414results about "Isotope introduction to organic compounds" patented technology

New microfluidic devices, useful for carrying out chemical reactions, are provided. The devices are adapted for on-chip solvent exchange, chemical processes requiring multiple chemical reactions, and rapid concentration of reagents.

The present application is generally directed to microfluidic devices and methods for the achievement and assessment of chemical and radiochemical purity of (microfluidic) radio-synthesis products. More particularly, the current application relates to systems for purification and analysis of radiochemical products yielded by microfluidic synthesis devices.

The present invention relates to processes and intermediates for preparing compounds useful as inhibitors of ATR kinase, such as aminopyrazine-isoxazole derivatives and related molecules. The present invention also relates to compounds useful as inhibitors of ATR protein kinase. The invention relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and solid forms of the compounds of this invention.

The compounds of this invention have formula I or II:

wherein the variables are as defined herein.

Tellurium (Te)-containing precursors, Te containing chalcogenide phase change materials are disclosed in the specification. A method of making Te containing chalcogenide phase change materials using ALD, CVD or cyclic CVD process is also disclosed in the specification in which at least one of the disclosed tellurium (Te)-containing precursors is introduced to the process.

Chemical syntheses and medical uses of novel inhibitors of the uptake of monoamine neurotransmitters and pharmaceutically acceptable salts and prodrugs thereof, for the treatment and/or management of psychotropic disorders, anxiety disorder, generalized anxiety disorder, depression, post-traumatic stress disorder, obsessive-compulsive disorder, panic disorder, hot flashes, senile dementia, migraine, hepatopulmonary syndrome, chronic pain, nociceptive pain, neuropathic pain, painful diabetic retinopathy, bipolar depression, obstructive sleep apnea, psychiatric disorders, premenstrual dysphoric disorder, social phobia, social anxiety disorder, urinary incontinence, anorexia, bulimia nervosa, obesity, ischemia, head injury, calcium overload in brain cells, drug dependence, attention deficit hyperactivity disorder, fibromyalgia, irritable bowel syndrome, and/or premature ejaculation are described.

In one aspect, the present invention provides a method for labeling a terminal olefin, the method comprising a step of treating a terminal olefin substrate having the structure:

with a labeled ethylene reagent in the presence of a suitable catalyst under suitable olefin metathesis reaction conditions to form a labeled terminal olefin having the structure:

wherein R^A and R^B are independently hydrogen, or an aliphatic, alicyclic, heteroaliphatic, heterocyclic, aryl or heteroaryl moiety, with the proviso that R^A and R^B are not each hydrogen, or R^A and R^B taken together with the carbon atom to which they are attached form an alicyclic or heterocyclic moiety; and * denotes the presence of an isotopic label on the terminal carbon atom.

Methods and compositions utilizing ether and alkyl phospholipid ether analog compounds for treating cancer and imaging, monitoring, and detecting cancer stem cells in humans.

Methods and apparatus enable radiosynthesis of radiolabeled compounds using electrochemical trapping and release. The trapping and release of radioactive isotopes all occur inside a microreactor, a vial or similar device, thus eliminating the need for azeotropic drying and several dead-end filling steps, as well as the necessity to move concentrated radioisotopes from one compartment of the chip to another. These and other features allow radioisotope enrichment to be carried out internally within a radiochemical synthesis chip, providing faster and more robust operation, as well as producing very high radiochemical labeling yields.

The present invention provides for a derivative of monoterpene or sesquiterpene, such as a perillyl alcohol derivative. For example, the perillyl alcohol derivative may be a perillyl alcohol carbamate. The perillyl alcohol derivative may be perillyl alcohol conjugated with a therapeutic agent such as a chemotherapeutic agent. The present invention also provides for a method of treating a disease such as cancer, comprising the step of delivering to a patient a therapeutically effective amount of a derivative of monoterpene (or sesquiterpene). The route of administration may vary, and can include, inhalation, intranasal, oral, transdermal, intravenous, subcutaneous or intramuscular injection.

The invention provides a diaminopyrimidine compound and a composition containing the same and discloses the diaminopyrimidine compound shown as in a formula (I) and a drug combination containing the compound or salt thereof acceptable in crystal form and pharmacy, hydrate or solvent complex, stereoisomer, pro-drug or isotope variant. The diaminopyrimidine compound and the composition containing the same have excellent inhibition effect on protein kinase and have better pharmacokinetic parameter characteristics, and drug concentration of the compound in animal bodies can be increased to improve drug efficacy and safety.

