The present disclosure provides crystalline forms of apalutamide. Specific crystalline forms provided by the disclosure include apalutamide Form APO-I, a cocrystal solvate of apalutamide, vanillin, and n-butyl acetate; apalutamide Form APO-II, a cocrystal solvate of apalutamide, ethylvanillin, and n-butyl acetate; apalutamide Form APO-III, a cocrystal of apalutamide and 4-aminobenzoic acid; and apalutamide Form APO-IV, a cocrystal of apalutamide and vanillin. Also provided are pharmaceutical compositions including the apalutamide crystalline forms and the use of these forms in the treatment of prostate cancer, and in particular metastatic and non-metastatic castration-resistant prostate cancer.
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
The present invention provides ruxolitinib salts and crystalline forms thereof, pharmaceutical compositions including these salts and crystalline forms thereof, and the use of these salts in the treatment of acute graft versus host disease, polycythemia vera, myelofibrosis, and atopic dermatitis.
C07C 309/04 - Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing only one sulfo group
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
C07C 309/05 - Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing at least two sulfo groups bound to the carbon skeleton
Provided are solid forms of upadacitinib. Specific solid forms include an amorphous solid dispersion of upadacitinib and magnesium chloride and crystalline forms of upadacitinib incorporating magnesium chloride, magnesium acetate, magnesium orotate, magnesium fumarate, magnesium citrate, or orotic acid. Also provided are pharmaceutical compositions including the upadacitinib solid forms and the use of these forms in the treatment of rheumatoid arthritis, psoriatic arthritis, atopic dermatitis, ulcerative colitis, and/or ankylosing spondylitis.
09 - Scientific and electric apparatus and instruments
Goods & Services
Computer application software for mobile phones, portable media players, handheld tablets, and computers, namely, software for internet and/or mobile access to licensed medical content, medical calculators, healthcare news and other pharmacy management resources directed to enhance patient care and advance pharmacy practice; Computer software, namely, software applications allowing healthcare professionals, pharmacists, their assistants and sales employees to update and receive data stored in centralized databases in real time, using a mobile device or computer
The present invention provides novel crystalline forms of acalabrutinib maleate. Specific crystalline forms provided by the present invention include acalabrutinib Form APO-I, Form APO-II, and Form APO-VI, 1,2-propanediol solvates of acalabrutinib maleate; Form APO-III, a crystalline form of acalabrutinib maleate; Form APO-IV and Form APO-V, 1,2-ethanediol solvates of acalabrutinib maleate, and Form APO-VII, a 1,2,3-propanetriol of acalabrutinib maleate. Also provided are pharmaceutical compositions including the acalabrutinib maleate crystalline forms and the use of these forms in the treatment of a Bruton's Tyrosine Kinase (Btk)-mediated disorder.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Pharmaceutical preparations for the treatment of musculoskeletal diseases, disorders and injuries namely connective tissue diseases, bone diseases and osteoporosis
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
10.
SEMI-BATCH PROCESSES FOR THE CRYSTALLIZATION OF A SOLID COMPRISING AN ACTIVE PHARMACEUTICAL INGREDIENT, ITS INTERMEDIATE, OR A SALT THEREOF
The present invention provides semi-batch processes for the crystallization of a compound (an API, intermediate, or salt thereof) wherein a continuous flow suspension comprising the compound undergoes dissolution by passage through a heated tubular heat exchanger to afford a solution that is induced to crystallize in batch mode.
C07C 309/04 - Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing only one sulfo group
C07D 401/12 - 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 chain containing hetero atoms as chain links
C30B 7/14 - Single-crystal growth from solutions using solvents which are liquid at normal temperature, e.g. aqueous solutions the crystallising materials being formed by chemical reactions in the solution
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Pharmaceutical preparations for medical use, namely Nonprescription (over the counter) analgesics and antipyretics, antihistamines, anti-inflammatory agents, azole antifungals and heartburn control.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Pharmaceutical preparations for medical use, namely Nonprescription (over the counter) analgesics and antipyretics, antihistamines, anti-inflammatory agents, azole antifungals and heartburn control.
The present invention provides novel salts of viloxazine and crystalline forms thereof. Specific salts of viloxazine provided by the present invention include fumarate, hemi-DL-tartrate, naphthalene-2-sulfonate, and citrate. Also provided are pharmaceutical compositions including the viloxazine salts and crystalline forms thereof and the use of these salts in the treatment of attention-deficit hyperactivity disorder in a human subject suffering therefrom.
The present invention provides novel salts of viloxazine and crystalline forms thereof. Specific salts of viloxazine provided by the present invention include fumarate, hemi-DL-tartrate, naphthalene-2-sulfonate, and citrate. Also provided are pharmaceutical compositions comprising the viloxazine salts and crystalline forms thereof and the use of these salts in the treatment of attention- deficit hyperactivity disorder in a human subject suffering therefrom.
The present invention provides processes for the preparation of fenfluramine and salts thereof, including reductive amination of 3- (trifluoromethyl)phenylacetone, as well as products prepared by such processes.
C07C 209/28 - Preparation of compounds containing amino groups bound to a carbon skeleton by reductive alkylation of ammonia, amines or compounds having groups reducible to amino groups, with carbonyl compounds by reduction with other reducing agents
A61K 31/137 - Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine
C07C 211/29 - Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing at least one six-membered aromatic ring the carbon skeleton being further substituted by halogen atoms or by nitro or nitroso groups
The present invention provides processes for the preparation of fenfluramine and salts thereof, including reductive amination of 3-(trifluoromethyl) phenylacetone, as well as products prepared by such processes.
