| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 21 | SULFONIUM SALT, RESIST COMPOSITION, AND PATTERNING PROCESS | US13243204 | 2011-09-23 | US20120100486A1 | 2012-04-26 | Masayoshi Sagehashi; Youichi Ohsawa; Koji Hasegawa; Takeshi Kinsho; Tomohiro Kobayashi |
| A sulfonium salt of a naphthyltetrahydrothiophenium cation having a fluoroalkoxy chain with a specific anion is provided. The sulfonium salt is used as a photoacid generator to form a resist composition which when processed by immersion lithography, offers advantages of restrained dissolution in the immersion water and less pattern dependence or dark/bright bias. | ||||||
| 22 | Inactive metabolite approach to soft drug design | US08431727 | 1995-05-01 | US06610675B1 | 2003-08-26 | Nicholas S. Bodor |
| The invention provides novel soft steroidal anti-inflammatory agents, pharmaceutical compositions containing said agents, and methods of administering same to mammals in the treatment of inflammation. Preferred compounds of the invention include haloalkyl 17&agr;-alkoxycarbonyloxy-11&bgr;-hydroxyandrost-4-en-3-one-17&bgr;-carboxylates and the corresponding &Dgr;1,4 compounds, optionally bearing 6&agr;- and/or 9&agr;-fluorine and 16&agr;- or 16&bgr;-methyl substituents. Especially preferred compounds include haloalkyl 17&agr;-alkoxycarbonyloxy-9&agr;-fluoro-11&bgr;-hydroxy-16-methylandrosta-1,4-dien-3-one-17&bgr;-carboxylates. | ||||||
| 23 | Anti-inflammatory androstane derivatives | US10066961 | 2002-02-04 | US06537983B1 | 2003-03-25 | Keith Biggadike; Paul Spencer Jones; Jeremy John Payne |
| According to one aspect of the invention, there is provided a pharmaceutical formulation for administration by inhalation comprising a compound of formula (I), wherein R1 represents C1-6 alkyl or C1-6 haloalkyl; R2 represents —C(═O)-aryl or —C(═O)-heteroaryl; R3 represents hydrogen, methyl (which may be in either the &agr; or &bgr; configuration) or methylene; R4 and R5 are the same or different and each represents hydrogen or halogen; and {overscore (-----)} represents a single or a double bond; and salts and solvates thereof together with a long-acting &bgr;2-adrenoreceptor agonist which formulation has a therapeutically useful effect in the treatment of inflammatory disorders of the respiratory tract over a period of 24 hours or more. | ||||||
| 24 | Methods for allosteric modulation of the GABA receptor by members of the androstane and pregnane series | US09547041 | 2000-04-11 | US06277838B1 | 2001-08-21 | Ravindra B. Upasani; Haiji Xia; Derk Hogenkamp |
| Methods, compositions, and compounds for modulating the GABAA receptor-chloride ionophore complex to alleviate stress, anxiety, seizures, mood disorders, PMS and PND and to induce anesthesia. | ||||||
| 25 | .increment..sup.16 unsaturated C.sub.17 heterocyclic steroids useful as steroid C.sub.17-20 lyase inhibitors | US72778 | 1998-05-06 | US5965548A | 1999-10-12 | Norton P. Peet; Joseph P. Burkhart; Cynthia A. Gates |
| The present invention relates to .DELTA..sup.16 unsaturated steroids which are useful as steroid C.sub.17-20 lyase inhibitors. | ||||||
| 26 | 17-deoxycorticosteroid-21-�O!carboxylic esters, processes for their preparation and pharmaceuticals containing these compounds | US529668 | 1995-09-18 | US5824670A | 1998-10-20 | Ulrich Stache; Hans-Georg Alpermann; Manfred Bohn |
