Described herein are methods of treating acute heart failure in a subject in need thereof, comprising administering a therapeutically effective amount of istaroxime by intravenous infusion over a period of at least 24 hours wherein the therapeutically effective amount of istaroxime is between about 0.1 μg/kg/min and about 3.0 g/kg/min; and wherein the subject's acute heart failure is treated.
A61K 31/5685 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstane, testosterone having an oxo group in position 17, e.g. androsterone
A61K 9/00 - Medicinal preparations characterised by special physical form
A61P 9/04 - Inotropic agents, i.e. stimulants of cardiac contractionDrugs for heart failure
2.
ISTAROXIME-CONTAINING INTRAVENOUS FORMULATION FOR THE TREATMENT OF PRE-CARDIOGENIC SHOCK AND CARDIOGENIC SHOCK
Compositions for intravenous infusion of istaroxime in human patients suffering from pre-cardiogenic shock or cardiogenic shock are disclosed. Likewise, methods of administering istaroxime to individuals exhibiting symptoms of, or having been diagnosed with pre-cardiogenic shock or cardiogenic shock are disclosed. In particular, disclosed herein is a method of treating or preventing pre-cardiogenic shock or cardiogenic shock in an individual by administering to the individual a dosage regimen of istaroxime by intravenous infusion for up to 24 hours.
A61K 31/5685 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstane, testosterone having an oxo group in position 17, e.g. androsterone
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 9/04 - Inotropic agents, i.e. stimulants of cardiac contractionDrugs for heart failure
3.
ISTAROXIME-CONTAINING INTRAVENOUS FORMULATION FOR THE TREATMENT OF ACUTE HEART FAILURE (AHF)
Compositions for intravenous infusion of istaroxime, or a metabolite of istaroxime, in human patients suffering from heart failure are disclosed. Likewise, methods for extended infusion of istaroxime or its metabolites in individuals with heart failure are disclosed. In particular, some methods disclosed herein include the infusion of istaroxime, or a metabolite thereof, for a period of time that is greater than six hours in order to improve cardiac relaxation without triggering arrhythmogenic events in an individual suffering from heart failure. Other methods include administration of istaroxime until certain plasma concentration thresholds of istaroxime metabolites are achieved. Also disclosed are istaroxime metabolites with selective SERCA2a activation.
A61K 31/5685 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstane, testosterone having an oxo group in position 17, e.g. androsterone
Compounds and compositions for the activation of SERCA2a are disclosed. In particular, provided are compounds that act as predominantly pure or pure SERCA2a activators while only moderately inhibiting the Na+/K+ ATPase. In general, the disclosed compounds are derivatives of androstane having the formula (I). Also disclosed herein are pharmaceutical compositions comprising one or more of the compounds of formula (I) for use for the treatment of heart failure.
Compounds and compositions for the activation of SERCA2a are disclosed. In particular, provided are compounds that act as predominantly pure or pure SERCA2a activators while only moderately inhibiting the Na+/K+ ATPase. In general, the disclosed compounds are derivatives of androstane having the formula (I). Also disclosed herein are pharmaceutical compositions comprising one or more of the compounds of formula (I) for use for the treatment of heart failure.
C07J 1/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, not substituted in position 17 beta by a carbon atom, e.g. oestrane, androstane
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
5.
INTRAVENOUS ISTAROXIME FOR THE TREATMENT OF ACUTE HEART FAILURE
Described herein are methods of treating acute heart failure in a subject in need thereof, comprising administering a therapeutically effective amount of istaroxime by intravenous infusion over a period of at least 24 hours wherein the therapeutically effective amount of istaroxime is between about 0.1 μg/kg/min and about 3.0 μg/kg/min; and wherein the subject's acute heart failure is treated.
A61K 31/5685 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstane, testosterone having an oxo group in position 17, e.g. androsterone
A61K 9/00 - Medicinal preparations characterised by special physical form
A61P 9/04 - Inotropic agents, i.e. stimulants of cardiac contractionDrugs for heart failure
6.
INHIBITORS OF ATYPICAL PROTEIN KINASE C AND THEIR USE IN TREATING HEDGEHOG PATHWAY-DEPENDENT CANCERS
Methods for treating hedgehog pathway-dependent cancers are provided. Aspects of the methods include the inhibition of hedgehog pathway-dependent cancer growth, proliferation, or metastasis that is promoted by hedgehog pathway signaling. In particular, methods of treating hedgehog pathway-dependent cancers with inhibitors of atypical protein kinase C iota are disclosed.
