公开(公告)号：US09351973B2

公开(公告)日：2016-05-31

申请号：US14346518

申请日：2012-09-17

Applicant: D. Jonathan Bennett ,  Jaiqiang Cai ,  Emma Carswell ,  Andrew Cooke ,  Scott B. Hoyt ,  Clare London ,  John MacLean ,  Min K. Park ,  Paul Ratcliffe ,  Yusheng Xiong ,  Swapan Kumar Samanta ,  Bheemashankar A. Kulkarni

Inventor： D. Jonathan Bennett ,  Jaiqiang Cai ,  Emma Carswell ,  Andrew Cooke ,  Scott B. Hoyt ,  Clare London ,  John MacLean ,  Min K. Park ,  Paul Ratcliffe ,  Yusheng Xiong ,  Swapan Kumar Samanta ,  Bheemashankar A. Kulkarni

IPC: C07D471/04 ,  A61K31/437 ,  C07D487/04 ,  A61K31/519 ,  A61P9/12 ,  A61P13/12 ,  A61P9/00 ,  A61P9/10 ,  A61P1/16

CPC classification number: A61K31/519 ,  A61K31/437 ,  A61K31/444 ,  C07D471/04 ,  C07D487/04

Abstract: This invention relates to pyrazolopyridyl compounds of the structural formula: or their pharmaceutically acceptable salts, wherein the variable are defined herein. The inventive compounds selectively inhibit aldosterone synthase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as potentially to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthase.

Abstract translation: 本发明涉及以下结构式的吡唑并吡啶基化合物或其药学上可接受的盐，其中该变量在本文中定义。 本发明化合物选择性地抑制醛固酮合酶。 本发明还提供包含式I化合物或其盐的药物组合物，以及潜在的治疗，改善或预防可通过抑制醛固酮合酶治疗的病症的方法。

公开(公告)号：US09173873B2

公开(公告)日：2015-11-03

申请号：US14346403

申请日：2012-09-17

Applicant: Amjad Ali ,  D. Jonathan Bennett ,  Jaiqiang Cai ,  Emma Carswell ,  Andrew Cooke ,  Scott B. Hoyt ,  Michael Lo ,  Clare London ,  John MacLean ,  Min K. Park ,  Paul Ratcliffe ,  Jerry Andrew Taylor ,  Brent Whitehead ,  Yusheng Xiong

Inventor： Amjad Ali ,  D. Jonathan Bennett ,  Jaiqiang Cai ,  Emma Carswell ,  Andrew Cooke ,  Scott B. Hoyt ,  Michael Lo ,  Clare London ,  John MacLean ,  Min K. Park ,  Paul Ratcliffe ,  Jerry Andrew Taylor ,  Brent Whitehead ,  Yusheng Xiong

IPC: A61K31/437 ,  C07D471/04 ,  C07D487/04

Abstract: This invention relates to imidazopyridyl compounds of the structural formula: I or their pharmaceutically acceptable salts, wherein the variable are defined herein. The inventive compounds selectively inhibit aldosterone synthase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as potentially to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthase.

公开(公告)号：US07572822B2

公开(公告)日：2009-08-11

申请号：US12011967

申请日：2008-01-30

Applicant: Prasun K. Chakravarty ,  Louis L. Zuegner, III, legal representative ,  William H. Parsons ,  Brenda Palucki ,  Bishan Zhou ,  Min K. Park

Inventor： Michael H. Fisher

IPC: A61K31/4196 ,  A61K31/41 ,  C07D249/08

CPC classification number: C07D249/08 ,  C07D249/10

Abstract: Biaryl substituted triazole compounds represented by Formula I, II or III, or pharmaceutically acceptable salts thereof, and a process for making such compounds and salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, epilepsy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds. A method of administering local anesthesia comprises administering an effective amount of a compound of the instant invention, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier.