C07C 209/74 - Preparation of compounds containing amino groups bound to a carbon skeleton from amines, by reactions not involving amino groups, e.g. reduction of unsaturated amines, aromatisation, or substitution of the carbon skeleton by halogenation, hydrohalogenation, dehalogenation, or dehydrohalogenation
C07C 211/15 - Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton the carbon skeleton being further substituted by halogen atoms or by nitro or nitroso groups
The present invention provides solvent-limited processes for the preparation of an existing crystalline solid form of an active pharmaceutical ingredient comprising mixing, in the presence of solvent vapour, of a solid active pharmaceutical ingredient and a pharmaceutically acceptable entity that is either a high-boiling liquid or a solid. Also provided is the use of a standard rotary apparatus, such as a rotary cone dryer, for application of the processes herein.
C07D 311/30 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4 with aromatic rings attached in position 2 or 3 with aromatic rings attached in position 2 only not hydrogenated in the hetero ring, e.g. flavones
The present invention provides novel salts of belumosudil (I) and crystalline forms thereof. Specific salts of belumosudil provided by the present invention include L-malate, acesulfamate, fumarate, maleate, isethionate, malonate, edisylate, citrate, and L-tartrate. Also provided are pharmaceutical compositions comprising the belumosudil salts and crystalline forms thereof and the use of these salts in the treatment of chronic graft- versus-host disease in a subject suffering therefrom.
C07D 403/12 - 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 chain containing hetero atoms as chain links
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
C07C 309/05 - Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing at least two sulfo groups bound to the carbon skeleton
C07C 309/08 - Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing oxygen atoms bound to the carbon skeleton containing hydroxy groups bound to the carbon skeleton
Provided is a cabozantinib acesulfamate salt and a crystalline form thereof. Also provided are pharmaceutical compositions including the salt and crystalline form thereof, and methods of treatment of progressive, metastatic medullary thyroid cancer (MTC) or advanced renal cell carcinoma (RCC) that has been treated previously with anti-angiogenic therapy using the cabozantinib acesulfamate salt.
The present invention provides a novel tenofovir alafenamide acesulfamate salt, a crystalline form thereof, compositions and processes for its preparation, and its use in the treatment of a human immunodeficiency virus (HIV) infection or a hepatitis B virus (HBV) infection.
C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
A61K 31/54 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame
A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
The present invention provides novel salts of remdesivir and crystalline forms thereof. Specific salts of remdesivir provided by the present invention include napsylate, tosylate, hydrochloride, phosphate, maleate, and oxalate. Also provided are pharmaceutical compositions including the remdesivir salts and crystalline forms thereof, the use of these salts in the treatment of a viral infection, and methods of treating viral infections using the same, and in particular, a viral infection caused by Severe Acute Respiratory Syndrome coronavirus 2 (SARS-CoV-2).
C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
The present invention provides novel crystalline forms of apalutamide. Specific crystalline forms provided by the invention include apalutamide Form APO-I, a cocrystal solvate of apalutamide, vanillin, and n-butyl acetate; apalutamide Form APO-II, a cocrystal solvate of apalutamide, ethylvanillin, and n-butyl acetate; apalutamide Form APO-III, a cocrystal of apalutamide and 4-aminobenzoic acid; and apalutamide Form APO-IV, a cocrystal of apalutamide and vanillin. Also provided are pharmaceutical compositions comprising the apalutamide crystalline forms and the use of these forms in the treatment of prostate cancer, and in particular metastatic and non-metastatic castration-resistant prostate cancer.
C07D 401/04 - 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 directly linked by a ring-member-to-ring- member bond
A61K 31/196 - Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
C07C 69/14 - Acetic acid esters of monohydroxylic compounds
C07C 229/60 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton with amino and carboxyl groups bound to carbon atoms of the same non-condensed six-membered aromatic ring with amino and carboxyl groups bound in meta- or para- positions
The present invention provides novel crystalline forms of apalutamide. Specific crystalline forms provided by the invention include apalutamide Form APO-I, a cocrystal solvate of apalutamide, vanillin, and n-butyl acetate; apalutamide Form APO-II, a cocrystal solvate of apalutamide, ethylvanillin, and n-butyl acetate; apalutamide Form APO-Ill, a cocrystal of apalutamide and 4-aminobenzoic acid; and apalutamide Form APO-IV, a cocrystal of apalutamide and vanillin. Also provided are pharmaceutical compositions comprising the apalutamide crystalline forms and the use of these forms in the treatment of prostate cancer, and in particular metastatic and non-metastatic castration-resistant prostate cancer.
C07D 401/04 - 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 directly linked by a ring-member-to-ring- member bond
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
C07C 229/60 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton with amino and carboxyl groups bound to carbon atoms of the same non-condensed six-membered aromatic ring with amino and carboxyl groups bound in meta- or para- positions
26.
SALTS OF RUXOLITINIB AND CRYSTALLINE FORMS THEREOF
Sulfonate salts of ruxolitinib and crystalline forms thereof, pharmaceutical compositions comprising these salts and crystalline forms thereof, and the use of these salts in the treatment of acute graft versus host disease, polycythemia vera, myelofibrosis, and atopic dermatitis are described. The solubility of individual salt and crystalline forms of a drug substance in an aqueous environment is an important aspect of their relative bioavailability. The specific counter anions of the present invention include mesylate, edisylate, napadisylate, and acesulfamate.
A61K 31/54 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame
A61K 31/185 - AcidsAnhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
C07C 309/04 - Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing only one sulfo group
C07C 309/05 - Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing at least two sulfo groups bound to the carbon skeleton
The present invention provides ruxolitinib salts and crystalline forms thereof, pharmaceutical compositions comprising these salts and crystalline forms thereof, and the use of these salts in the treatment of acute graft versus host disease, polycythemia vera, myelofibrosis, and atopic dermatitis.
