首页 / 专利分类库 / 有机化学 / 杂环化合物 / 杂环化合物,含大于七元环的、有1个氮原子作为惟一的杂环原子
序号 专利名 申请号 申请日 公开(公告)号 公开(公告)日 发明人
121 HEME CHOLINE ESTERS AND USES THEREOF US11958671 2007-12-18 US20090155829A1 2009-06-18 Thomas Pirrie Treynor; Anup Sood; Sean Richard Dinn
Methods of activating an apo-peroxidase are provided. The methods include the steps of providing a solution comprising an apo-peroxidase and a heme choline ester, hydrolyzing the heme choline ester with a choline esterase, and converting the apo-peroxidase to active peroxidase. The methods disclosed herein also provide for detecting the presence of an analyte in a sample. The methods include providing a binder capable of specifically binding the analyte wherein the binder is attached to a solid surface, applying the sample to the solid surface under conditions that permit binder-analyte binding, adding a choline esterase-conjugated binder that binds to the analyte, adding an apo-peroxidase, a heme choline ester, a peroxide, and a peroxide-activated signal generator, and detecting the signal produced by the peroxide-activated signal generator. An associated kit and components are also provided.
122 Phenylpiperazine cycloalkanol derivatives and methods of their use US10963458 2004-10-12 US07531543B2 2009-05-12 Paige Erin Mahaney; Eugene John Trybulski; Lori Krim Gavrin; An Thien Vu
The present invention is directed to phenylpiperazine cycloalkanol derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.
123 Cycloalkylamine derivatives as NK-1/SSRI antagonists US11183699 2005-07-18 US07494986B2 2009-02-24 Yong-Jin Wu; Huan He
The present disclosure relates to chemical compounds and their use in human therapy. A specific embodiment relates to compounds of Formula (I) or an isomer, a pharmaceutically acceptable salt or solvate thereof and pharmaceutically acceptable formulations comprising said compounds useful for the treatment or prevention of conditions mediated by tachykinins and/or selective inhibition of serotonin reuptake transporter protein. The compounds act as dual NK-1 antagonists and selective serotonin reuptake inhibitors.
124 Beta-Substituted Porphyrins US11576690 2005-10-10 US20080283122A1 2008-11-20 Wayne Mason Campbell; David Leslie Officer; Michael Graetzel; Md. Khaja Nazeeruddin
The invention relates to ÿ-substituted porphyrins, methods for their synthesis, and their use in the preparation of photoelectric materials. In particular, the invention relates to solid state photoelectric devices, including solar cells and photodetectors, incorporating these photoelectric materials, with improved photon-to-current conversion efficiencies.
125 Glycosylated Carboranylporphyrins and Uses Thereof US11746957 2007-05-10 US20080279781A1 2008-11-13 Michiko Miura; Haitao Wu
The present invention is directed to low toxicity boronated compounds and methods for their use in the treatment, visualization, and diagnosis of tumors. More specifically, the present invention is directed to low toxicity glycosylated carborane-containing 5,10,15,20-tetraphenylporphyrin compounds and methods for their use particularly in boron neutron capture therapy (BNCT) and photodynamic therapy (PDT) for the treatment of tumors of the brain, and head and neck. The invention is also directed to using these glycosylated carborane-containing tetraphenylporphyrin compounds in methods of tumor imaging and/or diagnosis such as MRI, SPECT, or PET.
126 Backbone-substituted bifunctional DOTA ligands, complexes and compositions thereof, and methods of using same US10525673 2003-09-05 US07368100B2 2008-05-06 Martin W. Brechbiel; Hyun-Soon Chong
Backbone-substituted 1,4,7,10-tetraaza cyclododecane-N,N′,N″,N′″-tetraacetic acid compounds, metal complexes thereof, compositions thereof, conjugates thereof, and methods of use in diagnostic imaging and treatment of a cellular disorder.
127 Preparation of metallotexaphyrins US10537379 2003-11-24 US20070287829A1 2007-12-13 Douglas Cary; Lei Fu; Tarak Mody
The present invention provides a process for replacing a metal cation, M1, from a compound of Formula L
128 Contrast Agents for Magnetic Resonance Imaging US11547088 2005-03-31 US20070218010A1 2007-09-20 Jens Hasserodt
The invention relates to contrast agents for magnetic resonance imaging comprising a chelating ligand and a transition metal ion, said ligand carrying a substituent capable of reacting chemically or biochemically with a target substance while bringing about a change in the spin state.
