| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 101 | Heterocyclic compounds | US067642 | 1993-05-25 | US5461167A | 1995-10-24 | Kozo Shiokawa; Shinichi Tsuboi; Shinzo Kagabu; Koichi Moriya |
| Novel insecticides of the formula ##STR1## in which n is 0 or 1,X is S, O, ##STR2## Y is N or ##STR3## Z is a 5- or 6-membered nitrogen-containing heterocyclic ring, and R to R.sup.9 variously represent hydrogen or specified organic radicals. | ||||||
| 102 | Heterocyclic compounds | US832174 | 1992-02-06 | US5298507A | 1994-03-29 | Kozo Shiokawa; Shinichi Tsuboi; Shinzo Kagabu; Koichi Moriya |
| Novel insecticides of the formula ##STR1## in which n is 1,X is ##STR2## Y is N or ##STR3## Z is a 5- or 6-membered nitrogen-containing heterocyclic ring, and R to R.sup.9 variously represent hydrogen or specified organic radicals. | ||||||
| 103 | Novel 4-cyanophenyl derivatives with action against cardiac arrhythmia | US289630 | 1988-12-22 | US5034411A | 1991-07-23 | Olle K. S. Almgren; Goran B. D. Duker; Gert C. Strandlund |
| This application relates to novel 4 cyanophenyl derivatives which are useful for the treatment of cardiac arrhythmia and pharmaceutical compositions containing these compounds as the active ingredients. | ||||||
| 104 | Heterocyclic thiazole compounds | US68991 | 1987-07-01 | US4845106A | 1989-07-04 | Kozo Shiokawa; Shinichi Tsuboi; Shinzo Kagabu; Koichi Moriya |
| Novel insecticides of the formula ##STR1## in which n is 0 or 1,X is S, O, ##STR2## Y is N or ##STR3## Z is a 5- or 6-membered nitrogen-containing heterocyclic ring, and R to R.sup.9 variously represent hydrogen or specified organic radicals. | ||||||
| 105 | Novel benzothiazine derivatives | US34164 | 1987-03-10 | US4786635A | 1988-11-22 | Jun-ichi Iwao; Tadashi Iso; Masayuki Oya |
| This invention relates to novel benzothizine derivatives of the formula [I], processes for preparing them and therapeutic agents for circulatory diseases containing them as an active ingredient, ##STR1## wherein R.sup.1 is one or more groups selected from those consisting of hydrogen, lower alkyl, halogen, nitro, hydroxy, lower alkoxy, lower alkanoyloxy, amino, lower alkylamino and lower alkoxycarbonyloxy;R.sup.2 is hydrogen, lower alkyl or (C.sub.3 -C.sub.6)cycloalkyl;R.sup.3 is one or more groups selected from those consisting of hydrogen, lower alkyl, hydroxy, lower alkoxy, halogen, nitro, lower alkylenedioxy, lower alkanoyloxy, lower alkanoyl, amino, lower alkylamino, lower alkanoylamino and lower alkoxycarbonyloxy or ##STR2## R.sup.4 is hydrogen or lower alkyl. | ||||||
| 106 | Novel complex amido and imido derivatives of carboxyalkyl peptides | US925232 | 1986-10-31 | US4766110A | 1988-08-23 | James W. Ryan; Alfred Chung |
| Novel inhibitors of angiotensin converting enzyme are disclosed which have the general formula ##STR1## wherein R.sub.1 and/or R.sub.3 form complex amides and imides thereof, R.sub.4 and R.sub.5 form with --N--C-- a 4-6 membered ring structure as described and the other R substituents are selected from a variety of disclosed groups. | ||||||
| 107 | 2-substituted-[2-substituted-amino]-N-arylalkyl-3-[indol-3-yl] | US912731 | 1986-09-30 | US4757151A | 1988-07-12 | David C. Horwell |
| Certain 2-substituted-[2-substituted-amino]-N-arylalkyl-3-[indol-3-yl]propanamides demonstrate activity as appetite suppressants. The compounds, pharmaceutical compositions, and a method of suppressing appetite are disclosed. | ||||||
| 108 | Pyrrolo[1,2-a]imidazole and pyrrolo[1,2-a]pyridine derivatives and their use as 5-lipoxygenase pathway inhibitor | US856928 | 1986-04-28 | US4719218A | 1988-01-12 | Paul E. Bender; Nabil Hanna |
| A method of inhibiting the production of 5-lipoxygenase products in an animal in need thereof which comprises administering an effective, 5-lipoxygenase pathway inhibiting amount of a 2(3)-(pyridyl)-3-(2)-substituted phenyl)-6,7-dihydro-[5H]-pyrrolo-[1,2-a]imidazole, a 2(3)-(pyridyl)-3(2)-(substituted phenyl)-5,6,7,8-tetrahydro-imidazo[1,2,-a]pyridine, or a pharmaceutically acceptable salt thereof, to such animal. | ||||||