A61K 31/185 - AcidsAnhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/54 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame
A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
C07C 309/04 - Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing only one sulfo group
C07C 309/05 - Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing at least two sulfo groups bound to the carbon skeleton
The present invention provides a cabozantinib acesulfamate salt and a crystalline form thereof, pharmaceutical compositions comprising the salt and crystalline form thereof, and the use of the salt in the treatment of progressive, metastatic medullary thyroid cancer (MTC) or advanced renal cell carcinoma (RCC) that has been treated previously with anti-angiogenic therapy.
A61K 31/54 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame
The present invention provides novel salts of nintedanib and crystalline forms thereof. Specific salts of nintedanib provided by the present invention include glutarate, hippurate, levulinate, acesulfamate, diacesulfamate, and saccharinate. Also provided are pharmaceutical compositions comprising the nintedanib salts and crystalline forms thereof, and the use of these salts in the treatment or prevention of fibrotic diseases selected from the group consisting of idiopathic pulmonary fibrosis, chronic fibrosing interstitial lung disease with a progressive phenotype, and systemic sclerosis-associated interstitial lung disease.
A61K 31/428 - Thiazoles condensed with carbocyclic rings
A61K 31/54 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame
C07C 59/185 - Saturated compounds having only one carboxyl group and containing keto groups
C07C 233/81 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
C07D 275/06 - Heterocyclic compounds containing 1, 2-thiazole or hydrogenated 1,2-thiazole rings condensed with carbocyclic rings or ring systems with hetero atoms directly attached to the ring sulfur atom
The present invention provides novel crystalline forms of tenofovir alafenamide comprising tenofovir alafenamide and two different pharmaceutically acceptable acids, compositions and processes for the preparation thereof, and their use in the treatment of a human immunodeficiency virus (HIV) infection or a hepatitis B virus (HBV) infection.
C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
ABSTRACT The present invention provides novel crystalline forms of tenofovir alafenamide comprising tenofovir alafenamide and two different pharmaceutically acceptable acids, compositions and processes for the preparation thereof, and their use in the treatment of a human immunodeficiency virus (HIV) infection or a hepatitis B virus (HBV) infection. - 35 - Date Recue/Date Received 2021-01-26
C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
The present invention provides a novel crystalline form of remdesivir, remdesivir Form APO-I, including remdesivir and dimethyl sulfoxide, compositions and processes for the preparation thereof, the use of this crystalline form in the treatment of a viral infection, and methods of treating viral infections using the same, and in particular, a viral infection caused by Severe Acute Respiratory Syndrome coronavirus 2 (SARS-CoV-2).
C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
C07H 13/12 - Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by acids having the group —X—C (=X)—X—, or halides thereof, in which X means nitrogen, oxygen, sulfur, selenium, or tellurium, e.g. carbonic acid, carbamic acid
The present invention provides continuous flow processes for the preparation of the compound of Formula (2-A), an intermediate used in the preparation of zuclomiphene or a salt thereof.
C07C 37/62 - Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom of a six-membered aromatic ring by introduction of halogenPreparation of compounds having hydroxy or O-metal groups bound to a carbon atom of a six-membered aromatic ring by substitution of halogen atoms by other halogen atoms
C07C 17/263 - Preparation of halogenated hydrocarbons by reactions involving an increase in the number of carbon atoms in the skeleton by condensation reactions
C07C 37/14 - Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom of a six-membered aromatic ring by reactions increasing the number of carbon atoms by addition reactions, i.e. reactions involving at least one carbon-to-carbon unsaturated bond
39 - Transport, packaging, storage and travel services
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services
Goods & Services
retail sale and wholesale of pharmaceutical and medical supplies, namely, medications, prescription drugs and non-prescription drugs; distribution and wholesale of pharmaceutical and medical supplies, namely, medications, prescription drugs and non-prescription drugs; retail pharmacy services drug courier and delivery services, namely, the courier and delivery of pharmaceutical and medical supplies, medications and prescription drugs providing information relating to the preparation and dispensing of medications and prescription drugs; dispensing of pharmaceuticals
The present invention provides novel salts of remdesivir and crystalline forms thereof. Specific salts of remdesivir provided by the present invention include napsylate, tosylate, hydrochloride, phosphate, maleate, and oxalate. Also provided are pharmaceutical compositions including the remdesivir salts and crystalline forms thereof, the use of these salts in the treatment of a viral infection, and methods of treating viral infections using the same, and in particular, a viral infection caused by Severe Acute Respiratory Syndrome coronavirus 2 (SARS-CoV-2).
C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
A61K 31/194 - Carboxylic acids, e.g. valproic acid having two or more carboxyl groups, e.g. succinic, maleic or phthalic acid
C07C 309/30 - 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
The present invention provides novel salts of remdesivir and crystalline forms thereof. Specific salts of remdesivir provided by the present invention include napsylate, tosylate, hydrochloride, phosphate, maleate, and oxalate. Also provided are pharmaceutical compositions including the remdesivir salts and crystalline forms thereof, the use of these salts in the treatment of a viral infection, and methods of treating viral infections using the same, and in particular, a viral infection caused by Severe Acute Respiratory Syndrome coronavirus 2 (SARS-CoV-2).
C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
A61K 31/185 - AcidsAnhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
A61K 31/194 - Carboxylic acids, e.g. valproic acid having two or more carboxyl groups, e.g. succinic, maleic or phthalic acid
A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
C07C 309/30 - 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
39 - Transport, packaging, storage and travel services
40 - Treatment of materials; recycling, air and water treatment,
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services
Goods & Services
(1) Retail sale and wholesale of pharmaceutical and medical supplies, medications and prescription drugs; distribution and wholesale of pharmaceutical and medical supplies, medications and prescription drugs;
(2) Drug courier and delivery services, namely, the courier and delivery of pharmaceutical and medical supplies, medications and prescription drugs;
(3) Providing information relating to the preparation and dispensing of medications and prescription drugs.