Abstract translation: 由式I，II或III表示的二芳基取代的三唑化合物或其药学上可接受的盐，以及制备这些化合物及其盐的方法。 药物组合物包含单独的或与一种或多种其它治疗活性化合物组合的有效量的本发明化合物和药学上可接受的载体。 治疗与钠通道活性相关或由其引起的疾病的方法，包括例如急性疼痛，慢性疼痛，内脏痛，炎性疼痛，神经性疼痛，癫痫，肠易激综合征，抑郁症，焦虑症，多发性硬化症和双相 包括单独施用有效量的本发明化合物或与一种或多种其它治疗活性化合物组合施用。 施用局部麻醉的方法包括单独施用有效量的本发明化合物或与一种或多种其它治疗活性化合物和药学上可接受的载体组合施用。

公开(公告)号：US07414057B2

公开(公告)日：2008-08-19

申请号：US10526178

申请日：2003-09-05

Applicant: Raman Kumar Bakshi ,  Ravi P. Nargund ,  Brenda L. Palucki ,  Min K. Park ,  Zhixiong Ye

Inventor： Raman Kumar Bakshi ,  Ravi P. Nargund ,  Brenda L. Palucki ,  Min K. Park ,  Zhixiong Ye

IPC: C07D401/12 ,  C07D403/12 ,  A61K31/453 ,  A61K31/4545 ,  A61P3/04 ,  A61P3/10

CPC classification number: C07D401/12 ,  C07D211/18 ,  C07D211/22 ,  C07D211/62 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D487/08

Abstract: Certain novel piperazine urea derivatives are agonists of the human melanocortin-4 receptor (MC-4R) and, in particular, are receptor-subtype selective agonists of MC-4R. They are useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity and diabetes.

Abstract translation: 某些新型哌嗪脲衍生物是人类黑皮质素-4受体（MC-4R）的激动剂，特别是MC-4R的受体亚型选择性激动剂。 它们可用于治疗，控制或预防对MC-4R活化反应的疾病和病症，例如肥胖症和糖尿病。

公开(公告)号：US07326726B2

公开(公告)日：2008-02-05

申请号：US10799230

申请日：2004-03-12

Applicant: Prasun K. Chakravarty ,  Louis L. Zuegner III, legal representative ,  Brenda Palucki ,  Min K. Park ,  William H. Parsons ,  Bishan Zhou

Inventor： Michael H. Fisher, deceased

IPC: A61K31/41 ,  C07D249/08

CPC classification number: C07D249/08 ,  C07D249/10

Abstract: Biaryl substituted triazole compounds represented by Formula I, II or III, or pharmaceutically acceptable salts thereof, and a process for making such compounds and salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, epilepsy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds. A method of administering local anesthesia comprises administering an effective amount of a compound of the instant invention, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier.

Abstract translation: 由式I，II或III表示的二芳基取代的三唑化合物或其药学上可接受的盐，以及制备这些化合物及其盐的方法。 药物组合物包含单独的或与一种或多种其它治疗活性化合物组合的有效量的本发明化合物和药学上可接受的载体。 治疗与钠通道活性相关或由其引起的疾病的方法，包括例如急性疼痛，慢性疼痛，内脏痛，炎性疼痛，神经性疼痛，癫痫，肠易激综合征，抑郁症，焦虑症，多发性硬化症和双相 包括单独施用有效量的本发明化合物或与一种或多种其它治疗活性化合物组合施用。 施用局部麻醉的方法包括单独施用有效量的本发明化合物或与一种或多种其它治疗活性化合物和药学上可接受的载体组合施用。

公开(公告)号：US20130317057A1

公开(公告)日：2013-11-28

申请号：US13811059

申请日：2011-07-20

Applicant: Scott B. Hoyt ,  Min K. Park ,  Clare London ,  Yusheng Xiong ,  D. Jonathan Bennett ,  Jaiqiang Cai ,  Paul Ratcliffe ,  Andrew Cooke ,  Emma Carswell ,  John MacLean ,  Rohit Saxena ,  Bheemashankar A. Kulkarni ,  Archana Gupta

Inventor： Scott B. Hoyt ,  Min K. Park ,  Clare London ,  Yusheng Xiong ,  D. Jonathan Bennett ,  Jaiqiang Cai ,  Paul Ratcliffe ,  Andrew Cooke ,  Emma Carswell ,  John MacLean ,  Rohit Saxena ,  Bheemashankar A. Kulkarni ,  Archana Gupta

