Carbon Bonded Directly At The 16-position Patents (Class 552/596)
  • Patent number: 6915962
    Abstract: Embodiments of the present invention include apparatus and methods for aerosolizing liquid. One embodiment of the invention provides an apparatus for generating an aerosol. The apparatus includes an actuator having a first face and a second face and defining an opening therethrough, as well as a vibratory element in mechanical communication with the actuator, and a sealing member configured to isolate the vibratory element from a surrounding environment. In accordance with certain embodiments, the apparatus further comprises an aerosolization element mounted on the actuator and disposed substantially over the opening, wherein the aerosolization element defines at least one aperture therethrough. Hence, the vibratory element may be operated to vibrate to cause movement of the aerosolization element in such a manner that a liquid at the first face of the aerosolization element can be dispensed as an aerosol through the at least one aperture.
    Type: Grant
    Filed: May 20, 2003
    Date of Patent: July 12, 2005
    Assignee: Aerogen, Inc.
    Inventors: John Power, Des Regan, Niall Smith
  • Patent number: 5723455
    Abstract: Novel antiandrogenic agents are provided. An exemplary group of compounds has the structural formula (I) ##STR1## wherein R.sup.1 through R.sup.10, a and b are as defined herein. Pharmaceutical compositions and methods for using the compounds of formula (I) to treat androgen-related clinical conditions are provided, as are methods and compositions for using the compounds as contraceptive agents.
    Type: Grant
    Filed: March 11, 1997
    Date of Patent: March 3, 1998
    Assignee: SRI International
    Inventors: Masato Tanabe, Wan-Ru Chao, Wesley K. M. Chong, David F. Crowe
  • Patent number: 5616742
    Abstract: Described is a process for the regioselective dehydration of 11-hydroxy steroids using PCl.sub.5, PCl.sub.3, POCl.sub.3 or either SO.sub.2 Cl.sub.2 and imidazole, or PPh.sub.3 and CCl.sub.4. The disclosed process selectively forms .DELTA..sup.9,11 steroids from either 11-.alpha.- or 11-.beta.-hydroxy steroids, and can also be used for the one-step conversion of 11,21-dihydroxy steroids to 21-chloro-.DELTA..sup.9,11 steroids.Also disclosed are processes for the regioselective conversion of 11-.beta.-chloro steroids to .DELTA..sup.9,11 steroids, and for regioselectively converting an 11,17,21-trihydroxy streoid to a 21-chloro-11,17-dihydroxy steroid.
    Type: Grant
    Filed: May 22, 1995
    Date of Patent: April 1, 1997
    Assignee: Schering Corporation
    Inventors: Xiaoyong Fu, Tiruvettipuram K. Thiruvengadam, Chou-Hong Tann, Cesar Colon
  • Patent number: 5596108
    Abstract: A new process for the preparation of 16.beta.-methyl-steroids of the formula ##STR1## and novel intermediates therefor which compounds are intermediates for betamethasone.
    Type: Grant
    Filed: May 18, 1995
    Date of Patent: January 21, 1997
    Assignee: Roussel Uclaf
    Inventors: Catherine Geurts, Michel Vivat
  • Patent number: 5502222
    Abstract: Described is a process for the regioselective dehydration of 11-hydroxy steroids using PCl.sub.5, PCl.sub.3, POCl.sub.3 or either SO.sub. Cl.sub.2 and imidazole, or PPh.sub.3 and CCl.sub.4. The disclosed process selectively forms .increment..sup.9,11 steroids from either 11-.alpha.- or 11-.beta.-hydroxy steroids, and can also be used for the one-step conversion of 11,21-dihydroxy steroids to 21-chloro-.increment..sup.9,11 steroids.
