Abstract: The present invention relates to the field of medical chemistry, and discloses a preparing method for three crystal forms of cabazitaxel, that is, crystalline form J of cabazitaxel esterate, crystalline form G of cabazitaxel hydrate and crystalline form I of cabazitaxel, and a novel crystalline form of cabazitaxel. The novel crystalline form of cabazitaxel according to the invention has good stability and good solubility in commonly used solvents, and is easy to be preserved and is stable under treatment during preparation of dosage forms, thus could be used for the preparation of a medicament for treating prostate cancer.

Abstract: The present invention relates to a novel crystalline ethyl acetate solvate form of cabazitaxel or 4?-acetoxy-2?-benzoyloxy-5?,20-epoxy-1?-hydroxy-7?,10?-dimethoxy-9-oxo-11-taxen-13?-yl(2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate and process for preparing the same.

Abstract: The disclosure provides metal organic frameworks useful for sensing, gas sorption, microelectronics and switches.

Abstract: The present invention provides Crystalline Forms of 4-acetoxy-2?-benzoyloxy-5?-20-epoxy-1-hydroxy-7?,10?-dimethoxy-9-oxotax-11-en-13?-yl(2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate, i.e Cabazitaxel. The present invention also discloses methods for the preparation of Crystalline Forms of Cabazitaxel and pharmaceutical compositions thereof.

Abstract: The present invention relates to the technical field of medicine, and specifically provides methods for preparing Icotinib, Icotinib hydrochloride, and intermediates thereof. These methods avoid the use of phosphorus oxychloride, thereby greatly reducing the emission of pollutants, which is of major benefits to the economy and environment.

Abstract: A co-crystal compound containing ammonium nitrate and benzo-18-crown-6-ether. Ammonium nitrate and benzo-18-crown-6-ether are used to form the co-crystal compound with hydrogen bonding in a mole ratio of 1:1. A melting point of the co-crystal compound falls within a range of 124˜130° C., and the co-crystal compound can be prepared by an evaporation method or an anti-solvent method. The co-crystal compound comes with a non-hygroscopic property, a low burning rate (7 MPa, 0.58 mm/s) and a high pressure index (n>0.6), which can be used for replacing the oxidizer of a common gas generator propellant.

Abstract: Salacinol and ponkoranol homologues, derivatives thereof and methods of synthesizing and using said homologies and derivatives. The derivatives include stereoisomers, de-O-sulfonated compounds and congeners of the naturally occurring homologues. Some of the derivatives exhibit enhanced glucosidase inhibitory bioactivity in comparison to the naturally occurring compounds which have been isolated from Salacia reticulata.

Abstract: A co-crystal compound containing ammonium nitrate and benzo-18-crown-6-ether. Ammonium nitrate and benzo-18-crown-6-ether are used to form the co-crystal compound with hydrogen bonding in a mole ratio of 1:1. A melting point of the co-crystal compound falls within a range of 124˜130° C., and the co-crystal compound can be prepared by an evaporation method or an anti-solvent method. The co-crystal compound comes with a non-hygroscopic property, a low burning rate (7 MPa, 0.58 mm/s) and a high pressure index (n>0.6), which can be used for replacing the oxidizer of a common gas generator propellant.

Abstract: [c2] daisy chain macromers, dimers and polymers and related compositions, materials, methods and systems are described.

Abstract: The disclosure provides metal organic frameworks useful for sensing, gas sorption, microelectronics and switches.

Abstract: [c2] daisy chain macromers, dimers and polymers and related compositions, materials, methods and systems are described.

Abstract: Radically polymerizable macrocyclic polyethers or macrocyclic heteroanalogous polyethers, preferably crown ethers, heteroanalogous crown ethers and cryptands for use in dental materials is disclosed.

Abstract: The invention relates to a process for the preparation of 13,14-dihydro-PGF2? derivatives of R or S configuration at carbon 15, represented by the general formula (I), wherein the identity of the substituents is defined in the description. Compounds of the formula (I) are valuable biologically-active substances or intermediates in the preparation thereof. The invention especially relates to the process for preparation of 13,14-dihydro-15(R)-17-substituted-18,19,20-trinor-PGF2?, i.e., latanoprost.

Abstract: The invention relates to a process for the preparation of 13,14-dihydro-PGF2? derivatives of R or S configuration at carbon 15, represented by the general formula (I), wherein the identity of the substituents is defined in the description. Compounds of the formula (I) are valuable biologically-active substances or intermediates in the preparation thereof. The invention especially relates to the process for preparation of 13,14-dihydro-15(R)-17-substituted-18,19,20-trinor-PGF2?, i.e., latanoprost.

Abstract: The invention relates to compounds of formula I in which R1, R2, E, X1, X2, and X3 have the meaning as described in the specification and claims, obtained by culturing Streptomyces species HAG 004107 (DSM 13381), and their physiologically tolerable salts and chemical equivalents. The invention furthermore relates to a process for the preparation of the cyclipostins, the microorganism HAG 004107 (DSM 13381), the use of the cyclipostins and their physiologically tolerable salts and chemical equivalents as pharmaceuticals, in particular as inhibitors of lipases, and pharmaceutical preparations which contain cyclipostin or a physiologically tolerable salt or equivalent thereof.

