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1. 发明授权

US5866587A Metalloprotease inhibitors 失效
标题翻译：金属蛋白酶抑制剂
公开(公告)号：US5866587A
公开(公告)日：1999-02-02
申请号：US842982
申请日：1997-04-25
申请人： Guillaume de Nanteuil , Joseph Paladino , Georges Remond , Ghanem Atassi , Alain Pierre , Gordon Tucker , Jacqueline Bonnet , Massimo Sabatini
发明人： Guillaume de Nanteuil , Joseph Paladino , Georges Remond , Ghanem Atassi , Alain Pierre , Gordon Tucker , Jacqueline Bonnet , Massimo Sabatini
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61K31/435 , A61K31/47 , A61K31/472 , A61K31/473 , A61P9/10 , A61P29/00 , A61P35/00 , A61P43/00 , C07D209/42 , C07D217/26 , C07D221/08 , C07D221/10 , C07D471/04 , C07D491/04 , C07D491/048 , C07D495/04
CPC分类号： C07D471/04 , C07D209/42 , C07D217/26 , C07D221/10 , C07D491/04 , C07D495/04
摘要： Compound of formula (I): ##STR1## in which: m, n, which are identical or different, represent 0, 1 or 2,R.sub.1, R.sub.2, which are identical or different, represent hydrogen, optionally substituted alkyl, aryl, or form with the carbon atom carrying them carbonyl or (C.sub.3 -C.sub.7)cycloalkyl,R.sub.3 represents hydrogen, alkyl, hydroxyl or aryl,R.sub.4 represents any of the groups as defined in the description,X represents --SO.sub.2 --, --CO-- or --SO.sub.2 NH--,R.sub.5 represents optionally substituted alkyl, (C.sub.3 -C.sub.7)cycloalkyl, aryl or heterocyclic,A represents an aryl ring or a heterocycle,its isomers as well as its addition salts with a pharmaceutically acceptable acid or base and medicinal products containing the same are useful as metalloprotease inhibitors.
摘要翻译：式（I）化合物：其中：m，n相同或不同，表示0,1或2，相同或不同的R 1，R 2表示氢，任选取代的烷基，芳基或与其中带有羰基或（C3-C7）环烷基的碳原子形成，R3表示氢，烷基，羟基或芳基，R4表示说明中定义的任何基团，X表示-SO 2 - ， - 或-SO 2 NH-，R 5表示任选取代的烷基，（C 3 -C 7）环烷基，芳基或杂环，A表示芳基环或杂环，其异构体以及其与药学上可接受的酸或碱的加成盐和含有这同样可用作金属蛋白酶抑制剂。

