HRP20200226T1 - Inhibitor glukozilceramid sintaze - Google Patents
Inhibitor glukozilceramid sintaze Download PDFInfo
- Publication number
- HRP20200226T1 HRP20200226T1 HRP20200226TT HRP20200226T HRP20200226T1 HR P20200226 T1 HRP20200226 T1 HR P20200226T1 HR P20200226T T HRP20200226T T HR P20200226TT HR P20200226 T HRP20200226 T HR P20200226T HR P20200226 T1 HRP20200226 T1 HR P20200226T1
- Authority
- HR
- Croatia
- Prior art keywords
- compound
- use according
- disease
- lysosomal
- lysosomal storage
- Prior art date
Links
- 239000003892 ceramide glucosyltransferase inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 15
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 208000015439 Lysosomal storage disease Diseases 0.000 claims 5
- 230000002132 lysosomal effect Effects 0.000 claims 5
- 102000044956 Ceramide glucosyltransferases Human genes 0.000 claims 4
- 102000004190 Enzymes Human genes 0.000 claims 4
- 108090000790 Enzymes Proteins 0.000 claims 4
- 108091000114 ceramide glucosyltransferase Proteins 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 3
- 208000035475 disorder Diseases 0.000 claims 3
- 208000015872 Gaucher disease Diseases 0.000 claims 2
- 102000004547 Glucosylceramidase Human genes 0.000 claims 2
- 108010017544 Glucosylceramidase Proteins 0.000 claims 2
- 102000005840 alpha-Galactosidase Human genes 0.000 claims 2
- 108010030291 alpha-Galactosidase Proteins 0.000 claims 2
- 208000006515 AB Variant Tay-Sachs Disease Diseases 0.000 claims 1
- 208000024720 Fabry Disease Diseases 0.000 claims 1
- 201000008892 GM1 Gangliosidosis Diseases 0.000 claims 1
- 208000037310 Gaucher disease type 2 Diseases 0.000 claims 1
- 208000037311 Gaucher disease type 3 Diseases 0.000 claims 1
- 102000016871 Hexosaminidase A Human genes 0.000 claims 1
- 108010053317 Hexosaminidase A Proteins 0.000 claims 1
- 102000016870 Hexosaminidase B Human genes 0.000 claims 1
- 108010053345 Hexosaminidase B Proteins 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 230000003197 catalytic effect Effects 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 150000002339 glycosphingolipids Chemical class 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 230000001939 inductive effect Effects 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 208000030159 metabolic disease Diseases 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 230000037361 pathway Effects 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000000758 substrate Substances 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/08—Bridged systems
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—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
- A61K31/439—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 the ring forming part of a bridged ring system, e.g. quinuclidine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—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
- A61K31/46—8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/43—Enzymes; Proenzymes; Derivatives thereof
- A61K38/46—Hydrolases (3)
- A61K38/47—Hydrolases (3) acting on glycosyl compounds (3.2), e.g. cellulases, lactases
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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- A—HUMAN NECESSITIES
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
- C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D455/00—Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine
- C07D455/02—Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing not further condensed quinolizine ring systems
-
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- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12Y—ENZYMES
- C12Y302/00—Hydrolases acting on glycosyl compounds, i.e. glycosylases (3.2)
- C12Y302/01—Glycosidases, i.e. enzymes hydrolysing O- and S-glycosyl compounds (3.2.1)
- C12Y302/01022—Alpha-galactosidase (3.2.1.22)
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- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Immunology (AREA)
- Emergency Medicine (AREA)
- Urology & Nephrology (AREA)
- Pulmonology (AREA)
- Rheumatology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Gastroenterology & Hepatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pain & Pain Management (AREA)
- Endocrinology (AREA)
- Cardiology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Psychology (AREA)
Claims (15)
1. Spoj predstavljen slijedećom strukturnom formulom,
[image]
ili njegova farmaceutski prihvatljiva sol.
2. Spoj prema patentnom zahtjevu 1, naznačen time što je za uporabu za liječenje lizosomske bolesti nakupljanja.
3. Spoj za uporabu u skladu s patentnim zahtjevom 2, naznačen time što lizosomska bolest nakupljanja nastaje kao rezultat oštećenja na putu glikosfingolipida.
4. Spoj za uporabu u skladu s patentnim zahtjevom 3, naznačen time što je lizosomska bolest nakupljanja izabrana iz skupine koja se sastoji od Gaucherove, Fabryjeve, GM1-gangliozidoze, nedostatka GM2 aktivatora, Tay-Sachs i Sandhoff.
5. Spoj za uporabu u skladu s patentnim zahtjevom 4, naznačen time što je lizosomska bolest nakupljanja Fabrijeva bolest.
6. Spoj za uporabu u skladu s patentnim zahtjevom 4, naznačen time što je lizosomska bolest nakupljanja Gaucherova bolest tip 2 ili tip 3.
7. Spoj za uporabu prema bilo kojem od patentnih zahtjeva 2 do 6, naznačen time što navedena upotreba nadalje obuhvaća korak davanja subjektu terapeutski učinkovite količine lizosomalnog enzima.
8. Spoj za uporabu u skladu s patentnim zahtjevom 7, naznačen time što je lizosomalni enzim odabran iz skupine koju čine glukocerebrozidaza, alfa-galaktozidaza A, heksosaminidaza A, heksosaminidaza B i GM1-gangliozid-β-galaktozidaza.