(4) Pharmacy services; pharmacy dispensary services.
The present invention provides a novel crystalline form of remdesivir, remdesivir Form APO-I, comprising remdesivir and dimethyl sulfoxide, compositions and processes for the preparation thereof, the use of this crystalline form in the treatment of a viral infection, and methods of treating viral infections using the same, and in particular, a viral infection caused by Severe Acute Respiratory Syndrome coronavirus 2 (SARS-CoV-2).
C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
The present invention provides a novel crystalline form of remdesivir, remdesivir Form APO-I, comprising remdesivir and dimethyl sulfoxide, compositions and processes for the preparation thereof, the use of this crystalline form in the treatment of a viral infection, and methods of treating viral infections using the same, and in particular, a viral infection caused by Severe Acute Respiratory Syndrome coronavirus 2 (SARS-CoV-2).
C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
50 ABSTRACT The present invention provides novel salts of zuclomiphene and crystalline forms thereof. Specific salts of zuclomiphene provided by the present invention include sulphate, phosphate, succinate, L-tartrate, tosylate, L-malate, maleate, malonate, fumarate, glycolate and hem i-citrate. Also provided are pharmaceutical compositions comprising the zuclomiphene salts and crystalline forms thereof and the use of these salts in the treatment of a disorder selected from the group consisting of osteoporosis, bone fractures, loss of bone mineral density (BMD) and hot flashes in a subject suffering therefrom. Date Recue/Date Received 2021-03-18
C07C 217/18 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted the oxygen atom of the etherified hydroxy group being further bound to a carbon atom of a six-membered aromatic ring the six-membered aromatic ring or condensed ring system containing that ring being further substituted
A61K 31/138 - Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
A61P 15/12 - Drugs for genital or sexual disordersContraceptives for climacteric disorders
A61P 19/08 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
C07C 309/30 - 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
C01B 17/96 - Methods for the preparation of sulfates in general
The present invention provides solvent-limited processes for the preparation of an existing crystalline solid form of an active pharmaceutical ingredient comprising mixing, in the presence of solvent vapour, of a solid active pharmaceutical ingredient and a pharmaceutically acceptable entity that is either a high-boiling liquid or a solid. Also provided is the use of a standard rotary apparatus, such as a rotary cone dryer, for application of the processes herein.
A61K 9/00 - Medicinal preparations characterised by special physical form
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 31/235 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group
A61K 31/352 - 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. cannabinols, methantheline
A61K 31/455 - Nicotinic acid, i.e. niacinDerivatives thereof, e.g. esters, amides
A61K 31/4745 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/706 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
C07D 311/30 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4 with aromatic rings attached in position 2 or 3 with aromatic rings attached in position 2 only not hydrogenated in the hetero ring, e.g. flavones
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 455/06 - Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing a quinolizine ring system condensed with only one six-membered carbocyclic ring, e.g. julolidine containing benzo [a] quinolizine ring systems
The present invention provides solvent-limited processes for the preparation of an existing crystalline solid form of an active pharmaceutical ingredient comprising mixing, in the presence of solvent vapour, of a solid active pharmaceutical ingredient and a pharmaceutically acceptable entity that is either a high-boiling liquid or a solid. Also provided is the use of a standard rotary apparatus, such as a rotary cone dryer, for application of the processes herein.
A61K 9/00 - Medicinal preparations characterised by special physical form
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 31/235 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group
A61K 31/352 - 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. cannabinols, methantheline
A61K 31/455 - Nicotinic acid, i.e. niacinDerivatives thereof, e.g. esters, amides
A61K 31/4745 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/706 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
C07D 311/30 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4 with aromatic rings attached in position 2 or 3 with aromatic rings attached in position 2 only not hydrogenated in the hetero ring, e.g. flavones
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 455/06 - Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing a quinolizine ring system condensed with only one six-membered carbocyclic ring, e.g. julolidine containing benzo [a] quinolizine ring systems
The present invention provides novel crystalline forms of zuclomiphene citrate. Specific crystalline forms provided by the present invention include zuclomiphene citrate Forms APO-I, APO-II, APO-III, and APO-IV. Also provided are pharmaceutical compositions including the zuclomiphene citrate crystalline forms, processes for the preparation thereof and the use of these forms in the treatment of a disorder selected from the group including osteoporosis, bone fractures, loss of bone mineral density (BMD) and hot flashes in a subject suffering therefrom.
C07C 217/48 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated and containing rings
WIPO WORLD Digital Access Service INTELLECTUAL PROPERTY (DAS) ORGANIZATION To: jgerster@apotexpharmachem.( CERTIFICATE OF AVAILABILITY OF A CERTIFIED PATENT DOCUMENT IN A DIGITAL LIBRARY The International Bureau certifies that a copy of the patent application indicated below has been available to the WIPO Digital Access Service since the date of availability indicated, and that the patent application has been available to the indicated Office(s) as of the date specified following the relevant Office code: Document details: Country/Office: US Filing date: 22 Jan 2020 (22.01.2020) Application number: 62964354 Date of availability of document: 06 Feb 2020 (06.02.2020) The following Offices can retrieve this document by using the access code: AR, AT, AU, BE, BR, CA, CL, CN, CO, DK, EA, EE, EP, ES, FI, GB, GE, IB, IL, IN, JP, KR, MA, MX, NL, NO, NZ, SE, US Date of issue of this certificate: 15 Jan 2021 (15.01.2021) 34, chemin des Colombettes 1211 Geneva 20, Switzerland W W WAN Date Recue/Date Received 2021-01-18
C07C 217/18 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted the oxygen atom of the etherified hydroxy group being further bound to a carbon atom of a six-membered aromatic ring the six-membered aromatic ring or condensed ring system containing that ring being further substituted
A61K 31/138 - Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
A61K 31/194 - Carboxylic acids, e.g. valproic acid having two or more carboxyl groups, e.g. succinic, maleic or phthalic acid
A61P 15/12 - Drugs for genital or sexual disordersContraceptives for climacteric disorders
The present invention provides zuclomiphene salts, zuclomiphene binaphthyl hydrogen phosphate salt (1-A)·(BPA) and zuclomiphene oxalate salt (1-A)·(OXL), crystalline forms thereof and processes for the preparation thereof.
