子分类：
| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 201 | Deuterated 3-piperidinopropiophenone and medicaments containing said compounds | US10476743 | 2004-05-07 | US20040186136A1 | 2004-09-23 | Rudolf-Gisbert Alken; Thomas Stabingis |
| The invention discloses deuterated 3-piperidinopropiophenones as well as their physiologically tolerated salts. Furthermore, the invention concerns the use of deuterated 3-piperidinopropiophenones for the treatment of muscular illnesses as well as for the preparation of pharmaceutical drugs for the treatment of muscular illnesses. In addition, the invention discloses pharmaceutical formulations containing deuterated 3-piperidinopropiophenones as well as their physiologically tolerated salts for the treatment of muscular illnesses in addition to containing pharmaceutically tolerated adjuvants and/or additives. | ||||||
| 202 | Method for labeling with tritium | US10296711 | 2002-11-27 | US20030194748A1 | 2003-10-16 | Tohru Nagasaki |
| The present invention provides a tritium-labeling method which allows the introduction of tritium at the last stage of preparation and thus the preparation of the tritium-labeled compound having a high specific radioactivity, and said compound prepared by the method. | ||||||
| 203 | Benzamide compounds for cancer imaging and therapy | US468907 | 1995-06-06 | US5993777A | 1999-11-30 | Christy S. John; Jesse Baumgold; John G. McAfee; Terry Moody; Wayne Bowen |
| The present invention relates to a class of compounds having affinity for certain cancer cells, e.g. lung carcinomas, colon carcinomas, renal carcinomas, prostate carcinomas, breast carcinomas, malignant melanomas, gliomas, neuroblastomas and pheochromocytomas. The compounds of the present invention can also bind with high specificity to cell surface sigma receptors and can therefore be used for diagnostic imaging of any tissue having an abundance of cells with sigma receptors. The present invention provides such compounds as agents for diagnostic imaging and for detecting and treating tumors containing the cancer cells described above. | ||||||
| 204 | Radiolabelled amino acid formulations stored in an unfrozen state | US872059 | 1997-06-10 | US5922301A | 1999-07-13 | Roger Malcolm Price; Christopher Charles May; Elizabeth Margaret Buckley; Timothy Stone |
| Additives are proposed for compositions comprising radiolabelled organic compounds e.g. 32P-labelled nucleotides. Stabilisers are selected from tryptophan, para-aminobenzoate, indoleacetate and the azole group. Dyes are selected from Sulphorhodamine B, Xylene Cyanol, Azocarmine B and New Coccine. Preferred compositions contain both stabiliser and dye. | ||||||
| 205 | Methods for cancer imaging and therapy using benzamine compounds | US426366 | 1995-04-21 | US5911970A | 1999-06-15 | Christy S. John; Jesse Baumgold; John G. McAfee; Terry Moody; Wayne Bowen |
| The present invention relates to a class of compounds having affinity for certain cancer cells, e.g. lung carcinomas, colon carcinomas, renal carcinomas, prostate carcinomas, breast carcinomas, malignant melanomas, gliomas, neuroblastomas and pheochromocytomas. The compounds of the present invention can also bind with high specificity to cell surface sigma receptors and can therefore be used for diagnostic imaging of any tissue having an abundance of cells with sigma receptors. The present invention provides such compounds as agents for diagnostic imaging and for detecting and treating tumors containing the cancer cells described above. | ||||||
| 206 | Quinuclidine derivatives | US821500 | 1997-03-21 | US5854256A | 1998-12-29 | John Adams Lowe, III |
| Quinuclidine derivatives of the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein m, P, Z, Y, R.sup.1, R.sup.2 and R.sup.3 are as defined below. The compounds are substance P antagonists and, therefore, are useful in treating gastrointestinal disorders, central nervous system disorders, inflammatory diseases, pain and migraine. | ||||||
| 207 | Method for stabilizing radiolabeled organic compounds by adding a separate stabilizing compound | US763428 | 1996-12-11 | US5843396A | 1998-12-01 | Nadine Michele Loretta Gan; Gary Thomas Overmeyer; Douglas Roger Dennistoun Shaw |