Abstract: Compounds are provided having the formula including pharmaceutically acceptable salts thereof, wherein R1 is lower alkyl, aryl or arylalkyl; A is hydrogen or B is hydrogen, alkyl, alkenyl, or but when A is hydrogen, B may only be R2, R2′, R2″, R3 R3′ and R3″ are as defined herein; m is 0−3. These compounds possess activity at the beta 3 adrenergic receptor in mammals and are useful in the treatment of diabetes, obesity, depression, achalasia and intestinal hypermotility disorders.

Abstract: Tin polyaalkanecarboxylates having the formula [(R1pR2qSn)rOs]t wherein R1 represents C1-C6 alkyl, branched or straight, substituted or not by one or more hydroxyl groups or halogen atoms, or a phenyl group, substituted or not by one or more hydroxyl groups or halogen atoms, R2 is carboxylic residue selected from (I), (II), (III) or (IV); and p, q, r, s and t have the following meanings: P=3, q=1, r=1, s=) and t=1, p=2, q=2, r=1, s=0, and t=1, p=2, q=1, r=2, s=1 and t=2, have anti-tumor activity.

Abstract: A method of modifying or altering the structure of a 1&agr;-hydroxylated vitamin D compound to increase its biological activity by altering the conformational equilibrium of the A-ring to favor a chair conformation that presents the 1&agr;-hydroxyl in the axial orientation. This is accomplished by either locking the A-ring chair conformation in a geometry having an axially orientated 1&agr;-hydroxyl, or by the addition of one or more substituents to the A-ring which interact with other substituents in the molecule or on the A-ring to provide a driving force to the A-ring to adopt a chair conformation which presents the 1&agr;-hydroxyl in the axial orientation.

Abstract: The present invention is a fluorine-containing compound having i) a perfluoropolyoxyalkyl or -alkylene chain having an average molecular weight of 800 or more and ii) a cyclic or non-cyclic polyether atomic group. Its use as a low-scattering lubricant or surface modifier (water repellent) brings about an improvement in sliding durability of magnetic recording media.

Abstract: The present invention relates to novel bicycloaliphatic 2-methylene-1,3-dioxepanes, which are suitable as starting materials for the preparation of polymers and copolymers, preferably of composite and dental materials. The 2-methylene-1,3-dioxepanes according to the invention, which can undergo radical polymerisation with ring opening with only very little volume shrinkage, can be prepared in a simple manner, are easy to purify and to modify chemically, and are characterised by lack of odour and advantageous physical properties.

Abstract: A process of preparing a purified crown compound is disclosed which comprises the steps of (a) dissolving a crown compound and a salt in an organic solvent to form a solution of a complex salt of a crown compound; (b) filtering the solution to obtain a filtrate; (c) adding water to the filtrate to produce a precipitate; and (d) filtering out the produced precipitate.

Abstract: A sensor (10) is provided for detecting the concentration of potassium ions which comprises a molecule which selectively complexes potassium ions. The molecule, e.g., 2,2-bis[3,4-(15-crown-5)-2-nitrophenylcarbamoxymethyl]tetradecanol-14, has at least one binding site and is provided with a fluorophore group, e.g., Rhodamine-B, at that site. The molecule is one that expands upon complexation of potassium ions, such that the intensity of fluorescence increases. The change in fluorescent intensity is a direct measure of the concentration of potassium ions. A detector employing the sensor is also provided.

Abstract: A composition for removing or inactivating harmful components including virus from blood or other extracellular liquids comprises a crownether compound substituted on a polysaccharide, preferably dextrane. The composition may be soluble in water, preferably for intraveneous application, or insoluble for extracorporeal application.

Abstract: Novel 1,2,4-trioxanes which possess anti-malarial activity.

Abstract: This invention is directed to the analogs of viscosin, pharmaceutical compositions thereof and to their use as antibacterial, antiviral and antitrypanosomal therapeutic compounds.

Abstract: Bis(carboalkoxy-substituted m-phenylene)-32-crown-10 compounds, useful as polymerizable monomers, can be formed in one step by reacting a functionalized dihydroxy aromatic compound with a dihalopolyether. In the same reaction, carboalkoxy-substituted m-phenylene-16-crown-5 is formed. Other mono- and di-functionalized bis(phenylene) crown ethers can be made by one step as well as multistep synthesis from similar starting materials.

Abstract: Novel fluorogenic ionophores have been synthesized which selectively bind ions such as potassium and sodium, even in neutral aqueous and alcoholic media and respond to such binding by fluorescence quenching or enhancement. These ionophores are ideal for the selective and direct determination of ions in biological or environmental samples and the like. The ionophores are also suitable for incorporation into fiber optic-based sensors for the continuous in vivo or in vitro monitoring of metal ions in blood or other biological fluids.

