公开(公告)号：US5389684A

公开(公告)日：1995-02-14

申请号：US108038

申请日：1993-08-17

申请人： John Fairhurst ,  David E. Tupper

发明人： John Fairhurst ,  David E. Tupper

IPC分类号： A61K31/165 ,  A61K31/40 ,  A61K31/403 ,  A61K31/4035 ,  A61P1/00 ,  A61P3/04 ,  A61P9/12 ,  A61P25/00 ,  A61P25/18 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  A61P43/00 ,  C07C231/14 ,  C07C235/66 ,  C07C237/48 ,  C07C319/20 ,  C07C323/38 ,  C07C323/62 ,  C07D209/48 ,  C07C233/22

CPC分类号： C07C323/38 ,  C07C235/66 ,  C07C237/48 ,  C07C2101/14 ,  C07C2101/18

摘要： Pharmaceutical compounds of the formula: ##STR1## in which each R.sup.1 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen or nitro, and n is 0, 1, 2 or 3, R.sup.2 is hydrogen, C.sub.1-4 alkyl or C.sub.2-4 alkenyl, R.sup.3 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, halogen, nitro or --NR'R" where R' and R" are each hydrogen or C.sub.1-4 alkyl, R.sup.4 and R.sup.5 are each hydrogen, C.sub.1-4 alkyl, optionally substituted phenyl or C.sub.6-9 cycloalkyl optionally substituted by 1 to 4 C.sub.1-4 alkyl groups, R.sup.6 is optionally substituted phenyl, tetrahydronaphthyl, phthalimido, saccharinyl, glutaramido, C.sub.6-10 cycloalkyl optionally substituted with 1 to 4 C.sub.1-4 alkyl groups or a phenyl group, or C.sub.4-9 heterosubstituted cycloalkyl optionally substituted with 1-4 alkyl groups, x is 1, 2 or 3, y is 0 or 1 and z is 0, 1, 2 or 3; and salts thereof.

摘要翻译： 下式的药物化合物：烷氧基，卤素或硝基，n为0,1,2或3，R2为氢，C1-4烷基或C2-4烯基，R3为氢，C1-4烷基，C1 -4-烷氧基，C 1-4烷硫基，卤素，硝基或-NR'R“，其中R'和R”各自为氢或C 1-4烷基，R 4和R 5各自为氢，C 1-4烷基，任选取代的苯基 或任选被1至4个C 1-4烷基取代的C 6-9环烷基，R 6是任选取代的苯基，四氢萘基，苯二甲酰亚氨基，糖精，戊二酰氨基，任选被1至4个C 1-4烷基取代的C 6-10环烷基或苯基 或任选被1-4个烷基取代的C 4-9杂取代的环烷基，x为1,2或3，y为0或1，z为0,1,2或3; 及其盐。

公开(公告)号：US5378699A

公开(公告)日：1995-01-03

申请号：US14016

申请日：1993-02-05

申请人： Michael Brunavs ,  Colin P. Dell ,  Peter T. Gallagher ,  William M. Owton ,  Jai P. Singh ,  Colin W. Smith

发明人： Michael Brunavs ,  Colin P. Dell ,  Peter T. Gallagher ,  William M. Owton ,  Jai P. Singh ,  Colin W. Smith

IPC分类号： A61K31/35 ,  A61K31/352 ,  A61K31/36 ,  A61K31/38 ,  A61K31/381 ,  A61K31/40 ,  A61K31/44 ,  A61K31/443 ,  A61K31/4433 ,  A61P1/16 ,  A61P3/10 ,  A61P9/10 ,  A61P19/02 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  A61P37/02 ,  A61P37/06 ,  A61P43/00 ,  C07D311/92 ,  C07D405/04 ,  C07D407/04 ,  C07D409/04 ,  C07D311/04

CPC分类号： C07D405/04 ,  A61K31/35 ,  A61K31/36 ,  A61K31/38 ,  A61K31/40 ,  A61K31/44 ,  C07D311/92 ,  C07D407/04 ,  C07D409/04

摘要： Methods of treating an immune disease, cell proliferation, restenosis and vascular smooth muscle cells using the pharmaceutical compounds of the formula ##STR1## in which R.sup.2 is phenyl, naphthyl or heteroaryl selected from thienyl, pyridyl, benzothienyl, quinolinyl, benzofuranyl or benzimidazolyl, said phenyl, naphthyl and heteroaryl groups being optionally substituted, or R.sup.2 is furanyl optionally substituted with C.sub.1-4 alkyl; and salts thereof.

