| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 141 | Steroid enamines | US80543659 | 1959-04-10 | US3192201A | 1965-06-29 | PIETER WESTERHOF |
| 142 | SIALYLTRANSFERASE INHIBITORS AND USES THEREOF | PCT/US2016/049084 | 2016-08-26 | WO2017035501A1 | 2017-03-02 | LI, Wen-Shan; HUNG, Wen-Chun; SHEN, Chia-Ning |
Disclosed herein are novel sialyltransferase inhibitors, and compositions and methods for treating diseases and/or conditions associated with the activation of sialyltransferase, such as a cancer, an immune disease or an inflammatory disease. |
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| 143 | SYNTHESIS OF ENT-PROGESTERONE AND INTERMEDIATES THEREOF | PCT/US2015/050631 | 2015-09-17 | WO2016044558A1 | 2016-03-24 | LEVY, Daniel, E.; CRAN, John, W. |
The present invention relates to the synthesis of ent-progesterone and intermediates thereof. |
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| 144 | 19-NOR C3,3-DISUBSTITUTED C21-N-PYRAZOLYL STEROIDS AND METHODS OF USE THEREOF | PCT/CN2014/075594 | 2014-04-17 | WO2014169833A9 | 2014-10-23 | BOTELLA, Gabriel Martinez; HARRISON, Boyd L.; ROBICHAUD, Albert Jean; SALITURO, Francesco G.; BERESIS, Richard Thomas |
Provided herein are 19-nor C3,3-disubstituted C21-pyrazolyl steroids of Formula (I), and pharmaceutically acceptable salts thereof; wherein-, R1, R2, R3a, R3b, R4a, R4b, R5, R6, and R7are as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, and tinnitus. |
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| 145 | POWER ASSISTED BOW | PCT/US2014029558 | 2014-03-14 | WO2014144945A2 | 2014-09-18 | PEACEMAKER SAMUEL R; PEACEMAKER BENJAMIN; PEACEMAKER ZACHARY |
| A compound bow may feature the ability to pre-store energy before the drawing back of the draw string. Various embodiments contemplate that this may allow an archer to draw back the draw string or cable, and upon reaching the let off region of the compound bow's draw profile, cause the pre-stored energy to be transferred to the energy being stored by the bow. Various embodiments contemplate that this addition of pre-stored energy may give the archer more energy, held in the draw string or cable, to transfer to an arrow upon release, propelling it at greater speeds than would have been achieved with a compound bow of equal draw weight that does not feature an energy storage mechanism. Various embodiments contemplate that a system may provide for a return position of the draw. For example, this may remove the pre-stored energy from the draw string or cable as the draw string or cable is returned to an undrawn position. | ||||||
| 146 | NOVEL C18 MODIFIED RETROSTEROIDS AS PROGESTERONE RECEPTOR MODULATOR COMPOUNDS | PCT/EP2006/066842 | 2006-09-28 | WO2007039544A1 | 2007-04-12 | MESSINGER, Josef; THOLE, Heinrich-Hubert; HUSEN, Bettina; BOECKER, Christiane; HINAJE, Maria; BUCHHOLZ, Monika; MARK, Christoph; KLINGER-DABRAL, Vibhuti |
Described herein are new retrosteroidal compounds of general formula (I), representing progesterone receptor modulators, and their production, and pharmaceutical preparations containing these compounds. Said compounds are preferably used for the treatment of benign gynecological disorders such as endometriosis and uterine fibroids, as well as for female birth control and for HRT. |
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| 147 | CYTOPROTECTIVE POLYCYCLIC COMPOUNDS | PCT/US0147262 | 2001-11-05 | WO0240032A2 | 2002-05-23 | COVEY DOUGLAS F |
| The present invention is generally directed to novel enantiomeric estrogen derivatives, some of which may have one or more unsaturated bonds in conjugation with the terminal or A-ring of the structure, which have cytoprotective activity. The present invention is further directed to a process for conferring cytoprotection to a population of cells, of a subject in need thereof, involving the administration of an effective dose of the compound. | ||||||
| 148 | 14 beta -H-STEROLS, PHARMACEUTICAL COMPOSITIONS COMPRISING THEM AND USE OF THESE DERIVATIVES FOR THE PREPARATION OF MEIOSIS REGULATING MEDICAMENTS | PCT/EP2000/004092 | 2000-05-05 | WO00068245A1 | 2000-11-16 | |
