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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

US06339092B1 Metalloprotease inhibitors 失效
标题翻译：金属蛋白酶抑制剂
公开(公告)号：US06339092B1
公开(公告)日：2002-01-15
申请号：US09608240
申请日：2000-06-30
申请人： Guillaume de Nanteuil , Alain Benoist , Jacqueline Bonnet , Massimo Sabatini , Ghanem Atassi , Alain Pierre
发明人： Guillaume de Nanteuil , Alain Benoist , Jacqueline Bonnet , Massimo Sabatini , Ghanem Atassi , Alain Pierre
IPC分类号： A61K31435
CPC分类号： C07D491/04
摘要： A compound selected from those of the formula (I): wherein: R1 represents hydrogen or halogen, or alkyl or alkoxy, R2 represents hydroxy, alkoxy or —NHOH, Ar1 represents phenylene or biphenylene, X represents oxygen or sulphur, NR, —C≡C— or a bond, R represents hydrogen or alkyl, n is an integer from 0 to 6 inclusive, Ar2 represents any one of the groups as defined in the description, its isomers and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same which are useful as metalloprotease inhibitors.
摘要翻译：选自式（I）的化合物：其中：R1表示氢或卤素，或烷基或烷氧基，R2表示羟基，烷氧基或-NHOH，Ar1表示亚苯基或亚联苯基，X表示氧或硫，NR，-C = C-或键，R表示氢或烷基，n为0至6的整数，Ar2表示在说明书中定义的基团中的任何一个，其异构体和与药学上可接受的酸或碱的加成盐，以及含有该金属蛋白酶抑制剂的药物。

4. 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。

5. 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。

6. 发明授权

US5391569A New chromene compounds having a triene side chain 失效
标题翻译：具有三烯侧链的新的色烯化合物
公开(公告)号：US5391569A
公开(公告)日：1995-02-21
申请号：US127804
申请日：1993-09-28
申请人： Jean-Daniel Brion , Guillaume Le Baut , Guillaume Poissonnet , Lucy De Montarby , Larbi Belachmi , Jacqueline Bonnet , Massimo Sabatini , Charles Tordjman
发明人： Jean-Daniel Brion , Guillaume Le Baut , Guillaume Poissonnet , Lucy De Montarby , Larbi Belachmi , Jacqueline Bonnet , Massimo Sabatini , Charles Tordjman
IPC分类号： A61K31/35 , A61K31/352 , A61K31/66 , A61P3/00 , A61P19/10 , A61P29/00 , A61P43/00 , C07D311/12 , C07D311/14 , C07D311/16 , C07D311/18 , C07D311/58 , C07D311/64 , C07D311/70 , C07D311/72 , C07D405/04 , C07D409/04 , C07F9/655 , A61K31/40 , A61K31/445 , A61K31/47
CPC分类号： C07D405/04 , C07D311/58 , C07D311/64 , C07D311/70 , C07D409/04
摘要： A compound selected from those of formula (I): ##STR1## in which the groups R.sub.1 to R.sub.8 are as defined the description. Medicaments.
摘要翻译：选自式（I）的化合物：其中基团R1至R8如说明书所定义。药剂

7. 发明授权

US5703074A Thiophene compounds 失效
标题翻译：噻吩化合物
公开(公告)号：US5703074A
公开(公告)日：1997-12-30
申请号：US771035
申请日：1996-12-20
申请人： Michel Wierzbicki , Frederic Sauveur , Marie-Francoise Boussard , Jacqueline Bonnet , Massimo Sabatini
发明人： Michel Wierzbicki , Frederic Sauveur , Marie-Francoise Boussard , Jacqueline Bonnet , Massimo Sabatini
IPC分类号： A61K31/495 , A61K31/535 , A61P3/00 , A61P19/10 , A61P43/00 , C07D333/20 , C07D413/06
CPC分类号： C07D333/20
摘要： Thiophene compounds of formula: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are as defined in the description, and salts thereof with appropriate acids. Those compounds and their physiologically tolerable salts can be used as medicaments in the treatment of pathologies characterized by a loss of bone tissue.
摘要翻译：下式的噻吩化合物：其中R 1，R 2和R 3如说明书中所定义，及其与适当的酸的盐。那些化合物及其生理上可耐受的盐可用作药物，用于治疗特征在于骨组织丢失的病态。