C07C 213/08 - Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions not involving the formation of amino groups, hydroxy groups or etherified or esterified hydroxy groups
C07C 51/41 - Preparation of salts of carboxylic acids by conversion of the acids or their salts into salts with the same carboxylic acid part
C07C 15/24 - Polycyclic condensed hydrocarbons containing two rings
C07C 217/54 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
The present invention provides processes for the preparation of zuclomiphene, as well as intermediates useful in the preparation thereof. In particular, processes are provided for the carbometallation of diphenylacetylene with a compound of Formula (3) to afford either zuclomiphene or an intermediate which is converted to zuclomiphene.
C07C 213/02 - Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions involving the formation of amino groups from compounds containing hydroxy groups or etherified or esterified hydroxy groups
C07C 217/60 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by singly-bound oxygen atoms linked by carbon chains having two carbon atoms between the amino groups and the six-membered aromatic ring or the condensed ring system containing that ring
52 ABSTRACT The present invention provides zuclomiphene salts, zuclomiphene binaphthyl hydrogen phosphate salt (1-A)-(BPA) and zuclomiphene oxalate salt (1-A)-(0XL), crystalline forms thereof and processes for the preparation thereof. Date Recue/Date Received 2020-11-10
C07C 217/18 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted the oxygen atom of the etherified hydroxy group being further bound to a carbon atom of a six-membered aromatic ring the six-membered aromatic ring or condensed ring system containing that ring being further substituted
C07C 213/10 - SeparationPurificationStabilisationUse of additives
C07F 9/12 - Esters of phosphoric acids with hydroxyaryl compounds
48.
PROCESSES FOR THE PREPARATION OF ZUCLOMIPHENE AND INTERMEDIATES THEREOF
ABSTRACT The present invention provides processes for the preparation of zuclomiphene, as well as intermediates useful in the preparation thereof. In particular, processes are provided for the carbometallation of diphenylacetylene with a compound of Formula (3) to afford either zuclomiphene or an intermediate which is converted to zuclomiphene. A . Mx (3) Date Recue/Date Received 2020-11-09
C07C 25/24 - Halogenated aromatic hydrocarbons with unsaturated side chains
C07C 213/08 - Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions not involving the formation of amino groups, hydroxy groups or etherified or esterified hydroxy groups
The present invention provides crystalline forms of Acalabrutinib, Specific crystalline forms provided by the present invention include Acalabrutinib Form APO-I, a co-crystal of Acalabrutinib and urea; APO-II, a co-crystal of Acalabrutinib and nicotinamide; APO-III, a co-crystal of Acalabrutinib and L-sorbitol; APO-IV, a crystalline form of Acalabrutinib; and APO-V, a co-crystal of Acalabrutinib and urea.
The present invention provides novel crystalline forms of niraparib tosylate. Specific crystalline forms provided by the present invention include niraparib tosylate Form APO-I, a co-crystal of niraparib tosylate and urea, and niraparib tosylate Form APO-II, a co-crystal of niraparib tosylate and oxalic acid. Also provided are pharmaceutical compositions including the niraparib tosylate crystalline forms, and the use of these forms in treatment or prevention of conditions which can be ameliorated by the inhibition of poly(ADP-ribose) polymerase (PARP), in particular certain forms of cancer.
C07D 401/10 - 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 aromatic rings
A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
The present invention provides novel crystalline forms of niraparib tosylate. Specific crystalline forms provided by the present invention include niraparib tosylate Form APO-I, a co-crystal of niraparib tosylate and urea, and niraparib tosylate Form APO-II, a co-crystal of niraparib tosylate and oxalic acid. Also provided are pharmaceutical compositions including the niraparib tosylate crystalline forms, and the use of these forms in treatment or prevention of conditions which can be ameliorated by the inhibition of poly(ADP-ribose) polymerase (PARP), in particular certain forms of cancer.
C07D 401/10 - 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 aromatic rings
A61K 31/454 - 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
C07C 309/30 - 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
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services
Goods & Services
(1) Providing information, advisory and consultancy services, specifically a controlled distribution program used in the prevention of fetal exposure in females treated with lenalidomide and its analogs as well as the female partners of male patients.
The present description relates to methods for physical process validation, qualification or verification. The methods are useful in a product lifecycle approach for the manufacture of physical products.
G06F 17/18 - Complex mathematical operations for evaluating statistical data
G16H 20/10 - ICT specially adapted for therapies or health-improving plans, e.g. for handling prescriptions, for steering therapy or for monitoring patient compliance relating to drugs or medications, e.g. for ensuring correct administration to patients
The present invention provides a novel crystalline form of Betrixaban maleate, Betrixaban maleate Form APO-I, comprising Betrixaban maleate and dimethyl sulfoxide, compositions and processes for the preparation thereof, and the use of this crystalline form in the treatment of conditions characterized by undesired thrombosis, and in particular, venous thromboembolism (VTE).
The present invention provides processes for the preparation of Tezacaftor, as well as intermediates useful in the preparation thereof. In particular, processes are provided for the preparation of a compound of Formula (3), and its conversion to Tezacaftor (1).