摘要翻译： 所述治疗免疫疾病，细胞增殖，再狭窄和血管平滑肌细胞的方法使用其中R 2为苯基，选自噻吩基，吡啶基，苯并噻吩基，喹啉基，苯并呋喃基或苯并咪唑基的萘基或杂芳基的式“IMAGE”的药物化合物， 苯基，萘基和杂芳基任选被取代，或R 2是任选被C 1-4烷基取代的呋喃基; 及其盐。

公开(公告)号：US5037698A

公开(公告)日：1991-08-06

申请号：US145444

申请日：1988-01-19

申请人： Francois Brunel

发明人： Francois Brunel

IPC分类号： A61K9/48

CPC分类号： A61K9/4866 ,  A61K9/4858 ,  Y10S514/962 ,  Y10S514/963 ,  Y10T428/2984

摘要： Capsules containing a hygroscopic or deliquescent component are stabilized by a) forming a mixture of the hydrogscopic or deliquescent compound with a sufficient quantity of water to achieve an equilibrium, b) adding a thickening agent and c) heating the solution or suspension; and introducing the heated composition so formed into the capsule. Preferably an equilibrium-protecting agent, such as glycerin, is also added.

公开(公告)号：US4968711A

公开(公告)日：1990-11-06

申请号：US182648

申请日：1988-04-18

申请人： Stephen R. Baker ,  John Goldsworthy ,  William J. Ross

发明人： Stephen R. Baker ,  John Goldsworthy ,  William J. Ross

IPC分类号： C07D233/76 ,  A61K31/41 ,  A61K31/415 ,  A61K31/4166 ,  A61P37/08 ,  C07C67/00 ,  C07C313/00 ,  C07C323/56 ,  C07C323/60 ,  C07D257/04 ,  C07D403/12 ,  C07D405/10

CPC分类号： C07D257/04 ,  C07D403/12 ,  Y02P20/55

摘要： There is disclosed a pharmaceutical compound of the formula ##STR1## in which R.sup.1 is C.sub.7-20 alkyl, C.sub.7-20 alkenyl, or C.sub.7-20 alkynyl, the alkyl, alkenyl or alkynyl group being optionally substituted by phenyl or substituted phenyl, R.sup.2 is --CN, --COOR.sup.3 or ##STR2## wherein R.sup.3 is hydrogen or a protecting group, X is alkylene containing 1 to 6 carbon atoms and Y is a nitrogen-containing group selected from ##STR3## where each R.sup.4 independently is hydrogen or C.sub.1-4 alkyl; and salts thereof.

公开(公告)号：US4963558A

公开(公告)日：1990-10-16

申请号：US447319

申请日：1989-12-07

申请人： Terrence M. Hotten ,  Graham H. Timms ,  David E. Tupper

发明人： Terrence M. Hotten ,  Graham H. Timms ,  David E. Tupper

IPC分类号： A61K31/47 ,  A61P1/08 ,  A61P25/08 ,  A61P25/18 ,  A61P25/20 ,  A61P25/26 ,  C07D471/04

CPC分类号： C07D471/04

摘要： Pharmaceutical compounds of the formula ##STR1## in which R.sup.1 is hydrogen or C.sub.1-6 alkyl, R.sup.2 is hydrogen, C.sub.1-6 alkyl optionally substituted by C.sub.3-9 cycloalkyl or optionally substituted phenyl, C.sub.3-9 cycloalkyl, optionally substituted phenyl, or --SR.sup.4 where R.sup.4 is C.sub.1-6 alkyl optionally substituted by C.sub.3-9 cycloalkyl or optionally substituted phenyl, or C.sub.3-9 cycloalkyl, R.sup.3 is hydrogen, C.sub.1-6 alkyl optionally substituted by C.sub.3-9 cycloalkyl or optionally substituted phenyl, c.sub.3-9 cycloalkyl, or optionally phenyl, and either X and Y are both hydrogen or together are .dbd.O; and acid addition salts thereof. These compounds show useful effects on the central nervous system.

