CYP11B, CYP17, AND/OR CYP21 INHIBITORS

Provided herein are inhibitors of CYP11B, CYP17, and/or CYP21 enzymes of Formula (Z), (IX), (X), (XI), (XII), (XIII), (XIV), (XV), (XVI), or (XVII). Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat androgen-dependent diseases, disorders and conditions. Formula (Z) 12.-. (canceled)45.-. (canceled)79.-. (canceled)1121.-. (canceled)22. A pharmaceutical composition comprising a compound of any of , and and a pharmaceutically acceptable carrier , excipient or binder.2310. A method for treating cancer in a subject comprising administering to a subject in need thereof 1) a therapeutically effective amount of a compound of any of , and or a pharmaceutically acceptable salt or solvate thereof or 2) a pharmaceutical composition comprising a therapeutically effective amount of a compound of any of , , and or a pharmaceutically acceptable salt or solvate thereof and a pharmaceutically acceptable carrier , excipient or binder.2435.-. (canceled)36. A method of treating a disease associated with hypercortisolism comprising administering to a subject in need thereof a therapeutically effective amount of a compound of , or , or a pharmaceutically acceptable salt or solvate thereof.3740.-. (canceled) Described herein are compounds, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat androgen-dependent diseases or conditions.The 17α-hydroxylase/Clyase enzyme complex is essential for the biosynthesis of androgens. CYP17 is a bifunctional enzyme which possess both a C-lyase activity and a C17-hydroxylase activity. These two alternative enzymatic activities of CYP17 result in the formation of critically different intermediates in steroid biosynthesis and each activity appear to be differentially and developmentally regulated.In the testes and adrenal ...

Synthesis of a substituted indene derivative

This invention is directed to methods of preparing AQX-1125 having the formula: This invention is also directed to intermediates utilized in the methods of preparing AQX-1125.

ANTIOXIDANT, ANTI-INFLAMMATORY AND ANTICANCER DERIVATIVES OF TRIPTOLIDE AND NANOSPHERES THEREOF

This invention relates to uses of conjugates of triptolide nanoprodrugs in cancer immunotherapy, specifically compound such as D-I or D-II wherein Xis a antioxidant, an anti-inflammatory or an anti-cancer agent and nanospheres thereof, and A is be selected from the group consisting of branched and unbranched alkyl, branched and unbranched alkenyl, branched and unbranched alkynyl, heteroatom-containing branched and unbranched alkyl, heteroatom-containing branched and unbranched alkenyl, heteroatom-containing branched and unbranched alkynyl, aryl, cyclic aliphatic, cyclic aromatic, heterocyclic, and aromatic heterocyclic groups. 2. The compound of claim 1 , wherein X1 is selected from the group consisting of camptothecin claim 1 , camptothecin analogs claim 1 , temozolomide claim 1 , temozolomide analogs claim 1 , nonsteroidal anti-inflammatory drug (NSAID) claim 1 , statin claim 1 , alpha-lipoic acid and chemotherapeutic agents.3. The compound of claim 1 , wherein the compound is of formula D-I.5. The compound of claim 1 , wherein the compound is of formula D-II.11. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier or excipient.12. A nanosphere comprising a compound of .13. The nanosphere of claim 12 , wherein the nanosphere further comprises an antioxidant.14. The nanosphere of claim 13 , wherein the antioxidant is tocopherol or a derivative thereof.15. The nanosphere of claim 12 , wherein the nanosphere further comprises a c compound of formula A-IV or A-V.16. The nanosphere of claim 12 , wherein the nanosphere further comprises an amphiphilic spacer.17. The nanosphere of claim 16 , wherein the amphiphilic spacer comprises a chemically active group selected from the group consisting of thiol claim 16 , amine claim 16 , carboxylic acid claim 16 , carboxylic acid NHS ester claim 16 , maleimide claim 16 , hydrazine claim 16 , ketone claim 16 , aledehyde claim 16 , and combinations thereof18. The nanosphere of claim 16 , ...

STEROL DERIVATIVE

The present invention provides a sterol derivative or a pharmaceutically acceptable salt thereof having an activity to promote proliferation of neural stem cells. Namely, the present invention provides a sterol derivative represented by the general formula (I) (wherein Y represents optionally substituted lower alkyl or the like; Xand Xare the same or different, and represent a bond or the like; R, R, R, R, Rand Rare the same or different, and represent a hydrogen atom or the like; Rand Rare the same or different, and represent a hydrogen atom or the like; Rrepresents a hydrogen atom or the like; Rand Rtogether represent a bond or the like; and Rrepresents a hydrogen atom or the like) or a pharmaceutically acceptable salt thereof. 116-. (canceled)19. The method according to claim 17 , wherein the protective group for a hydroxy group is trimethyl silyl claim 17 , tetrahydropyranyl or benzoyl.20. The method according to claim 18 , wherein the protective group for a hydroxy group is trimethyl silyl claim 18 , tetrahydropyranyl or benzoyl. The present invention relates to a sterol derivative having an activity to promote proliferation of neural stem cells.Neurodegenerative diseases are diseases in which cerebral and peripheral nerve cells are damaged by a hereditary factor, an environmental factor, an aging factor and the like. Specifically, they include Parkinson's disease, Alzheimer's disease, triplet repeat disease, amyotrophic lateral sclerosis, polyneuropathy, spinal cord injury, cerebrovascular disorders and the like.Although a general therapeutic method for these neurodegenerative diseases is a method in which neurotransmitters lost by the injury of nerve cells are supplemented, the diseases for which the therapeutic method is effective are limited to Parkinson's disease, Alzheimer's disease and the like at present. Additionally, the progress of nerve cell death cannot be stopped by the neurotransmitter supplementation method.Regenerative medicine which ...

HYDROXYSTEROID COMPOUNDS, THEIR INTERMEDIATES, PROCESS OF PREPARATION, COMPOSITION AND USES THEREOF

The present invention relates to novel steroidal compounds of formula (I), process for preparation of the same and composition comprising these compounds. 5. The compounds as claimed in 1 , selected from the group comprising:i. (10R,11S,13S,17S)-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-11-hydroxy-10,13-dimethyl-3-oxo-1H-cyclopenta[a]phenanthrene-17-carboxylic acid;ii. (3S,8S,9S,10S,11S,13S,14S,17S)-hexadecahydro-3,11-dihydroxy-N,10,13-trimethyl-1H-cyclopenta[a]phenanthrene-17-carboxamide;iii. (3S,8S,9S,10S,11S,13S,14S,17S)—N-(2-aminoethyl)-hexadecahydro-3,11-dihydroxy-10,13-dimethyl-1H-cyclopenta[a]phenanthrene-17-carboxamide;iv. (3S,5R,6R,10R,11S,13S,17S)-hexadecahydro-6-methoxy-10,13-dimethyl-17-(2-methyl-1,3-dioxolan-2-yl)-1H-cyclopenta[a]phenanthrene-3,5,11-triol;v. (4aR,5S,6aS)-5-hydroxy-4a,6a-dimethyl-4,4a,4b,5,6,6a,9,9a,9b,10-decahydro-1H-indeno[5,4-f]quinoline-2,7βH,8H)-dione;vi. (4a′R,5′S,6a'S)-5′-hydroxy-4a′,5′,6a′-trimethyl-3′,4′,4a′,4b′,5′,6′,6a′,8′,9′,9a′,9b′,10′-dodecahydrospiro[[1,3]dioxolane-2,7′-indeno[5,4-f]quinolin]-2′(1′H)-one;vii. (4aR,5S,6aS)-4,4a,4b,5,6,6a,9,9a,9b,10-decahydro-5-hydroxy-4a,6a-dimethyl-1H-indeno[5,4-f]quinoline-2,7βH,8H)-dione;viii. (4aR,5S,6aS)-7-acetyl-4,4a,4b,5,6,6a,7,8,9,9a,9b,10-dodecahydro-5-hydroxy-4a,5,6a-trimethyl-1H-indeno[5,4-f]quinolin-2(3H)-one;ix. (11S)-7,8,9,11,12,13,14,15,16,17-decahydro-3,11-dihydroxy-6H-cyclopenta[a]phenanthrene-17-carboxylic acid;x. (4aR,6aS)-2,3,4,4a,4b,5,6,6a,7,8,9,9a,9b,10-tetradecahydro-4a,6a-dimethyl-2,5-dioxo-1H-indeno[5,4-f]quinoline-7-carboxylic acid;xi. (17S)-17-acetyl-7,8,13,15,16,17-hexahydro-3-hydroxy-1-methyl-6H-cyclopenta [a]phenanthren-11(9H,12H,14H)-one;xii. (13S,17S)-17-acetyl-7,8,13,15,16,17-hexahydro-3-hydroxy-13-methyl-6H-cyclopenta[a]phenanthren-11(9H,12H,14H)-one;xiii. (10R,11S,13S,17S)-11-hydroxy-10,13-dimethyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthrene-17-carboxylic acid;xiv. (10R,11S,13S,17S)-11-hydroxy-N,N,10,13- ...