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07C 211/52 - Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having amino groups bound to only one six-membered aromatic ring the carbon skeleton being further substituted by halogen atoms or by nitro or nitroso groups
C07D 317/60 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
56.
PROCESSES FOR THE PREPARATION OF TEZACAFTOR AND INTERMEDIATES THEREOF
The present invention provides processes for the preparation of Tezacaftor, as well as intermediates useful in the preparation thereof. In particular, processes are provided for the preparation of a compound of Formula (3), and its conversion to Tezacaftor (1). (see formula 3)
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
The present invention provides a novel crystalline form of Valbenazine dibesylate, Valbenazine dibesylate Form APO-I, compositions and processes for the preparation thereof, and the use of this crystalline form in the treatment of hyperkinetic disorders, including tardive dyskinesia.
The present invention provides a novel crystalline form of Valbenazine dibesylate, Valbenazine dibesylate Form APO-I, compositions and processes for the preparation thereof, and the use of this crystalline form in the treatment of hyperkinetic disorders, including tardive dyskinesia.
A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
A61K 31/4745 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
The present invention provides novel crystalline forms of Ponatinib hydrochloride. Specific crystalline forms provided by the present invention include Ponatinib hydrochloride Form APO-I, APO-III and APO-IV, each of which is obtained from acetonitrile/formic acid solutions. Additionally, Form APO-V is provided, which is obtained from concentrated hydrochloric acid.
The present invention provides a novel crystalline form of Eluxadoline, Eluxadoline Form APO-I, a co-crystal of Eluxadoline and methyl nicotinate, compositions and processes for the preparation thereof, and the use of this crystalline form in the treatment of opioid-modulated disorders, and in particular, gastrointestinal disorders, including irritable bowel syndrome with diarrhea (IBS-D).
C07D 233/64 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
The present invention provides processes for the preparation of Acalabrutinib (1), as well as intermediates useful in the preparation thereof. In particular, processes are provided for coupling of a compound of Formula (5) and 2-butynoic acid in the presence of Carbodiimide (8) to afford Acalabrutinib (1).
The present invention provides a novel crystalline form of Ribociclib succinate, Ribociclib succinate Form APO-I, comprising Ribociclib succinate, benzyl alcohol and water, compositions thereof, processes for the preparation thereof, and the use of this crystalline form in the treatment of conditions associated with increased CDK4/6 kinase activity, and in particular, cancers, including certain forms of breast cancer.
The present invention provides a novel crystalline form of Ribociclib succinate, Ribociclib succinate Form APO-I, including Ribociclib succinate, benzyl alcohol and water, compositions thereof, processes for the preparation thereof, and the use of this crystalline form in the treatment of conditions associated with increased CDK4/6 kinase activity, and in particular, cancers, including certain forms of breast cancer.
C07D 401/14 - 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 three or more hetero rings
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
The present invention provides novel crystalline forms of lbrutinib. Specific crystalline forms provided by the present invention include lbrutinib Form APO-I, an anhydrous form; APO-II, a methyl benzoate solvate of lbrutinib; and APO-IV, a methyl salicylate solvate of lbrutinib.
The present invention provides crystalline forms of Deutetrabenazine. Specific crystalline forms provided by the present invention include Deutetrabenazine Form APO-I, a co-crystal of Deutetrabenazine and quercetin, and Deutetrabenazine Form APO-II, a co-crystal of Deutetrabenazine and luteolin. Also provided are pharmaceutical compositions including the Deutetrabenazine crystalline forms, and the use of these forms in the treatment of tardive dyskinesia and chorea associated with Huntington's disease.
A61K 31/4375 - 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 six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
A61K 31/353 - 3,4-Dihydrobenzopyrans, e.g. chroman, catechin
A61P 39/06 - Free radical scavengers or antioxidants
A61P 25/28 - 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
The present invention provides processes for the preparation of Ribociclib, as well as intermediates useful in the preparation thereof. In particular, processes are provided for the preparation of a compound of Formula (4), and its conversion to Ribociclib (1).
The present invention provides novel crystalline forms of Deutetrabenazine and Tetrabenazine. Specific crystalline forms provided by the present invention include Deutetrabenazine Form APO-I, a co-crystal of Deutetrabenazine and quercetin; Deutetrabenazine Form APO-II, a co-crystal of Deutetrabenazine and luteolin; Tetrabenazine Form APO-I, a co-crystal of Tetrabenazine and quercetin; and Tetrabenazine Form APO-II, a co-crystal of Tetrabenazine and luteolin. Also provided are pharmaceutical compositions comprising the Deutetrabenazine and Tetrabenazine crystalline forms, and the use of these forms in the treatment of tardive dyskinesia and chorea associated with Huntington's disease.
C07D 455/06 - Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing a quinolizine ring system condensed with only one six-membered carbocyclic ring, e.g. julolidine containing benzo [a] quinolizine ring systems
A61K 31/352 - 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. cannabinols, methantheline
A61K 31/4745 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
C07D 311/30 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4 with aromatic rings attached in position 2 or 3 with aromatic rings attached in position 2 only not hydrogenated in the hetero ring, e.g. flavones
77.
Processes for the preparation of Ribociclib and intermediates thereof
The present invention provides processes for the preparation of Ribociclib, as well as intermediates useful in the preparation thereof. In particular, processes are provided for the preparation of a compound of Formula (4), and its conversion to Ribociclib (1).
The present invention provides processes for the preparation of Apalutamide (1), as well as intermediates useful in the preparation thereof. In particular, the process of the invention utilizes the intermediate compound of Formula (2), wherein G is OH or a leaving group, which provides improvements over the known processes for the preparation of Apalutamide (1).
C07D 401/04 - 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 directly linked by a ring-member-to-ring- member bond
C07C 231/12 - Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
C07D 233/56 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
C07C 237/30 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having the nitrogen atom of the carboxamide group bound to hydrogen atoms or to acyclic carbon atoms
79.