公开(公告)号：US4845200A

公开(公告)日：1989-07-04

申请号：US877598

申请日：1986-06-23

申请人： George J. Cullinan ,  George F. Rowland ,  Robin G. Simmonds

发明人： George J. Cullinan ,  George F. Rowland ,  Robin G. Simmonds

IPC分类号： G01N33/531 ,  A61K39/395 ,  A61K47/48 ,  C07D519/04 ,  C07K17/02 ,  C12Q1/04

CPC分类号： C07D519/04 ,  A61K47/48392 ,  Y10S530/828

摘要： A conjugate comprising a vinca moiety convalently linked at the 4-position via a group of the formula --OCOXCO-- where X represents a single chemical bond or an optionally substituted C.sub.1-10 chain, to an immunoglobulin or an immunoglobulin fragment.The conjugates are useful in the treatment of cancer.

摘要翻译： 缀合物，其包含通过式-OCOXCO-基团（其中X表示单个化学键或任选取代的C 1-10链）在4-位上共价连接到长春花基团的免疫球蛋白或免疫球蛋白片段。 缀合物可用于治疗癌症。

公开(公告)号：US4801735A

公开(公告)日：1989-01-31

申请号：US801524

申请日：1985-11-25

申请人： Mark A. W. Finch ,  John R. Harris

发明人： Mark A. W. Finch ,  John R. Harris

IPC分类号： C07C43/23 ,  A61K31/047 ,  A61K31/05 ,  A61K31/11 ,  A61K31/12 ,  A61K31/135 ,  A61K31/15 ,  A61K31/165 ,  A61K31/19 ,  A61K31/195 ,  A61K31/23 ,  A61K31/445 ,  A61K31/535 ,  A61K31/5375 ,  A61P11/00 ,  A61P17/00 ,  A61P29/00 ,  A61P35/00 ,  A61P37/08 ,  A61P43/00 ,  C07C27/00 ,  C07C39/11 ,  C07C39/19 ,  C07C45/00 ,  C07C47/27 ,  C07C47/277 ,  C07C47/565 ,  C07C47/575 ,  C07C49/825 ,  C07C49/835 ,  C07C49/84 ,  C07C51/00 ,  C07C59/48 ,  C07C59/52 ,  C07C59/64 ,  C07C67/00 ,  C07C69/732 ,  C07C69/734 ,  C07C213/00 ,  C07C215/50 ,  C07C215/78 ,  C07C231/00 ,  C07C231/12 ,  C07C235/34 ,  C07C235/46 ,  C07C239/00 ,  C07C241/00 ,  C07C251/24 ,  C07C251/32 ,  C07C251/86 ,  C07D295/145 ,  C07D295/16 ,  C07D295/18 ,  C07D295/185 ,  C07D295/22 ,  C07D295/30 ,  C07C69/76 ,  C07C65/01

CPC分类号： C07D295/185 ,  C07C251/72 ,  C07C47/27 ,  C07C47/277 ,  C07C47/565 ,  C07C47/575 ,  C07C49/835 ,  C07C49/84 ,  C07D295/145 ,  C07D295/30 ,  Y02P20/55

