920results about "Urea derivatives preparation" patented technology

This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.

Described herein are compounds and compositions characterized, in certain embodiments, by conjugation of various groups, such as lipophilic groups, to an amino or amide group of an amino acid, a linear or cyclic peptide, a linear or cyclic polypeptide, or structural isomer thereof, to provide compounds of the present invention, collectively referred to herein as “APPLs”. Such APPLs are deemed useful for a variety of applications, such as, for example, improved nucleotide delivery. Exemplary APPLs include, but are not limited to, compounds of Formula (I), (II), (III), (IV), (V), and (VI), and salts thereof, as described herein:

wherein m, n, p, R′, R¹, R², R³, R⁴, R⁵, R⁸, Z, W, Y, and Z are as defined herein.

The invention provides novel classes of HDAC inhibitors. Methods of sensitizing a cancer cell to the cytotoxic effects of radiotherapy are also provided as well as methods for treating cancer and methods for treating neurological diseases. Additionally, the invention further provides pharmaceutical compositions comprising an HDAC inhibitor of the invention, and kits comprising a container containing an HDAC inhibitor of the invention.

This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor. The SARM compounds, either alone or as a composition, are useful for a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia, osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment and/or prevention of acute and/or chronic muscular wasting conditions; e) preventing and/or treating dry eye conditions; f) oral androgen replacement therapy; and/or g) decreasing the incidence of, halting or causing a regression of prostate cancer.

Described herein are prostate specific membrane antigen (PSMA) binding conjugates that are useful for delivering therapeutic, diagnostic and imaging agents. Also described herein are pharmaceutical composition containing them and methods of using the conjugates and compositions. Also described are processes for manufacture of the conjugates and the compositions containing them.

Compounds of formula (I)wherein the groups are as defined in the description are disclosed.The compounds of formula (I) are endowed with reversible inhibiting activity of carnitine palmitoyl-transferase and are useful in the preparation of medicaments useful in the pathologies related to a hyperactivity of carnitine palmitoyl-transferase, such as hyperglycemia, diabetes and pathologies related thereto, heart failure, ischemia.

This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor. The SARM compounds, either alone or as a composition, are usefull for a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia, osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment and/or prevention of acute and/or chronic muscular wasting conditions; e) preventing and/or treating dry eye conditions; f) oral androgen replacement therapy; and/or g) decreasing the incidence of, halting or causing a regression of prostate cancer.

Disclosed are novel aromatic compounds of the formula (I) wherein G, X, Ar, L and Q are defined herein. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are processes of making such compounds.

The present patent application relates to compounds having formula (I) or a pharmaceutically acceptable salt thereof wherein one of R1, R2 and R3 is a non-cyclic acidic group having a pKa value below 8 or a group which is in vivo convertible to such a group; R4, R5 and the other two of the substituents R1, R2 and R3 are each independently selected from hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, alkoxy, hydroxy, halogen, trifluoromethyl, trifluoromethoxy, cyano, nitro, amnino, and aryl, aralkyl, arylamino, aryloxy, aryl-CO-, or heteroaryl, wherein the aryl and heteroaryl groups may be substituted one or more times with substituents selected from alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, hydroxy, alkoxy, halogen, trifluoromethyl, trifluoromethoxy, cyano, nitro and amino; or R3 and R4 or R4 and R5 together form a fused 4- to 7-membered carbocyclic ring which may be unsaturated, or partially or fully saturated, while the other substituents R1, R2, R3, R4 and R5 are as defined above; Y is -CO-, -CS-, -SO2-, or -C(=N-R8)-, wherein R8 is hydrogen, alkyl, or cyano; X is -NH-, -CH2-NH-, or -SO2-NH-; Z is NR6, O, -CH=CH-, -C=C-, -N=CH-, or -CH=N-; wherein R6 is hydrogen, or alkyl; R11, R12, R13, R14 and R15 are each independently selected from hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, alkoxy, hydroxy, halogen, trifluoromethyl, trifluoromethoxy, cyano, nitro, amino, -NHSO2-R7, -COOR7, -SO2N(R7)2, -SO2OR7 and -CO-R7, wherein R7 is hydrogen alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, aryl or aralkyl; and aryl, aralkyl, arylamino, aryloxy, aryl-CO-, or heteroaryl, wherein the aryl and heteroaryl groups may be substituted one or more times with substituents selected from alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, hydroxy, alkoxy, halogen, trifluoromethyl, trifluoromethoxy, cyano, nitro and amino; or one of R11 and R12, R12 a