2. 发明授权

US6066633A Metalloproteinase inhibitors 失效
标题翻译：金属蛋白酶抑制剂
公开(公告)号：US6066633A
公开(公告)日：2000-05-23
申请号：US191323
申请日：1998-11-13
申请人： Guillaume De Nanteuil , Georges Remond , Joseph Paladino , Ghanem Atassi , Alain Pierre , Gordon Tucker , Jacqueline Bonnet , Massimo Sabatini
发明人： Guillaume De Nanteuil , Georges Remond , Joseph Paladino , Ghanem Atassi , Alain Pierre , Gordon Tucker , Jacqueline Bonnet , Massimo Sabatini
IPC分类号： A61K31/00 , A61K31/435 , A61K31/4353 , A61K31/437 , A61P9/00 , A61P9/10 , A61P29/00 , A61P35/00 , A61P43/00 , C07D471/04 , A61K31/5377 , A61K31/4523 , C07D487/44
CPC分类号： C07D471/04
摘要： Compound of formula (I): ##STR1## in which: m represents an integer from 1 to 4 inclusive, and n and p an integer from 0 to 4 inclusive,X represents O, S or a single bond,R.sub.1 represent hydrogen or halogen, or alkyl, alkoxy, hydroxy, trihaloalkyl or trihaloalkoxy,R.sub.2, R.sub.3 and R.sub.4, which may be same or different, each represents hydrogen or alkyl,R.sub.5 represents hydrogen or halogen, or alkoxy, aryloxy or heteroaryloxy,R.sub.6, R.sub.7 and R.sub.8, which may be same or different, each represents hydrogen or alkyl, or together form, with the atoms carrying them respectively, an optionally substituted heterocycle,R.sub.9 represents SO.sub.3 H, --CO.sub.2 R.sub.10, --CO--NR.sub.11 R.sub.12, or --NR.sub.13 R.sub.14, wherein R.sub.10, R.sub.11, R.sub.12, R.sub.13 and R.sub.14 each represents hydrogen or alkyl or together (R.sub.11 /R.sub.12 ; R.sub.13 /R.sub.14) form, with nitrogen carrying them, heterocycle,isomers thereof, and addition salts thereof with a pharmaceutically-acceptable acid or base.
摘要翻译：式（I）的化合物：其中：m表示1〜4的整数，n和p为0〜4的整数，X表示O，S或单键，R 1表示氢或卤素，或烷基，烷氧基，羟基，三卤代烷基或三卤代烷氧基，可以相同或不同的R 2，R 3和R 4各自表示氢或烷基，R 5表示氢或卤素，或烷氧基，芳氧基或杂芳氧基，R 6，R 7和R 8，其可以是相同或不同，各自表示氢或烷基，或与分别携带它们的原子一起形成任选取代的杂环，R 9表示SO 3 H，-CO 2 R 10，-CO-NR 11 R 12或-NR 13 R 14，其中R 10，R 11，R 12，R 13 和R 14各自表示氢或烷基或一起（R 11 / R 12; R 13 / R 14），带有氮的杂环，杂环，异构体及其与药学上可接受的酸或碱的加成盐。

3. 发明授权

US06605604B1 Carboxylic and hydroxamic acid compounds inhibiting metalloproteases, method for preparing same and pharmaceutical compositions containing them 失效
标题翻译：抑制金属蛋白酶的羧酸和异羟肟酸化合物，其制备方法和含有它们的药物组合物
公开(公告)号：US06605604B1
公开(公告)日：2003-08-12
申请号：US09720850
申请日：2000-12-26
申请人： Patrick Casara , Anne Marie Chollet , Thierry Le Diguarher , Ghanem Atassi , Jacqueline Bonnet , Alain Pierre , Massimo Sabatini , Gordon Tucker , Nicolas Guilbaud
发明人： Patrick Casara , Anne Marie Chollet , Thierry Le Diguarher , Ghanem Atassi , Jacqueline Bonnet , Alain Pierre , Massimo Sabatini , Gordon Tucker , Nicolas Guilbaud
IPC分类号： C07D20948
CPC分类号： C07D209/48 , C07C233/82 , C07C259/10 , C07C311/29 , C07D231/22 , C07D237/32 , C07D239/96 , C07D253/08 , C07D275/06 , C07D403/12 , C07D409/12 , C07D471/04
摘要： The invention concerns a compound of formula (I) wherein: n is equal to 0 or 1; R1, R2, R3, R4 represent a hydrogen or an alkyl group, or R1 and R3 together form a cycloalkyl group; R5 represents a hydrogen, an alkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl, hetereoalkylalkyl, hetereocycloalkyl, hetereocycloalkylalkyl group (all optionally substituted), or a —CO—R6 group; and R6 represents R7 or OR7 or NR7R8, with R7 representing an aryl, arylalkyl, heteroaryl or heteroarylalkyl, heterocycloalkyl, heterocycloalkylalkyl group (all optionally substituted), and R8 representing an alkyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl (all optionally substituted); or R5 and R6 form with the nitrogen atom and the Z group bearing them a saturated monocyclic, bicyclic or tricyclic group, partially unsaturated or unsaturated, with 5 to 16 chain links containing 1 to 7 heteroatoms and optionally substituted; R10 represents a hydrogen atom or a hydroxy group, and in the latter case R1, R2, R3, R4 are independently selected among hydrogen and alkyl; Z represents a hydroxy, alkoxy, alkenyloxy, benzyloxy group or a NH—OR group; X represents a sulphur, a SO, SO2 group (in those cases where R3 and R4 are different from an alkyl) or a group —CO—O— (in which case R1 and R3 form a cycloalkyl group), or X represents an oxygen atom; W represents a W1—(A)p or W1—B—W2—(A)p group wherein W1 and W2 represent an aryl or heteroaryl group, A is a standard substituent of aromatic cycles, B a bond, an oxygen or an alkylene, alkenylene, alkynylene group, and p is an integer ranging between 0 and 5; T1 and T2 represent a bond or an alkylene, alkenylene, or alkynylene group. The invention is useful for preparing medicines.
摘要翻译：本发明涉及式（I）的化合物，其中：n等于0或1; R1，R2，R3，R4表示氢或烷基，或R1和R3一起形成环烷基; R5代表氢，烷基，环烷基，环烷基烷基，芳基，芳烷基，杂芳基，杂芳烷基烷基，杂三环烷基，杂三环烷基烷基（全部任意取代）或-CO-R 6基团; 并且R 6表示R 7或OR 7或NR 7 R 8，其中R 7表示芳基，芳基烷基，杂芳基或杂芳基烷基，杂环烷基，杂环烷基烷基（全部被取代），R 8表示烷基，芳基，芳基烷基，杂芳基或杂芳基烷基（全部被取代）或R 5和R 6与氮原子一起形成，Z基团带有饱和的单环，双环或三环基团，部分不饱和或不饱和的，具有5至16个含有1至7个杂原子和任选取代的链节; R 10表示氢原子或羟基，在后一种情况下，R 1，R 2，R 3，R 4独立地选自氢和烷基; Z表示羟基，烷氧基，烯氧基，苄氧基或NH-OR基; X表示硫，SO，SO 2基（在那些R3和R4不同于烷基的情况下）或基团-CO-O-（在这种情况下，R1和R3形成环烷基），或X表示氧原子; W表示W1-（A）p或W1-B-W2-（A）p基团，其中W1和W2表示芳基或杂芳基，A是芳族环的标准取代基，B a键，氧或亚烷基亚烯基，亚炔基，p为0〜5的整数。 T1和T2表示键或亚烷基，亚烯基或亚炔基。本发明可用于制备药物。

