公开(公告)号：US20040054212A1

公开(公告)日：2004-03-18

申请号：US10660439

申请日：2003-09-10

Applicant: Bristol-Myers Squibb Company

Inventor： John J. Venit ,  Mandar V. Dall ,  Manisha M. Dall ,  Yande Huang ,  Charles E. Dahlheim ,  Ravindra W. Tejwani

IPC: C07F009/02

CPC classification number: C07D233/64 ,  C07C211/14 ,  C07C215/10 ,  C07C215/12 ,  C07C229/08 ,  C07C229/26 ,  C07C279/14 ,  C07F9/12

Abstract: Provided herein are novel and useful combretastatin A-4 prodrug salts that increase the solubility of combretastatin A-4, readily regenerate combretastatin A-4 in vivo under normal physiological conditions, and which produce physiologically tolerable products as a result of the regeneration of combretastatin A-4.

Abstract translation: 本文提供了新的和有用的考布他汀A-4前药盐，其增加了考布他汀A-4的溶解度，在正常生理条件下容易地在体内再生考布他汀A-4，并且由于考布他汀A的再生而产生生理上可耐受的产物 -4。

公开(公告)号：US06667404B2

公开(公告)日：2003-12-23

申请号：US10360325

申请日：2003-02-07

Applicant: Dale J. Kempf ,  Daniel W. Norbeck ,  Hing Leung Sham ,  Chen Zhao ,  Thomas J. Sowin ,  Daniel S. Reno ,  Anthony R. Haight

Inventor： Dale J. Kempf ,  Daniel W. Norbeck ,  Hing Leung Sham ,  Chen Zhao ,  Thomas J. Sowin ,  Daniel S. Reno ,  Anthony R. Haight

IPC: C07D27724

CPC classification number: C07D413/12 ,  A61K31/425 ,  A61K31/427 ,  A61K31/70 ,  A61K38/00 ,  A61K45/06 ,  C07C33/46 ,  C07C43/164 ,  C07C43/1742 ,  C07C43/2055 ,  C07C43/215 ,  C07C43/23 ,  C07C43/30 ,  C07C43/315 ,  C07C45/004 ,  C07C45/29 ,  C07C45/567 ,  C07C45/62 ,  C07C45/673 ,  C07C45/74 ,  C07C53/134 ,  C07C69/34 ,  C07C69/65 ,  C07C69/732 ,  C07C211/27 ,  C07C215/18 ,  C07C215/20 ,  C07C215/28 ,  C07C229/08 ,  C07C229/26 ,  C07C229/34 ,  C07C233/36 ,  C07C233/40 ,  C07C235/10 ,  C07C235/12 ,  C07C235/34 ,  C07C235/78 ,  C07C237/10 ,  C07C237/20 ,  C07C237/22 ,  C07C239/10 ,  C07C239/18 ,  C07C239/20 ,  C07C247/10 ,  C07C251/40 ,  C07C271/20 ,  C07C271/22 ,  C07C271/34 ,  C07C275/16 ,  C07C275/24 ,  C07C311/03 ,  C07C311/13 ,  C07C311/18 ,  C07C317/10 ,  C07C317/28 ,  C07C317/44 ,  C07C323/12 ,  C07C323/25 ,  C07C381/00 ,  C07D213/26 ,  C07D213/30 ,  C07D213/34 ,  C07D213/40 ,  C07D213/54 ,  C07D213/56 ,  C07D213/61 ,  C07D213/75 ,  C07D231/12 ,  C07D233/56 ,  C07D233/64 ,  C07D233/84 ,  C07D235/14 ,  C07D235/16 ,  C07D239/26 ,  C07D241/12 ,  C07D249/08 ,  C07D261/08 ,  C07D263/32 ,  C07D277/24 ,  C07D277/28 ,  C07D277/30 ,  C07D277/34 ,  C07D277/36 ,  C07D277/40 ,  C07D277/42 ,  C07D277/56 ,  C07D295/13 ,  C07D295/205 ,  C07D295/215 ,  C07D303/36 ,  C07D307/42 ,  C07D333/16 ,  C07D401/12 ,  C07D417/12 ,  C07K5/06026 ,  C07K5/06078 ,  A61K31/00 ,  A61K2300/00 ,  C07C49/233 ,  C07C49/255 ,  C07C49/215 ,  C07C49/245 ,  C07C49/235 ,  C07C49/223

Abstract: A retroviral protease inhibiting compound of the formula: is disclosed.

