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21. 发明授权

US06184226B2 Quinazoline derivatives as inhibitors of P-38 &agr; 有权
标题翻译：喹唑啉衍生物作为P-38α的抑制剂
公开(公告)号：US06184226B2
公开(公告)日：2001-02-06
申请号：US09141916
申请日：1998-08-28
申请人： Sarvajit Chakravarty , John J. Perumattam , George F. Schreiner , David Y. Liu , John A. Lewicki
发明人： Sarvajit Chakravarty , John J. Perumattam , George F. Schreiner , David Y. Liu , John A. Lewicki
IPC分类号： A01N5500
CPC分类号： C07D401/12 , A61K31/519 , C07D239/94 , C07D471/04
摘要： The invention describes compounds of the formula and the pharmaceutically acceptable salts thereof and the pharmaceutically acceptable salts thereof wherein each R2 is independently a noninterfering substituent; m is an integer of 0-4; Z is CH or N; R1 is H, alkyl (1-6C) or arylalkyl optionally substituted on the aryl group with 1-3 substituents independently selected from alkyl (1-6C), halo, OR, NR2, SR, —OOCR, —NROCR, RCO, —COOR, —CONR2, —SO2NR2, CN, CF3, and NO2, wherein each R is independently H or lower alkyl (1-4C); n is 0, 1 or 2; Ar is phenyl, pyridyl, indolyl, or pyrimidyl, each optionally substituted with a group selected from the group consisting of optionally substituted alkyl (1-6C), halo, OR, NR2, SR, —OOCR, —NROCR, RCO, —COOR, —CONR2, SO2NR2, CN, CF3, and NO2, wherein each R is independently H or lower alkyl (1-4C); and R3 is a branched or cyclic alkyl group (5-7C) or is phenyl optionally substituted with 1-2 substituents which substituents are selected from the group consisting of alkyl (1-6C), halo, OR, NR2, SR, —OOCR, —NROCR, RCO, —COOR, —CONR2, —SO2NR2, CN, CF3, and NO2, wherein each R is independently H or lower alkyl (1-4C) which are useful as antiinflammatories and in treating cardiac disorders.
摘要翻译：本发明描述了下式的化合物及其药学上可接受的盐及其药学上可接受的盐，其中R2各自独立地为非干扰性取代基; m为0-4的整数; Z为CH或N; R 1为H，烷基（1-6C）（1-6C），卤素，OR，NR2，SR，-OOCR，-NROCR，RCO，-COOR，-CONR2，-SO2NR2，CN等的任选取代的芳基， CF 3和NO 2，其中每个R独立地为H或低级烷基（1-4C）; n为0,1或2; Ar为苯基，吡啶基，吲哚基或嘧啶基，各自任选被选自以下的基团取代：任选取代的烷基（1-6C），卤素，OR，NR2，SR，-OOCR，-NROCR，RCO，-COOR，-CONR2，SO2NR2，CN，CF3和NO2，其中每个R独立地为H或低级烷基（1-4C）; 和R 3是支链或环状烷基（5-7C），或是任选被1-2个取代基取代的苯基，所述取代基选自烷基（1-6C），卤素，OR，NR2，SR，-OOCR， -NROCR，RCO，-COOR，-CONR2，-SO2NR2，CN，CF3和NO2，其中每个R独立地为H或可用作抗炎剂和治疗心脏疾病的低级烷基（1-4C）。

22. 发明授权

US5212286A Atrial Natriuretic/vasodilator peptide compounds 失效
标题翻译： ATRIAL NATRIURETIC / VASODILATOR PEPTIDE化合物
公开(公告)号：US5212286A
公开(公告)日：1993-05-18
申请号：US870795
申请日：1986-06-05
申请人： John A. Lewicki , Robert M. Scarborough, Jr.
发明人： John A. Lewicki , Robert M. Scarborough, Jr.
IPC分类号： A61K38/00 , C07K14/58 , C12N15/62 , C12N15/70 , C12N15/81 , C12N15/85
CPC分类号： C07K14/582 , C07K14/58 , C12N15/625 , C12N15/70 , C12N15/81 , C12N15/85 , A61K38/00 , C07K2319/036 , C07K2319/50 , C07K2319/75
摘要： Methods, compounds and compositions are provided for inducing natriuresis, diuresis and vasodilatation in mammalian hosts by administering atrial natriuretic/vasodilator peptides to said host. Also provided are methods for producing such peptide compounds.
摘要翻译：提供方法，化合物和组合物，用于通过向所述宿主施用心房钠尿素/血管舒张肽来在哺乳动物宿主中诱导利尿，利尿和血管扩张。还提供了生产这种肽化合物的方法。

