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1. 发明申请

WO1995024392A1 2-CHLORO AND 2-BROMO DERIVATIVES OF 1,5-IMINOSUGARS 审中-公开
标题翻译： 1-IMINOSUGARS的2-CHLORO和2-BROMO衍生物
公开(公告)号：WO1995024392A1
公开(公告)日：1995-09-14
申请号：PCT/US1995002168
申请日：1995-02-28
申请人： G. D. SEARLE & CO. , BARTA, Thomas, E. , MUELLER, Richard, A.
发明人： G. D. SEARLE & CO.
IPC分类号： C07D211/46
CPC分类号： C07D401/12 , C07D207/12 , C07D211/46 , C07D491/04 , C07F7/1804 , C07F7/2224
摘要： Novel 1,5-iminosugars of formula (I) wherein X is Cl or Br; R1 is H or a C1-C12 branched or unbranched alkyl group, alkoxyalkyl, alkenyl, alkynyl, arylalkyl, substituted arylalkyl, arylalkenyl, or substituted arylalkenyl; and R2, R3 and R4 are independently H or COR5 where R5 is C1-C6 branched or unbranched alkyl, or C6-C12 aryl or alkylaryl. Also claimed are compounds of the formulae II-V.
摘要翻译：式（I）的新的1,5-亚氨基二糖，其中X是Cl或Br; R1是H或C1-C12支链或非支链烷基，烷氧基烷基，烯基，炔基，芳基烷基，取代的芳基烷基，芳基烯基或取代的芳基烯基; 且R 2，R 3和R 4独立地为H或COR 5，其中R 5为C 1 -C 6支链或非支链烷基或C 6 -C 12芳基或烷基芳基。还要求的是式II-V的化合物。

2. 发明申请

WO1994004503A1 PYRIDINYL/QUINOLINYL-TERMINATED ALKYLAMINO ETHYNYL ALANINE AMINO DIOL COMPOUNDS FOR TREATMENT OF HYPERTENSION 审中-公开
标题翻译：吡啶二酮/喹啉氨基亚氨基亚氨基亚氨基氨基二醇化合物治疗高血压
公开(公告)号：WO1994004503A1
公开(公告)日：1994-03-03
申请号：PCT/US1993007428
申请日：1993-08-10
申请人： G. D. SEARLE & CO. , HANSON, Gunnar, J. , MANNING, Robert, E.
发明人： G. D. SEARLE & CO.
IPC分类号： C07D215/06
CPC分类号： C07D213/40 , C07D213/42 , C07D215/12 , C07D217/14
摘要： Compounds characterized generally as pyridinyl/quinolinyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of formula (I), wherein A is selected from CO and SO2; wherein X is selected from oxygen atom and methylene; wherein B is selected from pyridinyl, quinolinyl, isoquinolinyl, chloroquinolinyl, tetrahydroquinolinyl and oxo-substituted tetrahydroquinolinyl; wherein R1 is selected from hydrido, methyl, ethyl, isopropyl and n-propyl; wherein R2 is phenylmethyl; wherein each of R3 and R5 is hydrido; wherein R4 is selected from ((alpha)), wherein V is selected from hydrido and methyl; wherein R6 is cyclohexylmethyl; wherein R7 is selected from isobutyl, cyclopropyl and cyclopropylmethyl; wherein q is a number selected from zero through three, inclusive; and wherein n is a number selected from zero through three, inclusive; or a pharmaceutically-acceptable salt thereof.
摘要翻译：通常作为吡啶基/喹啉基封端的烷基氨基乙炔基丙氨酸氨基二醇衍生物表征的化合物可用作治疗高血压的肾素抑制剂。特别感兴趣的化合物是式（I）的化合物，其中A选自CO和SO 2; 其中X选自氧原子和亚甲基; 其中B选自吡啶基，喹啉基，异喹啉基，氯喹啉基，四氢喹啉基和氧代取代的四氢喹啉基; 其中R1选自氢，甲基，乙基，异丙基和正丙基; 其中R2是苯基甲基; 其中R3和R5各自是氢的; 其中R 4选自（（α）），其中V选自氢和甲基; 其中R6是环己基甲基; 其中R 7选自异丁基，环丙基和环丙基甲基; 其中q是选自0至3的数字（包括端值）; 并且其中n是选自0至3的数字，包括端值; 或其药学上可接受的盐。

