Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.

Compounds, compositions, and methods

Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N -oxides, and salts thereof, wherein Q is Q-1, Q-2, Q-3 or Q-4 and A, R 1 , m, X 1 , X 2 , X 3 , X 4 , Y 1 , Y 2 and Y 3 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.

Heterocycle-substituted bicyclic azole pesticides

A compound having structure (I) wherein (a) n is from 1 to about 3; (b) X is selected from the group consisting of O, S, SO, or SO2; (c) Y is independently hydrogen or straight, branched or cyclic alkyl having from 1 to about 4 carbon atoms, or the Y's are bonded together to form an alkanyl ring having from 3 to 7 atoms other than hydrogen; (d) Z is hydrogen or straight, branched or cyclic alkyl; Z having from 3 to about 10 atoms other than hydrogen; (e) R1 is hydrogen or straight, branched or cyclic alkyl, halo, carboxyl, carboxamido, alkoxycarbonyl or alkylcarbonyl; (f) T is O or S; (g) U is O, S, N or N-R2; (h) W is CR3R4, C=O, C=S, C=NR5, C-O-R6, C-S-R6, C-NH2, C-NH-R7, or C-NR6R7; (i) V is (CH2)n, O, S, or N-R2; (j) R2 is hydrogen, alkyl, hydroxy, alkoxy, alkoxycarbonyl, or alkylcarbonyl; (k) R3 and R4 are independently selected from the group consisting of hydrogen, alkyl, halo, hydroxy, alkoxy, mercapto, alkylthio, or cyano; (l) R5 is hydrogen, alkyl, hydroxy or alkoxy; (j) R6 is hydrogen or alkyl; and (k) R7 is hydrogen, alkyl or C(=NH)N(R6)2. Pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pain using such compounds.

Dihydrobenzofuran and related compounds useful as anti-inflammatory agents

φ-Substituted phenyl-prostaglandin E derivatives represented by general formula (I); and a process for producing the same, (I) wherein each symbol is as defined in the description. Because of binding strongly to PGE2 receptors (in particular, subtype EP4), the compounds represented by general formula (I) are useful in preventing and/or treating immunologic diseases (autoimmune diseases such as amyotrophic lateral sclerosis (ALS), rejection reactions following organ transplantation, etc.), asthma, bone dysplasia, nerve cell death, lung failure, liver failure, etc. Also, these compounds participate in sleep disorder and platelet agglutination and, therefore, are useful in treating diseases relating thereto.

$g(v)-SUBSTITUTED PHENYL-PROSTAGLANDIN E DERIVATIVES AND DRUGS CONTAINING THE SAME AS THE ACTIVE INGREDIENT

Aminoalkyl-substituted benzo-heterocyclic compounds of the formula ##STR1## wherein M, Q, R and T are as defined in the specification, as well as acid addition salts thereof. These compounds are useful as cholesterol level lowering agents and as antimycotic agents.

Aminoalkyl-substituted benzo-heterocyclic compounds

Pharmaceutical compositions containing a benzoxazole compound and a 2,3-dihydrobenzofuran compound represented by the following formula (I) and its pharmaceutically acceptable salt: ##STR1## In the formula, any one of P, Q, R and S is a group represented by the formula: ##STR2## and R1, R2 and the reining three substituents out of the substituents P to S each independently stand for various substituents. These compositions are used as an ATCAT inhibitor or for treating hyperlipidemia and atherosclerosis.

Benzoxa condensed ring compounds, process for producing the same and pharmaceutical composition comprising the same

A benzoxazole compound and a 2,3-dihydrobenzofuran compound, each represented by general formula (I), and a pharmaceutical composition containing a pharmaceutically acceptable salt thereof, which is used for inhibiting ATCAT and treating hyperlipemia and arteriosclerosis, wherein one member among P, Q, R and S represents a group of (a), and R₁, R₂ and the rest of P to S represent various substituents.

Condensed benzoxa ring compound, production thereof, and pharmaceutical composition containing the same

A benzopyran derivative represented by general formula (I), a pharmaceutically acceptable salt thereof, and an ACAT inhibitor, an antihyperlipemic agent and an antiarteriosclerotic composition each containing the same as the active ingredient; formula (I) wherein one of X and Y represents the group (1) and the other of X and Y and R?1 to R10? represent each a substituent.

Benzopyran derivative, production thereof, and pharmaceutical composition containing the same

PURPOSE: To obtain enol ester derivatives of a prostaglandin E1 and 7- thiaprostaglandin E1 compound easily and in high yield. CONSTITUTION: A reaction is couducted between a compound of formula I (P is a 1-6C alkyl or phenyl), an organocopper reagent prepared from a compound of the formula CuQ (Q is a halogen, CN, phenylthio, 1-pentynyl or 1- hexynyl) and a 1-4C alkyl lithium and a compound of formula II [A is S or CH2 ; R is a tri (1-7C hydrocarbon) silyl or a group capable of forming an acetal linkage with the O atom of OH; R is a 1-10C alkyl, 2-10C alkenyl, phenyl, 3-10C cycloalkyl or a phenyl-1-2C alkyl] followed by reaction with a compound of the formula (R CO)2 O or the formula R COCl (R is the same as R ) to produce a compound of formula III, which is reacted with a halogen to produce a compound of formula IV (X is I or Br), and then is reacted with a compound of formula V (R is a 1-10C alkyl, a 2-10C alkyl, a 2-10C alkyl, phenyl, phenoxy or a 3-10C cycloalkyl), thus obtaining the objective compound of formula VI.

Production of prostaglandin e1 compound and synthetic intermediate therefor

A benzopyran derivative represented by the formula (I) or its pharmaceutically acceptable salt: ##STR1## wherein either one of X and Y stands for the following formula ##STR2## and the other one of X and Y and R1 -R10 stand for various substituents, and ACAT inhibitor, anti-hyperlipidemia agent and anti-atherosclerosis agent compositions containing the same as an active ingredient.

Kataoka Kenichiro

Papers

Benzoxa condensed ring compounds, process for producing the same and pharmaceutical composition comprising the same

Condensed benzoxa ring compound, production thereof, and pharmaceutical composition containing the same

Benzopyran derivative, production thereof, and pharmaceutical composition containing the same

Production of prostaglandin e1 compound and synthetic intermediate therefor

Benzopyran derivative, process for producing the same and pharmaceutical composition containing the same