C07C229/42

OPHTHALMIC COMPOSITIONS AND METHODS FOR THE TREATMENT OF EYE DISORDERS AND SKIN DISEASES
20210188817 · 2021-06-24 · ·

The invention relates to the compounds or its pharmaceutical acceptable polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, formula II, formula III, formula IV, formula V and formula VI and the methods for the treatment of eye disorders and skin diseases and may be formulated for the topical eye drop, topical paste, ocular solution, device-drug delivery, oral, buccal, rectal, topical, transdermal, transmucosal, lozenge, spray, intravenous, oral solution, nasal spray, oral solution, cream, dermal ointment, gels, lotions, suspension, oral spray, buccal mucosal layer tablet, parenteral administration, syrup, or injection. Such compositions may be used to treatment of skin diseases such as acne, rosacea and eye disorders such as ocular redness, glaucoma, presbyopia, IOP, cataract, dry eye and oGVHD.

OPHTHALMIC COMPOSITIONS AND METHODS FOR THE TREATMENT OF EYE DISORDERS AND SKIN DISEASES
20210188817 · 2021-06-24 · ·

The invention relates to the compounds or its pharmaceutical acceptable polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, formula II, formula III, formula IV, formula V and formula VI and the methods for the treatment of eye disorders and skin diseases and may be formulated for the topical eye drop, topical paste, ocular solution, device-drug delivery, oral, buccal, rectal, topical, transdermal, transmucosal, lozenge, spray, intravenous, oral solution, nasal spray, oral solution, cream, dermal ointment, gels, lotions, suspension, oral spray, buccal mucosal layer tablet, parenteral administration, syrup, or injection. Such compositions may be used to treatment of skin diseases such as acne, rosacea and eye disorders such as ocular redness, glaucoma, presbyopia, IOP, cataract, dry eye and oGVHD.

NOVEL PHENOXUACETIC ACID DERIVATIVE, PREPARATION METHOD THEREFOR AND USES OF DERIVATIVE AS DRUG
20210122704 · 2021-04-29 ·

The present invention relates to a novel phenoxyacetic acid derivative represented by the general formula (I), preparation method thereof and use of a pharmaceutical composition containing the derivative in preparing a medicament for treating diabetes and metabolic syndrome. The phenoxyacetic acid derivatives have excellent in vivo hypoglycemic activity, which can be used for preventing or treating diabetes.

NOVEL PHENOXUACETIC ACID DERIVATIVE, PREPARATION METHOD THEREFOR AND USES OF DERIVATIVE AS DRUG
20210122704 · 2021-04-29 ·

The present invention relates to a novel phenoxyacetic acid derivative represented by the general formula (I), preparation method thereof and use of a pharmaceutical composition containing the derivative in preparing a medicament for treating diabetes and metabolic syndrome. The phenoxyacetic acid derivatives have excellent in vivo hypoglycemic activity, which can be used for preventing or treating diabetes.

Direct C—H amination and aza-annulation

In some aspects, the present disclosure provides methods of aminating an aromatic compound comprising reacting an aminating agent with an aromatic compound in the presence of a rhodium catalyst. In some embodiments, the methods may comprise aminating an aromatic compound which contains multiple different functional groups. The methods described herein may also be used to create bicyclic system comprising reacting an intramolecular aminating agent with an aromatic ring to obtain a second ring containing a nitrogen atom. In another aspect, the methods described herein may also be used to create a cyclic aliphatic cyclic/poly cyclic amine system comprising a reacting an intramolecular aminating agent by insertion into a C(sp3)-H bond.

Direct C—H amination and aza-annulation

In some aspects, the present disclosure provides methods of aminating an aromatic compound comprising reacting an aminating agent with an aromatic compound in the presence of a rhodium catalyst. In some embodiments, the methods may comprise aminating an aromatic compound which contains multiple different functional groups. The methods described herein may also be used to create bicyclic system comprising reacting an intramolecular aminating agent with an aromatic ring to obtain a second ring containing a nitrogen atom. In another aspect, the methods described herein may also be used to create a cyclic aliphatic cyclic/poly cyclic amine system comprising a reacting an intramolecular aminating agent by insertion into a C(sp3)-H bond.

Cyclohexyl GPR40 agonists for the treatment of type II diabetes

Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR40 receptor. Such compounds are represented by Formula (I) as follows: ##STR00001## wherein R.sup.1, R.sup.2, R.sup.3, A, W, L, R.sub.a, and G are defined herein:
and by Formula (II) as follows: ##STR00002##
wherein R.sup.1B, W.sub.B, L.sub.B, custom character, and G.sub.B are defined herein.

Cyclohexyl GPR40 agonists for the treatment of type II diabetes

Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR40 receptor. Such compounds are represented by Formula (I) as follows: ##STR00001## wherein R.sup.1, R.sup.2, R.sup.3, A, W, L, R.sub.a, and G are defined herein:
and by Formula (II) as follows: ##STR00002##
wherein R.sup.1B, W.sub.B, L.sub.B, custom character, and G.sub.B are defined herein.

Augmenting Moieties for Anti-Inflammatory Compounds

Augmented or synergized anti-inflammatory constructs are disclosed including anti-inflammatory terpenes and/or vanilloids covalently conjugated to one another so that the activity of the conjugate is greater than the sum of its parts. Also disclosed are methods of improving the potency of an anti-inflammatory terpene or vanilloid by linking it to another anti-inflammatory terpene or vanilloid via a carbamate linkage, where the potency of the conjugate is greater than the sum of its parts.

Augmenting Moieties for Anti-Inflammatory Compounds

Augmented or synergized anti-inflammatory constructs are disclosed including anti-inflammatory terpenes and/or vanilloids covalently conjugated to one another so that the activity of the conjugate is greater than the sum of its parts. Also disclosed are methods of improving the potency of an anti-inflammatory terpene or vanilloid by linking it to another anti-inflammatory terpene or vanilloid via a carbamate linkage, where the potency of the conjugate is greater than the sum of its parts.