| 109 | Xanthene and thioxanthene derivatives, compositions thereof and treatment therewith | US35735 | 1979-05-03 | US4285956A | 1981-08-25 | Niels Lassen; Klaus P. Boges; Peter B. Hansen; Jorn L. M. Buus; Allan J. Bigler |
| The present invention relates to novel thioxanthene and xanthene derivatives which have useful pharmacodynamic activity, such as neuroleptic activity and antiemetic activity, methods for the preparation of said derivatives, pharmaceutical compositions containing same, and a method for the treatment of psychic disorders by administering a therapeutically active amount of one of said derivatives to a living animal body, including human beings.The new compounds of the present invention correspond to the Formula I: ##STR1## wherein X is a halogen atom, an alkyl group with from one to four carbon atoms inclusive, an alkyloxy group with from one to four carbon atoms inclusive, a methylthio group, a methylsulphonyl group, a dimethylsulfamoyl group, a trifluoromethyl group or an acetyl group;Y is hydrogen, fluorine or a methyl group;Z is oxygen or sulphur;n is an integer from zero to three inclusive, andR is a cycloalkyl group with from four to six carbon atoms inclusive in the ring substituted with from one to four substituents selected from optionally esterified hydroxy- or hydroxymethyl groups, methyl groups, amino groups, acetamido groups, mesylamino groups or oxo groups, a five- or six-: membered saturated heterocyclic ring having one or two heteroatoms selected from oxygen and nitrogen atoms and being optionally substituted with an optionally esterified hydroxy group or oxo group, any esterified hydroxy group present being an ester of an aliphatic carboxylic acid having from ten to twentytwo carbon atoms inclusive, as well as their non-toxic pharmaceutically acceptable acid addition salts with the proviso that methyl is present only when one of the other named substituents is also present. | ||||||
| 110 | Antiviral thiazolinyl benzimidazoles | US769358 | 1977-02-16 | US4150028A | 1979-04-17 | Charles J. Paget; James W. Chamberlin; James H. Wikel |
| Certain thiazolinyl or thiazinyl ketobenzimidazole compounds and derivatives thereof are useful as antiviral agents. | ||||||
| 111 | 5,6-Dihydro-4H-1,3-thiazine-2-carboxaldehyde oxime useful as insecticides | US703043 | 1976-07-06 | US4061749A | 1977-12-06 | James E. Powell |
| 5,6-Dihydro-4H-1,3-thiazine-2-carboxaldehyde oxime useful as an insecticide. | ||||||
| 112 | Substituted (5,6,e) indoles | US453425 | 1974-03-21 | US3959270A | 1976-05-25 | Claude P. Fauran; Guy M. Raynaud; Michel J. Turin; Claude J. Gouret |
| A compound of the formula ##SPC1##Wherein R.sub.1 is alkyl having one to 4 carbon atoms, and R.sub.2 is (a) alkyl having one to 4 carbon atoms, or (b) alkyl having one to 4 carbon atoms and substituted by (1) dialkylamino the latter alkyl having from one to 3 carbon atoms, (2) pyrrolidino or (3) morpholino, with the proviso that when R.sub.1 is ethyl, R.sub.2 is not ethyl, propyl, or diethylamino. The compounds are prepared by reacting 2-methyl-3-alkoxycarbonyl-5-hydroxyindole with a primary amine. The compounds possess diuretic, antihypertensive, antiulcerous, antiinflammatory, sedative and analgesic properties. | ||||||
| 113 | 3-heterocyclicthiomethylcephalosporins | US30650772 | 1972-11-14 | US3868369A | 1975-02-25 | BERGES DAVID ALAN |
| Cephalosporins containing a heterocyclicthiomethyl group at position 3 are prepared. The heterocyclic group is 5-oxo- Delta 2-1,2,4-triazolinyl, 5-thiono- Delta 2-1,2,4-triazolinyl, 5-oxoDelta 2-1,2,4-thiadiazolinyl or 5-thiono- Delta 2-1,3,4thiadiazolinyl. The compounds have antibacterial activity.