23. 发明授权

US5114923A Recombinant techniques for production of novel natriuretic and vasodilator peptides 失效
标题翻译：用于生产新型利尿钠和血管舒张肽的重组技术
公开(公告)号：US5114923A
公开(公告)日：1992-05-19
申请号：US460855
申请日：1990-02-02
申请人： Jeffrey J. Seilhamer , John A. Lewicki , Robert M. Scarborough , J. Gordon Porter
发明人： Jeffrey J. Seilhamer , John A. Lewicki , Robert M. Scarborough , J. Gordon Porter
IPC分类号： A61K38/00 , C07K14/58
CPC分类号： C07K14/582 , C07K14/58 , A61K38/00
摘要： The cDNA sequence encoding porcine brain natriuretic peptide and related genes encoding canine and human peptides with natriuretic activity are disclosed. The gene is shown to make accessible the DNAs encoding analogous natriuretic peptides in other vertebrate species. The genes encoding these NPs can be used to effect modifications of the sequence to produce alternate forms of the NPs and to provide practical amounts of these proteins. The NPs of the invention can also be synthesized chemically. The invention peptides have the formula: ##STR1## wherein R.sup.1 is selected from the group consisting of: ##STR2## or a 10- to 109-amino acid sequence shown as the native upstream sequence for porcine, canine or human NP in FIG. 6, or a composite thereof;R.sup.2 is (OH), NH.sub.2, or NR'R" wherein R' and R" are independently lower alkyl (1-4C) or is ##STR3## or the amides (NH.sub.2 or NR'R") thereof, with the proviso that if formula (1) isR.sup.1 -Cys-Phe-Gly-Arg-Arg-Leu-Asp-Arg- Ile-Gly-Ser-Leu-Ser-Gly-Leu-Gly-Cys-R.sup.2and R.sup.1 is Asp-Ser-Gly-, R.sup.2 cannot be Asn-Val-Leu-Arg-Arg-Tyr.The peptides of the invention can be formulated into pharmaceutical compositions and used to treat conditions associated with high extracellular fluid levels, especially congestive heart failure.
摘要翻译： PCT No.PCT / US89 / 02373。 371日期1990年2月2日 102（e）1990年2月2日PCT PCT日期为1989年5月31日。公开了编码猪脑利钠肽的cDNA序列和编码具有利尿钠活性的犬和人肽的相关基因。该基因显示可使得其他脊椎动物物种中编码类似利尿钠肽的DNA可见。编码这些NP的基因可用于影响序列的修饰以产生NP的替代形式并提供实际量的这些蛋白质。本发明的NP也可以化学合成。本发明的肽具有下式：其中R 1选自：（H）;（C）甘氨酸 Ser-Gly-; 或者图像中显示为猪，犬或人NP的天然上游序列的10至109个氨基酸序列的图像。 6，或其复合物; R2是（OH），NH2或NR'R“，其中R'和R”独立地是低级烷基（1-4C），或者是或其酰胺（NH 2或NR'R“），条件是如果式（1）为R1-Cys-Phe-Gly-Arg-Arg-Leu-Asp-Arg-Ile-Gly-Ser-Leu- Ser-Gly-Leu-Gly-Cys-R2和R1是Asp-Ser-Gly-，R2不能是Asn-Val-Leu-Arg-Arg-Tyr。本发明的肽可以配制成药物组合物并用于治疗与高细胞外液体水平相关的病症，特别是充血性心力衰竭。

24. 发明授权

US5047397A Linear analogs of atrial natriuretic peptides 失效
标题翻译：心房利钠肽的线性类似物
公开(公告)号：US5047397A
公开(公告)日：1991-09-10
申请号：US285916
申请日：1988-12-16
申请人： Robert M. Scarborough , John A. Lewicki , Lorin K. Johnson
发明人： Robert M. Scarborough , John A. Lewicki , Lorin K. Johnson
IPC分类号： A61K38/00 , C07K14/58
CPC分类号： C07K14/58 , A61K38/00
摘要： Compounds and compositions comprising synthetic analogs of Atrial Natriuretic Peptides are provided, together with methods for their production and use as natriuretics, diuretics and/or vasodilators, or as intermediates for or modulators of such useful compounds or of native Atrial Natriuretic Peptides.
摘要翻译：提供包含心房利钠肽的合成类似物的化合物和组合物，以及其生产和用作利尿剂，利尿剂和/或血管扩张剂的方法，或作为这些有用化合物或天然心房钠尿肽的中间体或调节剂。

