公开(公告)号：US20210393671A1

公开(公告)日：2021-12-23

申请号：US17463391

申请日：2021-08-31

Applicant: Novartis AG

Inventor： Christoph Bucher ,  Dietmar Flubacher ,  Jeremiah Douglas Foutch ,  Malay Ghosh ,  Johannes Franz Kluge ,  Zaixing Li ,  Cale Ry McAlister ,  Liladhar Murlidhar Waykole ,  Jens Sören Worthmann ,  Tingying Zhu

IPC: A61K31/724 ,  A61K47/02 ,  A61K47/38 ,  C07D339/04 ,  A61K31/381 ,  C07C309/72

Abstract: The present disclosure provides salts of lipoic acid choline ester (LACE), crystalline forms thereof, and methods of use thereof. The present disclosure further provides pharmaceutical compositions of LACE salts and methods of use thereof.

公开(公告)号：US11021446B2

公开(公告)日：2021-06-01

申请号：US16854762

申请日：2020-04-21

Applicant: NOVARTIS AG

Inventor： Donatella Chianelli ,  Runyan Li ,  Valentina Molteni ,  John Nelson ,  Jason Thomas Roland ,  Paul Vincent Rucker ,  David Charles Tully ,  Xiaoyang Wang ,  Liladhar Murlidhar Waykole ,  Yubo Zhang ,  Bo Zhou

IPC: C07D231/54 ,  C07D471/04 ,  C07D491/052 ,  A61K31/416 ,  A61K31/4162 ,  A61K31/4439 ,  A61K31/4745 ,  C07D471/06

Abstract: The present invention relates to compounds of Formula I, a stereoisomer, enantiomer, a pharmaceutically acceptable salt or an amino acid conjugate thereof; wherein variables are as defined herein; and their pharmaceutical compositions, which are useful as modulators of the activity of Farnesoid X receptors (FXR).

公开(公告)号：US10934273B2

公开(公告)日：2021-03-02

申请号：US16341124

申请日：2017-10-13

Applicant: Novartis AG

Inventor： Arnaud Grandeury ,  Liladhar Murlidhar Waykole

IPC: C07D401/12 ,  A61P35/00

Abstract: This application relates to various crystalline forms of 4-(2-((1R,2R)-2-hydroxycyclohexylamino)benzothiazol-6-yloxy)-N-methylpicolinamide hydrochloride salts as well as compositions and methods of using the same. In some embodiments the crystalline forms also contain water (“hydrates”). These materials are useful in the treatment of various diseases, including glioblastoma multiforme, breast cancer, pancreatic cancer and other solid tumors.

公开(公告)号：US20210283171A1

公开(公告)日：2021-09-16

申请号：US17199736

申请日：2021-03-12

Applicant: Novartis AG

Inventor： Christoph Bucher ,  Dietmar Flubacher ,  Jeremiah Douglas Foutch ,  Malay Ghosh ,  Johannes Franz Kluge ,  Zaixing Li ,  Cale Ry McAlister ,  Liladhar Murlidhar Waykole ,  Jens Sören Worthmann ,  Tingying Zhu

IPC: A61K31/724 ,  A61K31/381 ,  C07D339/04 ,  C07C309/72 ,  A61K47/38 ,  A61K47/02

Abstract: The present disclosure provides salts of lipoic acid choline ester (LACE), crystalline forms thereof, and methods of use thereof. The present disclosure further provides pharmaceutical compositions of LACE salts and methods of use thereof.

公开(公告)号：US10947218B2

公开(公告)日：2021-03-16

申请号：US16884666

申请日：2020-05-27

Applicant: NOVARTIS AG

Inventor： Luca Arista ,  Sreehari Babu ,  Jianwei Bian ,  Kai Cui ,  Michael Patrick Dillon ,  Rene Lattmann ,  Jialiang Li ,  Lv Liao ,  Dimitrios Lizos ,  Rita Ramos ,  Nikolaus Johannes Stiefl ,  Thomas Ullrich ,  Peggy Usselmann ,  Xiaoyang Wang ,  Liladhar Murlidhar Waykole ,  Sven Weiler ,  Yubo Zhang ,  Yizong Zhou ,  Tingying Zhu

IPC: A61K31/4427 ,  C07D405/14 ,  C07D401/14 ,  C07D401/10 ,  C07D401/12 ,  C07D409/14 ,  C07D213/82 ,  C07D411/14 ,  C07D491/107 ,  A61P19/00 ,  C07D417/00 ,  C07D413/00 ,  C07D419/00 ,  A61P19/08 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D491/20

Abstract: The invention relates to a compound of formula (I) in free form or in pharmaceutically acceptable salt form to pharmaceutical compositions comprising said compound and to the use of said compound in the treatment of heterotopic ossification and fibrodysplasia ossificans progressiva.