| A stabilized composition comprising an organic compound labeled with a .beta.-emitting radionuclide and a stabilizing effective amount of a non-radiolabeled stabilizing compound selected from the group consisting of (i) heteroaryls having at least one nitrogen atom, said heteroaryl being substituted with at least one sulfur-containing moiety selected from the group consisting of thiol and thiocarbonyl provided that the nitrogen atoms are not adjacent to one another; (ii) aryls being substituted with at least one nitrogen-containing moiety selected from the group consisting of amino and isothiocyanate and with at least one sulfur-containing moiety selected from the group consisting of sulfonamide, sulfonate, and thiol; and (iii) alkylamines having at least one to four carbon atoms, said alkylamine being substituted with at least one sulfur-containing moiety selected from the group consisting of thioacid and thiocarbonyl provided that when the sulfur-containing moiety is a thioacid then the aminoalkyl contains only one nitrogen atom. | ||||||
| 208 | Quinuclidine derivatives | US821487 | 1997-03-21 | US5821248A | 1998-10-13 | John Adams Lowe, III |
| Quinuclidine derivatives of the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein m, P, Z, Y, R.sup.1, R.sup.2 and R.sup.3 are as defined below. The compounds are substance P antagonists and, therefore, are useful in treating gastrointestinal disorders, central nervous system disorders, inflammatory diseases, pain and migraine. | ||||||
| 209 | Process for the preparation of a deuterated compound | US754255 | 1996-11-20 | US5733984A | 1998-03-31 | Masaru Nakahara; Heiji Enomoto; Atsushi Kishita; Kenji Tsuda; Toshinari Tennoh; Emi Fujita |
| A process for the preparation of a deuterated compound, which requires neither many steps nor an expensive reagent, and is considerably economical and can be widely used for general-purposes because raw materials which can be used therein are not particularly limited. Specifically, a deuterated compound is obtained by a process comprising treating an organic compound (an aliphatic or alicyclic compound, an aromatic hydrocarbon or a polymer compound such as rubbers and proteins) in heavy water under high-temperature and high-pressure conditions not less than the subcritical temperature and the subcritical pressure. | ||||||
| 210 | Quinuclidine derivatives | US403967 | 1995-03-14 | US5698568A | 1997-12-16 | John Adams Lowe, III |
| Quinuclidine derivatives of the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein m, P, Z, Y, R.sup.1, R.sup.2 and R.sup.3 are as defined below. The compounds are substance P antagonists and, therefore, are useful in treating gastrointestinal disorders, central nervous system disorders, inflammatory diseases, pain and migraine. | ||||||
| 211 | Benzofuran derivatives | US220698 | 1994-03-31 | US5498722A | 1996-03-12 | Barry C. Ross; David Middlemiss; David I. C. Scopes; Torquil I. M. Jack; Kevin S. Cardwell; Michael D. Dowle; Duncan B. Judd; Stephen P. Watson |
| The invention provides compounds of formula (I): ##STR1## or a physiologically acceptable salt, solvate or metabolically labile ester thereof wherein the R groups are defined in the specification.The compounds may be used in the treatment or prophylaxis of hypertension and diseases associated with cognitive disorders. | ||||||
| 212 | Benzofuran derivatives | US883378 | 1992-05-15 | US5332831A | 1994-07-26 | Michael D. Dowle; Duncan B. Judd |
| The invention provides compounds of formula (I): ##STR1## or a physiologically acceptable salt, solvate or metabolically labile ester thereof whereinAr represents the group ##STR2## wherein R.sup.3 represents an acidic group selected from --CO.sub.2 H, --NHSO.sub.2 CF.sub.3 or a C-linked tetrazolyl group;Het represents the group ##STR3## with all other undefined groups being defined in the specification. The compounds may be used in the treatment or prophylaxis of hypertension and diseases associated with cognitive disorders. | ||||||
| 213 | Deuterated analogs of 1,25-dihydroxycholecalciferol | US907983 | 1992-07-02 | US5247123A | 1993-09-21 | Enrico G. Baggiolini; Bernard M. Hennessy; Milan R. Uskokovic |
| The invention is directed to deuterated vitamin D analogs, and processes and intermediates for their preparation. The end products, that is the deuterated vitamin D analogs, are useful for the treatment osteoporosis and cutaneous inflammations such as psoriasis, and contact dermatitis. | ||||||