ENZYME COMPOSITIONS, STEROID DERIVATIVES, ENZYME INHIBITORS, AND METHODS OF MAKING SAME FOR PHARMACEUTICAL APPLICATIONS

The present disclosure provides for a synthetic strategy to incorporate a C12α-hydroxy group from the methylene (—CH2-) in a steroid backbone, combining synthetic chemistry and enzymology techniques to develop a selective inhibitor for cytochrome P450 8B1, and developing a selective P450 8B1 inhibitor, which can be used as a tool to study P450 8B1 and treat health issues. 2. The compound of or pharmaceutically acceptable salt thereof claim 1 , wherein the compound is an inhibitor of P450 8B1.4. The compound of claim 3 , wherein the compound is an inhibitor of P450 8B1.6. The general formula of claim 5 , wherein the general formula is reductively animated to produce at least one derivative.7. The at least one derivative of claim 6 , wherein the derivative is a 12-dimethylamino derivative.8. The at least one derivative of claim 6 , wherein the derivative is a substrate of P450 8B1.9. (canceled)10. (canceled)11. (canceled)12. (canceled)13. A pharmaceutical composition comprising the compound of .14. The pharmaceutical composition of claim 13 , wherein the composition is used to treat obesity.15. The pharmaceutical composition of claim 13 , wherein the composition is used to treat cardiovascular disease.16. (canceled) This application claims priority to U.S. Provisional Application No. 62/733,179 filed Sep. 19, 2018, which is hereby incorporated by reference in its entirety.Cytochromes P450 8B1 and 8A1, two enzymes, are not well understood by the industry. There is little information about P450 8B1 biochemistry available to date, and there is no known reported expression and purification of this enzyme.Cholic acid is a molecule that falls in the class of bile acids, which are an important class of compounds with various functions. Cholic acid has been shown to increase cholesterol absorption in humans through the formation of micelles. It has also been suggested from a mice feeding study that the bile acid composition of the micelles affect the micellar solubilization ...

Synthesis of a substituted indene derivative

This invention is directed to methods of preparing AQX-1125 having the formula: This invention is also directed to intermediates utilized in the methods of preparing AQX-1125.

N-SUBSTITUTED INDENOISOQUINOLINES AND SYNTHESES THEREOF

N-Substituted indenoisoquinoline compounds, and pharmaceutical formulations of N-substituted indenoisoquinoline compounds are described. Also described are processes for preparing N-substituted indenoisoquinoline compounds. Also described are methods for treating cancer in mammals using the described N-substituted indenoisoquinoline compounds or pharmaceutical formulations thereof. 2. The compound of claim 1 , wherein Ris selected from the group consisting of amino claim 1 , alkylamino claim 1 , dialkylamino claim 1 , trialkylammonium claim 1 , hydroxyalkylamino claim 1 , bis(hydroxyalkyl)amino claim 1 , and hydroxyalkylaminoalkylamino claim 1 ,3. The compound of claim 1 , wherein Ris dialkylamino or hydroxyalkylamino.4. The compound of claim 1 , wherein Ris amino.5. The compound of claim 1 , wherein Rincludes one or more alkoxy groups.6. The compound of claim 1 , wherein Rincludes two or three alkoxy groups.7. The compound of claim 1 , wherein Rincludes an alkylenedioxy group.8. The compound of claim 1 , wherein Rincludes a nitro group.9. The compound of claim 1 , wherein Rincludes a nitro group at position 3 of the compound.10. The compound of claim 1 , wherein Rincludes an alkylenedioxy group.11. The compound of claim 1 , wherein Rincludes one or more alkoxy groups.12. The compound of claim 1 , wherein Rincludes two or three alkoxy groups.13. The compound of claim 1 , wherein Rincludes two or three methoxy groups.14. The compound of claim 1 , wherein Rincludes one methoxy group.15. The compound of wherein m is 3.16. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt claim 1 , hydrate claim 1 , or solvate thereof claim 1 , and one or more pharmaceutically acceptable carriers claim 1 , diluents claim 1 , and excipients.17. A method for treating cancer claim 1 , the method comprising the step of administering a therapeutically effective amount of a compound of to a patient in need of relief from said cancer. This ...

N-SUBSTITUTED INDENOISOQUINOLINES AND SYNTHESES THEREOF

N-Substituted indenoisoquinoline compounds, and pharmaceutical formulations of N-substituted indenoisoquinoline compounds are described. Also described are processes for preparing N-substituted indenoisoquinoline compounds. Also described are methods for treating cancer in mammals using the described N-substituted indenoisoquinoline compounds or pharmaceutical formulations thereof. 2. The compound of claim 1 , wherein Ris selected from the group consisting of amino claim 1 , alkylamino claim 1 , dialkylamino claim 1 , trialkylammonium claim 1 , bis(hydroxyalkyl)amino claim 1 , and hydroxyalkylaminoalkylamino.3. The compound of claim 1 , wherein Ris heteroaryl or heterocyclyl claim 1 , wherein each heteroaryl and heterocyclyl is optionally substituted.4. The compound of wherein Rrepresents four substituents each independently selected from the group consisting of hydrogen claim 1 , alkyl claim 1 , halo claim 1 , nitro claim 1 , hydroxyl claim 1 , alkoxy claim 1 , and thio claim 1 , or Rrepresents at least two adjacent substituents that are taken together with the attached carbons to form an optionally substituted heterocycle.5. The compound of wherein Rrepresents four substituents each independently selected from the group consisting of hydrogen and halo.6. The compound of claim 1 , wherein Rincludes an alkylenedioxy group.7. The compound of wherein Rrepresents two adjacent substituents that are taken together with the attached carbons to form an optionally substituted heterocycle.8. The compound of claim 1 , wherein Rincludes an alkylenedioxy group or a methoxy group.9. The compound of claim 1 , wherein Rincludes a methylenedioxy group.10. The compound of wherein m is 3.13. The compound of claim 11 , wherein Ris hydrogen and Ris halo.14. The compound of claim 11 , wherein both Rand Rare halo.16. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and one or more pharmaceutically acceptable carriers ...

N-SUBSTITUTED INDENOISOQUINOLINES AND SYNTHESES THEREOF

N-Substituted indenoisoquinoline compounds, and pharmaceutical formulations of N-substituted indenoisoquinoline compounds are described. Also described are processes for preparing N-substituted indenoisoquinoline compounds. Also described are methods for treating cancer in mammals using the described N-substituted indenoisoquinoline compounds or pharmaceutical formulations thereof. 210-. (canceled)1231-. (canceled)3342-. (canceled)43. A method for treating cancer claim 11 , the method comprising the step of administering a therapeutically effective amount of a compound of to a patient in need of relief from said cancer.45. The process of wherein the cyclizing step includes one or more acids.46. The process of wherein the cyclizing step includes dicyclohexylcarbodiimide.4951-. (canceled)52. The process of wherein R═Rand R═R claim 48 , and said process is performed in one step. This application claims the benefit under 35 U.S.C. §119 (e) of U.S. Provisional Application Ser. No. 60/736,471, filed Nov. 14, 2005, and U.S. Provisional Application Ser. No. 60/808,699, filed May 26, 2006, the disclosures of which are hereby incorporated herein by reference.The invention described herein pertains to N-substituted indenoisoquinoline compounds. The invention described herein also pertains to methods for treating cancer in mammals using indenoisoquinoline compounds.The control and cure of cancer represents one of our most challenging health problems. The treatment of cancer can be approached by several modes of therapy including surgery, radiation, chemotherapy or a combination of any of these treatments. Chemotherapy continues to be an indispensable therapy for inoperable or metastatic forms of the disease. Thus, the discovery of compounds specifically targeting cancer cells, or the cellular mechanisms involved in the proliferation of cancer cells, can provide significant advancement in the eradication or control of cancer.The selection of compounds having effective anticancer ...