| 17-Deoxycorticoid-21-carboxylic esters of the formula I ##STR1## are described, in which A is CHOH and CHCl, CH.sub.2, C.dbd.O or 9(11) double bond; Y is H, F or Cl; Z is H, F or CH.sub.3 ; R(1) is aryl or hetaryl and R(2) is H or methyl. They are obtained by reacting a compound of the formula II, ##STR2## in which R(4) is OH, with an activated carboxylic acid of the formula III,R(5)-CO--X-R(1) III. The compounds I possess very strong local and topical antiinflammatory activity and exhibit a very good ratio of local to systemic antiinflammatory effect, which ratio is often clearly superior to that of structurally related corticoid 21-esters which do not carry any aryl or hetaryl group in the 21-ester residue or to that of analogous 17-deoxycorticoids having an unesterified, that is a free, 21-hydroxyl group. | ||||||
| 27 | Corticosteroid 17-alkyl carbonate 21-[0]-carboxylic and carbonic esters, and pharmaceuticals containing these compounds | US294804 | 1994-08-25 | US5608093A | 1997-03-04 | Ulrich Stache; Hans-Georg Alpermann; Walter D urckheimer; Manfred Bohn |
| Corticoid 17-alkyl carbonate 21-carboxylic and carbonic esters of the formula I ##STR1## are described in which A is CHOH and CHCl, CH.sub.2, C.dbd.O or 9(11) double bond; Y is H, F or Cl; Z is H, F or CH.sub.3 ; R(1) is aryl or hetaryl; n and m are zero or 1; R(2) is alkyl or --(CH.sub.2).sub.2 --OCH.sub.3 ; R(3) is H or methyl. They are obtained by reacting a compound of the formula II, ##STR2## in which R(5) is OH, with an activated carboxylic acid of the formula III,R(6)--CO--(O).sub.n --(X)--R(1) III.The compounds I have a very strong local and topical antiinflammatory action and exhibit a very good ratio of local to systemic antiinflammatory effects, which ratio is often markedly superior to that of analogous corticoid 17-alkyl carbonate 21-esters which do not carry any aryl or heteraryl group in the 21-ester radical. | ||||||
| 28 | 17-Aryl and 17-heterocyclyl-5.beta.,14.beta.-androstane derivatives active on the cardiovascular system, processes for their preparation and pharmaceutical compositions containing same | US128114 | 1993-09-29 | US5567694A | 1996-10-22 | Nicoletta Almirante; Luigi Bernardi; Alberto Cerri; Piero Melloni; Gloria Padoani; Luisa Quadri |
| 17-aryl and heterocyclyl-5.beta.,14.beta.-androstane compounds having the formula (I) ##STR1## wherein R is an aryl ring or a saturated or unsaturated heterocyclic ring are active on the cardiovascular system and are useful in treating cardiovascular disorders. | ||||||
| 29 | Lipid-selective antioxidants and their preparation and use | US212863 | 1994-03-15 | US5508275A | 1996-04-16 | Klaus-Ulrich Weithmann; Gunther Wess; Dirk Seiffge |
| Lipid-selective antioxidants of the formula I(A).sub.a (L)(X).sub.a, (I),in whichA=an antioxidative component,L=a bridging member,X=a lipophilic componenta and a'=independently of one another the numbers 1 or 2.The compounds are used for the protection of lipid-containing substances against oxidation and in pharmaceuticals for the prophylaxis and treatment of diseases in which bioradicals are involved, in particular of coronary, circulatory and vascular diseases. | ||||||
| 30 | 13-alkyl-11beta-phenylgonanes | US144474 | 1993-11-02 | US5446036A | 1995-08-29 | Stefan Scholz; Eckhard Ottow; Guenter Neef; Walter Elger; Sybille Beier; Krzysztof Chwalisz |
| There are provided 13-alkyl-11beta-phenyl-gonanes of formula I ##STR1## wherein Z is an oxygen atom or N--OH;R.sup.2 is alpha- or beta-position methyl or ethyl;R.sup.1 is selected from heteroaryl radicals, cycloalkyl radicals, cycloalkenyl radicals, aryl radicals, alkenyl radicals, and alkyl radicals where R.sup.2 is in the alpha-position and an ethyl radical where R.sup.2 is in the beta-position; andR.sup.3 and R.sup.4 are selected from one of two different groups of substituent pairs, the group from which the selection is made being determined by the position of R.sup.2. | ||||||
