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1. 发明授权

US06667331B2 Non-peptidyl inhibitors of VLA-4 dependent cell binding useful in treating inflammatory, autoimmune, and respiratory diseases 失效
标题翻译：用于治疗炎症，自身免疫和呼吸道疾病的VLA-4依赖性细胞结合的非肽基抑制剂
公开(公告)号：US06667331B2
公开(公告)日：2003-12-23
申请号：US10171286
申请日：2002-06-12
申请人： Allen J. Duplantier , Louis S. Chupak , Anthony J. Milici , Wan F. Lau
发明人： Allen J. Duplantier , Louis S. Chupak , Anthony J. Milici , Wan F. Lau
IPC分类号： A61K314025
CPC分类号： C07D413/04 , C07C229/34 , C07C233/47 , C07C311/06 , C07D235/14 , C07D261/08
摘要： There is disclosed a genus of non-peptidyl compounds, wherein said compounds are VLA-4 inhibitors useful in treating inflammatory, autoimmune, and respiratory diseases, and wherein said compounds comprise a compound of Formula (1.0.0): and pharmaceutically acceptable salts and other prodrug derivatives thereof, wherein: A is (C1-C6) alkyl, cycloalkyl, aryl, heteroaryl or heterocyclyl as defined herein; where said alkyl, cycloalkyl, aryl, heteroaryl or heterocyclyl is optionally substituted with 0 to 3 R9; or is a member selected from the group consisiting of the following radicals: A1—NHC(═O)NH—A2—, A1—NHC(═O)O—A2—, A1—OC(═O)NH—A2—, A1—NHSO2NH—A2—, A1—NHC(═O)—A2—, A1—C(═O)NH—A2—, A1—NHSO2—A2—, A1—SO2NH—A2—, A1—(CH2)rO—A2—, A1—O(CH2)r—A2—, A1—(CH2)r—A2—, where A1 is aryl and A2 is aryl or pyridyl; where said aryl or pyridyl group is substituted with 0 to 3 R9; —B is oxazolinyl or isoxazolinyl; wherein said oxazolinyl and said isoxazolinyl may be optionally substituted with R9; R2 is hydrogen or methyl; R3 is taken together with R4 and the carbon and nitrogen atoms to which it is attached to form a pyrrolidinyl group substituted with 0 to 3 R13; and the remaining variables are as defined in the specification.
摘要翻译：公开了一种非肽基化合物，其中所述化合物是可用于治疗炎性，自身免疫性和呼吸系统疾病的VLA-4抑制剂，其中所述化合物包含式（1.0.0）化合物及其药学上可接受的盐和其中：A为本文定义的（C 1 -C 6）烷基，环烷基，芳基，杂芳基或杂环基; 其中所述烷基，环烷基，芳基，杂芳基或杂环基任选被0至3个R 9取代; 或者是选自以下基团的基团：A 1 -NHC（= O）NH-A 2 - ，A 1 -NHC（= O）OA 2 - ，A < 1 -OC（= O）NH-A 2 - ，A 1 -NHSO 2 NH-A 2 - ，A 1 -NHC（= O）-A 2 - ，A 1 -C（= O）NH-A 2 - ，A 1 -NHSO 2 -A 2 - ，A 1 -SO 2 NH-A 2 - ，A 1 - （CH 2） A 2 - ，A 1 -O（CH 2）r A 2 - ，A 1 - （CH 2）r A 2 - ，其中A 1是芳基，A 2是芳基或吡啶基其中所述芳基或吡啶基被0至3个R 9取代; -B是恶唑啉基或异恶唑啉基; 其中所述恶唑啉基和所述异唑啉基可以任选被R 9取代; R 2是氢或甲基; R 3与R 4一起并与其连接的碳原子和氮原子一起形成被0至3个R 13取代的吡咯烷基;其余的变量如本说明书中所定义。