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
Compositions for intravenous infusion of istaroxime, or a metabolite of istaroxime, in human patients suffering from heart failure are disclosed. Likewise, methods for extended infusion of istaroxime or its metabolites in individuals with heart failure are disclosed. In particular, some methods disclosed herein include the infusion of istaroxime, or a metabolite thereof, for a period of time that is greater than six hours in order to improve cardiac relaxation without triggering arrhythmogenic events in an individual suffering from heart failure. Other methods include administration of istaroxime until certain plasma concentration thresholds of istaroxime metabolites are achieved. Also disclosed are istaroxime metabolites with selective SERCA2a activation.
A61K 31/5685 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstane, testosterone having an oxo group in position 17, e.g. androsterone
Compositions for intravenous infusion of istaroxime, or a metabolite of istaroxime, in human patients suffering from heart failure are disclosed. Likewise, methods for extended infusion of istaroxime or its metabolites in individuals with heart failure are disclosed. In particular, some methods disclosed herein include the infusion of istaroxime, or a metabolite thereof, for a period of time that is greater than six hours in order to improve cardiac relaxation without triggering arrhythmogenic events in an individual suffering from heart failure. Other methods include administration of istaroxime until certain plasma concentration thresholds of istaroxime metabolites are achieved. Also disclosed are istaroxime metabolites with selective SERCA2a activation.
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
A61K 31/5685 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstane, testosterone having an oxo group in position 17, e.g. androsterone
Compounds and compositions for the activation of SERCA2a are disclosed. In particular, provided are compounds that act as predominantly pure or pure SERCA2a activators while only moderately inhibiting the Na+/K+ ATPase. In general, the disclosed compounds are derivatives of androstane having the formula (I). Also disclosed herein are pharmaceutical compositions comprising one or more of the compounds of formula (I) for use for the treatment of heart failure.
C07J 43/00 - Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta[a]hydrophenanthrene skeleton
A61K 31/566 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol having an oxo group in position 17, e.g. oestrone
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 9/04 - Inotropic agents, i.e. stimulants of cardiac contractionDrugs for heart failure
C07J 1/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, not substituted in position 17 beta by a carbon atom, e.g. oestrane, androstane
C07J 41/00 - Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
C07J 21/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, having an oxygen-containing hetero ring spiro-condensed with the cyclopenta[a]hydrophenanthrene skeleton
C07J 51/00 - Normal steroids with unmodified cyclopenta[a]hydrophenanthrene skeleton not provided for in groups
10.
ANDROSTANE DERIVATIVES WITH ACTIVITY AS PURE OR PREDOMINANTLY PURE STIMULATORS OF SERCA2a FOR THE TREATMENT OF HEART FAILURE
Compounds and compositions for the activation of SERCA2a are disclosed. In particular, provided are compounds that act as predominantly pure or pure SERCA2a activators while only moderately inhibiting the Na+/K+ ATPase. In general, the disclosed compounds are derivatives of androstane having the formula (I). Also disclosed herein are pharmaceutical compositions comprising one or more of the compounds of formula (I) for use for the treatment of heart failure.
C07J 1/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, not substituted in position 17 beta by a carbon atom, e.g. oestrane, androstane
C07J 41/00 - Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
C07J 43/00 - Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta[a]hydrophenanthrene skeleton
A61K 31/566 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol having an oxo group in position 17, e.g. oestrone
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 9/04 - Inotropic agents, i.e. stimulants of cardiac contractionDrugs for heart failure
C07J 21/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, having an oxygen-containing hetero ring spiro-condensed with the cyclopenta[a]hydrophenanthrene skeleton
C07J 51/00 - Normal steroids with unmodified cyclopenta[a]hydrophenanthrene skeleton not provided for in groups
11.