| 31 | Process for the production of 10.beta.-H-steroids | US952739 | 1992-11-30 | US5405979A | 1995-04-11 | Eckhard Ottow; Gunter Neef; Arwed Cleve; Rudolf Wiechert |
| A process for the production of 10.beta.-H-11.beta.-(substituted phenyl) steroids of the formulae Ia or Ib set forth in the claims by reduction of a compound of the formula III: ##STR1## followed by cleaving with a strong acid or partial cleaving with a less strong acid. Reduction with an electropositive metal in an electron-solvating solvent is preferred. | ||||||
| 32 | 13-alkyl-11.beta.-phenylgonanes | US374809 | 1989-07-03 | US5273971A | 1993-12-28 | Stefan Scholz; Eckhard Ottow; Guenter Neef; Walter Elger; Sybille Beier; Krzysztof Chwalisz |
| There are provided 13-alkyl-11beta-phenyl-gonanes of formula I ##STR1## wherein Z is an oxygen atom or N--OH;R.sup.2 is alpha- or beta-position methyl or ethyl;R.sup.1 is selected from heteroaryl radicals, cycloalkyl radicals, cycloalkenyl radicals, aryl radicals, alkenyl radicals, and alkyl radicals where R.sup.2 is in the alpha-position and an ethyl radical where R.sup.2 is in the beta-position; andR.sup.3 and R.sup.4 are selected from one of two different groups of substituent pairs, the group from which the selection is made being determined by the position of R.sup.2. | ||||||
| 33 | Intermediates for 3-keto-19-nor-.DELTA..sup.4,9 -steroids | US757261 | 1991-09-10 | US5182381A | 1993-01-26 | Daniel Philibert; Jean G. Teutsch; Germain Costerousse; Roger Deraedt |
| Novel 3-keto-19-nor-.DELTA..sup.4,9 -steroids of the formula ##STR1## and their non-toxic, pharmaceutically acceptable acid addition salts possessing a remarkable antiglucocorticoidal activity. | ||||||
| 34 | Coupling agents and products produced therefrom | US568698 | 1984-01-06 | US4595656A | 1986-06-17 | Stephen D. Allen; Michael Thompson |
| Isocyanate or isothiocyanate substituted lactone or thiolactone is employed for coupling one organic compound to another. For example, such coupling agents can be employed for coupling thyroxine or digoxin to a fluorescent compound for use as a tracer in an assay. | ||||||
| 35 | .DELTA..sup.1,3,5(10) -Estratrienes | US867486 | 1978-01-06 | US4272530A | 1981-06-09 | Jean G. Teutsch; Daniel Philibert |
| Novel 11.beta. -substituted-.DELTA. .sup.1,3,5(10) -estratrienes of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of optionally substituted unsaturated alkyl of 2 to 8 carbon atoms, optionally substituted aryl of 6 to 12 carbon atoms, optionally substituted aralkyl of 7 to 13 carbon atoms and heterocycle with at least one sulfur or oxygen heteroatom, R.sub.2 is alkyl of 1 to 4 carbon atoms, Z is selected from the group consisting of hydrogen, alkyl of 1 to 12 carbon atoms and aralkyl of 7 to 9 carbon atoms, R.sub.3 is selected from the group consisting of hydrogen, hydroxy, acyl of an organic carboxylic acid of 1 to 18 carbon atoms and acyloxy of an organic carboxylic acid of 1 to 18 carbon atoms and R.sub.4 is selected from the group consisting of hydrogen, hydroxy, alkyl and alkoxy of 1 to 8 carbon atoms, acyloxy of an organic carboxylic acid of 1 to 8 carbon atoms and alkenyl and alkynyl of 2 to 8 carbon atoms, with the proviso that R.sub.1 is not allyl when Z is hydrogen, R.sub.2 is methyl, R.sub.3 is hydroxy and R.sub.4 is hydrogen having estrogenic activity and their preparation. | ||||||
