4591 results about "Heteroatom" patented technology

This invention relates to a catalyst system for the production of polyolefins comprising:

(A) a Group IV B transition metal component represented by one of the two general formulae

wherein

(C₅H_5-y-xR_x) is a cylopentadienyl ring

(JR′_z-l-y) is a heteroatom ligand in which J is an element with a coordination number of three from Group V-A or an element with a coordination number of two rom Group VI-A of the Periodic Table of Elements,

each Q is independently, hydride, C₁—C₂₀ hydrocarbyl radicals, substituted hydrocarbyl radials wherein one or more hydrogen atoms is replaced by an electron withdrawing group, or C₁—C₂₀ hydrocarbyl-substituted metalloid radicals wherein the metalloid is selected from the group consisting of germanium and silicon, provided that Q is not a substituted or unsubstituted cyclopentadienyl ring, or both Q together may be an alkylidene, olefin, acetylene or a cyclometallated hydrocarbyl;

“y” is 0 or 1; when “y” is 1, T is a covalent bridging group containing a Group IV-A or V-A element;

L is a neutral Lewis base; and “w” is a number from 0 to 3;

(B) an activator compound comprising (1) a cation; and (2) a compatible noncoordinating anion.

A multi-stage catalytic hydrogenation and hydroconversion process for heavy hydrocarbon feed materials such as coal, heavy petroleum fractions, and plastic waste materials. In the process, the feedstock is reacted in a first-stage, back-mixed catalytic reactor with a highly dispersed iron-based catalyst having a powder, gel or liquid form. The reactor effluent is pressure-reduced, vapors and light distillate fractions are removed overhead, and the heavier liquid fraction is fed to a second stage back-mixed catalytic reactor. The first and second stage catalytic reactors are operated at 700-850.degree. F. temperature, 1000-3500 psig hydrogen partial pressure and 20-80 lb./hr per ft.sup.3 reactor space velocity. The vapor and light distillates liquid fractions removed from both the first and second stage reactor effluent streams are combined and passed to an in-line, fixed-bed catalytic hydrotreater for heteroatom removal and for producing high quality naphtha and mid-distillate or a full-range distillate product. The remaining separator bottoms liquid fractions are distilled at successive atmospheric and vacuum pressures, low and intermediate-boiling hydrocarbon liquid products are withdrawn, and heavier distillate fractions are recycled and further upgraded to provide additional low-boiling hydrocarbon liquid products. This catalytic multistage hydrogenation process provides improved flexibility for hydroprocessing the various carbonaceous feedstocks and adjusting to desired product structures and for improved economy of operations.

The invention describes a vitamin receptor binding drug delivery conjugate, and preparations therefor. The drug delivery conjugate consists of a vitamin receptor binding moiety, a bivalent linker (L), and a drug. The vitamin receptor binding moiety includes vitamins, and vitamin receptor binding analogs and derivatives thereof, and the drug includes analogs and derivatives thereof. The vitamin receptor binding moiety is covalently linked to the bivalent linker, and the drug, or the analog or the derivative thereof, is covalently linked to the bivalent linker, wherein the bivalent linker (L) includes components such as spacer linkers, releasable linkers, and heteroatom linkers, and combinations thereof. Methods and pharmaceutical compositions for eliminating pathogenic cell populations using the drug delivery conjugate are also described.

Melanocortin receptor-specific compounds of the general formulas

and pharmaceutically acceptable salts thereof, where J is a substituted or unsubstituted monocyclic or bicyclic ring structure, L is a linker, W is a heteroatom unit with at least one cationic center, hydrogen bond donor or hydrogen bond acceptor, Q includes a substituted or unsubstituted aromatic carbocyclic ring, R₆, R₇, y and z are as defined in the specification, and the carbon atom marked with an asterisk can have any stereochemical configuration, and optionally with one or two additional ring substituents as defined, which compounds bind to one or more melanocortin receptors and are optionally an agonist, a partial agonist, an antagonist, an inverse agonist or an antagonist of an inverse agonist, and may be employed for treatment of one or more melanocortin receptor-associated conditions or disorders, and methods for the use of the compounds of the invention.