Abstract translation: 公开了下式的逆转录病毒蛋白酶抑制化合物。

公开(公告)号：US06632830B1

公开(公告)日：2003-10-14

申请号：US09561759

申请日：2000-04-28

Applicant: Susan L. Acton ,  Timothy D. Ocain ,  Alexandra E. Gould ,  Natalie A. Dales ,  Bing Guan ,  James A. Brown

Inventor： Susan L. Acton ,  Timothy D. Ocain ,  Alexandra E. Gould ,  Natalie A. Dales ,  Bing Guan ,  James A. Brown

IPC: A61K31194

CPC classification number: C07D231/12 ,  C07B2200/07 ,  C07C229/16 ,  C07C229/24 ,  C07C229/26 ,  C07C229/36 ,  C07C271/20 ,  C07C275/24 ,  C07C323/52 ,  C07C323/58 ,  C07C2601/02 ,  C07C2601/14 ,  C07D209/20 ,  C07D213/55 ,  C07D233/64 ,  C07D235/16 ,  C07D249/08 ,  C07D261/08 ,  C07D277/06 ,  C07D277/30 ,  C07D277/40 ,  C07D277/42 ,  C07D333/24 ,  C07D405/06

Abstract: ACE-2 inhibiting compounds are disclosed. These compounds include compounds of formula (IV): wherein the variables are as described in the specification. Pharmaceutical compositions containing the compounds are also discussed. The pharmaceutical compositions may contain an effective amount of a compound of the invention to treat ACE-2 associated disorders such as a blood pressure related disease or disorder, cell proliferation disorder, kidney disorder, kinetensin associated disorder, inflammation associated disorder, or an allergic disorder.

Abstract translation: 公开了ACE-2抑制化合物。 这些化合物包括式（IV）的化合物：其中变量如说明书中所述。 还讨论了含有这些化合物的药物组合物。 药物组合物可以含有有效量的本发明化合物以治疗ACE-2相关疾病，例如与血压相关的疾病或病症，细胞增殖病症，肾脏疾病，激素相关病症，炎症相关疾病或过敏性疾病 。

公开(公告)号：US20030153784A1

公开(公告)日：2003-08-14

申请号：US10372627

申请日：2003-02-25

Inventor： Fabio Giannessi ,  Natalina Dell'uomo ,  Maria Ornella Tinti ,  Francesco De Angelis

IPC: C07F009/28 ,  C07C229/26

CPC classification number: C07C227/16 ,  C07C227/14 ,  C07C229/26 ,  C07F9/5407

Abstract: A process is described for the preparation of R or S aminocarnitine, R or S phosphonium aminocarnitine and R and S 3,4 diaminobutanoic acid, and their derivatives with the following formula: 1 where Y is as described in the attached description, starting from aspartic acid with the same configuration as the desired compounds. This process is advantageous from the industrial point of view in terms of the type of reactants used, the reduced volumes of solvents and the possibility of avoiding purification of the intermediate products.

公开(公告)号：US06528684B1

公开(公告)日：2003-03-04

申请号：US10018794

申请日：2001-12-21

Applicant: Fabio Giannessi ,  Natalina Dell'uomo ,  Maria Ornella Tinti ,  Francesco De Angelis

Inventor： Fabio Giannessi ,  Natalina Dell'uomo ,  Maria Ornella Tinti ,  Francesco De Angelis

IPC: C07C22900

CPC classification number: C07C227/14 ,  C07C229/26

Abstract: R or S aminocarnitine and their derivatives with formula (I) where Y is as described in the description, starting with aspartic acid with the same configuration as the aminocarnitine desired. This process has advantage in the type of reactants used, reduced volumes of solvents and the possibility of avoiding purification of intermediate products.

Abstract translation: R或S氨卡尼汀及其衍生物，其中Y如描述中所述，以与所需胺氨基酸相同构型的天冬氨酸开始。 该方法在所用反应物的类型，溶剂体积减少和避免中间产物净化的可能性方面具有优势。

公开(公告)号：US06458337B1

公开(公告)日：2002-10-01

申请号：US09620594

申请日：2000-07-20

Applicant: Pier Lucio Anelli ,  Marco Lolli ,  Franco Fedeli ,  Mario Virtuani ,  Marino Brocchetta ,  Pierfrancesco Morosini ,  Daniela Palano

Inventor： Pier Lucio Anelli ,  Marco Lolli ,  Franco Fedeli ,  Mario Virtuani ,  Marino Brocchetta ,  Pierfrancesco Morosini ,  Daniela Palano

IPC: A61B5055

CPC classification number: C07C229/26 ,  A61K49/06 ,  C07C229/36 ,  C07C233/48 ,  C07C233/51 ,  C07C237/06 ,  C07C2601/14 ,  C07D209/20 ,  C07D263/26 ,  Y10S977/928 ,  Y10S977/93

Abstract: Compounds of the formula when chelated with metals exhibit improved serum relaxivity and are used in magnetic resonance imaging, particularly for imaging the blood pool.