2. 发明授权

US06451842B1 Cyclic amine derivatives and their use as drugs 失效
公开(公告)号：US06451842B1
公开(公告)日：2002-09-17
申请号：US09554562
申请日：2000-05-16
申请人： Tatsuki Shiota , Ken-ichiro Kataoka , Minoru Imai , Takaharu Tsutsumi , Masaki Sudoh , Ryo Sogawa , Takuya Morita , Takahiko Hada , Yumiko Muroga , Osami Takenouchi , Minoru Furuya , Noriaki Endo , Christine M. Tarby , Wilna Moree , Steven Teig
发明人： Tatsuki Shiota , Ken-ichiro Kataoka , Minoru Imai , Takaharu Tsutsumi , Masaki Sudoh , Ryo Sogawa , Takuya Morita , Takahiko Hada , Yumiko Muroga , Osami Takenouchi , Minoru Furuya , Noriaki Endo , Christine M. Tarby , Wilna Moree , Steven Teig
IPC分类号： A61K314025
CPC分类号： C07D207/325 , C07D207/09 , C07D207/14 , C07D207/34 , C07D207/416 , C07D209/08 , C07D209/42 , C07D211/26 , C07D211/56 , C07D211/58 , C07D213/65 , C07D213/75 , C07D213/81 , C07D213/82 , C07D231/14 , C07D231/16 , C07D235/16 , C07D239/52 , C07D249/18 , C07D261/08 , C07D263/56 , C07D263/58 , C07D271/06 , C07D285/14 , C07D307/14 , C07D307/68 , C07D317/50 , C07D317/60 , C07D319/18 , C07D333/16 , C07D333/20 , C07D333/38 , C07D333/42 , C07D333/68 , C07D401/06 , C07D401/12 , C07D405/06 , C07D405/12 , C07D407/12 , C07D409/06 , C07D409/12 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D487/04 , C07D495/04 , C07D513/04
摘要： A compound represented by the general formula (I), a pharmaceutically acceptable acid addition salt thereof or a pharmaceutically acceptable C1-C6 alkyl addition salt thereof, and their medical applications. These compounds inhibit the action of chemokines such as MIP-1&agr; and/or MCP-1 on target cells, and are useful as therapeutic and/or preventative drugs in diseases, such as atherosclerosis, rheumatoid arthritis, and the like where blood monocytes and lymphocytes infiltrate into tissues.

3. 发明授权

US06211225B1 Heterocyclic aminopyrrolidine derivatives as melatonergic agents 有权
标题翻译：杂环氨基吡咯烷衍生物作为褪黑激素药
公开(公告)号：US06211225B1
公开(公告)日：2001-04-03
申请号：US09587928
申请日：2000-06-06
申请人： Katherine S. Takaki , Guanglin Luo , Stephen R. Bertenshaw
发明人： Katherine S. Takaki , Guanglin Luo , Stephen R. Bertenshaw
IPC分类号： A61K314025
CPC分类号： C07D405/04
摘要： There is provided a novel series of heterocyclic aminopyrrolidine compounds of Formula I wherein R1, R2, R3, R4, W, Z and the wavy bond are as defined herein which bind to the human melatonin receptor and therefore are useful as melatonergic agents.
摘要翻译：提供了R1，R2，R3，R4，W，Z和波浪键

4. 发明授权

US06552051B2 Energetic nitramine-linked azoles and related compounds as oxidizers, initiators and gas generators 失效
标题翻译：活性硝胺连接的唑类和相关化合物作为氧化剂，引发剂和气体发生器
公开(公告)号：US06552051B2
公开(公告)日：2003-04-22
申请号：US09877319
申请日：2001-06-07
申请人： Jeffrey C. Bottaro , Robert J. Schmitt , Mark A. Petrie , Paul E. Penwell
发明人： Jeffrey C. Bottaro , Robert J. Schmitt , Mark A. Petrie , Paul E. Penwell
IPC分类号： A61K314025
CPC分类号： C07D257/04 , C06B25/34 , C07C243/02 , C07D249/10
摘要： Novel compounds are provided having the structural formula R[—N(NO2)—L—R1]n wherein R, L, R1 and n are defined herein. The compounds are useful in a variety of contexts, but are primarily to be used as high energy oxidizing agents in explosive compositions, propellant formulations, gas-generating compositions and the like. The compounds are also useful as pharmaceutical agents. Compositions containing the compounds are also provided, including energetic compositions, as are methods for using the novel compounds and compositions.
摘要翻译：提供具有结构式R [-N（NO 2）-L-R 1] n的新化合物，其中R，L，R 1和n如本文所定义。这些化合物可用于各种情况，但主要用作爆炸组合物中的高能氧化剂，推进剂制剂，产气组合物等。这些化合物也可用作药剂。还提供了含有化合物的组合物，包括能量组合物，以及使用新化合物和组合物的方法。