THERAPEUTIC COMPOUNDS AND METHODS

Regulator of G Protein Signaling (RGS) proteins modulate the complex signaling pathways elicited by G protein coupled receptor activation. Recent studies have implicated RGS proteins in the development and progression of multiple cancers. Provided herein are inhibitors of RGS17, compositions thereof and methods of treating diseases using the inhibitors. 2. The method of wherein the compound is the compound of formula I or a pharmaceutically acceptable salt thereof.3. The method of claim 1 , wherein Rand Rare each H.4. The method of claim 1 , wherein Ris —OH or —O(C-C)alkyl.5. (canceled)6. The method of claim 1 , wherein Ris —OH or —O(C-C)alkyl.7. (canceled)8. The method of claim 1 , wherein Ris —OH or —O(C-C)alkyl.9. (canceled)10. The method of claim 1 , wherein Ris phenyl substituted with one or more groups independently selected from halo claim 1 , (C-C)alkyl claim 1 , (C-C)haloalkyl claim 1 , —OH claim 1 , —O(C-C)alkyl or —O(C-C)haloalkyl.11. The method of claim 1 , wherein Ris phenyl substituted with one or more —OH.1213-. (canceled)15. The method of claim 1 , wherein the aberrant G protein signaling is caused by increased RGS activity.16. The method of claim 1 , wherein the aberrant G protein signaling is caused by overexpression of RGS proteins.17. The method of claim 1 , wherein the RGS protein is RGS17.18. A method of treating or preventing a disease or disorder mediated by overexpression of RGS17 comprising administering to a patient in need thereof and which patient overexpresses RGS17 a therapeutically effective amount of a compound of that inhibits the interaction of RGS17 and Gαo20. The method of claim 1 , wherein the disease or disorder is cancer or Parkinson's disease.21. (canceled)22. A pharmaceutical composition comprising a compound of formula I claim 1 , formula II claim 1 , formula III or formula IV or a pharmaceutically acceptable salt thereof claim 1 , as described in claim 1 , and a pharmaceutically acceptable carrier or excipient.23. The ...

N-SUBSTITUTED INDENOISOQUINOLINES AND SYNTHESES THEREOF

N-Substituted indenoisoquinoline compounds, and pharmaceutical formulations of N-substituted indenoisoquinoline compounds are described. Also described are processes for preparing N-substituted indenoisoquinoline compounds. Also described are methods for treating cancer in mammals using the described N-substituted indenoisoquinoline compounds or pharmaceutical formulations thereof. 2. The compound of claim 1 , wherein Ris selected from the group consisting of amino claim 1 , alkyl and dialkylamino claim 1 , trialkylammonium claim 1 , hydroxyalkylamino claim 1 , bis(hydroxyalkyl)amino claim 1 , hydroxyalkylaminoalkylamino claim 1 , and azido.3. The compound of claim 1 , wherein Ris selected from the group consisting of heteroaryl claim 1 , heteroaryloxy claim 1 , and heteroarylamino claim 1 , heteroarylalkylaminoalkylamino claim 1 , heterocyclyl claim 1 , heterocyclylamino claim 1 , each of which is optionally substituted.4. The compound of claim 1 , wherein Ris optionally substituted heterocyclyl or optionally substituted heterocyclylamino.5. The compound of claim 1 , wherein Ris morpholin-4-yl.6. The compound of claim 1 , wherein Ris optionally substituted heteroaryl or optionally substituted heteroarylamino.7. The compound of claim 1 , wherein Ris imidazole-1-yl.8. The compound of claim 1 , wherein Rincludes an alkylenedioxy group.9. The compound of claim 1 , wherein Rincludes one or more optionally substituted alkoxy.10. The compound of claim 1 , wherein Rincludes one or more alkoxy optionally substituted with alkenyl claim 1 , alkynyl claim 1 , halo claim 1 , nitro claim 1 , cyano claim 1 , azido claim 1 , amino claim 1 , alkylamino claim 1 , dialkylamino claim 1 , hydroxyalkylamino claim 1 , bis(hydroxyalkyl)amino claim 1 , cycloalkyl claim 1 , aryl claim 1 , hetereocyclyl claim 1 , heteroaryl claim 1 , alkylcarbonyl claim 1 , alkoxycarbonyl claim 1 , or hydrazinecarbonyl.11. The compound of claim 10 , wherein said alkoxy is optionally substituted with amino ...

COMPOSITIONS AND METHODS FOR TREATING CNS DISORDERS

Provided herein is a compound of Formula (I-I), or a pharmaceutically acceptable salt thereof, wherein the variables are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I-I), and methods of using the compounds, e.g. in the treatment of CNS-related disorders. 3. The compound of or , wherein Rand Ris each independently hydrogen , halogen , cyano , hydroxyl , substituted or unsubstituted alkyl , substituted or unsubstituted alkenyl , substituted or unsubstituted heterocyclyl , or substituted or unsubstituted alkynyl , —OR , —OC(═O)R , —NH , —N(R) , or —NRC(═O)R , wherein each instance of Ris independently hydrogen , substituted or unsubstituted alkyl , substituted or unsubstituted alkenyl , substituted or unsubstituted alkynyl , substituted or unsubstituted carbocyclyl , substituted or unsubstituted heterocyclyl , substituted or unsubstituted aryl , or substituted or unsubstituted heteroaryl.4. The compound of any one of - , wherein Rand Ris each independently hydrogen , halogen , cyano , hydroxyl , substituted or unsubstituted alkyl , substituted or unsubstituted alkenyl , —OR , —OC(═O)R , —NH , or —N(R) , wherein each instance of Ris independently hydrogen , substituted or unsubstituted alkyl , substituted or unsubstituted carbocyclyl , substituted or unsubstituted heterocyclyl , substituted or unsubstituted aryl , or substituted or unsubstituted heteroaryl.5. The compound of any one of - , wherein Rand Ris each independently hydrogen , substituted or unsubstituted alkyl , —OR , —OC(═O)R , —NH , —N(R) , or —NRC(═O)R , wherein each instance of Ris independently hydrogen , substituted or unsubstituted alkyl , substituted or unsubstituted carbocyclyl , substituted or unsubstituted heterocyclyl , substituted or unsubstituted aryl , or substituted or unsubstituted heteroaryl.6. The compound of any one of - , wherein Rand Rare both hydrogen.7. The compound of any one of - , wherein Rand Ris each independently hydrogen ...

15-OXOSTEROID COMPOUND AND PROCESS FOR PRODUCING THE SAME

Provided is a process for producing a compound, which has an oxo group specifically introduced on the 15-position of a steroid skeleton and which is useful as an intermediate, with a high yield without complicated steps. A compound represented by the formula (2) is allowed to react with an oxidant (e.g., a hypervalent iodine compound) and a co-oxidant (e.g., a peroxide) to produce a 15-oxosteroid compound represented by the formula (1), which is useful as an intermediate: 3. The 15-oxosteroid compound according to claim 1 , wherein Ris a halogen atom claim 1 , Rand Rare the same or different and are an alkyl group or a haloalkyl group claim 1 , Rand Rare the same or a different acyl group claim 1 , Ris a hydrogen atom claim 1 , an acyl group claim 1 , or a sulfonyl group claim 1 , and X is an oxygen atom.5. The process according to claim 4 , wherein a coexisting substance is added in the oxidation with the oxidant and the co-oxidant.6. The process according to claim 4 , wherein the oxidant contains a hypervalent iodine compound claim 4 , and the co-oxidant contains a peroxide and/or a peroxy acid.7. The process according to claim 4 , wherein the compound is allowed to react with a hypervalent iodine compound and a peroxide in the presence of a strong acid in a solvent claim 4 , then an alkali metal carbonate is added to the reaction system and the reaction is continued. The present invention relates to a 15-oxosteroid compound useful as an intermediate for preparing a compound having an oxo group introduced on the 15-position of a steroid skeleton thereof and having a pharmacological activity (for example, an antiandrogenic activity), and a process for producing the 15-oxosteroid compound.Pregnane compounds (pregnane steroid compounds) having various physiological activities or pharmacological activities are prepared by introducing various functional groups or active groups to the steroid skeletons. Steroid compounds having antiandrogenic activities are used as ...

17beta-substituted 4-aza-5alpha-androstan-3-one derivatives

Method of producing 17-aza-16-keto-steroids derivatives

A kind of method of molecularly distilled purification tanshinone IIA

本发明实施例公开了一种分子蒸馏法提纯丹参酮ⅡA的方法，包括如下步骤：步骤100、向丹参中加入足量的乙醇，并通过加热回收收集粗提取液体；步骤200、将收集的粗提取液体进行分子蒸馏法脱去溶剂乙醇得到提取物；步骤300、对提取物进行二次提纯得到丹参酮ⅡA；采用分子蒸馏的方式进行提纯，由于蒸馏温度低，仅在30℃左右，丹参酮ⅡA不易发生分解，使得丹参酮ⅡA的提取率能够达到81％左右，大幅度提高了丹参酮ⅡA的提取率。

Androstenone derivatives

본 발명은 17β-N-(2,5-비스(트리플루오로메틸))페닐카르바모일-4-아자-5α-안드로스트-1-엔-3-온으로 알려진 하기 일반식 (I)의 화합물, 그의 용매화물, 그의 제조 방법, 그의 제조 과정에서 사용한 중간체, 그의 제약 제제, 및 안드로겐 반응성 및 매개형 질병의 치료에 있어서의 그의 용도에 관한 것이다. The present invention relates to compounds of the general formula (I) known as 17β-N- (2,5-bis (trifluoromethyl)) phenylcarbamoyl-4-aza-5α-androst-1-en-3-one Compounds, solvates thereof, methods of preparation thereof, intermediates used in the preparation thereof, pharmaceutical preparations thereof, and their use in the treatment of androgen reactivity and mediated diseases.

