公开(公告)号：US20050038068A1

公开(公告)日：2005-02-17

申请号：US10847144

申请日：2004-05-17

Applicant: Rajesh Iyengar ,  Andrew Judd ,  Gang Zhao ,  Philip Kym ,  Hing Sham ,  Yugui Gu ,  Gang Liu ,  Mei Liu ,  Hongyu Zhao ,  Richard Clark ,  Ernst Frevert ,  Barbara Cool ,  Tianyuan Zhang ,  Robert Keyes ,  Todd Hansen ,  Zhili Xin

Inventor： Rajesh Iyengar ,  Andrew Judd ,  Gang Zhao ,  Philip Kym ,  Hing Sham ,  Yugui Gu ,  Gang Liu ,  Mei Liu ,  Hongyu Zhao ,  Richard Clark ,  Ernst Frevert ,  Barbara Cool ,  Tianyuan Zhang ,  Robert Keyes ,  Todd Hansen ,  Zhili Xin

IPC: A61K31/4743 ,  C07D495/04 ,  C07D498/02

CPC classification number: C07D495/04

Abstract: The present invention relates to compounds that activate AMP-activated protein kinase (AMPK), including the preparation of the compounds, compositions containing the compounds and the use of the compounds in the prevention or treatment of disorders such as diabetes, metabolic syndrome, and obesity.

Abstract translation: 本发明涉及活化AMP-活化蛋白激酶（AMPK）的化合物，包括化合物的制备，含有这些化合物的组合物以及该化合物在预防或治疗诸如糖尿病，代谢综合征和肥胖症中的用途 。

公开(公告)号：US20090281050A1

公开(公告)日：2009-11-12

申请号：US12437616

申请日：2009-05-08

Applicant: Rajesh Iyengar ,  Yanchun Wang ,  Ly Tam Phan ,  Yat Sun Or

Inventor： Rajesh Iyengar ,  Yanchun Wang ,  Ly Tam Phan ,  Yat Sun Or

IPC: A61K31/7048 ,  C07H17/08 ,  A61P31/04

CPC classification number: A61K31/706 ,  A61K31/7056 ,  C07H17/08

Abstract: The present invention discloses compounds of formula (I) or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit superior antibacterial properties, particularly against Haemophilus influenzae. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.

Abstract translation: 本发明公开了式（I）化合物或其药学上可接受的盐，酯或前药：其表现出优异的抗菌性，特别是抗流感嗜血杆菌。 本发明还涉及包含上述化合物的药物组合物，用于给予需要抗生素治疗的受试者。 本发明还涉及通过施用包含本发明化合物的药物组合物来治疗受试者的细菌感染的方法。 本发明还包括制备本发明化合物的方法。

公开(公告)号：US20080064717A1

公开(公告)日：2008-03-13

申请号：US11749952

申请日：2007-05-17

Applicant: Rajesh Iyengar ,  Gang Zhao ,  Jennifer Freeman ,  Ju Gao ,  Andrew Judd ,  Philip Kym ,  John Lynch ,  Mathew Mulhern ,  Andrew Souers

Inventor： Rajesh Iyengar ,  Gang Zhao ,  Jennifer Freeman ,  Ju Gao ,  Andrew Judd ,  Philip Kym ,  John Lynch ,  Mathew Mulhern ,  Andrew Souers

IPC: A61K31/4402 ,  A61K31/17 ,  A61K31/19 ,  A61P3/00 ,  C07C61/06 ,  C07D471/04 ,  C07D213/46 ,  C07C275/28 ,  A61P1/16 ,  A61K31/4375

CPC classification number: C07C335/22 ,  C07C229/46 ,  C07C275/30 ,  C07C275/32 ,  C07C275/38 ,  C07C279/28 ,  C07C2601/08 ,  C07C2601/14 ,  C07D213/55 ,  C07D213/75 ,  C07D277/30 ,  C07D333/22 ,  C07D333/36 ,  C07D401/04 ,  C07D401/12 ,  C07D409/12 ,  C07D409/14

Abstract: The present invention relates to compounds of formula (I): wherein R1, R3, X, Q, Z, A, 9, m, and n are defined herein Pharmaceutical compositions and methods for treating DGAT-1 related diseases or conditions are also disclosed.

Abstract translation: 本发明涉及式（I）化合物：其中R 1，R 3，X，Q，Z，A，9，m和n如本文所定义 还公开了治疗DGAT-1相关疾病或病症的药物组合物和方法。

公开(公告)号：US06921821B2

公开(公告)日：2005-07-26

申请号：US10459682

申请日：2003-06-11

Applicant: Christopher Blackburn ,  Su-Jen Lai ,  Jennifer L. Che ,  Martin P. Maguire ,  Michael A. Patane ,  Matthew J. LaMarche ,  Courtney A. Cullis ,  James Brown ,  Anil Vasudevan ,  Jennifer C. Freeman ,  Mathew M. Mulhern ,  John K. Lynch ,  Ju Gao ,  Dariusz Wodka ,  Andrew J. Souers ,  Rajesh Iyengar ,  Mary Katherin Verzal ,  Philip R. Kym

Inventor： Christopher Blackburn ,  Su-Jen Lai ,  Jennifer L. Che ,  Martin P. Maguire ,  Michael A. Patane ,  Matthew J. LaMarche ,  Courtney A. Cullis ,  James Brown ,  Anil Vasudevan ,  Jennifer C. Freeman ,  Mathew M. Mulhern ,  John K. Lynch ,  Ju Gao ,  Dariusz Wodka ,  Andrew J. Souers ,  Rajesh Iyengar ,  Mary Katherin Verzal ,  Philip R. Kym

IPC: C07D403/14 ,  A61K31/453 ,  A61K31/4535 ,  A61K31/454 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/517 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P5/00 ,  A61P15/00 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P43/00 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D451/04 ,  C07D205/08 ,  C07D239/02 ,  C07D401/00

CPC classification number: C07D405/14 ,  C07D401/14 ,  C07D405/12 ,  C07D409/14 ,  C07D413/14

Abstract: This invention provides compounds that are antagonists of melanin concentrating hormone receptor-1 (MCH-R1). The compounds are represented by formula I: where m is zero or one, n is zero to two, Y is oxygen or —N(R9)—, R1, R2, R3, R4, R5, R9 and Ring A are defined in the specification. Coumarin and quinolone compounds where R1 and R2 together form a fused benzo ring are preferred. The invention also provides compounds of formula VI where the coumarin moiety is replaced by a quinazolinone ring. The compounds are useful for treating MCH-R1-related disorders, particularly overweight conditions including obesity.

Abstract translation: 本发明提供了作为黑色素浓缩激素受体-1（MCH-R1）的拮抗剂的化合物。 化合物由式I表示：其中m为0或1，n为0至2，Y为氧或-N（R 9） - ，R 1， R 2，R 3，R 4，R 5，R 9和R 9，和 环A在规范中定义。 其中R 1和R 2一起形成稠合苯并环的香豆素和喹诺酮化合物是优选的。 本发明还提供式VI的化合物，其中香豆素部分被喹唑啉酮环代替。 该化合物可用于治疗MCH-R1相关疾病，特别是超重状况，包括肥胖症。

公开(公告)号：US08383785B2

公开(公告)日：2013-02-26

申请号：US12437616

申请日：2009-05-08

Applicant: Rajesh Iyengar ,  Yanchun Wang ,  Ly Tam Phan ,  Yat Sun Or

Inventor： Rajesh Iyengar ,  Yanchun Wang ,  Ly Tam Phan ,  Yat Sun Or

IPC: C07H17/08 ,  A61K31/7048 ,  C07D493/08

CPC classification number: A61K31/706 ,  A61K31/7056 ,  C07H17/08

Abstract: The present invention discloses compounds of formula (I) or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit superior antibacterial properties, particularly against Haemophilus influenzae. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.

Abstract translation: 本发明公开了式（I）化合物或其药学上可接受的盐，酯或前药：其表现出优异的抗菌性，特别是抗流感嗜血杆菌。 本发明还涉及包含上述化合物的药物组合物，用于给予需要抗生素治疗的受试者。 本发明还涉及通过施用包含本发明化合物的药物组合物来治疗受试者的细菌感染的方法。 本发明还包括制备本发明化合物的方法。

公开(公告)号：US20060287356A1

公开(公告)日：2006-12-21

申请号：US11509383

申请日：2006-08-24

Applicant: Rajesh Iyengar ,  Andrew Judd ,  Gang Zhao ,  Philip Kym ,  Hing Sham ,  Yugui Gu ,  Gang Liu ,  Mei Liu ,  Hongyu Zhao ,  Richard Clark ,  Ernst Frevert ,  Barbara Cool ,  Tianyuan Zhang ,  Robert Keyes ,  Todd Hansen ,  Zhili Xin

Inventor： Rajesh Iyengar ,  Andrew Judd ,  Gang Zhao ,  Philip Kym ,  Hing Sham ,  Yugui Gu ,  Gang Liu ,  Mei Liu ,  Hongyu Zhao ,  Richard Clark ,  Ernst Frevert ,  Barbara Cool ,  Tianyuan Zhang ,  Robert Keyes ,  Todd Hansen ,  Zhili Xin

IPC: C07D498/02 ,  A61K31/4743

CPC classification number: C07D495/04

Abstract: The present invention relates to compounds that activate AMP-activated protein kinase (AMPK), including the preparation of the compounds, compositions containing the compounds and the use of the compounds in the prevention or treatment of disorders such as diabetes, metabolic syndrome, and obesity.