Abstract: New compounds are described of the formula: ##STR1## wherein Z is selected from ##STR2## each x is selected from ##STR3## n is an integer from 1-10; each Y is selected from hydrogen, --NH.sub.2, --COQ, --COOQ, --COONHQ, --COOH, --OH, W, halogen and Q; wherein each Q is independently selected from substituted and unsubstituted lower alkenyl and lower alkyl and wherein the substitutuents are selected from --NH.sub.2 halogen, --OH, and --COOH; D is selected from hydroxy, hydrogen and --NH.sub.2 ; and W is selected from ##STR4## wherein each R is independently selected from hydrogen and lower alkyl; R' is selected from ethylene, propylene, isopropylene and phenylene; M is selected from chlorine and hydroxy; A is selected from hydrogen, lower alkyl, lower alkenyl, cycloalkyl, and phenyl; (B) is selected from ##STR5## --CO--, --NHCO--, --O--, --COO--, --N.dbd.N--, or represents a confugate bond; L.sub.1 and L.sub.

Abstract: A series of tetrahydrofuran-containing, macrocyclic polyether compounds. The macrocycles have a 21-membered ring, incorporating six oxygen atoms, and they have a carboxy group (or a salt thereof) directed towards the interior of the ring. Administration of the compounds of the invention to ruminant animals (e.g. cattle and sheep) modifies their digestive fermentation processes such that the volatile fatty acids produced in the rumen contain a higher proportion of propionates rather than acetates, thereby increasing the efficiency of feed utilization in said ruminant animals. Additionally, the compounds of the invention show antibacterial activity in vitro against certain gram-positive microorganisms.

Abstract: A series of novel, macrocyclic polyether compounds. The macrocycles have a 21-membered ring, containing six oxygen atoms, and they have a carboxy group (or a salt thereof) directed towards the interior of the ring. Administration of the compounds of the invention to ruminant animals (e.g. cattle and sheep) modifies their digestive fermentation processes such that the volatile fatty acids produced in the rumen contain a higher proportion of propionates rather than acetates, thereby increasing the efficiency of feed utilization in said ruminant animals. Additionally, the compounds of the invention show antibacterial activity in vitro against certain gram-positive microorganisms.

Abstract: The invention relates to new crown ether derivatives of the general Formula I ##STR1## and a process for the preparation thereof wherein Z.sup.1 is a group of the general Formula ##STR2## R.sub.a and R.sub.b may be the same or different and R.sub.a represents an alkyl group having 1-4 carbon atoms and R.sub.b is an alkyl group having 1-20 carbon atoms.The new crown ethers are useful in the preparation of ion-selective electrodes having a long lifetime.

Abstract: A compound of the formula: ##STR1## useful as a fungicidal agent against phytopathogenic fungi, particularly strains thereof which are resistant to benzimidazole or thiophanate fungicides and/or cyclic imide fungicides.

Abstract: The present invention relates to polyacrylic ester polymers having pendant macrocyclic ethers as well as electrically-conducting compositions comprised thereof.

Abstract: New crown ether derivatives of formula (I) ##STR1## wherein R stands for hydrogen or C.sub.1-4 alkyln stands for 1,2,X stands for oxygen, sulphur or a NH-groupY represents hydrogen or nitroZ represents a chemical bond, --CH.sub.2 --, --(CH.sub.2).sub.2-4 --, --CH.sub.2 OCH.sub.2 --, --CH.sub.2 SCH.sub.2 --, ##STR2## or a group of the formula ##STR3## suitable for forming cation complexes, process for the preparation thereof and alkali or alkali earth metal ion-selective membrane electrodes containing said compounds are described.

Abstract: A photopolymerizable coating composition comprising(1) a nongaseous, ethylenically unsaturated, polymerizable compound,(2) a specified acidic o-nitroaromatic compound, and(3) an organic, radiation-sensitive, free-radical generating system which is useful for making a positive or negative polymeric image on a substrate.

Abstract: There is disclosed a process for the reductive alkylation of aromatic nitro-containing compounds with ketones or aldehydes wherein the improvement is characterized in that a specific polymer bound co-catalyst system is utilized. More specifically, a polymer bound anthranilic acid palladium complex is used in conjunction with a bound sulfonic acid resin as a catalyst system in a reaction to produce compounds such as N-phenyl-N'-alkyl-p-phenylenediamine.

Abstract: A method and reagent for the selective nitration of aromatic hydrocarbons which comprises contacting a complex of at least a catalytic amount of a polyether with a nitronium containing substance, e.g., NO.sub.2 BF.sub.4 with an aromatic hydrocarbon, e.g., toluene with at least one replaceable hydrogen. Nitration of toluene with these complexes at ambient temperature resulted in a reduction in meta substitution. In competitive studies, soluble crown ether complexes of NO.sub.2 BF.sub.4 in CH.sub.2 Cl.sub.2 nitrated toluene 45-59 times faster than they nitrated benzene.

Abstract: This invention provides a convenient and commercially adaptable process for the preparation of vinylcyclopropane derivatives in high yield. For the process an alkylating agent and activated methylene compound are reacted in the presence of a cyclic polyether compound and alkali metal compound. Water can also be present and/or the reaction may be carried out in an inert organic diluent.