公开(公告)号：US06958145B2

公开(公告)日：2005-10-25

申请号：US10312155

申请日：2001-06-28

Applicant: Naresh Kumar ,  Roger Wayne Read

Inventor： Naresh Kumar ,  Roger Wayne Read

IPC: A61K31/365 ,  A61P31/04 ,  A61P31/10 ,  C07B61/00 ,  C07C59/21 ,  C07C59/347 ,  C07D307/58 ,  C07D307/60 ,  C08F34/00 ,  C08F224/00 ,  C07D307/33

CPC classification number: C07D307/58 ,  C07C59/347 ,  C07D307/60 ,  C08F224/00

Abstract: A method for the preparation of a compound of formula (II) wherein R1 and R2 are independently H, alkyl, alkoxy, oxoalkyl, alkenyl, aryl or arylalkyl whether unsubstituted or substituted, optionally interrupted by one or more hetero atoms, straight chain or branched chain, hydrophilic, hydrophobic or fluorophilic; R3, R4, R5 and R6 are independently or all hydrogen or halogen; provided that at least two of the R3, R4, R5 and R6 are halogens.

Abstract translation: 制备式（II）化合物的方法，其中R 1和R 2独立地是H，烷基，烷氧基，氧代烷基，烯基，芳基或芳基烷基，无论是未取代的 或取代的，任选被一个或多个杂原子间隔的直链或支链，亲水的，疏水的或富含荧光的; R 3，R 4，R 5和R 6是独立地或全部是氢或卤素; 条件是R 3，R 4，R 5和R 6中的至少两个是卤素。

公开(公告)号：US20050027143A1

公开(公告)日：2005-02-03

申请号：US10487554

申请日：2002-08-23

Applicant: Mohammad Salman ,  Purna Ray ,  Suresh Babu ,  Naresh Kumar

Inventor： Mohammad Salman ,  Purna Ray ,  Suresh Babu ,  Naresh Kumar

IPC: C07C29/147 ,  C07C33/14 ,  C07C45/29 ,  C07C47/225 ,  C07C67/343 ,  C07C403/14 ,  C07C45/45

CPC classification number: C07C403/14 ,  C07B2200/09 ,  C07C29/147 ,  C07C33/14 ,  C07C67/343 ,  C07C403/08 ,  C07C403/20 ,  C07C2601/16 ,  C07C69/608

Abstract: The present invention relates to an industrially advantageous process for the preparation of beta-ionylidencacetaldehyde of structural Formula I, which is a key intermediate for the synthesis of vitamin A and related compounds such as tretinoin and isotretinoin.

Abstract translation: 本发明涉及一种工业上有利的制备结构式I的β-离子亚基乙醛的方法，其是合成维生素A和相关化合物如维A酸和异维A酸的关键中间体。

公开(公告)号：US06686497B1

公开(公告)日：2004-02-03

申请号：US10130579

申请日：2002-09-20

Applicant: Mohammad Salman ,  J. Suresh Babu ,  Purna C. Ray ,  Sujay Biswas ,  Naresh Kumar

Inventor： Mohammad Salman ,  J. Suresh Babu ,  Purna C. Ray ,  Sujay Biswas ,  Naresh Kumar

IPC: C07C6976

CPC classification number: C07C67/10 ,  C07C67/313 ,  C07C69/92

Abstract: The present invention relates to a new and industrially advantageous process for the preparation of 3-ethoxy-4-ethoxy-carbonyl-phenyl acetic acid. This compound is a key intermediate for the synthesis of Repaglinide, an oral hypoglycemic agent.

Abstract translation: 本发明涉及用于制备3-乙氧基-4-乙氧羰基 - 苯基乙酸的新的和工业上有利的方法。 该化合物是合成瑞格列奈（口服降糖药）的关键中间体。

公开(公告)号：US5792874A

公开(公告)日：1998-08-11

申请号：US918393

申请日：1997-08-26

Applicant: Jag Mohan Khanna ,  Naresh Kumar ,  Chandrahas Khanduri ,  Mukesh Kumar Sharma ,  Pankaj Sharma ,  Swargam Sathyanarayan ,  Girij Pal Singh