25. 发明授权

US08206713B2 Method of treating cancer using antibodies to a non-ligand binding region of NOTCH2 有权
标题翻译：使用NOTCH2非配体结合区域的抗体治疗癌症的方法
公开(公告)号：US08206713B2
公开(公告)日：2012-06-26
申请号：US13010486
申请日：2011-01-20
申请人： John A. Lewicki , Austin Gurney , Timothy Hoey , Wan-ching Yen , Sanjeev Satyal
发明人： John A. Lewicki , Austin Gurney , Timothy Hoey , Wan-ching Yen , Sanjeev Satyal
IPC分类号： A61K39/395 , C07K16/28 , C07K14/705
CPC分类号： C07K16/30 , A61K39/39558 , A61K45/06 , A61K2039/505 , A61K2039/507 , A61N5/10 , C07K16/18 , C07K16/28 , C07K16/3015 , C07K16/3046 , C07K2317/21 , C07K2317/24 , C07K2317/31 , C07K2317/34 , C07K2317/73 , C07K2317/732 , C07K2317/734 , C07K2317/76 , C07K2317/92
摘要： The present invention relates to compositions and methods for characterizing, diagnosing, and treating cancer. In particular the invention provides the means and methods for the diagnosis, characterization, prognosis and treatment of cancer and specifically targeting cancer stem cells. The present invention provides an antibody that specifically binds to a non-ligand binding region of the extracellular domain of a human NOTCH receptor and inhibits growth of tumor cells. The present invention further provides a method of treating cancer, the method comprising administering a therapeutically effective amount of an antibody that specifically binds to a non-ligand binding region of the extracellular domain of a human NOTCH receptor protein and inhibits growth of tumor cells.
摘要翻译：本发明涉及用于表征，诊断和治疗癌症的组合物和方法。特别地，本发明提供了用于癌症的诊断，表征，预后和治疗以及特异性靶向癌症干细胞的方法和方法。本发明提供了特异性结合人类NOTCH受体的细胞外结构域的非配体结合区并抑制肿瘤细胞生长的抗体。本发明还提供了一种治疗癌症的方法，所述方法包括施用治疗有效量的特异性结合人NOTCH受体蛋白的细胞外结构域的非配体结合区的抗体并抑制肿瘤细胞的生长。

26. 发明授权

US07919092B2 Antibodies to notch receptors 有权
标题翻译：抗缺陷受体的抗体
公开(公告)号：US07919092B2
公开(公告)日：2011-04-05
申请号：US11806472
申请日：2007-05-31
申请人： John A. Lewicki , Austin Gurney , Timothy Hoey , Wan-Ching Yen , Sanjeev Satyal
发明人： John A. Lewicki , Austin Gurney , Timothy Hoey , Wan-Ching Yen , Sanjeev Satyal
IPC分类号： A61K39/395 , C07K16/28 , C12P21/08 , C07K14/705
CPC分类号： C07K16/30 , A61K39/39558 , A61K45/06 , A61K2039/505 , A61K2039/507 , A61N5/10 , C07K16/18 , C07K16/28 , C07K16/3015 , C07K16/3046 , C07K2317/21 , C07K2317/24 , C07K2317/31 , C07K2317/34 , C07K2317/73 , C07K2317/732 , C07K2317/734 , C07K2317/76 , C07K2317/92
摘要： The present invention relates to compositions and methods for characterizing, diagnosing, and treating cancer. In particular the invention provides the means and methods for the diagnosis, characterization, prognosis and treatment of cancer and specifically targeting cancer stem cells. The present invention provides an antibody that specifically binds to a non-ligand binding region of the extracellular domain of a human NOTCH receptor and inhibits growth of tumor cells. The present invention further provides a method of treating cancer, the method comprising administering a therapeutically effective amount of an antibody that specifically binds to a non-ligand binding region of the extracellular domain of a human NOTCH receptor protein and inhibits growth of tumor cells.
摘要翻译：本发明涉及用于表征，诊断和治疗癌症的组合物和方法。特别地，本发明提供了用于癌症的诊断，表征，预后和治疗以及特异性靶向癌症干细胞的方法和方法。本发明提供了特异性结合人类NOTCH受体的细胞外结构域的非配体结合区并抑制肿瘤细胞生长的抗体。本发明还提供了一种治疗癌症的方法，所述方法包括施用治疗有效量的特异性结合人NOTCH受体蛋白的细胞外结构域的非配体结合区的抗体并抑制肿瘤细胞的生长。