IPC: C07D401/04 ,  C07D413/14 ,  A61K31/4375 ,  A61K31/4709 ,  A61K31/4439 ,  C07D471/04

CPC classification number: C07D401/04 ,  A61K31/4184 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/4709 ,  C07D413/14 ,  C07D471/04

Abstract: The invention involves compounds of structural Formula (I) and the pharmaceutically acceptable salts thereof. The compounds of the invention are effective at selectively inhibiting CYP11B2, and are therefore useful for the treatment or prophylaxis of disorders that are associated with elevated aldosterone levels, including, but not limited to, hypertension and heart failure.

Abstract translation: 本发明涉及结构式（I）的化合物及其药学上可接受的盐。 本发明的化合物对选择性抑制CYP11B2有效，因此可用于治疗或预防与升高的醛固酮水平相关的病症，包括但不限于高血压和心力衰竭。

公开(公告)号：US20090074890A1

公开(公告)日：2009-03-19

申请号：US10578950

申请日：2004-11-05

Applicant: Min K. Park ,  Prasun K. Chakravarty ,  Bishan Zhou ,  Edward Gonzalez ,  Hyun Ok ,  Brenda Palucki ,  William H. Parsons ,  Rosemary Sisco ,  Michael H. Fisher ,  Louis L. Zuegner, III

Inventor： Min K. Park ,  Prasun K. Chakravarty ,  Bishan Zhou ,  Edward Gonzalez ,  Hyun Ok ,  Brenda Palucki ,  William H. Parsons ,  Rosemary Sisco ,  Michael H. Fisher ,  Louis L. Zuegner, III

IPC: C07D249/08 ,  A61P29/00 ,  A61P9/00 ,  A61P25/00 ,  A61K33/00 ,  A61K31/4196 ,  A61P1/00 ,  A61P31/12 ,  A61P37/00

CPC classification number: C07D249/10 ,  C07D403/10

Abstract: Substituted triazole compounds represented by Formula I, II or III, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, migraine, headache pain, migraine headache, epilepsy, irritable bowel syndrome, diabetic neuropathy, multiple sclerosis, manic depression and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds. A method of administering local anesthesia comprises administering an effective amount of a compound of the instant invention, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier (I), (II), (III).

Abstract translation: 由式I，II或III表示的取代的三唑化合物或其药学上可接受的盐。 药物组合物包含单独的或与一种或多种其它治疗活性化合物组合的有效量的本发明化合物和药学上可接受的载体。 治疗与钠通道活性相关或由其引起的疾病的方法，包括例如急性疼痛，慢性疼痛，内脏痛，炎性疼痛，神经性疼痛，偏头痛，头痛，偏头痛，癫痫，肠易激综合征，糖尿病 神经病，多发性硬化症，躁狂抑郁症和双相性精神障碍，包括单独施用有效量的本发明化合物或与一种或多种其它治疗活性化合物组合施用。 施用局部麻醉的方法包括单独施用有效量的本发明化合物或与一种或多种其它治疗活性化合物和药学上可接受的载体（I），（II），（III） 。

公开(公告)号：US20080171777A1

公开(公告)日：2008-07-17

申请号：US12011967

申请日：2008-01-30

Applicant: Prasun K. Chakravarty ,  Michael H. Fisher ,  Louis L. Zuegner ,  William H. Parsons ,  Brenda Palucki ,  Bishan Zhou ,  Min K. Park

Inventor： Prasun K. Chakravarty ,  Michael H. Fisher ,  Louis L. Zuegner ,  William H. Parsons ,  Brenda Palucki ,  Bishan Zhou ,  Min K. Park

IPC: A61K31/4196 ,  C07D249/08 ,  A61P23/02 ,  A61P25/04

CPC classification number: C07D249/08 ,  C07D249/10

Abstract: Biaryl substituted triazole compounds represented by Formula I, II or III, or pharmaceutically acceptable salts thereof, and a process for making such compounds and salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, epilepsy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds. A method of administering local anesthesia comprises administering an effective amount of a compound of the instant invention, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier.