|
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| 114 | PROBES FOR IMAGING HUNTINGTIN PROTEIN | PCT/US2015/047407 | 2015-08-28 | WO2016033445A1 | 2016-03-03 | DOMINGUEZ, Celia; WITYAK, John; BARD, Jonathan; KISELYOV, Alex; BROWN, Christopher, John; GALAN, Sebastien, Rene Gabriel; PRIME, Michael, Edward; GILES, Paul, Richard; GADOULEAU, Elise, Luciennen Paulette; KRÜLLE, Thomas, Martin; CLARK-FREW, Daniel; JOHNSON, Peter, David; SCHAERTL, Sabine; HERRMANN, Frank; GRIMM, Steffen, Kaspar; KAHMANN, Jan, Dirk; SCHEICH, Christoph; COE, Samuel; HAYES, Sarah |
Provided are imaging agents comprising a compound of Formula (I), or a pharmaceutically acceptable salt thereof, and methods of their use. |
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| 115 | 2-ARYL-4-QUINOLINECARBOXAMIDE DERIVATIVES FOR TREATING THYROID DISEASES | PCT/US2015/038548 | 2015-06-30 | WO2016004035A1 | 2016-01-07 | LATIF, Rauf; DAVIES, Terry |
The use of 2-arylquinolinecarboxamides of formula (I): is disclosed. The compounds are agonists at the TSH receptor (TSHR) and are therefore useful in the treatment of patients with thyroid dysfunction and in the management of differentiated thyroid cancer. |
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| 116 | TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF | PCT/CN2014/074145 | 2014-03-26 | WO2015143654A8 | 2015-10-01 | MITCHELL, Helen; FRALEY, Mark E.; COOKE, Andrew J.; STUMP, Craig A.; SCHIRRIPA, Kathy; ZHANG, Xu-Fang; MCWHERTER, Melody; LIU, Chungsing; MAO, Qinghau |
The present invention is directed to six membered heteroaryl benzamide compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA. |
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| 117 | BICYCLIC COMPOUNDS HAVING BRADYKININ RECEPTORS AFFINITY AND PHARMACEUTICAL COMPOSITIONS THEREOF | PCT/US2004011105 | 2004-04-12 | WO2004092116A8 | 2005-05-06 | GRONEBERG ROBERT D; ASKEW BEN; D AMICO DERIN C; ZHAN JAMES; TORO ANDRAS; SUZUKI HIDEO; MARESKA DAVID A; HAN NIANH; FOTSCH CHRISTOPHER H; LIU QINGLAN; RIAHI BABAK; YANG KEVIN; LI AIWAN; YUAN CHESTER; BISWAS KAUSTAV; HARRIED SCOTT; NGUYEN TOM; QIAN WENYUAN; CHEN JIAN J; NOMAK RANA |
| Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes. | ||||||
| 118 | AN IMPROVED PROCESS FOR THE PREPARATION OF 3,4-DIHYDRO-1,4-BENZOTHIAZINE | PCT/IB2001/001615 | 2001-09-03 | WO02020498A2 | 2002-03-14 | |
| A process for the preparation of 3,4-dihydro-1,4-benozthiazine of the formula (1) which comprises, condensing of 2-aminothiophenol with dihaloethane of formula (11) wherein X represents halogen atom in presence of organic base and relatively non polar solvent at a temperature in the range of 40-80 DEG C followed by cyclization and formation of organic salt as by product and isolating the compound of formula (1) by conventional methods. | ||||||
| 119 | N-HETEROCYCLIC DERIVATIVES AS NOS INHIBITORS | PCT/US2000/023173 | 2000-08-24 | WO01014371A1 | 2001-03-01 | |
| N-Heterocyclic derivatives of formula (Ya) are described herein, as well as other N-heterocycles, as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of nitric oxide synthase and processes for synthesizing these compounds are also described herein. | ||||||
| 120 | METHODS AND AGENTS FOR MODULATING THE IMMUNE RESPONSE AND INFLAMMATION INVOLVING MONOCYTE AND DENDRITIC CELL MEMBRANE PROTEINS | PCT/US9912681 | 1999-06-04 | WO9962537A9 | 2000-03-09 | BEAULIEU SYLVIE; RANDOLPH GWENDALYN J; MULLER WILLIAM A; STEINMAN RALPH M |
| Methods and agents are provided to decrease or increase the migration of dendritic cells for the suppression or enhancement, respectively, of the development of immunity and the immune response, by modulating the dendritic cell membrane proteins p-glycoprotein (MDR-1) and tissue factor. Agents which suppress migration have utility in the treatment of immunologically-mediated and inflammatory diseases such as graft rejection, contact dermatitis, seasonal allergies, asthma, and food allergies. Agents which enhance migration are useful for increasing the effectiveness of vaccines. Agents are also disclosed which enhance the migration of monocytes, useful in the treatment of chronic inflammatory diseases. Methods are also provided for identifying useful agents by measuring the effect on dendritic cell migration of agents which modulate p-glycoprotein and tissue factor activity, as well as the effect of agents on monocyte migration. | ||||||
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