9. Spoj za uporabu u skladu s patentnim zahtjevom 8, naznačen time što je lizosomalni enzim alfa-galaktozidaza A.
10. Spoj za uporabu u skladu s patentnim zahtjevom 8, naznačen time što je lizosomalni enzim glukocerebrozidaza.
11. Spoj za uporabu u skladu s patentnim zahtjevom 7, naznačen time što prije tretmana subjekt ima povišene razine lizosomalnog supstrata.
12. Spoj prema patentnom zahtjevu 1 naznačen time što se upotrebljava u liječenju bolesti ili poremećaja posredovanog glukozilceramid sintazom (GCS) ili bolesti ili poremećaja u koji je uključena GCS, pri čemu je navedena bolest ili poremećaj rak ili metabolički poremećaj.
13. Postupak induciranja smanjene katalitičke aktivnosti glukozilceramid sintaze u stanici, in vitro, naznačen time što obuhvaća dovođenje u kontakt stanice s učinkovitom količinom spoja prema zahtjevu 1.
14. Farmaceutski pripravak naznačen time što sadrži spoj u skladu sa zahtjevom 1 i najmanje jedan farmaceutski prihvatljiv nosač.
15. Spoj prema patentnom zahtjevu 1, naznačen time što je za uporabu u terapiji.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161454034P | 2011-03-18 | 2011-03-18 | |
| US201261590711P | 2012-01-25 | 2012-01-25 | |
| PCT/US2012/029417 WO2012129084A2 (en) | 2011-03-18 | 2012-03-16 | Glucosylceramide synthase inhibitors |
| EP12760259.7A EP2685986B1 (en) | 2011-03-18 | 2012-03-16 | Glucosylceramide synthase inhibitor |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20200226T1 true HRP20200226T1 (hr) | 2020-05-29 |
Family
ID=46879977
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20200226TT HRP20200226T1 (hr) | 2011-03-18 | 2020-02-11 | Inhibitor glukozilceramid sintaze |
Country Status (36)
| Country | Link |
|---|---|
| US (5) | US9139580B2 (hr) |
| EP (2) | EP2685986B1 (hr) |
| JP (2) | JP6117708B2 (hr) |
| KR (1) | KR101987736B1 (hr) |
| CN (2) | CN103917094B (hr) |
| AR (1) | AR085425A1 (hr) |
| AU (2) | AU2012231275A1 (hr) |
| BR (2) | BR112013023774B1 (hr) |
| CA (1) | CA2830540C (hr) |
| CL (1) | CL2013002688A1 (hr) |
| CO (1) | CO6801749A2 (hr) |
| CR (1) | CR20190034A (hr) |
| DK (1) | DK2685986T3 (hr) |
| DO (1) | DOP2013000209A (hr) |
| EC (1) | ECSP13012978A (hr) |
| ES (1) | ES2774293T3 (hr) |
| GT (1) | GT201300215A (hr) |
| HR (1) | HRP20200226T1 (hr) |
| HU (1) | HUE047888T2 (hr) |
| IL (1) | IL228514B (hr) |
| LT (1) | LT2685986T (hr) |
| MA (1) | MA35023B1 (hr) |
| MX (3) | MX368340B (hr) |
| MY (1) | MY173998A (hr) |
| NI (1) | NI201300083A (hr) |
| PE (1) | PE20140412A1 (hr) |
| PL (1) | PL2685986T3 (hr) |
| PT (1) | PT2685986T (hr) |
| RS (1) | RS59963B1 (hr) |
| RU (2) | RU2018104472A (hr) |
| SI (1) | SI2685986T1 (hr) |
| TW (2) | TWI546301B (hr) |
| UA (1) | UA118248C2 (hr) |
| UY (1) | UY33958A (hr) |
| WO (1) | WO2012129084A2 (hr) |
| ZA (1) | ZA201307016B (hr) |
Families Citing this family (48)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL2685986T3 (pl) * | 2011-03-18 | 2020-07-27 | Genzyme Corporation | Inhibitor syntazy glukozyloceramidowej |
| MA37975B2 (fr) * | 2012-09-11 | 2021-03-31 | Genzyme Corp | Inhibiteurs de synthase de glucosylcéramide |
| AU2019222801B2 (en) * | 2012-09-11 | 2021-02-18 | Genzyme Corporation | Glucosylceramide synthase inhibitors |
| MX365464B (es) * | 2013-03-15 | 2019-06-04 | Genzyme Corp | Prodecimiento para preparar inhibidores de la glucosilceramida sintasa. |
| JO3713B1 (ar) * | 2013-03-15 | 2021-01-31 | Genzyme Corp | أشكال ملح (s)-كوينوكليدين-3-يل(2-(2-(4-فلوروفينيل)ثيازول-4-يل)بروبان-2-يل)كارباميت |
| CN104418851A (zh) * | 2013-09-02 | 2015-03-18 | 上海龙翔生物医药开发有限公司 | 奎宁环衍生物的制备方法及纯化方法 |
| CN117679415A (zh) * | 2013-12-11 | 2024-03-12 | 建新公司 | 葡糖神经酰胺合酶抑制剂 |
| JP6836502B2 (ja) * | 2014-05-30 | 2021-03-03 | スプハエラ ファーマ ピーヴィーティー リミテッド | 抗結核薬としての新規な化合物 |
| JP6749923B2 (ja) | 2015-02-02 | 2020-09-02 | ザ リージェンツ オブ ザ ユニバーシティー オブ ミシガン | グルコシルセラミドシンターゼ阻害剤及びそれを使用した治療方法 |
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