公开(公告)号：US20230220384A1

公开(公告)日：2023-07-13

申请号：US17766677

申请日：2020-10-06

Applicant: Prashant MONIAN ,  Chikdu Shakti SHIVAILA ,  Subramanian MARAPPAN ,  Chandra VARGEESE ,  Pachamuthu KANDASAMY ,  Genliang LU ,  Hui YU ,  David Charles Donnell BUTLER ,  Luciano Henrique APPONI ,  Mamoru SHIMIZU ,  Stephany Michelle STANDLEY ,  David John BOULAY ,  Andrew Guzior HOSS ,  Jigar DESAI ,  Jack David GODFREY ,  Hailin YANG ,  Naoki IWAMOTO ,  WAVE LIFE SCIENCES LTD.

Inventor： Prashant Monian ,  Chikdu Shakti Shivalila ,  Subramanian Marappan ,  Chandra Vargeese ,  Pachamuthu Kandasamy ,  Genliang Lu ,  Hui Yu ,  David Charles Donnell Butler ,  Luciano Henrique Apponi ,  Mamoru Shimizu ,  Stephany Michelle Standley ,  David John Boulay ,  Andrew Guzior Hoss ,  Jigar Desai ,  Jack David Godfrey ,  Hailin Yang ,  Naoki Iwamoto

IPC: C12N15/113

CPC classification number: C12N15/113 ,  C12N2310/14 ,  C12N2310/351 ,  C12N2310/314 ,  C12N2310/322 ,  C12N2310/321 ,  C12N2310/315

Abstract: Among other things, the present disclosure provides oligonucleotides and compositions thereof. In some embodiments, provided oligonucleotides and compositions are useful for adenosine modification. In some embodiments, the present disclosure provides methods for treating various conditions, disorders or diseases that can benefit from adenosine modification.

公开(公告)号：US08926944B2

公开(公告)日：2015-01-06

申请号：US13566849

申请日：2012-08-03

Applicant: John W. Babich ,  Craig Zimmerman ,  John L. Joyal ,  Genliang Lu

Inventor： John W. Babich ,  Craig Zimmerman ,  John L. Joyal ,  Genliang Lu

IPC: A61K51/04 ,  A61K49/00 ,  C07F5/00 ,  C07D257/02 ,  C07D255/02

CPC classification number: C07D257/02 ,  A61K49/0002 ,  A61K51/0478 ,  A61K51/0482 ,  C07D255/02 ,  C07D403/14 ,  C07F5/003

Abstract: Compounds according to Formula I and Formula II are potent inhibitors of PSMA activity: The invention also provides pharmaceutical compositions of a complex of a radionuclide and a Formula I compound or a Formula II compound and methods of using the radionuclide complex of a Formula I compound or a Formula II compound for treating or diagnosis of a disease or a condition associated with PSMA activity.

Abstract translation: 根据式I和式II的化合物是PSMA活性的有效抑制剂：本发明还提供了放射性核素和式I化合物或式II化合物的配合物的药物组合物和使用式I化合物的放射性核素复合物或 用于治疗或诊断与PSMA活性相关的疾病或病症的式II化合物。

公开(公告)号：US20130034494A1

公开(公告)日：2013-02-07

申请号：US13566849

申请日：2012-08-03

Applicant: John W. BABICH ,  Craig Zimmerman ,  John L. Joyal ,  Genliang Lu

Inventor： John W. BABICH ,  Craig Zimmerman ,  John L. Joyal ,  Genliang Lu

IPC: A61K51/04 ,  C07F5/00 ,  C07D257/02

CPC classification number: C07D257/02 ,  A61K49/0002 ,  A61K51/0478 ,  A61K51/0482 ,  C07D255/02 ,  C07D403/14 ,  C07F5/003

Abstract: Compounds according to Formula I and Formula II are potent inhibitors of PSMA activity: The invention also provides pharmaceutical compositions of a complex of a radionuclide and a Formula I compound or a Formula II compound and methods of using the radionuclide complex of a Formula I compound or a Formula II compound for treating or diagnosis of a disease or a condition associated with PSMA activity.