This invention describes novel pyrazole compounds of formula IV:

wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; R^x and R^y are independently selected from T-R³, or taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5-8 membered ring having 1-3 ring heteroatoms selected from oxygen, sulfur, or nitrogen; and R², R^2′, T, and R³ are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.

A compound of formula (I) and salts and solvates thereof, in which: R0 represents hydrogen, halogen, or C1-6alkyl; R1 represents hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, haloC1-6alkyl, C3-8cycloalkyl, C3-8cycloalkylC1-3alkyl, arylC1-3alkyl, or heteroarylC1-3alkyl; R2 represents an optionally substituted monocyclic aromatic ring selected from benzene, thiophene, furan, and pyridine, or an optionally substituted bicyclic ring (a) attached to the rest of the molecule via one of the benzene ring carbon atoms, and wherein the fused ring (A) is a 5- or 6-membered ring which may be saturated or partially or fully unsaturated, and comprises carbon atoms and optionally one or two heteroatoms selected from oxygen, sulphur, and nitrogen; and R3 represents hydrogen or C1-3alkyl, or R1 and R3 together represent a 3- or 4-membered alkyl or alkenyl chain. A compound of formula (I) is a potent and selective inhibitor of cyclic guanosine 3',5'-monophosphate specific phosphodiesterase (cGMP specific PDE) having a utility in a variety of therapeutic areas where such inhibition is beneficial, including the treatment of cardiovascular disorders and erectile dysfunction.

Compounds of Formula (Ia)

wherein R is a C₆-C₁₂ substituted or unsubstituted aryl, a C₆-C₁₂ substituted or unsubstituted heteroaryl, a C₁-C₆ substituted or unsubstituted alkyl or —NR′R′,

• Q is C(O), O, NR′, S, S(O)₂, C(O)₂ (CH2)p
• Y is C(O), O, NR′, S, S(O)₂, C(O)₂ (CH2)_p
• Z is H or C₁-C₄ alkyl,
• R′ is H, C(O), S(O)₂, C(O)₂, a C₆-C₁₂ substituted or unsubstituted aryl, a C₆-C₁₂ substituted or unsubstituted heteroaryl or a C₁-C₆ substituted or unsubstituted alkyl, when substituted, aryl, heteroaryl and alkyl are substituted with halogen, C₆-C₁₂ heteroaryl, —NR′R′ or COOZ, which have diagnostic and therapeutic properties, such as the treatment and management of prostate cancer and other diseases related to NAALADase inhibition. Radiolabels can be incorporated into the structure through a variety of prosthetic groups attached at the X amino acid side chain via a carbon or hetero atom linkage.

Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include at least three peptide units, an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.

The present invention provides a solid catalyst component for the polymerization of olefins, comprising magnesium, titanium, a halogen and an electron donor, wherein said electron donor comprises at least one selected from the group consisting of polyol ester compounds of the formula (I): R₁CO—O—CR₃R₄-A-CR₅R₆—O—CO—R₂ (I) wherein, R₁ and R₂ groups, which may be identical or different, can be substituted or unsubstituted hydrocarbyl having 1 to 20 carbon atoms, R₃-R₆ groups, which may be identical or different, can be selected from the group consisting of hydrogen, halogen or substituted or unsubstituted hydrocarbyl having 1 to 20 carbon atoms, R₁-R₆ groups optionally contain one or more hetero-atoms replacing carbon, hydrogen atom or the both, said hetero-atom is selected from the group consisting of nitrogen, oxygen, sulfur, silicon, phosphorus and halogen atom, two or more of R₃-R₆ groups can be linked to form saturated or unsaturated monocyclic or polycyclic ring; A is a single bond or bivalent linking group with chain length between two free radicals being 1-10 atoms, wherein said bivalent linking group is selected from the group consisting of aliphatic, alicyclic and aromatic bivalent radicals, and can carry C₁-C₂₀ linear or branched substituents; one or more of carbon atom and/or hydrogen atom on above-mentioned bivalent linking group and substituents can be replaced by a hetero-atom selected from the group consisting of nitrogen, oxygen, sulfur, silicon, phosphorus, and halogen atom, and two or more said substituents on the linking group as well as above-mentioned R₃-R₆ groups can be linked to form saturated or unsaturated monocyclic or polycyclic ring.