5. 发明授权

US06492413B2 3.4-diaryl thiophenes and analogs thereof having use as antiinflammatory agents 失效
标题翻译：具有用作抗炎剂的3,4-二芳基噻吩及其类似物
公开(公告)号：US06492413B2
公开(公告)日：2002-12-10
申请号：US09528934
申请日：2000-03-20
申请人： John J. Talley , Stephen R Bertenshaw , Paul W Collins , Thomas D. Penning , David B. Reitz , Roland S Rogers
发明人： John J. Talley , Stephen R Bertenshaw , Paul W Collins , Thomas D. Penning , David B. Reitz , Roland S Rogers
IPC分类号： A61K314025
CPC分类号： C07D307/38 , A61K31/341 , A61K31/365 , C07D307/58 , C07D333/16 , C07D333/18 , C07D333/28 , C07D333/38 , C07D409/04
摘要： A class of 3,4-diaryl substituted thiophene, furan and pyrrole derivatives and analogs thereof, pharmaceutical compositions containing them and methods of using them to treat inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I: wherein Y is selected from O, S and NR1; wherein R1 is selected from hydrido and lower alkyl; wherein X is one or two substituent selected from hydrido, halo, lower alkoxycarbonyl and carboxyl; wherein R2 and R3 are independently aryl or heteroaryl; and wherein R2 and R3 are optionally substituted at a substitutable position with one or more radicals selected from sulfamyl, alkylsulfonyl, halo, lower alkoxy and lower alkyl; or a pharmaceutically-acceptable salt thereof.
摘要翻译：一类3,4-二芳基取代的噻吩，呋喃和吡咯衍生物及其类似物，含有它们的药物组合物和使用它们治疗炎症和炎症相关疾病的方法。特别感兴趣的化合物由式I定义：其中Y选自O，S和NR1; 其中R1选自氢和低级烷基; 其中X是一个或两个选自氢，卤素，低级烷氧基羰基和羧基的取代基; 其中R2和R3独立地是芳基或杂芳基; 并且其中R2和R3任选在可取代的位置被一个或多个选自磺酰胺基，烷基磺酰基，卤素，低级烷氧基和低级烷基的基团取代; 或其药学上可接受的盐。

6. 发明授权

US06407134B1 Heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors 失效
标题翻译：杂环羰基氨基酸羟乙基氨基磺酰胺逆转录病毒蛋白酶抑制剂
公开(公告)号：US06407134B1
公开(公告)日：2002-06-18
申请号：US09775682
申请日：2001-02-05
申请人： Daniel P Getman , Gary A DeCrescenzo , John N Freskos , Michael L Vazquez , James A Sikorski , Balekudru Devadas , Srinivasan Nagarajan , David L Brown , Joseph J McDonald
发明人： Daniel P Getman , Gary A DeCrescenzo , John N Freskos , Michael L Vazquez , James A Sikorski , Balekudru Devadas , Srinivasan Nagarajan , David L Brown , Joseph J McDonald
IPC分类号： A61K314025
CPC分类号： C07K5/021 , A61K38/00 , C07K5/06139 , C07K5/06165
摘要： Selected heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.
摘要翻译：选择的杂环羰基氨基酸羟乙基氨基磺酰胺化合物作为逆转录病毒蛋白酶抑制剂是有效的，特别是作为HIV蛋白酶的抑制剂。本发明涉及这种逆转录病毒蛋白酶抑制剂，更具体地涉及所选择的新化合物，用于抑制逆转录病毒蛋白酶如人类免疫缺陷病毒（HIV）蛋白酶的组合物和方法，预防性地预防逆转录病毒感染或逆转录病毒的扩散，以及治疗逆转录病毒感染。