公开(公告)号：US10710980B2

公开(公告)日：2020-07-14

申请号：US16318250

申请日：2017-07-18

Applicant: NOVARTIS AG

Inventor： Luca Arista ,  Sreehari Babu ,  Jianwei Bian ,  Kai Cui ,  Michael Patrick Dillon ,  Rene Lattmann ,  Jialiang Li ,  Lv Liao ,  Dimitrios Lizos ,  Rita Ramos ,  Nikolaus Johannes Stiefl ,  Thomas Ullrich ,  Peggy Usselmann ,  Xiaoyang Wang ,  Liladhar Murlidhar Waykole ,  Sven Weiler ,  Yubo Zhang ,  Yizong Zhou ,  Tingying Zhu

IPC: C07D405/14 ,  C07D401/14 ,  C07D401/10 ,  C07D401/12 ,  C07D409/14 ,  C07D213/82 ,  C07D411/14 ,  C07D491/107 ,  A61P19/00 ,  C07D417/00 ,  C07D413/00 ,  C07D419/00 ,  A61P19/08 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D491/20

Abstract: The invention relates to a compound of formula (I) in free form or in pharmaceutically acceptable salt form (I) to pharmaceutical compositions comprising said compound and to the use of said compound in the treatment of heterotopic ossification and fibrodysplasia ossificans progressiva.

公开(公告)号：US09802931B2

公开(公告)日：2017-10-31

申请号：US14997207

申请日：2016-01-15

Applicant: Novartis AG

Inventor： Wolfgang Marterer ,  Mahavir Prashad ,  Edwin Bernard Villhauer ,  Liladhar Murlidhar Waykole ,  James Anthony Vivelo ,  Bertrand Sutter ,  Jean-Claude Bianchi ,  Raeann Wu ,  Denis Har ,  Piotr H. Karpinski ,  Massimo Pignone ,  Doris Stingelin ,  Eckart Buerger

IPC: C07C55/08 ,  C07D453/02 ,  A61K9/20 ,  A61K31/194 ,  A61K31/439 ,  C07C55/10 ,  C07C57/145 ,  C07C57/15 ,  C07C51/41

CPC classification number: C07D453/02 ,  A61K9/2054 ,  A61K31/194 ,  A61K31/439 ,  A61K2300/00 ,  C07B2200/07 ,  C07B2200/13 ,  C07C51/412 ,  C07C55/08 ,  C07C55/10 ,  C07C57/145 ,  C07C57/15

Abstract: The present invention relates to salts of (R)-3-(6-(4-methylphenyl)-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane, to methods for making them or their precursors, to pharmaceutical compositions comprising them, and to their use as medicaments.

公开(公告)号：US20160145253A1

公开(公告)日：2016-05-26

申请号：US14997207

申请日：2016-01-15

Applicant: Novartis AG

Inventor： Wolfgang Marterer ,  Mahavir Prashad ,  Edwin Bernard Villhauer ,  Liladhar Murlidhar Waykole ,  James Anthony Vivelo ,  Bertrand Sutter ,  Jean-Claude Bianchi ,  Raeann Wu ,  Denis Har ,  Piotr H. Karpinski ,  Massimo Pignone ,  Doris Stingelin ,  Eckart Buerger

IPC: C07D453/02 ,  C07C57/145 ,  C07C55/10 ,  C07C55/08 ,  C07C57/15 ,  C07C51/41

CPC classification number: C07D453/02 ,  A61K9/2054 ,  A61K31/194 ,  A61K31/439 ,  A61K2300/00 ,  C07B2200/07 ,  C07B2200/13 ,  C07C51/412 ,  C07C55/08 ,  C07C55/10 ,  C07C57/145 ,  C07C57/15

Abstract: The present invention relates to salts of (R)-3-(6-(4-methylphenyl)-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane, to methods for making them or their precursors, to pharmaceutical compositions comprising them, and to their use as medicaments.

Abstract translation: 本发明涉及（R）-3-（6-（4-甲基苯基） - 吡啶-3-基氧基）-1-氮杂 - 双环[2.2.2]辛烷的盐，其制备方法或其前体， 包含它们的药物组合物以及它们作为药物的用途。