    Type: Grant
    Filed: June 1, 1994
    Date of Patent: March 26, 1996
    Assignee: Schering Corporation
    Inventors: Xiaoyong Fu, Tiruvettipuram K. Thiruvengadam, Chou-Hong Tann, Junning Lee, Cesar Colon
  • Patent number: 5352808
    Abstract: A process for the preparation of a compound of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms optionally substituted by halogen or a nitrogen or oxygen function and alkenyl and alkynyl of 2 to 4 carbon atoms, R.sub.2 is alkyl of 1 to 4 carbon atoms and the A, B, C and D rings are optionally substituted by at least one member of the group consisting of optionally protected --OH or .dbd.0, halogen, alkyl and alkoxy of 1 to 4 carbon atoms and alkenyl and alkynyl of 2 to 4 carbon atoms comprising reacting a compound of the formula ##STR2## wherein R.sub.1 and R.sub.2 and the A, B, C and D rings are defined as above with an oxidizing agent in the presence of water and an at least partially water-miscible solvent to obtain a compound of the formula ##STR3## wherein R.sub.1 and R.sub.
    Type: Grant
    Filed: November 5, 1992
    Date of Patent: October 4, 1994
    Assignee: Roussel Uclaf
    Inventors: Jean Buendia, Michel Vivat
  • Patent number: 5273971
    Abstract: There are provided 13-alkyl-11beta-phenyl-gonanes of formula I ##STR1## wherein Z is an oxygen atom or N--OH;R.sup.2 is alpha- or beta-position methyl or ethyl;R.sup.1 is selected from heteroaryl radicals, cycloalkyl radicals, cycloalkenyl radicals, aryl radicals, alkenyl radicals, and alkyl radicals where R.sup.2 is in the alpha-position and an ethyl radical where R.sup.2 is in the beta-position; andR.sup.3 and R.sup.4 are selected from one of two different groups of substituent pairs, the group from which the selection is made being determined by the position of R.sup.2.
    Type: Grant
    Filed: July 3, 1989
    Date of Patent: December 28, 1993
    Assignee: Schering Aktiengesellschaft
    Inventors: Stefan Scholz, Eckhard Ottow, Guenter Neef, Walter Elger, Sybille Beier, Krzysztof Chwalisz
  • Patent number: 5132440
    Abstract: A process for the production of progresterone derivatives of general formula I ##STR1## in which symbolizes a single bond or a double bond,X represents a hydrogen atom, a fluorine atom or a methyl group andV means a methylene group, an ethylene group, an ethylidene group or a vinylidene group, is described.
    Type: Grant
    Filed: July 15, 1991
    Date of Patent: July 21, 1992
    Assignee: Schering Aktiengesellschaft
    Inventors: Helmut Hauser, Hans D. Berndt
  • Patent number: 5068368
    Abstract: A process for the preparation of ethynyl carbinols of the formula: ##STR1## wherein R" is hydrogen, a substituted or unsubstituted aliphatic or aromatic hydrocarbon, R'" is a substituted or unsubstituted aliphatic or aromatic hydrocarbon or R" and R'" together to the carbon atom to which they are joined represent a steroid, which comprises the steps ofA. reacting in a solvent system comprising an aromatic hydrocarbon, at least one lithium alkylamide selected from the group consisting of: ##STR2## wherein R is a hydrogen or lower alkyl, R' is hydrogen, lower alkyl, a substituted or unsubstituted aliphatic, alicyclic or aromatic hydrocarbon, x is an integer of 2 to 8, y and z are each 0 to 1, with acetylene to form a monolithium acetylideB. reacting in a solvent system comprising an aromatic hydrocarbon, the monolithium acetylene from Part A with a ketone of the formula R"R'"C.dbd.O, wherein R" and R'" are as hereinbefore defined, and thenC.
    Type: Grant
    Filed: May 10, 1990
    Date of Patent: November 26, 1991
    Assignee: Cyprus Foote Mineral Company
    Inventors: W. Novis Smith, Christopher Louer
  • Patent number: 5026693
    Abstract: Novel esters of 9.alpha.-fluoro- and chloro-corticosteroids of the formula ##STR1## wherein Y is chlorine or OR.sub.1, R.sub.1 and R.sub.2 represent an acyl group of 2-6 carbon atoms or a benzoyl group and where R.sub.1 and R.sub.2 can be the same or different in the same molecule, R.sub.3 is methyl or fluorine in either the .alpha.- or .beta.- orientation, X is chlorine or fluorine, and the C.sub.1 C.sub.2 bond can be saturated or not, especially those compounds of the formula ##STR2## wherein Y and R.sub.2 have the significance given above, are prepared by reacting the respective 9.beta.,11.beta.-epoxy compounds with hydrogen fluoride or chloride.