| The present invention relates to pharmaceutically active 14 beta -H-sterols, to pharmaceutical compositions comprising them and to the use of these novel compounds for the preparation of medicaments. More particularly it has been found that the 14 beta -H-sterols of the invention can be used for regulating meiosis. | ||||||
| 149 | 16-HYDROXYESTRATRIENES AS SELECTIVE ESTROGENS | PCT/EP0001073 | 2000-02-09 | WO0047603A2 | 2000-08-17 | KUENZER HERMANN; KNAUTHE RUDOLF; LESSL MONIKA; FRITZEMEIER KARL-HEINRICH; HEGELE-HARTUNG CHRISTA; BOEMER ULF; MUELLER GERD; KOSEMUND DIRK |
| The invention relates to novel compounds as pharmaceutical agents which have in vitro a higher affinity to estrogen receptor preparations of the rat prostate than to estrogen receptor preparations of the rat uterus and which preferably have in vivo a preferential effect on bones as compared to the uterus and/or a marked effect with regard to the stimulation of the expression of the 5HT2a receptor and transporter. The invention also relates to the production and to the use in therapy of these compounds and to pharmaceutical administration forms containing said novel compounds. The novel compounds are 16 alpha and 16 beta hydroxy-estra,1,3,5(10)-estratriene which carry additional substituents at the steroid backbone and one or more additional double bonds on the B, C and/or D rings. | ||||||
| 150 | PHARMACEUTICAL COMPOSITIONS HAVING APPETITE SUPPRESSANT ACTIVITY | PCT/GB1998/001100 | 1998-04-15 | WO98046243A2 | 1998-10-22 | |
| A pharmaceutical composition contains an extract obtainable from a plant of the genus Trichocaulon or Hoodia containing an appetite suppressant agent having the formula (1). A process for obtaining the extract and a process for synthesizing compound (1) and its analogues and derivatives is also provided. The invention also extends to the use of such extracts and compound (1) and its analogues for the manufacture of medicaments having appetite suppressant activity. The invention further provides novel intermediates for the synthesis of compound (1). | ||||||
| 151 | 19-nor C3, 3-disubstituted C21-C-bound heteroaryl steroids and methods of use thereof | US16507214 | 2019-07-10 | US11344563B2 | 2022-05-31 | Gabriel Martinez Botella; Boyd L. Harrison; Albert Jean Robichaud; Francesco G. Salituro; Richard Thomas Beresis |
| Provided herein are 19-nor C3,3-disubstituted steroids of Formula (I): and pharmaceutically acceptable salts thereof; wherein , R1, R2, R3a, R3b, R4a, and R4b are as defined herein, and A is a carbon bound substituted or unsubstituted 5- to 6-membered heteroaryl ring as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, and tinnitus. | ||||||
| 152 | 19-NOR C3, 3-DISUBSTITUTED C21-N-PYRAZOLYL STEROIDS AND METHODS OF USE THEREOF | US16428386 | 2019-05-31 | US20200155576A1 | 2020-05-21 | Gabriel Martinez Botella; Boyd L. Harrison; Albert Jean Robichaud; Francesco G. Salituro; Richard Thomas Beresis |
| Provided herein are 19-nor C3,3-disubstituted C21-pyrazolyl steroids of Formula (I): and pharmaceutically acceptable salts thereof; wherein , R1, R2, R3a, R3b, R4a, R4b, R5, R6, and R7 are as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, and tinnitus. | ||||||
| 153 | Process for the preparation of 9 beta,10 alpha-progesterone (retroprogesterone) | US16479160 | 2018-01-18 | US10654885B2 | 2020-05-19 | Roberto Lenna; Claudio Delfrate; Davide Rigamonti |
| The present invention refers to a new process for the synthesis of (9β,10α)-pregn-4-ene-3,20-dione, commonly known as retroprogesterone, having the formula (1) shown below. | ||||||
| 154 | 19-nor C3, 3-disubstituted C21-N-pyrazolyl steroids and methods of use thereof | US16020641 | 2018-06-27 | US10342810B2 | 2019-07-09 | Gabriel Martinez Botella; Boyd L. Harrison; Albert Jean Robichaud; Francesco G. Salituro; Richard Thomas Beresis |
| Provided herein are 19-nor C3,3-disubstituted C21-pyrazolyl steroids of Formula (I): and pharmaceutically acceptable salts thereof; wherein , R1, R2, R3a, R3b, R4a, R4b, R5, R6, and R7 are as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, and tinnitus. | ||||||
| 155 | SYNTHESIS OF ENT-PROGESTERONE AND INTERMEDIATES THEREOF | US14214864 | 2014-03-15 | US20140275572A1 | 2014-09-18 | John W. Cran; Yinglin Han; Faliang Zhang |