摘要： Compounds are described of the following formula ##STR1## in which R.sup.1 and R.sup.2 are each hydrogen, C.sub.1-12 alkyl or C.sub.2-12 alkenyl, at least one of R.sup.1 and R.sup.2 being C.sub.1-12 alkyl or C.sub.2-12 alkenyl; X.sup.1 and X.sup.2 are each hydrogen or a protecting group; and Y is(a) --(CH.dbd.CH).sub.n Z in which n is 1, 2 or 3 and Z is --CHO, --CH.sub.2 OH, --COR.sup.3, --(CH.sub.2).sub.m --COR.sup.3 or --(CH.sub.2).sub.p CH.dbd.CH(CH.sub.2).sub.q --COR.sup.3 in which m is an integer of 1 to 12, p is an integer of 1 to 4, q is an integer of 1 to 10 and R.sup.3 is (i) --OH or (ii) --NR.sup.4 R.sup.5 where R.sup.4 and R.sup.5 are each hydrogen, C.sub.1-4 alkyl or optionally substituted phenyl, or R.sup.4 and R.sup.5 together with the nitrogen atom to which they are attached form a morpholino, pyrrolidinyl or piperidino ring,(b) --CH.dbd.NR.sup.6 in which R.sup.6 is (i) --OH, (ii) C.sub.1-12 alkyl optionally substituted by --OH, --COOH or --NR.sup.7 R.sup.8 where R.sup.7 and R.sup.8 are each hydrogen or C.sub.1-4 alkyl, (iii) optionally substituted phenyl or (iv) --NR.sup.9 R.sup.10 in which R.sup.9 is hydrogen and R.sup.10 is optionally substituted phenyl or C.sub.1-4 alkyl CO--, or in which R.sup.9 and R.sup.10 together with the nitrogen atom to which they are attached form a morpholino, pyrrolidinyl or piperidino ring,(c) --CH.sub.2 NHR.sup.11 in which R.sup.11 is C.sub.1-12 alkyl optionally substituted with hydroxy or carboxy or optionally substituted phenyl, or(d) --CHOHR.sup.12 or ##STR2## in which R.sup.12 is hydrogen or C.sub.1-12 alkyl; and lactones, salts and esters thereof; provided that when one of R.sup.1 and R.sup.2 is hydrogen and the other is C.sub.1-12 alkyl, Y is --(CH.dbd.CH).sub.n Z, n is 1 and Z is --COOH only salts are included.The compounds have pharmaceutical activity.

摘要翻译： 其中R 1和R 2各自为氢，C 1-12烷基或C 2-12烯基，R 1和R 2中的至少一个为C 1-12烷基或C 2-12链烯基; X1和X2各自为氢或保护基; 并且Y是（a） - （CH = CH）nZ，其中n是1,2或3，Z是-CHO，-CH 2 OH，-COR 3， - （CH 2）m -CON 3或 - （CH 2）p CH = CH CH 2）q-COR 3，其中m为1至12的整数，p为1至4的整数，q为1至10的整数，R 3为（i）-OH或（ii）-NR 4 R 5，其中R 4和 R5分别是氢，C1-4烷基或任选取代的苯基，或者R4和R5与它们所连接的氮原子一起形成吗啉代，吡咯烷基或哌啶子基环，（b）-CH = NR6，其中R6是（i ）-OH，（ii）任选被-OH，-COOH或-NR 7 R 8取代的C 1-12烷基，其中R 7和R 8各自为氢或C 1-4烷基，（iii）任选取代的苯基或（iv）-NR 9 R 10，其中R 9 是氢，R 10是任选取代的苯基或C 1-4烷基CO-，或者其中R 9和R 10与它们所连接的氮原子一起形成吗啉代，吡咯烷基或哌啶子基环，（c）-CH 2 NHR 11，其中R 11是 任选被羟基或羧基或任选取代的苯基取代的C 1-12烷基，或（d）-CHOH R12或其中R12是氢或C1-12烷基; 及其内酯，其盐和酯; 条件是当R1和R2中的一个是氢而另一个是C 1-12烷基时，Y是 - （CH = CH）nZ，n是1，Z是-COOH，只包括盐。 这些化合物具有药物活性。

公开(公告)号：US4596676A

公开(公告)日：1986-06-24

申请号：US593442

申请日：1984-03-26

申请人： George J. Cullinan

发明人： George J. Cullinan

IPC分类号： A61K31/475 ,  A61P35/00 ,  C07D519/04 ,  C07K15/00

CPC分类号： C07D519/04 ,  Y02P20/55 ,  Y10S530/816

摘要： Bifunctional ester derivatives at C-4 carbon of dimeric indole-dihydroindole alkaloids; e.g., VLB 4-hemisuccinate.