8. 发明授权

US5670535A Thiophene compounds 失效
标题翻译：噻吩化合物
公开(公告)号：US5670535A
公开(公告)日：1997-09-23
申请号：US618969
申请日：1996-03-20
申请人： Michel Wierzbicki , Marie-Fran.cedilla.oise Boussard , Jacqueline Bonnet , Massimo Sabatini , Philippe Pastoureau
发明人： Michel Wierzbicki , Marie-Fran.cedilla.oise Boussard , Jacqueline Bonnet , Massimo Sabatini , Philippe Pastoureau
IPC分类号： A61K31/38 , A61K31/381 , A61K31/495 , A61P3/00 , A61P19/10 , A61P43/00 , C07D333/22 , C07D411/06
CPC分类号： C07D333/22
摘要： The invention provides new compounds pertaining to the class of: 2-(aminocarbonylalkylcarbonyl)-5-phenylalkyllthiophene, enantiomers and physiologically tolerable salts thereof. For example: 5-�4-(4-methylphenyl)butyl-2-{3,3-dimethyl-4-�N'-(2,3,4-trimethoxybenzyl)-N-piperazinylcarbonyl!butyryl}thiophene is described. Medicinal products containing the same are useful in the treatment of any pathology involving bone hyper-resorption.
摘要翻译：本发明提供了关于下列类别的新化合物：2-（氨基羰基烷基羰基）-5-苯基烷基噻吩，其对映异构体和其生理上可耐受的盐。例如：5- [4-（4-甲基苯基）丁基-2- {3,3-二甲基-4- [N' - （2,3,4- trim + E，acu e + EE羟基苄基）-N- 哌嗪基羰基]丁酰基}噻吩。含有该药物的药物可用于治疗涉及骨超吸收的任何病理学。

9. 发明授权

US5408041A Process of purifying antler-derived bone growth factors 失效
标题翻译：纯化鹿茸骨生长因子的方法
公开(公告)号：US5408041A
公开(公告)日：1995-04-18
申请号：US180572
申请日：1994-01-13
申请人： Gregory R. Mundy , Gloria E. Gutierrez , Ian R. Garrett , Massimo Sabatini , Elzbieta Izbicka , Wilson Burgess , Gregg R. Crumley , Clarence C. Morse , Timothy R. Arnett
发明人： Gregory R. Mundy , Gloria E. Gutierrez , Ian R. Garrett , Massimo Sabatini , Elzbieta Izbicka , Wilson Burgess , Gregg R. Crumley , Clarence C. Morse , Timothy R. Arnett
IPC分类号： C12N15/09 , A61K35/32 , A61K38/00 , A61K38/22 , A61K39/395 , A61P3/00 , A61P43/00 , C07K1/16 , C07K1/20 , C07K1/22 , C07K14/51 , C07K14/65 , C07K16/00 , C07K16/22 , C12P21/02 , C07K1/00 , C07K3/00 , C07K15/00
CPC分类号： C07K14/65 , C07K14/51 , C07K16/22 , A61K38/00
摘要： The present invention relates to the development of bone growth factors as therapeutics for the prevention and treatment of pathological conditions involving bone tissue. The present invention provides biologically active proteinaceous factors comprising polypeptides containing the amino acid sequence M-A-G-L-G-D-E-F-G-D, [SEQ ID NO: 1], (X) F E T L F G A/V E D V I/D A L Q F V C G D, [SEQ ID NO: 2], or A-Y-I-P-I-E-T-L-E-G-I/G-E-L-V-D/Q-T-G/L-Q-F, [SEQ ID NO: 3], or biologically active fragments or sequence analogues thereof. Among the biological properties of the proteinaceous materials of the present invention is the capability to promote the growth and/or differentiation of osteoblastic cells.
摘要翻译：本发明涉及作为预防和治疗涉及骨组织的病理状况的治疗剂的骨生长因子的发展。本发明提供包含含有氨基酸序列MAGLGDEFGD，[SEQ ID NO：1]，（X）FETLFGA / VEDVI / DALQFVCGD，[SEQ ID NO：2]或AYIPIETLEGI / GELVD / QTG / LQF的多肽的生物活性蛋白质因子，[SEQ ID NO：3]或其生物活性片段或序列类似物。本发明的蛋白质材料的生物学特性是促进成骨细胞生长和/或分化的能力。

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