PH-responsive rosin-based rigid surfactant and preparation method and application thereof

以松香为原料，经D‑A加成、酰亚胺化、重氮化、偶合和酸碱中和反应制备了一种pH响应型松香基全刚性阴离子表面活性剂(Na‑MPA‑AZO‑Na)，该表面活性剂可用于制备碳纳米管分散液。由Na‑MPA‑AZO‑Na制备的pH响应型碳纳米管分散液，当pH大于9.97时，碳纳米管分散液可稳定90天；当pH小于5.5时，碳纳米管会完全析出，并且析出的碳纳米管，只需将pH调至大于9.97即可再次分散，不需要再次超声，这使得该pH响应型碳纳米管分散液在传感器件、生物医疗及能量储存中更具有潜在的应用价值。

A kind of production technology of high-purity dutasteride

本发明公开了一种高纯度的度他雄胺的提纯生产工艺，所要解决的问题是：提高度他雄胺的纯度，降低生产成本。该方法在得到度他雄胺粗品后经过两次结晶，得到收率高且纯度高的度他雄胺。本发明具有高效率、清洁化生产的优势，可操作性强。通过对中间体的精制，使得度他雄胺成品的质量更易控制，获得的度他雄胺产品的纯度不低于99.5％，其中任一单个杂质不超过0.1％。

Brassinosteroidal derivatives and plant growth regulating agent

FIELD: agriculture. SUBSTANCE: present invention describes brassinosteroidal derivatives represented in formula (I) and formula (II): ЭРУ ГЕС ПЧ Го РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (19) (51) МПК ВИ” 2114 116. 13) СЛ С 07 4 63/00, 73/00, А 01 М 43/22 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 96101167/04, 31.05.1994 (30) Приоритет: 01.06.1993 УР 5/130826 (46) Дата публикации: 27.06.1998 (56) Ссылки: УР, 64-960, С 07 + 53100, 1989. Доклады АН СССР, 1989, 305, М 5, с.1277-1 279. Воспет.Зос.Тгап$, 1983, 11, М5, с.543 - 548. (86) Заявка РСТ: УР 9400881 (31.05.94) (71) Заявитель: Тама Биокемикал Ко., Лтд. (Р)} (72) Изобретатель: Сугуру Такацуто (.Р), Ясуо Камуро (ШР), Цуеси Ватанабе (.Р), Хироки Курияма (.Р) (73) Патентообладатель: Тама Биокемикал Ко., Лтд. (Р)} (54) БРАССИНОСТЕРОИДНЫЕ ПРОИЗВОДНЫЕ И РЕГУЛИРУЮЩЕЕ РОСТ РАСТЕНИЙ СРЕДСТВО (57) Реферат: Брассиностероидные производные, представленные формулой (1!) и формулой (11) СН ов’ 3 СН -СН С" “2 И о о И СН_-—СН_-СН_-с-© 3 2 2, ',, СН_-СН_-СнН_-<-0" 73 ПЕН о и регулятор роста растений, содержащий по меньшей мере один из них в качестве активного ингредиента, тем самым изобретение представляет новые брассиностероидподобные — соединения, выраженные формулой (1) и формулой (11) и регулятор роста растений, содержащий эти соединения, проявляющие устойчивое регулирующее воздействие на рост растений. 3 с.п.Ф-лы, 8 табл. 2114116 С1 КО ЭРУ ГЕС ПЧ Го КУЗЗАМ АСЕМСУ ГОК РАТЕМТ$ АМО ТКАОЕМАКК$ ЗВО“” 2114 116 Сл (51) 1пЕ. С1.6 43/22 12) АВЗТКАСТ ОЕ 1МУЕМТОМ С 07 4 63/00, 73/00, А 01 М (21), (22) АррИсаНоп: 96101167/04, 31.05.1994 (30) Рнощу: 01.06.1993 УР 5/130826 (46) Рае о! рибИсаНоп: 27.06.1998 (86) РСТ аррИсанНоп: УР 9400881 (31.05.94) (72) |пуетог: (71) АррИсапе: Тата ВюкКепика! Ко., Ца. (3Р) Зидиуги Таказщо (.Р), чазио Катуго (.Р), Тзиез! Маапабе (УР), Кыгок! Кигуата (/Р) (73) Ргорпеюг: Тата ВюкКепика! Ко., Ца. (}Р) (54) ВВАЗЗМОЗТЕКОШЮАЕ ОВЕКМАТМЕЗ$З АМО РЕАМТ СКОМТН ВКЕСОУГАТМС ...

7β-METHYL-3,17αβ-DISULFAMOYLOXY-D-HOMO-6-OXA-ESTRA-1,3,5(10), 8,14-PENTAEN AS BREAST CANCER MCF-7 CELLS GROWTH INHIBITOR

FIELD: pharmacology. SUBSTANCE: invention relates to 7β-methyl-3,17αβ-disulfamoyloxy-D-homo-6-oxa-estra-1,3,5(10), 8,14-pentaene of formula as breast cancer MCF-7 cells growth inhibitor. EFFECT: new compound is obtained that can be used for breast cancer treatment. 1 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 619 457 C1 (51) МПК C07J 73/00 (2006.01) A61K 31/566 (2006.01) A61P 35/00 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ФОРМУЛА (21)(22) Заявка: ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ 2016116869, 29.04.2016 (24) Дата начала отсчета срока действия патента: 29.04.2016 Дата регистрации: Приоритет(ы): (22) Дата подачи заявки: 29.04.2016 (45) Опубликовано: 16.05.2017 Бюл. № 14 C 1 2-Alkylestra-1,3,5(10)-trien-3-ol Derivatives: Synthesis, In Vitro and Vivo Anticancer Activity" JOURNAL OF MEDICINAL CHEMISTRY, Vol. 50, N18, 2007, 4431-4443, фиг. 1, соед. 4. RU 2562242 C1, 10.09.2015. EA 019708 B1, 30.05.2014. С.Н. Морозкина и др. "Синтез и исследование некоторых биологических свойств (см. прод.) (54) 7β-Метил-3,17αβ-дисульфамоилокси-D-гомо-6-окса-эстра-1,3,5(10),8,14-пентаен в качестве ингибитора роста клеток рака молочной железы MCF-7 (57) Формула изобретения 7β-метил-3,17αβ-дисульфамоилокси-D-гомо-6-окса-эстра-1,3,5(10),8,14-пентаен формулы в качестве ингибитора роста клеток рака молочной железы МСF-7. (56) (продолжение): сульфаматов 8α-аналогов стероидных эстрогенов" ЖУРНАЛ ОРГАНИЧЕСКОЙ ХИМИИ, т. 51, вып. 3, 2015, 425-430. Стр.: 1 C 1 2 6 1 9 4 5 7 (56) Список документов, цитированных в отчете о поиске: C. Bubert et al. "3,17-Disubstituted 2 6 1 9 4 5 7 Адрес для переписки: 690091, кр. Приморский, г. Владивосток, ул. Суханова, 8, отдел интеллектуальной собственности ДВФУ R U (73) Патентообладатель(и): Федеральное государственное автономное образовательное учреждение высшего образования "Дальневосточный федеральный университет" (ДВФУ) (RU) 16.05.2017 R U (72) Автор(ы): Шавва Александр Григорьевич (RU), Морозкина Светлана Николаевна (RU), ...