27. 发明授权

US07345045B2 Pyrido-pyrimidine compounds as medicaments 有权
标题翻译：吡啶 - 嘧啶化合物作为药物
公开(公告)号：US07345045B2
公开(公告)日：2008-03-18
申请号：US11053121
申请日：2005-02-07
申请人： Sarvajit Chakravarty , Sundeep Dugar , John J. Perumattam , George F. Schreiner , David Y. Liu , John A. Lewicki
发明人： Sarvajit Chakravarty , Sundeep Dugar , John J. Perumattam , George F. Schreiner , David Y. Liu , John A. Lewicki
IPC分类号： A61K31/4375 , C07D471/04
CPC分类号： C07D401/12 , A61K31/519 , C07D239/94 , C07D471/04
摘要： The invention is directed to methods to inhibit TGF-β and/or p38-α kinase using compounds of the formula or the pharmaceutically acceptable salts thereof wherein R3 is a noninterfering substituent; each Z is CR2 or N, wherein no more than two Z positions in ring A are N, and wherein two adjacent Z positions in ring A cannot be N; each R2 is independently a noninterfering substituent; L is a linker; n is 0 or 1; and Ar′ is the residue of a cyclic aliphatic, cyclic heteroaliphatic, aromatic or heteroaromatic moiety optionally substituted with 1-3 noninterfering substituents.
摘要翻译：本发明涉及使用下式的化合物或其药学上可接受的盐抑制TGF-β和/或p38-α激酶的方法，其中R 3是非干扰性取代基; 每个Z是CR 2或N，其中环A中不超过两个Z位是N，并且其中环A中的两个相邻Z位不能是N; 每个R 2独立地是非干扰取代基; L是连接体; n为0或1; 并且Ar'是任选被1-3个非干扰取代基取代的环脂族，环状杂脂族，芳族或杂芳族部分的残基。

28. 发明授权

US06476031B1 Quinazoline derivatives as medicaments 有权
标题翻译：喹唑啉衍生物作为药物
公开(公告)号：US06476031B1
公开(公告)日：2002-11-05
申请号：US09383825
申请日：1999-08-27
申请人： Sarvajit Chakravarty , Sundeep Dugar , John J. Perumattam , George F. Schreiner , David Y. Liu , John A. Lewicki
发明人： Sarvajit Chakravarty , Sundeep Dugar , John J. Perumattam , George F. Schreiner , David Y. Liu , John A. Lewicki
IPC分类号： C07D23994
CPC分类号： C07D401/12 , A61K31/519 , C07D239/94 , C07D471/04
摘要： The invention is directed to methods to inhibit TGF-&bgr; and/or p38-&agr; kinase using compounds of the formula or the pharmaceutically acceptable salts thereof wherein R3 is a noninterfering substituent; each Z is CR2 or N, wherein no more than two Z positions in ring A are N, and wherein two adjacent Z positions in ring A cannot be N; each R2 is independently a noninterfering substituent; L is a linker; n is 0 or 1; and Ar′ is the residue of a cyclic aliphatic, cyclic heteroaliphatic, aromatic or heteroaromatic moiety optionally substituted with 1-3 noninterfering substituents.
摘要翻译：本发明涉及使用下式的化合物或其药学上可接受的盐抑制TGF-β和/或p38-α激酶的方法，其中R3是不干扰取代基;每个Z是CR2或N，其中环中不超过两个Z位置 A是N，并且其中环A中的两个相邻Z位不能是N;每个R2独立地是非干扰取代基; L是连接基; n是0或1; 并且Ar'是任选被1-3个非干扰取代基取代的环状脂族，环状杂脂族，芳族或杂芳族部分的残基。