3. 发明申请

WO1995015316A1 SUBSTITUTED PYRAZOLYL BENZENESULFONAMIDES FOR THE TREATMENT OF INFLAMMATION 审中-公开
标题翻译：用于治疗炎症的取代的吡唑并苯并呋喃
公开(公告)号：WO1995015316A1
公开(公告)日：1995-06-08
申请号：PCT/US1994012720
申请日：1994-11-14
申请人： G. D. SEARLE & CO. , TALLEY, John, J. , PENNING, Thomas, D. , COLLINS, Paul, W. , ROGIER, Donald, J., Jr. , MALECHA, James, W. , MIYASHIRO, Julie, M. , BERTENSHAW, Stephen, R. , KHANNA, Ish, K. , GRANETS, Matthew, J. , ROGERS, Roland, S. , CARTER, Jeffery, S. , DOCTER, Stephen, H. , YU, Stella, S.
发明人： G. D. SEARLE & CO.
IPC分类号： C07D231/12
CPC分类号： C07D495/04 , C07D231/12 , C07D231/14 , C07D231/16 , C07D231/54 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04
摘要： A class of pyrazolyl benzenesulfonamide compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by formula (II), whrein R is selected from hydrido, alkyl, haloalkyl, alkoxycarbonyl, cyano, cyanoalkyl, carboxyl, aminocarbonyl, alkylaminocarbonyl, cycloalkylaminocarbonyl, arylaminocarbonyl, carboxyalkylaminocarbonyl, carboxyalkyl, aralkoxycarbonylalkylaminocarbonyl, aminocarbonylalkyl, alkoxycarbonylcyanoalkenyl and hydroxyalkyl; wherein R is selected from hydrido, alkyl, cyano, hydroxyalkyl, cycloalkyl, alkylsulfonyl and halo; and wherein R is selected from aralkenyl, aryl, cycloalkyl, cycloalkenyl and heterocyclic; wherein R is optionally substituted at a substitutable position with one or more radicals selected from halo, alkylthio, alkylsulfonyl, cyano, nitro, haloalkyl, alkyl, hydroxyl, alkenyl, hydroxyalkyl, carboxyl, cycloalkyl, alkylamino, dialkylamino, alkoxycarbonyl, aminocarbonyl, alkoxy, haloalkoxy, sulfamyl, heterocyclic and amino; provided R and R are not both hydrido; further provided that R is not carboxyl or methyl when R is hydrido and when R is phenyl; further provided that R is not triazolyl when R is methyl; further provided that R is not aralkenyl when R is carboxyl, aminocarbonyl or ethoxycarbonyl; further provided that R is not phenyl when R is methyl and R is carboxyl; and further provided that R is not unsubstituted thienyl when R is trifluoromethyl; or a pharmaceutically acceptable salt thereof.
摘要翻译：描述了一类吡唑基苯磺酰胺化合物用于治疗炎症和炎症相关疾病。特别感兴趣的化合物由式（II）定义，R 2选自氢，烷基，卤代烷基，烷氧基羰基，氰基，氰基烷基，羧基，氨基羰基，烷基氨基羰基，环烷基氨基羰基，芳基氨基羰基，羧基烷基氨基羰基，羧基烷基，芳烷氧基羰基烷基氨基羰基，氨基羰基烷基，烷氧羰基氰基烯基和羟烷基; 其中R 3选自氢化，烷基，氰基，羟基烷基，环烷基，烷基磺酰基和卤素; 其中R 4选自芳烯基，芳基，环烷基，环烯基和杂环; 其中R 4在可取代位置任选被一个或多个选自卤素，烷硫基，烷基磺酰基，氰基，硝基，卤代烷基，烷基，羟基，烯基，羟基烷基，羧基，环烷基，烷基氨基，二烷基氨基，烷氧基羰基，氨基羰基，烷氧基，卤代烷氧基，氨磺酰基，杂环和氨基; 条件是R 2和R 3都不是氢的; 进一步提供当R 3是氢的时，当R 4是苯基时，R 2不是羧基或甲基; 进一步提供当R 2是甲基时，R 4不是三唑基; 进一步提供当R 2是羧基时，R 4不是芳烯基，氨基羰基或乙氧基羰基; 进一步提供当R 2是甲基且R 3是羧基时，R 4不是苯基; 并且进一步提供当R 2为三氟甲基时R 4为未取代的噻吩基; 或其药学上可接受的盐。