ISTAROXIME-CONTAINING INTRAVENOUS FORMULATION FOR THE TREATMENT OF ACUTE HEART FAILURE (AHF)
(12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) CORRECTED VERSION (19) World Intellectual Property Organization I II 111E31E11 111111 11111 1 11111111 110111110111 11111 1111 1 11111E11 1111 11111111111 1111 11 11 International Bureau (10) International Publication Number (43) International Publication Date WO 2020/180356 A9 September 2020 (10.09.2020) WIIIPO PCT (51) International Patent Classification: Milano (IT). BARRASSI, Paolo; Via Campagnetta 6/B, A 61K 31/5685 (2006.01) A 61P 9/00 (2006.01) 21010 Castelveccana (VA) (IT). A 61K 45/06 (2006.01) A 61P 9/04 (2006. 01) (74) Agent: REED, Janet E. et al.; Potter Anderson and Cor- (21) International Application Number: roon LLP, 1313 N. Market Street, Wilmington, Delaware PCT/US2019/060961 19801 (US). (22) International Filing Date: (81) Designated States (unless otherwise indicated, for every 12 November 2019 (12.11.2019) kind of national protection available): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, (25) Filing Language: English CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, (26) Publication Language: English DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, IID, EL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, (30) Prio rity Data: KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, 62/814,149 05 March 2019 (05.03.2019) .. US MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, (71) Applicant: WINDTREE THERAPEUTICS, INC. OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, [US/US]; 2600 Kelly Road, Warrington, Pennsylvania SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, 18976 (US). TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (72) Inventors: BIANCHI, Giuseppe; Piazza Adigrat 4, 20133 (84) Designated States (unless otherwise indicated, for every Milano (IT). FERRARI, Patrizia; Gasparotto 57A, 21100 kind of regional protection available): ARIPO (BW, GH, Varese (IT). FERRANDI, Mara; Via Cenisio 34, 20100 GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, - (54) Title: ISTAROXIME-CONTAINING INTRAVENOUS FORMULATION FOR THE TREATMENT OF ACUTE HEART - FAILURE (AHF) 1 - 0 =!-- = T j0001000.H__ 74 -2 placebo E -3 - Istar 0.5 pg/kg/rnin pØ003 L)c- - !star 1.0 pg/kg/min p=0.014 -5 - = -A- Mar 1.S mg/kg/min -6 - p=0.001 0 2 4 6 8 Time (h) FIG. 1 = (57) Abstract: Compositions for intravenous infusion of istaroxime, or a metabolite of istaroxime, in human patients suffering from GO heart failure are disclosed. Likewise, methods for extended infusion of istaroxime or its metabolites in individuals with heart failure are 11 disclosed. In particular, some methods disclosed herein include the infusion of istaroxime, or a metabolite thereof, for a period of time el-a--) that is greater than six hours in order to improve cardiac relaxation without triggering arrhythmogenic events in an individual suffering = from heart failure. Other methods include administration of istaroxime until certain plasma concentration thresholds of istaroxime el metabolites are achieved. Also disclosed are istaroxime metabolites with selective SERCA2a activation. [Continued on next page] Date Recue/Date Received 2021-08-12 CA 03130261 2021-08-13 WO 2020/180356 A9 11111 11111111111111111111111111 11111 11 II II 111 01111110 11111 111111111 I 0E11E111 11111111 UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, Iva, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). Published: ¨ with international search report (Art. 21(3)) ¨ with information concerning authorization of rectification ()fan obvious mistake under Rule 91.3 (1)) (Rule 48.2(i)) (48) Date of publication of this corrected version: 12 November 2020 (12.11.2020) (15) Information about Correction: see Notice of 12 November 2020 (12 11.2020) Date Recue/Date Received 2021-08-12
C07J 1/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, not substituted in position 17 beta by a carbon atom, e.g. oestrane, androstane
A61K 31/5685 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstane, testosterone having an oxo group in position 17, e.g. androsterone
A61P 9/04 - Inotropic agents, i.e. stimulants of cardiac contractionDrugs for heart failure
12.
ISTAROXIME-CONTAINING INTRAVENOUS FORMULATION FOR THE TREATMENT OF ACUTE HEART FAILURE (AHF)
Compositions for intravenous infusion of istaroxime, or a metabolite of istaroxime, in human patients suffering from heart failure are disclosed. Likewise, methods for extended infusion of istaroxime or its metabolites in individuals with heart failure are disclosed. In particular, some methods disclosed herein include the infusion of istaroxime, or a metabolite thereof, for a period of time that is greater than six hours in order to improve cardiac relaxation without triggering arrhythmogenic events in an individual suffering from heart failure. Other methods include administration of istaroxime until certain plasma concentration thresholds of istaroxime metabolites are achieved. Also disclosed are istaroxime metabolites with selective SERCA2a activation.