公开(公告)号：US06767915B2

公开(公告)日：2004-07-27

申请号：US10343040

申请日：2003-01-27

Applicant: Raman K. Bakshi ,  Khaled J. Barakat ,  Yingjie Lai ,  Ravi P. Nargund ,  Brenda L. Palucki ,  Min K. Park ,  Iyassu K. Sebhat ,  Zhixiong Ye ,  Arthur A. Patchett

Inventor： Raman K. Bakshi ,  Khaled J. Barakat ,  Yingjie Lai ,  Ravi P. Nargund ,  Brenda L. Palucki ,  Min K. Park ,  Iyassu K. Sebhat ,  Zhixiong Ye ,  Arthur A. Patchett

IPC: A61K31445

CPC classification number: C07D211/62 ,  A61K31/445 ,  A61K31/451 ,  A61K31/454 ,  A61K31/4545 ,  C07D211/20 ,  C07D211/24 ,  C07D211/26 ,  C07D401/06 ,  C07D409/12 ,  C07D413/06 ,  C07D417/06 ,  C07D487/08 ,  C07D491/08

Abstract: Certain novel 4-substituted piperidine compounds are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.

Abstract translation: 某些新的4-取代的哌啶化合物是人类黑皮质素受体的激动剂，特别是人黑素皮质素-4受体（MC-4R）的选择性激动剂。 因此，它们可用于治疗，控制或预防对MC-4R的激活反应的疾病和病症，例如肥胖，糖尿病，性功能障碍，包括勃起功能障碍和女性性功能障碍。

公开(公告)号：US10442819B2

公开(公告)日：2019-10-15

申请号：US15532549

申请日：2015-12-01

Applicant: Christian Fischer ,  Stephane L. Bogen ,  Matthew L. Childers ,  Francesc Xavier Fradera Llinas ,  J. Michael Ellis ,  Sara Esposite ,  Qingmei Hong ,  Chunhui Huang ,  Alexander J. Kim ,  John W. Lampe ,  Michelle R. Machacek ,  Daniel R. McMasters ,  Ryan D. Otte ,  Dann L. Parker, Jr. ,  Michael Reutershan ,  Nunzio Sciammetta ,  Pengcheng P. Shao ,  David L. Sloman ,  Feroze Ujjainwalla ,  Catherine White ,  Zhicai Wu ,  Yang Yu ,  Kake Zhao ,  Craig Gibeau ,  Tesfaye Biftu ,  Purakkattle Biju ,  Lei Chen ,  Joshua Close ,  Peter H. Fuller ,  Xianhai Huang ,  Min K. Park ,  Valdimir Simov ,  David J. Witter ,  Hongjun Zhang

Inventor： Christian Fischer ,  Stephane L. Bogen ,  Matthew L. Childers ,  Francesc Xavier Fradera Llinas ,  J. Michael Ellis ,  Sara Esposite ,  Qingmei Hong ,  Chunhui Huang ,  Alexander J. Kim ,  John W. Lampe ,  Michelle R. Machacek ,  Daniel R. McMasters ,  Ryan D. Otte ,  Dann L. Parker, Jr. ,  Michael Reutershan ,  Nunzio Sciammetta ,  Pengcheng P. Shao ,  David L. Sloman ,  Feroze Ujjainwalla ,  Catherine White ,  Zhicai Wu ,  Yang Yu ,  Kake Zhao ,  Craig Gibeau ,  Tesfaye Biftu ,  Purakkattle Biju ,  Lei Chen ,  Joshua Close ,  Peter H. Fuller ,  Xianhai Huang ,  Min K. Park ,  Valdimir Simov ,  David J. Witter ,  Hongjun Zhang

IPC: A61K31/351 ,  A61K31/4353 ,  A61K31/5355 ,  A61K31/551 ,  C07D471/04 ,  C07D471/14 ,  C07D498/08 ,  C07D471/08 ,  C07D498/04 ,  C07D498/10 ,  A01N43/00

Abstract: The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes: (I). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.