4. 发明申请

WO1995011231A1 AMIDINO DERIVATIVES USEFUL AS NITRIC OXIDE SYNTHASE INHIBITORS 审中-公开
标题翻译：氨氮衍生物作为氮氧化物合成酶抑制剂有用
公开(公告)号：WO1995011231A1
公开(公告)日：1995-04-27
申请号：PCT/US1994011832
申请日：1994-10-20
申请人： G. D. SEARLE & CO. , HANSEN, Donald, W., Jr. , CURRIE, Mark, G. , HALLINAN, E., Ann , FOK, Kam, F. , HAGEN, Timothy, J. , BERGMANIS, Arija, A. , KRAMER, Steven, W. , LEE, Len, F. , METZ, Suzanne , MOORE, William, M. , PETERSON, Karen, B. , PITZELE, Barnett, S. , SPANGLER, Dale, P. , WEBBER, R., Keith , TOTH, Mihaly, V. , TRIVEDI, Mahima , TJOENG, Foe, S.
发明人： G. D. SEARLE & CO.
IPC分类号： C07D207/22
CPC分类号： C07D213/06 , A61K31/395 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/425 , A61K31/435 , A61K31/44 , A61K31/445 , A61K31/47 , A61K31/505 , A61K31/535 , A61K31/54 , A61K31/55 , C07D207/22 , C07D209/44 , C07D211/72 , C07D211/74 , C07D215/38 , C07D217/22 , C07D221/22 , C07D221/24 , C07D223/12 , C07D225/02 , C07D233/46 , C07D239/12 , C07D239/14 , C07D263/28 , C07D265/08 , C07D277/18 , C07D279/06 , C07D405/06
摘要： The current invention discloses useful pharmaceutical compositions containing amidino derivatives of formula (I) as nitric oxide synthase inhibitors.
摘要翻译：本发明公开了含有式（I）的脒基衍生物作为一氧化氮合酶抑制剂的有用的药物组合物。

5. 发明申请

WO1992021672A1 PLA2 INHIBITORS 审中-公开
标题翻译： PLA2抑制剂
公开(公告)号：WO1992021672A1
公开(公告)日：1992-12-10
申请号：PCT/US1992001190
申请日：1992-02-25
申请人： G. D. SEARLE & CO. , DJURIC, Stevan, Wakefield , DOCTER, Stephen, H. , HAACK, Richard, Arthur
发明人： G. D. SEARLE & CO.
IPC分类号： C07D333/38
CPC分类号： C07D307/68 , C07C69/76 , C07D333/38
摘要： This invention relates to novel compounds for treating inflammatory conditions by inhibition of phospholipase A2 activity of formula (I) wherein X is oxygen, sulfur or -CH=CH-; wherein R1 is hydrogen, alkyl of 1 to 6 carbons or a pharmaceutically acceptable cation; wherein R2 is phenoxy, alkoxy, methyl, trifluoromethyl or phenyl; wherein n is an integer from 1 to 20; compositions comprised of the novel compounds; and methods of treating inflammatory conditions with these compositions.

6. 发明申请

WO1993003033A1 CARBONATE-SUBSTITUTED IMIDAZO[4,5-d] PYRIDAZINE COMPOUNDS FOR TREATMENT OF CARDIOVASCULAR DISORDERS 审中-公开
标题翻译：碳酸酯取代的咪唑并[4,5-d]吡啶化合物用于治疗心血管疾病
公开(公告)号：WO1993003033A1
公开(公告)日：1993-02-18
申请号：PCT/US1992005856
申请日：1992-07-21
申请人： G. D. SEARLE & CO. , BOVY, Philippe, R.
发明人： G. D. SEARLE & CO.
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： A class of carbonate-substituted imidazo[4,5-d] pyridazine compounds is described for use in treatment of circulatory disorders. Compounds of particular interest are angiotensin II antagonists of formula (I), wherein each of R and R is independently selected from radicals of formula (a) and of formula (b), with the proviso that at least one of R and R must be a radical of formula (a); wherein R is selected from hydrido, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, isopentyl, methylbutyl, dimethylbutyl, neopentyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, cyclononyl, cyclodecyl, cyclopropylmethyl, cyclopropylethyl, cyclopentylmethyl, cyclopentylethyl, cyclohexylmethyl, cyclohexylethyl, cyclohexylpropyl, naphthyl, imidazole, pyridyl, pyrimidyl, naphthylmethyl, naphthylethyl, imidazolemethyl, imidazoleethyl, pyridylmethyl, pyridylethyl, pyrimidylmethyl, pyrimidylethyl, indanoylmethyl, indanoylethyl, pyrrolylmethyl, pyrrolylethyl, thienylmethyl, thienylethyl, furanylmethyl, furanylethyl, pyrazolemethyl and pyrazoleethyl; wherein R is hydrido; wherein R is selected from hydrido, linear or branched alkyl (C1-C10), linear or branched alkenyl (C2-C10), linear or branched alkynyl (C2-C10), cycloalkyl (C3-C10), cycloalkenyl (C3-C10), cycloalkylalkyl (C4-C10) and cycloalkenylalkyl (C4-C10); wherein at least one of R , R , R and R is an acidic group selected from CO2H, SH, PO3H2, SO3H, CONHNH2, CONHNHSO2CF3, OH, NHSO2CH3, NHSO2CF3, NHCOCF3, CONHSO2C6H5, CONHOH, CONHOCH3, CONHSO2CH3 and tetrazole; or a tautomer thereof or a pharmaceutically-acceptable salt thereof. These compounds are particularly useful in treatment or control of circulatory and cardiovascular disorders such as hypertension and congestive heart failure.
摘要翻译：描述了一类用于治疗循环障碍的碳酸酯取代的咪唑并[4,5-d]哒嗪化合物。特别感兴趣的化合物是式（I）的血管紧张素II拮抗剂，其中R a和R b各自独立地选自式（a）和式（b）的基团，条件是至少一个 R a和R b必须是式（a）的基团; 其中R 1选自氢，甲基，乙基，正丙基，异丙基，正丁基，仲丁基，异丁基，叔丁基，正戊基，异戊基，甲基丁基，二甲基丁基，新戊基，环丙基，环丁基，环戊基，环己基，环庚基，环辛基，环丙基，环丙基，环辛基，环丙基乙基，环戊基甲基，环戊基乙基，环己基甲基，环己基乙基，环己基丙基，萘基，咪唑，吡啶基，嘧啶基，萘甲基，萘乙基，咪唑甲基，咪唑基，吡啶基甲基，吡啶基乙基，嘧啶基甲基，嘧啶基乙基，吡啶甲基，吡咯基乙基，噻吩基甲基，噻吩乙基，呋喃基甲基，呋喃基乙基，吡唑甲基和吡唑基乙基; 其中R 2是氢的; 其中R 39选自氢化，直链或支链烷基（C1-C10），直链或支链烯基（C2-C10），直链或支链炔基（C2-C10），环烷基（C3-C10），环烯基 -C 10），环烷基烷基（C 4 -C 10）和环烯基烷基（C 4 -C 10）; 其中R 5，R 6，R 8和R 9中的至少一个是选自CO 2 H，SH，PO 3 H 2，SO 3 H，CONHNH 2，CONHNHSO 2 CF 3，OH，NHSO 2 CH 3，NHSO 2 CF 3，NHCOCF 3， CONHSO2C6H5，CONHOH，CONHOCH3，CONHSO2CH3和四唑; 或其互变异构体或其药学上可接受的盐。这些化合物特别可用于治疗或控制循环和心血管疾病如高血压和充血性心力衰竭。