A61K 31/5685 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstane, testosterone having an oxo group in position 17, e.g. androsterone
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 9/00 - Drugs for disorders of the cardiovascular system
A61P 9/04 - Inotropic agents, i.e. stimulants of cardiac contractionDrugs for heart failure
13.
Thienopyrimidine inhibitors of atypical protein kinase C
The present application provides a compound of formula (I)
6, A, G, M, Q and X are as defined herein. A compound of formula (I) and its salts have a PKC inhibitory activity, and may be used to treat proliferative disorders.
C07F 7/08 - Compounds having one or more C—Si linkages
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
14.
Thienopyrimidine inhibitors of atypical protein kinase C
The present application provides a compound of formula (I)
6, A, G, M, Q and X are as defined herein. A compound of formula (I) and its salts have aPKC inhibitory activity, and may be used to treat proliferative disorders.
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
C07F 7/08 - Compounds having one or more C—Si linkages
A61P 35/02 - Antineoplastic agents specific for leukemia
A61P 35/04 - Antineoplastic agents specific for metastasis
05 - Pharmaceutical, veterinary and sanitary products
10 - Medical apparatus and instruments
42 - Scientific, technological and industrial services, research and design
Goods & Services
Pharmaceutical preparations and substances for treatment of upper and lower respiratory diseases and disorders; Pharmaceutical preparations, namely, synthetic pulmonary surfactants for treatment of respiratory conditions Medical device, namely, a device for improving delivery of liquid, powder or aerosolized pharmaceutical preparations and substances; Medical device, namely, a device for improving delivery of liquid, powder or aerosolized pharmaceutical preparations and substances for treatment of various medical conditions; Medical device, namely, an adapter for facilitating entrainment of liquid, powder or aerosolized pharmaceutical preparations and substances; aerosol dispensers for medical use not filled with pharmaceuticals; medical apparatus which uses heat to generate aerosolized pharmaceutical preparations and substances which is then delivered to patients Pharmaceutical research, drug discovery, and drug development services; medical and scientific research in the field of pulmonary diseases; research and development of pharmaceutical preparations for the treatment of pulmonary diseases and disorders; research and development of pharmaceutical preparations and substances for treatment of respiratory conditions; research and development of new products in the field of surfactant replacement therapies for respiratory diseases; research and development of pharmaceutical preparations, namely, pulmonary lung surfactants; pharmaceutical research and development in the field of inhaled pharmaceutical products for all human respiratory indications; research and development services in the field of medical apparatus, appliances and instruments for producing and/or delivering aerosolized pharmaceutical preparations; providing scientific information about pharmaceutical products and services; providing scientific information about pharmaceutical products and services via a website and other forms of media
05 - Pharmaceutical, veterinary and sanitary products
10 - Medical apparatus and instruments
42 - Scientific, technological and industrial services, research and design
Goods & Services
Pharmaceutical preparations and substances for treatment of upper and lower respiratory diseases and disorders; Pharmaceutical preparations, namely, synthetic pulmonary surfactants for treatment of respiratory conditions Medical device, namely, a device for improving delivery of liquid, powder or aerosolized pharmaceutical preparations and substances; Medical device, namely, a device for improving delivery of liquid, powder or aerosolized pharmaceutical preparations and substances for treatment of various medical conditions; Medical device, namely, an adapter for facilitating entrainment of liquid, powder or aerosolized pharmaceutical preparations and substances; aerosol dispensers for medical use not filled with pharmaceuticals; medical apparatus which uses heat to generate aerosolized pharmaceutical preparations and substances which is then delivered to patients Pharmaceutical research, drug discovery, and drug development services; medical and scientific research in the field of pulmonary diseases; research and development of pharmaceutical preparations for the treatment of pulmonary diseases and disorders; research and development of pharmaceutical preparations and substances for treatment of respiratory conditions; research and development of new products in the field of surfactant replacement therapies for respiratory diseases; research and development of pharmaceutical preparations, namely, pulmonary lung surfactants; pharmaceutical research and development in the field of inhaled pharmaceutical products for all human respiratory indications; research and development services in the field of medical apparatus, appliances and instruments for producing and/or delivering aerosolized pharmaceutical preparations; providing scientific information about pharmaceutical products and services; providing scientific information about pharmaceutical products and services via a website and other forms of media
17.
Azaquinazoline inhibitors of atypical protein kinase C
The present application provides a compound of formula (I)
9, G, and X are as defined herein. This application further describes compositions comprising the same. Compounds of formula (I) and their salts have aPKC inhibitory activity, and may be used to treat proliferative diseases.