4. 发明授权

US06686348B2 Metalloprotease inhibitors 失效
标题翻译：金属蛋白酶抑制剂
公开(公告)号：US06686348B2
公开(公告)日：2004-02-03
申请号：US10036689
申请日：2001-12-21
申请人： Guillaume De Nanteuil , Alain Benoist , Philippe Pastoureau , Massimo Sabatini , John Hickman , Alain Pierre , Gordon Tucker
发明人： Guillaume De Nanteuil , Alain Benoist , Philippe Pastoureau , Massimo Sabatini , John Hickman , Alain Pierre , Gordon Tucker
IPC分类号： A61K3133
CPC分类号： C07D417/14 , C07D405/14 , C07D491/04
摘要： A compound of formula (I): wherein: R1 represents hydrogen, halogen, alkyl or alkoxy, X represents oxygen, sulphur or NR wherein R represents hydrogen or alkyl, A represents any one of the groups described in the description, their isomers and addition salts thereof with a pharmaceutically acceptable acid or base and medicinal products containing the same are useful as metalloprotease inhibitor.
摘要翻译：式（I）的化合物：其中：R1表示氢，卤素，烷基或烷氧基，X表示氧，硫或NR，其中R表示氢或烷基，A表示说明书中所述的任何一种基团，其异构体和加成其与药学上可接受的酸或碱的盐和含有它们的药物可用作金属蛋白酶抑制剂。