The present invention is in the area of novel compounds and salts thereof, their syntheses, and their use as anti-cancer agents. The compounds include compounds of Formula I:

and solvates, hydrates and pharmaceutically-acceptable salts thereof, wherein A¹ is N or CR¹; A³ is N or CR³; A⁵ is N or CR⁵; R¹, R³-R⁶ and L are defined in the specification; n is 0 or 1; and X is an optionally-substituted aryl group having 6-10 carbons in the ring portion, an optionally-substituted 6-membered heteroaryl group having 1-3 nitrogen atoms in the ring portion, an optionally-substituted 5-membered heteroaryl group having 0-4 nitrogen atoms in the ring portion and optionally having 1 sulfur atom or 1 oxygen atom in the ring portion, or an optionally-substituted heteroaryl group in which a 6-membered ring is fused either to a 5-membered ring or to a 6-membered ring, wherein in each case 1, 2, 3 or 4 ring atoms are heteroatoms independently selected from nitrogen, oxygen and sulfur. They are effective against a broad range of cancers, especially leukemia, prostate, non-small cell lung and colon. They are additionally useful in the treatment of proliferative retinopathies such as diabetic neuropathy and macular degeneration.

Nucleoside phosphinoamidite carboxylates and analogs are provided that have the structure of formula (III)

wherein A is hydrogen, hydroxyl, lower alkoxy, lower alkoxy-substituted lower alkoxy, halogen, SH, NH₂, azide or DL wherein D is O, S or NH and L is a heteroatom-protecting group, unsubstituted hydrocarbyl, substituted hydrocarbyl, heteroatom-containing hydrocarbyl, or substituted heteroatom-containing hydrocarbyl; B is a nucleobase; and one of R¹¹ and R¹² is a blocking group and the other is (IV) or (VI)

in which W, X, Y, Z, R¹ and n are as defined herein.

This invention relates to in-situ preparation of the derivatives of various hydroxy acids (HA), such as alpha-(Alpha) Hydroxy Acids (AHA), beta-(Beta) Hydroxy Acids (BHA), and Poly-Hydroxy Acids (PHA) with certain skin beneficial organic hetero-atom bases and their application in skin resurfacing (exfoliation), and in the synergistic treatment and regulation of topical disorders of skin such as skin aging, wrinkles, acne, rosacea, age-spots, canker sores, striae distensae (stretch marks), pimples, skin redness, and dry skin conditions of cracking, flaking, and scaling. Most HA derivatives produced by the in-situ method do not cause skin irritation and skin redness effects that are commonly experienced with AHA and BHA, yet there is no loss of their skin beneficial effects. These compositions can be traditional water and oil emulsions, liposomes, suspensions, colloids, solutions, masks, muds, serums, sprays, gels, lotions, creams, cleansers, and anhydrous systems, thus offering a wide choice of formulations to meet their consumer appeal and acceptance requirements.

The present invention is directed to branched reactive water-soluble polymers comprising at least two polymer arms, such as poly(ethylene glycol), attached to a central aliphatic hydrocarbon core molecule through heteroatom linkages. The branched polymers bear at least one functional group for reacting with a biologically active agent to form a biologically active conjugate. The functional group of the branched polymer can be directly attached to the aliphatic hydrocarbon core or via an intervening linkage, such as a heteroatom, -alkylene-, —O-alkylene-O—, -alkylene-O-alkylene-, -aryl-O—, —O-aryl-, (—O-alkylene-)_m, or (-alkylene-O—)_m linkage, wherein m is 1–10.