A61K 31/407 - 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 heterocyclic ring systems, e.g. ketorolac, physostigmine
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
C07F 9/6584 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms having one phosphorus atom as ring hetero atom
Lyophilized pulmonary surfactants having an increased specific surface area and porosity are described. Methods of making the lyophilized pulmonary surfactants are also described.
A61K 31/685 - Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols one of the hydroxy compounds having nitrogen atoms, e.g. phosphatidylserine, lecithin
A61K 31/20 - Carboxylic acids, e.g. valproic acid having a carboxyl group bound to an acyclic chain of seven or more carbon atoms, e.g. stearic, palmitic or arachidic acid
A61K 31/683 - Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 31/661 - Phosphorus acids or esters thereof not having P—C bonds, e.g. fosfosal, dichlorvos, malathion
F26B 5/06 - Drying solid materials or objects by processes not involving the application of heat by evaporation or sublimation of moisture under reduced pressure, e.g. in a vacuum the process involving freezing
20.
Azaquinazoline inhibitors of atypical protein kinase C
The present application provides a compound of formula (I)
1, G, and X are as defined herein. A compound of formula (I) and/or its salts have aPKC inhibitory activity, and may be used to treat proliferative disorders. Compositions comprising a compound of Formula (I) and/or a salt thereof are also provided.
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
A61P 35/02 - Antineoplastic agents specific for leukemia
A61P 35/04 - Antineoplastic agents specific for metastasis
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
05 - Pharmaceutical, veterinary and sanitary products
10 - Medical apparatus and instruments
Goods & Services
(1) Pharmaceutical preparations and substances for treatment of respiratory conditions; Medical device, namely, a device which uses heat to generate aerosolized pharmaceutical preparations and substances for delivery to patients; a medical device, namely, a pump and a capillary tube to generate aerosolized pharmaceutical preparations and substances; an aerosol delivery system for medical use comprised of a base unit serving as a reusable aerosol control unit and a disposable aerosol delivery pack, a container for pharmaceuticals sold empty, ventilation tubing and a capillary tube; aerosol dispensers for medical use not filled with pharmaceuticals
(2) Medical device, namely, a device which uses heat to generate aerosolized pharmaceutical preparations and substances for delivery to patients; a medical device, namely, a pump and a capillary tube to generate aerosolized pharmaceutical preparations and substances; an aerosol delivery system for medical use comprised of a base unit serving as a reusable aerosol control unit and a disposable aerosol delivery pack, a container for pharmaceuticals sold empty, ventilation tubing and a capillary tube; aerosol dispensers for medical use not filled with pharmaceuticals
(3) Pharmaceutical preparations and substances for treatment of respiratory conditions
22.
Thienopyrimidine inhibitors of atypical protein kinase C
The present application provides a compound of formula (I)
6, A, G, M, Q and X are as defined herein. A compound of formula (I) and its salts have aPKC inhibitory activity, and may be used to treat proliferative disorders.
An adaptor for delivering an aerosolized active agent to a patient with concomitant positive pressure ventilation includes an aerosol flow channel having an aerosol inlet port and a patient interface port, and defining an aerosol flow path from the aerosol inlet port to and through the patient interface port; and a ventilation gas flow channel in fluid communication with the aerosol flow channel and having a gas inlet port and a gas outlet port, and defining a ventilation gas flow path from the gas inlet port to and through the gas outlet port, wherein the ventilation gas flow path is at least partially offset from the aerosol flow path and at least partially encircles the aerosol flow path. Systems and methods for delivering an aerosolized active agent to a patient with concomitant positive pressure ventilation incorporate the adaptor.
The present application provides azaquinazoline compounds as defined herein. This application further describes compositions comprising the same. These azaquinazoline compounds and their salts have atypical protein kinase C (“aPKC”) inhibitory activity, and may be used to treat proliferative disorders.
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
C07F 9/6584 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms having one phosphorus atom as ring hetero atom
25.
Lyophilization of synthetic liposomal pulmonary surfactant
Lyophilized pulmonary surfactants having an increased specific surface area and porosity are described. A method of making lyophilized pulmonary surfactants is described.
A61K 31/685 - Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols one of the hydroxy compounds having nitrogen atoms, e.g. phosphatidylserine, lecithin
A61K 31/20 - Carboxylic acids, e.g. valproic acid having a carboxyl group bound to an acyclic chain of seven or more carbon atoms, e.g. stearic, palmitic or arachidic acid
A61K 31/683 - Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
26.