Abstract translation: 根据式I和式II的化合物是PSMA活性的有效抑制剂：本发明还提供了放射性核素和式I化合物或式II化合物的配合物的药物组合物和使用式I化合物的放射性核素复合物或 用于治疗或诊断与PSMA活性相关的疾病或病症的式II化合物。

公开(公告)号：US20100178247A1

公开(公告)日：2010-07-15

申请号：US12631343

申请日：2009-12-04

Applicant: John W. Babich ,  Craig Zimmerman ,  John Joyal ,  Kevin P. Maresca ,  Genliang Lu ,  Shawn Hillier

Inventor： John W. Babich ,  Craig Zimmerman ,  John Joyal ,  Kevin P. Maresca ,  Genliang Lu ,  Shawn Hillier

IPC: A61K51/04 ,  C07D401/12 ,  C07F13/00 ,  A61K31/444 ,  A61K31/555 ,  A61K49/00 ,  A61P35/00

CPC classification number: C07D213/38 ,  A61K51/0478 ,  C07C311/16 ,  C07F13/005

Abstract: A compound that recognizes and binds to the CA-IX protein has Formula I, II, III, or IV. The compounds may include a radioactive element for radioimaging or therapeutic applications. Thus, pharmaceutical compositions may be prepared with one or more of the compounds of Formula I, II, III, or IV.

Abstract translation: 识别和结合CA-IX蛋白质的化合物具有式I，II，III或IV。 化合物可以包括用于放射成像或治疗应用的放射性元件。 因此，药物组合物可以用一种或多种式I，II，III或IV的化合物制备。

公开(公告)号：US20090281088A1

公开(公告)日：2009-11-12

申请号：US12411220

申请日：2009-03-25

Applicant: Charles Z. Ding ,  Genliang Lu ,  Keith Combrink ,  Dianjun D. Chen ,  Minsoo Song ,  Jiancheng Wang ,  Zhenkun Ma ,  Brian Desmond Palmer ,  Adrian Blaser ,  Andrew M. Thompson ,  Iveta Kmentova ,  Hamish Scott Sutherland ,  William Alexander Denny

Inventor： Charles Z. Ding ,  Genliang Lu ,  Keith Combrink ,  Dianjun D. Chen ,  Minsoo Song ,  Jiancheng Wang ,  Zhenkun Ma ,  Brian Desmond Palmer ,  Adrian Blaser ,  Andrew M. Thompson ,  Iveta Kmentova ,  Hamish Scott Sutherland ,  William Alexander Denny

IPC: A61K31/5365 ,  C07D498/04 ,  A61K31/551 ,  A61K31/496 ,  A61K31/4439 ,  A61K31/506 ,  A61P31/04

CPC classification number: C07D498/04

Abstract: The current invention provides a series of bicyclic nitroimidazole-substituted phenyl oxazolidinones in which a bicyclic nitroimidazole pharmacophore is covalently bonded to a phenyl oxazolidinone, their pharmaceutical compositions, and the method of use of the compositions for prevention and treatment of bacterial infections. The bicyclic nitroimidazole-substituted phenyl oxazolidinones possess surprising antibacterial activity against wild-type and resistant strains of pathogens, and are therefore useful for the prevention, control and treatment of a number of human and veterinary bacterial infections caused by these pathogens, such as Mycobacterium tuberculosis.

Abstract translation: 本发明提供了一系列双环硝基咪唑取代的苯基恶唑烷酮，其中双环硝基咪唑药效团与苯基恶唑烷酮共价键合，其药物组合物，以及组合物用于预防和治疗细菌感染的方法。 双环硝基咪唑取代的苯基恶唑烷酮对于野生型和抗性病原体菌株具有惊人的抗菌活性，因此可用于预防，控制和治疗由这些病原体引起的许多人和兽医细菌感染如结核分枝杆菌 。

公开(公告)号：US20220356204A1

公开(公告)日：2022-11-10

申请号：US16624896

申请日：2018-06-21

Applicant: David Charles Donnell BUTLER ,  Christopher P. HENCKEN ,  Nao-ki IWAMOTO ,  Pachamuthu KANDASAMY ,  Alvaro Andres LANAO ,  Genliang LU ,  Mamoru SHIMIZU ,  Sethumadhavan DIVAKARAMENON ,  Chandra VARGEESE ,  Gopal Reddy BOMMINENI ,  Subramanian MARAPPAN ,  WAVE LIFE SCIENCES LTD.