    Type: Grant
    Filed: May 21, 1990
    Date of Patent: June 25, 1991
    Assignee: Hovione Inter Ltd.
    Inventors: Ivan Villax, William Heggie, Philip R. Page
  • Patent number: 5003063
    Abstract: The invention involves a two step chemical transformation of a steroidal 17-cyanohydrin (II) ##STR1## to a 17.alpha.-hydroxy-21-halo-20-keto steroid (IV) ##STR2## intermediate which can readily be converted to pharmaceutically useful corticoids.
    Type: Grant
    Filed: January 30, 1990
    Date of Patent: March 26, 1991
    Assignee: The Upjohn Company
    Inventor: John G. Reid
  • Patent number: 4954490
    Abstract: A 11.beta.-aryl-19-norprogesterone steroid of the formula: ##STR1## wherein (i) R.sup.1 is H, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl, OH, OC(O)CH.sub.3, or OC(O)R.sup.5, wherein R.sup.5 is C.sub.2-8 alkyl, C.sub.2-8 alkenyl, C.sub.2-8 alkynyl or aryl, R.sub.2 is H, R.sup.3 is H, C.sub.1-4 alkyl, C.sub.2-4 alkenyl or C.sub.2-4 alkynyl, R.sup.4 is H, CH.sub.3, F or Cl, R.sup.6 is H, (CH.sub.3).sub.2 N, CH.sub.3 O, CH.sub.3 CO, CH.sub.3 S, CH.sub.3 SO, CH.sub.3 SO.sub.2, and X is O or NOCH.sub.3 ; or(ii) R.sup.1 and R.sup.2 taken together are a carbon-carbon bond and R.sup.3, R.sup.4, R.sup.6 and X are as defined above; or(iii) R.sup.1 and R.sup.3 taken together are --CH.sub.2 -- or --N.dbd.N--CH.sub.2 --, R.sup.2 is H and R.sup.4, R.sup.6 and X are as defined above; or(iv) R.sup.2 and R.sup.3 taken together are .dbd.CH.sub.2 and R.sup.1, R.sup.4, R.sup.6 and X are as defined above.
    Type: Grant
    Filed: June 23, 1988
    Date of Patent: September 4, 1990
    Assignee: Research Triangle Institute
    Inventors: C. Edgar Cook, Mansukh C. Wani, Y.-W Lee, Jerry R. Reel, Douglas Rector
  • Patent number: 4921638
    Abstract: The invention is the compound 17.beta.-cyano-9.alpha., 17.alpha.-dihydroxyandrost-4-en-3-one (I) which is particularly useful as an intermediate in the production of the 17.alpha.-halo silyl ethers (II).
    Type: Grant
    Filed: October 3, 1988
    Date of Patent: May 1, 1990
    Assignee: The Upjohn Company
    Inventors: Douglas A. Livingston, Bruce A. Pearlman, Scott Denmark, Joel E. Huber
  • Patent number: 4913852
    Abstract: Compounds obtained from the associative synthesis of sulfur-containing or sulfur-free amino acids with derivatives of .DELTA.-4-pregnene-3,20-dione or with derivatives of .DELTA.-1,4-pregnadiene-3,20-dione of the general formulas (I), (II) and (III), having glucocorticoidal and anti-inflammatory properties have been prepared and tested. Pharmaceutical compositions, medicaments containing them as well as their applications are claimed, particularly in the cutaneous and ophthalmic fields.
    Type: Grant
    Filed: February 24, 1988
    Date of Patent: April 3, 1990
    Inventors: Catherine Milioni, Constantin Efthyimiopoulos, Bernard Koch, Louis Jung, Jean Jung