PROCESSES FOR THE PREPARATION OF APALUTAMIDE AND INTERMEDIATES THEREOF
The present invention provides processes for the preparation of Apalutamide (1), as well as intermediates useful in the preparation thereof. In particular, the process of the invention utilizes the intermediate compound of Formula (2), wherein G is OH or a leaving group, which provides improvements over the known processes for the preparation of Apalutamide (1). (see above formula)
C07C 237/30 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having the nitrogen atom of the carboxamide group bound to hydrogen atoms or to acyclic carbon atoms
C07D 401/04 - 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 directly linked by a ring-member-to-ring- member bond
The present invention provides novel crystalline forms of Lesinurad, pharmaceutical compositions including these crystalline forms, and their use in the treatment of hyperuricemia associated with gout. Specific crystalline forms provided by the present invention include Lesinurad Forms APO-I, a hemi-methanolate, APO-II, a hemi-ethanolate, and APO-III, a co-crystal of Lesinurad and nicotinamide.
The present invention provides a novel crystalline form of Olaparib comprising Olaparib and benzyl alcohol, compositions thereof, and the use of this crystalline form in the treatment of cancers, such as germline BRCA-mutated (gBRCAm) advanced ovarian cancer.
C07D 403/12 - 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 chain containing hetero atoms as chain links
A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
The present invention provides a novel crystalline form of Olaparib comprising Olaparib and benzyl alcohol, compositions thereof, and the use of this crystalline form in the treatment of cancers, such as germline BRCA-mutated (gBRCAm) advanced ovarian cancer.
The present invention provides a novel crystalline form of Selexipag, Selexipag Form APO-I, which is a methanol solvate of Selexipag, compositions thereof, and the use of this crystalline form in the treatment of pulmonary arterial hypertension.
The present invention provides a novel crystalline form of Selexipag, Selexipag Form APO-1, which is a methanol solvate of Selexipag, compositions thereof, and the use of this crystalline form in the treatment of pulmonary arterial hypertension.
The invention is directed to pharmaceutical compositions such as tablets that exhibit delayed release properties when administered as either whole or half tablets. The invention is also directed to delayed release tablets comprising deferiprone for oral administration, for which twice daily administration is bioequivalent to the same daily dose of an immediate release tablet administered thrice daily. The invention is also directed to methods of making and using the same.
A61K 9/22 - Sustained or differential release type
A61K 31/4412 - Non-condensed pyridinesHydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
A61P 25/28 - 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
The present invention provides processes for the preparation of Veliparib (1), as well as intermediates useful in the preparation thereof. In particular, processes are provided for the production of the compound of Formula (3), or a salt thereof, and cyclization to afford Veliparib (1).
C07D 403/04 - 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 directly linked by a ring-member-to-ring- member bond
C07D 207/16 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
87.
PROCESSES FOR THE PREPARATION OF VELIPARIB AND INTERMEDIATES THEREOF
The present invention provides processes for the preparation of Veliparib (1), as well as intermediates useful in the preparation thereof. In particular, processes are provided for the production of the compound of Formula (3), or a salt thereof, and cyclization to afford Veliparib (1). (see formula 3)
C07D 207/16 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 403/04 - 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 directly linked by a ring-member-to-ring- member bond
The present invention provides a novel crystalline form of Lumacaftor, specifically Lumacaftor Form APO-I, a co-crystal of Lumacaftor and nicotinamide, compositions including this crystalline form, and processes for the preparation of this crystalline form.
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
The present invention provides a novel crystalline form of Lumacaftor, specifically Lumacaftor Form APO-1, a co-crystal of Lumacaftor and nicotinamide, compositions and processes for the preparation thereof, and the use of this crystalline form in the treatment of cystic fibrosis.
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
09 - Scientific and electric apparatus and instruments
35 - Advertising and business services
41 - Education, entertainment, sporting and cultural services
42 - Scientific, technological and industrial services, research and design
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services
Goods & Services
Downloadable computer application software for mobile phones, portable media players, handheld tablets, and computers, namely, software for internet and/or mobile access to medical content, medical calculators, healthcare news and other pharmacy management resources directed to enhance patient care and advance pharmacy practice; Downloadable computer software, namely, software applications allowing healthcare professionals, pharmacists, their assistants and sales employees to access medical and pharmaceutical related reference data for use in advising on drug use, drug interactions and medical counselling stored in a centralized database in real time, using a mobile computer device or computers; Downloadable electronic newsletters, in the field of patient care, medication, health, pharmaceutical, medical and clinical related questions and issues Business information services provided to the healthcare industry, namely, provision of reports, industry analysis, news and industry trends in the field of patient care, medication, medicine, healthcare and pharmacy for business purposes Providing patient education resources via a website in the nature of providing non-downloadable electronic newsletters in the field of patient care, medication, health, pharmaceutical, medical and clinical related questions and issues for patients Providing online-non-downloadable computer application software for mobile phones, portable media players, handheld tablets, and computers, namely, software for internet and/or mobile access to medical content, medical calculators, healthcare news and other pharmacy management resources directed to enhance patient care and advance pharmacy practice; Providing on-line, non-downloadable computer software, namely, software applications allowing healthcare professionals, pharmacists, their assistants and sales employees to access medical and pharmaceutical related reference data for use in advising on drug use, drug interactions and medical counselling stored in a centralized database in real time, using a mobile computer device or computers Advisory services in the nature of medical and pharmaceutical consultation in the fields of patient care, medication, health, pharmaceutical, medical and clinical related questions and issues; Digital platform in the nature of an online database of patient medical information that provides information relating to patient care, medication, medical, health, pharmaceutical and clinical related questions and issues