7. 发明授权

US06384070B2 Indole derivatives useful as endothelin receptor antagonists 失效
标题翻译：用作内皮素受体拮抗剂的吲哚衍生物
公开(公告)号：US06384070B2
公开(公告)日：2002-05-07
申请号：US09756835
申请日：2001-01-09
申请人： David James Rawson , Kevin Neil Dack , Roger Peter Dickinson , Kim James
发明人： David James Rawson , Kevin Neil Dack , Roger Peter Dickinson , Kim James
IPC分类号： A61K314025
CPC分类号： C07D405/06 , C07D209/18 , C07D405/14 , C07D409/14 , C07D413/14
摘要： Compounds of formula (I), and their pharmaceutically acceptable derivatives, wherein R1 and R2 are optional substituents and independently represent C1-6 alkyl, C2-6 alkenyl, optionally substituted by CO2H or CO2(C1-6 alkyl), C2-6 alkynyl, halogen, C1-3 perfluoroalkyl, (CH2)mAr1, (CH2)mHet1, (CH2)mCONR7R8, (CH2)mCO2R8, O(CH2)qCO2R8, (CH2)mCOR8, (CH2)mOR8, O(CH2)pOR8, (CH2)mNR7R8, CO2(CH2)qNR7R8, (CH2)mCN, S(O)nR8, SO2NR7R8, CONH(CH2)mAr1 or CONH(CH2)mHet1; R3 represents H, C1-6 alkyl, (CH2)pNR9R10, SO2R10, SO2NR9R10, (CH2)mCO2R10, C2-6 alkenyl, C2-6 alkynyl, (CH2)mCONR9R10, (CH2)mCO2R10, (CH2)pCN, (CH2)pR10 or (CH2)pOR10; R4 represents H or C1-6 alkyl; R5 represents H or OH; R6 represents phenyl optionally fused to a heterocyclic ring, the group as a whole being optionally substituted; R7-10 are fully defined herein and may independently represent Ar2 or Het2; Z represents CO2H, CONH(tetrazol-5-yl), CONHSO2O(C1-4 alkyl), CO2Ar3, CO2(C1-6 alkyl), tetrazol-5-yl, CONHSO2Ar3, CONHSO2(CH2)qAr3 or CONHSO2(C1-4 alkyl); Ar1-3 independently represent phenyl, naphthyl, or an aromatic heterocycle, which groups are optionally fused and optionally substituted; and Het1 and Het2 independently represent a non-aromatic heterocycle which is optionally substituted; are useful in the treatment of restenosis, renal failure and pulmonary hypertension.
摘要翻译：式（I）化合物及其药学上可接受的衍生物，其中R 1和R 2是任选的取代基并且独立地表示任选被CO 2 H或CO 2（C 1-6烷基）取代的C 1-6烷基，C 2-6烯基，C 2-6炔基，（CH 2）m CO 2 R 8，O（CH 2）q CO 2 R 8，（CH 2）m COOR 8，（CH 2）mOR 8，O（CH 2）pOR 8，C 1 -C 3全氟烷基，（CH 2）mr 1，（CH 2）m Het1，（CH 2）m CONR 7 R 8，（CH2）mNR7R8，CO2（CH2）qNR7R8，（CH2）mCN，S（O）nR8，SO2NR7R8，CONH（CH2）mAr1或CONH（CH2）mHet1; R3表示H，C1-6烷基，（CH2）pNR9R10，SO2R10，SO2NR9R10，（CH2）mCO2R10，C2-6烯基，C2-6炔基，（CH2）

