HRP20211151T1 - Kristalinska tosilatna sol pi3k delta selektivnog inhibitora za uporabu u farmaceutskim formulacijama - Google Patents
Kristalinska tosilatna sol pi3k delta selektivnog inhibitora za uporabu u farmaceutskim formulacijama Download PDFInfo
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- HRP20211151T1 HRP20211151T1 HRP20211151TT HRP20211151T HRP20211151T1 HR P20211151 T1 HRP20211151 T1 HR P20211151T1 HR P20211151T T HRP20211151T T HR P20211151TT HR P20211151 T HRP20211151 T HR P20211151T HR P20211151 T1 HRP20211151 T1 HR P20211151T1
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- 229940124639 Selective inhibitor Drugs 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000005490 tosylate group Chemical class 0.000 title 1
- 150000003839 salts Chemical class 0.000 claims 15
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 8
- 201000010099 disease Diseases 0.000 claims 5
- 206010028980 Neoplasm Diseases 0.000 claims 4
- 206010052779 Transplant rejections Diseases 0.000 claims 3
- 208000035475 disorder Diseases 0.000 claims 3
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 3
- 102000010400 1-phosphatidylinositol-3-kinase activity proteins Human genes 0.000 claims 2
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 2
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 2
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- 201000004624 Dermatitis Diseases 0.000 claims 2
- 208000035186 Hemolytic Autoimmune Anemia Diseases 0.000 claims 2
- 206010061218 Inflammation Diseases 0.000 claims 2
- 206010025323 Lymphomas Diseases 0.000 claims 2
- 108091007960 PI3Ks Proteins 0.000 claims 2
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- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 claims 1
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- JOXIMZWYDAKGHI-UHFFFAOYSA-N p-toluenesulfonic acid Substances CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 claims 1
- -1 p-toluenesulfonic acid compound Chemical class 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
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- 239000002245 particle Substances 0.000 claims 1
- 201000001976 pemphigus vulgaris Diseases 0.000 claims 1
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- 238000000634 powder X-ray diffraction Methods 0.000 claims 1
- 201000011461 pre-eclampsia Diseases 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
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- 201000000849 skin cancer Diseases 0.000 claims 1
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 1
- 210000000278 spinal cord Anatomy 0.000 claims 1
- 206010041823 squamous cell carcinoma Diseases 0.000 claims 1
- 150000003431 steroids Chemical class 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 230000009885 systemic effect Effects 0.000 claims 1
- 206010043207 temporal arteritis Diseases 0.000 claims 1
- 208000001608 teratocarcinoma Diseases 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 206010043554 thrombocytopenia Diseases 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 208000030901 thyroid gland follicular carcinoma Diseases 0.000 claims 1
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- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
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Classifications
-
- 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
- C07D487/04—Ortho-condensed systems
-
- 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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—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
- A61K31/352—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 condensed with carbocyclic rings, e.g. methantheline
-
- 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
- C07C309/01—Sulfonic acids
- C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
- C07C309/29—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
- C07C309/30—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings of six-membered aromatic rings substituted by alkyl groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Claims (9)
1. Kristalna sol spoja p-toluensulfonske kiseline
[image]
pri čemu sol pokazuje XRPD uzorak koji ima jedan ili više vrhova odabranih između 5.0, 10.1, 22.1 i 24.5 + 0.2 ° 2Θ, mjereno na X’PertPRO MPD difraktometru opremljenom Cu CFF rendgenskom cijevi; i pri čemu kristalna sol ima raspodjelu veličine čestica d (0.9) od 5 do 50 µm.
2. Sol prema zahtjevu 1, naznačena time, da sol ima d (0.5) od 1 do 10 µm.
3. Sol prema zahtjevu 1 ili zahtjevu 2, naznačena time da sol ima d (0.5) od 2 do 5 µm.
4. Sol prema bilo kojem od zahtjeva 1 do 3, naznačena time, da sol ima d (0.9) od 5 do 25 µm ili 5 do 15 µm.
5. Sol prema bilo kojem od zahtjeva 1 do 4, naznačena time, da sol ima d (0.1) od 0.5 do 1.5 µm ili 0.5 do 1.0 µm.
6. Sol prema bilo kojem od zahtjeva 1 do 5, naznačena time da sol pokazuje uzorak diferencijalnog skenirajućeg kalorimetra (DSC) s karakterističnim endotermnim vrhom na 146 ° C.
7. Farmaceutski pripravak, naznačen time, da sadrži sol prema bilo kojem od prethodnih zahtjeva i farmaceutski prihvatljiv ekscipijens.
8. Farmaceutski pripravak prema zahtjevu 7, naznačen time, da nadalje sadrži jedno ili više dodatnih terapijskih sredstava odabranih između sredstava protiv raka, protuupalnih sredstava, imunosupresiva, steroida, nesteroidnih protuupalnih sredstava, antihistaminika, analgetika i njihovih smjesa.