A method of preparing triptonide

本发明公开了一种制备雷公藤内酯酮的方法。存在于雷公藤中的雷公藤内酯酮、雷公藤甲素、雷公藤乙素和2‑表雷公藤乙素结构非常接近，其中雷公藤乙素和2‑表雷公藤乙素为一对手性异构体，分离难度大。现有技术在分离这四种化合物时，无不依赖于反复硅胶柱层析，然而反复硅胶柱层析耗费溶剂、重现性差，只适合于实验室少量分离，难以在工业生产中推广。目前工业生产中，唯一在使用的柱色谱只有大孔树脂。本发明提供的方法不依赖于反复硅胶柱层析即可分离制备雷公藤内酯酮、雷公藤甲素、雷公藤乙素和2‑表雷公藤乙素。本发明提供的HPLC方法基于常规的C18色谱柱即可有效分离手性异构体雷公藤乙素和2‑表雷公藤乙素，成本低、重复性高。

Azasteroids

NEW 3-AMINO-17A-AZA-D-HOMOANDROSTANE DERIVATIVES, THEIR PREPARATION PROCESS AND THE PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

Nouveaux dérivés du 3-amino-17a-aza-D-homo-5 alpha -androstane de formule générale I : New derivatives of 3-amino-17a-aza-D-homo-5 alpha -androstane of general formula I:

Process for preparing 7-oxa-d-homo-pregnenes and-alpha-nor-pregnenes

2-oxo-3-oxo-estra 4,9-dienes having hormonal - activity

2-Oxo-3-oxo-estra 4, 9-dienes having hormonal activity Title steroids, of general formula (I): where R1=H, acyl or alkyl, R2=H, or an opt. substd. hydrocarbon radical, are prepd by reacting a hydrogenation agent, preferably H in the presence of a catalyst such as palladium on alumina, inactivated by the addition of lead acetate, pyridine or both, with the corresponding 2-oxo-3-oxo estra 4,9,11-triene (II) to produce the novel 2-oxo-3-oxo estra 5(10) 9 (11) -diene (III). This is isomerised with for example a strong acid such as perchloric or polyphosphoric, giving the title 4,9-dienes (I) which have known hormonal activity, as do their triene intermediates. Example prepares 2-oxo-3-oxo 17 beta-benzoyloxy estra 4,9-diene.

17-Aza-16-ketosteroids - useful as inters

Hydroxy-17β oxa-4 δ -5α androstenones-3, in particular those 17-alkylated, and esters derived therefrom.

New indazole derivatives and their preparation

METHYL-28 BRASSINOSTEROIDES, PROCESS FOR THE PREPARATION THEREOF, AS WELL AS PRODUCTS CONTAINING SUCH COMPOUNDS AND HAVING A REGULATORY ACTION ON PLANT GROWTH

Aromatic steroid derivatives substituted by an endocyclic nitrogen atom and method of preparation

Androstenone derivative

(22R, 23R, 24S) -22,23-EPOXY-2-ALPHA, 3-ALPHA-ISOPROPYLIDENDIOXY-B-HOMO-7-OXA 5-ALPHA-STIGMASTAN-6-ON, METHOD FOR THE PRODUCTION THEREOF AND PLANT GROWTH REGULATION REGULATORY REGULATION THEY INCLUDE.

A kind of method that use membrane separation technique prepares high-purity triptolide

本发明公开了一种采用膜分离技术分离雷公藤甲素的方法，以乙醇溶液为溶剂提取的雷公藤为原料，经粗过滤，再用适当的膜进行分离除杂,去除大分子杂质后得雷公藤甲素粗品，进一步浓缩，过一次硅胶柱，即可得纯度为99%以上的雷公藤甲素无色针状结晶产品。本发明取代了传统工艺中先用大量有机溶剂进行萃取后再多次过柱层析的方法，简化了工艺，可常温分离，对热敏性物质不会产生破坏，并大量节约有毒的有机溶剂，保护环境，降低生产成本，且收率高，安全可靠，具有很强的经济竞争力，符合国家倡导的绿色发展中药理念。

Methods of treating androgenic alopecia with finasteride [17β-N-mono-substituted-carbamoyl-4-aza-5-α-androst-1-en-ones]

17β-N-monosubstituted-carbamoyl-4-5α-androst-1-en-3-ones of the formula ##STR1## wherein R 1 is selected from hydrogen, methyl and ethyl and R 2 is a branched chain alkyl of from 3-12 carbons, and R', R", R'" are hydrogen or methyl are active as testosterone 5α-reductase inhibitors and thus are useful topically for treatment of androgenic alopecia.

Process for obtainin new 3-amino-17a-aza-d-homoandrostane derivatives

One class dehydroabietic acid quinoxaline derivant and its preparation method and application

本发明公开了一类脱氢枞酸喹喔啉衍生物及其制备方法和应用，所述一种具有通式(Ⅰ)所示结构的脱氢枞酸喹喔啉衍生物I‑a至I‑i及其在药学上可接受的盐： 其中，脱氢枞酸喹喔啉衍生物I‑a至I‑i对应的R分别为： 所述的通式I所示结构的脱氢枞酸喹喔啉衍生物I‑a至I‑i的制备方法，包括如下步骤：

17-alkyl-7-substituted-4-aza steroid derivatives

The novel compounds of the present invention are those of structural formula (I), or a pharmaceutically acceptable salt, or stereoisomer thereof, which are inhibitors of 5.alpha.-reductase, particularly 5.alpha.-reductase type 1. The compounds of formula (I) are useful in the systemic, including oral, or parenteral or topical treatment of hyperandrogenic conditions such as acne vulgaris, seborrhea, androgenic alopecia which includes female and male pattern baldness, female hirsutism, benign prostatic hyperplasia, and the prevention and treatment of prostatic carcinoma, as well as in the treatment of prostatitis. Methods of using the compounds of formula (I) for the treatment of hyperandrogenic conditions such as acne vulgaris, seborrhea, androgenic alopecia, male pattern baldness, female hirsutism, benign prostatic hyperplasia, and the prevention and treatment of prostatic carcinoma, as well as the treatment of prostatitis are provided, as well as pharmaceutical compositions for the compounds of formula (I). The use of compounds of formula (I) in combination with other active agents, for example with a 5.alpha.reductase type 2 inhibitor such as finasteride or epristeride, or a potassium channel opener, such as minoxidil, or a retinoic acid or a derivative thereof is also taught, wherein such combinations would be useful in one or more of the above-mentioned methods of treatment or pharmaceutical compositions.

Process for the production of 6- and 7-membered A-ring lactams of the androstane series

17beta-n-(2,5-bis-(trifluoromethyl)-phenylcarbamoyl-4-aza-5alfa- -androst-1-ene-3-one, methods of its synthesis, pharmaceutical composition, method of treatment

FIELD: organic chemistry, steroids. SUBSTANCE: invention describes a new compound of the formula (I) Эсбо0оу7тЬс ПЧ Го РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (19) ВО “” 2 140 926 ' МК" С 07 4 73/00, 41/00, А бл К 13) СЛ 31/58 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 96108410/04, 16.09.1994 (24) Дата начала действия патента: 16.09.1994 (30) Приоритет: 17.09.1993 Ц$ 08/123,280 (46) Дата публикации: 10.11.1999 (56) Ссылки: 1. Сит. шуез,, 89, 293 (1992). Машге, 354, 159 (1991). 4. Ст. шуез, ЗО, 799 (1992). Зегоч$, 32, 257 (1978). Тринус Ф.П. Фармакотерапевтический справочник. - Киев, Здоровья, 1989, с. 263. (85) Дата перевода заявки РСТ на национальную фазу: 17.04.96 (86) Заявка РСТ: 1$ 94/10530 (16.09.94) (87) Публикация РСТ: М/О 95/07927 (23.03.95) (98) Адрес для переписки: 193036, Санкт-Петербург, а/я 24, НЕВИНПАТ (71) Заявитель: Глаксо Веллкам Инк. (0$) (72) Изобретатель: Бэчелор Кеннет Уильям (ЦЗ), Фрай Стивен Вернон (Ц$) (73) Патентообладатель: Глаксо Веллкам Инк. (0$) (54) 17В-М-(2,5-БИС(ТРИФТОРМЕТИЛ)ФЕНИЛКАРБАМОИЛ-4-АЗА-5 а-АНДРОСТ-1-ЕН-3-ОН, СПОСОБЫ ЕГО ПОЛУЧЕНИЯ, ФАРМАЦЕВТИЧЕСКИЙ СОСТАВ, СПОСОБ ЛЕЧЕНИЯ (57) Реферат: Описывается новое соединение формулы |: 17 В-№-(2,5-бис(трифторметил)фенилкарбамо ил-4-аза-5х-андрост-1-ен-3-он как необычайно сильный и избирательный двойственный ингибитор человеческой 5а-редуктазы типа 1 и 2. Описывается также способ его получения, фармацевтический состав на основе указанного соединения и способ лечения. 5 с. и 2 3.п.Ф-Лы. 1 табл. СЕ 3 2140926 С1 КО Эсбо0оу7тЬс ПЧ Го (19) КУЗЗАМ АСЕМСУ ГОК РАТЕМТ$ АМО ТКАОЕМАКК$ 12) АВЗТКАСТ ОЕ 1МУЕМТОМ ВИ "” 2 140 926” Сл (ть 216 073 73/00, 41/00, Аб К 31/58 (21), (22) АррИсаНоп: 96108410/04, 16.09.1994 (24) ЕНесНуе дае Гог ргорейу па: 16.09.1994 (30) Рпогйу: 17.09.1993 4$ 08/123,280 (46) Рае оГ рибИсаНоп: 10.11.1999 (85) Соттепсетеп+ о! пайопа! рпазе: 17.04.96 (86) РСТ аррИсаНоп: ($ 94/10530 (16.09.94) (87) РСТ рибсаНоп: М/О 95/07927 (23.03.95) (98 ...