| 214 | Process for the production of deuterated acid or deuterated methacrylic acid | US522418 | 1990-05-07 | US5221768A | 1993-06-22 | Masaaki Kato; Tetsuya Uno; Masao Kobayashi; Naoto Osuga |
| In accordance with the present invention, there is provided a process for the production of deuterated acrylic acid or deuterated methacrylic acid comprising the exchange of hydrogens in acrylic acid or methacrylic acid with deuteriums in the presence of a catalyst. The deuterated acrylic or methacrylic acid is very useful as a starting material in the production of high quality optical plastic fibers. | ||||||
| 215 | Kit for preparation of rhenium therapeutic agents for bone cancer without purification | US673000 | 1991-03-21 | US5192526A | 1993-03-09 | David W. Pipes |
| The process of the present invention includes preparing a first aqueous solution of rhenium in the form of radioactive perrhenate, wherein the concentration of rhenium in said solution is within the range of about 5.times.10.sup.-6 M to about 2.times.10.sup.-3 M, and then reducing and complexing the radioactive perrhenate by mixing a second solution or lyophilized solid with the first solution. The second solution or lyophilized solid comprises a ligand which complexes with the radioactive perrhenate and a reductant wherein the reductant is present in the second solution at a concentration in the range of about 0.005M to about 0.020M and the ligand is present in the second solution at a concentration in the range of about 0.01M and about 0.15M. The pH of the resultant solution is within the range of about 1.5 to about 5.5. | ||||||
| 216 | Methods for tritium labeling | US505257 | 1990-04-05 | US5186868A | 1993-02-16 | Hendrik Andres; Hiromi Morimoto; Philip G. Williams |
| Reagents and processes for reductively introducing deuterium or tritium into organic molecules are described. The reagents are deuterium or tritium analogs of trialkyl boranes, borane or alkali metal aluminum hydrides. The process involves forming these reagents in situ from alkali metal tritides or deuterides. | ||||||
| 217 | Preparation of rhenium phosphonate therapeutic agents for bone cancer without purification | US346411 | 1989-05-02 | US5021235A | 1991-06-04 | David W. Pipes |
| The process of the present invention includes preparing a first aqueous solution of rhenium in the form of radioactive perrhenate, wherein the concentration of rhenium in said solution is within the range of about 5.times.10.sup.-6 M to about 2.times.10.sup.-3 M, and then reducing and complexing the radioactive perrhenate by mixing a second solution or lyophilized solid with the first solution. The second solution or lyophilized solid comprises a ligand which complexes with the radioactive perrhenate and a reductant wherein the reductant is present in the second solution at a concentration in the range of about 0.005M to about 0.020M and the ligand is present in the second solution at a concentration in the range of about 0.01M and about 0.15M. The pH of the resultant solution is within the range of about 1.5 to about 5.5. | ||||||
| 218 | Process for preparation of deuterated methylene chloride | US242354 | 1988-09-09 | US4967021A | 1990-10-30 | Cal Y. Meyers; Roch Chan-Yu-King |
| A process for the preparation of deuterated methylene chloride. The process comprises contacting methylene chloride with an aqueous phase containing deuteroxide ions in the presence of a phase-transfer catalyst. | ||||||
| 219 | Novel radioactive propyl 2-iodospiroperidol and processes for the preparation thereof | US128821 | 1987-12-04 | US4945162A | 1990-07-31 | Iwao Nakatsuka; Masami Okuno |
| A radioactive propyl 2-iodospiroperidol of the formula: ##STR1## wherein I* is a radioactive iodine atom. The radioactive compound has a high affinity for dopamine receptors and is very useful as a radioactive diagnostic agent and as a radiopharmaceutical. | ||||||
| 220 | Deuterated analogs of 1,25-dihydroxycholecalciferol | US96981 | 1987-09-14 | US4898855A | 1990-02-06 | Enrico G. Baggiolini; Bernard M. Hennessy; Milan R. Uskokovic |
| The invention is directed to deuterated vitamin D analogs, and processes and intermediates for their preparation. The end products, that is the deuterated vitamin D analogs, are useful for the treatment osteoporosis and cutaneous inflammations such as psoriasis, and contact dermatitis. | ||||||
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