Cholesgen (Shanghai) Co.Ltd.

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IPC Class
A61P 35/00 - Antineoplastic agents 4
A61P 3/06 - Antihyperlipidemics 3
C07J 9/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane 3
A61K 31/16 - Amides, e.g. hydroxamic acids 2
A61K 31/575 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol 2
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1.

STEROID COMPOUND, AND PREPARATION METHOD THEREFOR AND USE THEREOF

      
Application Number CN2024107804
Publication Number 2025/021193
Status In Force
Filing Date 2024-07-26
Publication Date 2025-01-30
Owner CHOLESGEN (SHANGHAI) CO.LTD. (China)
Inventor
  • Liu, Jinbiao
  • Tang, Jingjie

Abstract

Disclosed in the present invention are a steroid compound, and a preparation method therefor and the use thereof. Specifically disclosed is a steroid compound having a structure as shown in formula I, etc. or a pharmaceutically acceptable salt thereof. The compound in the present invention has an SREBP pathway inhibitory activity, and can be used for preventing and/or treating diseases such as obesity, hyperlipidemia, fatty liver, diabetes, atherosclerosis, cardiovascular and cerebrovascular diseases, liver cancer and skin injuries.

IPC Classes  ?

  • C07J 9/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
  • A61K 31/58 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
  • A61P 3/06 - Antihyperlipidemics

2.

STEROID COMPOUND, PREPARATION METHOD THEREFOR AND USE THEREOF

      
Application Number CN2024107810
Publication Number 2025/021195
Status In Force
Filing Date 2024-07-26
Publication Date 2025-01-30
Owner CHOLESGEN (SHANGHAI) CO.LTD. (China)
Inventor
  • Liu, Jinbiao
  • Tang, Jingjie

Abstract

Disclosed are a steroid compound, a preparation method therefor and a use thereof. Specifically disclosed is a steroid compound having a structure as represented by formula I, II or III, or a pharmaceutically acceptable salt thereof. The compound has SREBP pathway inhibitory activity, and can be used for preventing and/or treating diseases such as obesity, hyperlipidemia, fatty liver, diabetes, atherosclerosis, cardiovascular and cerebrovascular diseases, liver cancer, and skin injury.

IPC Classes  ?

  • C07J 9/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
  • A61K 31/575 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
  • A61P 3/06 - Antihyperlipidemics
  • A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
  • A61P 35/00 - Antineoplastic agents

3.

TRICYCLIC COMPOUND, PHARMACEUTICAL COMPOSITION THEREOF AND USE THEREOF

      
Application Number CN2023141627
Publication Number 2024/140595
Status In Force
Filing Date 2023-12-25
Publication Date 2024-07-04
Owner CHOLESGEN (SHANGHAI) CO.LTD. (China)
Inventor
  • Liu, Jinbiao
  • Tang, Jingjie
  • Gao, Ang
  • Deng, Xiangjun

Abstract

Disclosed in the present invention are a tricyclic compound, a pharmaceutical composition thereof and the use thereof. Specifically, disclosed in the present invention is a compound as represented by formula (I) or a pharmaceutically acceptable salt thereof. The compound as represented by formula (I) or the pharmaceutically acceptable salt thereof has one or more of the following advantages: a good SMO inhibitory activity; a good Hh signal path inhibitory capability; and a good metabolic stability in liver microsomes.

IPC Classes  ?