公开(公告)号：US20050209274A1

公开(公告)日：2005-09-22

申请号：US11065918

申请日：2005-02-25

Applicant: John Lynch ,  Christine Collins ,  Jennifer Freeman ,  Ju Gao ,  Rajesh Iyengar ,  Andrew Judd ,  Philip Kym ,  Mathew Mulhern ,  Hing Sham ,  Andrew Souers ,  Gang Zhao ,  Dariusz Wodka

Inventor： John Lynch ,  Christine Collins ,  Jennifer Freeman ,  Ju Gao ,  Rajesh Iyengar ,  Andrew Judd ,  Philip Kym ,  Mathew Mulhern ,  Hing Sham ,  Andrew Souers ,  Gang Zhao ,  Dariusz Wodka

IPC: A61K31/452 ,  A61K31/4709 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D45/02

CPC classification number: C07D417/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14

Abstract: The present invention is directed to compounds of formula (I), which antagonize of the effects of melanin-concentrating hormone (MCH) through the melanin concentrating hormone receptor which is useful for the prevention or treatment of eating disorders, weight gain, obesity, abnormalities in reproduction and sexual behavior, thyroid hormone secretion, diuresis and water/electrolyte homeostasis, sensory processing, memory, sleeping, arousal, anxiety, depression, seizures, neurodegeneration and psychiatric disorders.

公开(公告)号：US20150274712A1

公开(公告)日：2015-10-01

申请号：US14428844

申请日：2013-09-18

Applicant: G-Yoon Jamie IM ,  Rajesh IYENGAR ,  Joel MOORE ,  Angelika FRETZEN

Inventor： G-Yoon Jamie Im ,  Rajesh Iyengar ,  Joel Moore ,  Angelika Fretzen

IPC: C07D413/14 ,  A61K31/506 ,  A61K31/513

CPC classification number: A61K31/513 ,  A61K31/506 ,  A61K45/06 ,  C07D407/14 ,  C07D409/14 ,  C07D413/14

Abstract: Compounds of Formula I are described. They are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds may be useful for treating, preventing or managing various disorders that are herein disclosed.

Abstract translation: 描述式I化合物。 它们作为sGC的刺激剂是有用的，特别是NO不依赖于血红素依赖性刺激物。 这些化合物可用于治疗，预防或治疗本文公开的各种疾病。

公开(公告)号：US20050187387A1

公开(公告)日：2005-08-25

申请号：US10787694

申请日：2004-02-25

Applicant: John Lynch ,  Christine Collins ,  Jennifer Freeman ,  Ju Gao ,  Rajesh Iyengar ,  Andrew Judd ,  Philip Kym ,  Mathew Mulhern ,  Hing Sham ,  Andrew Souers ,  Gang Zhao

Inventor： John Lynch ,  Christine Collins ,  Jennifer Freeman ,  Ju Gao ,  Rajesh Iyengar ,  Andrew Judd ,  Philip Kym ,  Mathew Mulhern ,  Hing Sham ,  Andrew Souers ,  Gang Zhao

IPC: B32B27/02 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

CPC classification number: C07D405/12 ,  C07D401/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention is directed to compounds of formula (I), which antagonize of the effects of melanin-concentrating hormone (MCH) through the melanin concentrating hormone receptor which is useful for the prevention or treatment of eating disorders, weight gain, obesity, abnormalities in reproduction and sexual behavior, thyroid hormone secretion, diuresis and water/electrolyte homeostasis, sensory processing, memory, sleeping, arousal, anxiety, depression, seizures, neurodegeneration and psychiatric disorders.

Abstract translation: 本发明涉及通过黑色素浓缩激素受体拮抗黑色素浓缩激素（MCH）的作用的式（I）化合物，其可用于预防或治疗进食障碍，体重增加，肥胖症，异常 生殖和性行为，甲状腺激素分泌，利尿和水/电解质体内平衡，感觉加工，记忆，睡眠，觉醒，焦虑，抑郁，癫痫发作，神经变性和精神疾病。