The discovery of orally available thrombin inhibitors: Studies towards the optimisation of CGH1668

DOI: 10.1016/S0960-894X(98)00640-4

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 3583 - 3588 (1998)

Update date:2022-08-03

Topics:

Authors:

Ambler, John

Baker, Emma

Brown, Lyndon

Butler, Paul

Farr, Dave

Dunnet, Karen

Le Grand, Darren

Janus, Diana

Jones, Darryl

Menear, Keith

Mercer, Mark

Smith, Garrick

Talbot, Mark

Tweed, Morris

Read Full Text PDF DownLoad Join now for total 90,000,000 free articles

Article abstract of DOI:10.1016/S0960-894X(98)00640-4

The chemical optimisation of CGH1668 1 is described employing an in vivo model of absorption to determine the influence on bioavailability of single point modifications to five key molecular templates. The discovery of an orally bioavailable and selective thrombin inhibitor, 24, highlights the utility of this approach.

Full text of DOI:10.1016/S0960-894X(98)00640-4

Products guided by the article

Product name:N-[2-(4-Aminophenyl)-1(S)-[4-(2-fluoroethyl)piperidin-1-ylcarbonyl]ethyl]-4-[1(S)-benzyl-2-(4-morpholinyl)ethyl]pyridine-3-sulfonamide

Cas No:200270-65-1

R&D Labs maybe for 200270-65-1

UNION PHARMPRO CO.,LTD

Contact:18710867521(wechat)

Address:Rm10516,Galaxy Tech Building #2,No.25 Tangyan Rd,Hi-Tech Zone,Xi'an, China
Kaymossy BioChem Tech Co., Ltd

website:http://www.kaimosi.com

Contact:0571-87191913/0571-87199097

Address:Room 215, Building 3rd, No.288 Ningxia Road, Qingdao city, China
Wuhan Yitongtai Science and Technology Co.,Ltd.

Contact:+86-27-88933550

Address:27th Fl. Bldg. 1, Shuian International Mansion, Heping Ave, Wuhan, Hubei, China
Taizhou Sunny Chemical Co.,Ltd

Contact:+86-523-86920899 +86-13951172783

Address:No.11 Xingyuang road, Gaoyong Chemical Industry Park, Gaogang Jiangsu China
Junkai (Tianjin) Chemical Co., Ltd.

website:http://www.junkaichem.com

Contact:86-22-85689515

Address:Room 8-501, Building K2, The Hi-Tech Green Industrial Base, No.6, 6th Road, Hi-Tech Development Road, Tianjin Hi-Tech IndustrialPark, Tianjin, China.

Relevant to this article

An effective aza-michael addition of aromatic amines to electron-deficient alkenes in alkaline Al₂O₃

Doi:10.1016/j.tet.2010.05.054
(2010)
Highly diastereoselective hetero-Diels-Alder reactions of alkenyldihydrooxazoles as an approach to novel pyrimidine derivatives

Doi:10.1039/a705571d
(1997)
Synthesis of N-acetyl derivatives of 5- and 6-ethoxy-2-methylthiobenzimidazole and their cardiotonic activity

Doi:10.1007/BF02291796
(1997)
Doi:10.1021/jm00301a034
(1969)
The Generation and Reactivity of Versatile Ruthenium Carbonyl Organometallic Intermediates by Cluster Photochemistry

Doi:10.1039/DT9950002923
(1995)
Experimental and theoretical studies on the hydrogen-bond-promoted enantioselective hetero-Diels-Alder reaction of Danishefsky's diene with benzaldehyde

Doi:10.1021/jo060129c
(2006)

Article Doi