09 - Scientific and electric apparatus and instruments
35 - Advertising and business services
42 - Scientific, technological and industrial services, research and design
Goods & Services
Downloadable computer software, namely, software applications allowing healthcare professionals, pharmacists, their assistants and sales employees to update and receive data in the field of healthcare and pharmaceuticals stored in centralized databases in real time, using computers; none of the aforementioned goods being for quality assurance, quality control or certification purposes Business services provided to the healthcare industry, namely, provision of business information in the nature of reports, industry analysis, news and industry trends in the field of patient care, medication, medicine, healthcare and pharmacy for business purposes; none of the aforementioned services being for quality assurance, quality control or certification purposes Providing on-line, non-downloadable computer software, namely, software applications allowing healthcare professionals, pharmacists, their assistants and sales employees to update and receive data in the field of healthcare and pharmaceuticals stored in a centralized databases in real time, using a computers
09 - Scientific and electric apparatus and instruments
41 - Education, entertainment, sporting and cultural services
42 - Scientific, technological and industrial services, research and design
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services
Goods & Services
Downloadable computer application software for mobile phones, portable media players, handheld tablets, and computers, namely, software for internet and/or mobile access to medical content, medical calculators, healthcare news and other pharmacy management resources directed to enhance patient care and advance pharmacy practice; Downloadable computer software, namely, software applications allowing healthcare professionals, pharmacists, their assistants and sales employees to access medical and pharmaceutical related reference material for use in advising on drug use, drug interactions and medical counselling stored in a centralized databases in real time, using a computer or mobile computer device; Downloadable electronic newsletters, in the field of patient care, medication, health, pharmaceutical, medical and clinical related questions and issues Providing non-downloadable electronic newsletters, in the field of patient care, medication, health, pharmaceutical, medical and clinical related questions and issues Providing online-non-downloadable computer application software for mobile phones, portable media players, handheld tablets, and computers, namely, software for internet and/or mobile access to medical content, medical calculators, healthcare news and other pharmacy management resources directed to enhance patient care and advance pharmacy practice; Providing on-line, nondownloadable computer software, namely, software applications allowing healthcare professionals, pharmacists, their assistants and sales employees to access medical and pharmaceutical related reference material for use in advising on drug use, drug interactions and medical counselling stored in a centralized databases in real time, using a computer or mobile computer device Advisory services in the nature of medical and pharmaceutical consultation in the fields of patient care, medication, health, pharmaceutical, medical and clinical related questions and issues; Digital platform in the nature of an online database of patient medical information that provides information relating to patient care, medication, medical, health, pharmaceutical and clinical related questions and issues
The present invention provides a novel crystalline form of Eluxadoline, Eluxadoline Form APO-I, a co-crystal of Eluxadoline and methyl nicotinate, compositions and processes for the preparation thereof, and the use of this crystalline form in the treatment of opioid-modulated disorders, and in particular, gastrointestinal disorders, including irritable bowel syndrome with diarrhea (IBS-D).
C07D 233/64 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
The present invention provides a novel crystalline form of Eluxadoline, Eluxadoline Form APO-I, a co-crystal of Eluxadoline and methyl nicotinate, compositions and processes for the preparation thereof, and the use of this crystalline form in the treatment of opioid-modulated disorders, and in particular, gastrointestinal disorders, including irritable bowel syndrome with diarrhea (IBS-D).
C07D 233/64 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 31/417 - Imidazole-alkylamines, e.g. histamine, phentolamine
A61K 31/455 - Nicotinic acid, i.e. niacinDerivatives thereof, e.g. esters, amides
A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
A61P 25/04 - Centrally acting analgesics, e.g. opioids
The present invention provides novel crystalline forms of Acalabrutinib, Specific crystalline forms provided by the present invention include Acalabrutinib Form APO-I, a co-crystal of Acalabrutinib and urea; APO-II, a co-crystal of Acalabrutinib and nicotinamide; APO-III, a co-crystal of Acalabrutinib and L- sorbitol; APO-IV, a crystalline form of Acalabrutinib; and APO-V, a co-crystal of Acalabrutinib and urea.
The present invention provides novel crystalline forms of Acalabrutinib, Specific crystalline forms provided by the present invention include Acalabrutinib Form APO-I, a co-crystal of Acalabrutinib and urea; APO-II, a co-crystal of Acalabrutinib and nicotinamide; APO-III, a co-crystal of Acalabrutinib and L- sorbitol; APO-IV, a crystalline form of Acalabrutinib; and APO-V, a co-crystal of Acalabrutinib and urea.
The present invention provides novel crystalline forms of Ponatinib hydrochloride. Specific crystalline forms provided by the present invention include Ponatinib hydrochloride Form APO-I, APO-III and APO-IV, each of which is obtained from acetonitrile/formic acid solutions. Additionally, Form APO-V is provided, which is obtained from concentrated hydrochloric acid.
The present invention provides novel crystalline forms of Ponatinib hydrochloride. Specific crystalline forms provided by the present invention include Ponatinib hydrochloride Form APO-I, APO-III and APO-IV, each of which is obtained from acetonitrile/formic acid solutions. Additionally, Form APO-V is provided, which is obtained from concentrated hydrochloric acid.
The present invention provides processes for the preparation of Acalabrutinib (1), as well as intermediates useful in the preparation thereof. In particular, processes are provided for coupling of a compound of Formula (5) and 2-butynoic acid in the presence of Carbodiimide (8) to afford Acalabrutinib (1).
The present invention provides processes for the preparation of Acalabrutinib (1), as well as intermediates useful in the preparation thereof. In particular, processes are provided for coupling of a compound of Formula (5) and 2-butynoic acid in the presence of Carbodiimide (8) to afford Acalabrutinib (1).
