公开(公告)号：US10383863B2

公开(公告)日：2019-08-20

申请号：US16203122

申请日：2018-11-28

申请人： NOVARTIS AG

发明人： Ha-Soon Choi ,  James Paul Lajiness ,  Srinivasa Reddy Natala ,  Bao Nguyen ,  Hank Michael James Petrassi ,  Zhicheng Wang

IPC分类号： A61K31/443 ,  C07D493/08 ,  A61K31/506 ,  A61K31/351 ,  A61K31/416 ,  A61K31/4155 ,  C12N5/077 ,  C07D491/18 ,  A61L27/54 ,  A61K45/06 ,  A61K31/5377 ,  A61K31/497 ,  A61K31/4545 ,  A61K31/4525 ,  A61K31/4439 ,  A61K31/4433 ,  A61K31/444 ,  A61K31/4245 ,  A61K31/34

摘要： The present invention provides compounds of formula I: or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds, and methods of using such compounds for treatment of joint damage or joint injury in a mammal, and for inducing differentiation of mesenchymal stem cells into chondrocytes.

公开(公告)号：US10077317B2

公开(公告)日：2018-09-18

申请号：US14280017

申请日：2014-05-16

申请人： Novartis AG

发明人： Andrew Paul Garner ,  Elizabeth Anne Reisinger Sprague ,  Seth Alexander Ettenberg ,  Christian Kunz ,  Nicole Haubst ,  Winfried Elis

IPC分类号： C07K16/30 ,  C07K16/32 ,  A61K39/395 ,  A61K45/06 ,  A61K39/00

CPC分类号： C07K16/32 ,  A61K39/39558 ,  A61K45/06 ,  A61K2039/505 ,  C07K16/30 ,  C07K16/3015 ,  C07K16/3023 ,  C07K16/303 ,  C07K16/3038 ,  C07K16/3046 ,  C07K16/3053 ,  C07K16/3061 ,  C07K16/3069 ,  C07K2317/21 ,  C07K2317/24 ,  C07K2317/33 ,  C07K2317/34 ,  C07K2317/522 ,  C07K2317/524 ,  C07K2317/526 ,  C07K2317/55 ,  C07K2317/56 ,  C07K2317/565 ,  C07K2317/567 ,  C07K2317/73 ,  C07K2317/76 ,  C07K2317/92 ,  A61K2300/00

摘要： The present invention relates to antibodies or fragments thereof that target a conformational epitope of a HER receptor. In particular, the invention relates to antibodies or fragments thereof that target a conformational epitope of HER3 receptor and compositions and methods of use thereof.

公开(公告)号：US10077240B2

公开(公告)日：2018-09-18

申请号：US15598734

申请日：2017-05-18

申请人： NOVARTIS AG

发明人： Donatella Chianelli ,  Valentina Molteni ,  John Nelson ,  Jason Thomas Roland ,  Paul Vincent Rucker ,  David Charles Tully

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

摘要： 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：USRE46942E1

公开(公告)日：2018-07-10

申请号：US15786125

申请日：2017-10-17

申请人： NOVARTIS AG

发明人： Christine Hiu-Tung Chen ,  Donovan Noel Chin ,  Lucien V. DiPietro ,  Jianmei Fan ,  Mark G. Palermo ,  Michael David Shultz ,  Bakary-Barry Toure

IPC分类号： C07D491/052 ,  C07D493/04 ,  C07D401/12 ,  C07D401/04 ,  C07D401/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04

CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D491/052 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04

摘要： The present invention provides for compounds of formula (I): wherein R1-R4 and n are defined herein. The present invention also provides for pharmaceutical compositions and combinations comprising a compound of formula (I) as well as for the use of such compounds as tankyrase inhibitors and in the treatment of Wnt signaling and tankyrase 1 and 2 signaling related disorders which include, but are not limited to, cancer.

公开(公告)号：US09981926B2

公开(公告)日：2018-05-29

申请号：US15104729

申请日：2014-12-18

申请人： Birgit Bollbuck ,  Christian Markert ,  Wolfgang Miltz ,  Till Roehn

发明人： Birgit Bollbuck ,  Christian Markert ,  Wolfgang Miltz ,  Till Roehn

IPC分类号： C07D257/04 ,  C07D401/00 ,  C07D403/00 ,  A61K31/41 ,  C07D231/12 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12 ,  C07D271/10 ,  A61K45/06 ,  A61K31/415 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/428 ,  A61K31/4439

CPC分类号： C07D257/04 ,  A61K31/41 ,  A61K31/415 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/428 ,  A61K31/4439 ,  A61K45/06 ,  C07D231/12 ,  C07D271/10 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12

摘要： The present invention describes novel heteroaryl butanoic acid derivatives that are good drug candidates especially with regard to leukotriene A4 hydrolase (LTA4H). The present invention also relates to pharmaceutical compositions comprising said novel heteroaryl butanoic acid derivatives, methods of using said compounds in the treatment of various diseases and disorders, and processes for preparing the said novel compounds.

公开(公告)号：US09815813B2

公开(公告)日：2017-11-14

申请号：US15110504

申请日：2015-01-16

申请人： Zhuoliang Chen ,  Michael Dore ,  Jorge Garcia Fortanet ,  Rajesh Karki ,  Mitsunori Kato ,  Matthew J. LaMarche ,  Lawrence Blas Perez ,  Sarah Williams ,  Martin Sendzik

发明人： Zhuoliang Chen ,  Michael Dore ,  Jorge Garcia Fortanet ,  Rajesh Karki ,  Mitsunori Kato ,  Matthew J. LaMarche ,  Lawrence Blas Perez ,  Sarah Williams ,  Martin Sendzik

IPC分类号： A61K31/4427 ,  C07D401/04 ,  C07D401/14 ,  C07D241/26 ,  C07D249/14

CPC分类号： C07D401/04 ,  C07D241/26 ,  C07D249/14 ,  C07D401/14

摘要： The present invention relates to compounds of formula I: in which Y1, Y2, Y3, R1, R2a, R2b, R3a, R3b, R4a, R4b, R5a, R5b are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.

