Sunday Gazette-Mail from Charleston, West Virginia on June 27, 1976 · Page 114
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June 27, 1976

Sunday Gazette-Mail from Charleston, West Virginia · Page 114

Charleston, West Virginia
Issue Date:
Sunday, June 27, 1976
Page 114
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Page 114 article text (OCR)

gradually fell in love. Marriage on $60 a month did not project a particularly bountiful future, so Sternbach applied to Hoffmann-La Roche in Basel as a senior chemist. He was taken on and assigned to a group of chemists working intensively in vitamins. Fiancee Herta got a job as an office secretary, and the couple were married in 1941. To U.S. for security With World War II raging across the ' Swiss borders, the Hoffmann-La Roche director decided as a security precaution to send some of their most talented and "endangered scientists" to their U.S. branch in Nutley, N. J. Because he was both Polish and Jewish, Sternbach was one of the first to leave Basel. He and Mrs. Sternbach arrived in Montclair, N. J., in 1941, rented a furnished house, and then in 1943, when the first of their two sons was born, bought the white clapboard, two-story house in Montclair in which they have lived for 33 years. In the Roche lab in Nutley, Sternbach began to synthesize vitamins, which were then the rage. He worked out the synthesis of biotin in the vitamin ,B category. "In the United States," he explains, "patents are issued to a person, never to a company. So the biotin patents were issued to me, and I in turn signed .them over to Roche. For 10 years the company gave me a royalty on sales, which were rather small. But I had no complaints. I was grateful to the company for bringing us over from Europe, for providing my family with a certain security. After all, many people work for 30 and 40 years and invent nothing that's of value to the company. He and company 'lucky' "In my case I was lucky and so was Roche. I had worked on the development of processes for the intermediate synthesis of riboflavin, which is vitamin B-2. And again the company, to show its appreciation, gave me a small royalty." Leo Sternbach has been granted 200 U.S. patents, many of them commercially exploited by Hoffmann-La Roche. The best sellers, of course, are Valium and Librium, which together have captured more than 80 percent of the tranquilizer market in the U.S. There has always been a tremendous market for mood-altering drugs in a high-pressure society. In 1955 Dr. Frank Berger of Wallace Laboratories of Cranbury, N. J., synthesized mepro- bamate, the first of the anti-anxiety drugs. Marketed as Miltown and Equanil, the drug proved an instantaneous success. It also drove competing manufacturers to discover similar drugs that might earn a share of the constantly expanding market. At Hoffmann-La Roche, Leo Stern- bach was assigned that job. How did he go about it? "First off," he points out, "I decided that it wouldn't be very attractive to take something like Equanil and chlorpromazine and try to modify them [by changing their molecular structure]. I thought instead that it might be worthwhile to attack the problem chemically. "In thinking about classes of compounds which I could use for that purpose, I recalled a group of compounds I had worked with in Cracow--the benzheptoxdiazines. Hept is for seven, which means the compounds have an inner ring, of seven carbon atoms. "I worked with this group of compounds. They crystallized rather nicely. They had been discovered around 1900 by a German, Von Auwers. Nobody had studied their biological properties. So I thought to myself this is a wide-open field, the compounds are relatively unexplored, they might lead us to other compounds with the desired biological properties of making people calm and tranquil." The OK to work on benzheptoxdia- zines was given most reluctantly to Sternbach by his then section chief, Wolf Goldberg, "who frankly was not too optimistic." A discovery In a short time, Sternbach discovered that the benzheptoxdiazines were in fact quinazoline and oxides which were structured in such a way that he could react them with amines so as to produce a basic sidechain. After years of experimentation on number "RO5-0690," Sternbach was told by Dr. Lowell Randall, in charge of the company's biological testing, "that I had finally found something really worthwhile, that the compound showed up very nicely in the pharmacological testing and compared very nicely with meprobromate." RO5-0690 was trade-named Librium, marketed by Hoffmann-La Roche in 1960 and gradually overtook Miltown as the country's No. 1 tranquilizer. From 1960 to 1963, while Librium was overwhelming the tranquilizer market, Sternbach began changing the Dr. Leo Slernbach holds a model of the molecule of Valium, the tranquilizer that has become the world's most widely prescribed drug (he also invented Librium). A refugee from Hitler's war, he has led a happy life in the U.S., says,-"I never made money my major objective; it has always been chemistry." molecular structure of Librium, degrading it, making various transformations, and finally coming up with diarepam, trade-named Valium, a compound five to 10 times as potent as Librium. "I sat down with Dr. Randall," Sternbach narrates, "and after much testing and investigation, we both came to the conclusion that there was nothing which spoke ngainst this compound. "It was very potent but it did not show any toxicity. It did not show any unpleasant side effects. Its synthesis did not present any difficulties. So we proposed the compound for clinical testing at a meeting of the research steering committee. The right dosage' "They started testing it on humans, and it turned out that we didn't have the difficulties with the dosage thai we had previously encountered with Lib- rium. With Valium we hit the right dosage at once. "It took us four years to introduce Vnlium, and in 1963 it took off very nicely. Soon it was found that in addition to sedative and Iranquilizing properties, Valium was a muscle relaxant. According to Sternbach, no one knows exactly how Valium works except that it depresses a part of the central nervous system, reducing the anxiety quotient of its users. "We suspect," says Sternbnch, "thnl it works through the limbic system of the brain. But we do not know for sure." What Sternbnch likes about his mood-altering drug is that it does more good and less harm than any other similar drug in the modern pharma- copia. It is fairly non-nddictive. Unlike the barbiturates, it is no instrument for suicide, since an overdose of Valium will not stop the respiratory center from functioning. Wide range of uses Not only do a great number of family physicians prescribe Valium, but so do psychiatrists, neurologists, orthopedists and internists. Anesthesiologists use it, as do pediatricians .ind cardiologists. It is administered to pregnant women in the early stages of labor but never before that. It is prescribed for athletes with strained muscles, for patients who arc about to undergo surgery. It has a calming effect on hypertensives. Physicians swear by it for patients who complain of anxiety. And who in this day and age does not? Most physicians who prescribe Valium believe it to be effective. To date the female users of Valium outnumber the males by 2.5 lo 1. Like all drugs, Valium is capable of being misused, especially in some nursing homes where it has been used to put old people to bed and keep them there. continued

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