Abstract translation: 与金属螯合的化合物表现出改善的血清舒张性，并用于磁共振成像，特别是用于血液成像。

公开(公告)号：US20020072507A1

公开(公告)日：2002-06-13

申请号：US09950500

申请日：2001-09-11

Inventor： John J. Venit ,  Mandar V. Dali ,  Manisha M. Dali ,  Yande Huang ,  Charles E. Dahlheim ,  Ravindra W. Tejwani

IPC: A61K031/7008 ,  A61K031/675 ,  C07D233/61 ,  C07F009/02

CPC classification number: C07D233/64 ,  C07C211/14 ,  C07C215/10 ,  C07C215/12 ,  C07C229/08 ,  C07C229/26 ,  C07C279/14 ,  C07F9/12

Abstract: Provided herein are novel and useful combretastatin A-4 prodrug salts that increase the solubility of combretastatin A-4, readily regenerate combretastatin A-4 in vivo under normal physiological conditions, and which produce physiologically tolerable products as a result of the regeneration of combretastatin A-4.

Abstract translation: 本文提供了新的和有用的考布他汀A-4前药盐，其增加了考布他汀A-4的溶解度，在正常生理条件下容易地在体内再生考布他汀A-4，并且由于考布他汀A的再生而产生生理上可耐受的产物 -4。

公开(公告)号：US06403055B1

公开(公告)日：2002-06-11

申请号：US09612392

申请日：2000-07-07

Applicant: Luisella Calabi ,  Alessandro Maiocchi ,  Marco Lolli ,  Fabrizio Rebasti

Inventor： Luisella Calabi ,  Alessandro Maiocchi ,  Marco Lolli ,  Fabrizio Rebasti

IPC: A61B5055

CPC classification number: C07D209/20 ,  A61K49/06 ,  C07C229/26 ,  C07C229/36 ,  C07C229/76 ,  Y10S977/928 ,  Y10S977/93

Abstract: Compounds of formula (I): are used as their paramagnetic chelates as contrast agents in magnetic resonance imaging. These compounds have high affinity to plasma proteins and exhibit extremely high values of relaxivity in serum and are thus useful as blood pool contrast agents.

Abstract translation: 式（I）化合物在磁共振成像中用作对比剂作为它们的顺磁性螯合物。 这些化合物对血浆蛋白质具有高亲和力，并且在血清中表现出非常高的舒张度值，因此可用作血液池造影剂。

公开(公告)号：US20020035269A1

公开(公告)日：2002-03-21

申请号：US09808123

申请日：2001-03-15

Inventor： John Soper ,  Ahmad K. Hilaly ,  Kevin Moore ,  Thomas P. Binder

IPC: C07D233/61 ,  C07D209/20

CPC classification number: C07C227/40 ,  C07C229/26

Abstract: This invention relates to a method for separating basic amino acids from fermentation broth comprising contacting the broth with strong acid cation exchange resins that have a low degree of cross-linkage and eluting the amino acid. The method described herein results in higher yield and higher purity of lysine, in addition to higher throughput, as compared to conventional processes of purification of lysine from fermentation broth.

公开(公告)号：US20020016350A1

公开(公告)日：2002-02-07

申请号：US09927111

申请日：2001-08-10

Inventor： Peter J. Connolly ,  Victor T. Bandurco ,  Steven K. Wetter ,  Sigmond Johnson ,  Jacqueline Bussolari ,  William V. Murray

IPC: A61K031/4178 ,  A61K031/404 ,  A61K031/4025 ,  A61K031/17 ,  A61K031/165 ,  C07D43/14

CPC classification number: C07D213/81 ,  C07C229/14 ,  C07C229/22 ,  C07C229/24 ,  C07C229/26 ,  C07C229/36 ,  C07C233/43 ,  C07C233/51 ,  C07C233/80 ,  C07C235/06 ,  C07C235/34 ,  C07C235/56 ,  C07C235/68 ,  C07C237/06 ,  C07C237/08 ,  C07C237/10 ,  C07C237/22 ,  C07C255/58 ,  C07C271/22 ,  C07C271/58 ,  C07C275/24 ,  C07C279/14 ,  C07C311/21 ,  C07C2601/08 ,  C07D307/68 ,  C07D333/20 ,  C07D333/36 ,  C07D409/12

Abstract: This invention relates to a series of substitituted amino acids of Formula I 1 pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention are small molecules which bind to the erythropoietin receptor and compete with the natural ligand for binding to this receptor.

Abstract translation: 本发明涉及一系列含有它们的式I药物组合物的取代氨基酸及其生产中使用的中间体。 本发明的化合物是与促红细胞生成素受体结合并与天然配体竞争结合该受体的小分子。