Inventor： David Charles Donnell Butler ,  Christopher P. Hencken ,  Naoki Iwamoto ,  Pachamuthu Kandasamy ,  Alvaro Andres Lanao ,  Genliang Lu ,  Mamoru Shimizu ,  Sethumadhavan Divakaramenon ,  Chandra Vargeese ,  Gopal Reddy Bommineni ,  Subramanian Marappan

IPC: C07H21/04 ,  C07F7/08 ,  C07D207/08 ,  C07H19/06 ,  C07C215/20 ,  C07C213/00 ,  C07D211/22 ,  C07C215/44

Abstract: The present disclosure, among other things, provides technologies for synthesis, including reagents and methods for stereoselective synthesis. In some embodiments, the present disclosure provides compounds useful as chiral auxiliaries. In some embodiments, the present disclosure provides reagents and methods for oligonucleotide synthesis. In some embodiments, the present disclosure provides reagents and methods for chirally controlled preparation of oligonucleotides. In some embodiments, technologies of the present disclosure are particularly useful for constructing challenging internucleotidic linkages, providing high yields and stereoselectivity.

公开(公告)号：US20200157545A1

公开(公告)日：2020-05-21

申请号：US16618010

申请日：2018-06-01

Applicant: Chandra VARGEESE ,  Naoki IWAMOTO ,  David Charles Donnell BUTLER ,  Subramanian MARAPPAN ,  Genliang LU ,  Jason Jingxin ZHANG ,  Vinod VATHIPADIEKAL ,  Maria David FRANK-KAMENETSKY ,  Luciano Henrique APPONI ,  WAVE LIFE SCIENCES LTD.

Inventor： Chandra Vargeese ,  Naoki Iwamoto ,  David Charles Donnell Butler ,  Subramanian Marappan ,  Genliang Lu ,  Jason Jingxin Zhang ,  Vinod Vathipadiekal ,  Maria David Frank-Kamenetsky ,  Luciano Henrique Apponi ,  Young Jin Cho

IPC: C12N15/113 ,  A61K31/712

Abstract: Among other things, the present disclosure provides designed oligonucleotides, compositions, and methods thereof. In some embodiments, provided oligonucleotide compositions provide improved single-stranded RNA interference and/or RNase H-mediated knockdown. Among other things, the present disclosure encompasses the recognition that structural elements of oligonucleotides, such as base sequence, chemical modifications (e.g., modifications of sugar, base, and/or internucleotidic linkages) or patterns thereof, conjugation with additional chemical moieties, and/or stereochemistry [e.g., stereochemistry of backbone chiral centers (chiral internucleotidic linkages)], and/or patterns thereof, can have significant impact on oligonucleotide properties and activities, e.g., RNA interference (RNAi) activity, stability, delivery, etc. In some embodiments, the present disclosure provides methods for treatment of diseases using provided oligonucleotide compositions, for example, in RNA interference and/or RNase H-mediated knockdown.

公开(公告)号：US08562945B2

公开(公告)日：2013-10-22

申请号：US12631312

申请日：2009-12-04

Applicant: John W. Babich ,  Craig Zimmerman ,  John Joyal ,  Kevin P. Maresca ,  John Marquis ,  Genliang Lu ,  Jian-cheng Wang ,  Shawn Hillier

Inventor： John W. Babich ,  Craig Zimmerman ,  John Joyal ,  Kevin P. Maresca ,  John Marquis ,  Genliang Lu ,  Jian-cheng Wang ,  Shawn Hillier

IPC: A61K31/18 ,  A61K31/4192 ,  A61K31/444 ,  A61K31/555 ,  A61K51/04 ,  C07D213/38 ,  C07D403/12 ,  C07F13/00 ,  A61P1/00

CPC classification number: A61K31/18 ,  A61K31/4192 ,  A61K31/444 ,  A61K31/555 ,  A61K47/22 ,  A61K49/00 ,  A61K51/04 ,  A61K51/0406 ,  A61K51/041 ,  A61K51/0446 ,  A61K51/0474 ,  A61K51/0478 ,  C07C275/16 ,  C07C311/16 ,  C07D213/38 ,  C07D403/06 ,  C07D403/12 ,  C07F13/005

Abstract: Complexes of heterocyclic radionuclides are prepared based upon ligands having substituted pyridyl and imidazolyl groups. The ligands are bifunctional, having amino acid residues that may act as a linker to a bioactive molecule, and a tridentate chelator that may complex the radionuclide. The bioactive molecule may be a peptide or somatostatin.