| The present invention relates to the synthesis of ent-progesterone and intermediates thereof. | ||||||
| 156 | Method of controlling fertility in males with 20-substitute of steroids | US691667 | 1996-08-02 | US5679668A | 1997-10-21 | Armelle Bonfils; Daniel Philibert |
| The invention is a method of controlling fertility in male warm-blooded animals by administering a compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from the group consisting of alkyl of 1 to 12 carbon atoms and aralkyl of 7 to 15 carbon atoms or taken together form a saturated heterocycle of 5 to 6 ring members optionally having a second ring heteroatom selected from the group consisting of sulfur, oxygen and nitrogen, R.sub.3 is an .alpha.-alkyl of 1 to 8 carbon atoms, n is an integer from 2 to 15, R.sub.4 is alkyl of 1 to 12 carbon atoms, R.sub.5 is selected from the group consisting of hydrogen, alkyl of 1 to 12 carbon atoms and acyl of an organic carboxylic acid of up to 12 carbon atoms and the wavy lines indicate that the 17- and 20- asymmetrical centers are independent of the absolute R and S configurations and their non-toxic, pharmaceutically acceptable acid addition salts. | ||||||
| 157 | Contignasterol, and related 3-alpha hydroxy-6-alpha hydroxy-7-beta hydroxy-15-keto-14-beta steroids useful as anti-inflammatory and anti-thrombosis agents | US226179 | 1994-04-12 | US5506221A | 1996-04-09 | Raymond J. Andersen; Theresa M. Allen; David L. Burgoyne |
| The invention presents compounds useful for the prevention of inflammatory or allergic reaction or the treatment of cardiovascular or haemodynamic disorders having the formula: ##STR1## where R= ##STR2## where R= ##STR3## or pharmaceutically acceptable acids or salts thereof. | ||||||
| 158 | 11 .beta.-phenyl-gonanes, their manufacture and pharmaceutical preparations containing them | US827050 | 1986-02-07 | US5089635A | 1992-02-18 | Gunter Neef; Sybille Beier; Walter Elger; David Henderson; Eckard Otto; Ralph Rohde |
| 13-alkyl-11.beta.-phenyl-gonanes of general formula I ##STR1## wherein A and B together stand for an oxygen atom, a CH.sub.2 group or a second bond between carbon atoms 9 and 10,X is an oxygen atom or the hydroxyimino grouping N.about.OH,R.sub.1 is a straight-chained or branched, saturated or unsaturated alkyl radical with up to 8 carbon atoms, which contains the grouping ##STR2## with X as described above, R.sub.2 is a methyl or ethyl radical in the .alpha. or .beta. position,R.sub.9, R.sub.10, R.sub.11 and R.sub.12 each stand for a hydrogen atom, a hydroxy, alkyl, alkoxy or acyloxy group with 1 to 4 carbon atoms respectively or a halogen atom and R.sub.3 and R.sub.4 have a variety of meanings, have antigestagenic and antiglucocorticoid effects. | ||||||
| 159 | Asymmetric synthesis of organic compounds | US723127 | 1976-09-14 | US4108898A | 1978-08-22 | Zoltan George Hajos; David Richard Parrish |
| Optically active organic compounds are prepared starting from optically inactive reactants by means of an optically active agent which influences the course of the reaction. In particular optically active compounds having a "meso" type carbon atom undergo an intramolecular ring closure in the presence of an optically active agent to yield an optically active product having one additional ring. The present process is particularly useful in the preparation of optically active bicyclic diketones which are important intermediates in the total synthesis of steroids. | ||||||
| 160 | Asymmetric synthesis of organic compounds | US720717 | 1976-09-07 | US4105696A | 1978-08-08 | Zoltan G. Hajos; David R. Parrish |
| Optically active organic compounds are prepared starting from optically inactive reactants by means of an optically active agent which influences the course of the reaction. In particular optically active compounds having a "meso" type carbon atom undergo an intramolecular ring closure in the presence of an optically active agent to yield an optically active product having one additional ring. The present process is particularly useful in the preparation of optically active bicyclic diketones which are important intermediates in the total synthesis of steroids. | ||||||
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