| 36 | COMPOSITIONS AND METHODS FOR TREATING CNS DISORDERS | US15531313 | 2015-11-27 | US20170342102A1 | 2017-11-30 | Gabriel Martinez Botella; Boyd L. Harrison; Albert J. Robichaud; Francesco G. Salituro; Richard T. Beresis |
| Described herein are neuroactive steroids of the Formula (II): or a pharmaceutically acceptable salt thereof; wherein A, R1, R2a, R2b, R3a, R3b, R4a, R4b, R5, R6 and are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. The present invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of use and treatment, e.g., such for inducing sedation and/or anesthesia. | ||||||
| 37 | 19-nor C3, 3-disubstituted C21-C-bound heteroaryl steroids and methods of use thereof | US14785175 | 2014-04-17 | US09725481B2 | 2017-08-08 | Gabriel Martinez Botella; Boyd L. Harrison; Albert Jean Robichaud; Francesco G. Salituro; Richard Thomas Beresis |
| Provided herein are 19-nor C3,3-disubstituted steroids of Formula (I): and pharmaceutically acceptable salts thereof; wherein, , R1, R2, R3a, R3b, R4a, and R4b are as defined herein, and A is a carbon bound substituted or unsubstituted 5-to6-membered heteroaryl ring as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, and tinnitus. | ||||||
| 38 | Sulfonium salt, resist composition, and patterning process | US13243204 | 2011-09-23 | US08597869B2 | 2013-12-03 | Masayoshi Sagehashi; Youichi Ohsawa; Koji Hasegawa; Takeshi Kinsho; Tomohiro Kobayashi |
| A sulfonium salt of a naphthyltetrahydrothiophenium cation having a fluoroalkoxy chain with a specific anion is provided. The sulfonium salt is used as a photoacid generator to form a resist composition which when processed by immersion lithography, offers advantages of restrained dissolution in the immersion water and less pattern dependence or dark/bright bias. | ||||||
| 39 | Organic compounds | US10312021 | 2001-06-26 | US06921757B2 | 2005-07-26 | Bernard Cuenoud; David Beattie; Thomas Hugo Keller; Gaynor Elizabeth Pilgrim; David Andrew Sandham; Simon James Watson |
| Compounds of formula (I), where R is a monovalent cyclic organic group having from 3 to 15 atoms in the ring system, useful as pharmaceuticals | ||||||
| 40 | Corticoid 17,21-dicarboxylic esters and corticosteroid 17-carboxylic ester 21-carbonic esters, processes for their preparation and pharmaceuticals containing these compounds | US08897455 | 1997-07-22 | US06835724B2 | 2004-12-28 | Ulrich Stache; Hans-Georg Alpermann; Walter Dürckheimer; Manfred Bohn |
| Corticoid 17,21-dicarboxylic esters and corticosteroid 17-carboxylic ester 21-carbonic esters, processes for their preparation and pharmaceuticals containing these compounds Corticoid 17,21-dicarboxylic esters and corticoid 17-carboxylic ester 21-carbonic esters of the formula I: are described, in which A is CHOH and CHCl, CH2, C═O or 9(11) double bond; Y is H, F or Cl; Z is H, F or methyl; R(1) is aryl or hetaryl; R(2) is alkyl and R(3) is H or methyl. They are obtained, inter alia, by reacting a compound of the formula II: in which R(5) is OH, with an activated carboxylic acid of the formula III: R(6)-CO—(O)n[(C1-C4)-alkyl]m-R(1) III. They have a very strong local and topical antiinflammatory action and exhibit a very good ratio of local to systemic antiinflammatory effects. They are used, inter alia, as agents for treating inflammatory dermatoses. | ||||||
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