专利号:US-7700654-B2 优先权日:2005-02-05 标 题:Isolation of N-butylbenzenesulfonamide, synthesis of benzenesulfonamide derivatives, and use of N-butylbenzenesulfonamide and benzenesulfonamide derivatives for treating benign prostatic hyperplasia and/or prostate carcinoma 发明人:HOFFMANN HANS-RAINER; MATUSCH RUDOLF; BANIAHMAD ARIA 权利人:LOHMANN THERAPIE SYST LTS 摘要:A process for isolating N-butylbenzenesulfonamide (NBBS) from biological material, the chemical synthesis of benzenesulfonamide derivatives, the use of NBBS and benzenesulfonamide derivatives for treating benign prostatic hyperplasia and/or prostate carcinoma, the production of medicaments for the treatment thereof, and the use of NBBS and benzenesulfonamide derivatives as a lead substance in the development of active substances for treating benign prostatic hyperplasia and/or prostate carcinoma are provided.
专利号:US-2012053350-A1 优先权日:2009-04-30 标题 :Preparation of alkyl esters of n-protected oxo-azacycloalkylcarboxylic acids 发明人:MANGION IAN; HUFFMAN MARK A; RUCK REBECCA T; LYNCH JOSEPH; CHUNG JOHN Y L; MARCUNE BENJAMIN 权利人:MANGION IAN; HUFFMAN MARK A; RUCK REBECCA T; LYNCH JOSEPH; CHUNG JOHN Y L; MARCUNE BENJAMIN 摘要:A process for the preparation of alkyl esters of N-protected oxo-azacycloalkylcarboxylic acids of Formula III: comprises contacting a ketosulfoxonium ylide of Formula II: with an iridium catalyst to obtain Compound III, wherein P G1 is an amine protective group; k is 0, 1, or 2; and R U , R 1 , R 2 , and R 3 are defined herein. An embodiment of the process further com rises contacting a compound of Formula I: with a sulfoxonium halide of formula (R U ) 3 S(O)Z, wherein Z is halide, in the presence of a strong base to obtain Compound II. Additional embodiments add a series of process steps leading to the synthesis of 7-oxo-1,6-diazabicyclo[3.2.1]octanes suitable for use as β-lactamase inhibitors.
专利号:US-8710261-B2 优先权日:2005-02-22 标 题:5-phenyl-pentanoic acid derivatives as matrix metalloproteinase inhibitors for the treatment of asthma and other diseases 发明人:PALLE VENKATA P; SATTIGERI VISWAJANANI JITENDRA; KHERA MANOJ KUMAR; VOLETI SREEDHARA RAO; RAY ABHIJIT; DASTIDAR SUNANDA G 权利人:PALLE VENKATA P; SATTIGERI VISWAJANANI JITENDRA; KHERA MANOJ KUMAR; VOLETI SREEDHARA RAO; RAY ABHIJIT; DASTIDAR SUNANDA G; RANBAXY LAB LTD 摘要:The present invention relates to Compounds having the structure of Formula I: wherein n is an integer from 1 to 5; R 1 is optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocyclyl, heteroaryl, aralkyl, alkoxy, aryloxy, alkenyloxy or alkynyloxy; R 2 is alkenyl, allcynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, NR 4 R 5 , —NHC(â•?Y)R 4 , —NHC(â•?Y)NR 5 R χ , —NHC(â•?O)OR 4 , —NHSO 2 R 4 , C(â•?Y)NR 4 R 5 , C(â•?O)OR 6 [wherein Y is oxygen or sulphur], OR 5 , —O(Câ•?O)NR 4 R 5 , O-acyl, S(O) m R 4 , —SO 2 N(R 4 ) 2 , cyano, amidino or guanidino [wherein R 4 is alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocyclyl, heteroaryl, aralkyl, heteroarylalkyl, heterocyclylalkyl or cycloalkylalkyl and m is an integer 0-2; R 5 is hydrogen or R 4 ; R x is R 4 or —SO 2 N(R 4 ) 2 and R 6 is hydrogen, alkyl, cycloalkyl, aralkyl, heteroarylalkyl, heterocyclylalkyl or cycloalkylalkyl]; R 3 is hydrogen, fluorine, alkyl, cycloalkylalkyl or aralkyl; A is OH, OR 4 , —OC(â•?O)NR 4 R 5 , O-acyl, NH 2 , NR 4 R 5 , —NHC(â•?Y)R 4 , —NHC(â•?Y)NR 5 R x , —NHC(â•?O)OR 4 , —NHSO 2 R 4 , and to processes for the synthesis of the same. This invention also relates to pharmacological compositions containing the compounds of the present invention, and methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, renal diseases, tumor metastasis, and other inflammatory disorders characterize by over-expression and over-activation of an matrix metalloproteinase, using the compounds.