Inventor： Jag Mohan Khanna ,  Naresh Kumar ,  Chandrahas Khanduri ,  Mukesh Kumar Sharma ,  Pankaj Sharma ,  Swargam Sathyanarayan ,  Girij Pal Singh

IPC: A61K31/55 ,  A61P21/02 ,  A61P23/00 ,  A61P25/20 ,  C07D339/06 ,  C07D339/08 ,  C07D409/10 ,  C07D487/04 ,  C07D204/04

CPC classification number: C07D339/08 ,  C07D339/06 ,  C07D409/10 ,  C07D487/04

Abstract: A multistep process for producing 8-chloro-6-(2-fluorophenyl)-1-methyl-4-H-imidazo�1,5a!�1,4!benzodiazepine (midazolam) comprises treating a compound of Formula II with a lower alkyl dithiol to produce a compound of Formula III, wherein n=2 or 3, converting the compound of Formula III to a compound of Formula VII, and then treating the compound of Formula VII with a deprotecting agent, thereby producing midazolam. Novel intermediate compounds are also disclosed.

Abstract translation: 用于制备8-氯-6-（2-氟苯基）-1-甲基-4H-咪唑并[1,5a] [1,4]苯并二氮杂（咪达唑仑）的多步方法包括用较低的 制备式III化合物，其中n = 2或3，将式III化合物转化为式VII化合物，然后用脱保护剂处理式VII化合物，从而产生咪达唑仑。 还公开了新的中间体化合物。

公开(公告)号：US5621120A

公开(公告)日：1997-04-15

申请号：US265307

申请日：1994-06-24

Applicant: Jag M. Khanna ,  Naresh Kumar ,  Brij Khera ,  Mahavir S. Khanna

Inventor： Jag M. Khanna ,  Naresh Kumar ,  Brij Khera ,  Mahavir S. Khanna

IPC: C07D307/52 ,  C07D307/02

CPC classification number: C07D307/52

Abstract: A process for the manufacture of Form 1 ranitidine hydrochloride (N-[2-[[[5-(Dimethylamino)methyl]-2-furanyl]methyl]thio]ethyl-N'-methyl-2-nitro-1,1-ethenediamine) hydrochloride, is described. A process to convert ranitidine hydrochloride Form 2 to Form 1 is also described.

Abstract translation: 制备形式1盐酸雷尼替丁的方法（N- [2 - [[[5-（二甲基氨基）甲基] -2-呋喃基]甲基]硫基]乙基-N'-甲基-2-硝基-1,1- 乙烯二胺）盐酸盐。 还描述了将盐酸雷尼替丁形式2转化为形式1的方法。

公开(公告)号：US4995593A

公开(公告)日：1991-02-26

申请号：US453999

申请日：1989-12-20

Applicant: David A. Ford ,  Gordon J. S. Higginbotham ,  David R. Pugh ,  Naresh Kumar

Inventor： David A. Ford ,  Gordon J. S. Higginbotham ,  David R. Pugh ,  Naresh Kumar

IPC: B22D41/01 ,  B22D41/05 ,  B22D43/00 ,  C22C1/02 ,  H05B6/06 ,  H05B6/22

CPC classification number: H05B6/22 ,  B22D41/01 ,  B22D41/05 ,  B22D43/001 ,  H05B6/067

Abstract: Apparatus for pouring molten metal comprises a cold crucible 15 which has a recess adjacent its top and a pouring spout 16 positioned in the recess just below the level of the surface of the melt. The recess defines a lip above the spout which helps to ensure that there is a constant pressure head above the spout. Pivotally mounted on the lip, and biased to assume a horizontal position irrespective of the angle of tilt of the crucible is an induction coil 21. The coil induces currents in the surface of the melt and thereby moves the dross away from the pouring spout. The crucible 15 pours into a constant head hopper 22 and the opening and closing of the crucible pouring spout 16 and the angle of tilt of the crucible are controlled to ensure constant pressure head in the hopper.