5. 发明授权

US06846833B2 Vitronectin receptor antagonist bicyclic compounds, preparation method and compositions containing same 失效
标题翻译： Vitronectin受体拮抗剂双环化合物，制备方法和含有它们的组合物
公开(公告)号：US06846833B2
公开(公告)日：2005-01-25
申请号：US10220755
申请日：2001-03-06
申请人： Patrick Casara , Françoise Perron-Sierra , Ghanem Atassi , Gordon Tucker , Dominique Saint-Dizier
发明人： Patrick Casara , Françoise Perron-Sierra , Ghanem Atassi , Gordon Tucker , Dominique Saint-Dizier
IPC分类号： C07D233/24 , A61K31/4164 , A61K31/4168 , A61K31/417 , A61K31/4184 , A61K31/426 , A61K31/4375 , A61K31/44 , A61K31/4402 , A61K31/505 , A61K31/55 , A61P9/00 , A61P19/10 , A61P27/02 , A61P29/00 , A61P33/14 , A61P35/00 , A61P43/00 , C07D213/36 , C07D213/74 , C07D223/04 , C07D223/12 , C07D233/48 , C07D233/54 , C07D235/10 , C07D235/14 , C07D235/30 , C07D239/14 , C07D277/18 , C07D277/20 , C07D277/42 , C07D401/12 , C07D403/12 , C07D471/04 , C07D211/72 , C07D235/22 , C07D239/02 , C07D267/02
CPC分类号： C07D213/74 , C07D223/12 , C07D233/64 , C07D235/14
摘要： Compounds of formula (1): wherein: G represents an optionally substituted phenyl or optionally substituted heterocycle, G1 and G2 being N or C, T1 represents —CH2—CH2—, —CH═CH— or ═CH—CH2—, and T2 is a bond, or T1 represents —CH2— or ═CH— and T2 is —CH2—, ═CH—, R5 represents —(CH2)m—COOR6, R6 and R6′ represent hydrogen, alkyl, optionally substituted aryl or optionally substituted arylalkyl, A represents —CO—, —CH2—, ═CH— or —CH═ and W represents —CH—, ═C— or —C═, or A represents —CO— or —CH2— and W represents N, X represents —CO—X1—, —CO—NR6—X1—, —NR6—CO—X1—, —O—X1—, —SO2—NR6—X1— or —S(O)n—X1—, Y represents —Y1—, —Y2—Y1— or —Y1—Y2—Y1—, Y1 being an alkylene, alkenylene or alkynylene, and Y2 being an arylene, heteroarylene, cycloalkylene or heterocycloalkylene, Z represents —Z1—, —Z10—NR6—, and —Z10—NR6—CO—, Z1 being a heteroaryl, heterocycloalkyl, heteroarylalkyl, heterocycloalkylalkyl, fused arylheteroaryl, fused arylheterocycloalkyl, fused heteroarylheterocycloalkyl, fused heterocycloalkylheteroaryl or fused heteroarylheteroaryl, each of which is optionally substituted, or a group, Z2—NR6 or Z2—NR6—CO, Z2 being a group Z1, alkyl or heteroalkyl, and Z10 represents Z1 or an alkyl, its enantiomers, diastereoisomers, and addition salts thereof with a pharmaceutically acceptable acid or base, and medicinal products containing the same which are useful as vitronectin receptor antagonists.
摘要翻译：式（1）的化合物：其中：G表示任选取代的苯基或任选取代的杂环，G 1和G 2是N或C，T 1表示-CH 2 -CH 2 - ， - CH = CH-或= CH-CH 2 - ，和T 2 或者T 1表示-CH 2 - ，= CH-，R 5表示 - （CH 2）m -COOR 6，R 6和R 6'表示氢，烷基，任选取代的芳基或任意取代的芳基烷基，A表示-CO-，-CH 2 - ，= CH-或-CH =，W表示-CH-，= C-或-C =，或A表示-CO-或-CH 2 - ，W表示N，X 表示-CO-X1-，-CO-NR6-X1-，-NR6-CO-X1，-O-X1-，-SO2-NR6-X1-或-S（O）n-X1-，Y表示 - Y1-，-Y2-Y1-或-Y1-Y2-Y1-，Y1为亚烷基，亚烯基或亚炔基，Y2为亚芳基，亚杂芳基，亚环烷基或亚杂环烷基，Z表示-Z1，-Z10-NR6-，和-Z10-NR6-CO-，Z1是杂芳基，杂环烷基，杂芳基烷基，杂环烷基烷基，稠合芳基杂芳基，稠合芳基杂环烷基，稠合杂芳基杂环烷基，稠合杂环烷基或者Z 2 -NR 6或Z 2 -NR 6 -CO，Z 2为基团Z 1，烷基或杂烷基，Z 10表示Z 1或烷基，其对映异构体，非对映异构体和加成物的基团其与药学上可接受的酸或碱的盐，以及含有它们的药物，可用作玻连蛋白受体拮抗剂。