专利号:US-11485721-B2 优先权日:2017-11-21 标 题:Method for the metal-free preparation of a biaryl by a photosplicing reaction and their uses 发明人:KLOSS FLORIAN; NEUWIRTH TONI; HAENSCH VEIT; HERTWECK CHRISTIAN 权利人:LEIBNIZ INST FUER NATURSTOFF FORSCHUNG UND INFEKTIONSBIOLOGIE E V HANS KNOELL INST HKI; LEIBNIZ INST FUER NATURSTOFF FORSCHUNG UND INFEKTIONSBIOLOGIE E V HANS KNOELL INST 摘要:The present invention relates to a method for the metal-free preparation of a biaryl compound by a photosplicing reaction and its use in the preparation of chemical compounds, preferably of active ingredients e.g. in the fields of pharmaceuticals and agrochemicals. In particular, it refers to a method for the regiocontrolled preparation of a biaryl compound of formula (I): Ar—Ar′ by photochemically reacting a precursor compound of formula (II): Ar—L—Ar′ to form a biaryl compound of general formula: Ar—L—Ar′(II)→Ar—Ar′ (I) wherein Ar and Ar′, independently of each other, represent an unsubstituted or substituted C6-C20 aryl group or a heteroaryl group with 5-20 ring atoms selected from carbon, nitrogen, oxygen and sulfur, and L represents a group —X—Y—Z— as defined herein. The biaryl compounds are generally suitable as intermediates or key building blocks in a very broad spectrum of organic chemical syntheses and their respective utilities. Their use within the field of synthesis of active ingredients is an aspect of the invention, and their use in the preparation of pharmaceutically active ingredients is particularly preferred.
专利号:US-5081306-A 优先权日:1989-04-25 标题:Synthesis of dihalobenzene disulfone compounds 发明人:KNOX DAVID E 权利人:AMOCO CORP 摘要:A process for producing dihalobenzene disulfone compounds, comprising reacting, in the presence of aluminum trichloride n a halobenzene sulfonyl halide of the formula ##STR1## wherein X and Y are halogen which may be the same or different, with a compound of the formula n n H - Q - H n n wherein Q is a divalent radical containing benzenoid unsaturation and the hydrogens are replaceable under electrophilic Friedel-Crafts reaction conditions, n in a solvent consisting essentially of about 1 to about 25 volume %, based on the solvent volume, of nitromethane and, correspondingly, about 99 to about 75 volume %, of a polar aliphatic halohydrocarbon, the total solvent volume employed being sufficient to provide between about 0.5 and about 1.5 moles of nitromethane per mole of aluminum trichloride, n thereby producing a dihalobenzene disulfone compound of the formula ##STR2##
专利号:US-9574189-B2 优先权日:2005-12-01 标题:Enzymatic encoding methods for efficient synthesis of large libraries 发明人:FRANCH THOMAS; LUNDORF MIKKEL DYBRO; JACOBSEN SØREN NYBOE; OLSEN EVA KAMPMANN; ANDERSEN ANNE LEE; HOLTMANN ANETTE; HANSEN ANDERS HOLM; SØRENSEN ANDERS MALLING; GOLDBECH ANNE; DE LEON DAEN; KALDOR DITTE KIEVSMOSE; SLØK FRANK ABILDGAARD; HUSEMOEN GITTE NYSTRUP; DOLBERG JOHANNES; Jensen Kim Birkebæ; PEDERSEN LENE; NØRREGAARD-MADSEN MADS; GODSKESEN MICHAEL ANDERS; GLAD SANNE SCHRØDER; NEVE SØREN; THISTED THOMAS; KRONBORG TINE TITILOLA AKINLEMINU; SAMS CHRISTIAN KLARNER; FELDING JAKOB; FRESKGÃ…RD PER-OLA; GOULIAEV ALEX HAAHR; PEDERSEN HENRIK 权利人:FRANCH THOMAS; LUNDORF MIKKEL DYBRO; JACOBSEN SØREN NYBOE; OLSEN EVA KAMPMANN; ANDERSEN ANNE LEE; HOLTMANN ANETTE; HANSEN ANDERS HOLM; SØRENSEN ANDERS MALLING; GOLDBECH ANNE; DE LEON DAEN; KALDOR DITTE KIEVSMOSE; SLØK FRANK ABILDGAARD; HUSEMOEN GITTE NYSTRUP; DOLBERG JOHANNES; Jensen Kim Birkebæ; PEDERSEN LENE; NØRREGAARD-MADSEN MADS; GODSKESEN MICHAEL ANDERS; GLAD SANNE SCHRØDER; NEVE SØREN; THISTED THOMAS; KRONBORG TINE TITILOLA AKINLEMINU; SAMS CHRISTIAN KLARNER; FELDING JAKOB; FRESKGÃ…RD PER-OLA; GOULIAEV ALEX HAAHR; PEDERSEN HENRIK; NUEVOLUTION AS 摘要:Disclosed is a method for obtaining a bifunctional complex comprising a molecule linked to a single stranded identifier oligonucleotide, wherein a nascent bifunctional complex comprising a chemical reaction site and a priming site for enzymatic addition of a tag is a) reacted at the chemical reaction site with one or more reactants, and b) reacted enzymatically at the priming site with one or more tag(s) identifying the reactant(s).
摘要:Kawęcki, R., Science of Synthesis Knowledge Updates, (2018) 4, 296. 摘要:Kashemirov, B. A.; Błażewska, K.; Justyna, K.; Lyu, J.; McKenna, C. E., Science of Synthesis Knowledge Updates, (2021) 1, 414. 摘要:Zhang, M.; Su, W., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 3, 127. 摘要:Inamoto, K., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 2, 432. 摘要:Chen, P.; Liu, G., Science of Synthesis: Knowledge Updates, (2023) 1, 442.