Apparatus and methods for producing urea are provided. In one or more embodiments, an apparatus for producing urea can include a first zone, which can include a first flow channel in fluid communication with a first tube disposed about a first end of a plurality of trays, a second flow channel in fluid communication with a second tube disposed about the first end of the trays and a second end of the trays, and a third flow channel in fluid communication with a third tube disposed about the first and second ends of the trays. The apparatus can include a second zone, which can include a fixed bed comprising one or more inert packing materials disposed therein to provide additional surface area. The apparatus can include a third zone, which can include a plurality of tubes disposed therein. The second zone can be disposed between the first and third zones.

The present invention provides for a rheology control agent that includes a following compound represented by the following formula:

wherein A, B, C and D equal CH₂, CHR, NH, or O, and A, B, C and D may be the same or different and at least one of A and B equals NH and at least one of C and D equals NH; and wherein R₁, R₂, and R₃ may be the same or different and represent a linear, branched, hyper-branched, or dendritic ether, polyether or hydrocarbon based chain, optionally forming at least one carbon-based ring, being saturated or unsaturated and R₂ represents linear or branched alkylenes, ethers, polyethers, or polyester linkages and at least one of R₁, R₂, and R₃ comprises an ester group or an amide group which is branched off from the main chain; excluded from Formula (1) is a compound wherein R₂ is CH₂—CH₂—CH₂—CH₂—CH(C(O)OCH₃), A, B, C, and D are equal to NH and R₁ and R₃ are both equal to a linear octyl hydrocarbon chain; the rheology control agent is suitable for solvent-borne and water-borne coating composition having improved rheology control useful for OEM refinishing or repainting the exterior of automobile and truck bodies and parts thereof.

A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any glucagon-mediated conditions and diseases such as hyperglycemia, Type 1 diabetes, Type 2 diabetes and obesity.

A pharmaceutical composition includes a therapeutically effective amount of exo-S-mecamylamine or a pharmaceutically acceptable salt thereof, substantially free of exo-R-mecamylamine in combination with a pharmaceutically acceptable carrier. Preferably the amount is about 0.5 mg to about 20 mg. Medical conditions are treated by administering a therapeutically effective amount of exo-S-mecamylamine or a pharmaceutically acceptable salt thereof, substantially free of its exo-R-mecamylamine, said amount being sufficient to ameliorate the medical condition. The medical conditions include but are not limited to substance addiction (involving nicotine, cocaine, alcohol, amphetamine, opiate, other psychostimulant and a combination thereof), aiding smoking cessation, treating weight gain associated with smoking cessation, hypertension, hypertensive crisis, Tourette's Syndrome and other tremors, cancer (such as small cell lung cancer), atherogenic profile, neuropsychiatric disorders (such as bipolar disorder, depression, an anxiety disorder, schizophrenia, a seizure disorder, Parkinson's disease and attention deficit hyperactivity disorder), chronic fatigue syndrome, Crohn's disease, autonomic dysreflexia, and spasmogenic intestinal disorders.