17-Aza-16-ketosteroids

17-Aza-16-keto-steroids - useful as intermediates. Title steroids have formula (I) and (Ia): (where R is free or masked oxo or is H and a free or masked hydroxy gp.; R1 is H or 1-4 C alkyl, and R2 is alkoxy) and are key inters. for therapeutically valuable bactericides and bacteriostats and hypocholesterolaemics.

Process for iodinating or brominating the alpha-methylenic carbon of a secondary amide

A kind of triptolide alcohol derivative, Preparation Method And The Use

本发明涉及一种雷公藤内酯醇衍生物，所述雷公藤内酯醇衍生物为具有式(I)和/或式(II)结构的化合物，或具有式(I)和/或式(II)结构的化合物医学上可接受的盐，或具有式(I)和/或式(II)结构的化合物的光学异构体，或具有式(I)和/或式(II)结构的化合物医学上可接受的盐的光学异构体。本发明提供的雷公藤内酯醇类衍生物在pM(10 ‑12 mol/L)溶度即可高效抑制胶质细胞BV2分泌TNF‑α的作用，同时本发明化合物可抵制Aβ 1‑42 对原代皮层神经元的毒性。

Synthesis method of C-19 single-acyl triptolide derivative

本发明公开了一种C‑19位单酰基化雷公藤内酯醇衍生物的合成方法，以雷公藤内酯醇及其衍生物为原料，与酰化试剂和缚酸剂在反应溶剂中在‑78～0℃反应后升温至‑5～5℃，加酸溶液淬灭反应，反应液用萃取溶剂稀释萃取，得到的有机相经饱和氯化钠水溶液洗、浓缩、柱层析得到C‑19位单酰基化雷公藤内酯醇衍生物。本发明的合成方法，步骤少，耗时短，收率高，纯度高。

Inhibitors of 5-alpha-testosterone reductase

The present invention relates to certain substituted 17.beta.-substituted carbonyl-6-azaandrost-4-en-3-ones of formula (I), especially those of formula (IG) wherein R1 and R1 are: i) independently hydrogen or lower alkyl and the bond between the carbons bearing R1 and R2 is a single or a double bond, or ii) taken together are a -CH2- group to form a cyclopropane ring, and the bond between the carbons bearing R1 and R2 is a single bond; R3c is hydrogen; R4c is hydrogen, lower alkyl, lower cycloalkyl, lower alkenyl, alkanoyl of 2-6 carbons, -(CH2)mCO2R16, -(CH2)mAra, -(CH2)n'CONR17R18, -(CH2)n'NR17R18 or -(CH2)n'OR16, wherein R16 is hydrogen, lower alkyl or lower alkenyl; R17 and R18 are independly hydrogen, lower alkyl lower cycloalkyl or lower alkenyl; Ara is an aromatic group of 6 to 12 carbons; n' is 0 or an integer from 1 to 5; m is an integer from 1 to 5; R19 and R20 are independently hydrogen or lower alkyl, or taken together R19 and R20 form a carbonyl group(=O); R5c is lower alkyl, lower alkenyl, lower cycloalkyl, lower alkoxy, or NR21R22, wherein R21 and R22 are independently hydrogen, lower alkyl or lower alkenyl; and pharmaceutically acceptable salts thereof, their preparation, medical use and pharmaceutical formulations.

Synthesis of a substituted indene derivative

This invention is also directed to intermediates utilized in the methods of preparing AQX-1125.

Inhibitors of testosterone 5-alpha reductase activity

Aldehyde metabolite of 17β-N-monosubstituted-carbamoyl-4-aza-5α-a

17β-N-monosubstituted-carbamoyl-4-aza-5α-androst-1-en-3-ones of the formula: ##STR1## wherein the dotted line can represent a double bond when present, R 1 is selected from hydrogen, methyl and ethyl and R 2 is CONHC(CH 3 ) 2 CHO, and Ra is methyl, are described as being useful for the treatment of benign prostatic hypertrophy.

Novel 6-substituted oxa- or azasteroid compound

A 6-substituted oxa- or azasteroid compound represented by general formula (I), having an excellent aromatase inhibitory activity, and being useful for preventing or treating diseases caused by estrogens, such as mammary cancer, uterus carcinoma, prostatic hypertrophy, and so forth. This compound has an oxygen or nitrogen atom in the steroidal D ring and the 6-position (R1) is substituted by -S-R2 (R2 representing hydrogen, lower alkyl, cyano or acyl), O-R3 (R3 representing hydrogen, lower alkyl, or acyl), azido or amino.

OXIDIZATION METABOLITES OF 5α-23-METHYL-4-AZA-21-NOR-CHOL-1-ENE-3,20-DIONE

The compounds of formula (I) wherein R is selected from the group hydroxymethyl and carboxy, have been identified as metabolites of 5α-23-methyl-4-aza-21-nor-chol-1-ene-3,20-dione and are believed to be active as testosterone 5α-reductase inhibitors and would thus be useful for treatment of acne, seborrhea, female hirsutism or benign prostatic hypertrophy.

4-azasteroids for treatment of hyperandrogenic conditions

Compounds of structural Formula (I), and pharmacologically acceptable salts and esters thereof possess 5α-reductase inhibitory activity. These compounds inhibit 5α-reductase type 1 and type 2. The compounds of structural Formula (I) are useful in the systemic, including oral, and parenteral, including topical, treatment and prevention of hyperandrogenic conditions including prostatic carcinoma, benign prostatic hyperplasia, acne vulgaris, seborrhea, androgenic alopecia (also called androgenetic alopecia) which includes male- and female-pattern baldness, female hirsutism, and prostatitis. A class of compounds of the present invention are also potent anti-androgens. The present invention also relates to novel compositions containing such compounds, methods of their use and methods of their manufacture.

17-HALOGEN-4-AZAANDROSTEN DERIVATIVES AND METHOD FOR THE PRODUCTION THEREOF

Triptolidenol derivative and application thereof

本发明公开了雷醇内酯衍生物及其应用。具体而言，如通式(Ι)所示的化合物及其光学异构体和药学上可接受的盐；这类新的雷醇内酯衍生物的制备方法；含有这类雷醇内酯衍生物的药物组合物；以及这类雷醇内酯衍生物在制备抗肿瘤药物上的应用。

A method of preparing triptolide

本发明公开了一种制备雷公藤甲素的方法。存在于雷公藤中的雷公藤内酯酮、雷公藤甲素、雷公藤乙素和2‑表雷公藤乙素结构非常接近，其中雷公藤乙素和2‑表雷公藤乙素为一对手性异构体，分离难度大。现有技术在分离这四种化合物时，无不依赖于反复硅胶柱层析，然而反复硅胶柱层析耗费溶剂、重现性差，只适合于实验室少量分离，难以在工业生产中推广。目前工业生产中，唯一在使用的柱色谱只有大孔树脂。本发明提供的方法不依赖于反复硅胶柱层析即可分离制备雷公藤内酯酮、雷公藤甲素、雷公藤乙素和2‑表雷公藤乙素。本发明提供的HPLC方法基于常规的C18色谱柱即可有效分离手性异构体雷公藤乙素和2‑表雷公藤乙素，成本低、重复性高。

Androstenone derivatives

EPIMERS OF (22RS) -N- (1,1,1-TRIFLUORO-2-PHENYLPROP-2-IL) -3-BONE -4-AZA-5ALFA-ANDROST-1-ENE-17BETA-CARBOSSAMIDE

New process for producing 17-betha-hydroxy-17-alpha-methyl-2-oxa-5-alpha-androstan-3-on and intermediate thereof

Novel 17.beta.-substituted 4-azaandrostane derivatives, pharmaceutical compositions containing them and process for preparing same

The invention relates to novel 17.beta.-substituted 4-azaandrostane derivatives of general Formula (I), wherein R means hy-drogen or a C1-3alkyl group; R1 and R2 are the same or different and stand for hydrogen or a C1-4alkyl group with the provi-so that both can mean hydrogen only in the case when n is higher than 5; or R1 and R2 together mean an .alpha.,.omega.-alkylene group containing 5 to 7 carbon atoms, the terminal carbon atoms of said alkylene group being bound to the same ring carbon atom; n is 4, 5, 6 or 7; and --- bond line represents a single or double bond. Furthermore, the invention relates to pharmaceutical composi-tion containing these compounds as well as a process for the preparation of the compounds of general Formula (I). The com-pounds of general Formula (I) exert a 5.alpha.-reductase enzyme-inhibiting effect and therefore, they are useful for treating all diseas-es, where the aim is to reduce the tissue dihydrotestosterone level, such as the benign prostatic hyperplasia, acne, seborrhoea, female hirsutism or androgenic alopecia.