6. 发明授权

US6063816A Hydroxamic acid compounds 失效
标题翻译：羟肟酸化合物
公开(公告)号：US6063816A
公开(公告)日：2000-05-16
申请号：US370712
申请日：1999-08-09
申请人： Stephen Hanessian , Ghanem Atassi , Gordon Tucker , Daniel-Henri Caignard , Pierre Renard
发明人： Stephen Hanessian , Ghanem Atassi , Gordon Tucker , Daniel-Henri Caignard , Pierre Renard
IPC分类号： C12N9/99 , A61K31/18 , A61K31/185 , A61K31/35 , A61K31/351 , A61K31/4406 , A61K31/4418 , A61K31/445 , A61P43/00 , C07C319/14 , C07C319/20 , C07C323/60 , C07D211/20 , C07D213/34 , C07D309/04 , A01N37/28 , A01K31/19 , A01N43/40 , C07C259/04 , C07D211/32
CPC分类号： C07C323/60
摘要： A compound selected from those of formula (I): ##STR1## wherein: R.sub.1 represents optionally substituted alkyl, acyl, cycloalkyl, aryl, aminocarbonylalkyl, or heterocycle,R.sub.2 represents alkylene,R.sub.3 represents X or Y as defined in the description,R.sub.4 represents--either alkyl, cycloalkyl, aryl, arylalkyl, cycloalkylalkyl, heterocycloalkylene, or heterocycle when R.sub.3 represents Y, or biaryl, arylheteroaryl or heteroarylaryl, when R.sub.3 represents X or Y,their isomers and also pharmaceutically-acceptable acid or base addition salts thereof, and medicinal products containing the same which are useful as metalloprotease inhibitors in the treatment of cancers.
摘要翻译：酰基，环烷基，芳基，氨基羰基烷基或杂环，R 2表示亚烷基，R 3表示如说明书中所定义的X或Y，R 4表示 - 烷基，当R 3表示Y时，环烷基，芳基，芳基烷基，环烷基烷基，杂环亚烷基或杂环，或当R 3表示X或Y时，联芳基，芳基杂芳基或杂芳基芳基，它们的异构体及其药学上可接受的酸或碱加成盐，它们在金属蛋白酶抑制剂治疗癌症中是有用的。