The invention relates to polymers with antimicrobial properties, consisting of: a) 99-40 wt % non functional vinylically polymerizable monomers and b) 1-60 wt % functional vinylically polymerizable monomers of general formula (I) wherein V=vinyl, (meth)acroyl, allyl or styryl, A=a possibly available linking unit, which can be alkyl, aryl, arylalkyl or hydroxy alkyl, which can also be interrupted by hetero atoms, e.g. by hetero atoms in urethane, carbonate, ester, amide or ether groups, wherein y=0 or is 1, Hsp=a hydrophilic spacer of general formula (i) -(O-CH2-CH2)r- and/or (ii) -(O-CH2-CH(CH3))s with r=0-40, s=0-40 and r+s=2-40, also m=1.2 or 3 and R1=CH3, ethyl or benzyl, R2=an alkyl radical with 8-20 C-atoms, wherein t=1, 2 or 3 and X-=Cl-, Br-, I- or alkyl sulphate.

The present invention provides compounds of formula (I),

wherein:

• • R₁ is unsubstituted C₁-C₆ alkyl;
  • L_a is substituted or unsubstituted C₁-C₆ alkyl linker, substituted or unsubstituted C₃-C₁₀ carbocycle, substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S, or substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S; and
  • R₂ and R₃ are each, independently, H, substituted or unsubstituted C₁-C₆ alkyl, or substituted or unsubstituted C₆-C₁₀ aryl;
  • or alternatively, R₂ and R₃, together with the nitrogen atom to which they are attached, form a substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S or a substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S.

The invention also provides pharmaceutical compositions and methods for treating neurological diseases, such as multiple sclerosis.

Photoacid generators generate sulfonic acids of formula (1a) or (1b) upon exposure to high-energy radiation.

R¹—COOCH₂CF₂SO₃⁻H⁺  (1a)

R¹—O—COOCH₂CF₂SO₃⁻H⁺  (1b)

R¹ is a monovalent C₂₀-C₅₀ hydrocarbon group of steroid structure which may contain a heteroatom. The bulky steroid structure ensures adequate control of acid diffusion. The photoacid generators are compatible with resins and suited for use in chemically amplified resist compositions.

Vitamin D compounds of formula (I) with a label attached to a spacer group in the 3 position are disclosed.In the above formula (I), X is an optionally substituted hydrocarbon group with a length of 0.8-4.2 nm, optionally containing the heteroatoms S, O, N or P; Y is H or OH; A is a label capable of binding with high affinity to a protein; R is an optionally substituted hydrocarbon side chain of a D vitamin or a D vitamin metabolite. Also disclosed is the preparation of formula (I).

One aspect of the present invention relates to novel ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in transition metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The subject methods provide improvements in many features of the transition metal-catalyzed reactions, including the range of suitable substrates, reaction conditions, and efficiency.

The present invention is directed to the preparation of photoresist polymers via living free radical polymerization techniques. Sterically bulky ester monomers are utilized as the polymerization components. Use of chain transfer agents is included in polymerization processing conditions. Cleavage of polymer terminal end groups that include a heteroatom are described.

A composition suitable for tantalum chemical-mechanical polishing (CMP) comprises an abrasive, an organic oxidizer, and a liquid carrier therefor. The organic oxidizer has a standard redox potential (E⁰) of not more than about 0.5 V relative to a standard hydrogen electrode. The oxidized form comprises at least one pi-conjugated ring, which includes at least one heteroatom directly attached to the ring. The heteroatom can be a N, O, S or a combination thereof. In a method embodiment, a CMP composition comprising an abrasive, and organic oxidizer having an E⁰ of not more than about 0.7 V relative to a standard hydrogen electrode, and a liquid carrier therefor, is utilized to polish a tantalum-containing surface of a substrate, by abrading the surface of the substrate with the composition, preferably with the aid of a polishing pad.