公开(公告)号：US09688689B2

公开(公告)日：2017-06-27

申请号：US14709852

申请日：2015-05-12

申请人： Ha-Soon Choi ,  James Paul Lajiness ,  Srinivasa Reddy Natala ,  Bao Nguyen ,  Hank Michael James Petrassi ,  Zhicheng Wang

发明人： Ha-Soon Choi ,  James Paul Lajiness ,  Srinivasa Reddy Natala ,  Bao Nguyen ,  Hank Michael James Petrassi ,  Zhicheng Wang

IPC分类号： C07D493/08 ,  A61K31/443 ,  A61K31/4245 ,  A61K31/4155 ,  A61K31/506 ,  A61K31/34 ,  A61K31/4439 ,  A61K31/5377 ,  A61K31/351 ,  A61K31/4545 ,  A61K31/4525 ,  A61K31/497 ,  A61K31/444 ,  A61K45/06 ,  C07D491/18

CPC分类号： A61K31/443 ,  A61K31/34 ,  A61K31/351 ,  A61K31/4155 ,  A61K31/416 ,  A61K31/4245 ,  A61K31/4433 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4525 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  A61L27/54 ,  A61L2300/412 ,  A61L2430/06 ,  C07D491/18 ,  C07D493/08 ,  C12N5/0655 ,  C12N2501/999 ,  C12N2506/1346

摘要： The present invention provides compounds of formula I: or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds, and methods of using such compounds for treatment of joint damage or joint injury in a mammal, and for inducing differentiation of mesenchymal stem cells into chondrocytes.

公开(公告)号：US09682939B2

公开(公告)日：2017-06-20

申请号：US15034280

申请日：2014-11-04

申请人： Donatella Chianelli ,  Xiaodong Liu ,  Valentina Molteni ,  John Nelson ,  Jason Thomas Roland ,  Paul Vincent Rucker ,  David Charles Tully

发明人： Donatella Chianelli ,  Xiaodong Liu ,  Valentina Molteni ,  John Nelson ,  Jason Thomas Roland ,  Paul Vincent Rucker ,  David Charles Tully

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

CPC分类号： C07D231/54 ,  A61K31/416 ,  A61K31/4162 ,  A61K31/4439 ,  A61K31/4745 ,  C07D471/04 ,  C07D471/06 ,  C07D491/052

摘要： 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：US09546138B2

公开(公告)日：2017-01-17

申请号：US14648217

申请日：2013-12-12

申请人： Ravinder Reddy Kondreddi ,  Ngai Ling Ma ,  Stefan Peukert ,  Srinivasa P S Rao ,  Manjunatha Ujjini

发明人： Ravinder Reddy Kondreddi ,  Ngai Ling Ma ,  Stefan Peukert ,  Srinivasa P S Rao ,  Manjunatha Ujjini

IPC分类号： C07D213/69 ,  C07F9/58 ,  C07D401/06 ,  C07D405/06 ,  C07D213/64 ,  A61K31/4412 ,  A61K31/4433 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/675 ,  A61K45/06 ,  C07D401/04

CPC分类号： C07D213/69 ,  A61K31/4412 ,  A61K31/4433 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/675 ,  A61K45/06 ,  C07D213/64 ,  C07D401/04 ,  C07D401/06 ,  C07D405/06 ,  C07F9/58

摘要： A compound of Formula (I) is provided that has been shown to be useful for treating a disease, disorder or syndrome that is mediated by the inhibition of mycolic acid biosynthesis through inhibition of M. tuberculosis Enoyl Acyl Carrier Protein Reductase enzyme (InhA): wherein R1, R2, R3, R4 and R5 are as defined herein.

摘要翻译： 提供式（I）的化合物，其已被证明可用于治疗通过抑制结核分枝杆菌乙酰基酰基载体蛋白还原酶（InhA）而抑制霉菌酸生物合成介导的疾病，病症或综合征： 其中R1，R2，R3，R4和R5如本文所定义。

公开(公告)号：US09303034B2

公开(公告)日：2016-04-05

申请号：US14574775

申请日：2014-12-18

申请人： Agnes Biggart ,  Fang Liang ,  Casey Jacob Nelson Mathison ,  Valentina Molteni ,  Advait Suresh Nagle ,  Frantisek Supek ,  Vince Yeh

发明人： Agnes Biggart ,  Fang Liang ,  Casey Jacob Nelson Mathison ,  Valentina Molteni ,  Advait Suresh Nagle ,  Frantisek Supek ,  Vince Yeh

IPC分类号： A61K31/519 ,  C07D487/04 ,  C07D519/00 ,  C07F5/02 ,  C07F7/08

CPC分类号： A61K31/519 ,  A61K31/5377 ,  A61K31/695 ,  A61K45/06 ,  C07D487/04 ,  C07D519/00 ,  C07F5/027 ,  C07F7/0814

摘要： The present invention provides compounds of Formula A: or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a parasite, such as leishmaniasis, human African trypanosomiasis and Chagas disease.

摘要翻译： 本发明提供式A化合物或其药学上可接受的盐，互变异构体或立体异构体，其中变量如本文所定义。 本发明还提供了包含这些化合物的药物组合物和使用这些化合物治疗，预防，抑制，改善或消除由寄生虫引起的疾病的病理和/或症状的方法，例如利什曼病，人非洲锥虫病和查加斯 疾病。