1
Thomas R Blohm, Brian W Metcalf: Novel steroid 5.alpha.-reductase inhibitors. Richardson Merrell, John J Kolano, Raymond A McDonald, William J Stein, March 2, 1982: US04317817 (45 worldwide citation)

Compounds of the following general formula are testosterone 5.alpha.-reductase inhibitors rendering the compounds useful in the treatment of acne and oily skin and benign prostatic hypertrophy: ##STR1## wherein R is: .dbd.O, --OH, --OCO--alkyl C.sub.1-5, --COOH, --CH.sub.2 OH, --COO--alkyl C.sub.1-6 ...


2
Dennis A Holt, Mark A Levy, Brian W Metcalf: Steroid 5-alpha-reductase inhibitors. SmithKline Beckman Corporation, Stuart R Suter, Alan D Lourie, March 20, 1990: US04910226 (40 worldwide citation)

Invented are substituted acrylate analogues of steroidal synthetic compounds, pharmaceutical compositions containing the compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase. Also invented are intermediates used in preparing these compounds.


3
Dennis A Holt, Mark A Levy, Brian W Metcalf: Phosphonic acid substituted aromatic steroids as inhibitors of steroid 5-.alpha.-reductase. SmithKline Beckman Corporation, Stuart R Suter, Alan D Lourie, November 21, 1989: US04882319 (37 worldwide citation)

Invented are phosphonic acid substituted analogues of steroidal synthetic compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase, including using these compounds to reduce or maintain prostate size. Also invented ...


4
Dennis A Holt, Conrad J Kowalski, Mark A Levy, Brian W Metcalf, Ann M Tickner: Steriod 5-alpha-reductase inhibitors. SmithKline Beecham Corporation, Wayne J Dustman, Stuart R Suter, Edward T Lentz, May 21, 1991: US05017568 (31 worldwide citation)

Invented are substituted acrylate analogues of steroidal synthetic compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase. Also invented are intermediates used in preparing these compounds.


5
Jiacheng Zhou, Pingli Liu, Qiyan Lin, Brian W Metcalf, David Meloni, Yongchun Pan, Michael Xia, Mei Li, Tai Yuen Yue, James D Rodgers, Haisheng Wang: Processes for preparing JAK inhibitors and related intermediate compounds. Incyte Corporation, Lathrop & Gage, Brian C Trinque, April 2, 2013: US08410265 (28 worldwide citation)

The present invention is related to processes for preparing chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines of Formula III, and related synthetic intermediate compounds. The chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines are useful as inhibitors of the Janus Kinase family of protein t ...


6
Dennis A Holt, Mark A Levy, Brian W Metcalf: Steroid 5-alpha-reductase inhibitors. SmithKline Beckman Corporation, Mary E McCarthy, Stuart R Suter, Alan D Lourie, December 19, 1989: US04888336 (26 worldwide citation)

Invented are 4-aza-5-alpha-8(14)-17 substituted-androsten-3-ones having an 8(14), 7(8), or 16(17) double bond, optionally also having a 1(2) double bond, pharmaceutical compositions containing the compounds, and methods of using these compounds to inhibit steroid 5-alpha-reductase.


7
Philippe Bey, Brian W Metcalf, Jeffrey S Wiseman: Novel enzyme inhibitors. Richardson Merrell, John J Kolano, Raymond A McDonald, Salvatore R Conte, July 7, 1981: US04277395 (26 worldwide citation)

Compounds of the following general formula are irreversible inhibitors of pancreatic elastase: ##STR1## wherein M is hydroxy, lower alkoxy, benzyloxy or --NY.sub.1 Y.sub.2 wherein each of R.sub.4 and R.sub.5 is hydrogen or lower alkyl; R is CF.sub.3, CHF.sub.2 or CH.sub.2 F; R.sub.1 is straight or b ...


8
Dennis A Holt, Mark A Levy, Brian W Metcalf: Phosphinic acid substituted aromatic steroids as inhibitors of steroid 5-60 -reductase. SmithKline Beckman Corporation, Stuart R Suter, Edward T Lentz, June 26, 1990: US04937237 (18 worldwide citation)

Invented are phosphinic acid substituted analogues of steroidal synthetic compounds, pharamaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase, including using these compounds to reduce or maintain prostate size.


9
Brian W Metcalf, Michel Jung: .alpha.-Ethynyl tryptophanes. Merrell Toraude et Compagnie, L Ruth Hattan, Eugene O Retter, George W Rauchfuss Jr, December 25, 1979: US04180509 (18 worldwide citation)

Novel compounds of the following general formula ##STR1## and pharmaceutically acceptable salts and individual optical isomers thereof. The compounds are useful as aromatic amine decarboxylase inhibitors.


10
Brian W Metcalf, J O Neal Johnston: 10-Alkynyl steroids. Merrell Dow Pharmaceuticals, John J Kolano, Raymond A McDonald, Gary D Street, March 30, 1982: US04322416 (18 worldwide citation)

Aromatase inhibitors are provided having the formula ##STR1## wherein represents a single or double bond; R is hydrogen or C.sub.1-4 alkyl; R.sup.1 is methyl or ethyl; R.sup.2 is (H) (OR.sup.8) or .dbd.O; R.sup.3 is H or C.sub.1-3 alkyl; R.sup.4 is H or OR.sup.8 ; R.sup.5 is H, C.sub.1-3 alkyl or, w ...