This invention relates to novel compounds of Formula (I), and a novel use of these compounds in treating chemokine mediated diseases, wherein the chemokine binds to an IL-8 a or b receptor. Compounds of Formula (1) are represented by the structure:wherein interalia, X is oxygen or sulfur;R is any functional moiety having an ionizable hydrogen and a pKa of 10 or less;R1 is independently selected from hydrogen; halogen; nitro; cyano; C1-C10 alkyl; halosubstituted C1-10 alkyl; C2-10 alkenyl; C1-10 alkoxy; halosubstituted C1-10 alkoxy; azide; (CR8R8)qS(O)tR4; hydroxy; hydroxy substituted C1-4 alkyl; aryl; aryl C1-4 alkyl; aryl C2-10 alkenyl; aryloxy; aryl C1-4 alkyloxy; heteroaryl; heteroarylalkyl; heteroaryl C2-10 alkenyl; heteroaryl C1-4 alkyloxy; heterocyclic, heterocyclic C1-4 alkyl; heterocyclic C1-4 alkyloxy; heterocyclic C2-10 alkenyl;q is 0 or an integer having a value of 1 to 10; n is an integer having a value of 1 to 3;m is an integer having a value of 1 to 3;n is an integer having a value of 1 to 3;Y is hydrogen; halogen; nitro; cyano; halosubstituted C1-10 alkyl; C1-10 alkyl; C2-10 alkenyl; C1-10 alkoxy; halosubstituted C1-1- alkoxy; azide; (CR8R8)qS(O)tR4, (CR8R8)qOR4; hydroxy; hydroxy substituted C1-4 alkyl; aryl; aryl C1-4 alkyl; aryloxy; aryC1-4 alkyloxy; aryl C2-10 alkenyl; heteroaryl; heteroarylalkyl; heteroaryl C1-4 alkyloxy; heteroaryl C2-10 alkenyl; heterocyclic, heterocyclic C1-4 alkyl; heterocyclic C2-10 alkenyl;or a pharmaceutically acceptable salt thereof.

The present invention relates to therapeutic targets for cancer. In particular, the present invention relates to small molecules and nucleic acids that target EZH2 expression in cancer (e.g., prostate cancer, breast cancer, other solid tumors, multiple myeloma).

A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any diseases and disorders, wherein a glucagon antagonistic action is beneficial, such as hyperglycemia, Type 1 diabetes, Type 2 diabetes, disorders of the lipid metabolism, such as dyslipidemia, and obesity.

The invention relates to small molecules which function as inhibitors of anti-apoptotic Bcl-2 family member proteins (e.g., Bcl-2 and Bcl-xL). The invention also relates to the use of these compounds for inducing apoptotic cell death and sensitizing cells to the induction of apoptotic cell death.

The present invention provides methods of forming carbamates, ureas, and isocyanates. In certain embodiments these methods include the step of reacting an amine with an ester-substituted diaryl carbonate to form an activated carbamate which can be further derivitized to form non-activated carbamate or a urea. The urea or carbamate can be subjected to a pyrolysis reaction to form isocyanate.

The present invention relates to antibacterial agents that are useful for sterilization, sanitation, antisepsis, and disinfection

PCT No. PCT/EP95/03539 Sec. 371 Date Mar. 21, 1997 Sec. 102(e) Date Mar. 21, 1997 PCT Filed Sep. 8, 1995 PCT Pub. No. WO96/09136 PCT Pub. Date Mar. 28, 1996A method for repairing and restoring the functionality of equipment subjected to internal corrosion during its operation at high or medium pressure in a plant for the synthesis of urea. The method includes the cleaning of the corroded area, the formation of suitable supporting and/or holding surfaces for the placement of a new metallic lining, the formation of a new anticorrosive sealed off lining, obtained by positioning and welding flat elements and metallic plates which are suitably shaped and placed next to each other to become adapted to the internal profile of the equipment. The spaces and interstices below this new lining all communicate with at least one weep-hole present in the pressure resistant body. The entire repair is carried out through the manhole of the equipment and enables the restoring of its functionality for times similar to the normal duration of corresponding newly constructed equipment.

The present invention is directed to providing a method of producing synthetic fuels and organic chemicals from atmospheric carbon dioxide. Carbon dioxide gas is extracted from the atmosphere, hydrogen gas is obtained by splitting water, a mixture of the carbon dioxide gas and the hydrogen gas (synthesis gas) is generated, and the synthesis gas is converted into synthetic fuels and/or organic products. The present invention is also directed to utilizing a nuclear power reactor to provide power for the method of the present invention.

Prostate-specific membrane antigen (PSMA) binding compounds having radioisotope substituents are described, as well as chemical precursors thereof. Compounds include pyridine containing compounds, compounds having phenylhydrazine structures, and acylated lysine compounds. The compounds allow ready incorporation of radionuclides for single photon emission computed tomography (SPECT) and positron emission tomography (PET) for imaging, for example, prostate cancer cells and angiogenesis.

