BTK inhibitors

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The Merck Sharp & Dohme Corp. patent solves the following problem:

B lymphocyte activation is key to the generation of adaptive immune responses. Derailed B lymphocyte activation is a sign of many autoimmune diseases and in the modulation of the immune response and therapeutic interest. Recently the success of B cell therapy in autoimmune disease is established. Treatment of rheumatoid arthritis (RA) patients with Rituximab (anti-CD20 therapy) is an accepted clinical therapy today. More recent clinical trial studies showed that treatment with Rituximab also ameliorates symptoms of the disease in relapsing remitting multiple sclerosis (RRMS) and systemic lupus erythematosus (murder) patients. This success supports the potential for future therapies for autoimmune diseases targeted B cell immunity.

Our analysis of this patent is as follows:

Merck Sharp & Dohme Corp.’s patent US 9446130 B2 deals with BTK inhibitors.
The present invention provides Bruton's tyrosine kinase (Btk) inhibitor compounds according to Formula I or pharmaceutically acceptable salt thereof. Formula I or a pharmaceutically acceptable salt thereof or pharmaceutical compositions comprising these compounds and their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds for the treatment of Btk mediated disorder.

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Compounds

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The Glaxo Group Limited patent solves the following problem:

Syk is a non-receptor tyrosine kinase involved in coupling activated immunoreceptors signal consuming events that mediate diverse cellular responses, including proliferation, distinction, and phagocytosis. Syk is widely expressed in hematopoietic cells. Syk inhibitor with potential anti-inflammatory and immunomodulating activities. They inhibit SYK-mediated IgG Fc epsilon and gamma receptor and BCR receptor signaling, resulting in inhibition of activation of mast cells, macrophages, and B-cells and relevant inflammatory responses and tissue damage. Mast cells play a major role in type I hypersensitivity reactions associated with urticaria, bronchial asthma, anaphylaxis and other allergic conditions. Therefore, SYK inhibitor has attracted interest from a number of therapeutic areas, including the treatment of rheumatoid arthritis, B-cell lymphoma, asthma, rhinitis and cutaneous disorders such as acute and chronic urticaria, mastocytosis, cutaneous lupus , atopic dermatitis, autoimmune bullous conditions including Pemphigus and pemphigoid and other mast cell mediated skin disease.

Our analysis of this patent is as follows:

Glaxo Group Limited’s patent US 9447074 B2 deals with Compounds.
A compound of formula (I): or a salt thereof; which is an inhibitor of spleen tyrosine kinase (SYK) and therefore potential use in the treatment of diseases resulting from inappropriate activation of mast cells, macrophages, and B-cells and related inflammatory responses and tissue damage, for example inflammatory diseases and / or allergic conditions, in cancer therapy, especially heme malignancies, and autoimmune conditions.

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Substituted diazine and triazine spleen tyrosine kinease (Syk) inhibitors

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The Merck Sharp & Dohme Corp. patent solves the following problem:

Spleen Tyrosine Kinase (SYK) is a protein tyrosine kinase described as a key mediator of immunoreceptor signaling a host of inflammatory cells including mast cells, B-cells, macrophages and neutrophils. These immunoreceptors, including Fc receptor and the B-cell receptor, is important for allergic diseases, and antibody-mediated autoimmune diseases and thus pharmacologically interfering SYK conceivably treat these diseases.

Our analysis of this patent is as follows:

Merck Sharp & Dohme Corp.’s patent US 9416111 B2 deals with Substituted diazine and triazine spleen tyrosine kinease (Syk) inhibitors.
invention provides certain substituted diazine and triazine compounds of Formula (I) (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, P3, R4, rcy, CY, and t as described here. invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated spleen tyrosine kinase (SYK) kinase.

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Ingredients for inhalation and methods for making the same

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The Vectura Limited patent solves the following problem:

Our analysis of this patent is as follows:

Vectura Limited’s patent US 9381189 B2 deals with Ingredients for inhalation and methods for making the same.
A method of processing an active ingredient, the method comprising submit a pharmaceutically active substances in excipients and / or additives to compression and shearing forces. The invention also relates to compositions comprising an active prepared by the procedure.

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Aerodynamic device for the rear of a trailer

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The Trailstar International, Inc. patent solves the following problem:

The present invention relates generally to the field of aerodynamic devices to reduce drag. Particularly, the present invention relates to a flying device adapted to extend from the back of a trailer or semi-trailer container. In particular, the present invention relates to an air intake scoop and an inflatable member extending outwardly from a trailer.

Our analysis of this patent is as follows:

Trailstar International, Inc.’s patent US 9371097 B1 deals with Aerodynamic device for the rear of a trailer.
A flying device for a trailer includes an inflatable member with a back wall of a trailer adapted to inflate its rearwardly to reduce drag as the trailer pulled forwardly. The flying device further includes an air intake scoop mounted under the rear wall of the trailer in fluid communication with inflatable member filling the inflatable member in the air as the trailer moves forward.