28-METHYL BRASSINOSTEROID DERIVATIVES; METHOD FOR PREPARING THESE COMPOUNDS; AGENTS WITH GROWTH CONTROLLING ACTION FOR PLANTS CONTAINING THESE COMPOUNDS.

Method for preparing finasteride

The present invention relates to a process for the preparation of finasteride, the compound of formula (I), comprising the reaction of the compound of formula (II) with t-butylamine. ##STR1##

A kind of method that limonin substances are extracted from orange peel

本发明公开了一种从柑橘果皮中提取柠檬苦素类物质的方法，其工艺包括下述步骤：柑橘果皮脱脂、抽提、纯化、浓缩复溶、结晶、干操，得最终产品。本发明的有益效果是：利用热回流提取、吸附树脂分离杂质等过程。本发明方法提取纯度高，操作简单，试剂消耗少，污染少，所得固形物中柠檬苦素类似物含量＞30%，柠檬苦素含量＞9%，诺米林含量＞10%的固形物。

17 β-acyl-4-aza-5 α-androst-1-ene-3-ones as 5 α-reductase inhibitors

17β-Acyl-4-aza-5α-Androst-1-end-3-ones of the formula: ##STR1## wherein R is selected from hydrogen, methyl and ethyl and R 3 is cycloalkyl of from 4-8 carbons; and pharmaceutical formulation of the above compounds are active as testosterone 5α-reductase inhibitors and thus are useful for treatment of acne, seborrhea, female hirsutism, androgenic alopecia, prostatic carcinoma and benign prostatic hypertrophy.

Preparation method of 28-high brassinolide

本发明涉及一种28‑高芸苔素内酯制备方法，属于有机合成技术领域。本发明以(2,22)‑二烯‑24S‑乙基‑5α‑胆甾‑6‑酮为原料在手性催化剂和氧化剂作用下得到相应的不对称环氧化物，然后经酯化、氧化、水解反应得到。本发明催化剂选择性高，高效，用量少，成本低，工艺简单，操作方便，环境友好具有较好工业应用价值。

Androstenone derivative

Intermediates for the production of sometimes tritiated 16-imino-17-azasteroids

Selective estrogen receptor modulators

The present invention relates to a selective estrogen receptor modulator of formula I: I; or a pharmaceutical acid addition salt thereof; useful, e.g., for treating endometriosis and uterine leiomyoma. X16065 PCT - -

Substituted 6-azacholesten-3-ones

The present invention relates to 17β-substituted-6-azacholesten-3-ones of Formula (I) wherein: R?1 and R2¿ represent independently hydrogen or alkyl and the bond between carbons 1 and 2 is a single or a double bond, or R?1 and R2¿ may be joined together to form a fused cyclopropane ring; R3 represents hydrogen, alkyl or halogen; R?4 and R5¿ represent independently hydrogen or alkyl; R6 represents alkyl; and the pharmaceutically acceptable salts and solvates thereof, and their use as 5α-testosterone reductase inhibitors.

Steroid 5-alpha-reductase inhibitors

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, processes for their preparation, pharmaceutical compositions contaning them and their use in therapy as inhibitors of steroid 5-alpha-reductase.

Novel 6-substituted oxa- or azasteroid compound

4-azasteroid 5-alpha-reductase inhibitors

Novel substituted 4-azasteroid 5-.alpha.-reductase inhibitors of formula (I), wherein A is (a), (b) or (c), are claimed as well as pharmaceutically acceptable salts and formulations thereof. These compounds are effective inhibitors of testosterone 5.alpha.-reductase(s) and are thus useful in the treatment of a number of hyperandrogenic conditions including benign prostatic hypertrophy, acne, seborrhea, female hirsutism, and male and female pattern baldness (alopecia).

Epimers of (22rs)-n-(1,1,1-trifluoro-2-phenylprop-2-yl)-3-oxo-4-aza-5.alpha.-androst-1-ene-17.beta.-carboxamide

The present invention relates to the epimers: (22R)-N-(1,1,1-trifluoro-2-phenylprop-2-yl)-3-oxo-4-aza-5.alpha.-androst-1-ene-17.beta.-carboxamide and (22S)-N-(1,1,1-trifluoro-2-phenylprop-2-yl)-3-oxo-4-aza-5.alpha.-androst-1-ene-17.beta.-carboxamide useful as inhibitors of testosterone 5.alpha.-reductase enzyme, to a process for their preparation and to pharmaceutical compositions containing them.

Process for the production of physiologically active steroids

Preparation method of N-substituted maleopimarimide

本发明涉及一种N-取代马来海松酸酰亚胺的制备方法，主要解决现有技术中合成工艺困难、反应温度较高、产品收率较低的问题。本发明通过采用一种N-取代马来海松酸酰亚胺的制备方法，以马来松香和苯胺或马来松香和苯胺衍生物作为原料、以聚乙二醇作为溶剂、以苯及其衍生物作为带水剂、在溶剂和带水剂同时存在时，在反应温度为80-140℃时，经酰胺化、脱水环合反应得到产品的技术方案较好地解决了上述问题，可用于N-取代马来海松酸酰亚胺的制备中。

METHOD FOR PRODUCING CARBOXAMIDO-4-AZASTEROIDS

17-BETA-SUBSTITUTED-4-AZA-5-ALPHA-ANDROSTENONE AND THEIR APPLICATIONS AS 5-ALPHA-REDUCTAE INHIBITORS.

Compounds of formula: <CHEM> in which R is hydrogen, methyl or ethyl; R<2> is a branched alkyl radical having up to 12 carbon atoms; R min is hydrogen or methyl; R sec is hydrogen, alpha -methyl or beta -methyl, and R''' is hydrogen, alpha -methyl or beta -methyl, and pharmaceutical formulations containing the above compounds are active as testosterone 5 alpha -reductase inhibitors and thus are useful topically for treatment of acne, seborrhoea and female hirsutism, and systemically in the treatment of benign prostatic hypertrophy.

17-aza-16-keto-steroid derivatives and the preparation thereof

Derivatives of 17-halogen-4-azaaNdrostAnE

Derivatives of 17-halogen-4-azaandrostane of the general formula (I) in which R – hydrogen or C1-C3 alkyl, X - chlorine, bromine or iodine, and: - single or olefinic link.

A-furan steroids

Richard brasch

28-methyl-brassinosteroid derivatives having a plant growth-regulating action and their manufacture and use

Solid and crystalline dutasteride and processes for preparation thereof

The present invention relates to a synthetic process for manufacturing Dutasteride comprising the mixed anhydride formation, subsequent reaction with 2,5- bis(trifluoromethyl)phenylamine in the presence of an appropriate Lewis catalyst and its isolation, purification and crystallization from acetonitrile/water. The invention also relates to a novel polymorphic form of Dutasteride, called form III, and a pharmaceutical composition comprising it.

Purification 4-aza-androst-1-ene-17-oic acid from 4-aza-androstan-17-oic acid

The present invention relates to a process of separation of 4-aza-androst-1-ene-17-oic acid from 4-aza-androstan-17-oic acid, which brings to 4-aza-androst-1-ene-17-oic containing less than 0.05% w/w of 4-aza-androstan-17-oic acid, with high yield and productivity. In particular, the present invention relates to a process for the separation of 4-aza-androstan-17-oic acid from 4-aza-androst-1-ene-17-oic acid, comprising the steps of treating the crude 4-aza-androst-1-ene-17-oic acid with formic acid and recovering the purified 4-aza-androst-1-ene-17-oic acid containing 4-aza-androstan-17-oic acid in w/w% less than 0,05%.

Novel oxa- or azasteroid derivative

A compound represented by general formula (I), which has an aromatase inhibitory activity and is useful for preventing and treating diseases caused by hyperestrogenosis, such as mastocarcinoma, metrocarcinoma and prostatomegaly. In formula (I) A represents C=O, CH₂, C=CH₂ or C=CH-lower alkyl; B represents O, NH or N-lower alkyl; X is nil, or represents C=O or CH₂; n is 2 or 3 when X is nil, or 1 or 2 when X represents C=O or CH₂; and the broken line between the 1-position and the 2-position in the steroidal skeleton means an optional presence of a double bond therebetween.