7. 发明申请

WO1992021644A1 LTB4 SYNTHESIS INHIBITORS 审中-公开
标题翻译： LTB4合成抑制剂
公开(公告)号：WO1992021644A1
公开(公告)日：1992-12-10
申请号：PCT/US1992003572
申请日：1992-05-06
申请人： G. D. SEARLE & CO. , DJURIC, Stevan, Wakefield , HAACK, Richard, Arthur , MIYASHIRO, Julie, Marion
发明人： G. D. SEARLE & CO.
IPC分类号： C07C65/32
CPC分类号： C07C63/64 , C07C43/215 , C07C63/66 , C07C65/32 , C07C65/34 , C07C65/38 , C07C65/40 , C07D213/79 , C07D257/04 , C07D307/68 , C07D333/38 , C07F7/081
摘要： This invention relates to a compound of formula (I), or a pharmaceutically acceptable salt thereof wherein X is oxygen, sulfur, -CH=CH-, or -CH=N-; wherein R is -CO2R or tetrazole; wherein R is hydrogen, alkyl of 1 to 6 carbons or a pharmaceutically acceptable cation; wherein R is an alkyl of from 1 to 20 carbons, -(CH2)pCF3 or -(CH2)qR wherein R is alkoxy, phenoxy or alkoxy substituted phenoxy wherein the alkoxy group has from 1 to 8 carbons; wherein p and q are integers from 0 to 20; weherein n is 0 or 1; and wherein m is 0, 1, 2 or 3.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，其中X是氧，硫，-CH = CH-或-CH = N-; 其中R 1是-CO 2 R 2或四唑; 其中R 2是氢，1至6个碳的烷基或药学上可接受的阳离子; 其中R是1至20个碳的烷基， - （CH 2）p CF 3或 - （CH 2）q R 3其中R 3是烷氧基，苯氧基或烷氧基取代的苯氧基，其中烷氧基具有1至8个碳; 其中p和q为0至20的整数; weherein n为0或1; 并且其中m为0,1,2或3。