7. 发明授权

US06638962B2 Cycloheptene compounds 失效
标题翻译：环庚烯化合物
公开(公告)号：US06638962B2
公开(公告)日：2003-10-28
申请号：US10050666
申请日：2002-01-16
申请人： Patrick Casara , Thierry Le Diguarher , Gilbert Dorey , John Hickman , Alain Pierre , Gordon Tucker , Nicolas Guilbaud
发明人： Patrick Casara , Thierry Le Diguarher , Gilbert Dorey , John Hickman , Alain Pierre , Gordon Tucker , Nicolas Guilbaud
IPC分类号： A61K314174
CPC分类号： C07D233/64 , A61K31/4164 , C07D213/38 , C07D401/06
摘要： Compound of formula (I): wherein: X represents a bond or alkylene, CO, S(O)n, —S(O)n—A1—, —CO—A1—, —A—S(O)n—A′1— or —A1—CO—A′1—, Y represents aryl, heteroaryl, cycloalkyl or heterocycloalkyl, each unsubstituted or substituted, R1, R2, R3 and R4 each independently of the others represent hydrogen or aryl, heteroaryl, cycloalkyl or heterocycloalkyl, each unsubstituted or substituted, or R1, R2, R3 and R4, taken in pairs, together form a bond, or form a fused benzene ring or a fused aromatic or partially unsaturated heterocycle, T represents —CH(R5)—, —N(R5)— or —N(R5)CO—, V represents hydrogen or unsubstituted or substituted aryl or heteroaryl, A2 represents [C(R6)(R′6)]p, R7 and R8 are as defined in the description, their isomers and addition salts thereof with a pharmaceutically acceptable acid or base and medicinal products containing the same are useful as farnesyl transferase inhibitors.
摘要翻译：式（I）的化合物：其中：X表示键或亚烷基，CO，S（O）n，-S（O）n -A1，-CO-A1-，-AS（O）n-A'1 - 或-A1-CO-A'1-，Y表示芳基，杂芳基，环烷基或杂环烷基，每个未取代或取代的，R 1，R 2，R 3和R 4各自独立地表示氢或芳基，杂芳基，环烷基或杂环烷基，每个未取代或取代的或R 1，R 2，R 3和R 4成对取代，一起形成键，或形成稠合苯环或稠合芳族或部分不饱和杂环，T表示-CH（R 5） - ， - N（ R5） - 或-N（R5）CO-，V表示氢或未取代或取代的芳基或杂芳基，A2表示[C（R6）（R'6）] p，R7和R8如说明书中所定义，并且其与药学上可接受的酸或碱的加成盐和含有它们的药物可用作法呢基转移酶抑制剂。

8. 发明授权

US09278143B2 Imaging agents, process for the preparation thereof and pharmaceutical compositions containing same 有权
标题翻译：成像剂，其制备方法和含有其的药物组合物
公开(公告)号：US09278143B2
公开(公告)日：2016-03-08
申请号：US14232163
申请日：2012-07-12
申请人： Alain Lepape , Stéphanie Lerondel , Guillaume Reveillon , Jean-Marie Delbos , Luc Demuynck , Hubert Grandon , François Lefoulon , Gordon Tucker
发明人： Alain Lepape , Stéphanie Lerondel , Guillaume Reveillon , Jean-Marie Delbos , Luc Demuynck , Hubert Grandon , François Lefoulon , Gordon Tucker
IPC分类号： A61K49/00 , C07D401/12 , C07D209/60 , C07D213/74 , C07D401/14 , C07D493/10
CPC分类号： A61K49/0004 , C07D209/60 , C07D213/74 , C07D401/12 , C07D401/14 , C07D493/10
摘要： Compounds of formula (I) in which: >R is a linear or branched (C1-C6) alkyl, >L is a spacer group, >A is a diagnostic agent, and >m is equal to 1 or 2.
摘要翻译：式（I）化合物，其中：> R是直链或支链（C1-C6）烷基，> L是间隔基，> A是诊断剂，> m等于1或2。

9. 发明申请

US20140241989A1 NOVEL IMAGING AGENTS, PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME 有权
标题翻译：新型成像剂，其制备方法和含有其的药物组合物
公开(公告)号：US20140241989A1
公开(公告)日：2014-08-28
申请号：US14232163
申请日：2012-07-12
申请人： Alain Lepape , Stéphanie Lerondel , Guillaume Reveillon , Jean-Marie Delbos , Luc Demuynck , Hubert Grandon , François Lefoulon , Gordon Tucker
发明人： Alain Lepape , Stéphanie Lerondel , Guillaume Reveillon , Jean-Marie Delbos , Luc Demuynck , Hubert Grandon , François Lefoulon , Gordon Tucker
IPC分类号： A61K49/00 , C07D401/12 , C07D213/74 , C07D493/10 , C07D401/14
CPC分类号： A61K49/0004 , C07D209/60 , C07D213/74 , C07D401/12 , C07D401/14 , C07D493/10
摘要： Compounds of formula (I) in which: >R is a linear or branched (C1-C6) alkyl, >L is a spacer group, >A is a diagnostic agent, and >m is equal to 1 or 2.
摘要翻译：式（I）化合物，其中：> R是直链或支链（C1-C6）烷基，> L是间隔基，> A是诊断剂，> m等于1或2。

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