9. Sol prema bilo kojem od zahtjeva 1 do 6, naznačena time, da se koristi u liječenju bolesti ili poremećaja povezanih s PI3K, naznačena time što je bolest, poremećaj ili stanje povezano s PI3K bolest povezana s imunološkim sustavom, bolest ili poremećaj koji uključuje upalu, rak ili druge proliferativne bolesti, jetrenu bolest ili poremećaj ili bubrežnu bolest ili poremećaj i odabrani su između krvotvornih tumora limfoidne loze, leukemije, akutne limfocitne leukemije, akutne limfoblastne leukemije, B-staničnog limfoma, T-staničnog limfoma, Hodgkinovog limfoma, non-Hodgkinsova limfoma, limfoma dlakavih stanica i Burkettova limfoma; hematopoetskih tumora mijeloidne loze, akutne mijelogene leukemije, kronične mijelogene leukemije, mijelodisplastičnog sindroma, mijelocitne leukemije; karcinoma mokraćnog mjehura, karcinoma dojke, karcinoma debelog crijeva, karcinoma bubrega, karcinoma jetre, karcinoma pluća, karcinoma malih stanica pluća, karcinoma jednjaka, karcinoma žuči, raka jajnika, karcinoma gušterače, raka želuca, raka vrata maternice, raka štitnjače, raka prostate, raka kože, karcinoma skvamoznih stanica; tumori mezenhimskog porijekla, fibrosarkoma, rabdomiosarkoma; tumora središnjeg i perifernog živčanog sustava, astrocitoma, neuroblastoma, glioma, svannoma; melanoma, seminoma, teratokarcinoma, osteosarkoma, ksenoderoma pigmentosum, keratoktantoma, folikularni karcinom štitnjače, Kaposijev sarkom, upala, glomerulonefritis, uveitis, jetrene bolesti ili poremećaji, bubrežne bolesti ili poremećaji, kronična opstruktivna plućna bolest, reumatoidni artritis, upalni dermatitis, osteoartritis, upalna bolest mišića, alergijski rinitis, vaginitis, intersticijski cistitis, skleroderma, osteoporoza, ekcem, alogena ili ksenogena transplantacija, odbacivanje transplantata, bolest transplantata protiv domaćina, eritematozni lupus, plućna fibroza, dermatomiozitis, tiroiditis, mijasthezija autoimuna hemolitička anemija, cistična fibroza, kronični recidivirajući hepatitis, primarna bilijarna ciroza, alergijski konjunktivitis, hepatitis, atopijski dermatitis, astma, Sjogrenov sindrom, odbacivanje transplantata organa, multipla skleroza, Guillain-Barre, autoimuni uveitis, autoimuna hemolitička anemija, perniciozna anemija trombocitopenija, temporalni arteritis, antifosfolipidni sindrom, vaskulitidi poput Wegenerove granulomatoze, Behcetove bolesti, psorijaze, dermatitisa herpetiformisa, vulgarnog pemfigusa, vitiliga, Crohnove bolesti, kolitisa, ulceroznog kolitisa, primarne bilijarne imunološke ciroze, autoimunog hepatitisa tipa 1, autoimunog hepatitisa dijabetes melitus, Graveova bolest, Hashimotov tireoiditis, autoimuni ooforitis i orhitis, autoimuni poremećaj nadbubrežne žlijezde, sistemski eritematozni lupus, polimiozitis, dermatomiozitis, ankilozirajući spondilitis, odbacivanje transplantata, odbacivanje transplantata kože, artritis, bolesti kostiju povezane s povećanom resorpcijom kostiju ; ileitis, Barrettov sindrom, respiratorni distres sindrom odrasle osobe, kronična opstruktivna bolest dišnih putova; distrofija rožnice, trahom, onhocercijaza, simpatički oftalmitis, endoftalmitis; gingivitis, parodontitis; tuberkuloza; guba; uremičke komplikacije, nefroza; sklerodermatitis, psorijaza, kronične demijelinizirajuće bolesti živčanog sustava, neurodegeneracija povezana sa AIDS-om, Alzheimerova bolest, zarazni meningitis, encefalomijelitis, Parkinsonova bolest, Huntingtonova bolest, amiotrofična lateralna skleroza virusni ili autoimuni encefalitis; autoimuni poremećaji, vaskulitis imunog kompleksa, sistemski lupus i eritematode; sistemski eritemski lupus (SLE); kardiomiopatija, ishemijska bolest srca hiperkolesterolemija, ateroskleroza, preeklampsija; kronično zatajenje jetre, trauma mozga i leđne moždine i rak.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN2597CH2014 | 2014-05-27 | ||