129 Light-harvesting discotic liquid crystalline porphyrins and metal complexes US11638163 2006-12-13 US20070152189A1 2007-07-05 Quan Li; Xiaoli Zhou
Novel discotic liquid crystalline porphyrins and discotic liquid crystalline metal complexes, methods for their preparation, and device fabrication are disclosed. Materials with partially perfluorinated alkyl group in the peripheral chains show a strong tendency towards the formation of homeotropic alignment. These compounds are capable of being used as high-efficiency photovoltaic materials, organic semiconducting materials, and organic light emitting materials.
130 Cascade polymer complexes, process for their production and pharmaceutical agents containing said complexes US10686717 2003-10-17 US07211241B2 2007-05-01 Heribert Schmitt-Willich; Johannes Platzek; Bernd Radüchel; Andreas Mühler; Thomas Frenzel
Described are new cascade polymer complexes, compositions containing them and use of the complexes in diagnosis and therapy, particularly for magnetic resonance imaging and computer tomography imaging.
131 Process for labeling a nucleic acid US09736151 2000-12-15 US06902891B2 2005-06-07 Ali Laayoun; Lionel Menou; Christelle Tora; Aloke R. Banerjee; Michael M. Becker; Kenneth A. Browne; Matthew C. Friedenberg; Fred F. Hajjar
A process of fragmenting and labeling a synthetic or natural nucleic acid, comprising the steps of providing a mixture containing a nucleic acid, a labeling agent containing a detectable label, and at least one multivalent metal cation in a substantially aqueous solution; chemically fragmenting the nucleic acid in the mixture to produce a multiplicity of nucleic acid fragments; and attaching at least one label to at least one of the nucleic acid fragments to produce a detectably labeled nucleic acid fragment.
132 Process for the preparation of an N-alkyl or N-aryl carbamoyl derivative US09815268 2001-03-23 US20020028932A1 2002-03-07 Jacobus A. Loontjens; Bartholomeus J.M. Plum
The invention relates to a process for the preparation of an N-alkyl or N-aryl carbamoyl derivative in which an amine is contacted with a carbonic acid derivative according to the general formula: 1 where fragments X in the form of XH are a lactam, oxime, imide or triazole. In particular the invention relates to the preparation of a blocked isocyanate according to a process in which no isocyanate is used. The invention also relates to the use of the N-alkyl or N-aryl carbamoyl derivative prepared according to the process according to the invention in a coating.
133 Process for the preparation of macrocyclic metalloprotease inhibitors US09919564 2001-07-31 US20020013459A1 2002-01-31 Roberta L. Dorow; Silvio Campagna; Pasquale N. Confalone; Fuqiang Jin; Zhe Wang
The present invention relates to processes for the preparation of macrocyclic molecules containing anti-succinate residues which inhibit metalloproteinases such as aggrecanase, and the production of tumor necrosis factor (TNF). The anti-succinates are formed by an Ireland Claisen rearrangement of a silyl ketene acetal which proceeds with high stereoselectivity.
134 Fungicidal trifluorophenyl-triazolopyrimidines US273151 1999-03-19 US6117865A 2000-09-12 Klaus-Juergen Pees
The novel compounds of formula I: ##STR1## (R.sup.1, R.sup.2 and Hal are defined in the specification) show selective fungicidal activity. The new compounds are processed with carriers and adjuvants to form fungicidal compositions.
135 Dichelants US898376 1997-07-22 US5972307A 1999-10-26 Joan Carvalho; Alan D. Watson; Jere D. Fellmann; Michael Koo
This invention relates to dichelants, in particular compounds having two macrocyclic chelant groups linked by a bridge containing an ester or amide bond, especially compounds of formula Vb ##STR1## (wherein each X which may be the same or different is NZ, O or S, at least two Xs being NZ;each Z is a group R.sup.1 or a group CR.sup.1.sub.2 Y, at least one Z, and preferably 2 or 3 Zs, on each macrocyclic ring being a group CR.sup.1.sub.2 Y;each Y is a group CO.sub.2 H, PO.sub.3 H, SO.sub.3 H, CONR.sup.1.sub.2, CON(OR.sup.1)R.sup.1, CNS or CONR.sup.1 NR.sup.1.sub.2, preferably COOH;m is 0 or 1 or 2, preferably 1; each n is 2 or 3, preferably 2; q is 1 or 2, preferably 1;each R.sup.1 which may be the same or different is a hydrogen atom or an alkyl group optionally substituted by one or more hydroxy and/or alkoxy groups;and D is a bridging group having a molecular weight of less than 1000, preferably less than 500, joining two macrocyclic rings via at least one amide or ester bond) and salts and metal chelates thereof.
136 Tricyclic benzazepine vasopressin antagonists US639014 1996-04-24 US5869483A 1999-02-09 Jay Donald Albright; Fuk-Wah Sum
Tricyclic compounds of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and processes for preparing such compounds.
137 Chelant moieties linked to an aryl moiety by an interrupted alkylene linker US727594 1997-01-17 US5798089A 1998-08-25 John Varadarajan; Alan David Watson; Arne Berg
The invention provides amphiphilic compounds of the formula (I) Ch--(--L--Ar--(--AH).sub.n).sub.m (where Ch is a hydrophilic chelant moiety or a salt or a chelate thereof); each L is an optionally oxo substituted C.sub.2-25 -alkylene linker wherein at least one CH.sub.2 moiety is replaced by a group X.sup.1 (e.g. L may include a chain sequence, an X.sup.1 (CH.sub.2 CH.sub.2 X.sup.1).sub.u (where u is a positive integer) such as X.sup.1 (CH.sub.2 CH.sub.2 X.sup.1).sub.u, CH.sub.2 X.sup.1 CH.sub.2 CH.sub.2 X.sup.1 CH.sub.2 CH.sub.2 X.sup.1, CH.sub.2 X.sup.1 CH.sub.2 CH.sub.2 X.sup.1 CH.sub.2 CH.sub.2 X.sup.1 CH.sub.2 CH.sub.2 X.sup.1, etc.), and wherein L is optionally interrupted by a metabolizable group M but with the provisos that the terminus of L adjacent Ch is CH.sub.2 and that the terminus of L adjacent Ar is X.sup.1 or a CH.sub.2 group adjacent or separated by one CH.sub.2 from a group X.sup.1 (thus, for example the L--Ar linkage may be L.sup.1 --X.sup.1 --Ar, L.sup.1 --CH.sub.2 --Ar, L.sup.1 --X.sup.1 CH.sub.2 --Ar or L.sup.1 --X.sup.1 CH.sub.2 CH.sub.2 --Ar, where L.sup.1 is the residue of L; each Ar is an aryl ring optionally substituted by or having fused thereto a further aryl ring; each AH is a protic acid group, preferably an oxyacid, e.g. a carbon, sulphur or phosphorus oxyacid or a salt thereof; each X.sup.1 is O, S, NR.sup.1 or PR.sup.1, preferably no more than 3 X.sup.1 groups being present in L; each R.sup.1 is hydrogen, alkyl or aryl; and m and n are positive integers, m being for example 1 to 4, especially 1 or 2 and n being for example, 1, 2 or 3) which are especially suited for use in diagnostic imaging of the hepatobiliary system.
138 Macrocyclic complexing agents and targeting immunoreagents useful in therapeutic and diagnostic compositions and methods US392614 1995-02-22 US5760191A 1998-06-02 Robert A. Snow; Daniel J. Delecki; Chandra R. Shah
A metal chelate comprising a compound having the following formula and one or more metal ions which metal ions are a radionucleotide or a paramagnetic metal ion: ##STR1##
139 Tricyclic benzazepine vasopressin antagonists US662546 1996-06-13 US5693635A 1997-12-02 Jay Donald Albright; Marvin Fred Reich
Tricyclic compounds of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and processes for preparing such compounds.
140 Pyridobenzoxazepine and pyridobenzothiazepine vasopressin antagonists US637908 1996-04-25 US5686445A 1997-11-11 Jay Donald Albright; Xuemei Du
Tricyclic compounds of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and processes for preparing such compounds.
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