A method for producing a compound having a deuterated aromatic ring or heterocyclic ring according to the invention includes heating a compound having an aromatic ring or heterocyclic ring in the presence of heavy water, a transition metal and a metal which generates deuterium. As the metal which generates deuterium, at least one metal selected from the group consisting of aluminum, magnesium, zinc, iron, lead and tin is preferred. As the transition metal, at least one metal selected from the group consisting of platinum, palladium, ruthenium and rhodium is preferred. The heating is preferably carried out by microwave irradiation.

A carbon hydrogen structure (C: H) is one of the basic structures in the pharmaceutical chemistry structure and a formed C-H bond is the basic chemical bond. The invention discloses a preparation method and an application of deuterated drugs which can change the chemical bond energy and the hydrogen bond energy in the structure of pharmaceutical compound. The hydrogen atom (H) in pharmaceutical compound structure is substituted by the A deuterium atom (D) which is the isotope of hydrogen, therefore changing the molecular structure and the bond energy of the substituted pharmaceutical compound so as to form a new deuterated drug. The deuterated drugs can be used for pharmacokinetics research, can obviously enhance the disease-preventing or treating function of the drugs, and can reduce the toxic and side effect of the drugs.

The present invention relates to methods of eluting radionuclide-labeled or radionuclide-labeled compounds using solid phase extraction resins, devices for carrying out such methods and computer programs for controlling such devices. In particular, the method of the invention enables the automated synthesis of radionuclide-labeled compounds using anion-exchange resins or reversed-phase resins, and involves removing or eluting the anion-exchange resin-bound The step of radionuclide labeling (fluorine-18, etc.) or a radionuclide-labeled compound bound to a reversed-phase resin.

The present invention relates to an apparatus for synthesizing F-18 labeled radioactive pharmaceutical. The apparatus for synthesizing F-18 labeled radioactive pharmaceutical includes an F-18 radioactive isotope supplier, a reagent supplier, a polymer precursor cartridge, a first heating unit, a polymer compound cartridge, a synthesizing container, a second heating unit, a water liquid container, a transmitting gas supplier, a cleansing liquid supplier, a connection tube, a plurality of control valves, and a controller.

The invention relates to a method for preparing deuterated diphenyl urea. Specifically, the invention provides an intermediate N-(1, 1, 1-3 deuterated methyl) benzo succinimide which can be used for preparing a deuterated diphenyl urea compound and an application of the intermediate in the preparation of the deuterated diphenyl urea compound. The method can be used for conveniently preparing the intermediate with the high purity and various deuterated diphenyl urea compounds in high efficiency.

The invention provides a method for the synthesis of an 18F-labelled product comprising deprotected of a protected 18F-labelled compound using a deprotection agent comprising a weak acid and wherein neutralisation and buffering of the deprotected product are carried out by the addition of a neutralisation agent. The deprotected product is buffered in a pH range suitable for subsequent autoclaving and formulation into an injectable radiopharmaceutical.

The invention provides a small modular multifunctional automatic 18F labelling PET (positron emission tomography) drug synthesizer and relates to an automatic PET drug synthesizer. The small modular multifunctional automatic 18F labelling PET drug synthesizer comprises a single FDG (fluorodeoxyglucose) synthesis module or two FDG synthesis modules which are connected in series, namely a module FDG1 and a module FDG2, a PET drug product separating system and a control system, wherein the single FDG synthesis module or the two FDG synthesis modules which are connected in series are used for independently completing FDG synthesis or continuously completing double-batch FDG synthesis in a combined manner; the PET drug product separating system is connected with the single FDG synthesis module or a second module, namely the module FDG2, in the two FDG synthesis modules which are connected in series; and the control system is used for connecting and controlling the FDG synthesis module and the PET drug product separating system. The small modular multifunctional automatic PET drug synthesizer has the characteristics of ingenious structure, small size, simple mounting, friendly interface, simple operation, safety, stability, reliability, convenience in maintenance, powerful function and flexibility, is simple to mount and operate, and convenient to maintain, and the production requirement of 18F labelling PET drugs for the current market and scientific research can be met.

The invention relates to a synthesis method of a stable isotope-labeled beta receptor agonist type compound. The synthesis method comprises the following steps: (1) by taking stable isotope-labeled methanol as a raw material, reacting with acetone or stable isotope-labeled acetone, and ammonifying to obtain stable isotope-labeled tert-butylamine; and (2) by taking a bromoketone type compound as a precursor of the beta receptor agonist type compound, reacting with stable isotope-labeled tert-butylamine to prepare the stable isotope-labeled beta receptor agonist type compound. Compared with the prior art, the method for preparing the stable isotope-labeled beta receptor agonist, provided by the invention, is simple, safe and reliable, the chemical purity of the product after separation and purification is above 99.0%, the isotopic abundance is above 98.0% atom, and the product can fully meet the requirements of residual detection in the field of food safety.