| IN2596CH2014 | 2014-05-27 | ||
| PCT/IB2015/053940 WO2015181728A1 (en) | 2014-05-27 | 2015-05-26 | Improved forms of a pi3k delta selective inhibitor for use in pharmaceutical formulations |
| EP15733532.4A EP3149000B1 (en) | 2014-05-27 | 2015-05-26 | Crystalline tosylate salt of a pi3k delta selective inhibitor for use in pharmaceutical formulations |
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| Publication Number | Publication Date |
|---|---|
| HRP20211151T1 true HRP20211151T1 (hr) | 2021-10-15 |
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| HRP20211151TT HRP20211151T1 (hr) | 2014-05-27 | 2021-07-19 | Kristalinska tosilatna sol pi3k delta selektivnog inhibitora za uporabu u farmaceutskim formulacijama |
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| US (4) | US9969740B2 (hr) |
| EP (2) | EP3149000B1 (hr) |
| JP (3) | JP6987501B2 (hr) |
| KR (1) | KR20170007480A (hr) |
| CN (2) | CN106661030B (hr) |
| AU (1) | AU2015265542B2 (hr) |
| BR (1) | BR112016027674A2 (hr) |
| CA (1) | CA2949932C (hr) |
| CY (1) | CY1124316T1 (hr) |
| DK (1) | DK3149000T3 (hr) |
| EA (1) | EA032506B1 (hr) |
| ES (1) | ES2880999T3 (hr) |
| HR (1) | HRP20211151T1 (hr) |
| HU (1) | HUE054916T2 (hr) |
| IL (1) | IL249058B2 (hr) |
| LT (1) | LT3149000T (hr) |
| PL (1) | PL3149000T3 (hr) |
| PT (1) | PT3149000T (hr) |
| RS (1) | RS62136B1 (hr) |
| SI (1) | SI3149000T1 (hr) |
| WO (1) | WO2015181728A1 (hr) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SI3149000T1 (sl) * | 2014-05-27 | 2021-09-30 | Rhizen Pharmaceuticals S.A. | Kristalinična tosilatna sol selektivnega inhibitorja PI3K delta za uporabo v farmacevtskih oblikah |
| EA201892284A1 (ru) | 2016-05-27 | 2019-08-30 | Тг Терапьютикс, Инк. | Комбинация антитела против cd20, селективного ингибитора pi3-киназы-дельта и ингибитора btk для лечения b-клеточных пролиферативных расстройств |
| BR112019004185A2 (pt) | 2016-09-09 | 2019-09-03 | Lab Francais Du Fractionnement | combinação de um anticorpo anti-cd20, inibidor de pi3-quinase-delta inibidor e anticorpo anti-pd-1 ou anti-pd-l1 para tratamento de cânceres hematológicos |
| JP2022540466A (ja) | 2019-07-15 | 2022-09-15 | ジョンソン、マッセイ、パブリック、リミテッド、カンパニー | 非晶質ウムブラリシブモノトシレート |
| US20220143026A1 (en) | 2020-11-12 | 2022-05-12 | Tg Therapeutics, Inc. | Triple combination to treat b-cell malignancies |
| US11814439B1 (en) | 2022-06-01 | 2023-11-14 | Tg Therapeutics, Inc. | Anti-CD20 antibody compositions |
| US11884740B1 (en) | 2022-06-01 | 2024-01-30 | Tg Therapeutics, Inc. | Anti-CD20 antibody compositions |
| US11807689B1 (en) | 2022-06-01 | 2023-11-07 | Tg Therapeutics, Inc. | Anti-CD20 antibody compositions |
| US11965032B1 (en) | 2022-06-01 | 2024-04-23 | Tg Therapeutics, Inc. | Anti-CD20 antibody compositions |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| PT1939203E (pt) * | 2000-04-25 | 2015-02-04 | Icos Corp | Inibidores da isoforma delta da fosfatidil-inositol 3-quinase humana |
| TWI335821B (en) | 2002-12-16 | 2011-01-11 | Genentech Inc | Immunoglobulin variants and uses thereof |
| WO2005016348A1 (en) | 2003-08-14 | 2005-02-24 | Icos Corporation | Method of inhibiting immune responses stimulated by an endogenous factor |
| CN104042618B (zh) | 2008-11-13 | 2018-02-16 | 吉利德卡利斯托加公司 | 恶性血液病的治疗 |
| AU2010229968A1 (en) | 2009-03-24 | 2011-10-13 | Gilead Calistoga Llc | Atropisomers of2-purinyl-3-tolyl-quinazolinone derivatives and methods of use |
| EA201101507A1 (ru) | 2009-04-20 | 2012-05-30 | Гилеад Калистога Ллс. | Способы лечения солидных опухолей |
| SI2870157T1 (en) * | 2012-07-04 | 2018-02-28 | Rhizen Pharmaceuticals S.A. | SELECTIVE PI3K-DELTA INHIBITORS |
| SI3149000T1 (sl) * | 2014-05-27 | 2021-09-30 | Rhizen Pharmaceuticals S.A. | Kristalinična tosilatna sol selektivnega inhibitorja PI3K delta za uporabo v farmacevtskih oblikah |
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