Abstract translation: 用于浇注熔融金属的设备包括冷坩埚15，其具有邻近其顶部的凹部和位于刚好在熔体表面的水平面下方的凹部中的倾倒口16。 凹口限定出口上方的唇缘，这有助于确保在喷嘴上方有恒定的压力头。 偏心地安装在唇缘上并被偏置以呈现水平位置，而与坩埚的倾斜角度无关的是感应线圈21.线圈在熔体的表面中引起电流，从而将浮渣从倾倒口移出。 将坩埚15倒入恒定的顶部料斗22中，并且控制坩埚倾倒咀16的打开和关闭以及坩埚的倾斜角度以确保料斗中的恒定压力头。

公开(公告)号：US20140187554A1

公开(公告)日：2014-07-03

申请号：US14118116

申请日：2012-05-16

Applicant: Theodore Mark Kamenecka ,  Patrick R. Griffin ,  Youseung Shin ,  Yuanjun He ,  Anne-Laure Blayo ,  Brent R. Lyda ,  Marcel Koenig ,  Naresh Kumar ,  Thomas Burris

Inventor： Theodore Mark Kamenecka ,  Patrick R. Griffin ,  Youseung Shin ,  Yuanjun He ,  Anne-Laure Blayo ,  Brent R. Lyda ,  Marcel Koenig ,  Naresh Kumar ,  Thomas Burris

IPC: C07D317/50 ,  A61K31/496 ,  C07D295/096 ,  A61K45/06 ,  C07D295/185 ,  A61K31/5375 ,  A61K31/5377 ,  C07D213/36 ,  A61K31/495

CPC classification number: C07D317/50 ,  A61K31/495 ,  A61K31/496 ,  A61K31/5375 ,  A61K31/5377 ,  A61K45/06 ,  C07D207/09 ,  C07D209/14 ,  C07D211/22 ,  C07D213/36 ,  C07D213/61 ,  C07D213/64 ,  C07D213/74 ,  C07D213/82 ,  C07D215/12 ,  C07D233/61 ,  C07D277/28 ,  C07D277/64 ,  C07D295/096 ,  C07D295/185 ,  C07D295/205 ,  C07D295/215 ,  C07D295/26 ,  C07D307/24 ,  C07D317/58 ,  C07D319/20 ,  C07D333/20 ,  C07D333/34 ,  C07D401/12

Abstract: The invention provides small molecule modulators of retinoic acid receptor-related orphan receptors such as RORα, RORβ, or RORγ. Compounds of the invention can be effective modulators at concentrations ineffective to act on LXR receptors, or on other nuclear receptors, or other biological targets. Methods of modulation the RORs and methods of treating metabolic disorders, immune disorders, cancer, and CNS disorders wherein modulation of an ROR is medically indicated are also provided.

Abstract translation: 本发明提供了视黄酸受体相关的孤儿受体如RORα，ROR和bgr或RORγ的小分子调节剂。 本发明的化合物可以是无效作用于LXR受体或其它核受体或其他生物靶标的有效调节剂。 还提供调节ROR的方法和治疗代谢紊乱，免疫疾病，癌症和中枢神经系统疾病的方法，其中医学指示ROR的调节。

公开(公告)号：US20100222393A1

公开(公告)日：2010-09-02

申请号：US12159505

申请日：2006-12-21

Applicant: Naresh Kumar ,  Jaskiran Kaur ,  Venkata P. Palle ,  Beenu Bhatt ,  Shelly Jindal ,  Anita Chugh ,  Suman Gupta ,  Abhijit Ray ,  Shivani Malhotra ,  Raj Kumar Shirumalla

Inventor： Naresh Kumar ,  Jaskiran Kaur ,  Venkata P. Palle ,  Beenu Bhatt ,  Shelly Jindal ,  Anita Chugh ,  Suman Gupta ,  Abhijit Ray ,  Shivani Malhotra ,  Raj Kumar Shirumalla

IPC: A61K31/4439 ,  C07D233/54 ,  A61K31/4164 ,  C07D401/02 ,  A61P11/00 ,  A61P13/00 ,  A61P1/00 ,  A61P3/04 ,  A61P3/10

CPC classification number: C07D233/54 ,  C07D233/14 ,  C07D233/56 ,  C07D233/64 ,  C07D401/12

Abstract: Compounds of Formula (I), wherein represents a single bond when G is —OH and double bond when G is —O; R1 and R2 are independently selected from hydrogen, alkyl, alkenyl, alkynyl, aralkyl, cycloalkyl, aryl, heteroaryl, heterocyclyl, heterocyclylalkyl or heteroarylalkyl; R3 is selected from the group selected from hydrogen, hydroxy, alkoxy, alkenyloxy or alkynyloxy; X is selected from oxygen, —NH, —NR (wherein R is alkyl, alkenyl, alkenyl, alkynyl or aryl), sulphur or no atom; Het is heterocyclyl or heteroaryl; n is an integer from 1 to 6; are muscarinic receptor antagonists, which are useful, among other uses, for the treatment of various diseases of the respiratory, urinary and 4 i gastrointestinal systems mediated through muscarinic receptors.