Substituted 6-azacholesten-3-ones

2-ethyl-6-oxaestra-1,3,5(10),8,14-pentenes sulfamates as mcf-7 tumour cells proliferation inhibitors

FIELD: pharmacology. SUBSTANCE: invention relates to sulfamate of 2-ethyl-6-oxaestra-1,3,5(10),8,14-pentenes of the formula as MCF-7 tumour cells proliferation inhibitors. EFFECT: new compounds are obtained which can be used in medicine for hormone-dependent cancers treatment. 2 ex

NOVEL 1-OXA-5-HYDROXY-9alpha-HALO-17beta-ACYLOXY-A-NOR-10alpha-ESTRAN-2-ONES, SULPHONATES THEREOF, AND PROCESSES FOR THEIR PREPARATION

1,274,034. 1-Oxa-A-norestranes; de-4-estranes., ROUSSEL-UCLAF. 9 July, 1969 [9 July, 1968], No. 30116/71. Divided out of 1,274,031; Heading C2C. Novel compounds of formula (wherein R<SP>3</SP> is H, mesyl or tosyl, X is Cl or Br and Ac is C 1-18 carboxylic acyl) are prepared from compounds of formula (wherein R<SP>2</SP> is alkyl) by reaction with HCl or HBr, followed, when required, by mesylation or tosylation. 5# - Hydroxy - 5# - ethoxycarbonylmethyl - 9#, 10# - epoxy - 17# - acetoxy - de - A - estrane (XI) is prepared from 17#-hydroxy-de-A-estr-9-en-5- one (X) by the sequence X #9#,10#-epoxy-17#- hydroxy-de-A-estran-5-one #9#,10#-epoxy-17#- acetoxy-de-A-estan-5-one #XI.

Androstenones

The present invention relates to compounds of formula (I), wherein carbons 1 and 2 are joined by either a single or a double bond; R1 is hydrogen or methyl; R2 is hydrogen or methyl; R3 is (A) or (B) wherein X, W, Z, R?4, R5, R6, R7 and R8¿ are various groups, and pharmaceutically acceptable solvates thereof and their use in the treatment of androgen responsive and mediated diseases.

4-oxa- and 4-oxa-a-homo-steroids

1,261,981. 4-Oxa- and 4-oxa-A-homosteroids. E. R. SQUIBB & SONS Inc. 25 Feb., 1969 [5 March, 1968], No. 10071/69. Heading C2C. The invention comprises compounds of the formulµ wherein R is H or Me, Acyl is a hydrocarbon carboxylic acyl radical of less than twelve carbon atoms, and the wavy lines denote either the α- or #-configuration. The compounds of Formula II are prepared by treating 17α- acyloxy-progesterones or -19-norprogesterones with organic peracids, and are converted into the compounds of Formula III by heating (preferably to 170-200‹ C.) or by treatment with an acid or base. The compounds of Formula III are stated to possess anti-estrogenic activity and may be made up with carriers into pharmaceutical or veterinary compositions for oral or parenteral administration.

PROCESS FOR THE PREPARATION OF A STEREID 16-IMINO 17-AZA WHICH CAN BE TRIUTED AND INTERMEDIATE THEREIN

L'INVENTION A POUR OBJET UN PROCEDE DE PREPARATION DES PRODUITS DE FORMULE I : (CF DESSIN DANS BOPI) DANS LAQUELLE A REPRESENTE UN ATOME D'HYDROGENE OU DE TRITIUM A PARTIR DES PRODUITS DE FORMULE II : (CF DESSIN DANS BOPI) DANS LAQUELLE R REPRESENTE UN RADICAL ACYLE AYANT DE 1 A 8 ATOMES DE CARBONE,AINSI QUE DES PRODUITS INTERMEDIAIRES DE CE PROCEDE. THE SUBJECT OF THE INVENTION IS A PROCESS FOR PREPARING THE PRODUCTS OF FORMULA I: (CF DRAWING IN BOPI) IN WHICH A HYDROGEN OR TRITIUM ATOM IS REPRESENTED FROM THE PRODUCTS OF FORMULA II: (CF DRAWING IN BOPI) IN WHICH R REPRESENTS AN ACYL RADICAL HAVING 1 TO 8 CARBON ATOMS, AS WELL AS INTERMEDIATE PRODUCTS OF THIS PROCESS.

Plant growth controlling agent and method of obtaining derivatives of 28-methylbrassinolyde

compounds and application thereof in treating cataract

本发明公开了一种化合物及其在治疗白内障中的应用。所述化合物的结构式如式Ⅰ所示。式Ⅰ所示化合物、其前药或其药学上可接受的盐可用于阻止、缓解或者逆转晶状体蛋白在细胞内的聚集；在晶状体细胞中，90％以上的蛋白组分是晶状体蛋白(crystallin，CRY)，包括α‑、β‑和γ‑CRY三个家族，而晶状体蛋白发生突变后，会引发细胞内的蛋白聚集，导致白内障疾病，本发明将选取α‑CRY家族突变体αA‑Y118D、αB‑R120G、β‑CRY家族突变体βB2‑V187E、γ‑CRY家族突变体γC‑G129C和γD‑W43R为白内障疾病的研究模型检测了本发明化合物的效果。本发明提供的具有新颖结构的小分子，与现有的小分子(如C29，Science,350,674)相比，在抑制细胞内晶状体蛋白突变导致的蛋白聚集具有更好的活性，且提高药物的可被机体吸收性，并且对正常晶状体细胞没有毒副作用。

Brassinosteroid Derivative and Plant Growth Regulator Using the Same

Disclosed is a brassinosteroid derivative represented by the formula (II): (see fig. I) and a plant growth regulator containing the brassinosteroid derivative as an active ingredient showing a persisting plant growth regulating action.

A NEW PROCESS FOR PREPARING 17BETA-SUBSTITUTED 4-AZAANDROSTAN DERIVATIVES

NOVEL 1-OXA-5alpha,17beta-DIHYDROXY-9alpha-HALO-13beta-ALKYL-17alpha-METHYL-A-NOR-10alpha-GONAN-2-ONES, AND PROCESSES FOR THEIR PREPARATION

1,274,033. 1-Oxa-A-norgonanes; de-A-gonanes. ROUSSEL-UCLAF. 9 July, 1969 [24 July, 1968], No. 30115/71. Divided out of 1,274,032. Heading C2C. Novel compounds of formula (wherein R<SP>1</SP> is C 1-3 alkyl and X is Cl or Br) are prepared from compounds of formula (wherein R<SP>5</SP> is alkyl) by reaction with HCl or HBr. 5α,17# - Dihydroxy - 5# - ethoxycarbonylmethyl - 9#,10# - epoxy - 17α - methyl - de - A- estrane (XI) is prepared from 5-pyrrolidino-17α- methyl - de - A - extra - 5(10),9(11) - dien - 17# - ol (X) by the sequence X#17#-hydroxy-17α-methylde-A-estr-9-en-5-one #9#,10#-epoxy-17#-methyl- 17#-hydroxy-de-A-estran-5-one # XI. 5 - Pyrrolidino - 13# - propyl - 17α - methyl - de- A-gona-5(10),9(11)-dien-17#-ol (XIII) is prepared from 5-pyrrolidino-13#-propyl-17#-benzoyloxyde - A - gona -5(10),9(11) - diene (XII) by the sequence XII #5-pyrrolidino-13# -propyl-de-A- gona-5(10),9(11)-dien-17#-ol#5-pyrrolidino-13#- propyl=de-A-gona-5(10 ),9(11)-dien-17-one#XIII.

Optionally 17-alkylated 2-oxa-5alpha-androstane-3beta,17beta-diols, ethers and esters thereof

2 - methyl - 7 - hydroxy - tetrahydrophenanthrene - carboxylic acid derivatives and the production thereof

17-ethers and thioethers of 4-aza-steroids.

Optical selective process synthesis method of (5R) -5-hydroxyl triptolide

本发明涉及一种(5R)‑5‑羟基雷公藤内酯醇的光学选择性工艺合成方法，具体公开一种以雷公藤内酯酮(式II化合物)作为原料，经氧化、还原得到(5R)‑5‑羟基雷公藤内酯醇(式I化合物)纯品的方法。该方法原料来源简单且稳定、后处理操作简单、易于工业化。

PROCEDURE FOR THE PREPARATION OF A 16-IMMINO 17-AZA STEROID POSSIBLY SHREDDED AND INTERMEDIATE OF SUCH PROCEDURE