摘要翻译： 二聚吲哚二氢吲哚生物碱C-4碳的双官能酯衍生物; 例如VLB 4-半琥珀酸盐。

公开(公告)号：US4595540A

公开(公告)日：1986-06-17

申请号：US543196

申请日：1983-10-19

申请人： John Goldsworthy ,  Winston S. Marshall ,  John P. Verge

发明人： John Goldsworthy ,  Winston S. Marshall ,  John P. Verge

IPC分类号： A61K31/41 ,  A61P11/00 ,  A61P37/08 ,  C07C67/00 ,  C07C313/00 ,  C07C315/02 ,  C07C317/24 ,  C07C317/44 ,  C07C323/22 ,  C07C323/56 ,  C07C323/62 ,  C07C323/65 ,  C07C325/00 ,  C07C331/10 ,  C07D257/04 ,  C07C121/76 ,  C07C161/02

CPC分类号： C07D257/04

摘要： There are described compounds of the formula ##STR1## in which R.sup.1 is hydrogen or C.sub.1-6 alkyl, R.sup.2 is hydrogen, C.sub.1-6 alkyl or C.sub.3-6 alkenyl, X and Y are each oxygen, sulphur, sulphinyl or sulphonyl, n is 2 to 6 and Z is 1H-tetrazol-5-yl, 1H-tetrazol-5-ylthio, 1H-tetrazol-5-ylsulphinyl, 1H-tetrazol-5-ylsulphonyl, cyano or thiocyano, provided that when both X and Y are oxygen Z is 1H-tetrazol-5-ylthio, 1H-tetrazol-5-ylsulphinyl, 1H-tetrazol-5-ylsulphonyl or thiocyano; and salts thereof. The compounds in which Z is other than cyano or thiocyano have pharmaceutical activity and inhibit leukotriene action or formation. '

摘要翻译： 描述了式（I）的化合物，其中R 1是氢或C 1-6烷基，R 2是氢，C 1-6烷基或C 3-6烯基，X和Y各自是氧，硫，亚磺酰基或磺酰基，n是 2〜6，Z为1H-四唑-5-基，1H-四唑-5-基硫基，1H-四唑-5-基亚磺酰基，1H-四唑-5-基磺酰基，氰基或硫氰基，条件是当X和Y均为 氧Z是1H-四唑-5-基硫基，1H-四唑-5-基亚磺酰基，1H-四唑-5-基磺酰基或硫氰基; 及其盐。 其中Z不同于氰基或硫氰酸的化合物具有药物活性并抑制白三烯作用或形成。

公开(公告)号：US4532257A

公开(公告)日：1985-07-30

申请号：US556473

申请日：1983-11-30

申请人： Stephen R. Baker ,  Terry D. Lindstrom ,  William B. Jamieson ,  William J. Ross

发明人： Stephen R. Baker ,  Terry D. Lindstrom ,  William B. Jamieson ,  William J. Ross

IPC分类号： C07D307/83 ,  A61K31/34

CPC分类号： C07D307/83

摘要： There are described compounds of the formula ##STR1## in which either R.sup.1 and R.sup.2 are both hydrogen or R.sup.1 is carboxyl and R.sup.2 is hydrogen, C.sub.3-4 alkenyl or C.sub.1-4 alkyl, and R.sup.3, R.sup.4 and R.sup.5 are each hydrogen, nitro, hydroxyl, carboxyl, carboxyC.sub.1-2 alkoxy, C.sub.3-4 alkenyl, C.sub.1-4 alkyl, C.sub.3-4 alkenyloxy, C.sub.1-4 alkoxy or the group ##STR2## where R.sup.6 and R.sup.7 are each hydrogen or C.sub.1-4 alkyl; and salts and esters thereof. The compounds are indicated for use in the treatment of immediate sensitivity reactions and inflammatory diseases.

摘要翻译： 描述了式“IMAGE”的化合物，其中R1和R2都是氢或R1是羧基，R2是氢，C3-4链烯基或C1-4烷基，R3，R4和R5各自是氢，硝基，羟基， 羧基，羧基C 1-2烷氧基，C 3-4烯基，C 1-4烷基，C 3-4烯氧基，C 1-4烷氧基或基团，其中R 6和R 7各自为氢或C 1-4烷基; 及其盐和酯。 该化合物用于治疗立即敏感反应和炎性疾病。