The invention relates to a method for preparing urea catalytic liquid for a vehicle, which comprises the following steps: (1) preparing purified water of which the conductivity is below 10 mu s/em and the resistivity is between 16 and 19 MOmega cm by utilizing a two-step method; (2) adding the purified water prepared in the step (1) into raw material urea, and stirring and heating the mixture to between 50 and 70 DEG C, and performing absorption treatment on the obtained urea solution by using activated carbon so as to enable the specific gravity of the urea solution to reach 1.18-1.20; and (3) preparing solution of which the crystalline urea accounts for 25 to 40 weight percent by adding the purified water prepared in the step (1) into the crystalline urea obtained in the step (2), and filtering the solution by using a superfine film once more so as to obtain the required catalytic liquid containing the urea. The impurity content of the catalytic liquid (particularly the content of biuret) prepared by the method fully meets requirements of the standard.

Polyurethane compositions are produced in a two-stage method. In a first step, a diol component with a molecular weight of less than 2000 is reacted with a monomeric diisocyanate with a molecular weight of less than 500 and the unreacted monomeric diisocyanate is removed from this reaction product. In a second step, the resulting high-molecular diisocyanate is reacted with a polyol to produce a reactive prepolymer with isocyanate and groups. The addition of polyisocyanates which are capable of migration and which have a substantially lower vapor pressure than diphenylmethanediisocyanate, improves the addition behavior of the invention polyurethane compositions. Reactive polyurethane compositions of this type are suitable for using as binding agents for reactive one or two component adhesives/sealants, which may optionally contain solvents. These compositions are also suitable for producing reactive hot melt adhesives when suitable polyols are selected. A substantial advantage of these compositions compared to known polyurethane compositions is the considerably lower proportion of monomeric diisocyanates with a molecular weight of less than 500.

Coating compositions contain hydroxyl- or carbamate functional resins with a relatively low equivalent weight. The resins are based on a polyol core containing urea and hydroxyl groups, and made by reacting a polyisocyanate, preferably a triisocyanate, with an amino functional polyol, preferably a polyol having one amino group and two or more hydroxyl groups. The polyol core may be further extended to a first or higher generation dendrimer or hyperbranched structure by reacting the initial polyol core with a compound having one carboxyl group and two or more hydroxyl groups.

The invention provides compounds and methods for inhibition of kinases, such as those of the TAO family, more specifically KIAA1361, TAO, and JIK kinases. The invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinase receptor signal transduction pathways related to the changes in cellular activities as mentioned above, and the invention includes compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions.

The present invention relates to tetra-substituted urea compounds which are modulators of 11-β hydroxyl steroid dehydrogenase type 1 (11βHSD1), their pharmaceutical compositions, and methods of using the same.

The invention provides for novel compounds which are inhibitors of lysine-specific demethylase 1 (LSD1). Such compounds may be used to treat disorders, including cancer.

The invention relates to a household garbage treatment method. According to the household garbage treatment method, the household garbage is subjected to thermal cracking to form mixed combustible gases containing carbon monoxide (CO), carbon dioxide (CO2), hydrogen (H2), methane (CH4), nitrogen (N2) and inert argon (Ar) by a full gasification process; and the mixed combustible gas flow is purified and separated and then are used for synthesizing methanol and/or dimethyl ether, generating electricity and synthesizing urea. The household garbage treatment method comprises eight steps of: performing pyrolysis gasification, cooling, removing dust, performing deacidification and desulfuration, performing transformation reaction, adjusting the ratio of components, compressing and synthesizing. By adopting the method, the optimal ratio of the components required by the synthesis reaction can be adjusted, in particular the CO, the CO2, the H2 and the N2 can be comprehensively utilized, the N2 of an air separation device and the H2 of a purification system are synthesized to generate NH3, and the NH3 and the CO2 are synthesized to generate urea; biomass gas is used for generating electricity, so the heat efficiency can reach 30 to 40 percent; and by adopting the method, reclamation and zero emission of the household garbage can be realized.

Phenylalanine derivatives of the following formulae and analogues thereof have an antagonistic activity to α4 integrin. They are used as therapeutic agents for various diseases concerning α4 integrin