8. 发明授权

US06620838B1 Benzopyrazone compounds, compositions thereof, and methods of treatment therewith 失效
标题翻译：苯并吡唑酮化合物，其组合物及其处理方法
公开(公告)号：US06620838B1
公开(公告)日：2003-09-16
申请号：US10125965
申请日：2002-04-19
申请人： Jeffrey A. McKie , Shripad S. Bhagwat , Johanne Renaud , Martin Missbach
发明人： Jeffrey A. McKie , Shripad S. Bhagwat , Johanne Renaud , Martin Missbach
IPC分类号： A61K314025
CPC分类号： C07D311/16
摘要： Benzopyranone compounds having the following structure: wherein R1, X, Y and n are as defined here, are disclosed. The compounds of formula (I), wherein R1 is H, can be prepared by demethylation of the corresponding phenolic methyl ether. The compounds are useful for treating a bone-resorbing disease, cancer, arthritis or an estrogen-related condition such as breast cancer, osteoporosis and endometriosis.
摘要翻译：公开了具有以下结构的苯并吡喃酮化合物：其中R1，X，Y和n如本文所定义。其中R 1为H的式（I）化合物可通过相应的酚甲醚的去甲基化制备。该化合物可用于治疗骨吸收性疾病，癌症，关节炎或雌激素相关病症如乳腺癌，骨质疏松症和子宫内膜异位症。

9. 发明授权

US06605635B1 N-substituted benzyl or phenyl aromatic sulfamides compounds and the use thereof 有权
标题翻译： N-取代的苄基或苯基芳香族磺酰胺化合物及其用途
公开(公告)号：US06605635B1
公开(公告)日：2003-08-12
申请号：US10149236
申请日：2002-06-07
申请人： Donglu Bai , Weizhou Chen , Yunxin Bu , Yiping Wang , Yueli Dong , Aili Kang
发明人： Donglu Bai , Weizhou Chen , Yunxin Bu , Yiping Wang , Yueli Dong , Aili Kang
IPC分类号： A61K314025
CPC分类号： C07D295/135 , A61K31/4025 , A61K31/4545
摘要： N-(3,5-bis-disubstituted aminomethyl-4-hydroxy)benzyl aromatic sulfonamides and N-(3,5-bis-disubstituted aminomethyl-4-hydroxy)phenyl aromatic sulfonamides compounds in accordance with the animal test, are active in the prevention and the treatment of cardiac arrhythmia. These compounds are prepared as corresponding diamines by the condensation of optionally substituted aromatic sulfochlorides with p-hydroxybenzylamine, p-aminophenol, or the like, which followed by the Mannich reaction of the resulted corresponding aromatic sulfamides with formaldehyde and secondary amines; or directly obtained by the reaction of the aromatic sulfamides with 4-amino-2,6-bis-disubstituted aminomethylphenol. Subsequently, the diamines are reacted with various acids to provide their salts.
摘要翻译：根据动物试验的N-（3,5-双 - 二取代氨基甲基-4-羟基）苄基芳族磺酰胺和N-（3,5-双 - 二取代氨基甲基-4-羟基）苯基芳族磺酰胺化合物在预防和治疗心律失常。这些化合物通过任选取代的芳族磺基氯与对羟基苄基胺，对氨基苯酚等的缩合制备成相应的二胺，其后所得到的相应的芳族磺酰胺与甲醛和仲胺进行曼尼希反应; 或通过芳族磺酰胺与4-氨基-2,6-二取代的氨基甲基苯酚的反应直接获得。随后，二胺与各种酸反应以提供它们的盐。

10. 发明授权

US06369096B1 Benzyloxy prodigiosine compounds 失效
标题翻译：苄氧基孕激素化合物
公开(公告)号：US06369096B1
公开(公告)日：2002-04-09
申请号：US09402455
申请日：1999-10-07
申请人： Roberto D'Alessio , Ermes Vanotti , Alberto Bargiotti , Marcellino Tibolla , Mario Ferrari , Anna Maria Isetta , Francesco Colotta
发明人： Roberto D'Alessio , Ermes Vanotti , Alberto Bargiotti , Marcellino Tibolla , Mario Ferrari , Anna Maria Isetta , Francesco Colotta
IPC分类号： A61K314025
CPC分类号： C07D207/44
摘要： A compound, having utility as an immunomodulating agent, which is a prodigiosine of formula (I): wherein R1 is hydrogen or C1-C5 alkyl; and R2 is a C1-C5 alkyl; or a pharmaceutically acceptable salt thereof.
摘要翻译：具有作为免疫调节剂的作用的化合物，其是式（I）的产物：其中R 1是氢或C 1 -C 5烷基; 并且R 2是C 1 -C 5烷基;或其药学上可接受的盐。

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