29. 发明授权

US06448257B1 Compounds and methods to treat cardiac failure and other disorders 有权
标题翻译：治疗心力衰竭和其他疾病的化合物和方法
公开(公告)号：US06448257B1
公开(公告)日：2002-09-10
申请号：US09535316
申请日：2000-03-24
申请人： Babu J. Mavunkel , David Y. Liu , George F. Schreiner , John A. Lewicki
发明人： Babu J. Mavunkel , David Y. Liu , George F. Schreiner , John A. Lewicki
IPC分类号： A61K31437
CPC分类号： C07D209/08 , C07D209/24 , C07D235/06 , C07D401/06 , C07D401/14 , C07D403/06 , C07D471/04
摘要： Compounds of the formula: wherein the dotted line represents an optional bond; and the pharmaceutically acceptable salts thereof, wherein X1 is an alkyl bridge optionally containing an O, S, or N heteroatom that forms an aliphatic 5-7 membered ring and is optionally substituted by one or more of halo, OR, SR, NR2, RCO, COOR, CONR2, OOCR, or NROCR where R is H or alkyl (1-6C), or by one or more CN or═O, or by one or more aliphatic or aromatic 5- or 6-membered rings optionally containing 1-2 heteroatoms; R1 is wherein X2 is CO or an isostere thereof; m is 0 or 1; Y is optionally substituted alkyl, optionally substituted aryl, or optionally substituted arylalkyl or two Y taken together may form an alkylene (2-3C) bridge; n is 0-4; Z1 is CH or N; X3 is CH or CHR where R is H or alkyl (1-6C), or an isostere thereof; and Ar, R2 and R3 are as defined in the specification. These compounds are selective inhibitors of p38&agr; kinase.
摘要翻译：下式的化合物：其中虚线表示任选的键;及其药学上可接受的盐，其中X 1是任选地含有O，S或N杂原子的烷基桥，其形成脂族5-7元环并任选被取代其中R是H或烷基（1-6C），或一个或多个CN或= O，或一个或多个卤素，OR，SR，NR 2，RCO，COOR，CONR 2，OOCR或NROCR 任选含有1-2个杂原子的脂族或芳族五元或六元环; R 1是其中X 2是CO或其等价物; m是0或1; Y是任选取代的烷基，任选取代的芳基或任选取代的芳基烷基或两个Y 一起可以形成亚烷基（2-3C）桥; n为0-4; Z1为CH或N; X3为CH或CHR，其中R为H或烷基（1-6C）或其等同体; 并且Ar，R 2和R 3如本说明书中所定义。这些化合物是p38alpha激酶的选择性抑制剂。

30. 发明授权

US06410540B1 Inhibitors of p38-&agr;kinase 有权
标题翻译： p38-alphakinase的抑制剂
公开(公告)号：US06410540B1
公开(公告)日：2002-06-25
申请号：US09385494
申请日：1999-08-27
申请人： R. Richard Goehring , Gregory R. Luedtke , Babu J. Mavunkel , Sarvajit Chakravarty , Sundeep Dugar , George F. Schreiner , David Y. Liu , John A. Lewicki
发明人： R. Richard Goehring , Gregory R. Luedtke , Babu J. Mavunkel , Sarvajit Chakravarty , Sundeep Dugar , George F. Schreiner , David Y. Liu , John A. Lewicki
IPC分类号： A61K3150
CPC分类号： A61K45/06 , A61K31/00 , A61K31/426 , A61K31/4365 , A61K31/437 , A61K31/445 , A61K31/4535 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/495 , A61K31/496 , A61K31/4965 , A61K31/497 , A61K31/506 , A61K31/519 , A61K31/522 , Y02A50/411
摘要： The invention is directed to methods to treat conditions mediated by p38-&agr;kinase using compounds of the formula and the pharmaceutically acceptable salts thereof, or a pharmaceutical composition thereof, wherein Z is N or CR1, R1 is a noninterfering substituent, each of X1 and X2 is a linker, Ar1 and Ar2 are identical or different, and represent optionally substituted C1-C20 hydrocarbyl residues wherein at least one of Ar1 and Ar2 is an optionally substituted aryl group, with the proviso that when X2 is CH2 or an isostere thereof, X1 is CO or an isostere thereof, and Ar2 is optionally substituted phenyl, Ar1 is other than an optionally substituted indolyl, benzimidazolyl or benzotriazolyl substituent, and wherein said optionally substituted phenyl is not an optionally substituted indolyl, benzimidazolyl, or benzotriazolyl, Y is a noninterfering substituent, wherein n is an integer from 0-4, and wherein m is an integer from 0-4 and 1 is an integer from 0-3.
摘要翻译：本发明涉及使用下式的化合物及其药学上可接受的盐或其药物组合物治疗由p38-阿拉蛋白酶介导的病症的方法，其中Z是N或CR1，R1是不干扰取代基，X1和X2分别是连接基，Ar 1和Ar 2相同或不同，并且表示任选取代的C 1 -C 20烃基残基，其中Ar 1和Ar 2中的至少一个是任选取代的芳基，条件是当X 2是CH 2或其等同体时，X 1是CO 或其等同物，Ar 2是任选取代的苯基，Ar 1不同于任选取代的吲哚基，苯并咪唑基或苯并三唑基取代基，并且其中所述任选取代的苯基不是任选取代的吲哚基，苯并咪唑基或苯并三唑基，Y是非干扰取代基，其中n是0-4的整数，其中m是0-4的整数，1是0-3的整数。

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