Lyophilization of synthetic liposomal pulmonary surfactant
Lyophilized pulmonary surfactants having an increased specific surface area and porosity are described. Methods of making the lyophilized pulmonary surfactants are also described.
A61K 31/685 - Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols one of the hydroxy compounds having nitrogen atoms, e.g. phosphatidylserine, lecithin
A61K 31/20 - Carboxylic acids, e.g. valproic acid having a carboxyl group bound to an acyclic chain of seven or more carbon atoms, e.g. stearic, palmitic or arachidic acid
A61K 31/683 - Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
Medical device, namely, a device which uses heat to generate aerosolized pharmaceutical preparations and substances for delivery to patients; a medical device, namely, a pump and a capillary tube to generate aerosolized pharmaceutical preparations and substances; an aerosol delivery system for medical use comprised of a base unit serving as a reusable aerosol control unit and a disposable aerosol delivery pack, a container for pharmaceuticals sold empty, ventilation tubing and a capillary tube; aerosol dispensers for medical use not filled with pharmaceuticals
Medical device, namely, a device for improving delivery of liquid, powder or aerosolized pharmaceutical preparations and substances, a device for improving delivery of liquid, powder or aerosolized pharmaceutical preparations and substances for treatment of various medical conditions, an adapter for facilitating entrainment of liquid, powder or aerosolized pharmaceutical preparations and substances; medical apparatus for facilitating the inhalation of pharmaceutical preparations; medical ventilator tubing and tubing connectors
29.
Ventilation circuit adaptor and proximal aerosol delivery system
An adaptor for delivering an aerosolized active agent to a patient with concomitant positive pressure ventilation includes an aerosol flow channel having an aerosol inlet port and a patient interface port, and defining an aerosol flow path from the aerosol inlet port to and through the patient interface port; and a ventilation gas flow channel in fluid communication with the aerosol flow channel and having a gas inlet port and a gas outlet port, and defining a ventilation gas flow path from the gas inlet port to and through the gas outlet port, wherein the ventilation gas flow path is at least partially offset from the aerosol flow path and at least partially encircles the aerosol flow path. Systems and methods for delivering an aerosolized active agent to a patient with concomitant positive pressure ventilation incorporate the adaptor.
Medical devices, namely, a device for improving delivery of
liquid, powder or aerosolized pharmaceutical preparations
and substances, a device for improving delivery of liquid,
powder or aerosolized pharmaceutical preparations and
substances for treatment of various medical conditions, an
adapter for facilitating entrainment of liquid, powder or
aerosolized pharmaceutical preparations and substances.
Medical device, namely, a device for improving delivery of liquid, powder or aerosolized pharmaceutical preparations and substances, a device for improving delivery of liquid, powder or aerosolized pharmaceutical preparations and substances for treatment of various medical conditions, an adapter for facilitating entrainment of liquid, powder or aerosolized pharmaceutical preparations and substances
32.
Ventilation circuit adaptor and proximal aerosol delivery system
An adaptor for delivering an aerosolized active agent to a patient with concomitant positive pressure ventilation includes an aerosol flow channel having an aerosol inlet port and a patient interface port, and defining an aerosol flow path from the aerosol inlet port to and through the patient interface port; and a ventilation gas flow channel in fluid communication with the aerosol flow channel and having a gas inlet port and a gas outlet port, and defining a ventilation gas flow path from the gas inlet port to and through the gas outlet port, wherein the ventilation gas flow path is at least partially offset from the aerosol flow path and at least partially encircles the aerosol flow path. Systems and methods for delivering an aerosolized active agent to a patient with concomitant positive pressure ventilation incorporate the adaptor.
Methods and compositions to enhance mucus clearance and to treat pulmonary lung disorders such as cystic fibrosis are disclosed. The methods utilize compositions including synthetic pulmonary surfactants having one or more phospholipids and a synthetic polypeptide, administered alone or combined with hyperosmotic agents, to patients in an amount effective to enhance mucus clearance.
Regimens for the therapeutic or prophylactic administration of pulmonary surfactant to infants exhibiting or at risk of developing bronchopulmonary dysplasia are disclosed.
A01N 37/18 - Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids containing the group —CO—N, e.g. carboxylic acid amides or imidesThio-analogues thereof