Abstract translation: 式（I）的化合物，当G为-OH时，当G为-O时，表示单键; R 1和R 2独立地选自氢，烷基，烯基，炔基，芳烷基，环烷基，芳基，杂芳基，杂环基，杂环基烷基或杂芳基烷基; R3选自氢，羟基，烷氧基，烯氧基或炔氧基; X选自氧，-NH，-NR（其中R是烷基，烯基，烯基，炔基或芳基），硫或无原子; Het是杂环基或杂芳基; n是1至6的整数; 是毒蕈碱受体拮抗剂，其可用于治疗通过毒蕈碱受体介导的呼吸，尿和4I胃肠系统的各种疾病，以及其它用途。

公开(公告)号：US20100056496A1

公开(公告)日：2010-03-04

申请号：US12439771

申请日：2007-09-04

Applicant: Naresh Kumar ,  Kirandeep Kaur ,  Yogesh D. Shejul ,  Abhijit Ray ,  Suman Gupta ,  Shivani Malhotra ,  Rajkumar Shirumalla

Inventor： Naresh Kumar ,  Kirandeep Kaur ,  Yogesh D. Shejul ,  Abhijit Ray ,  Suman Gupta ,  Shivani Malhotra ,  Rajkumar Shirumalla

IPC: A61K31/55 ,  C07D223/14 ,  A61P1/00 ,  A61P11/00 ,  A61P3/00

CPC classification number: C07D221/24 ,  C07D209/12 ,  C07D209/14

Abstract: The present invention generally relates to muscarinic receptor antagonists, which are useful, among other uses, for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The present invention also relates to processes for preparing compounds described herein, pharmaceutical compositions thereof, and methods for treating diseases mediated through muscarinic receptors. Formula (I) or a pharmaceutically accepted salt, pharmaceutically acceptable solvate, enantiomers, diastereomer, polymorph or N-oxide thereof, wherein X is.

Abstract translation: 本发明一般涉及毒蕈碱受体拮抗剂，其可用于治疗通过毒蕈碱受体介导的呼吸，泌尿和胃肠系统的各种疾病，以及其它用途。 本发明还涉及制备本文所述化合物的方法，其药物组合物，以及用于治疗通过毒蕈碱受体介导的疾病的方法。 式（I）或其药学上可接受的盐，药学上可接受的溶剂合物，对映异构体，非对映体，多晶型物或N-氧化物，其中X为。

公开(公告)号：US20100016400A1

公开(公告)日：2010-01-21

申请号：US11719687

申请日：2005-11-18

Applicant: Naresh Kumar ,  Mohammad Salman ,  Kirandeep Kaur ,  Anita Mehta ,  Sudershan K. Arora ,  Anita Chugh

Inventor： Naresh Kumar ,  Mohammad Salman ,  Kirandeep Kaur ,  Anita Mehta ,  Sudershan K. Arora ,  Anita Chugh

IPC: A61K31/403 ,  C07D209/52 ,  C07D409/06 ,  A61P11/00

CPC classification number: C07D209/52 ,  C07D409/06

Abstract: The present invention generally relates to muscarinic receptor antagonists, which are useful for treating various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to processes for preparing compounds described herein, pharmaceutical compositions containing the disclosed compounds, and the methods for treating diseases mediated through muscarinic receptors.

Abstract translation: 本发明一般涉及毒蕈碱受体拮抗剂，其可用于治疗通过毒蕈碱受体介导的呼吸，泌尿和胃肠系统的各种疾病。 本发明还涉及制备本文所述化合物的方法，含有所公开化合物的药物组合物，以及用于治疗通过毒蕈碱受体介导的疾病的方法。