  • C07C 235/30 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being unsaturated and containing rings other than six-membered aromatic rings
  • C07C 235/82 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring
  • C07C 49/737 - Unsaturated compounds containing a keto group being part of a ring containing hydroxy groups polycyclic a keto group being part of a condensed ring system having three rings
  • C07C 49/757 - Unsaturated compounds containing a keto group being part of a ring containing —CHO groups
  • C07C 59/46 - Unsaturated compounds containing hydroxy or O-metal groups containing rings other than six-membered aromatic rings
  • C07C 205/04 - Compounds containing nitro groups bound to a carbon skeleton having nitro groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing six-membered aromatic rings
  • C07C 255/60 - Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton at least one of the singly-bound nitrogen atoms being acylated
  • C07C 275/22 - Derivatives of urea, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings other than six-membered aromatic rings
  • C07C 311/08 - Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
  • C07D 209/08 - IndolesHydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
  • C07D 209/30 - IndolesHydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
  • C07D 211/26 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms
  • C07D 211/58 - Nitrogen atoms attached in position 4
  • C07D 213/38 - Radicals substituted by singly-bound nitrogen atoms having only hydrogen or hydrocarbon radicals attached to the substituent nitrogen atom
  • C07D 213/74 - Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
  • C07D 235/06 - BenzimidazolesHydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
  • C07D 237/08 - Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
  • C07D 239/26 - Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
  • C07D 239/74 - QuinazolinesHydrogenated quinazolines with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to ring carbon atoms of the hetero ring
  • C07D 249/04 - 1,2,3-TriazolesHydrogenated 1,2,3-triazoles
  • C07D 265/36 - 1,4-OxazinesHydrogenated 1,4-oxazines condensed with carbocyclic rings condensed with one six-membered ring
  • C07D 285/14 - ThiadiazolesHydrogenated thiadiazoles condensed with carbocyclic rings or ring systems
  • C07D 295/182 - Radicals derived from carboxylic acids
  • C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 471/04 - Ortho-condensed systems
  • C07D 241/12 - Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
  • A61K 31/16 - Amides, e.g. hydroxamic acids
  • A61K 31/166 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon atom of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
  • A61K 31/17 - Amides, e.g. hydroxamic acids having the group N—C(O)—N or N—C(S)—N, e.g. urea, thiourea, carmustine
  • A61K 31/18 - Sulfonamides
  • A61K 31/277 - NitrilesIsonitriles having a ring, e.g. verapamil
  • A61K 31/351 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
  • A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
  • A61K 31/403 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
  • A61K 31/4045 - Indole-alkylaminesAmides thereof, e.g. serotonin, melatonin
  • A61K 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
  • A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
  • A61K 31/4192 - 1,2,3-Triazoles
  • A61K 31/4245 - Oxadiazoles
  • A61K 31/433 - Thiadiazoles
  • A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
  • A61K 31/4402 - Non-condensed pyridinesHydrogenated derivatives thereof only substituted in position 2, e.g. pheniramine, bisacodyl
  • A61K 31/4465 - Non-condensed piperidines, e.g. piperocaine only substituted in position 4
  • A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
  • A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
  • A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
  • A61K 31/50 - PyridazinesHydrogenated pyridazines
  • A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
  • A61K 31/538 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
  • A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
  • A61K 31/5375 - 1,4-Oxazines, e.g. morpholine
  • A61P 35/00 - Antineoplastic agents

4.

STEROID COMPOUND, PREPARATION METHOD THEREFOR AND USE THEREOF

      
Application Number CN2023073237
Publication Number 2023/143400
Status In Force
Filing Date 2023-01-19
Publication Date 2023-08-03
Owner CHOLESGEN (SHANGHAI) CO.LTD. (China)
Inventor
  • Liu, Jinbiao
  • Tang, Jingjie

Abstract

Provided are a steroid compound, a preparation method therefor and a use thereof. The steroid compound may have a structure as shown in formula VI. The compound has SREBP pathway inhibitory activity, and can be used for preventing and/or treating diseases such as obesity, hyperlipidemia, fatty liver, diabetes, atherosclerosis, cardiovascular and cerebrovascular diseases, liver cancer, and skin injury.

IPC Classes  ?

  • C07J 9/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
  • C07J 31/00 - Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
  • C07J 41/00 - Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
  • A61K 31/575 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
  • A61P 3/06 - Antihyperlipidemics
  • A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
  • A61P 9/00 - Drugs for disorders of the cardiovascular system
  • A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
  • A61P 35/00 - Antineoplastic agents

5.

TRICYCLIC DITERPENE ANALOGUE, AND SYNTHESIS AND APPLICATION THEREOF

      
Application Number CN2022113625
Publication Number 2023/030043
Status In Force
Filing Date 2022-08-19
Publication Date 2023-03-09
Owner CHOLESGEN (SHANGHAI) CO.LTD. (China)
Inventor
  • Qiu, Wenwei
  • Song, Baoliang
  • He, Liming
  • Liu, Yuanbin

Abstract

Disclosed are a tricyclic diterpene analogue represented by formula (I) and a preparation method therefor. By using testosterone as a raw material, and by means of methylation, ethylene glycol protection, oxidation, Baeyer-Villiger oxidation, reduction, hydrolysis and other reactions, and passing through cyanation and a Wittig reaction to extend a carbon chain, a corresponding parent nucleus compound is obtained; and the parent core compound is subjected to amidation to obtain the tricyclic diterpene analogue. Also disclosed is an application of the tricyclic diterpene analog in inhibiting a smoothened (SMO) protein and resisting against tumors. The tricyclic diterpene analog binds to a cysteine rich domain (CRD) at an N-terminal of the SMO protein to inhibit the activity of a hedgehog (Hh) signaling pathway, which thus inhibits the growth of tumor cells and has good tumor-resisting application prospects. In addition, the present application may solve the problem of drug resistance of existing clinical SMO inhibitors, thus providing a new solution for the treatment of related diseases.

IPC Classes  ?

  • C07C 235/78 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton the carbon skeleton containing rings
  • A61P 35/00 - Antineoplastic agents
  • A61K 31/16 - Amides, e.g. hydroxamic acids
  • C07C 53/132 - Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen containing rings
  • C07C 51/16 - Preparation of carboxylic acids or their salts, halides, or anhydrides by oxidation
  • C07C 231/02 - Preparation of carboxylic acid amides from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines