula I or Formula IA, uses of the compounds and compositions to modulate insect behaviour and methods for modulating insect behaviour. Also provided are biosensors for detecting an analyte in a sample, uses of the biosensor, and methods for detecting an analyte in a sample.

Provided are a compound of Formula I or Formula IA, a composition comprising a compound of Formula I or Formula IA, uses of the compounds and compositions to modulate insect behaviour and methods for modulating insect behaviour. Also provided are biosensors for detecting an analyte in a sample, uses of the biosensor, and methods for detecting an analyte in a sample.

Disclosed herein are certain acetamido derivatives that are DNA Polymerase Theta (Polθ) inhibitors of Formula (I).

##STR00001##

Also, disclosed are pharmaceutical compositions comprising such compounds and methods of treating diseases treatable by inhibition of Polθ such as cancer, including homologous recombination (HR) deficient cancers.

The invention discloses a monosubstituted or polysubstituted amphiphilic hypocrellin derivative, and a preparation method and application thereof. The amphiphilic hypocrellin derivative substituted by a group containing PEG, a quaternary ammonium salt or the like prepared according to the invention has an obvious red shift in its absorption spectrum and a significantly enhanced molar extinction coefficient, compared with the parent hypocrellin, can efficiently produce singlet state oxygen and other reactive oxygen species under photosensitive conditions; has different amphiphilicities and increased biocompatibility with cells or tissues by regulating its hydrophilicity and hydrophobicity; can meet the requirements of different clinical drugs, and solves the requirements of different drug delivery methods for different drug hydrophilicity and lipophilicity. Under identical conditions, the amphiphilic hypocrellin derivative photosensitizer according to the invention has higher ability to photodynamically inactivate tumor cells than the first and second generation commercial photosensitizers.

The invention discloses a monosubstituted or polysubstituted amphiphilic hypocrellin derivative, and a preparation method and application thereof. The amphiphilic hypocrellin derivative substituted by a group containing PEG, a quaternary ammonium salt or the like prepared according to the invention has an obvious red shift in its absorption spectrum and a significantly enhanced molar extinction coefficient, compared with the parent hypocrellin, can efficiently produce singlet state oxygen and other reactive oxygen species under photosensitive conditions; has different amphiphilicities and increased biocompatibility with cells or tissues by regulating its hydrophilicity and hydrophobicity; can meet the requirements of different clinical drugs, and solves the requirements of different drug delivery methods for different drug hydrophilicity and lipophilicity. Under identical conditions, the amphiphilic hypocrellin derivative photosensitizer according to the invention has higher ability to photodynamically inactivate tumor cells than the first and second generation commercial photosensitizers.

This invention relates to 4-substituted isoquinoline compounds and their derivatives and uses thereof for treatment of cancer, for example, acute myeloid leukemia.