8. 发明申请

WO1994012639A2 INTERLEUKIN-3 (IL-3) MUTANT POLYPEPTIDES 审中-公开
标题翻译：白细胞介素-3（IL-3）突变多糖
公开(公告)号：WO1994012639A2
公开(公告)日：1994-06-09
申请号：PCT/US1993011198
申请日：1993-11-22
申请人： G. D. SEARLE & CO. , THE MONSANTO COMPANY , BAUER, S., Christopher , ABRAMS, Mark, Allen , BRAFORD-GOLDBERG, Sarah, Ruth , CAPARON, Maire, Helena , EASTON, Alan, Michael , KLEIN, Barbara, Kure , MCKEARN, John, Patrick , OLINS, Peter, O. , PAIK, Kumman , POLAZZI, Joseph, O. , THOMAS, John, Warren
发明人： G. D. SEARLE & CO. , THE MONSANTO COMPANY
IPC分类号： C12N15/24
CPC分类号： C07K14/5403 , A61K38/00 , C07K2319/00 , C07K2319/02 , Y10S930/141
摘要： The present invention relates to a recombinant human interleukin-3 (hIL-3) variant or mutant proteins (muteins). These hIL-3 muteins contain one or more amino acid substitutions and may also have amino acid deletions at both the N- and C-termini. The invention also relates to pharmaceutical compositions containing the hIL-3 muteins and methods for using them. Additionally, the present invention relates to recombinant expression vectors comprising nucleotide sequences encoding the hIL-3 muteins, related microbial expression systems, and processes for making the hIL-3 muteins using the microbial expression systems. Included in the present invention are deletion mutants of hIL-3 in which from 1 to 14 amino acids have been deleted from the N-terminus, and from 1 to 15 amino acids C corresponding to residues 119 to 133) have been deleted from the C-terminus, and which also contain one to three amino acid substitutions in the polypeptide. These hIL-3 mutant polypeptides may have biological activities similar to or better than hIL-3 and, in some cases, may also have an improved side effect profile.
摘要翻译：本发明涉及重组人白细胞介素-3（hIL-3）变体或突变蛋白（突变蛋白）。这些hIL-3突变蛋白含有一个或多个氨基酸取代，并且在N-和C-末端也可具有氨基酸缺失。本发明还涉及含有hIL-3突变蛋白的药物组合物及其使用方法。另外，本发明涉及包含编码hIL-3突变蛋白的核苷酸序列，相关微生物表达系统和使用微生物表达系统制备hIL-3突变蛋白的方法的重组表达载体。在本发明中包括hIL-3的缺失突变体，其中从N末端缺失1至14个氨基酸，对应于残基119至133的1至15个氨基酸C）已从C - 末端，并且其还在多肽中含有一至三个氨基酸取代。这些hIL-3突变体多肽可具有类似于或优于hIL-3的生物活性，并且在一些情况下也可具有改善的副作用特征。

9. 发明申请

WO1993016038A1 PHENYL AMIDINES SULFONAMIDES USEFUL AS PLATELET AGGREGATION INHIBITORS 审中-公开
标题翻译：苯胺氨基磺酸盐有助于平板电泳抑制剂
公开(公告)号：WO1993016038A1
公开(公告)日：1993-08-19
申请号：PCT/US1993001185
申请日：1993-02-12
申请人： G. D. SEARLE & CO. , THE MONSATO COMPANY , MIYANO, Masateru , ADAMS, Stephen, Paul , RICO, Joseph, Gerace
发明人： G. D. SEARLE & CO. , THE MONSATO COMPANY
IPC分类号： C07C311/19
CPC分类号： C07C311/29 , C07C311/19
摘要： This invention relates to compounds having formula (I), which are useful in the inhibition of platelet aggregation. This invention also relates to pharmaceutical compositions of such phenyl amidine sulfones derivates.

10. 发明申请

WO1992019605A1 SUBSTITUTED DIBENZOXAZEPINE COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE 审中-公开
标题翻译：取代的二苯并恶唑化合物，药物组合物和使用方法
公开(公告)号：WO1992019605A1
公开(公告)日：1992-11-12
申请号：PCT/US1992003027
申请日：1992-04-16
申请人： G. D. SEARLE & CO. , HALLINAN, E., Ann , HUSA, Robert, Knol , PETERSEN, Karen, Berenice
发明人： G. D. SEARLE & CO.
IPC分类号： C07D267/20
CPC分类号： C07D413/10 , C07D267/20 , C07D281/16 , C07D417/12 , C07F9/6527
摘要： The present invention provides substituted dibenzoxazepine compounds of formula (I) which are useful as analgesic agents for the treatment of pain, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of formula (I) in combination with a pharmaceutically-acceptable carrier, and a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of formula (I) to the animal.

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