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Processes for making lactose utilizing pre-classification techniques and pharmaceutical formulations formed therefrom

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The Dmv-Fonterra Excipients Technology Gmbh, , Glaxo Group Limited patent solves the following problem:

In the field of inhalation therapy, it is generally desirable to use therapeutic molecules having a particle size (ie, diameter) in the range of 1 to 10 m. carrier molecule or excipients, such as lactose, canine therapeutic preparation also includes significantly larger diameter particles (for example, 100 to 150 m) which are not normally penetrate into the upper respiratory tract to the same degree as the active ingredient. In general, it is better to use a smaller particle size for the lactose or a lactose blend having a defined ratio of coarse and fine lactose.

Our analysis of this patent is as follows:

Dmv-Fonterra Excipients Technology Gmbh, , Glaxo Group Limited’s patent US 9365905 B2 deals with Processes for making lactose utilizing pre-classification techniques and pharmaceutical formulations formed therefrom.
A process for forming lactose suitable for use in a pharmaceutical formulation comprises providing a plurality of lactose particles containing no more than 10% w / w of lactose particles with a number average the particle size of about 70 microns or less; stands the plurality of lactose particles to yield a plurality of milled lactose particles with an average particle size, (D50), from 50 micron to 100 micron; and classifying the plurality of milled lactose particles at least two pieces consisting of a fine particle and a coarse particle in which the fine particle has an average particle size, (D50), from 3 microns to 50 microns, and the coarse particle has an average particle size, (D50), from 40 micron to 250 micron.

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Neurogenesis screening method and uses thereof

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The Mead Johnson Nutrition Company patent solves the following problem:

The brain has only 2% of the total weight of the body, but it is a difficult organ used in 30% of calories in the day and nutrients. (Harris, JJ et al, The Energetics of CNS White Matter jour Neuroscience, January 2012: 32 (1): 356-371). The human brain and nervous system begin construction early in prenatal life and the two continue to develop until the age of three. This early development may have lifelong effects on overall brain and nervous system health. Therefore, brain nutrients become important additives in the diet of infants, children and pregnant and lactating women because of their ability to improve early brain development and the prevention and protection from brain and nervous system injury or illness. Moreover, brain nutrition is important for adults, as many nutrients to the developing nervous system to repair and provide neuroprotective benefits to health.

Our analysis of this patent is as follows:

Mead Johnson Nutrition Company’s patent US 9351978 B2 deals with Neurogenesis screening method and uses thereof.
If there are methods for detecting and / or evidence of neurogenesis effect on cholesterol and / or oxysterol using adipose-derived stem cells (ADSCs). Also given are the ways to promote neurogenesis in ADSCs. It also gives the approach to the use of cholesterol and / or production oxysterol for a neurologic component to be incorporated into a nutritional composition for increasing neurogenesis in a pediatric subject.

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Dry powder pharmaceutical composition for inhalation

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The Daiichi Sankyo Company, Limited patent solves the following problem:

Japanese Patent No. 3209946 (Patent Document 1) discloses compounds with neuraminidase inhibitory activity, including the compound represented by formula (I) shown below. The compound represented by formula (I) have excellent neuraminidase inhibitory activity and is expected to be useful as a drug for treating and preventing influenza virus infection. Japanese Patent No. 4205314 (Patent Document 2) revealed a concentration of the compound represented by formula (I) can remain on for a long time in the respiratory tissues like lung (Patent Document 2).

Our analysis of this patent is as follows:

Daiichi Sankyo Company, Limited’s patent US 9339487 B2 deals with Dry powder pharmaceutical composition for inhalation.
There was a dry powder pharmaceutical composition for inhalation is useful for preventing and / or treating influenza virus infections included as a medicinal component of a compound represented by formula (I): and optionally a compound represented by formula (II): a pharmacologically acceptable salt thereof, or a hydrate thereof.

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Aminopyrimidines as Syk inhibitors

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The Merck Sharp & Dohme Corp. patent solves the following problem:

Spleen Tyrosine Kinase (SYK) is a protein tyrosine kinase described as a key mediator of immunoreceptor signaling a host of inflammatory cells including mast cells, B-cells, macrophages and neutrophils. These immunoreceptors, including Fc receptor and the B-cell receptor, is important for allergic diseases, and antibody-mediated autoimmune diseases and thus, pharmacologically interfering with SYK conceivably treat these diseases.

Our analysis of this patent is as follows:

Merck Sharp & Dohme Corp.’s patent US 9290490 B2 deals with Aminopyrimidines as Syk inhibitors.
The present invention provides new pyrimidine amines of formula I are potent inhibitor of spleen tyrosine kinase, and is useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis and cancer.

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Process for the production of ultrapure galacto-oligosaccharides

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The Ritter Pharmaceuticals, Inc. patent solves the following problem:

Our analysis of this patent is as follows:

Ritter Pharmaceuticals, Inc.’s patent US 9200303 B2 deals with Process for the production of ultrapure galacto-oligosaccharides.
The present invention describes a process for preparing pure (95%) galacto-oligosaccharides (gos), starting from the forced low purities by the use of continuous microbiological preparations involving Saccharomyces cerevisiae and streptococcus thermophilics.

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