Abstract translation: 基于具有取代的吡啶基和咪唑基的配体制备杂环放射性核素的配合物。 配体是双功能的，具有可以作为生物活性分子的连接体的氨基酸残基，以及可能使该放射性核素复合的三齿螯合剂。 生物活性分子可以是肽或生长抑素。

公开(公告)号：US20100178246A1

公开(公告)日：2010-07-15

申请号：US12631337

申请日：2009-12-04

Applicant: John W. Babich ,  Craig Zimmerman ,  John Joyal ,  Kevin P. Maresca ,  Genliang Lu ,  Shawn Hillier

Inventor： John W. Babich ,  Craig Zimmerman ,  John Joyal ,  Kevin P. Maresca ,  Genliang Lu ,  Shawn Hillier

IPC: A61K51/04 ,  C07D403/12 ,  C07F13/00 ,  C07D401/12 ,  A61K31/555 ,  A61K49/00 ,  C07D213/56 ,  A61P25/18 ,  A61P29/00 ,  A61P13/08 ,  A61P35/00

CPC classification number: C07D213/38 ,  A61K31/18 ,  A61K31/4192 ,  A61K31/444 ,  A61K31/555 ,  A61K51/0406 ,  A61K51/041 ,  A61K51/0474 ,  A61K51/0478 ,  C07C275/16 ,  C07C311/16 ,  C07D403/06 ,  C07D403/12 ,  C07F13/005

Abstract: A compound of Formula I, a pharmaceutically acceptable salt, or solvate thereof: complexes with metals such as rhenium, technetium, and others to provide a complex for imaging tissues or treating disease, particularly where the metal is radioactive. Such complexes are specific to PSMA protein and can therefore be used in imaging or treating cancer of the prostate and other tissue where the protein is expressed.

Abstract translation: 式I的化合物，其药学上可接受的盐或溶剂化物：与金属如铼，锝等复合，以提供用于成像组织或治疗疾病的复合物，特别是在金属是放射性的情况下。 这种复合物对PSMA蛋白质是特异性的，因此可用于成像或治疗前列腺癌和表达蛋白质的其他组织的癌症。

公开(公告)号：US07678791B2

公开(公告)日：2010-03-16

申请号：US11827467

申请日：2007-07-12

Applicant: Charles Z. Ding ,  In Ho Kim ,  Jiancheng Wang ,  Zhenkun Ma ,  Yafei Jin ,  Keith D. Combrink ,  Genliang Lu ,  A. Simon Lynch

Inventor： Charles Z. Ding ,  In Ho Kim ,  Jiancheng Wang ,  Zhenkun Ma ,  Yafei Jin ,  Keith D. Combrink ,  Genliang Lu ,  A. Simon Lynch

IPC: C07D498/22 ,  A61K31/535 ,  A61P31/00

CPC classification number: C07D498/18 ,  C07D498/08 ,  C07D498/22 ,  C07D519/00

Abstract: Substituted rifamycin derivatives in which a nitroimidazole, nitrothiazole or nitrofuran pharmacophore is covalently bonded to a rifamycin, methods of using the rifamycin derivatives, and pharmaceutical compositions containing the rifamycin derivatives are disclosed. Methods of synthesizing these substituted rifamycin derivatives are also disclosed. The rifamycin derivatives possess antibacterial activity, and are effective against a number of human and veterinary pathogens in the treatment of bacterial diseases.

Abstract translation: 公开了其中硝基咪唑，硝基噻唑或硝基呋喃药效团与利福霉素共价结合的取代的利福霉素衍生物，使用利福霉素衍生物的方法和含有利福霉素衍生物的药物组合物。 还公开了合成这些取代的利福霉素衍生物的方法。 利福霉素衍生物具有抗菌活性，并且在治疗细菌性疾病中对许多人和兽医病原体有效。